# Patent

## Title
Pyridopyrazine derivatives, process of manufacturing and uses thereof

## Abstract

1-ethyl-3-[3-(1-methyl-1H-pyrazol-4-yl)-pyrido[2.3-b]pyrazine-6-yl]thiourea which HAS activity to the modulation of misdirected cellular signal transduction processes such as tyrosine kinases, serine/threonine kinases and/or lipid kinases.

## Background
CROSS-REFERENCE TO RELATED APPLICATIONS
This application is a continuation application of U.S. Ser. No. 12/117,942 filed May 9, 2008, now U.S. Pat. No. 8,202,883 and claims the benefit of U.S. 60/917,129 filed May 10, 2007.


BACKGROUND OF THE INVENTION
1. Field of the Invention
The invention relates to novel pyrido[2,3-b]pyrazine derivatives, to processes of manufacturing and use thereof, in particular as medicaments for the modulation of misdirected cellular signal transduction processes, such as modulation of tyrosine kinases, serine/threonine kinases and/or lipid kinases and for the treatment or prophylaxis of malignant or benign oncoses and other disorders based on pathological cell proliferation, for example restenosis, psoriasis, arteriosclerosis and cirrhosis of the liver.
2. Description of Related Art
The activation of protein kinases is a central event in cellular signal transduction processes. Aberrant kinase activation is observed in various pathological states. Targeted inhibition of kinases is therefore a fundamental therapeutic aim.
The phosphorylation of proteins is generally initiated by extracellular signals and represents a universal mechanism for controlling various cellular events, for example metabolic processes, cell growth, cell migration, cell differentiation, membrane trans-port and apoptosis. The kinase protein family is responsible for protein phosphorylation. These enzymes catalyse transfer of phosphate to specific substrate proteins. Based on the substrate specificity, the kinases are divided into three main classes, tyrosine kinases, serine/threonine kinases and lipid kinases. Both receptor tyrosine kinases and cytoplasmic tyrosine, serine/threonine and lipid kinases are important proteins in cellular signal transduction. Overexpression or overactivation of these proteins plays an important part in disorders based on pathological cell proliferations. These include metabolic disorders, disorders of the connective tissue and of the blood vessels, and malignant and benign oncoses. In tumor initiation and development they frequently occur as oncogens, i.e. as aberrant, constitutively active kinase proteins. The consequences of this excessive kinase activation are, for example, uncontrolled cell growth and reduced cell death. Stimulation of tumor-induced growth factors may also be the cause of overstimulation of kinases. The development of kinase modulators is therefore of particular interest for all pathogenic processes influenced by kinases.
Ras-Raf-Mek-Erk and PI3K-Akt signal transduction cascades play a central role in cell growth, cell proliferation, apoptosis, adhesion, migration and glucose metabolism. Thus, the fundamental involvement in the pathogenesis of disorders such as cancer, neurodegeneration and inflammatory disorders has been demonstrated both for rasRaf-Mek-Erk and for PI3K-Akt signaling pathway. Therefore, the individual components of these signal cascades constitute important therapeutic points of attack for the intervention in the various disease processes (Weinstein-Oppenheimer C R et al., Pharmacol Ther. 2000, 88(3): 229-279, Chang F et al., Leukemia 2003, 17(3): 590-603; Chang F et al., Leukemia 2003, 17(7): 1263-1293; Katso R et al., Annu Rev Cell Dev Biol. 2001, 17: 615-675; and Lu Y et al., Rev Clin Exp Hematol. 2003, 7(2): 205-228; Hennessy B T et al., Nat Rev Drug Discov 2005, 4, 988-1004).
In the following, the molecular and biochemical properties of the two signaling pathways are first described separately.
A multitude of growth factors, cytokines and oncogens transduce their growth-promoting signals via the activation of G-protein-coupled ras, which leads to the activation of serine-threonine kinase Raf and to the activation of mitogen-activated protein kinase 1 and 2 (MAPKK1/2 or Mek1/2), and results in the phosphorylation and activation of MAPK 1 and 2—also known as extracellular signal-regulated kinase (Erk1 and 2). Compared to other signaling pathways, ras-Raf-Mek-Erk signaling pathway combines a large number of proto-oncogenes, including ligands, tyrosine kinase receptors, G proteins, kinases and nuclear transcription factors. Tyrosine-kinases, for example EGFR (Mendelsohn J et al., Oncogene. 2000, 19(56): 6550-6565) mediate, in the course of tumor process, caused by overexpression and mutation, frequently constitutively active signals to downstream ras-Raf-Mek-Erk signaling pathway. Ras is mutated in 30% of all human tumors (Khleif S N et al., J Immunother. 1999, 22(2): 155-165; Marshall C, Curr Opin Cell Biol. 1999, 11(6): 732-736) the highest incidence at 90% being in pancreas carcinomas (Friess H et al., J Mol. Med. 1996, 74(1): 35-42; Sidvatanauksorn V et al., Langenbecks Arch Surg. 1998, 383(2): 105-115). As for c-Raf, deregulated expression and/or activation have been described in various tumors (Hoshino R et al., Oncogene 1999, 18(3): 813-822; McPhillips F et al., Br J Cancer 2001, 85(11): 1753-1758). B-Raf point mutants have been detected in 66% of all human malignant melanomas, 14% of ovarian carcinomas and 12% of colon carcinomas (Davies H et al., Nature 2002, 417(6892): 949-954). It is therefore not surprising that Erk1/2 is involved at primary stage in many cellular processes, such as cell growth, cell proliferation and cell differentiation (Lewis T S et al., Adv Cancer Res. 1998, 74: 49-139; Chang F et al., Leukemia 2003, 17(3): 590-603; Chang F et al., Leukemia 2003, 17(7): 1263-1293).
In addition, members of Raf kinases also have Mek-Erk-independent, anti-apoptotic functions whose molecular steps have not yet been fully described. Possible interaction partners described for the Mek-Erk-independent Raf activity have been Ask1, Bcl-2, Akt and Bag1 (Chen J et al., Proc Natl Acad Sci USA 2001, 98(14): 7783-7788; Troppmair J et al., Biochem Pharmacol 2003, 66(8): 1341-1345; Rapp U R et al., Biochim Biophys Acta 2004, 1644(2-3): 149-158; Gotz R et al., Nat Neurosci 2005, 8(9): 1169-1178). It is now assumed that both Mek-Erk-dependent and Mek-Erk-independent signal transduction mechanisms control the activation of upstream ras and Raf stimuli.
The isoenzymes of the phosphatidylinositol 3-kinases (PI3Ks) function primarily as lipid kinases and catalyse the D3 phosphorylation of second messenger lipids PtdIns (phosphatidylinositol) to PtdIns(3)P, PtdIns(3,4)P2, PtdIns(3,4,5)P3 phosphatidylinositol phosphates. PI3Ks of class I are composed in structural terms of catalytic subunit (p110alpha, beta, gamma, delta) and of regulatory subunit (p85alpha, beta or p101gamma). In addition, class II (PI3K-C2alpha, PI3K-C2beta) and class III (Vps34p) enzymes also belong to the family of PI3 kinases (Wymann M P et al., Biochim Biophys Acta 1998, 1436(1-2): 127-150; Vanhaesebroeck B et al., Annu Rev Biochem 2001, 70: 535-602). PIP rise induced by PI3Ks activates proliferative ras-Raf-Mek-Erk signaling pathway via the coupling of ras (Rodriguez-Viciana P et al., Nature 1994, 370(6490): 527-532) and stimulates the anti-apoptotic signaling pathway by recruiting Akt to the cell membrane and consequently overactivating this kinase (Alessi D R et al., EMBO J. 1996, 15(23): 6541-6551; Chang H W et al., Science 1997, 276(5320): 1848-1850; Moore S M et al., Cancer Res 1998, 58(22): 5239-5247). Thus, activation of PI3Ks fulfils at least two crucial mechanisms of tumor development, specifically activation of cell growth and cell differentiation, and inhibition of apoptosis. In addition, PI3Ks also have protein-phosphorylating properties (Dhand R et al., EMBO J. 1994, 13(3): 522-533; Bondeva T et al., Science 1998, 282(5387): 293-296; Bondev A et al., Biol Chem 1999, 380(11): 1337-1340; Vanhaesebroeck B et al., EMBO J. 1999, 18(5): 1292-1302), which, for example, can induce serine autophosphorylation which intrinsically regulates PI3Ks. It is also known that PI3Ks have kinase-independent, regulating effector properties, for example in the control of heart contraction (Crackower M A et al., Cell 2002, 110(6): 737-749; Patrucco E et al., Cell. 2004, 118(3): 375-387). It has also been demonstrated that PI3 Kdelta and PI3 Kgamma are expressed specifically on haematopoietic cells and are thus potential points of attack for isoenzyme-specific PI3 Kdelta and PI3 Kgamma inhibitors in the treatment of inflammatory disorders, such as rheumatism, asthmas, allergies and in the treatment of B cell and T cell lymphomas (Okkenhaug K et al., Nat Rev Immunol 2003, 3(4): 317-330; Ali K et al., Nature 2004, 431(7011): 1007-1011; Sujobert P et al., Blood 2005, 106(3): 1063-1066). PI3Kalpha, which has recently been identified as a proto-oncogen (Shayesteh L et al., Nat Genet. 1999, 21(1): 99-102; Ma Y Y et al., Oncogene 2000, 19(23): 2739-2744; Samuels Y et al., Science 2004, 304(5670): 554; Campbell I G, et al., Cancer Res 2004, 64(21): 7678-7681; Levine D A et al., Clin Cancer Res 2005, 11(8): 2875-2878) is an important target in the therapy of tumor disorders. The significance of the PI3K species as a target for active pharmaceutical ingredient (API) development is therefore extremely wide (Chang F et al., Leukemia 2003, 17(3): 590-603).
Of equally great interest are PI3K-related kinases (PIKKs), which include serine/threonine kinases mTOR, ATM, ATR, h-SMG-1 and DNA-PK (Sabatini D M, Nat Rev Canc 2006, 6: 729-34; Chiang G G et al., Methods Mol Biol 2004, 281: 125-141). Their catalytic domains have a high sequence homology to the catalytic domains of PI3Ks.
Moreover, loss of tumor suppressor protein PTEN (Li J et al., Science 1997, 275(5308): 1943-1947; Steck P A et al., Nat Genet. 1997, 15(4): 356-362; Cully M et al., Nat Rev Canc 2006, 6: 184-192)—whose function is the reversal of the phosphorylation initiated by PI3K—contributes to overactivation of Akt and its downstream cascade components and hence underlines the causal significance of PI3K as a target molecule for tumor therapy.
Various inhibitors of individual components of ras-Raf-Mek-Erk and PI3K-Akt signaling pathways have already been published and patented.
The current state of development in the field of the kinase-inhibitors, particularly of ras-Raf-Mek-Erk and of PI3K-Akt pathway, is detailed in the reviews by J. S. Sebolt-Leopold et al., Nat Rev Cancer 2004, 4(12): 937-947; R. Wetzker et al., Curr Pharm Des 2004, 10(16): 1915-1922; Z. A. Knight et al., Biochem Soc Trans. 2007, 35(Pt 2):245-9; R. A. Smith et al., Curr. Top. Med. Chem. 2006, 6, 1071-89; S. Faivre et al., Nat Rev Drug Discov 2006, 5, 671-688. Said publications contain a comprehensive list of published patent applications and patents which describe the synthesis and use of low molecular weight ras-Raf-Mek-Erk and PI3K inhibitors.
European Commission has granted marketing authorization to Nexavar(R) (sorafenib, Bay 43-9006; WO 99/32111, WO 03/068223 in July 2006 for the treatment of patients with advanced renal cell carcinoma who have failed prior interferon-alpha or interleukin-2 based therapy or are considered unsuitable for such therapy. Nexavar (Bay 43-9006) exhibits a relatively unspecific inhibition pattern of serine/threonine kinases and of tyrosine kinases, such as Raf, VEGFR2/3, Flt-3, PDGFR, c-Kit and further kinases. Great significance is attributed to this inhibitor in advanced tumor disorders induced by angiogenesis (for example in the case of kidney cell carcinoma) but also in the case of melanomas with high B-Raf mutation rate. The clinical action of Bay 43-9006 is currently also being determined in patients having refractory solid tumors in combination, for example, with docetaxel. To date, mild side effects and promising anti-tumor effects have been described. Inhibition of the kinases in the PI3K-Akt signaling pathway has neither been described nor disclosed for Bay 43-9006. Recent advances in the research and development of Raf Kinase inhibitors are described in a review of R. A. Smith et al., Curr. Top. Med. Chem. 2006, 6, 1071-89.
Mek1/2 inhibitor PD0325901 (WO 02/06213) is currently in phase II clinical trials for lung cancer and phase I/II clinical trials for the treatment of other solid tumors. The precursor substance CI-1040 (WO 00/35435, WO 00/37141) was noticeable by its high Mek specificity and target affinity. However, this compound was found to be metabolically unstable in phase I/II studies. Clinical data for the current successor substance PD0325901 are still to come. However, neither interaction with Erk1 or Erk2 nor a function inhibiting the PI3K-Akt signaling pathway or their simultaneous modulation has been published or disclosed for this Mek inhibitor.
A phase II study in malignant melanoma is under way for AZD-6244 (ARRY-142886), a selective MEK inhibitor from Array BioPharmaArray.
The PI3K/mTOR inhibitor BEZ-235 from Novartis (WO 06122806) entered a phase I clinical program as a targeted anticancer agent. The compound inhibited mTOR (IC50=21 nM), p110alpha, p110alpha E542K, p110alpha H107R and p110alpha E545K (IC50=4, 5, 18 and 4 nM, respectively) and p110beta, gamma and delta (IC50=76, 5 and 7 nM, respectively), while preserving selectivity over a panel of other kinases
Recent developments at Piramed have resulted in the synthesis of two series of compounds that act as phosphatidylinositol 3-kinase of class Ib (PI3K-Ib) inhibitors and are described as possessing potent anticancer activity. Additional indications include immune disorders, cardiovascular diseases, metabolism/endocrine disorders, neurodegenerative diseases and bacterial or viral infections (WO 06046035, WO 06046040).
Semafore recently initiated a phase I trial of its lead phosphoinositide 3-kinase (PI3K) inhibitor, SF-1126 (WO 04089925), in patients with solid tumor cancers. SF-1126 is a small-molecule conjugate containing a pan-PI3K inhibitor that selectively inhibits all PI3K class IA isoforms and other key members of the PI3K superfamily, including DNA PK and mTOR. Preclinically, SF-1126 has been shown to inhibit angiogenesis and cellular proliferation, induce apoptosis, block pro-survival signals and produce synergistic antitumor effects in combination with chemotherapy.
ICOS disclosed a PI3K inhibitor IC87114 with high PI3 Kdelta isoenzyme specificity (WO 01/81346). For PI103 (WO 04/017950).
Exelixis has submitted an IND for XL-147, a novel anticancer compound. XL-147 is an orally available small-molecule inhibitor of phosphoinositide-3 kinase (PI3K). Inactivation of PI3K has been shown to inhibit growth and induce apoptosis in tumor cells. In preclinical studies, XL-147 slowed tumor growth or caused tumor shrinkage in multiple preclinical cancer models, including breast, lung, ovarian and prostate cancers, and gliomas.
Moreover, a highly noted field of research exists in the early development of PI3K inhibitors (see reviews of Z. A. Knight et al., Biochem Soc Trans. 2007, 35(Pt 2):245-9; R. Wetzker et al., Curr Pharm Des 2004, 10(16): 1915-19222004).
Inhibitors of SAPK signaling pathway, either of Jnk or of p38, are described in the literature (Gum R J et al., J Biol Chem 1998, 273(25): 15605-15610; Bennett B L et al., Proc Natl Acad Sci USA. 2001, 98(24): 13681-13686; Davies S P et al., Biochem J. 2000, 351(Pt 1): 95-105). However, no function of inhibiting the PI3Ks nor any specific inhibition of Erk1 or Erk2 or else any specific inhibition of SAPKs, Erk1, Erk2, or PI3Ks has been disclosed for these SAPK inhibitors.
6- or 7-substituted pyrido[2,3-b]pyrazine derivatives find wide use in pharmaceutical chemistry as pharmacologically active compounds and as synthetic units.
Patent applications WO 04/104002 and WO 04/104003, for example, describe pyrido[2,3-b]pyrazines which may be 6- or 7-substituted by urea, thiourea, amidine or guanidine groups. These compounds have properties as inhibitors or modulators of kinases, especially of tyrosine and serine/threonine kinases. The use as a medicament is reported. In contrast, use of these compounds as modulators of lipid kinases, alone or in combination with tyrosine and serine/threonine kinases, has not been described.
Moreover, WO 99/17759 describes pyrido[2,3-b]pyrazines which bear, in 6-position, inter alia, alkyl-, aryl- and heteroaryl-substituted carbamates. These compounds are intended to be used for the modulation of serine-threonine protein kinase function.
Patent application WO 05/007099 describes, inter alia, urea-substituted pyrido[2,3-b]pyrazines as inhibitors of serine/threonine kinase PKB. However, the document does not further define the R radical, which describes the range of possible substitutions on urea. Therefore, the range of possible substitution on urea is thus not clearly disclosed. As for these compounds, use in the treatment of cancer disorders is reported. However, no specific examples of urea-substituted pyridopyrazines having the claimed biological properties are given. In addition, the pyridopyrazines described here differ significantly in structure from the novel pyrido[2,3-b]pyrazines described in this invention.
Further examples of 6- and 7-urea-substituted pyrido[2,3-b]pyrazines are reported in WO 05/056547. However, the compounds disclosed there have additional carbonyl, sulphoxy, sulphone or imine substitution in the 2- or 3-position, which means that the compounds differ structurally significantly from the novel pyrido[2,3-b]pyrazines described in this invention. The pyridopyrazines reported in WO 05/056547 are described as inhibitors of protein kinases, especially of GSK-3, Syk and JAK-3. Uses reported include use in the treatment of proliferative disorders. Use of these compounds as modulators of lipid kinases, alone or in combination with serine/threonine kinases, is not described.
WO 04/005472 describes, inter alia, 6-carbamate-substituted pyrido[2,3-b]pyrazines which, as antibacterial substances, inhibit the growth of bacteria. Antitumor action is not described.
Certain diphenylquinoxalines and -pyrido[2,3-b]pyrazines with specific alkylpyrrolidine, alkylpiperidine or alkylsulphonamide radicals on a phenyl ring, which may additionally also bear urea or carbamate substitutions in 6- or 7-position, are described in patent applications WO 03/084473, WO 03/086394 and WO 03/086403 as inhibitors of serine/threonine kinase Akt. For these compounds, use in the treatment of cancer disorders is reported. For pyrido[2,3-b]pyrazine example compounds described there, no defined indication of biological action is specified. Moreover, there is a significant structural difference to the novel pyrido[2,3-b]pyrazines described in this invention.
Moreover, patent application WO 03/024448 describes amide- and acrylamide-substituted pyrido[2,3-b]pyrazines which also contain carbamates as additional substitutents and can be used as histone deacetylase inhibitors for the treatment of cell proliferation disorders.
A further publication (Temple, C. Jr.; J. Med. Chem. 1990: 3044-3050) exemplarily describes the synthesis of a 6-ethyl carbamate-substituted pyrido[2,3-b]pyrazine derivative. Antitumor action is neither disclosed nor rendered obvious.
The synthesis of further derivatives of 6-ethyl carbamate-substituted pyrido[2,3-b]pyrazine is described in a publication by R. D. Elliott (Elliott R D, J. Org. Chem. 1968: 2393-2397). Biological action of these compounds is neither described nor rendered obvious.
The publication by C. Temple (Temple, C. Jr., J. Med. Chem. 1968: 1216-1218) describes the synthesis and examination of 6-ethyl carbamate-substituted pyrido[2,3-b]pyrazines as potential active antimalarial ingredients. Antitumor action is neither disclosed nor rendered obvious.
WO 2005/021513 is directed to the preparation of condensed n-pyrazinyl-sulfonamides and their use in the treatment of chemokine mediated diseases. Antitumor action is neither disclosed nor rendered obvious.
JP 2006137723 describes the preparation of sulfonamides, their use as CCL17 and/or 22 regulators, and pharmaceuticals containing them for treatment of the chemokine-associated diseases. Antitumor action is neither disclosed nor rendered obvious.
Sako M. (Sako M., Houben-Weyl, Science of Synthesis 2004, 16.20: 1269-1290) gives a general overview about the synthesis of pyridopyrazines. Antitumor action is neither disclosed nor rendered obvious.
U.S. Pat. No. 4,082,845 discloses 3-(1-piperazinyl)-pyrido[2,3-b]pyrazines. Antitumor action is neither disclosed nor rendered obvious.
WO 04/005472 relates to antibacterial inhibitors of Ftsz protein. Pyridopyrazines are not explicitly mentioned. Antitumor action is neither disclosed nor rendered obvious.
WO 02/090355 describes the preparation of N-aroyl cyclic amines as orexin antagonists. Pyrido[2,3-b]pyrazines are not mentioned.
JP 50053394 discloses 3-substituted 5-alkyl-5,8-dihydro-8-oxopyrido[2,3-b]pyrazine-7-carboxylic acids and their esters. Antitumor action is neither disclosed nor rendered obvious.
U.S. Pat. No. 3,209,004 relates to 3,6-diamino-N-(2,2-dialkoxyethyl)pyrido[2,3-b]pyrazine-2-carboxamides. Antitumor action is neither disclosed nor rendered obvious.
U.S. Pat. No. 3,180,868 describes 3,6-diamino-N-(substituted)pyrido[2,3-b]pyrazine-2-carboxamides. Antitumor action is neither disclosed nor rendered obvious.
Chen J J et al. (Chen J J et al., J. Am. Chem. Soc. 1996, 118: 8953-8954) discuss the synthesis of pyrido[2,3-b]pyrazines from pyrazine C-nucleosides. Antitumor action is neither disclosed nor rendered obvious.
Nagel A et al. (Nagel A et al., J. Heterocyclic Chem. 1979, 16: 301-304) show NMR data of pyrido[2,3-b]pyrazine derivatives. Antitumor action is neither disclosed nor rendered obvious.
Tanaka T et al. (Tanaka T et al., Yakugaku Zasshi 1975, 95(9): 1092-1097) describe the synthesis of certain pyrido[2,3-b]pyrazine derivatives. Antitumor action is neither disclosed nor rendered obvious.
Osdene T S et al. (Osdene T S et al., J. Chem. Soc. 1955, pp. 2032-2035) discuss the synthesis of 3,6-diaminopyridopyrazine and derived compounds with potential anti-folic acid activity. Antitumor action is neither disclosed nor rendered obvious.
WO 2006/128172 is directed to a method for treating B cell regulated autoimmune disorders. Pyrido[2,3-b]pyrazines are not disclosed. Antitumor action is neither disclosed nor rendered obvious.
WO 2006/091395 relates to inhibitors of serine/threonine kinase Akt activity. Pyrido[2,3-b]pyrazine derivatives are comprised. However, possible pyrido[2,3-b]pyrazine derivatives are substituted with substituted phenyl and (C3-C8)cycloalkyl, aryl, heteroaryl and heterocyclyl.
WO 06/081179, WO 06/017326, WO 06/017468, WO 06/014580, WO 06/012396, WO 06/002047 and WO 06/020561 are all directed to antibacterial agents. Pyrido[2,3-b]pyrazines are not disclosed. Antitumor action is neither disclosed nor rendered obvious.
WO 2006/074147 discloses 4-arylamino-quinazolines as activatots of caspases and inducers of apoptosis. Pyrido[2,3-b]pyrazines are not disclosed. Antitumor action is neither disclosed nor rendered obvious.
WO 2006/024666 relates to the preparation of pyridine methylene thioxothiazolidinones as phosphoinositide inhibitors. Pyrido[2,3-b]pyrazine derivatives are comprised. However, the displayed pyrido[2,3-b]pyrazine derivatives are not substituted at their pyrazine moiety.
WO 06/021448 is directed to compounds with antibacterial action. Pyrido[2,3-b]pyrazines are not disclosed. Antitumor action is neither disclosed nor rendered obvious.
WO 2005/123733 describes pyrido[2,3-b]pyrazine derivatives as agents for combatting phytopathogenic fungi. However, possible pyrido[2,3-b]pyrazine derivatives are substituted with aryl, heteraryl, halogen or substituted amino at their pyridine moiety.
WO 2005/123698 describes agents for combatting phytopathogenic fungi. Pyrido[2,3-b]pyrazine derivatives are comprised. However, the comprised pyrido[2,3-b]pyrazine derivatives are substituted with aryl, heteraryl, halogen or substituted amino at their pyridine moiety.
US 2005/0272736 relates to tri- and bi-cyclic heteroaryl histamine-3 receptor ligands. Pyrido[2,3-b]pyrazines are not disclosed. Antitumor action is neither disclosed nor rendered obvious.
US 2005/0272728 discloses bicyclic amines bearing heterocyclic substituents as H3 receptor ligands. Pyrido[2,3-b]pyrazines are not disclosed. Antitumor action is neither disclosed nor rendered obvious.
US 2005/0256309 relates to tri- and bi-cyclic heteroaryl histamine-3 receptor ligands. Pyrido[2,3-b]pyrazines are not disclosed. Antitumor action is neither disclosed nor rendered obvious.
US 2005/0256118 discloses bicyclic amines bearing heterocyclic substituents as H3 receptor ligands. Pyrido[2,3-b]pyrazines are not disclosed. Antitumor action is neither disclosed nor rendered obvious.
US 2005/0165028 is directed to N-heteroaryl substituted benzamides as vanilloid receptor ligands. Pyrido[2,3-b]pyrazines are not disclosed. Antitumor action is neither disclosed nor rendered obvious.
WO 05/023807 describes bicyclic quinazolin-4-ylamine derivatives as capsaicin receptor modulators. Pyrido[2,3-b]pyrazines are not disclosed. Antitumor action is neither disclosed nor rendered obvious.
EP 1 661 889, which corresponds to WO 2005/07099, relates to pyridinyl benzene-sulfonylamide derivatives as chemokine receptor antagonist. Pyrido[2,3-b]pyrazine derivatives are comprised. However, the comprised pyrido[2,3-b]pyrazine derivatives are concomitantly substituted with sulfonamides and cyclic structures.
WO 04/055003 discloses quinazolin-4-yl)amines as capsaicin receptor modulators. Pyrido[2,3-b]pyrazines are not disclosed. Antitumor action is neither disclosed nor rendered obvious.
US 2004/0092521 discloses bicyclic amines bearing heterocyclic substituents as H3 receptor ligands. Pyrido[2,3-b]pyrazines are not disclosed. Antitumor action is neither disclosed nor rendered obvious.
WO 2004/030635 is directed to vasculostatic agents. Pyrido[2,3-b]pyrazine derivatives are comprised. However, the comprised pyrido[2,3-b]pyrazine derivatives are substituted with aryl or heteraryl at their pyrazine moiety.
WO 03/064421 describes aminopiperidine derivatives as antibacterial agents. Pyrido[2,3-b]pyrazines are not disclosed. Antitumor action is neither disclosed nor rendered obvious.
WO 03/064431 also describes aminopiperidine derivatives as antibacterial agents. Pyrido[2,3-b]pyrazines are not disclosed. Antitumor action is neither disclosed nor rendered obvious.
WO 02/055079 relates to 8-hydroxy-1,6-naphthyridine-7-carboxamides as inhibitors of HIV integrase and HIV replication. Pyrido[2,3-b]pyrazines are not disclosed. Antitumor action is neither disclosed nor rendered obvious.
WO 00/12497 discloses quinazoline derivatives as TGF-beta and p38-alpha kinase inhibitors. However, pyrido[2,3-b]pyrazines are not disclosed.
WO 99/43681 is directed to N-(4-piperidinylmethyl)thieno[3,2-b]pyridin-7-amines and related compounds as GABA brain receptor ligands. Pyrido[2,3-b]pyrazines are not disclosed. Antitumor action is neither disclosed nor rendered obvious.
WO 95/15758 describes aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase. Pyrido[2,3-b]pyrazines are not disclosed.
U.S. Pat. No. 5,480,883 describes bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase. Pyrido[2,3-b]pyrazine derivatives are comprised. However, the comprised pyrido[2,3-b]pyrazine derivatives are directly substituted with aryl or heteraryl at their pyrazine moiety.
WO 2006/059103 relates to substituted pyridines and derivatives thereof. Pyrido[2,3-b]pyrazines are not disclosed.
WO 2007/023186 discloses pyrazine derivatives and their use as PI3K inhibitors. Pyrido[2,3-b]pyrazine derivatives are comprised. However, the comprised pyrido[2,3-b]pyrazine derivatives are directly substituted with sulfonamides at their pyrazine moiety.
WO 2007/044729 also describes pyrazine derivatives and their use as PI3K inhibitors. Pyrido[2,3-b]pyrazine derivatives are comprised. However, the comprised pyrido[2,3-b]pyrazine derivatives are directly substituted with sulfonamides at their pyrazine moiety.
WO 2004/108702 is directed to indole derivatives. Pyrido[2,3-b]pyrazine derivatives are comprised. However, the comprised pyrido[2,3-b]pyrazine derivatives are directly substituted with glyoxyl-indolyl at their pyrimidine moiety.


DESCRIPTION OF THE INVENTION
The present invention has the object to provide novel pyrido[2,3-b]pyrazine derivatives that act as kinase modulators.
The object of the present invention has surprisingly been solved in one aspect by providing pyrido[2,3-b]pyrazine derivatives according to general formula (Ia)




wherein:

one of radicals R3, R4 independently is selected, or both of radicals R3, R4 independently from each other are selected from the group consisting of:

    (1) “—NR6R7”;

wherein radicals R6, R7 are independently from each other selected from the group consisting of:

(a) “hydrogen, alkyl, arylalkyl, heteroarylalkyl”;
    
        with the first proviso that radicals R6, R7 are not both hydrogen, alkyl, arylalkyl or heteroarylalkyl at the same time;
        with the second proviso that, if one of radicals R6, R7 independently is “hydrogen”, radical R5 is not selected from the group consisting of: “—NH-cycloalkyl, —NH-heterocyclyl, —NH-aryl, —NH-heteroaryl, halogen, —F, —Cl, —Br, —I, —NRaRb”, with Ra, Rb being independently selected from the group consisting of: “H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —NRcRd”, Rc, Rd in turn being independently selected from the group consisting of: “H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl”;

(b) “—C(Y1)NR8R9, —C(Y1b)OR9b, —C(═NR10)-R11, —C(Y2)NR12-Y3-R13”;

        wherein Y1, Y1b, Y2 are independently from each other selected from the group consisting of: “═O, ═S, ═NH, ═NR14”;
        wherein Y3 is independently selected from the group consisting of: “O, S”;
        wherein radicals R8, R9, R9b, R10, R11, R12, R13, R14 are independently from each other selected from the group consisting of:
        (I) “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHX1, —NX2X3, —NO2, —OH, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, SO3H, —P(O)(OH)2, —C(O)—X4, —C(O)O—X5, —C(O)NH—X6, —C(O)NX7X8, —O—X9, —O(—X10-O)a—H (a=1, 2, 3, 4, 5), —O(—X11-O)b—X12 (b=1, 2, 3, 4, 5), —OC(O)—X13, —OC(O)—O—X14, —OC(O)—NHX15, —O—C(O)—NX16X17, —OP(O)(OX18)(OX19), —OSi(X20)(X21)(X22), —OS(O2)—X23, —NHC(O)—NH2, —NHC(O)—X24, —NX25C(O)—X26, —NH—C(O)—O—X27, —NH—C(O)—NH—X28, —NH—C(O)—NX29X30, —NX31-C(O)—O—X32, —NX33-C(O)—NH—X34, —NX35-C(O)—NX36X37, —NHS(O2)—X38, —NX39S(O2)—X40, —S—X41, —S(O)—X42, —S(O2)—X43, —S(O2)NH—X44, —S(O2)NX45X46, —S(O2)O—X47, —P(O)(OX48)(OX49), —Si(X50)(X51)(X52), —C(NH)—NH2, —C(NX53)-NH2, —C(NH)—NHX54, —C(NH)—NX55X56, —C(NX57)-NHX58, —C(NX59)-NX60X61, —NH—C(O)—NH—O—X62, —NH—C(O)—NX63-O—X64, —NX65-C(O)—NX66-O—X67, —N(—C(O)—NH—O—X68)2, —N(—C(O)—NX69-O—X70)2, —N(—C(O)—NH—O—X71)(—C(O)—NX72-O—X73), —C(S)—X74, —C(S)—O—X75, —C(S)—NH—X76, —C(S)—NX77X78, —C(O)—NH—O—X79, —C(O)—NX80-O—X81, —C(S)—NH—O—X82, —C(S)—NX83-O—X84, —C(O)—NH—NH—X85, —C(O)—NH—NX86X87, —C(O)—NX88-NX89X90, —C(S)—NH—NH—X91, —C(S)—NH—NX92X93, —C(S)—NX94-NX95X96, —C(O)—C(O)—O—X97, —C(O)—C(O)—NH2, —C(O)—C(O)—NHX98, —C(O)—C(O)—NX99X100, —C(S)—C(O)—O—X101, —C(O)—C(S)—O—X102, —C(S)—C(S)—O—X103, —C(S)—C(O)—NH2, —C(S)—C(O)—NHX104, —C(S)—C(O)—NX105X106, —C(S)—C(S)—NH2, —C(S)—C(S)—NHX107, —C(S)—C(S)—NX108X109, —C(O)—C(S)—NH2, —C(O)—C(S)—NHX110, —C(O)—C(S)—NX111X112”;
        
            wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12, X13, X14, X15, X16, X17, X18, X19, X20, X21, X22, X23, X24, X25, X26, X27, X28, X29, X30, X31, X32, X33, X34, X35, X36, X37, X38, X39, X40, X41, X42, X43, X44, X45, X46, X47, X48, X49, X50, X51, X52, X53, X54, X55, X56, X57, X58, X59, X60, X61, X62, X63, X64, X65, X66, X67, X68, X69, X70, X71, X72, X73, X74, X75, X76, X77, X78, X79, X80, X81, X82, X83, X84, X85, X86, X87, X88, X89, X90, X91, X92, X93, X94, X95, X96, X97, X98, X99, X100, X101, X102, X103, X104, X105, X106, X107, X108, X109, X110, X111, X112 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively X7, X8 and/or X16, X17 and/or X29, X30 and/or X36, X37 and/or X45, X46 and/or X55, X56 and/or X60, X61 and/or X77, X78 and/or X86, X87 and/or X89, X90 and/or X92, X93 and/or X95, X96 and/or X99, X100 and/or X105, X106 and/or X108, X109 and/or X111, X112 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (I)—if not hydrogen—can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (i) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHX201, —NX202X203, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—X204, —C(O)O—X205, —C(O)NH—X206, —C(O)NX207X208, —O—X209, —O(—X210-O)c—H (c=1, 2, 3, 4, 5), —O(—X211-O)d—X212 (d=1, 2, 3, 4, 5), —OC(O)—X213, —OC(O)—O—X214, —OC(O)—NHX215, —O—C(O)—NX216X217, —OP(O)(OX218)(OX219), —OSi(X220)(X221)(X222), —OS(O2)—X223, —NHC(O)—NH2, —NHC(O)—X224, —NX225C(O)—X226, —NH—C(O)—O—X227, —NH—C(O)—NH—X228, —NH—C(O)—NX229X230, —NX231-C(O)—O—X232, —NX233-C(O)—NH—X234, —NX235-C(O)—NX236X237, —NHS(O2)—X238, —NX239S(O2)—X240, —S—X241, —S(O)—X242, —S(O2)—X243, —S(O2)NH—X244, —S(O2)NX245X246, —S(O2)O—X247, —P(O)(OX248)(OX249), —Si(X250)(X251)(X252), —C(NH)—NH2, —C(NX253)-NH2, —C(NH)—NHX254, —C(NH)—NX255X256, —C(NX257)-NHX258, —C(NX259)-NX260X261, —NH—C(O)—NH—O—X262, —NH—C(O)—NX263-O—X264, —NX265-C(O)—NX266-O—X267, —N(—C(O)—NH—O—X268)2, —N(—C(O)—NX269-O—X270)2, —N(—C(O)—NH—O—X271)(—C(O)—NX272-O—X273), —C(S)—X274, —C(S)—O—X275, —C(S)—NH—X276, —C(S)—NX277X278, —C(O)—NH—O—X279, —C(O)—NX280-O—X281, —C(S)—NH—O—X282, —C(S)—NX283-O—X284, —C(O)—NH—NH—X285, —C(O)—NH—NX286X287, —C(O)—NX288-NX289X290, —C(S)—NH—NH—X291, —C(S)—NH—NX292X293, —C(S—NX294-NX295X296, —C(O)—C(O)—O—X297, —C(O)—C(O)—NH2, —C(O)—C(O)—NHX298, —C(O)—C(O)—NX299X300, —C(S)—C(O)—O—X301, —C(O)—C(S)—O—X302, —C(S)—C(S)—O—X303, —C(S)—C(O)—NH2, —C(S)—C(O)—NHX304, —C(S)—C(O)—NX305X306, —C(S)—C(S)—NH2, —C(S)—C(S)—NHX307, —C(S)—C(S)—NX308X309, —C(O)—C(S)—NH2, —C(O)—C(S)—NHX310, —C(O)—C(S)—NX311X312”;
        
            wherein X201, X202, X203, X204, X205, X206, X207, X208, X209, X210, X211, X212, X213, X214, X215, X216, X217, X218, X219, X220, X221, X222, X223, X224, X225, X226, X227, X228, X229, X230, X231, X232, X233, X234, X235, X236, X237, X238, X239, X240, X241, X242, X243, X244, X245, X246, X247, X248, X249, X250, X251, X252, X253, X254, X255, X256, X257, X258, X259, X260, X261, X262, X263, X264, X265, X266, X267, X268, X269, X270, X271, X272, X273, X274, X275, X276, X277, X278, X279, X280, X281, X282, X283, X284, X285, X286, X287, X288, X289, X290, X291, X292, X293, X294, X295, X296, X297, X298, X299, X300, X301, X302, X303, X304, X305, X306, X307, X308, X309, X310, X311, X312 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively X207, X208 and/or X216, X217 and/or X229, X230 and/or X236, X237 and/or X245, X246 and/or X255, X256 and/or X260, X261 and/or X277, X278 and/or X286, X287 and/or X289, X290 and/or X292, X293 and/or X295, X296 and/or X299, X300 and/or X305, X306 and/or X308, X309 and/or X311, X312 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (i) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (ii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHX401, —NX402X403, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—X404, —C(O)O—X405, —C(O)NH—X406, —C(O)NX407X408, —O—X409, —O(—X410-O)e—H (e=1, 2, 3, 4, 5), —O(—X411-O)f—X412 (f=1, 2, 3, 4, 5), —OC(O)—X413, —OC(O)—O—X414, —OC(O)—NHX415, —O—C(O)—NX416X417, —OP(O)(OX418)(OX419), —OSi(X420)(X421)(X422), —OS(O2)—X423, —NHC(O)—NH2, —NHC(O)—X424, —NX425C(O)—X426, —NH—C(O)—O—X427, —NH—C(O)—NH—X428, —NH—C(O)—NX429X430, —NX431-C(O)—O—X432, —NX433-C(O)—NH—X434, —NX435-C(O)—NX436X437, —NHS(O2)—X438, —NX439S(O2)—X440, —S—X441, —S(O)—X442, —S(O2)—X443, —S(O2)NH—X444, —S(O2)NX445X446, —S(O2)O—X447, —P(O)(OX448)(OX449), —Si(X450)(X451)(X452), —C(NH)—NH2, —C(NX453)-NH2, —C(NH)—NHX454, —C(NH)—NX455X456, —C(NX457)-NHX458, —C(NX459)-NX460X461, —NH—C(O)—NH—O—X462, —NH—C(O)—NX463-O—X464, —NX465-C(O)—NX466-O—X467, —N(—C(O)—NH—O—X468)2, —N(—C(O)—NX469-O—X470)2, —N(—C(O)—NH—O—X471) (—C(O)—NX472-O—X473), —C(S)—X474, —C(S)—O—X475, —C(S)—NH—X476, —C(S)—NX477X478, —C(O)—NH—O—X479, —C(O)—NX480-O—X481, —C(S)—NH—O—X482, —C(S)—NX483-O—X484, —C(O)—NH—NH—X485, —C(O)—NH—NX486X487, —C(O)—NX488-NX489X490, —C(S)—NH—NH—X491, —C(S)—NH—NX492X493, —C(S)—NX494-NX495X496, —C(O)—C(O)—O—X497, —C(O)—C(O)—NH2, —C(O)—C(O)—NHX498, —C(O)—C(O)—NX499X500, —C(S)—C(O)—O—X501, —C(O)—C(S)—O—X502, —C(S)—C(S)—O—X503, —C(S)—C(O)—NH2, —C(S)—C(O)—NHX504, —C(S)—C(O)—NX505X506, —C(S)—C(S)—NH2, —C(S)—C(S)—NHX507, —C(S)—C(S)—NX508X509, —C(O)—C(S)—NH2, —C(O)—C(S)—NHX510, —C(O)—C(S)—NX511X512”;
        
            wherein X401, X402, X403, X404, X405, X406, X407, X408, X409, X410, X411, X412, X413, X414, X415, X416, X417, X418, X419, X420, X421, X422, X423, X424, X425, X426, X427, X428, X429, X430, X431, X432, X433, X434, X435, X436, X437, X438, X439, X440, X441, X442, X443, X444, X445, X446, X447, X448, X449, X450, X451, X452, X453, X454, X455, X456, X457, X458, X459, X460, X461, X462, X463, X464, X465, X466, X467, X468, X469, X470, X471, X472, X473, X474, X475, X476, X477, X478, X479, X480, X481, X482, X483, X484, X485, X486, X487, X488, X489, X490, X491, X492, X493, X494, X495, X496, X497, X498, X499, X500, X501, X502, X503, X504, X505, X506, X507, X508, X509, X510, X511, X512 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively X407, X408 and/or X416, X417 and/or X429, X430 and/or X436, X437 and/or X445, X446 and/or X455, X456 and/or X460, X461 and/or X477, X478 and/or X486, X487 and/or X489, X490 and/or X492, X493 and/or X495, X496 and/or X499, X500 and/or X505, X506 and/or X508, X509 and/or X511, X512 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (ii) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (iii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHX601, —NX602X603, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—X604, —C(O)O—X605, —C(O)NH—X606, —C(O)NX607X608, —O—X609, —O(—X610-O)e—H (e=1, 2, 3, 4, 5), —O(—X611-O)f—X612 (f=1, 2, 3, 4, 5), —OC(O)—X613, —OC(O)—O—X614, —OC(O)—NHX615, —O—C(O)—NX616X617, —OP(O)(OX618)(OX619), —OSi(X620)(X621)(X622), —OS(O2)—X623, —NHC(O)—NH2, —NHC(O)—X624, —NX625C(O)—X626, —NH—C(O)—O—X627, —NH—C(O)—NH—X628, —NH—C(O)—NX629X630, —NX631-C(O)—O—X632, —NX633-C(O)—NH—X634, —NX635-C(O)—NX636X637, —NHS(O2)—X638, —NX639S(O2)—X640, —S—X641, —S(O)—X642, —S(O2)—X643, —S(O2)NH—X644, —S(O2)NX645X646, —S(O2)O—X647, —P(O)(OX648)(OX649), —Si(X650)(X651)(X652), —C(NH)—NH2, —C(NX653)-NH2, —C(NH)—NHX654, —C(NH)—NX655X656, —C(NX657)-NHX658, —C(NX659)-NX660X661, —NH—C(O)—NH—O—X662, —NH—C(O)—NX663-O—X664, —NX665-C(O)—NX666-O—X667, —N(—C(O)—NH—O—X668)2, —N(—C(O)—NX669-O—X670)2, —N(—O(O)—NH—O—X671)(—C(O)—NX672-O—X673), —C(S)—X674, —C(S)—O—X675, —C(S)—NH—X676, —C(S)—NX677X678, —C(O)—NH—O—X679, —C(O)—NX680-O—X681, —C(S)—NH—O—X682, —C(S)—NX683-O—X684, —C(O)—NH—NH—X685, —C(O)—NH—NX686X687, —C(O)—NX688-NX689X690, —C(S)—NH—NH—X691, —C(S)—NH—NX692X693, —C(S)—NX694-NX695X696, —C(O)—C(O)—O—X697, —C(O)—C(O)—NH2, —C(O)—C(O)—NHX698, —C(O)—C(O)—NX699X700, —C(S)—C(O)—O—X701, —C(O)—C(S)—O—X702, —C(S)—C(S)—O—X703, —C(S)—C(O)—NH2, —C(S)—C(O)—NHX704, —C(S)—C(O)—NX705X706, —C(S)—C(S)—NH2, —C(S)—C(S)—NHX707, —C(S)—C(S)—C(S)—NX711X712”;
        
            wherein X601, X602, X603, X604, X605, X606, X607, X608, X609, X610, X611, X612, X613, X614, X615, X616, X617, X618, X619, X620, X621, X622, X623, X624, X625, X626, X627, X628, X629, X630, X631, X632, X633, X634, X635, X636, X637, X638, X639, X640, X641, X642, X643, X644, X645, X646, X647, X648, X649, X650, X651, X652, X653, X654, X655, X656, X657, X658, X659, X660, X661, X662, X663, X664, X665, X666, X667, X668, X669, X670, X671, X672, X673, X674, X675, X676, X677, X678, X679, X680, X681, X682, X683, X684, X685, X686, X687, X688, X689, X690, X691, X692, X693, X694, X695, X696, X697, X698, X699, X700, X701, X702, X703, X704, X705, X706, X707, X708, X709, X710, X711, X712 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively X607, X608 and/or X616, X617 and/or X629, X630 and/or X636, X637 and/or X645, X646 and/or X655, X656 and/or X660, X661 and/or X677, X678 and/or X686, X687 and/or X689, X690 and/or X692, X693 and/or X695, X696 and/or X699, X700 and/or X705, X706 and/or X708, X709 and/or X711, X712 and/or respectively together can also form “heterocyclyl”;
        
        
        with the first proviso that if “—C(Y1)-NR8R9” is selected from the group consisting of: “—C(O)—NRaRb”, with Ra, Rb independently from each other being selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl” or with Ra, Rb forming together “heterocyclyl”, one of radicals R1, R2 is not “hydrogen” and the other one of radicals R1, R2 is not “—NRcRd with Rc, Rd independently from each other being selected from the group consisting of: “hydrogen, alkyl, (C9-C30alkyl), cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —C(Ya1)NXa16Xa17, —C(═NXa18)-Xa19, —C(Ya2)NXa20-Ya3-Xa21”; with the proviso that Rc, Rd are not “hydrogen” or “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” at the same time, with the further proviso that if one of radicals Rc, Rd is “hydrogen” or “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl”, the other radical Rc, Rd is “—C(Ya1)NXa16Xa17”, “—C(═NXa18)-Xa19” oder “—C(Ya2)NXa20-Ya3-Xa21”, where Ya1, Ya2, Ya3 are independently from each other selected from the group consisting of “O, S, ═NH, ═NXa22”; where Xa16, Xa17, Xa18, Xa19, Xa20, Z21, Z22 are independently from each other selected from the group consisting of: hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl”;
        with the second proviso that if at least one of radicals R1, R2 is “—NXa26Xa27” with at least one of radicals Xa26, Xa27 being “—C(O)—NReRf where at least one of radicals Re, Rf is selected from the group consisting of: “alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, C(O)-alkyl, C(O)-aryl, C(O)-heteroaryl, (C9-C30)alkyl, cycloalkylalkyl, heterocyclylalkyl, arylalkyl, heteroarylalkyl, —C(O)—(C9-C30)alkyl, —C(O)-cycloalkyl, —C(O)-cycloalkylalkyl, —C(O)-arylalkyl, —C(O)heteroarylalkyl, —C(O)-heterocyclyl, —C(O)-heterocyclylalkyl, —S(O2)-alkyl, —S(O2)—(C9-C30)alkyl, —S(O2)-cycloalkyl, —S(O2)-cycloalkylalkyl, —S(O2)-aryl, —S(O2)-arylalkyl, —S(O2)-heteroaryl, —S(O2)-heteroarylalkyl, —S(O2)— heterocyclyl, —S(O2)-heterocyclylalkyl”, radicals R3, R4 are not “—C(O)—NXa1135Xa1136 with Xa1135, Xa1136 independently being selected from the group consisting of: hydrogen, alkyl, (C9-C30alkyl), cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” or with Xa1135, Xa1136 forming together “heterocyclyl”;
        with the third proviso that, if “—C(Y1)-NR8R9” independently is selected from the group consisting of: “—C(O)—N[C(O)—O-alkyl]2, —C(O)—N[C(O)-alkyl]2, —C(O)—N[S(O2)-alkyl]2, —C(O)—N[S(O2)-cycloalkyl]2, —C(O)—N[S(O2)—cycloalkylalkyl]2, —C(O)—N[S(O2)-aryl]2, —C(O)—N[S(O2)-heterocyclyl]2”, radicals R1, R2 independently from each other are not “phenyl”;
        with the fourth proviso that, if “—C(Y2)-NR12-Y3-R13” independently is selected from the group consisting of: “—C(O)—N[O-alkyl]2”, radicals R1, R2 independently from each other are not “phenyl”;

(c) “—C(O)—C(O)—R16”;

        wherein radical R16 is independently selected from the group consisting of:
        (II) “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHZ1, —NZ2Z3, —NO2, —OH, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—Z4, —C(O)O—Z5, —C(O)NH—Z6, —C(O)NZ7Z8, —O—Z9, —O(—Z10-O)a—H (a=1, 2, 3, 4, 5), —O(—Z11-O)b—Z12 (b=1, 2, 3, 4, 5), —OC(O)—Z13, —OC(O)—O—Z14, —OC(O)—NHZ15, —O—C(O)—NZ16Z17, —OP(O)(OZ18)(OZ19), —OSi(Z20)(Z21)(Z22), —OS(O2)—Z23, —NHC(O)—NH2, —NHC(O)—Z24, —NZ25C(O)—Z26, —NH—C(O)—O—Z27, —NH—C(O)—NH—Z28, —NH—C(O)—NZ29Z30, —NZ31-C(O)—O—Z32, —NZ33-C(O)—NH—Z34, —NZ35-C(O)—NZ36Z37, —NHS(O2)—Z38, —NZ39S(O2)—Z40, —S—Z41, —S(O)—Z42, —S(O2)—Z43, —S(O2)NH—Z44, —S(O2)NZ45Z46, —S(O2)O—Z47, —P(O)(OZ48)(OZ49), —Si(Z50)(Z51)(Z52), —C(NH)—NH2, —C(NZ53)-NH2, —C(NH)—NHZ54, —C(NH)—NZ55Z56, —C(NZ57)-NHZ58, —C(NZ59)-NZ60Z61, —NH—C(O)—NH—O—Z62, —NH—C(O)—NZ63-O—Z64, —NZ65-C(O)—NZ66-O—Z67, —N(—C(O)—NH—O—Z68)2, —N(—C(O)—NZ69-O—Z70)2, —N(—C(O)—NH—O—Z71)(—C(O)—NZ72-O—Z73), —C(S)—Z74, —C(S)—O—Z75, —C(S)—NH—Z76, —C(S)—NZ77Z78, —C(O)—NH—O—Z79, —C(O)—NZ80-O—Z81, —C(S)—NH—O—Z82, —C(S)—NZ83-O—Z84, —C(O)—NH—NH—Z85, —C(O)—NH—NZ86Z87, —C(O)—NZ88-NZ89Z90, —C(S)—NH—NH—Z91, —C(S)—NH—NZ92Z93, —C(S)—NZ94-NZ95Z96, —C(O)—C(O)—O—Z97, —C(O)—C(O)—NH2, —C(O)—C(O)—NHZ98, —C(O)—C(O)—NZ99Z100, —C(S)—C(O)—O—Z101, —C(O)—C(S)—O—Z102, —C(S)—C(S)—O—Z103, —C(S)—C(O)—NH2, —C(S)—C(O)—NHZ104, —C(S)—C(O)—NZ105Z106, —C(S)—C(S)—NH2, —C(S)—C(S)—NHZ107, —C(S)—C(S)—NZ108Z109, —C(O)—C(S)—NH2, —C(O)—C(S)—NHZ110, —C(O)—C(S)—NZ111Z112”;
        
            wherein Z1, Z2, Z3, Z4, Z5, Z6, Z7, Z8, Z9, Z10, Z11, Z12, Z13, Z14, Z15, Z16, Z17, Z18, Z19, Z20, Z21, Z22, Z23, Z24, Z25, Z26, Z27, Z28, Z29, Z30, Z31, Z32, Z33, Z34, Z35, Z36, Z37, Z38, Z39, Z40, Z41, Z42, Z43, Z44, Z45, Z46, Z47, Z48, Z49, Z50, Z51, Z52, Z53, Z54, Z55, Z56, Z57, Z58, Z59, Z60, Z61, Z62, Z63, Z64, Z65, Z66, Z67, Z68, Z69, Z70, Z71, Z72, Z73, Z74, Z75, Z76, Z77, Z78, Z79, Z80, Z81, Z82, Z83, Z84, Z85, Z86, Z87, Z88, Z89, Z90, Z91, Z92, Z93, Z94, Z95, Z96, Z97, Z98, Z99, Z100, Z101, Z102, Z103, Z104, Z105, Z106, Z107, Z108, Z109, Z110, Z111, Z112 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively Z7, Z8 and/or Z16, Z17 and/or Z29, Z30 and/or Z36, Z37 and/or Z45, Z46 and/or Z55, Z56 and/or Z60, Z61 and/or Z77, Z78 and/or Z86, Z87 and/or Z89, Z90 and/or Z92, Z93 and/or Z95, Z96 and/or Z99, Z100 and/or Z105, Z106 and/or Z108, Z109 and/or Z111, Z112 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (II)—if not hydrogen—can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (i) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHZ201, —NZ202Z203, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—Z204, —C(O)O—Z205, —C(O)NH—Z206, —C(O)NZ207Z208, —O—Z209, —O(—Z210-O)c—H (c=1, 2, 3, 4, 5), —O(—Z211-O)d—Z212 (d=1, 2, 3, 4, 5), —OC(O)—Z213, —OC(O)—O—Z214, —OC(O)—NHZ215, —O—C(O)—NZ216Z217, —OP(O)(OZ218)(OZ219), —OSi(Z220)(Z221)(Z222), —OS(O2)—Z223, —NHC(O)—NH2, —NHC(O)—Z224, —NZ225C(O)—Z226, —NH—C(O)—O—Z227, —NH—C(O)—NH—Z228, —NH—C(O)—NZ229Z230, —NZ231-C(O)—O—Z232, —NZ233-C(O)—NH—Z234, —NZ235-C(O)—NZ236Z237, —NHS(O2)—Z238, —NZ239S(O2)— Z240, —S—Z241, —S(O)—Z242, —S(O2)—Z243, —S(O2)NH—Z244, —S(O2)NZ245Z246, —S(O2)O—Z247, —P(O)(OZ248)(OZ249), —Si(Z250)(Z251)(Z252), —C(NH)—NH2, —C(NZ253)-NH2, —C(NH)—NHZ254, —C(NH)—NZ255Z256, —C(NZ257)-NHZ258, —C(NZ259)-NZ260Z261, —NH—C(O)—NH—O—Z262, —NH—C(O)—NZ263-O—Z264, —NZ265-C(O)—NZ266-O—Z267, —N(—C(O)—NH—O—Z268)2, —N(—C(O)—NZ269-O—Z270)2, —N(—C(O)—NH—O—Z271)(—C(O)—NZ272-O—Z273), —C(S)—Z274, —C(S)—O—Z275, —C(S)—NH—Z276, —C(S)—NZ277Z278, —C(O)—NH—O—Z279, —C(O)—NZ280-O—Z281, —C(S)—NH—O—Z282, —C(S)—NZ283-O—Z284, —C(O)—NH—NH—Z285, —C(O)—NH—NZ286Z287, —C(O)—NZ288-NZ289Z290, —C(S)—NH—NH—Z291, —C(S)—NH—NZ292Z293, —C(S)—NZ294-NZ295Z296, —C(O)—C(O)—O—Z297, —C(O)—C(O)—NH2, —C(O)—C(O)—NHZ298, —C(O)—C(O)—NZ299Z300, —C(S)—C(O)—O—Z301, —C(O)—C(S)—O—Z302, —C(S)—C(S)—O—Z303, —C(S)—C(O)—NH2, —C(S)—C(O)—NHZ304, —C(S)—C(O)—NZ305Z306, —C(S)—C(S)—NH2, —C(S)—C(S)—NHZ307, —C(S)—C(S)—NZ308Z309, —C(O)—C(S)—NH2, —C(O)—C(S)—NHZ310, —C(O)—C(S)—NZ311Z312”;
        
            wherein Z201, Z202, Z203, Z204, Z205, Z206, Z207, Z208, Z209, Z210, Z211, Z212, Z213, Z214, Z215, Z216, Z217, Z218, Z219, Z220, Z221, Z222, Z223, Z224, Z225, Z226, Z227, Z228, Z229, Z230, Z231, Z232, Z233, Z234, Z235, Z236, Z237, Z238, Z239, Z240, Z241, Z242, Z243, Z244, Z245, Z246, Z247, Z248, Z249, Z250, Z251, Z252, Z253, Z254, Z255, Z256, Z257, Z258, Z259, Z260, Z261, Z262, Z263, Z264, Z265, Z266, Z267, Z268, Z269, Z270, Z271, Z272, Z273, Z274, Z275, Z276, Z277, Z278, Z279, Z280, Z281, Z282, Z283, Z284, Z285, Z286, Z287, Z288, Z289, Z290, Z291, Z292, Z293, Z294, Z295, Z296, Z297, Z298, Z299, Z300, Z301, Z302, Z303, Z304, Z305, Z306, Z307, Z308, Z309, Z310, Z311, Z312 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively Z207, Z208 and/or Z216, Z217 and/or Z229, Z230 and/or Z236, Z237 and/or Z245, Z246 and/or Z255, Z256 and/or Z260, Z261 and/or Z277, Z278 and/or Z286, Z287 and/or Z289, Z290 and/or Z292, Z293 and/or Z295, Z296 and/or Z299, Z300 and/or Z305, Z306 and/or Z308, Z309 and/or Z311, Z312 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (i) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (ii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHZ401, —NZ402Z403, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—Z404, —C(O)O—Z405, —C(O)NH—Z406, —C(O)NZ407Z408, —O—Z409, —O(—Z410-O)e—H (e=1, 2, 3, 4, 5), —O(—Z411-O)f—Z412 (f=1, 2, 3, 4, 5), —OC(O)—Z413, —OC(O)—O—Z414, —OC(O)—NHZ415, —O—C(O)—NZ416Z417, —OP(O)(OZ418)(OZ419), —OSi(Z420)(Z421)(Z422), —OS(O2)—Z423, —NHC(O)—NH2, —NHC(O)—Z424, —NZ425C(O)—Z426, —NH—C(O)—OZ427, —NH—C(O)—NH—Z428, —NH—C(O)—NZ429Z430, —NZ431-C(O)—O—Z432, —NZ433-C(O)—NH—Z434, —NZ435-C(O)—NZ436Z437, —NHS(O2)—Z438, —NZ439S(O2)—Z440, —S—Z441, —S(O)—Z442, —S(O2)—Z443, —S(O2)NH—Z444, —S(O2)NZ445Z446, —S(O2)O—Z447, —P(O)(OZ448)(OZ449), —Si(Z450)(Z451)(Z452), —C(NH)—NH2, —C(NZ453)-NH2, —C(NH)—NHZ454, —C(NH)—NZ455Z456, —C(NZ457)-NHZ458, —C(NZ459)-NZ460Z461, —NH—C(O)—NH—O—Z462, —NH—C(O)—NZ463-O—Z464, —NZ465-C(O)—NZ466-O—Z467, —N(—C(O)—NH—O—Z468)2, —N(—C(O)—NZ469-OZ470)2, —N(—C(O)—NH—O—Z471)(—C(O)—NZ472-O—Z473), —C(S)Z474, —C(S)—O—Z475, —C(S)—NH—Z476, —C(S)—NZ477Z478, —C(O)—NH—O—Z479, —C(O)—NZ480-O—Z481, —C(S)—NH—O—Z482, —C(S)—NZ483-O—Z484, —C(O)—NH—NH—Z485, —C(O)—NH—NZ486Z487, —C(O)—NZ488-NZ489Z490, —C(S)—NH—NH—Z491, —C(S)—NHNZ492Z493, —C(S)—NZ494-NZ495Z496, —C(O)—C(O)—O—Z497, —C(O)—C(O)—NH2, —C(O)—C(O)—NHZ498, —C(O)—C(O)—NZ499Z500, —C(S)—C(O)—O—Z501, —C(O)—C(S)—O—Z502, —C(S)—C(S)—O—Z503, —C(S)—C(O)—NH2, —C(S)—C(O)—NHZ504, —C(S)—C(O)—NZ505Z506, —C(S)—C(S)—NH2, —C(S)—C(S)—NHZ507, —C(S)—C(S)—NZ508Z509, —C(O)—C(S)—NH2, —C(O)—C(S)—NHZ510, —C(O)—C(S)—NZ511Z512”;
        
            wherein Z401, Z402, Z403, Z404, Z405, Z406, Z407, Z408, Z409, Z410, Z411, Z412, Z413, Z414, Z415, Z416, Z417, Z418, Z419, Z420, Z421, Z422, Z423, Z424, Z425, Z426, Z427, Z428, Z429, Z430, Z431, Z432, Z433, Z434, Z435, Z436, Z437, Z438, Z439, Z440, Z441, Z442, Z443, Z444, Z445, Z446, Z447, Z448, Z449, Z450, Z451, Z452, Z453, Z454, Z455, Z456, Z457, Z458, Z459, Z460, Z461, Z462, Z463, Z464, Z465, Z466, Z467, Z468, Z469, Z470, Z471, Z472, Z473, Z474, Z475, Z476, Z477, Z478, Z479, Z480, Z481, Z482, Z483, Z484, Z485, Z486, Z487, Z488, Z489, Z490, Z491, Z492, Z493, Z494, Z495, Z496, Z497, Z498, Z499, Z500, Z501, Z502, Z503, Z504, Z505, Z506, Z507, Z508, Z509, Z510, Z511, Z512 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively Z407, Z408 and/or Z416, Z417 and/or Z429, Z430 and/or Z436, Z437 and/or Z445, Z446 and/or Z455, Z456 and/or Z460, Z461 and/or Z477, Z478 and/or Z486, Z487 and/or Z489, Z490 and/or Z492, Z493 and/or Z495, Z496 and/or Z499, Z500 and/or Z505, Z506 and/or Z508, Z509 and/or Z511, Z512 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (ii) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (iii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHZ601, —NZ602Z603, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—Z604, —C(O)O—Z605, —C(O)NH—Z606, —C(O)NZ607Z608, —O—Z609, —O(—Z610-O)e—H (e=1, 2, 3, 4, 5), —O(—Z611-O)f—Z612 (f=1, 2, 3, 4, 5), —OC(O)—Z613, —OC(O)—O—Z614, —OC(O)—NHZ615, —O—C(O)—NZ616Z617, —OP(O)(OZ618)(OZ619), —OSi(Z620)(Z621)(Z622), —OS(O2)—Z623, —NHC(O)—NH2, —NHC(O)—Z624, —NZ625C(O)—Z626, —NH—C(O)—O—Z627, —NH—C(O)—NH—Z628, —NH—C(O)—NZ629Z630, —NZ631-C(O)—O—Z632, —NZ633-C(O)—NH—Z634, —NZ635-C(O)—NZ636Z637, —NHS(O2)—Z638, —NZ639S(O2)—Z640, —S—Z641, —S(O)—Z642, —S(O2)—Z643, —S(O2)NH—Z644, —S(O2)NZ645Z646, —S(O2)O—Z647, —P(O)(OZ648)(OZ649), —Si(Z650)(Z651)(Z652), —C(NH)—NH2, —C(NZ653)-NH2, —C(NH)—NHZ654, —C(NH)—NZ655Z656, —C(NZ657)-NHZ658, —C(NZ659)-NZ660Z661, —NH—C(O)—NH—O—Z662, —NH—C(O)—NZ663-O—Z664, —NZ665-C(O)—NZ666-O—Z667, —N(—C(O)—NH—O—Z668)2, —N(—C(O)—NZ669-O—Z670)2, —N(—C(O)—NH—O—Z671)(—C(O)—NZ672-O—Z673), —C(S)—Z674, —(C)—O—Z675, —C(S)—NH—Z676, —C(S)—NZ677Z678, —C(O)—NH—O—Z679, —C(O)—NZ680-O—Z681, —C(S)—NH—O—Z682, —C(S)—NZ683-O—Z684, —C(O)—NH—NH—Z685, —C(O)—NH—NZ686Z687, —C(O)—NZ688-NZ689Z690, —C(S)—NH—NH—Z691, —C(S)—NH—NZ692Z693, —C(S)—NZ694-NZ695Z696, —C(O)—C(O)—O—Z697, —C(O)—C(O)—NH2, —C(O)—C(O)—NHZ698, —C(O)—C(O)—NZ699Z700, —C(S)—C(O)—O—Z701, —C(O)—C(S)—O—Z702, —C(S)—C(S)—O—Z703, —C(S)—C(O)—NH2, —C(S)—C(O)—NHZ704, —C(S)—C(O)—NZ705Z706, —C(S)—C(S)—NH2, —C(S)—C(S)—NHZ707, —C(S)—C(S)—NZ708Z709, —C(O)—C(S)—NH2, —C(O)—C(S)—NHZ710, —C(O)—C(S)—NZ711Z712”;
        
            wherein Z601, Z602, Z603, Z604, Z605, Z606, Z607, Z608, Z609, Z610, Z611, Z612, Z613, Z614, Z615, Z616, Z617, Z618, Z619, Z620, Z621, Z622, Z623, Z624, Z625, Z626, Z627, Z628, Z629, Z630, Z631, Z632, Z633, Z634, Z635, Z636, Z637, Z638, Z639, Z640, Z641, Z642, Z643, Z644, Z645, Z646, Z647, Z648, Z649, Z650, Z651, Z652, Z653, Z654, Z655, Z656, Z657, Z658, Z659, Z660, Z661, Z662, Z663, Z664, Z665, Z666, Z667, Z668, Z669, Z670, Z671, Z672, Z673, Z674, Z675, Z676, Z677, Z678, Z679, Z680, Z681, Z682, Z683, Z684, Z685, Z686, Z687, Z688, Z689, Z690, Z691, Z692, Z693, Z694, Z695, Z696, Z697, Z698, Z699, Z700, Z701, Z702, Z703, Z704, Z705, Z706, Z707, Z708, Z709, Z710, Z711, Z712 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively Z607, Z608 and/or Z616, Z617 and/or Z629, Z630 and/or Z636, Z637 and/or Z645, Z646 and/or Z655, Z656 and/or Z660, Z661 and/or Z677, Z678 and/or Z686, Z687 and/or Z689, Z690 and/or Z692, Z693 and/or Z695, Z696 and/or Z699, Z700 and/or Z705, Z706 and/or Z708, Z709 and/or Z711, Z712 and/or respectively together can also form “heterocyclyl”;

with the proviso that radical R16 is not “indol-yl”;

(d) “—S(O2)—R18”;

        
        
        wherein radical R18 is independently selected from the group consisting of:
        (III)“—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHW1, —NW2W3, —NO2, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—W4, —C(O)O—W5, —C(O)NH—W6, —C(O)NW7W8, —O—W9, —O(—W10-O)a—H (a=1, 2, 3, 4, 5), —O(—W11-O)b—W12 (b=1, 2, 3, 4, 5), —OC(O)—W13, —OC(O)—O—W14, —OC(O)—NHW15, —O—C(O)—NW16W17, —OP(O)(OW18)(OW19), —OSi(W20)(W21)(W22), —OS(O2)—W23, —NHC(O)—NH2, —NHC(O)—W24, —NW25C(O)—W26, —NH—C(O)—O—W27, —NH—C(O)—NH—W28, —NH—C(O)—NW29W30, —NW31—C(O)—O—W32, —NW33-C(O)—NH—W34, —NW35—C(O)—NW36W37, —NHS(O2)—W38, —NW39S(O2)—W40, —S—W41, —S(O)—W42, —S(O2)—W43, —S(O2)NH—W44, —S(O2)NW45W46, —S(O2)O—W47, —P(O)(OW48)(OW49), —Si(W50)(W51)(W52), —C(NH)—NH2, —C(NW53)-NH2, —C(NH)—NHW54, —C(NH)—NW55W56, —C(NW57)-NHW58, —C(NW59)-NW60W61, —NH—C(O)—NH—O—W62, —NH—C(O)—NW63-O—W64, —NW65-C(O)—NW66-O—W67, —N(—C(O)—NH—O—W68)2, —N(—C(O)—NW69-O—W70)2, —N(—C(O)—NH—O—W71)(—C(O)—NW72-O—W73), —C(S)—W74, —C(S)—O—W75, —C(S)—NH—W76, —C(S)—NW77W78, —C(O)—NH—O—W79, —C(O)—NW80-O—W81, —C(S)—NH—O—W82, —C(S)—NW83-O—W84, —C(O)—NH—NH—W85, —C(O)—NH—NW86W87, —C(O)—NW88-NW89W90, —C(S)—NH—NH—W91, —C(S)—NH—NW92W93, —C(S)—NW94-NW95W96, —C(O)—C(O)—O—W97, —C(O)—C(O)—NH2, —C(O)—C(O)—NHW98, —C(O)—C(O)—NW99W100, —C(S)—C(O)—O—W101, —C(O)—C(S)—O—W102, —C(S)—C(S)—O—W103, —C(S)—C(O)—NH2, —C(S)—C(O)—NHW104, —C(S)—C(O)—NW105W106, —C(S)—C(S)—NH2, —C(S)—C(S)—NHW107, —C(S)—C(S)—NW108W109, —C(O)—C(S)—NH2, —C(O)—C(S)—NHW110, —C(O)—C(S)—NW111W112”;
        
            wherein W1, W2, W3, W4, W5, W6, W7, W8, W9, W10, W11, W12, W13, W14, W15, W16, W17, W18, W19, W20, W21, W22, W23, W24, W25, W26, W27, W28, W29, W30, W31, W32, W33, W34, W35, W36, W37, W38, W39, W40, W41, W42, W43, W44, W45, W46, W47, W48, W49, W50, W51, W52, W53, W54, W55, W56, W57, W58, W59, W60, W61, W62, W63, W64, W65, W66, W67, W68, W69, W70, W71, W72, W73, W74, W75, W76, W77, W78, W79, W80, W81, W82, W83, W84, W85, W86, W87, W88, W89, W90, W91, W92, W93, W94, W95, W96, W97, W98, W99, W100, W101, W102, W103, W104, W105, W106, W107, W108, W109, W110, W111, W112 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively W7, W8 and/or W16, W17 and/or W29, W30 and/or W36, W37 and/or W45, W46 and/or W55, W56 and/or W60, W61 and/or W77, W78 and/or W86, W87 and/or W89, W90 and/or W92, W93 and/or W95, W96 and/or W99, W100 and/or W105, W106 and/or W108, W109 and/or W111, W112 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (III) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (i) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHW201, —NW202W203, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—W204, —C(O)O—W205, —C(O)NH—W206, —C(O)NW207W208, —O—W209, —O(—W210-O)c—H (c=1, 2, 3, 4, 5), —O(—W211-O)d—W212 (d=1, 2, 3, 4, 5), —OC(O)—W213, —OC(O)—O—W214, —OC(O)—NHW215, —O—C(O)—NW216W217, —OP(O)(OW218)(OW219), —OSi(W220)(W221)(W222), —OS(O2)—W223, —NHC(O)—NH2, —NHC(O)—W224, —NW225C(O)—W226, —NH—C(O)—O—W227, —NH—C(O)—NH—W228, —NH—C(O)—NW229W230, —NW231—C(O)—O—W232, —NW233-C(O)—NH—W234, —NW235—C(O)—NW236W237, —NHS(O2)—W238, —NW239S(O2)—W240, —S—W241, —S(O)—W242, —S(O2)—W243, —S(O2)NH—W244, —S(O2)NW245W246, —S(O2)O—W247, —P(O)(OW248)(OW249), —Si(W250)(W251)(W252), —C(NH)—NH2, —C(NW253)-NH2, —C(NH)—NHW254, —C(NH)—NW255W256, —C(NW257)-NHW258, —C(NW259)-NW260W261, —NH—C(O)—NH—O—W262, —NH—C(O)—NW263-O—W264, —NW265—C(O)—NW266-O—W267, —N(—C(O)—NH—O—W268)2, —N(—C(O)—NW269-O—W270)2, —N(—C(O)—NH—O—W271)(—C(O)—NW272—O—W273), —C(S)—W274, —C(S)—O—W275, —C(S)—NH—W276, —C(S)—NW277W278, —C(O)—NH—O—W279, —C(O)—NW280-O—W281, —C(S)—NH—O—W282, —C(S)—NW283-O—W284, —C(O)—NH—NH—W285, —C(O)—NH—NW286W287, —C(O)—NW288-NW289W290, —C(S)—NH—NH—W291, —C(S)—NH—NW292W293, —C(S)—NW294-NW295W296, —C(O)—C(O)—O—W297, —C(O)—C(O)—NH2, —C(O)—C(O)—NHW298, —C(O)—C(O)—NW299W300, —C(S)—C(O)—O—W301, —C(O)—C(S)—O—W302, —C(S)—C(S)—O—W303, —C(S)—C(O)—NH2, —C(S)—C(O)—NHW304, —C(S)—C(O)—NW305W306, —C(S)—C(S)—NH2, —C(S)—C(S)—NHW307, —C(S)—C(S)—NW308W309, —C(O)—C(S)—NH2, —C(O)—C(S)—NHW310, —C(O)—C(S)—NW311W312”;
        
            wherein W201, W202, W203, W204, W205, W206, W207, W208, W209, W210, W211, W212, W213, W214, W215, W216, W217, W218, W219, W220, W221, W222, W223, W224, W225, W226, W227, W228, W229, W230, W231, W232, W233, W234, W235, W236, W237, W238, W239, W240, W241, W242, W243, W244, W245, W246, W247, W248, W249, W250, W251, W252, W253, W254, W255, W256, W257, W258, W259, W260, W261, W262, W263, W264, W265, W266, W267, W268, W269, W270, W271, W272, W273, W274, W275, W276, W277, W278, W279, W280, W281, W282, W283, W284, W285, W286, W287, W288, W289, W290, W291, W292, W293, W294, W295, W296, W297, W298, W299, W300, W301, W302, W303, W304, W305, W306, W307, W308, W309, W310, W311, W312 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively W207, W208 and/or W216, W217 and/or W229, W230 and/or W236, W237 and/or W245, W246 and/or W255, W256 and/or W260, W261 and/or W277, W278 and/or W286, W287 and/or W289, W290 and/or W292, W293 and/or W295, W296 and/or W299, W300 and/or W305, W306 and/or W308, W309 and/or W311, W312 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (i) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (ii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHW401, —NW402W403, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—W404, —C(O)O—W405, —C(O)NH—W406, —C(O)NW407W408, —O—W409, —O(—W410-O)e—H (e=1, 2, 3, 4, 5), —O(—W411-O)f—W412 (f=1, 2, 3, 4, 5), —OC(O)—W413, —OC(O)—O—W414, —OC(O)—NHW415, —O—C(O)—NW416W417, —OP(O)(OW418)(OW419), —OSi(W420)(W421)(W422), —OS(O2)—W423, —NHC(O)—NH2, —NHC(O)—W424, —NW425C(O)—W426, —NH—C(O)—O—W427, —NH—C(O)—NH—W428, —NH—C(O)—NW429W430, —NW431-C(O)—O—W432, —NW433-C(O)—NH—W434, —NW435-C(O)—NW436W437, —NHS(O2)—W438, —NW439S(O2)—W440, —S—W441, —S(O)—W442, —S(O2)—W443, —S(O2)NH—W444, —S(O2)NW445W446, —S(O2)O—W447, —P(O)(OW448)(OW449), —Si(W450)(W451)(W452), —C(NH)—NH2, —C(NW453)-NH2, —C(NH)—NHW454, —C(NH)—NW455W456, —C(NW457)-NHW458, —C(NW459)-NW460W461, —NH—C(O)—NH—O—W462, —NH—C(O)—NW463-O—W464, —NW465-C(O)—NW466—O—W467, —N(—C(O)—NH—O—W468)2, —N(—C(O)—NW469-O—W470)2, —N(—C(O)—NH—O—W471)(—C(O)—NW472-O—W473), —C(S)—W474, —C(S)—O—W475, —C(S)—NH—W476, —C(S)—NW477W478, —C(O)—NH—O—W479, —C(O)—NW480-O—W481, —C(S)—NH—O—W482, —C(S)—NW483-O—W484, —C(O)—NH—NH—W485, —C(O)—NH—NW486W487, —C(O)—NW488-NW489W490, —C(S)—NH—NH—W491, —C(S)—NH—NW492W493, —C(S)—NW494-NW495W496, —C(O)—C(O)—O—W497, —C(O)—C(O)—NH2, —C(O)—C(O)—NHW498, —C(O)—C(O)—NW499W500, —C(S)—C(O)—O—W501, —C(O)—C(S)—O—W502, —C(S)—C(S)—O—W503, —C(S)—C(O)—NH2, —C(S)—C(O)—NHW504, —C(S)—C(O)—NW505W506, —C(S)—C(S)—NH2, —C(S)—C(S)—NHW507, —C(S)—C(S)—NW508W509, —C(O)—C(S)—NH2, —C(O)—C(S)—NHW510, —C(O)—C(S)—NW511W512”;
        
            wherein W401, W402, W403, W404, W405, W406, W407, W408, W409, W410, W411, W412, W413, W414, W415, W416, W417, W418, W419, W420, W421, W422, W423, W424, W425, W426, W427, W428, W429, W430, W431, W432, W433, W434, W435, W436, W437, W438, W439, W440, W441, W442, W443, W444, W445, W446, W447, W448, W449, W450, W451, W452, W453, W454, W455, W456, W457, W458, W459, W460, W461, W462, W463, W464, W465, W466, W467, W468, W469, W470, W471, W472, W473, W474, W475, W476, W477, W478, W479, W480, W481, W482, W483, W484, W485, W486, W487, W488, W489, W490, W491, W492, W493, W494, W495, W496, W497, W498, W499, W500, W501, W502, W503, W504, W505, W506, W507, W508, W509, W510, W511, W512 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively W407, W408 and/or W416, W417 and/or W429, W430 and/or W436, W437 and/or W445, W446 and/or W455, W456 and/or W460, W461 and/or W477, W478 and/or W486, W487 and/or W489, W490 and/or W492, W493 and/or W495, W496 and/or W499, W500 and/or W505, W506 and/or W508, W509 and/or W511, W512 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (ii) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (iii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHW601, —NW602W603, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—W604, —C(O)O—W605, —C(O)NH—W606, —C(O)NW607W608, —O—W609, —O(—W610-O)e—H (e=1, 2, 3, 4, 5), —O(—W611-O)f—W612 (f=1, 2, 3, 4, 5), —OC(O)—W613, —OC(O)—O—W614, —OC(O)—NHW615, —O—C(O)—NW616W617, —OP(O)(OW618)(OW619), —OSi(W620)(W621)(W622), —OS(O2)—W623, —NHC(O)—NH2, —NHC(O)—W624, —NW625C(O)—W626, —NH—C(O)—O—W627, —NH—C(O)—NH—W628, —NH—C(O)—NW629W630, —NW631-C(O)—O—W632, —NW633-C(O)—NH—W634, —NW635-C(O)—NW636W637, —NHS(O2)—W638, —NW639S(O2)—W640, —S—W641, —S(O)—W642, —S(O2)W643, —S(O2)NH—W644, —S(O2)NW645W646, —S(O2)O—W647, —P(O)(OW648)(OW649), —Si(W650)(W651)(W652), —C(NH)—NH2, —C(NW653)-NH2, —C(NH)—NHW654, —C(NH)—NW655W656, —C(NW657)-NHW658, —C(NW659)-NW660W661, —NH—C(O)—NH—O—W662, —NH—C(O)—NW663-O—W664, —NW665-C(O)—NW666-O—W667, —N(—C(O)—NH—O—W668)2, —N(—C(O)—NW669-O—W670)2, —N(—C(O)—NH—O—W671)(—C(O)—NW672—O—W673), —C(S)—W674, —C(S)—O—W675, —C(S)—NH—W676, —C(S)—NW677W678, —C(O)—NH—O—W679, —C(O)—NW680-O—W681, —C(S)—NH—O—W682, —C(S)—NW683-O—W684, —C(O)—NH—NH—W685, —C(O)—NH—NW686W687, —C(O)—NW688-NW689W690, —C(S)—NH—NH—W691, —C(S)—NH—NW692W693, —C(S)—NW694-NW695W696, —C(O)—C(O)—O—W697, —C(O)—C(O)—NH2, —C(O)—C(O)—NHW698, —C(O)—C(O)—NW699W700, —C(S)—C(O)—O—W701, —C(O)—C(S)—O—W702, —C(S)—C(S)—O—W703, —C(S)—C(O)—NH2, —C(S)—C(O)—NHW704, —C(S)—C(O)—NW705W706, —C(S)—C(S)—NH2, —C(S)—C(S)—NHW707, —C(S)—C(S)—NW708W709, —C(O)—C(S)—NH2, —C(O)—C(S)—NHW710, —C(O)—C(S)—NW711W712”;
        
            wherein W601, W602, W603, W604, W605, W606, W607, W608, W609, W610, W611, W612, W613, W614, W615, W616, W617, W618, W619, W620, W621, W622, W623, W624, W625, W626, W627, W628, W629, W630, W631, W632, W633, W634, W635, W636, W637, W638, W639, W640, W641, W642, W643, W644, W645, W646, W647, W648, W649, W650, W651, W652, W653, W654, W655, W656, W657, W658, W659, W660, W661, W662, W663, W664, W665, W666, W667, W668, W669, W670, W671, W672, W673, W674, W675, W676, W677, W678, W679, W680, W681, W682, W683, W684, W685, W686, W687, W688, W689, W690, W691, W692, W693, W694, W695, W696, W697, W698, W699, W700, W701, W702, W703, W704, W705, W706, W707, W708, W709, W710, W711, W712 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalky, aryl, arylaklkyl, heteroaryl, heteroarylalkyl” and wherein alternatively W607, W608 and/or W616, W617 and/or W629, W630 and/or W636, W637 and/or W645, W646 and/or W655, W656 and/or W660, W661 and/or W677, W678 and/or W686, W687 and/or W689, W690 and/or W692, W693 and/or W695, W696 and/or W699, W700 and/or W705, W706 and/or W708, W709 and/or W711, W712 and/or respectively together can also form “heterocyclyl”;
        
        
        with the first proviso that radical R18 is not selected from the group consisting of: “—O-alkyl, —O—(C9-C30)alkyl, —O-aryl, —O-arylalkyl, —O-heteroaryl, —O-heteroarylalkyl, —O-cycloalkyl, —O-cycloalkylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl”;
        with the second proviso that, if radical R18 independently is selected from the group consisting of: “—NRaRb”, with Ra, Rb independently from each other being selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl”, radical R1 is not selected from the group consisting of: “heterocyclylalkyl being substituted with ═O, where heterocyclyl is 5-membered; alkyl being substituted with heterocyclyl, where heterocyclyl is 5-membered and substituted with ═O”;

and one of radicals R3, R4 or neither of radicals R3, R4 independently is selected from the group consisting of:

    
    
    (2) “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHA1, —NA2A3, —NO2, —OH, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)-A4, —C(O)O-A5, —C(O)NH-A6, —C(O)NA7A8, —O-A9, —O(-A10-O)a—H (a=1, 2, 3, 4, 5), —O(-A11-O)b-A12 (b=1, 2, 3, 4, 5), —OC(O)-A13, —OC(O)—O-A14, —OC(O)—NHA15, —O—C(O)—NA16A17, —OP(O)(OA18)(OA19), —OSi(A20)(A21)(A22), —OS(O2)-A23, —NHC(O)—NH2, —NHC(O)-A24, —NA25C(O)-A26, —NH—C(O)—O-A27, —NH—C(O)—NH-A28, —NH—C(O)—NA29A30, —NA31-C(O)—O-A32, —NA33-C(O)—NH-A34, —NA35-C(O)—NA36A37, —NHS(O2)-A38, —NA39S(O2)-A40, —S-A41, —S(O)-A42, —S(O2)— A43, —S(O2)NH-A44, —S(O2)NA45A46, —S(O2)O-A47, —P(O)(OA48)(OA49), —Si(A50)(A51)(A52), —C(NH)—NH2, —C(NA53)-NH2, —C(NH)—NHA54, —C(NH)—NA55A56, —C(NA57)-NHA58, —C(NA59)-NA60A61, —NH—C(O)—NH—O-A62, —NH—C(O)—NA63-O-A64, —NA65-C(O)—NA66-O-A67, —N(—C(O)—NH—O-A68)2, —N(—C(O)—NA69-O-A70)2, —N(—C(O)—NH—O-A71)(—C(O)—NA72-O-A73), —C(S)-A74, —C(S)—O-A75, —C(S)—NH-A76, —C(S)—NA77A78, —C(O)—NH—O-A79, —C(O)—NA80-O-A81, —C(S)—NH—O-A82, —C(S)—NA83-O-A84, —C(O)—NH—NH-A85, —C(O)—NH—NA86A87, —C(O)—NA88-NA89A90, —C(S)—NH—NH-A91, —C(S)—NH—NA92A93, —C(S)—NA94-NA95A96, —C(O)—C(O)—O-A97, —C(O)—C(O)—NH2, —C(O)—C(O)—NHA98, —C(O)—C(O)—NA99A100, —C(S)—C(O)—O-A101, —C(O)—C(S)—O-A102, —C(S)—C(S)—O-A103, —C(S)—C(O)—NH2, —C(S)—C(O)—NHA104, —C(S)—C(O)—NA105A106, —C(S)—C(S)—NH2, —C(S)—C(S)—NHA107, —C(S)—C(S)—NA108A109, —C(O)—C(S)—NH2, —C(O)—C(S)—NHA110, —C(O)—C(S)—NA111A112”;
    
        wherein A1, A2, A3, A4, A5, A6, A7, A8, A9, A10, A11, A12, A13, A14, A15, A16, A17, A18, A19, A20, A21, A22, A23, A24, A25, A26, A27, A28, A29, A30, A31, A32, A33, A34, A35, A36, A37, A38, A39, A40, A41, A42, A43, A44, A45, A46, A47, A48, A49, A50, A51, A52, A53, A54, A55, A56, A57, A58, A59, A60, A61, A62, A63, A64, A65, A66, A67, A68, A69, A70, A71, A72, A73, A74, A75, A76, A77, A78, A79, A80, A81, A82, A83, A84, A85, A86, A87, A88, A89, A90, A91, A92, A93, A94, A95, A96, A97, A98, A99, A100, A101, A102, A103, A104, A105, A106, A107, A108, A109, A110, A111, A112 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively A7, A8 and/or A16, A17 and/or A29, A30 and/or A36, A37 and/or A45, A46 and/or A55, A56 and/or A60, A61 and/or A77, A78 and/or A86, A87 and/or A89, A90 and/or A92, A93 and/or A95, A96 and/or A99, A100 and/or A105, A106 and/or A108, A109 and/or A111, A112 and/or respectively together can also form “heterocyclyl”;
        wherein optionally above substituents of substituents group (2)—if not hydrogenn—can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        (i) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHA201, —NA202A203, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)-A204, —C(O)O-A205, —C(O)NH-A206, —C(O)NA207A208, —O-A209, —O(-A210-O)c—H (c=1, 2, 3, 4, 5), —O(-A211-O)d-A212 (d=1, 2, 3, 4, 5), —OC(O)-A213, —OC(O)—O-A214, —OC(O)—NHA215, —O—C(O)—NA216A217, —OP(O)(OA218)(OA219), —OSi(A220)(A221)(A222), —OS(O2)-A223, —NHC(O)—NH2, —NHC(O)-A224, —NA225C(O)-A226, —NH—C(O)—O-A227, —NH—C(O)—NH-A228, —NH—C(O)—NA229A230, —NA231-C(O)—O-A232, —NA233-C(O)—NH-A234, —NA235-C(O)—NA236A237, —NHS(O2)-A238, —NA239S(O2)-A240, —S-A241, —S(O)-A242, —S(O2)-A243, —S(O2)NH-A244, —S(O2)NA245A246, —S(O2)O-A247, —P(O)(OA248)(OA249), —Si(A250)(A251)(A252), —C(NH)—NH2, —C(NA253)-NH2, —C(NH)—NHA254, —C(NH)—NA255A256, —C(NA257)-NHA258, —C(NA259)-NA260A261, —NH—C(O)—NH—O-A262, —NH—C(O)—NA263-O-A264, —NA265-C(O)—NA266-O-A267, —N(—C(O)—NH—O-A268)2, —N(—C(O)—NA269-O-A270)2, —N(—C(O)—NH—O-A271)(—C(O)—NA272-O-A273), —C(S)-A274, —C(S)—O-A275, —C(S)—NH-A276, —C(S)—NA277A278, —C(O)—NH—O-A279, —C(O)—NA280-O-A281, —C(S)—NH—O-A282, —C(S)—NA283-O-A284, —C(O)—NH—NH-A285, —C(O)—NH—NA286A287, —C(O)—NA288-NA289A290, —C(S)—NH—NH-A291, —C(S)—NH—NA292A293, —C(S)—NA294-NA295A296, —C(O)—C(O)—O-A297, —C(O)—C(O)—NH2, —C(O)—C(O)—NHA298, —C(O)—C(O)—NA299A300, —C(S)—C(O)—O-A301, —C(O)—C(S)—O-A302, —C(S)—C(S)—O-A303, —C(S)—C(O)—NH2, —C(S)—C(O)—NHA304, —C(S)—C(O)—NA305A306, —C(S)—C(S)—NH2, —C(S)—C(S)—NHA307, —C(S)—C(S)—NA308A309, —C(O)—C(S)—NH2, —C(O)—C(S)—NHA310, —C(O)—C(S)—NA311A312”;
        wherein A201, A202, A203, A204, A205, A206, A207, A208, A209, A210, A211, A212, A213, A214, A215, A216, A217, A218, A219, A220, A221, A222, A223, A224, A225, A226, A227, A228, A229, A230, A231, A232, A233, A234, A235, A236, A237, A238, A239, A240, A241, A242, A243, A244, A245, A246, A247, A248, A249, A250, A251, A252, A253, A254, A255, A256, A257, A258, A259, A260, A261, A262, A263, A264, A265, A266, A267, A268, A269, A270, A271, A272, A273, A274, A275, A276, A277, A278, A279, A280, A281, A282, A283, A284, A285, A286, A287, A288, A289, A290, A291, A292, A293, A294, A295, A296, A297, A298, A299, A300, A301, A302, A303, A304, A305, A306, A307, A308, A309, A310, A311, A312 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively A207, A208 and/or A216, A217 and/or A229, A230 and/or A236, A237 and/or A245, A246 and/or A255, A256 and/or A260, A261 and/or A277, A278 and/or A286, A287 and/or A289, A290 and/or A292, A293 and/or A295, A296 and/or A299, A300 and/or A305, A306 and/or A308, A309 and/or A311, A312 and/or respectively together can also form “heterocyclyl”;
        
            wherein optionally above substituents of substituents group (i) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (ii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHA401, —NA402A403, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)-A404, —C(O)O-A405, —C(O)NH-A406, —C(O)NA407A408, —O-A409, —O(-A410-O)e—H (e=1, 2, 3, 4, 5), —O(-A411-O)f-A412 (f=1, 2, 3, 4, 5), —OC(O)-A413, —OC(O)—O-A414, —OC(O)—NHA415, —O—C(O)—NA416A417, —OP(O)(OA418)(OA419), —OSi(A420)(A421)(A422), —OS(O2)-A423, —NHC(O)—NH2, —NHC(O)-A424, —NA425C(O)-A426, —NH—C(O)—O-A427, —NH—C(O)—NH-A428, —NH—C(O)—NA429A430, —NA431-C(O)—O-A432, —NA433-C(O)—NH-A434, —NA435-C(O)—NA436A437, —NHS(O2)-A438, —NA439S(O2)-A440, —S-A441, —S(O)-A442, —S(O2)— A443, —S(O2)NH-A444, —S(O2)NA445A446, —S(O2)O-A447, —P(O)(OA448)(OA449), —Si(A450)(A451)(A452), —C(NH)—NH2, —C(NA453)-NH2, —C(NH)—NHA454, —C(NH)—NA455A456, —C(NA457)-NHA458, —C(NA459)-NA460A461, —NH—C(O)—NH—O-A462, —NH—C(O)—NA463-O-A464, —NA465-C(O)—NA466-O-A467, —N(—C(O)—NH—O-A468)2, —N(—C(O)—NA469-O-A470)2, —N(—C(O)—NH—O-A471)(—C(O)—NA472-O-A473), —C(S)-A474, —C(S)—O-A475, —C(S)—NH-A476, —C(S)—NA477A478, —C(O)—NH—O-A479, —C(O)—NA480-O-A481, —C(S)—NH—O-A482, —C(S)—NA483-O-A484, —C(O)—NH—NH-A485, —C(O)—NH—NA486A487, —C(O)—NA488-NA489A490, —C(S)—NH—NH-A491, —C(S)—NH—NA492A493, —C(S)—NA494-NA495A496, —C(O)—C(O)—O-A497, —C(O)—C(O)—NH2, —C(O)—C(O)—NHA498, —C(O)—C(O)—NA499A500, —C(S)—C(O)—O-A501, —C(O)—C(S)—O-A502, —C(S)—C(S)—O-A503, —C(S)—C(O)—NH2, —C(S)—C(O)—NHA504, —C(S)—C(O)—NA505A506, —C(S)—C(S)—NH2, —C(S)—C(S)—NHA507, —C(S)—C(S)—NA508A509, —C(O)—C(S)—NH2, —C(O)—C(S)—NHA510, —C(O)—C(S)—NA511A512”;
        
            wherein A401, A402, A403, A404, A405, A406, A407, A408, A409, A410, A411, A412, A413, A414, A415, A416, A417, A418, A419, A420, A421, A422, A423, A424, A425, A426, A427, A428, A429, A430, A431, A432, A433, A434, A435, A436, A437, A438, A439, A440, A441, A442, A443, A444, A445, A446, A447, A448, A449, A450, A451, A452, A453, A454, A455, A456, A457, A458, A459, A460, A461, A462, A463, A464, A465, A466, A467, A468, A469, A470, A471, A472, A473, A474, A475, A476, A477, A478, A479, A480, A481, A482, A483, A484, A485, A486, A487, A488, A489, A490, A491, A492, A493, A494, A495, A496, A497, A498, A499, A500, A501, A502, A503, A504, A505, A506, A507, A508, A509, A510, A511, A512 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively A407, A408 and/or A416, A417 and/or A429, A430 and/or A436, A437 and/or A445, A446 and/or A455, A456 and/or A460, A461 and/or A477, A478 and/or A486, A487 and/or A489, A490 and/or A492, A493 and/or A495, A496 and/or A499, A500 and/or A505, A506 and/or A508, A509 and/or A511, A512 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (ii) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (iii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHA601, —NA602A603, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)-A604, —C(O)O—A605, —C(O)NH-A606, —C(O)NA607A608, —O-A609, —O(-A610-O)e—H (e=1, 2, 3, 4, 5), —O(-A611-O)f-A612 (f=1, 2, 3, 4, 5), —OC(O)-A613, —OC(O)—O-A614, —OC(O)—NHA615, —O—C(O)—NA616A617, —OP(O)(OA618)(OA619), —OSi (A620)(A621)(A622), —OS(O2)-A623, —NHC(O)—NH2, —NHC(O)-A624, —NA625C(O)-A626, —NH—C(O)—O-A627, —NH—C(O)—NH-A628, —NH—C(O)—NA629A630, —NA631-C(O)—O-A632, —NA633-C(O)—NH-A634, —NA635-C(O)—NA636A637, —NHS(O2)-A638, —NA639S(O2)-A640, —S-A641, —S(O)-A642, —S(O2)-A643, —S(O2)NH-A644, —S(O2)NA645A646, —S(O2)O-A647, —P(O)(OA648)(OA649), —Si(A650)(A651)(A652), —C(NH)—NH2, —C(NA653)-NH2, —C(NH)—NHA654, —C(NH)—NA655A656, —C(NA657)-NHA658, —C(NA659)-NA660A661, —NH—C(O)—NH—O-A662, —NH—C(O)—NA663-O-A664, —NA665-C(O)—NA666-O-A667, —N(—C(O)—NH—O-A668)2, —N(—C(O)—NA669-O-A670)2, —N(—C(O)—NH—O-A671)(—C(O)—NA672-O-A673), —C(S)-A674, —C(S)—O-A675, —C(S)—NH-A676, —C(S)—NA677A678, —C(O)—NH—O-A679, —C(O)—NA680-O-A681, —C(S)—NH—O-A682, —C(S)—NA683-O-A684, —C(O)—NH—NH-A685, —C(O)—NH—NA686A687, —C(O)—NA688-NA689A690, —C(S)—NH—NH-A691, —C(S)—NH—NA692A693, —C(S)—NA694-NA695A696, —C(O)—C(O)—O-A697, —C(O)—C(O)—NH2, —C(O)—C(O)—NHA698, —C(O)—C(O)—NA699A700, —C(S)—C(O)—O-A701, —C(O)—C(S)—O-A702, —C(S)—C(S)—O-A703, —C(S)—C(O)—NH2, —C(S)—C(O)—NHA704, —C(S)—C(O)—NA705A706, —C(S)—C(S)—NH2, —C(S)—C(S)—NHA707, —C(S)—C(S)—NA708A709, —C(O)—C(S)—NH2, —C(O)—C(S)—NHA710, —C(O)—C(S)—NA711A712”;
        
            wherein A601, A602, A603, A604, A605, A606, A607, A608, A609, A610, A611, A612, A613, A614, A615, A616, A617, A618, A619, A620, A621, A622, A623, A624, A625, A626, A627, A628, A629, A630, A631, A632, A633, A634, A635, A636, A637, A638, A639, A640, A641, A642, A643, A644, A645, A646, A647, A648, A649, A650, A651, A652, A653, A654, A655, A656, A657, A658, A659, A660, A661, A662, A663, A664, A665, A666, A667, A668, A669, A670, A671, A672, A673, A674, A675, A676, A677, A678, A679, A680, A681, A682, A683, A684, A685, A686, A687, A688, A689, A690, A691, A692, A693, A694, A695, A696, A697, A698, A699, A700, A701, A702, A703, A704, A705, A706, A707, A708, A709, A710, A711, A712 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively A607, A608 and/or A616, A617 and/or A629, A630 and/or A636, A637 and/or A645, A646 and/or A655, A656 and/or A660, A661 and/or A677, A678 and/or A686, A687 and/or A689, A690 and/or A692, A693 and/or A695, A696 and/or A699, A700 and/or A705, A706 and/or A708, A709 and/or A711, A712 and/or respectively together can also form “heterocyclyl”;

and radicals R1, R2, R5 independently from each other are selected from the group consisting of:

        
        
    
    
    (3) “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHB1, —NB2B3, —NO2, —OH, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—B4, —C(O)O—B5, —C(O)NH—B6, —C(O)NB7B8, —O—B9, —O(—B10-O)a—H (a=1, 2, 3, 4, 5), —O(—B11-O)b—B12 (b=1, 2, 3, 4, 5), —OC(O)—B13, —OC(O)—O—B14, —OC(O)—NHB15, —O—C(O)—NB16B17, —OP(O)(OB18)(OB19), —OSi(B20)(B21)(B22), —OS(O2)—B23, —NHC(O)—NH2, —NHC(O)—B24, —NB25C(O)—B26, —NH—C(O)—O—B27, —NH—C(O)—NH—B28, —NH—C(O)—NB29B30, —NB31-C(O)—O—B32, —NB33-C(O)—NH—B34, —NB35-C(O)—NB36B37, —NHS(O2)—B38, —NB39S(O2)—B40, —S—B41, —S(O)—B42, —S(O2)— B43, —S(O2)NH—B44, —S(O2)NB45B46, —S(O2)O—B47, —P(O)(OB48)(OB49), —Si(B50)(B51)(B52), —C(NH)—NH2, —C(NB53)-NH2, —C(NH)—NHB54, —C(NH)—NB55B56, —C(NB57)-NHB58, —C(NB59)-NB60B61, —NH—C(O)—NH—O—B62, —NH—C(O)—NB63-O—B64, —NB65-C(O)—NB66-O—B67, —N(—C(O)—NH—O—B68)2, —N(—C(O)—NB69-O—B70)2, —N(—C(O)—NH—O—B71)(—C(O)—NB72-O—B73), —C(S)—B74, —C(S)—O—B75, —C(S)—NH—B76, —C(S)—NB77B78, —C(O)—NH—O—B79, —C(O)—NB80-O—B81, —C(S)—NH—O—B82, —C(S)—NB83-O—B84, —C(O)—NH—NH—B85, —C(O)—NH—NB86B87, —C(O)—NB88-NB89B90, —C(S)—NH—NH—B91, —C(S)—NH—NB92B93, —C(S)—NB94-NB95B96, —C(O)—C(O)—O—B97, —C(O)—C(O)—NH2, —C(O)—C(O)—NHB98, —C(O)—C(O)—NB99B100, —C(S)—C(O)—O—B101, —C(O)—C(S)—O—B102, —C(S)—C(S)—O—B103, —C(S)—C(O)—NH2, —C(S)—C(O)—NHB104, —C(S)—C(O)—NB105B106, —C(S)—C(S)—NH2, —C(S)—C(S)—NHB107, —C(S)—C(S)—NB108B109, —C(O)—C(S)—NH2, —C(O)—C(S)—NHB110, —C(O)—C(S)—NB111B112”;
    
        wherein B1, B2, B3, B4, B5, B6, B7, B8, B9, B10, B11, B12, B13, B14, B15, B16, B17, B18, B19, B20, B21, B22, B23, B24, B25, B26, B27, B28, B29, B30, B31, B32, B33, B34, B35, B36, B37, B38, B39, B40, B41, B42, B43, B44, B45, B46, B47, B48, B49, B50, B51, B52, B53, B54, B55, B56, B57, B58, B59, B60, B61, B62, B63, B64, B65, B66, B67, B68, B69, B70, B71, B72, B73, B74, B75, B76, B77, B78, B79, B80, B81, B82, B83, B84, B85, B86, B87, B88, B89, B90, B91, B92, B93, B94, B95, B96, B97, B98, B99, B100, B101, B102, B103, B104, B105, B106, B107, B108, B109, B110, B111, B112 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively B2, B3 and/or B7, B8 and/or B16, B17 and/or B29, B30 and/or B36, B37 and/or B45, B46 and/or B55, B56 and/or B60, B61 and/or B77, B78 and/or B86, B87 and/or B89, B90 and/or B92, B93 and/or B95, B96 and/or B99, B100 and/or B105, B106 and/or B108, B109 and/or B111, B112 and/or respectively together can also form “heterocyclyl”;
        wherein optionally above substituents of substituents group (3)—if not hydrogen—can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        (i) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHB201, —NB202B203, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—B204, —C(O)O—B205, —C(O)NH—B206, —C(O)NB207B208, —O—B209, —O(—B210-O)c—H (c=1, 2, 3, 4, 5), —O(—B211-O)d—B212 (d=1, 2, 3, 4, 5), —OC(O)—B213, —OC(O)—O—B214, —OC(O)—NHB215, —O—C(O)—N B216B217, —OP(O)(OB218)(OB219), —OSi(B220)(B221)(B222), —OS(O2)— B223, —NHC(O)—NH2, —NHC(O)—B224, —NB225C(O)—B226, —NH—C(O)—O—B227, —NH—C(O)—NH—B228, —NH—C(O)—NB229B230, —NB231-C(O)—O—B232, —NB233-C(O)—NH—B234, —NB235-C(O)—NB236B237, —NHS(O2)— B238, —NB239S(O2)—B240, —S—B241, —S(O)—B242, —S(O2)—B243, —S(O2)NH—B244, —S(O2)NB245B246, —S(O2)O—B247, —P(O)(OB248)(OB249), —Si(B250)(B251)(B252), —C(NH)—NH2, —C(NB253)-NH2, —C(NH)—NHB254, —C(NH)—NB255B256, —C(NB257)-NHB258, —C(NB259)-NB260B261, —NH—C(O)—NH—O—B262, —NH—C(O)—NB263-O—B264, —NB265-C(O)—NB266-O—B267, —N(—C(O)—NH—O—B268)2, —N(—C(O)—NB269-O—B270)2, —N(—C(O)—NH—O—B271)(—C(O)—NB272-O—B273), —C(S)—B274, —C(S)—O—B275, —C(S)—NH—B276, —C(S)—NB277B278, —C(O)—NH—O—B279, —C(O)—NB280-O—B281, —C(S)—NH—O—B282, —C(S)—NB283-O—B284, —C(O)—NH—NH—B285, —C(O)—NH—NB286B287, —C(O)—NB288-NB289B290, —C(S)—NH—NH—B291, —C(S)—NH—NB292B293, —C(S)—NB294-NB295B296, —C(O)—C(O)—O—B297, —C(O)—C(O)—NH2, —C(O)—C(O)—NHB298, —C(O)—C(O)—NB299B300, —C(S)—C(O)—O—B301, —C(O)—C(S)—O—B302, —C(S)—C(S)—O—B303, —C(S)—C(O)—NH2, —C(S)—C(O)—NHB304, —C(S)—C(O)—NB305B306, —C(S)—C(S)—NH2, —C(S)—C(S)—NHB307, —C(S)—C(S)—NB308B309, —C(O)—C(S)—NH2, —C(O)—C(S)—NHB310, —C(O)—C(S)—NB311B312”;
        
            wherein B201, B202, B203, B204, B205, B206, B207, B208, B209, B210, B211, B212, B213, B214, B215, B216, B217, B218, B219, B220, B221, B222, B223, B224, B225, B226, B227, B228, B229, B230, B231, B232, B233, B234, B235, B236, B237, B238, B239, B240, B241, B242, B243, B244, B245, B246, B247, B248, B249, B250, B251, B252, B253, B254, B255, B256, B257, B258, B259, B260, B261, B262, B263, B264, B265, 8266, B267, B268, B269, B270, B271, B272, B273, B274, B275, B276, B277, B278, B279, B280, B281, B282, B283, B284, B285, B286, B287, B288, B289, B290, B291, B292, B293, B294, B295, B296, B297, B298, B299, B300, B301, B302, B303, B304, B305, B306, B307, B308, B309, B310, B311, B312 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively B207, B208 and/or B216, B217 and/or B229, B230 and/or B236, B237 and/or 8245, B246 and/or B255, B256 and/or B260, B261 and/or 8277, B278 and/or 8286, B287 and/or B289, B290 and/or B292, B293 and/or 8295, B296 and/or 8299, B300 and/or 8305, B306 and/or B308, B309 and/or B311, B312 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (i) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (ii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHB401, —NB402B403, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—B404, —C(O)O—B405, —C(O)NH—B406, —C(O)NB407B408, —O—B409, —O(—B410-O)e—H (e=1, 2, 3, 4, 5), —O(—B411-O)f—B412 (f=1, 2, 3, 4, 5), —OC(O)—B413, —OC(O)—O—B414, —OC(O)—NHB415, —O—C(O)—NB416B417, —OP(O)(OB418)(OB419), —OSi(B420)(B421)(B422), —OS(O2)—B423, —NHC(O)—NH2, —NHC(O)—B424, —NB425C(O)—B426, —NH—C(O)—O—B427, —NH—C(O)—NH—B428, —NH—C(O)—NB429B430, —NB431-C(O)—O—B432, —NB433-C(O)—NH—B434, —NB435-C(O)—NB436B437, —NHS(O2)—B438, —NB439S(O2)— B440, —S—B441, —S(O)—B442, —S(O2)—B443, —S(O2)NH—B444, —S(O2)NB445B446, —S(O2)O—B447, —P(O)(OB448)(OB449), —Si(B450)(B451)(B452), —C(NH)—NH2, —C(NB453)-NH2, —C(NH)—NHB454, —C(NH)—NB455B456, —C(NB457)-NHB458, —C(NB459)-NB460B461, —NH—C(O)—NH—O—B462, —NH—C(O)—NB463-O—B464, —NB465-C(O)—NB466-O—B467, —N(—C(O)—NH—O—B468)2, —N(—C(O)—NB469-O—B470)2, —N(—C(O)—NH—O—B471)(—C(O)—NB472-O—B473), —C(S)—B474, —C(S)—O—B475, —C(S)—NH—B476, —C(S)—NB477B478, —C(O)—NH—O—B479, —C(O)—NB480-O—B481, —C(S)—NH—O—B482, —C(S)—NB483-O—B484, —C(O)—NH—NH—B485, —C(O)—NH—NB486B487, —C(O)—NB488-NB489B490, —C(S)—NH—NH—B491, —C(S)—NH—NB492B493, —C(S)—NB494-NB495B496, —C(O)—C(O)—O—B497, —C(O)—C(O)—NH2, —C(O)—C(O)—NHB498, —C(O)—C(O)—NB499B500, —C(S)—C(O)—O—B501, —C(O)—C(S)—O—B502, —C(S)—C(S)—O—B503, —C(S)—C(O)—NH2, —C(S)—C(O)—NHB504, —C(S)—C(O)—NB505B506, —C(S)—C(S)—NH2, —C(S)—C(S)—NHB507, —C(S)—C(S)—NB508B509, —C(O)—C(S)—NH2, —C(O)—C(S)—NHB510, —C(O)—C(S)—NB511B512”;
        
            wherein B401, B402, B403, B404, B405, B406, B407, B408, B409, B410, B411, B412, B413, B414, B415, B416, B417, B418, B419, B420, B421, B422, B423, B424, B425, B426, B427, B428, B429, B430, B431, B432, B433, B434, B435, B436, B437, B438, B439, B440, B441, B442, B443, B444, B445, B446, B447, B448, B449, B450, B451, B452, B453, B454, B455, B456, B457, B458, B459, B460, B461, B462, B463, B464, B465, B466, B467, B468, B469, B470, B471, B472, B473, B474, B475, B476, B477, B478, B479, B480, B481, B482, B483, B484, B485, B486, B487, B488, B489, B490, B491, B492, B493, B494, B495, B496, B497, B498, B499, B500, B501, B502, B503, B504, B505, B506, B507, B508, B509, B510, B511, B512 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively B407, B408 and/or B416, B417 and/or B429, B430 and/or B436, B437 and/or B445, B446 and/or B455, B456 and/or B460, B461 and/or B477, B478 and/or B486, B487 and/or B489, B490 and/or B492, B493 and/or B495, B496 and/or B499, B500 and/or B505, B506 and/or B508, B509 and/or B511, B512 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (ii) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (iii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHB601, —NB602B603, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—B604, —C(O)O—B605, —C(O)NH—B606, —C(O)NB607B608, —O—B609, —O(—B610-O)e—H (e=1, 2, 3, 4, 5), —O(—B611-O)f—B612 (f=1, 2, 3, 4, 5), —OC(O)—B613, —OC(O)—O—B614, —OC(O)—NHB615, —O—C(O)—NB616B617, —OP(O)(OB618)(OB619), —OSi(B620)(B621)(B622), —OS(O2)—B623, —NHC(O)—NH2, —NHC(O)—B624, —NB625C(O)—B626, —NH—C(O)—O—B627, —NH—C(O)—NH—B628, —NH—C(O)—NB629B630, —NB631—C(O)—O—B632, —NB633-C(O)—NH—B634, —NB635-C(O)—NB636B637, —NHS(O2)—B638, —NB639S(O2)—B640, —S—B641, —S(O)—B642, —S(O2)—B643, —S(O2)NH—B644, —S(O2)NB645B646, —S(O2)O—B647, —P(O)(OB648)(OB649), —Si(B650)(B651)(B652), —C(NH)—NH2, —C(NB653)-NH2, —C(NH)—NHB654, —C(NH)—NB655B656, —C(NB657)-NHB658, —C(NB659)-NB660B661, —NH—C(O)—NH—O—B662, —NH—C(O)—NB663-O—B664, —NB665-C(O)—NB666-O—B667, —N(—C(O)—NH—O—B668)2, —N(—C(O)—NB669-O—B670)2, —N(—C(O)—NH—O—B671)(—C(O)—NB672-O—B673), —C(S)—B674, —C(S)—O—B675, —C(S)—NH—B676, —C(S)—NB677B678, —C(O)—NH—O—B679, —C(O)—NB680-O—B681, —C(S)—NH—O—B682, —C(S)—NB683-O—B684, —C(O)—NH—NH—B685, —C(O)—NH—NB686B687, —C(O)—NB688-NB689B690, —C(S)—NH—NH—B691, —C(S)—NH—NB692B693, —C(S)—NB694-NB695B696, —C(O)—C(O)—O—B697, —C(O)—C(O)—NH2, —C(O)—C(O)—NHB698, —C(O)—C(O)—NB699B700, —C(S)—C(O)—O—B701, —C(O)—C(S)—O—B702, —C(S)—C(S)—O—B703, —C(S)—C(O)—NH2, —C(S)—C(O)—NHB704, —C(S)—C(O)—NB705B706, —C(S)—C(S)—NH2, —C(S)—C(S)—NHB707, —C(S)—C(S)—NB708B709, —C(O)—C(S)—NH2, —C(O)—C(S)—NHB710, —C(O)—C(S)—NB711B712”;
        
            wherein B601, B602, B603, B604, B605, B606, B607, B608, B609, B610, B611, B612, B613, B614, B615, B616, B617, B618, B619, B620, B621, B622, B623, B624, B625, B626, B627, B628, B629, B630, B631, B632, B633, B634, B635, B636, B637, B638, B639, B640, B641, B642, B643, B644, B645, B646, B647, B648, B649, B650, B651, B652, B653, B654, B655, B656, B657, B658, B659, B660, B661, B662, B663, B664, B665, B666, B667, B668, B669, B670, B671, B672, B673, B674, B675, B676, B677, B678, B679, B680, B681, B682, B683, B684, B685, B686, B687, B688, B689, B690, B691, B692, B693, B694, B695, B696, B697, B698, B699, B700, B701, B702, B703, B704, B705, B706, B707, B708, B709, 8710, B711, B712 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively B607, B608 and/or B616, B617 and/or B629, B630 and/or B636, B637 and/or B645, B646 and/or B655, B656 and/or B660, B661 and/or B677, B678 and/or B686, B687 and/or B689, B690 and/or B692, B693 and/or B695, B696 and/or B699, B700 and/or B705, B706 and/or B708, B709 and/or B711, B712 and/or respectively together can also form “heterocyclyl”.
        
        
    
    


The object of the present invention has surprisingly been solved in one aspect by providing pyrido[2,3-b]pyrazine derivatives according to general formula (Ib)




wherein:

one of radicals R3, R4 independently is selected, or both of radicals R3, R4 independently from each other are selected from the group consisting of:

    (1) “—NR6R7”;

wherein radicals R6, R7 are independently from each other selected from the group consisting of:

(a) “hydrogen”;
    
        with the first proviso that radicals R6, R7 are not both hydrogen at the same time;
        with the second proviso that, if one of radicals R6, R7 independently is “hydrogen”, radical R5 is not selected from the group consisting of: “—NH-cycloalkyl, —NH-heterocyclyl, —NH-aryl, —NH-heteroaryl, halogen, —F, —Cl, —Br, —I, —NRaRb”, with Ra, Rb being independently selected from the group consisting of: “H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —NRcRd”, Rc, Rd in turn being independently selected from the group consisting of: “H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl”;

(b) “—C(Y1)NR8R9, —C(═NR10)-R11, —C(Y2)NR12-Y3-R13”;

        wherein Y1, Y2 are independently from each other selected from the group consisting of: “═O, ═S, ═NH, ═NR14”;
        wherein Y3 is independently selected from the group consisting of: “O, S”;
        wherein radicals R8, R9, R10, R11, R12, R13, R14 are independently from each other selected from the group consisting of:
        (I) “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHX1, —NX2X3, —NO2, —OH, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—X4, —C(O)O—X5, —C(O)NH—X6, —C(O)NX7X8, —O—X9, —O(—X10-O)a—H (a=1, 2, 3, 4, 5), —O(—X11-O)b—X12 (b=1, 2, 3, 4, 5), —OC(O)—X13, —OC(O)—O—X14, —OC(O)—NHX15, —O—C(O)—NX16X17, —OP(O)(OX18)(OX19), —OSi(X20)(X21)(X22), —OS(O2)—X23, —NHC(O)—NH2, —NHC(O)—X24, —NX25C(O)—X26, —NH—C(O)—O—X27, —NH—C(O)—NH—X28, —NH—C(O)—NX29X30, —NX31-C(O)—O—X32, —NX33-C(O)—NH—X34, —NX35-C(O)—NX36X37, —NHS(O2)—X38, —NX39S(O2)—X40, —S—X41, —S(O)—X42, —S(O2)—X43, —S(O2)NH—X44, —S(O2)NX45X46, —S(O2)O—X47, —P(O)(OX48)(OX49), —Si(X50)(X51)(X52), —C(NH)—NH2, —C(NX53)-NH2, —C(NH)—NHX54, —C(NH)—NX55X56, —C(NX57)-NHX58, —C(NX59)-NX60X61, —NH—C(O)—NH—O—X62, —NH—C(O)—NX63-O—X64, —NX65-C(O)—NX66-O—X67, —N(—C(O)—NH—O—X68)2, —N(—C(O)—NX69-O—X70)2, —N(—C(O)—NH—O—X71)(—C(O)—NX72-O—X73), —C(S)—X74, —C(S)—O—X75, —C(S)—NH—X76, —C(S)—NX77X78, —C(O)—NH—O—X79, —C(O)—NX80-O—X81, —C(S)—NH—O—X82, —C(S)—NX83-O—X84, —C(O)—NH—NH—X85, —C(O)—NH—NX86X87, —C(O)—NX88-NX89X90, —C(S)—NH—NH—X91, —C(S)—NH—NX92X93, —C(S)—NX94-NX95X96, —C(O)—C(O)—O—X97, —C(O)—C(O)—NH2, —C(O)—C(O)—NHX98, —C(O)—C(O)—NX99X100, —C(S)—C(O)—O—X101, —C(O)—C(S)—O—X102, —C(S)—C(S)—O—X103, —C(S)—C(O)—NH2, —C(S)—C(O)—NHX104, —C(S)—C(O)—NX105X106, —C(S)—C(S)—NH2, —C(S)—C(S)—NHX107, —C(S)—C(S)—NX108X109, —C(O)—C(S)—NH2, —C(O)—C(S)—NHX110, —C(O)—C(S)—NX111X112”;
        
            wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12, X13, X14, X15, X16, X17, X18, X19, X20, X21, X22, X23, X24, X25, X26, X27, X28, X29, X30, X31, X32, X33, X34, X35, X36, X37, X38, X39, X40, X41, X42, X43, X44, X45, X46, X47, X48, X49, X50, X51, X52, X53, X54, X55, X56, X57, X58, X59, X60, X61, X62, X63, X64, X65, X66, X67, X68, X69, X70, X71, X72, X73, X74, X75, X76, X77, X78, X79, X80, X81, X82, X83, X84, X85, X86, X87, X88, X89, X90, X91, X92, X93, X94, X95, X96, X97, X98, X99, X100, X101, X102, X103, X104, X105, X106, X107, X108, X109, X110, X111, X112 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively X7, X8 and/or X16, X17 and/or X29, X30 and/or X36, X37 and/or X45, X46 and/or X55, X56 and/or X60, X61 and/or X77, X78 and/or X86, X87 and/or X89, X90 and/or X92, X93 and/or X95, X96 and/or X99, X100 and/or X105, X106 and/or X108, X109 and/or X111, X112 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (I)—if not hydrogen—can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (i) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHX201, —NX202X203, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—X204, —C(O)O—X205, —C(O)NH—X206, —C(O)NX207X208, —O—X209, —O(—X210-O)c—H (c=1, 2, 3, 4, 5), —O(—X211-O)d—X212 (d=1, 2, 3, 4, 5), —OC(O)—X213, —OC(O)—O—X214, —OC(O)—NHX215, —O—C(O)—NX216X217, —OP(O)(OX218)(OX219), —OSi(X220)(X221)(X222), —OS(O2)—X223, —NHC(O)—NH2, —NHC(O)—X224, —NX225C(O)—X226, —NH—C(O)—O—X227, —NH—C(O)—NH—X228, —NH—C(O)—NX229X230, —NX231-C(O)—O—X232, —NX233-C(O)—NH—X234, —NX235-C(O)—NX236X237, —NHS(O2)—X238, —NX239S(O2)—X240, —S—X241, —S(O)—X242, —S(O2)—X243, —S(O2)NH—X244, —S(O2)NX245X246, —S(O2)O—X247, —P(O)(OX248)(OX249), —Si(X250)(X251)(X252), —C(NH)—NH2, —C(NX253)-NH2, —C(NH)—NHX254, —C(NH)—NX255X256, —C(NX257)-NHX258, —C(NX259)-NX260X261, —NH—C(O)—NH—O—X262, —NH—C(O)—NX263-O—X264, —NX265-C(O)—NX266-O—X267, —N(—C(O)—NH—O—X268)2, —N(—C(O)—NX269-O—X270)2, —N(—C(O)—NH—O —X271)(—C(O)—NX272-O—X273), —C(S)—X274, —C(S)—O—X275, —C(S)—NH—X276, —C(S)—NX277X278, —C(O)—NH—O—X279, —C(O)—NX280-O—X281, —C(S)—NH—O—X282, —C(S)—NX283-O—X284, —C(O)—NH—NH—X285, —C(O)—NH—NX286X287, —C(O)—NX288-NX289X290, —C(S)—NH—NH—X291, —C(S)—NH—NX292X293, —C(S)—NX294-NX295X296, —C(O)—C(O)—O—X297, —C(O)—C(O)—NH2, —C(O)—C(O)—NHX298, —C(O)—C(O)—NX299X300, —C(S)—C(O)—O—X301, —C(O)—C(S)—O—X302, —C(S)—C(S)—O—X303, —C(S)—C(O)—NH2, —C(S)—C(O)—NHX304, —C(S)—C(O)—NX305X306, —C(S)—C(S)—NH2, —C(S)—C(S)—NHX307, —C(S)—C(S)—NX308X309, —C(O)—C(S)—NH2, —C(O)—C(S)—NHX310, —C(O)—C(S)—NX311X312”;
        
            wherein X201, X202, X203, X204, X205, X206, X207, X208, X209, X210, X211, X212, X213, X214, X215, X216, X217, X218, X219, X220, X221, X222, X223, X224, X225, X226, X227, X228, X229, X230, X231, X232, X233, X234, X235, X236, X237, X238, X239, X240, X241, X242, X243, X244, X245, X246, X247, X248, X249, X250, X251, X252, X253, X254, X255, X256, X257, X258, X259, X260, X261, X262, X263, X264, X265, X266, X267, X268, X269, X270, X271, X272, X273, X274, X275, X276, X277, X278, X279, X280, X281, X282, X283, X284, X285, X286, X287, X288, X289, X290, X291, X292, X293, X294, X295, X296, X297, X298, X299, X300, X301, X302, X303, X304, X305, X306, X307, X308, X309, X310, X311, X312 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively X207, X208 and/or X216, X217 and/or X229, X230 and/or X236, X237 and/or X245, X246 and/or X255, X256 and/or X260, X261 and/or X277, X278 and/or X286, X287 and/or X289, X290 and/or X292, X293 and/or X295, X296 and/or X299, X300 and/or X305, X306 and/or X308, X309 and/or X311, X312 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (i) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (ii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHX401, —NX402X403, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—X404, —C(O)O—X405, —C(O)NH—X406, —C(O)NX407X408, —O—X409, —O(—X410-O)e—H (e=1, 2, 3, 4, 5), —O(—X411-O)f—X412 (f=1, 2, 3, 4, 5), —OC(O)—X413, —OC(O)—O—X414, —OC(O)—NHX415, —O—C(O)—NX416X417, —OP(O)(OX418)(OX419), —OSi(X420)(X421)(X422), —OS(O2)—X423, —NHC(O)—NH2, —NHC(O)—X424, —NX425C(O)—X426, —NH—C(O)—O—X427, —NH—C(O)—NH—X428, —NH—C(O)—NX429X430, —NX431-C(O)—O—X432, —NX433-C(O)—NH—X434, —NX435-C(O)—NX436X437, —NHS(O2)—X438, —NX439S(O2)—X440, —S—X441, —S(O)—X442, —S(O2)—X443, —S(O2)NH—X444, —S(O2)NX445X446, —S(O2)O—X447, —P(O)(OX448)(OX449), —Si(X450)(X451)(X452), —C(NH)—NH2, —C(NX453)-NH2, —C(NH)—NHX454, —C(NH)—NX455X456, —C(NX457)-NHX458, —C(NX459)-NX460X461, —NH—C(O)—NH—O—X462, —NH—C(O)—NX463-O—X464, —NX465-C(O)—NX466-O—X467, —N(—C(O)—NH—O—X468)2, —N(—C(O)—NX469-O—X470)2, —N(—C(O)—NH—O—X471)(—C(O)—NX472-O—X473), —C(S)—X474, —C(S)—O—X475, —C(S)—NH—X476, —C(S)—NX477X478, —C(O)—NH—O—X479, —C(O)—NX480-O—X481, —C(S)—NH—O—X482, —C(S)—NX483-O—X484, —C(O)—NH—NH—X485, —C(O)—NH—NX486X487, —C(O)—NX488-NX489X490, —C(S)—NH—NH—X491, —C(S)—NH—NX492X493, —C(S)—NX494-NX495X496, —C(O)—C(O)—O—X497, —C(O)—C(O)—NH2, —C(O)—C(O)—NHX498, —C(O)—C(O)—NX499X500, —C(S)—C(O)—O—X501, —C(O)—C(S)—O—X502, —C(S)—C(S)—O—X503, —C(S)—C(O)—NH2, —C(S)—C(O)—NHX504, —C(S)—C(O)—NX505X506, —C(S)—C(S)—NH2, —C(S)—C(S)—NHX507, —C(S)—C(S)—NX508X509, —C(O)—C(S)—NH2, —C(O)—C(S)—NHX510, —C(O)—C(S)—NX511X512”;
        
            wherein X401, X402, X403, X404, X405, X406, X407, X408, X409, X410, X411, X412, X413, X414, X415, X416, X417, X418, X419, X420, X421, X422, X423, X424, X425, X426, X427, X428, X429, X430, X431, X432, X433, X434, X435, X436, X437, X438, X439, X440, X441, X442, X443, X444, X445, X446, X447, X448, X449, X450, X451, X452, X453, X454, X455, X456, X457, X458, X459, X460, X461, X462, X463, X464, X465, X466, X467, X468, X469, X470, X471, X472, X473, X474, X475, X476, X477, X478, X479, X480, X481, X482, X483, X484, X485, X486, X487, X488, X489, X490, X491, X492, X493, X494, X495, X496, X497, X498, X499, X500, X501, X502, X503, X504, X505, X506, X507, X508, X509, X510, X511, X512 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively X407, X408 and/or X416, X417 and/or X429, X430 and/or X436, X437 and/or X445, X446 and/or X455, X456 and/or X460, X461 and/or X477, X478 and/or X486, X487 and/or X489, X490 and/or X492, X493 and/or X495, X496 and/or X499, X500 and/or X505, X506 and/or X508, X509 and/or X511, X512 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (ii) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (iii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHX601, —NX602X603, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—X604, —C(O)O—X605, —C(O)NH—X606, —C(O)NX607X608, —O—X609, —O(—X610-O)e—H (e=1, 2, 3, 4, 5), —O(—X611-O)1—X612 (f=1, 2, 3, 4, 5), —OC(O)—X613, —OC(O)—O—X614, —OC(O)—NHX615, —O—C(O)—NX616X617, —OP(O)(OX618)(OX619), —OSi(X620)(X621)(X622), —OS(O2)—X623, —NHC(O)—NH2, —NHC(O)—X624, —NX625C(O)—X626, —NH—C(O)—O—X627, —NH—C(O)—NH—X628, —NH—C(O)—NX629X630, —NX631-C(O)—O—X632, —NX633-C(O)—NH—X634, —NX635-C(O)—NX636X637, —NHS(O2)—X638, —NX639S(O2)—X640, —S—X641, —S(O)—X642, —S(O2)—X643, SO2)NH—X644, —S(O2)NX645X646, —S(O2)O—X647, —P(O)(OX648)(OX649), —Si(X650)(X651)(X652), —C(NH)—NH2, —C(NX653)-NH2, —C(NH)—NHX654, —C(NH)—NX655X656, —C(NX657)-NHX658, —C(NX659)-NX660X661, —NH—C(O)—NH—O—X662, —NH—C(O)—NX663-O—X664, —NX665-C(O)—NX666—O—X667, —N(—C(O)—NH—O—X668)2, —N(—C(O)—NX669-O—X670)2, —N(—C(O)—NH—O—X671)(—C(O)—NX672-O—X673), —C(S)—X674, —C(S)—O—X675, —C(S)—NH—X676, —C(S)—NX677X678, —C(O)—NH—O—X679, —C(O)—NX680-O—X681, —C(S)—NH—O—X682, —C(S)—NX683-O—X684, —C(O)—NH—NH—X685, —C(O)—NH—NX686X687, —C(O)—NX688-NX689X690, —C(S)—NH—NH—X691, —C(S)—NH—NX692X693, —C(S)—NX694-NX695X696, —C(O)—C(O)—O—X697, —C(O)—C(O)—NH2, —C(O)—C(O)—NHX698, —C(O)—C(O)—NX699X700, —C(S)—C(O)—O—X701, —C(O)—C(S)—O—X702, —C(S)—C(S)—O—X703, —C(S)—C(O)—NH2, —C(S)—C(O)—NHX704, —C(S)—C(O)—NX705X706, —C(S)—C(S)—NH2, —C(S)—C(S)—NHX707, —C(S)—C(S)—NX708X709, —C(O)—C(S)—NH2, —C(O)—C(S)—NHX710, —C(O)—C(S)—NX711X712”;
        
            wherein X601, X602, X603, X604, X605, X606, X607, X608, X609, X610, X611, X612, X613, X614, X615, X616, X617, X618, X619, X620, X621, X622, X623, X624, X625, X626, X627, X628, X629, X630, X631, X632, X633, X634, X635, X636, X637, X638, X639, X640, X641, X642, X643, X644, X645, X646, X647, X648, X649, X650, X651, X652, X653, X654, X655, X656, X657, X658, X659, X660, X661, X662, X663, X664, X665, X666, X667, X668, X669, X670, X671, X672, X673, X674, X675, X676, X677, X678, X679, X680, X681, X682, X683, X684, X685, X686, X687, X688, X689, X690, X691, X692, X693, X694, X695, X696, X697, X698, X699, X700, X701, X702, X703, X704, X705, X706, X707, X708, X709, X710, X711, X712 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively X607, X608 and/or X616, X617 and/or X629, X630 and/or X636, X637 and/or X645, X646 and/or X655, X656 and/or X660, X661 and/or X677, X678 and/or X686, X687 and/or X689, X690 and/or X692, X693 and/or X695, X696 and/or X699, X700 and/or X705, X706 and/or X708, X709 and/or X711, X712 and/or respectively together can also form “heterocyclyl”;
        
        
        with the first proviso that “—C(Y1)-NR8R9” is not selected from the group consisting of: “—C(O)—NRaRb”, with Ra, Rb independently from each other being selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl”
        with the second proviso that, if “—C(Y1)-NR8R9” independently is selected from the group consisting of: “—C(O)—N[C(O)—O-alkyl]2, —C(O)—N[C(O)-alkyl]2, —C(O)—N[S(O2)-alkyl]2, —C(O)—N[S(O2)-cycloalkyl]2, —C(O)—N[S(O2)—cycloalkylalkyl]2, —C(O)—N[S(O2)-aryl]2, —C(O)—N[S(O2)-heterocyclyl]2”, radicals R1, R2 independently from each other are not “phenyl”;
        with the third proviso that, if “—C(Y2)-NR12-Y3-R13” independently is selected from the group consisting of: “—C(O)—N[O-alkyl]2”, radicals R1, R2 independently from each other are not “phenyl”;

(c) “—C(O)—C(O)—R16”;

        wherein radical R16 is independently selected from the group consisting of:
        (II) “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHZ1, —NZ2Z3, —NO2, —OH, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—Z4, —C(O)O—Z5, —C(O)NH—Z6, —C(O)NZ7Z8, —O—Z9, —O(—Z10-O)a—H (a=1, 2, 3, 4, 5), —O(—Z11-O)b—Z12 (b=1, 2, 3, 4, 5), —OC(O)—Z13, —OC(O)—O—Z14, —OC(O)—NHZ15, —O—C(O)—NZ16Z17, —OP(O)(OZ18)(OZ19), —OSi(Z20)(Z21)(Z22), —OS(O2)—Z23, —NHC(O)—NH2, —NHC(O)—Z24, —NZ25C(O)—Z26, —NH—C(O)—O—Z27, —NH—C(O)—NH—Z28, —NH—C(O)—NZ29Z30, —NZ31-C(O)—O—Z32, —NZ33-C(O)—NH—Z34, —NZ35-C(O)—NZ36Z37, —NHS(O2)—Z38, —NZ39S(O2)—Z40, —S—Z41, —S(O)—Z42, —S(O2)—Z43, —S(O2)NH—Z44, —S(O2)NZ45Z46, —S(O2)O—Z47, —P(O)(OZ48)(OZ49), —Si(Z50)(Z51)(Z52), —C(NH)—NH2, —C(NZ53)-NH2, —C(NH)—NHZ54, —C(NH)—NZ55Z56, —C(NZ57)-NHZ58, —C(NZ59)-NZ60Z61, —NH—C(O)—NH—O—Z62, —NH—C(O)—NZ63-O—Z64, —NZ65—C(O)—NZ66-O—Z67, —N(—C(O)—NH—O—Z68)2, —N(—C(O)—NZ69-O—Z70)2, —N(—C(O)—NH—O—Z71)(—C(O)—NZ72-O—Z73), —C(S)—Z74, —C(S)—O—Z75, —C(S)—NH—Z76, —C(S)—NZ77Z78, —C(O)—NH—O—Z79, —C(O)—NZ80-O—Z81, —C(S)—NH—O—Z82, —C(S)—NZ83-O—Z84, —C(O)—NH—NH—Z85, —C(O)—NH—NZ86Z87, —C(O)—NZ88-NZ89Z90, —C(S)—NH—NH—Z91, —C(S)—NH—NZ92Z93, —C(S)—NZ94-NZ95Z96, —C(O)—C(O)—O—Z97, —C(O)—C(O)—NH2, —C(O)—C(O)—NHZ98, —C(O)—C(O)—NZ99Z100, —C(S)—C(O)—O—Z101, —C(O)—C(S)—O—Z102, —C(S)—C(S)—O—Z103, —C(S)—C(O)—NH2, —C(S)—C(O)—NHZ104, —C(S)—C(O)—NZ105Z106, —C(S)—C(S)—NH2, —C(S)—C(S)—NHZ107, —C(S)—C(S)—NZ108Z109, —C(O)—C(S)—NH2, —C(O)—C(S)—NHZ110, —C(O)—C(S)—NZ111Z112”;
        
            wherein Z1, Z2, Z3, Z4, Z5, Z6, Z7, Z8, Z9, Z10, Z11, Z12, Z13, Z14, Z15, Z16, Z17, Z18, Z19, Z20, Z21, Z22, Z23, Z24, Z25, Z26, Z27, Z28, Z29, Z30, Z31, Z32, Z33, Z34, Z35, Z36, Z37, Z38, Z39, Z40, Z41, Z42, Z43, Z44, Z45, Z46, Z47, Z48, Z49, Z50, Z51, Z52, Z53, Z54, Z55, Z56, Z57, Z58, Z59, Z60, Z61, Z62, Z63, Z64, Z65, Z66, Z67, Z68, Z69, Z70, Z71, Z72, Z73, Z74, Z75, Z76, Z77, Z78, Z79, Z80, Z81, Z82, Z83, Z84, Z85, Z86, Z87, Z88, Z89, Z90, Z91, Z92, Z93, Z94, Z95, Z96, Z97, Z98, Z99, Z100, Z101, Z102, Z103, Z104, Z105, Z106, Z107, Z108, Z109, Z110, Z111, Z112 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively Z7, Z8 and/or Z16, Z17 and/or Z29, Z30 and/or Z36, Z37 and/or Z45, Z46 and/or Z55, Z56 and/or Z60, Z61 and/or Z77, Z78 and/or Z86, Z87 and/or Z89, Z90 and/or Z92, Z93 and/or Z95, Z96 and/or Z99, Z100 and/or Z105, Z106 and/or Z108, Z109 and/or Z111, Z112 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (II)—if not hydrogen—can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (i) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclyalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHZ201, —NZ202Z203, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—Z204, —C(O)O—Z205, —C(O)NH—Z206, —C(O)NZ207Z208, —O—Z209, —O(—Z210-O), —H (c=1, 2, 3, 4, 5), —O(—Z211-O)d—Z212 (d=1, 2, 3, 4, 5), —OC(O)—Z213, —OC(O)—O—Z214, —OC(O)—NHZ215, —O—C(O)—NZ216Z217, —OP(O)(OZ218)(OZ219), —OSi(Z220)(Z221)(Z222), —OS(O2)—Z223, —NHC(O)—NH2, —NHC(O)—Z224, —NZ225C(O)—Z226, —NH—C(O)—O—Z227, —NH—C(O)—NH—Z228, —NH—C(O)—NZ229Z230, —NZ231-C(O)—O—Z232, —NZ233-C(O)—NH—Z234, —NZ235-C(O)—NZ236Z237, —NHS(O2)—Z238, —NZ239S(O2)—Z240, —S—Z241, —S(O)—Z242, —S(O2)—Z243, —S(O2)NH—Z244, —S(O2)NZ245Z246, —S(O2)O—Z247, —P(O)(OZ248)(OZ249), —Si(Z250)(Z251)(Z252), —C(NH)—NH2, —C(NZ253)-NH2, —C(NH)—NHZ254, —C(NH)—NZ255Z256, —C(NZ257)-NHZ258, —C(NZ259)-NZ260Z261, —NH—C(O)—NH—O—Z262, —NH—C(O)—NZ263-O—Z264, —NZ265-C(O)—NZ266-O—Z267, —N(—C(O)—NH—O—Z268)2, —N(—C(O)—NZ269-O—Z270)2, —N(—C(O)—NH—O—Z271)(—C(O)—NZ272-O—Z273), —C(S)—Z274, —C(S)—O—Z275, —C(S)—NH—Z276, —C(S)—NZ277Z278, —C(O)—NH—O—Z279, —C(O)—NZ280-O—Z281, —C(S)—NH—O—Z282, —C(S)—NZ283-O—Z284, —C(O)—NH—NH—Z285, —C(O)—NH—NZ286Z287, —C(O)—NZ288-NZ289Z290, —C(S)—NH—NH—Z291, —C(S)—NH—NZ292Z293, —C(S)—NZ294-NZ295Z296, —C(O)—C(O)—O—Z297, —C(O)—C(O)—NH2, —C(O)—C(O)—NHZ298, —C(O)—C(O)—NZ299Z300, —C(S)—C(O)—O—Z301, —C(O)—C(S)—O—Z302, —C(S)—C(S)—O—Z303, —C(S)—C(O)—NH2, —C(S)—C(O)—NHZ304, —C(S)—C(O)—NZ305Z306, —C(S)—C(S)—NH2, —C(S)—C(S)—NHZ307, —C(S)—C(S)—NZ308Z309, —C(O)—C(S)—NH2, —C(O)—C(S)—NHZ310, —C(O)—C(S)—NZ311Z312”;
        
            wherein Z201, Z202, Z203, Z204, Z205, Z206, Z207, Z208, Z209, Z210, Z211, Z212, Z213, Z214, Z215, Z216, Z217, Z218, Z219, Z220, Z221, Z222, Z223, Z224, Z225, Z226, Z227, Z228, Z229, Z230, Z231, Z232, Z233, Z234, Z235, Z236, Z237, Z238, Z239, Z240, Z241, Z242, Z243, Z244, Z245, Z246, Z247, Z248, Z249, Z250, Z251, Z252, Z253, Z254, Z255, Z256, Z257, Z258, Z259, Z260, Z261, Z262, Z263, Z264, Z265, Z266, Z267, Z268, Z269, Z270, Z271, Z272, Z273, Z274, Z275, Z276, Z277, Z278, Z279, Z280, Z281, Z282, Z283, Z284, Z285, Z286, Z287, Z288, Z289, Z290, Z291, Z292, Z293, Z294, Z295, Z296, Z297, Z298, Z299, Z300, Z301, Z302, Z303, Z304, Z305, Z306, Z307, Z308, Z309, Z310, Z311, Z312 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively Z207, Z208 and/or Z216, Z217 and/or Z229, Z230 and/or Z236, Z237 and/or Z245, Z246 and/or Z255, Z256 and/or Z260, Z261 and/or Z277, Z278 and/or Z286, Z287 and/or Z289, Z290 and/or Z292, Z293 and/or Z295, Z296 and/or Z299, Z300 and/or Z305, Z306 and/or Z308, Z309 and/or Z311, Z312 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (i) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (ii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHZ401, —NZ402Z403, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—Z404, —C(O)O—Z405, —C(O)NH—Z406, —C(O)NZ407Z408, —O—Z409, —O(—Z410-O)e—H (e=1, 2, 3, 4, 5), —O(—Z411-O)f—Z412 (f=1, 2, 3, 4, 5), —OC(O)—Z413, —O(O)—O—Z414, —OC(O)—NHZ415, —O—C(O)—NZ416Z417, —OP(O)(OZ418)(OZ419), —OSi(Z420)(Z421)(Z422), —OS(O2)—Z423, —NHC(O)—NH2, —NHC(O)—Z424, —NZ425C(O)—Z426, —NH—C(O)—O—Z427, —NH—C(O)—NH—Z428, —NH—C(O)—NZ429Z430, —NZ431-C(O)—O—Z432, —NZ433-C(O)—NH—Z434, —NZ435-C(O)—NZ436Z437, —NHS(O2)—Z438, —NZ439S(O2)—Z440, —S—Z441, —S(O)—Z442, —S(O2)—Z443, —S(O2)NH—Z444, —S(O2)NZ445Z446, —S(O2)O—Z447, —P(O)(OZ448)(OZ449), —Si(Z450)(Z451)(Z452), —C(NH)—NH2, —C(NZ453)-NH2, —C(NH)—NHZ454, —C(NH)—NZ455Z456, —C(NZ457)-NHZ458, —C(NZ459)-NZ460Z461, —NH—C(O)—NH—O—Z462, —NH—C(O)—NZ463-O—Z464, —NZ465-C(O)—NZ466-O—Z467, —N(—C(O)—NH—O—Z468)2, —N(—C(O)—NZ469-O—Z470)2, —N(—C(O)—NH—O—Z471)(—C(O)—NZ472-O—Z473), —C(S)—Z474, —C(S)—O—Z475, —C(S)—NH—Z476, —C(S)—NZ477Z478, —C(O)—NH—O—Z479, —C(O)—NZ480-O—Z481, —C(S)—NH—O—Z482, —C(S)—NZ483-O—Z484, —C(O)—NH—NH—Z485, —C(O)—NH—NZ486Z487, —C(O)—NZ488-NZ489Z490, —C(S)—NH—NH—Z491, —C(S)—NH—NZ492Z493, —C(S)—NZ494-NZ495Z496, —C(O)—C(O)—O—Z497, —C(O)—C(O)—NH2, —C(O)—C(O)—NHZ498, —C(O)—C(O)—NZ499Z500, —C(S)—C(O)—O—Z501, —C(O)—C(S)—O—Z502, —C(S)—C(S)—O—Z503, —C(S)—C(O)—NH2, —C(S)—C(O)—NHZ504, —C(S)—C(O)—NZ505Z506, —C(S)—C(S)—NH2, —C(S)—C(S)—NHZ507, —C(S)—C(S)—NZ508Z509, —C(O)—C(S)—NH2, —C(O)—C(S)—NHZ510, —C(O)—C(S)—NZ511Z512”;
        
            wherein Z401, Z402, Z403, Z404, Z405, Z406, Z407, Z408, Z409, Z410, Z411, Z412, Z413, Z414, Z415, Z416, Z417, Z418, Z419, Z420, Z421, Z422, Z423, Z424, Z425, Z426, Z427, Z428, Z429, Z430, Z431, Z432, Z433, Z434, Z435, Z436, Z437, Z438, Z439, Z440, Z441, Z442, Z443, Z444, Z445, Z446, Z447, Z448, Z449, Z450, Z451, Z452, Z453, Z454, Z455, Z456, Z457, Z458, Z459, Z460, Z461, Z462, Z463, Z464, Z465, Z466, Z467, Z468, Z469, Z470, Z471, Z472, Z473, Z474, Z475, Z476, Z477, Z478, Z479, Z480, Z481, Z482, Z483, Z484, Z485, Z486, Z487, Z488, Z489, Z490, Z491, Z492, Z493, Z494, Z495, Z496, Z497, Z498, Z499, Z500, Z501, Z502, Z503, Z504, Z505, Z506, Z507, Z508, Z509, Z510, Z511, Z512 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively Z407, Z408 and/or Z416, Z417 and/or Z429, Z430 and/or Z436, Z437 and/or Z445, Z446 and/or Z455, Z456 and/or Z460, Z461 and/or Z477, Z478 and/or Z486, Z487 and/or Z489, Z490 and/or Z492, Z493 and/or Z495, Z496 and/or Z499, Z500 and/or Z505, Z506 and/or Z508, Z509 and/or Z511, Z512 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (ii) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (iii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHZ601, —NZ602Z603, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—Z604, —C(O)O—Z605, —C(O)NH—Z606, —C(O)NZ607Z608, —O—Z609, —O(—Z610-O)e—H (e=1, 2, 3, 4, 5), —O(—Z611-O)f—Z612 (f=1, 2, 3, 4, 5), —OC(O)—Z613, —OC(O)—O—Z614, —OC(O)—NHZ615, —O—C(O)—NZ616Z617, —OP(O)(OZ618)(OZ619), —OSi(Z620)(Z621)(Z622), —OS(O2)—Z623, —NHC(O)—NH2, —NHC(O)—Z624, —NZ625C(O)—Z626, —NH—C(O)—O—Z627, —NH—C(O)—NH—Z628, —NH—C(O)—NZ629Z630, —NZ631-C(O)—O—Z632, —NZ633-C(O)—NH—Z634, —NZ635-C(O)—NZ636Z637, —NHS(O2)—Z638, —NZ639S(O2)—Z640, —S—Z641, —S(O)—Z642, —S(O2)—Z643, —S(O2)NH—Z644, —S(O2)NZ645Z646, —S(O2)O—Z647, —P(O)(OZ648)(OZ649), —Si(Z650)(Z651)(Z652), —C(NH)—NH2, —C(NZ653)-NH2, —C(NH)—NHZ654, —C(NH)—NZ655Z656, —C(NZ657)-NHZ658, —C(NZ659)-NZ660Z661, —NH—C(O)—NH—O—Z662, —NH—C(O)—NZ663-O—Z664, —NZ665—C(O)—NZ666—O—Z667, —N(—C(O)—NH—O—Z668)2, —N(—C(O)—NZ669-O—Z670)2, —N(—C(O)—NH—O—Z671)(—C(O)—NZ672-O—Z673), —C(S)—Z674, —C(S)—O—Z675, —C(S)—NH—Z676, —C(S)—NZ677Z678, —C(O)—NH—O—Z679, —C(O)—NZ680-O—Z681, —C(S)—NH—O—Z682, —C(S)—NZ683-O—Z684, —C(O)—NH—NH—Z685, —C(O)—NH—NZ686Z687, —C(O)—NZ688-NZ689Z690, —C(S)—NH—NH—Z691, —C(S)—NH—NZ692Z693, —C(S)—NZ694-NZ695Z696, —C(O)—C(O)—O—Z697, —C(O)—C(O)—NH2, —C(O)—C(O)—NHZ698, —C(O)—C(O)—NZ699Z700, —C(S)—C(O)—O—Z701, —C(O)—C(S)—O—Z702, —C(S)—C(S)—O—Z703, —C(S)—C(O)—NH2, —C(S)—C(O)—NHZ704, —C(S)—C(O)—NZ705Z706, —C(S)—C(S)—NH2, —C(S)—C(S)—NHZ707, —C(S)—C(S)—NZ708Z709, —C(O)—C(S)—NH2, —C(O)—C(S)—NHZ710, —C(O)—C(S)—NZ711Z712”;
        
            wherein Z601, Z602, Z603, Z604, Z605, Z606, Z607, Z608, Z609, Z610, Z611, Z612, Z613, Z614, Z615, Z616, Z617, Z618, Z619, Z620, Z621, Z622, Z623, Z624, Z625, Z626, Z627, Z628, Z629, Z630, Z631, Z632, Z633, Z634, Z635, Z636, Z637, Z638, Z639, Z640, Z641, Z642, Z643, Z644, Z645, Z646, Z647, Z648, Z649, Z650, Z651, Z652, Z653, Z654, Z655, Z656, Z657, Z658, Z659, Z660, Z661, Z662, Z663, Z664, Z665, Z666, Z667, Z668, Z669, Z670, Z671, Z672, Z673, Z674, Z675, Z676, Z677, Z678, Z679, Z680, Z681, Z682, Z683, Z684, Z685, Z686, Z687, Z688, Z689, Z690, Z691, Z692, Z693, Z694, Z695, Z696, Z697, Z698, Z699, Z700, Z701, Z702, Z703, Z704, Z705, Z706, Z707, Z708, Z709, Z710, Z711, Z712 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively Z607, Z608 and/or Z616, Z617 and/or Z629, Z630 and/or Z636, Z637 and/or Z645, Z646 and/or Z655, Z656 and/or Z660, Z661 and/or Z677, Z678 and/or Z686, Z687 and/or Z689, Z690 and/or Z692, Z693 and/or Z695, Z696 and/or Z699, Z700 and/or Z705, Z706 and/or Z708, Z709 and/or Z711, Z712 and/or respectively together can also form “heterocyclyl”;
        
        
        with the proviso that radical R16 is not “indol-yl”;

(d) “—S(O2)—R18”;

        wherein radical R18 is independently selected from the group consisting of:
        (III) “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHW1, —NW2W3, —NO2, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—W4, —C(O)O—W5, —C(O)NH—W6, —C(O)NW7W8, —O—W9, —O(—W10-O), —H (a=1, 2, 3, 4, 5), —O(—W11-O)b—W12 (b=1, 2, 3, 4, 5), —OC(O)—W13, —OC(O)—O—W14, —OC(O)—NHW15, —O—C(O)—NW16W17, —OP(O)(OW18)(OW19), —OSi(W20)(W21)(W22), —OS(O2)—W23, —NHC(O)—NH2, —NHC(O)—W24, —NW25C(O)—W26, —NH—C(O)—O—W27, —NH—C(O)—NH—W28, —NH—C(O)—NW29W30, —NW31-C(O)—O—W32, —NW33-C(O)—NH—W34, —NW35-C(O)—NW36W37, —NHS(O2)—W38, —NW39S(O2)—W40, —S—W41, —S(O)—W42, —S(O2)—W43, —S(O2)NH—W44, —S(O2)NW45W46, —S(O2)O—W47, —P(O)(OW48)(OW49), —Si(W50)(W51)(W52), —C(NH)—NH2, —C(NW53)-NH2, —C(NH)—NHW54, —C(NH)—NW55W56, —C(NW57)-NHW58, —C(NW59)-NW60W61, —NH—C(O)—NH—O—W62, —NH—C(O)—NW63-O—W64, —NW65-C(O)—NW66-O—W67, —N(—C(O)—NH—O—W68)2, —N(—C(O)—NW69-O—W70)2, —N(—C(O)—NH—O—W71)(—C(O)—NW72-O—W73), —C(S)—W74, —C(S)—O—W75, —C(S)—NH—W76, —C(S)—NW77W78, —C(O)—NH—O—W79, —C(O)—NW80-O—W81, —C(S)—NH—O—W82, —C(S)—NW83-O—W84, —C(O)—NH—NH—W85, —C(O)—NH—NW86W87, —C(O)—NW88-NW89W90, —C(S)—NH—NH—W91, —C(S)—NH—NW92W93, —C(S)—NW94-NW95W96, —C(O)—C(O)—O—W97, —C(O)—C(O)—NH2, —C(O)—C(O)—NHW98, —C(O)—C(O)—NW99W100, —C(S)—C(O)—O—W101, —C(O)—C(S)—O—W102, —C(S)—C(S)—O—W103, —C(S)—C(O)—NH2, —C(S)—C(O)—NHW104, —C(S)—C(O)—NW105W106, —C(S)—C(S)—NH2, —C(S)—C(S)—NHW107, —C(S)—C(S)—NW108W109, —C(O)—C(S)—NH2, —C(O)—C(S)—NHW110, —C(O)—C(S)—NW111W112”;
        
            wherein W1, W2, W3, W4, W5, W6, W7, W8, W9, W10, W11, W12, W13, W14, W15, W16, W17, W18, W19, W20, W21, W22, W23, W24, W25, W26, W27, W28, W29, W30, W31, W32, W33, W34, W35, W36, W37, W38, W39, W40, W41, W42, W43, W44, W45, W46, W47, W48, W49, W50, W51, W52, W53, W54, W55, W56, W57, W58, W59, W60, W61, W62, W63, W64, W65, W66, W67, W68, W69, W70, W71, W72, W73, W74, W75, W76, W77, W78, W79, W80, W81, W82, W83, W84, W85, W86, W87, W88, W89, W90, W91, W92, W93, W94, W95, W96, W97, W98, W99, W100, W101, W102, W103, W104, W105, W106, W107, W108, W109, W110, W111, W112 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively W7, W8 and/or W16, W17 and/or W29, W30 and/or W36, W37 and/or W45, W46 and/or W55, W56 and/or W60, W61 and/or W77, W78 and/or W86, W87 and/or W89, W90 and/or W92, W93 and/or W95, W96 and/or W99, W100 and/or W105, W106 and/or W108, W109 and/or W111, W112 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (III) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (i) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHW201, —NW202W203, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—W204, —C(O)O—W205, —C(O)NH—W206, —C(O)NW207W208, —O—W209, —O(—W210-O)c—H (c=1, 2, 3, 4, 5), —O(—W211-O)d—W212 (d=1, 2, 3, 4, 5), —OC(O)—W213, —OC(O)—O—W214, —OC(O)—NHW215, —O—C(O)—NW216W217, —OP(O)(OW218)(OW219), —OSi(W220)(W221)(W222), —OS(O2)—W223, —NHC(O)—NH2, —NHC(O)—W224, —NW225C(O)—W226, —NH—C(O)—O—W227, —NH—C(O)—NH—W228, —NH—C(O)—NW229W230, —NW231-C(O)—O—W232, —NW233-C(O)—NH—W234, —NW235-C(O)—NW236W237, —NHS(O2)—W238, —NW239S(O2)—W240, —S—W241, —S(O)—W242, —S(O2)—W243, —S(O2)NH—W244, —S(O2)NW245W246, —S(O2)O—W247, —P(O)(OW248)(OW249), —Si(W250)(W251)(W252), —C(NH)—NH2, —C(NW253)-NH2, —C(NH)—NHW254, —C(NH)—NW255W256, —C(NW257)-NHW258, —C(NW259)-NW260W261, —NH—C(O)—NH—O—W262, —NH—C(O)—NW263-O—W264, —NW265-C(O)—NW266-O—W267, —N(—C(O)—NH—O—W268)2, —N(—C(O)—NW269-O—W270)2, —N(—C(O)—NH—O—W271)(—C(O)—NW272-O—W273), —C(S)—W274, —C(S)—O—W275, —C(S)—NH—W276, —C(S)—NW277W278, —C(O)—NH—O—W279, —C(O)—NW280-O—W281, —C(S)—NH—O—W282, —C(S)—NW283-O—W284, —C(O)—NH—NH—W285, —C(O)—NH—NW286W287, —C(O)—NW288-NW289W290, —C(S)—NH—NH—W291, —C(S)—NH—NW292W293, —C(S)—NW294-NW295W296, —C(O)—C(O)—O—W297, —C(O)—C(O)—NH2, —C(O)—C(O)—NHW298, —C(O)—C(O)—NW299W300, —C(S)—C(O)—O—W301, —C(O)—C(S)—O—W302, —C(S)—C(S)—O—W303, —C(S)—C(O)—NH2, —C(S)—C(O)—NHW304, —C(S)—C(O)—NW305W306, —C(S)—C(S)—NH2, —C(S)—C(S)—NHW307, —C(S)—C(S)—NW308W309, —C(O)—C(S)—NH2, —C(O)—C(S)—NHW310, —C(O)—C(S)—NW311W312”;
        
            wherein W201, W202, W203, W204, W205, W206, W207, W208, W209, W210, W211, W212, W213, W214, W215, W216, W217, W218, W219, W220, W221, W222, W223, W224, W225, W226, W227, W228, W229, W230, W231, W232, W233, W234, W235, W236, W237, W238, W239, W240, W241, W242, W243, W244, W245, W246, W247, W248, W249, W250, W251, W252, W253, W254, W255, W256, W257, W258, W259, W260, W261, W262, W263, W264, W265, W266, W267, W268, W269, W270, W271, W272, W273, W274, W275, W276, W277, W278, W279, W280, W281, W282, W283, W284, W285, W286, W287, W288, W289, W290, W291, W292, W293, W294, W295, W296, W297, W298, W299, W300, W301, W302, W303, W304, W305, W306, W307, W308, W309, W310, W311, W312 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively W207, W208 and/or W216, W217 and/or W229, W230 and/or W236, W237 and/or W245, W246 and/or W255, W256 and/or W260, W261 and/or W277, W278 and/or W286, W287 and/or W289, W290 and/or W292, W293 and/or W295, W296 and/or W299, W300 and/or W305, W306 and/or W308, W309 and/or W311, W312 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (i) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (ii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHW401, —NW402W403, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—W404, —C(O)O—W405, —C(O)NH—W406, —C(O)NW407W408, —O—W409, —O(—W410-O)e—H (e=1, 2, 3, 4, 5), —O(—W411-O)f—W412 (f=1, 2, 3, 4, 5), —OC(O)—W413, —OC(O)—O—W414, —OC(O)—NHW415, —O—C(O)—NW416W417, —OP(O)(OW418)(OW419), —OSi(W420)(W421)(W422), —OS(O2)—W423, —NHC(O)—NH2, —NHC(O)—W424, —NW425C(O)—W426, —NH—C(O)—O—W427, —NH—C(O)—NH—W428, —NH—C(O)—NW429W430, —NW431-C(O)—O—W432, —NW433-C(O)—NH—W434, —NW435-C(O)—NW436W437, —NHS(O2)—W438, —NW439S(O2)—W440, —S—W441, —S(O)—W442, —S(O2)—W443, —S(O2)NH—W444, —S(O2)NW445W446, —S(O2)O—W447, —P(O)(OW448)(OW449), —Si(W450)(W451)(W452), —C(NH)—NH2, —C(NW453)-NH2, —C(NH)—NHW454, —C(NH)—NW455W456, —C(NW457)-NHW458, —C(NW459)-NW460W461, —NH—C(O)—NH—O—W462, —NH—C(O)—NW463-O—W464, —NW465—C(O)—NW466—O—W467, —N(—C(O)—NH—O—W468)2, —N(—C(O)—NW469-O—W470)2, —N(—C(O)—NH—O—W471)(—C(O)—NW472-O—W473), —C(S)—W474, —C(S)—O—W475, —C(S)—NH—W476, —C(S)—NW477W478, —C(O)—NH—O—W479, —C(O)—NW480-O—W481, —C(S)—NH—O—W482, —C(S)—NW483-O—W484, —C(O)—NH—NH—W485, —C(O)—NH—NW486W487, —C(O)—NW488-NW489W490, —C(S)—NH—NH—W491, —C(S)—NH—NW492W493, —C(S)—NW494-NW495W496, —C(O)—C(O)—O—W497, —C(O)—C(O)—NH2, —C(O)—C(O)—NHW498, —C(O)—C(O)—NW499W500, —C(S)—C(O)—O—W501, —C(O)—C(S)—O—W502, —C(S)—C(S)—O—W503, —C(S)—C(O)—NH2, —C(S)—C(O)—NHW504, —C(S)—C(O)—NW505W506, —C(S)—C(S)—NH2, —C(S)—C(S)—NHW507, —C(S)—C(S)—NW508W509, —C(O)—C(S)—NH2, —C(O)—C(S)—NHW510, —C(O)—C(S)—NW511W512”;
        
            wherein W401, W402, W403, W404, W405, W406, W407, W408, W409, W410, W411, W412, W413, W414, W415, W416, W417, W418, W419, W420, W421, W422, W423, W424, W425, W426, W427, W428, W429, W430, W431, W432, W433, W434, W435, W436, W437, W438, W439, W440, W441, W442, W443, W444, W445, W446, W447, W448, W449, W450, W451, W452, W453, W454, W455, W456, W457, W458, W459, W460, W461, W462, W463, W464, W465, W466, W467, W468, W469, W470, W471, W472, W473, W474, W475, W476, W477, W478, W479, W480, W481, W482, W483, W484, W485, W486, W487, W488, W489, W490, W491, W492, W493, W494, W495, W496, W497, W498, W499, W500, W501, W502, W503, W504, W505, W506, W507, W508, W509, W510, W511, W512 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively W407, W408 and/or W416, W417 and/or W429, W430 and/or W436, W437 and/or W445, W446 and/or W455, W456 and/or W460, W461 and/or W477, W478 and/or W486, W487 and/or W489, W490 and/or W492, W493 and/or W495, W496 and/or W499, W500 and/or W505, W506 and/or W508, W509 and/or W511, W512 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (ii) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (iii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHW601, —NW602W603, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—W604, —C(O)O—W605, —C(O)NH—W606, —C(O)NW607W608, —O—W609, —O(—W610-O)e—H (e=1, 2, 3, 4, 5), —O(—W611-O)f—W612 (f=1, 2, 3, 4, 5), —OC(O)—W613, —OC(O)—O—W614, —OC(O)—NHW615, —O—C(O)—NW616W617, —OP(O)(OW618)(OW619), —OSi(W620)(W621)(W622), —OS(O2)—W623, —NHC(O)—NH2, —NHC(O)—W624, —NW625C(O)—W626, —NH—C(O)—O—W627, —NH—C(O)—NH—W628, —NH—C(O)—NW629W630, —NW631-C(O)—O—W632, —NW633-C(O)—NH—W634, —NW635-C(O)—NW636W637, —NHS(O2)—W638, —NW639S(O2)—W640, —S—W641, —S(O)—W642, —S(O2)—W643, —S(O2)NH—W644, —S(O2)NW645W646, —S(O2)O—W647, —P(O)(OW648)(OW649), —Si(W650)(W651)(W652), —C(NH)—NH2, —C(NW653)-NH2, —C(NH)—NHW654, —C(NH)—NW655W656, —C(NW657)-NHW658, —C(NW659)-NW660W661, —NH—C(O)—NH—O—W662, —NH—C(O)—NW663-O—W664, —NW665-C(O)—NW666-O—W667, —N(—C(O)—NH—O—W668)2, —N(—C(O)—NW669-O—W670)2, —N(—C(O)—NH—O—W671)(—C(O)—NW672-O—W673), —C(S)—W674, —C(S)—O—W675, —C(S)—NH—W676, —C(S)—NW677W678, —C(O)—NH—O—W679, —C(O)—NW680-O—W681, —C(S)—NH—O—W682, —C(S)—NW683-O—W684, —C(O)—NH—NH—W685, —C(O)—NH—NW686W687, —C(O)—NW688-NW689W690, —C(S)—NH—NH—W691, —C(S)—NH—NW692W693, —C(S)—NW694-NW695W696, —C(O)—O—W697, —C(O)—C(O)—NH2, —C(O)—C(O)—NHW698, —C(O)—C(O)—NW699W700, —C(S)—C(O)—O—W701, —C(O)—C(S)—O—W702, —C(S)—C(S)—O—W703, —C(S)—C(O)—NH2, —C(S)—C(O)—NHW704, —C(S)—C(O)—NW705W706, —C(S)—C(S)—NH2, —C(S)—C(S)—NHW707, —C(S)—C(S)—NW708W709, —C(O)—C(S)—NH2, —C(O)—C(S)—NHW710, —C(O)—C(S)—NW711W712”;
        
            wherein W601, W602, W603, W604, W605, W606, W607, W608, W609, W610, W611, W612, W613, W614, W615, W616, W617, W618, W619, W620, W621, W622, W623, W624, W625, W626, W627, W628, W629, W630, W631, W632, W633, W634, W635, W636, W637, W638, W639, W640, W641, W642, W643, W644, W645, W646, W647, W648, W649, W650, W651, W652, W653, W654, W655, W656, W657, W658, W659, W660, W661, W662, W663, W664, W665, W666, W667, W668, W669, W670, W671, W672, W673, W674, W675, W676, W677, W678, W679, W680, W681, W682, W683, W684, W685, W686, W687, W688, W689, W690, W691, W692, W693, W694, W695, W696, W697, W698, W699, W700, W701, W702, W703, W704, W705, W706, W707, W708, W709, W710, W711, W712 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively W607, W608 and/or W616, W617 and/or W629, W630 and/or W636, W637 and/or W645, W646 and/or W655, W656 and/or W660, W661 and/or W677, W678 and/or W686, W687 and/or W689, W690 and/or W692, W693 and/or W695, W696 and/or W699, W700 and/or W705, W706 and/or W708, W709 and/or W711, W712 and/or respectively together can also form “heterocyclyl”;
        
        
        with the first proviso that radical R18 is not selected from the group consisting of: “−O-alkyl, —O—(C9-C30)alkyl, —O-aryl, —O-arylalkyl, —O-heteroaryl, —O-heteroarylalkyl, —O-cycloalkyl, —O-cycloalkylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl”;
        with the second proviso that, if radical R18 independently is selected from the group consisting of: “—NRaRb”, with Ra, Rb independently from each other being selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl”, radical R1 is not selected from the group consisting of: “heterocyclylalkyl being substituted with ═O, where heterocyclyl is 5-membered; alkyl being substituted with heterocyclyl, where heterocyclyl is 5-membered and substituted with ═O”;

and one of radicals R3, R4 or neither of radicals R3, R4 independently is selected from the group consisting of:

    
    
    (2) “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHA1, —NA2A3, —NO2, —OH, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)-A4, —C(O)O-A5, —C(O)NH-A6, —C(O)NA7A8, —O-A9, —O(-A10-O)a—H (a=1, 2, 3, 4, 5), —O(-A11-O)b-A12 (b=1, 2, 3, 4, 5), —OC(O)-A13, —OC(O)—O-A14, —OC(O)—NHA15, —O—C(O)—NA16A17, —OP(O)(OA18)(OA19), —OSi(A20)(A21)(A22), —OS(O2)-A23, —NHC(O)—NH2, —NHC(O)-A24, —NA25C(O)-A26, —NH—C(O)—O-A27, —NH—C(O)—NH-A28, —NH—C(O)—NA29A30, —NA31-C(O)—O-A32, —NA33-C(O)—NH-A34, —NA35-C(O)—NA36A37, —NHS(O2)-A38, —NA39S(O2)-A40, —S-A41, —S(O)-A42, —S(O2)— A43, —S(O2)NH-A44, —S(O2)NA45A46, —S(O2)O-A47, —P(O)(OA48)(OA49), —Si(A50)(A51)(A52), —C(NH)—NH2, —C(NA53)-NH2, —C(NH)—NHA54, —C(NH)—NA55A56, —C(NA57)-NHA58, —C(NA59)-NA60A61, —NH—C(O)—NH—O-A62, —NH—C(O)—NA63-O-A64, —NA65-C(O)—NA66-O-A67, —N(—C(O)—NH—O-A68)2, —N(—C(O)—NA69-O-A70)2, —N(—C(O)—NH—O-A71)(—C(O)—NA72-O-A73), —C(S)-A74, —C(S)—O-A75, —C(S)—NH-A76, —C(S)—NA77A78, —C(O)—NH—O-A79, —C(O)—NA80-O-A81, —C(S)—NH—O-A82, —C(S)—NA83-O-A84, —C(O)—NH—NH-A85, —C(O)—NH—NA86A87, —C(O)—NA88-NA89A90, —C(S)—NH—NH-A91, —C(S)—NH—NA92A93, —C(S)—NA94-NA95A96, —C(O)—C(O)—O-A97, —C(O)—C(O)—NH2, —C(O)—C(O)—NHA98, —C(O)—C(O)—NA99A100, —C(S)—C(O)—O-A101, —C(O)—C(S)—O-A102, —C(S)—C(S)—O-A103, —C(S)—C(O)—NH2, —C(S)—C(O)—NHA104, —C(S)—C(O)—NA105A106, —C(S)—C(S)—NH2, —C(S)—C(S)—NHA107, —C(S)—C(S)—NA108A109, —C(O)—C(S)—NH2, —C(O)—C(S)—NHA110, —C(O)—C(S)—NA111A112”;
    
        wherein A1, A2, A3, A4, A5, A6, A7, A8, A9, A10, A11, A12, A13, A14, A15, A16, A17, A18, A19, A20, A21, A22, A23, A24, A25, A26, A27, A28, A29, A30, A31, A32, A33, A34, A35, A36, A37, A38, A39, A40, A41, A42, A43, A44, A45, A46, A47, A48, A49, A50, A51, A52, A53, A54, A55, A56, A57, A58, A59, A60, A61, A62, A63, A64, A65, A66, A67, A68, A69, A70, A71, A72, A73, A74, A75, A76, A77, A78, A79, A80, A81, A82, A83, A84, A85, A86, A87, A88, A89, A90, A91, A92, A93, A94, A95, A96, A97, A98, A99, A100, A101, A102, A103, A104, A105, A106, A107, A108, A109, A110, A111, A112 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively A7, A8 and/or A16, A17 and/or A29, A30 and/or A36, A37 and/or A45, A46 and/or A55, A56 and/or A60, A61 and/or A77, A78 and/or A86, A87 and/or A89, A90 and/or A92, A93 and/or A95, A96 and/or A99, A100 and/or A105, A106 and/or A108, A109 and/or A111, A112 and/or respectively together can also form “heterocyclyl”;
        wherein optionally above substituents of substituents group (2)—if not hydrogenn—can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        (i) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHA201, —NA202A203, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)-A204, —C(O)O-A205, —C(O)NH-A206, —C(O)NA207A208, —O-A209, —O(-A210-O), —H (c=1, 2, 3, 4, 5), —O(-A211-O)d-A212 (d=1, 2, 3, 4, 5), —OC(O)-A213, —OC(O)—O-A214, —OC(O)—NHA215, —O—C(O)—NA216A217, —OP(O)(OA218)(OA219), —OSi (A220)(A221)(A222), —OS(O2)— A223, —NHC(O)—NH2, —NHC(O)-A224, —NA225C(O)-A226, —NH—C(O)—O-A227, —NH—C(O)—NH-A228, —NH—C(O)—NA229A230, —NA231-C(O)—O-A232, —NA233-C(O)—NH-A234, —NA235-C(O)—NA236A237, —NHS(O2)— A238, —NA239S(O2)-A240, —S-A241, —S(O)-A242, —S(O2)-A243, —S(O2)NH-A244, —S(O2)NA245A246, —S(O2)O-A247, —P(O)(OA248)(OA249), —Si(A250)(A251)(A252), —C(NH)—NH2, —C(NA253)-NH2, —C(NH)—NHA254, —C(NH)—NA255A256, —C(NA257)-NHA258, —C(NA259)-NA260A261, —NH—C(O)—NH—O-A262, —NH—C(O)—NA263-O-A264, —NA265-C(O)—NA266-O-A267, —N(—C(O)—NH—O-A268)2, —N(—C(O)—NA269-O-A270)2, —N(—C(O)—NH—O-A271)(—C(O)—NA272-O-A273), —C(S)-A274, —C(S)—O-A275, —C(S)—NH-A276, —C(S)—NA277A278, —C(O)—NH—O-A279, —C(O)—NA280-O-A281, —C(S)—NH—O-A282, —C(S)—NA283-O-A284, —C(O)—NH—NH-A285, —C(O)—NH—NA286A287, —C(O)—NA288-NA289A290, —C(S)—NH—NH-A291, —C(S)—NH—NA292A293, —C(S)—NA294-NA295A296, —C(O)—C(O)—O-A297, —C(O)—C(O)—NH2, —C(O)—C(O)—NHA298, —C(O)—C(O)—NA299A300, —C(S)—C(O)—O-A301, —C(O)—C(S)—O-A302, —C(S)—C(S)—O-A303, —C(S)—C(O)—NH2, —C(S)—C(O)—NHA304, —C(S)—C(O)—NA305A306, —C(S)—C(S)—NH2, —C(S)—C(S)—NHA307, —C(S)—C(S)—NA308A309, —C(O)—C(S)—NH2, —C(O)—C(S)—NHA310, —C(O)—C(S)—NA311A312”;
        
            wherein A201, A202, A203, A204, A205, A206, A207, A208, A209, A210, A211, A212, A213, A214, A215, A216, A217, A218, A219, A220, A221, A222, A223, A224, A225, A226, A227, A228, A229, A230, A231, A232, A233, A234, A235, A236, A237, A238, A239, A240, A241, A242, A243, A244, A245, A246, A247, A248, A249, A250, A251, A252, A253, A254, A255, A256, A257, A258, A259, A260, A261, A262, A263, A264, A265, A266, A267, A268, A269, A270, A271, A272, A273, A274, A275, A276, A277, A278, A279, A280, A281, A282, A283, A284, A285, A286, A287, A288, A289, A290, A291, A292, A293, A294, A295, A296, A297, A298, A299, A300, A301, A302, A303, A304, A305, A306, A307, A308, A309, A310, A311, A312 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively A207, A208 and/or A216, A217 and/or A229, A230 and/or A236, A237 and/or A245, A246 and/or A255, A256 and/or A260, A261 and/or A277, A278 and/or A286, A287 and/or A289, A290 and/or A292, A293 and/or A295, A296 and/or A299, A300 and/or A305, A306 and/or A308, A309 and/or A311, A312 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (i) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (ii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHA401, —NA402A403, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)-A404, —C(O)O-A405, —C(O)NH-A406, —C(O)NA407A408, —O-A409, —O(-A410-O)e—H (e=1, 2, 3, 4, 5), —O(-A411-O)f-A412 (f=1, 2, 3, 4, 5), —OC(O)-A413, —OC(O)—O-A414, —OC(O)—NHA415, —O—C(O)—NA416A417, —OP(O)(OA418)(OA419), —OSi(A420)(A421)(A422), —OS(O2)-A423, —NHC(O)—NH2, —NHC(O)-A424, —NA425C(O)-A426, —NH—C(O)—O-A427, —NH—C(O)—NH-A428, —NH—C(O)—NA429A430, —NA431-C(O)—O-A432, —NA433-C(O)—NH-A434, —NA435-C(O)—NA436A437, —NHS(O2)-A438, —NA439S(O2)— A440, —S-A441, —S(O)-A442, —S(O2)-A443, —S(O2)NH-A444, —S(O2)NA445A446, —S(O2)O-A447, —P(O)(OA448)(OA449), —Si(A450)(A451)(A452), —C(NH)—NH2, —C(NA453)-NH2, —C(NH)—NHA454, —C(NH)—NA455A456, —C(NA457)-NHA458, —C(NA459)-NA460A461, —NH—C(O)—NH—O-A462, —NH—C(O)—NA463-O-A464, —NA465-C(O)—NA466-O-A467, —N(—C(O)—NH—O-A468)2, —N(—C(O)—NA469-O-A470)2, —N(—C(O)—NH—O-A471)(—C(O)—NA472-O-A473), —C(S)-A474, —C(S)—O-A475, —C(S)—NH-A476, —C(S)—NA477A478, —C(O)—NH—O-A479, —C(O)—NA480-O-A481, —C(S)—NH—O-A482, —C(S)—NA483-O-A484, —C(O)—NH—NH-A485, —C(O)—NH—NA486A487, —C(O)—NA488-NA489A490, —C(S)—NH—NH-A491, —C(S)—NH—NA492A493, —C(S)—NA494-NA495A496, —C(O)—C(O)—O-A497, —C(O)—C(O)—NH2, —C(O)—C(O)—NHA498, —C(O)—C(O)—NA499A500, —C(S)—C(O)—O-A501, —C(O)—C(S)—O-A502, —C(S)—C(S)—O-A503, —C(S)—C(O)—NH2, —C(S)—C(O)—NHA504, —C(S)—C(O)—NA505A506, —C(S)—C(S)—NH2, —C(S)—C(S)—NHA507, —C(S)—C(S)—NA508A509, —C(O)—C(S)—NH2, —C(O)—C(S)—NHA510, —C(O)—C(S)—NA511A512”;
        
            wherein A401, A402, A403, A404, A405, A406, A407, A408, A409, A410, A411, A412, A413, A414, A415, A416, A417, A418, A419, A420, A421, A422, A423, A424, A425, A426, A427, A428, A429, A430, A431, A432, A433, A434, A435, A436, A437, A438, A439, A440, A441, A442, A443, A444, A445, A446, A447, A448, A449, A450, A451, A452, A453, A454, A455, A456, A457, A458, A459, A460, A461, A462, A463, A464, A465, A466, A467, A468, A469, A470, A471, A472, A473, A474, A475, A476, A477, A478, A479, A480, A481, A482, A483, A484, A485, A486, A487, A488, A489, A490, A491, A492, A493, A494, A495, A496, A497, A498, A499, A500, A501, A502, A503, A504, A505, A506, A507, A508, A509, A510, A511, A512 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively A407, A408 and/or A416, A417 and/or A429, A430 and/or A436, A437 and/or A445, A446 and/or A455, A456 and/or A460, A461 and/or A477, A478 and/or A486, A487 and/or A489, A490 and/or A492, A493 and/or A495, A496 and/or A499, A500 and/or A505, A506 and/or A508, A509 and/or A511, A512 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (ii) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (iii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHA601, —NA602A603, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)-A604, —C(O)O-A605, —C(O)NH-A606, —C(O)NA607A608, —O-A609, —O(-A610-O), —H (e=1, 2, 3, 4, 5), —O(-A611-O)f-A612 (f=1, 2, 3, 4, 5), —OC(O)-A613, —OC(O)—O-A614, —OC(O)—NHA615, —O—C(O)—NA616A617, —OP(O)(OA618)(OA619), —OSi(A620)(A621)(A622), —OS(O2)-A623, —NHC(O)—NH2, —NHC(O)-A624, —NA625C(O)-A626, —NH—C(O)—O-A627, —NH—C(O)—NH-A628, —NH—C(O)—NA629A630, —NA631—C(O)—O-A632, —NA633-C(O)—NH-A634, —NA635—C(O)—NA636A637, —NHS(O2)-A638, —NA639S(O2)-A640, —S-A641, —S(O)-A642, —S(O2)-A643, —S(O2)NH-A644, —S(O2)NA645A646, —S(O2)O-A647, —P(O)(OA648)(OA649), —Si(A650)(A651)(A652), —C(NH)—NH2, —C(NA653)-NH2, —C(NH)—NHA654, —C(NH)—NA655A656, —C(NA657)-NHA658, —C(NA659)-NA660A661, —NH—C(O)—NH—O-A662, —NH—C(O)—NA663-O-A664, —NA665-C(O)—NA666-O-A667, —N(—C(O)—NH—O-A668)2, —N(—C(O)—NA669-O-A670)2, —N(—C(O)—NH—O-A671)(—C(O)—NA672-O-A673), —C(S)-A674, —C(S)—O-A675, —C(S)—NH-A676, —C(S)—NA677A678, —C(O)—NH—O-A679, —C(O)—NA680-O-A681, —C(S)—NH—O-A682, —C(S)—NA683-O-A684, —C(O)—NH—NH-A685, —C(O)—NH—NA686A687, —C(O)—NA688-NA689A690, —C(S)—NH—NH-A691, —C(S)—NH—NA692A693, —C(S)—NA694-NA695A696, —C(O)—C(O)—O-A697, —C(O)—C(O)—NH2, —C(O)—C(O)—NHA698, —C(O)—C(O)—NA699A700, —C(S)—C(O)—O-A701, —C(O)—C(S)—O-A702, —C(S)—C(S)—O-A703, —C(S)—C(O)—NH2, —C(S)—C(O)—NHA704, —C(S)—C(O)—NA705A706, —C(S)—C(S)—NH2, —C(S)—C(S)—NHA707, —C(S)—C(S)—NA708A709, —C(O)—C(S)—NH2, —C(O)—C(S)—NHA710, —C(O)—C(S)—NA711A712”;
        
            wherein A601, A602, A603, A604, A605, A606, A607, A608, A609, A610, A611, A612, A613, A614, A615, A616, A617, A618, A619, A620, A621, A622, A623, A624, A625, A626, A627, A628, A629, A630, A631, A632, A633, A634, A635, A636, A637, A638, A639, A640, A641, A642, A643, A644, A645, A646, A647, A648, A649, A650, A651, A652, A653, A654, A655, A656, A657, A658, A659, A660, A661, A662, A663, A664, A665, A666, A667, A668, A669, A670, A671, A672, A673, A674, A675, A676, A677, A678, A679, A680, A681, A682, A683, A684, A685, A686, A687, A688, A689, A690, A691, A692, A693, A694, A695, A696, A697, A698, A699, A700, A701, A702, A703, A704, A705, A706, A707, A708, A709, A710, A711, A712 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively A607, A608 and/or A616, A617 and/or A629, A630 and/or A636, A637 and/or A645, A646 and/or A655, A656 and/or A660, A661 and/or A677, A678 and/or A686, A687 and/or A689, A690 and/or A692, A693 and/or A695, A696 and/or A699, A700 and/or A705, A706 and/or A708, A709 and/or A711, A712 and/or respectively together can also form “heterocyclyl”;

and radicals R1, R2, R5 independently from each other are selected from the group consisting of:

        
        
    
    
    (3) “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHB1, —NB2B3, —NO2, —OH, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—B4, —C(O)O—B5, —C(O)NH—B6, —C(O)NB7B8, —O—B9, —O(—B10-O)a—H (a=1, 2, 3, 4, 5), —O(—B11-O)b—B12 (b=1, 2, 3, 4, 5), —OC(O)—B13, —OC(O)—O—B14, —OC(O)—NHB15, —O—C(O)—NB16B17, —OP(O)(OB18)(OB19), —OSi(B20)(B21)(B22), —OS(O2)—B23, —NHC(O)—NH2, —NHC(O)—B24, —NB25C(O)—B26, —NH—C(O)—O—B27, —NH—C(O)—NH—B28, —NH—C(O)—NB29B30, —NB31-C(O)—O—B32, —NB33-C(O)—NH—B34, —NB35-C(O)—NB36B37, —NHS(O2)—B38, —NB39S(O2)—B40, —S—B41, —S(O)—B42, —S(O2)— B43, —S(O2)NH—B44, —S(O2)NB45B46, —S(O2)O—B47, —P(O)(OB48)(OB49), —Si(B50)(B51)(B52), —C(NH)—NH2, —C(NB53)-NH2, —C(NH)—NHB54, —C(NH)—NB55B56, —C(NB57)-NHB58, —C(NB59)-NB60B61, —NH—C(O)—NH—O—B62, —NH—C(O)—NB63-O—B64, —NB65-C(O)—NB66-O—B67, —N(—C(O)—NH—O—B68)2, —N(—C(O)—NB69-O—B70)2, —N(—C(O)—NH—O—B71)(—C(O)—NB72-O—B73), —C(S)—B74, —C(S)—O—B75, —C(S)—NH—B76, —C(S)—NB77B78, —C(O)—NH—O—B79, —C(O)—NB80-O—B81, —C(S)—NH—O—B82, —C(S)—NB83-O—B84, —C(O)—NH—NH—B85, —C(O)—NH—NB86B87, —C(O)—NB88-NB89B90, —C(S)—NH—NH—B91, —C(S)—NH—NB92B93, —C(S)—NB94-NB95B96, —C(O)—C(O)—O—B97, —C(O)—C(O)—NH2, —C(O)—C(O)—NHB98, —C(O)—C(O)—NB99B100, —C(S)—C(O)—O—B101, —C(O)—C(S)—O—B102, —C(S)—C(S)—O—B103, —C(S)—C(O)—NH2, —C(S)—C(O)—NHB104, —C(S)—C(O)—NB105B106, —C(S)—C(S)—NH2, —C(S)—C(S)—NHB107, —C(S)—C(S)—NB108B109, —C(O)—C(S)—NH2, —C(O)—C(S)—NHB110, —C(O)—C(S)—NB111B112”;
    
        wherein B1, B2, B3, B4, B5, B6, B7, B8, B9, B10, B11, B12, B13, B14, B15, B16, B17, B18, B19, B20, B21, B22, B23, B24, B25, B26, B27, B28, B29, B30, B31, B32, B33, B34, B35, B36, B37, B38, B39, B40, B41, B42, B43, B44, B45, B46, B47, B48, B49, B50, B51, B52, B53, B54, B55, B56, B57, B58, B59, B60, B61, B62, B63, B64, B65, B66, B67, B68, B69, B70, B71, B72, B73, B74, B75, B76, B77, B78, B79, B80, B81, B82, B83, B84, B85, B86, B87, B88, B89, B90, B91, B92, B93, B94, B95, B96, B97, B98, B99, B100, B101, B102, B103, B104, B105, B106, B107, B108, B109, B110, B111, B112 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively B2, B3 and/or B7, B8 and/or B16, B17 and/or B29, B30 and/or B36, B37 and/or B45, B46 and/or B55, B56 and/or B60, B61 and/or B77, B78 and/or B86, B87 and/or B89, B90 and/or B92, B93 and/or B95, B96 and/or B99, B100 and/or B105, B106 and/or B108, B109 and/or B111, B112 and/or respectively together can also form “heterocyclyl”;
        wherein optionally above substituents of substituents group (3)—if not hydrogen—can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        (i) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHB201, —NB202B203, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—B204, —C(O)O—B205, —C(O)NH—B206, —C(O)NB207B208, —O—B209, —O(—B210-O), —H (c=1, 2, 3, 4, 5), —O(—B211-O)d—B212 (d=1, 2, 3, 4, 5), —OC(O)—B213, —OC(O)—O—B214, —OC(O)—NHB215, —O—C(O)—NB216B217, —OP(O)(OB218)(OB219), —OSi(B220)(B221)(B222), —OS(O2)— B223, —NHC(O)—NH2, —NHC(O)—B224, —NB225C(O)—B226, —NH—C(O)—O—B227, —NH—C(O)—NH—B228, —NH—C(O)—NB229B230, —NB231-C(O)—O—B232, —NB233-C(O)—NH—B234, —NB235-C(O)—NB236B237, —NHS(O2)— B238, —NB239S(O2)—B240, —S—B241, —S(O)—B242, —S(O2)—B243, —S(O2)NH—B244, —S(O2)NB245B246, —S(O2)O—B247, —P(O)(OB248)(OB249), —Si(B250)(B251)(B252), —C(NH)—NH2, —C(NB253)-NH2, —C(NH)—NHB254, —C(NH)—NB255B256, —C(NB257)-NHB258, —C(NB259)-NB260B261, —NH—C(O)—NH—O—B262, —NH—C(O)—NB263-O—B264, —NB265-C(O)—NB266-O—B267, —N(—C(O)—NH—O—B268)2, —N(—C(O)—NB269-O—B270)2, —N(—C(O)—NH—O—B271)(—C(O)—NB272-O—B273), —C(S)—B274, —C(S)—O—B275, —C(S)—NH—B276, —C(S)—NB277B278, —C(O)—NH—O—B279, —C(O)—NB280-O—B281, —C(S)—NH—O—B282, —C(S)—NB283-O—B284, —C(O)—NH—NH—B285, —C(O)—NH—NB286B287, —C(O)—NB288-NB289B290, —C(S)—NH—NH—B291, —C(S)—NH—NB292B293, —C(S)—NB294-NB295B296, —C(O)—C(O)—O—B297, —C(O)—C(O)—NH2, —C(O)—C(O)—NHB298, —C(O)—C(O)—NB299B300, —C(S)—C(O)—O—B301, —C(O)—C(S)—O—B302, —C(S)—C(S)—O—B303, —C(S)—C(O)—NH2, —C(S)—C(O)—NH B304, —C(S)—C(O)—NB305B306, —C(S)—C(S)—NH2, —C(S)—C(S)—NHB307, —C(S)—C(S)—NB308B309, —C(O)—C(S)—NH2, —C(O)—C(S)—NHB310, —C(O)—C(S)—NB311B312”;
        
            wherein 8201, B202, B203, B204, B205, B206, B207, B208, B209, B210, 8211, B212, B213, B214, B215, B216, B217, B218, B219, B220, B221, B222, B223, B224, B225, B226, B227, B228, B229, B230, B231, B232, B233, B234, B235, B236, B237, B238, B239, B240, B241, B242, B243, B244, B245, B246, B247, B248, B249, B250, B251, B252, B253, B254, B255, B256, B257, B258, B259, B260, B261, B262, B263, B264, B265, B266, B267, B268, B269, B270, B271, B272, B273, B274, B275, B276, B277, B278, B279, B280, B281, B282, B283, B284, B285, B286, B287, B288, B289, B290, B291, B292, B293, B294, B295, B296, B297, B298, B299, B300, B301, B302, B303, B304, B305, B306, B307, B308, B309, B310, B311, B312 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively B207, B208 and/or B216, B217 and/or B229, B230 and/or B236, B237 and/or B245, B246 and/or B255, B256 and/or B260, B261 and/or B277, B278 and/or B286, B287 and/or B289, B290 and/or B292, B293 and/or B295, B296 and/or B299, B300 and/or B305, B306 and/or B308, B309 and/or B311, B312 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (i) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (ii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHB401, —NB402B403, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—B404, —C(O)O—B405, —C(O)NH—B406, —C(O)NB407B408, —O—B409, —O(—B410-O), —H (e=1, 2, 3, 4, 5), —O(—B411-O)f—B412 (f=1, 2, 3, 4, 5), —OC(O)—B413, —OC(O)—O—B414, —OC(O)—NHB415, —O—C(O)—NB416B417, —OP(O)(OB418)(OB419), —OSi(B420)(B421)(B422), —OS(O2)—B423, —NHC(O)—NH2, —NHC(O)—B424, —NB425C(O)—B426, —NH—C(O)—O—B427, —NH—C(O)—NH—B428, —NH—C(O)—NB429B430, —NB431-C(O)—O—B432, —NB433-C(O)—NH—B434, —NB435-C(O)—NB436B437, —NHS(O2)—B438, —NB439S(O2)— B440, —S—B441, —S(O)—B442, —S(O2)—B443, —S(O2)NH—B444, —S(O2)NB445B446, —S(O2)O—B447, —P(O)(OB448)(OB449), —Si(B450)(B451)(B452), —C(NH)—NH2, —C(NB453)-NH2, —C(NH)—NHB454, —C(NH)—NB455B456, —C(NB457)-NHB458, —C(NB459)-NB460B461, —NH—C(O)—NH—O—B462, —NH—C(O)—NB463-O—B464, —NB465-C(O)—NB466-O—B467, —N(—C(O)—NH—O—B468)2, —N(—C(O)—NB469-O—B470)2, —N(—C(O)—NH—O—B471)(—C(O)—NB472-O—B473), —C(S)—B474, —C(S)—O—B475, —C(S)—NH—B476, —C(S)—NB477B478, —C(O)—NH—O—B479, —C(O)—NB480-O—B481, —C(S)—NH—O—B482, —C(S)—NB483-O—B484, —C(O)—NH—NH—B485, —C(O)—NH—NB486B487, —C(O)—NB488-NB489B490, —C(S)—NH—NH—B491, —C(S)—NH—NB492B493, —C(S)—NB494-NB495B496, —C(O)—C(O)—O—B497, —C(O)—C(O)—NH2, —C(O)—C(O)—NHB498, —C(O)—C(O)—NB499B500, —C(S)—C(O)—O—B501, —C(O)—C(S)—O—B502, —C(S)—C(S)—O—B503, —C(S)—C(O)—NH2, —C(S)—C(O)—NHB504, —C(S)—C(O)—NB505B506, —C(S)—C(S)—NH2, —C(S)—C(S)—NHB507, —C(S)—C(S)—NB508B509, —C(O)—C(S)—NH2, —C(O)—C(S)—NHB510, —C(O)—C(S)—NB511B512”;
        
            wherein B401, B402, B403, B404, B405, B406, B407, B408, B409, B410, B411, B412, B413, B414, B415, B416, B417, B418, B419, B420, B421, B422, B423, B424, B425, B426, B427, B428, B429, B430, B431, B432, B433, B434, B435, B436, B437, B438, B439, B440, B441, B442, B443, B444, B445, B446, B447, B448, B449, B450, B451, B452, B453, B454, B455, B456, B457, B458, B459, B460, B461, B462, B463, B464, B465, B466, B467, B468, B469, B470, B471, B472, B473, B474, B475, B476, B477, B478, B479, B480, B481, B482, B483, B484, B485, B486, B487, B488, B489, B490, B491, B492, B493, B494, B495, B496, B497, B498, B499, B500, B501, B502, B503, B504, B505, B506, B507, B508, B509, B510, B511, B512 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively B407, B408 and/or B416, B417 and/or 8429, B430 and/or 8436, B437 and/or B445, B446 and/or B455, B456 and/or B460, B461 and/or B477, B478 and/or B486, B487 and/or B489, B490 and/or B492, B493 and/or B495, B496 and/or B499, B500 and/or B505, B506 and/or B508, B509 and/or B511, B512 and/or respectively together can also form “heterocyclyl”;
            wherein optionally above substituents of substituents group (ii) can in turn independently from each other be substituted with at least one substituent, identical or different, selected from the group consisting of:
        
        
        (iii) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, —F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NHB601, —NB602B603, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —C(O)—B604, —C(O)O—B605, —C(O)NH—B606, —C(O)NB607B608, —O—B609, —O(—B610-O)e—H (e=1, 2, 3, 4, 5), —O(—B611-O)f—B612 (f=1, 2, 3, 4, 5), —OC(O)—B613, —OC(O)—O—B614, —OC(O)—NHB615, —O—C(O)—NB616B617, —OP(O)(OB618)(OB619), —OSi(B620)(B621)(B622), —OS(O2)—B623, —NHC(O)—NH2, —NHC(O)—B624, —NB625C(O)—B626, —NH—C(O)—O—B627, —NH—C(O)—NH—B628, —NH—C(O)—NB629B630, —NB631-C(O)—O—B632, —NB633-C(O)—NH—B634, —NB635-C(O)—NB636B637, —NHS(O2)—B638, —NB639S(O2)—B640, —S—B641, —S(O)—B642, —S(O2)—B643, —S(O2)NH—B644, —S(O2)NB645B646, —S(O2)O—B647, —P(O)(OB648)(OB649), —Si(B650)(B651)(B652), —C(NH)—NH2, —C(NB653)-NH2, —C(NH)—NHB654, —C(NH)—NB655B656, —C(NB657)-NHB658, —C(NB659)-NB660B661, —NH—C(O)—NH—O—B662, —NH—C(O)—NB663-O—B664, —NB665-C(O)—NB666-O—B667, —N(—C(O)—NH—O—B668)2, —N(—C(O)—NB669-O—B670)2, —N(—C(O)—NH—O—B671)(—C(O)—NB672-O—B673), —C(S)—B674, —C(S)—O—B675, —C(S)—NH—B676, —C(S)—NB677B678, —C(O)—NH—O—B679, —C(O)—NB680-O—B681, —C(S)—NH—O—B682, —C(S)—NB683-O—B684, —C(O)—NH—NH—B685, —C(O)—NH—NB686B687, —C(O)—NB688-NB689B690, —C(S)—NH—NH—B691, —C(S)—NH—NB692B693, —C(S)—NB694-NB695B696, —C(O)—C(O)—O—B697, —C(O)—C(O)—NH2, —C(O)—C(O)—NHB698, —C(O)—C(O)—NB699B700, —C(S)—C(O)—O—B701, —C(O)—C(S)—O—B702, —C(S)—C(S)—O—B703, —C(S)—C(O)—NH2, —C(S)—C(O)—NHB704, —C(S)—C(O)—NB705B706, —C(S)—C(S)—NH2, —C(S)—C(S)—NHB707, —C(S)—C(S)—NB708B709, —C(O)—C(S)—NH2, —C(O)—C(S)—NHB710, —C(O)—C(S)—NB711B712”;
        
            wherein B601, B602, B603, B604, B605, B606, B607, B608, B609, B610, B611, B612, B613, B614, B615, B616, B617, B618, B619, B620, B621, B622, B623, B624, B625, B626, B627, B628, B629, B630, B631, B632, B633, B634, B635, B636, B637, B638, B639, B640, B641, B642, B643, B644, B645, B646, B647, B648, B649, B650, B651, B652, B653, B654, B655, B656, B657, B658, B659, B660, B661, B662, B663, B664, B665, B666, B667, B668, B669, B670, B671, B672, B673, B674, B675, B676, B677, B678, B679, B680, B681, B682, B683, B684, B685, B686, B687, B688, B689, B690, B691, B692, B693, B694, B695, B696, B697, B698, B699, B700, B701, B702, B703, B704, B705, B706, B707, B708, B709, B710, B711, B712 are independently from each other selected from the group consisting of: “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively B607, B608 and/or B616, B617 and/or 8629, B630 and/or B636, B637 and/or B645, B646 and/or 8655, B656 and/or B660, B661 and/or B677, B678 and/or B686, B687 and/or B689, B690 and/or B692, B693 and/or B695, B696 and/or 8699, B700 and/or B705, B706 and/or B708, B709 and/or B711, B712 and/or respectively together can also form “heterocyclyl”.
        
        
    
    


In order to avoid ambiguities, the cases (1)(a) to (d) detailed above for the general formula (I) are to establish novelty over the prior art as follows: novelty is established by the fact that at least one of radicals R3, R4 must be one of the substituents as illustrated under (1) (a), (b), (c) and (d), whereas the other one of radicals R3, R4 can be either one of the substituents as illustrated under (1) (a), (b), (c) and (d) or it can be one of the substituents as illustrated under (2). Radicals R1, R2 and R5 can in all cases be one of the substituents as illustrated under (3).
In a preferred embodiment, pyrido[2,3-b]pyrazine derivatives according to above general formula (I) are provided, wherein:
radical R1 independently is selected from the group consisting of:

    
    
        (i) “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, —NH-alkyl, —NH—(C9-C30)alkyl, —NH-cycloalkyl, —NH-cycloalkylalkyl, —NH-aryl, —NH-arylalkyl, —NH-heteroaryl, —NH-heteroarylalkyl, —NH-heterocyclyl, —NH-heterocyclylalkyl”;
        
            where above substituents of substituents group (i)—if not hydrogen or nitrogen—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-I, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-Cl, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
        
        
    
    


radical R2 independently is “hydrogen”;
radical R3 independently is selected from the group consisting of:

    
    
        (i) “—NH—C(O)—NH—C(O)—O-alkyl, —NH—C(O)—NH—C(O)—O—(C9-C30)alkyl, —NH—C(O)—NH—C(O)—O-cycloalkyl, —NH—C(O)—NH—C(O)—O-cycloalkylalkyl, —NH—C(O)—NH—C(O)—O-aryl, —NH—C(O)—NH—C(O)—O-arylalkyl, —NH—C(O)—NH—C(O)—O-heteroaryl, —NH—C(O)—NH—C(O)—O-heteroarylalkyl, —NH—C(O)—NH—C(O)—O-heterocyclyl, —NH—C(O)—NH—C(O)—O-heterocyclylalkyl —NH—C(S)—NH-alkyl, —NH—C(S)—NH—(C9-C30)alkyl, —NH—C(S)—NH-cycloalkyl, —NH—C(S)—NH-cycloalkylalkyl, —NH—C(S)—NH-aryl, —NH—C(S)—NH-arylalkyl, —NH—C(S)—NH-heteroaryl, —NH—C(S)—NH-heteroarylalkyl, —NH—C(S)—NH-heterocyclyl, —NH—C(S)—NH-heterocyclylalkyl, —NH—C(═NH)-alkyl, —NH—C(═NH)—(C9-C30)alkyl, —NH—C(═NH)-cycloalkyl, —NH—C(═NH)-cycloalkylalkyl, —NH—C(═NH)-aryl, —NH—C(═NH)-arylalkyl, —NH—C(═NH)-heteroaryl, —NH—C(═NH)-heteroarylalkyl, —NH—C(═NH)-heterocyclyl, —NH—C(═NH)-heterocyclylalkyl, —NH—C(O)—C(O)-alkyl, —NH—C(O)—C(O)—(C9-C30)alkyl, —NH—C(O)—C(O)-cycloalkyl, —NH—C(O)—C(O)-cycloalkylalkyl, —NH—C(O)—C(O)-aryl, —NH—C(O)—C(O)-arylalkyl, —NH—C(O)—C(O)-heteroaryl, —NH—C(O)—C(O)-heteroarylalkyl, —NH—C(O)—C(O)-heterocyclyl, —NH—C(O)—C(O)-heterocyclylalkyl”
        
            where above substituents of substituents group (i)—if not hydrogen or nitrogen—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-I, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-Cl, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
        
        
    
    


radical R4 independently is selected from the group consisting of:

    
    
        (i) “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, —NH-alkyl, —NH—(C9-C30)alkyl, —NH-cycloalkyl, —NH-cycloalkylalkyl, —NH-aryl, —NH-arylalkyl, —NH-heteroaryl, —NH-heteroarylalkyl, —NH-heterocyclyl, —NH-heterocyclylalkyl”;
        
            where above substituents of substituents group (i)—if not hydrogen or nitrogen—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-I, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-C1, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
        
        
    
    


radical R5 independently is “hydrogen”.
In a further preferred embodiment, pyrido[2,3-b]pyrazine derivatives according to above general formula (I) are provided, wherein:
radical R1 independently is selected from the group consisting of:

    
    
        (i) “hydrogen, methyl, ethyl, propyl, isopropyl, tert-butyl, hexyl, allyl, propenyl, prop-2-en-1-yl, cyclopropyl, cyclopropylmethyl, cyclopropylethyl, cyclopropylpropyl, cyclopropylbutyl, cyclopentyl, cyclopentylmethyl, cyclopentylethyl, cyclopentylpropyl, cyclopentylbutyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, cyclohexylbutyl, phenyl, naphthalenyl, naphthalen-1-yl, naphthalen-2-yl, benzyl, phenyl-ethyl, isoxazol, pyridinyl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyrazolyl, pyrazol-3-yl, pyrazol-4-yl, quinolinyl, quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-8-yl, thiophenyl, thiophen-2-yl, thiophen-3-yl, furanyl, furan-2-yl, furan-3-yl, pyrimidinyl, pyrimidin-5-yl, imidazolyl, imidazol-4-yl, imidazol-3-yl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-b]pyridin-5-yl, indolyl, 1H-indol-2-yl, dibenzofuranyl, dibenzofuran-4-yl, piperidinyl, piperidinylmethyl, piperidinylethyl, piperidinylpropyl, piperidinylbutyl, piperidin-1-yl, piperidin-3-yl, piperidin-4-yl, piperazinyl, piperazinylmethyl, piperazinylethyl, piperazinylpropyl, piperazinylbutyl, piperazin-1-yl, diazepanyl, diazepanylmethyl, diazepanylethyl, diazepanylpropyl, diazepanylbuytl, diazepan-1-yl, morpholinyl, morpholinylmethyl, morpholinylethyl, morpholinylpropyl, morpholinylbuytyl, morpholin-4-yl, 2-morpholin-4-yl-ethyl, 1,2,3,4-tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydro-isoquinolinylmethyl, 1,2,3,4-tetrahydro-isoquinolinylethyl, 1,2,3,4-tetrahydro-isoquinolinylpropyl, 1,2,3,4-tetrahydro-isoquinolinylbutyl, 1,2,3,4-tetrahydro-isoquinolin-7-yl, benzo[1,3]dioxolyl, benzo[1,3]dioxolylmethyl, benzo[1,3]dioxolylethyl, benzo[1,3]dioxolylpropyl, benzo[1,3]dioxolylbutyl, benzo[1,3]dioxol-5-yl, benzo[1,4]oxazinyl, benzo[1,4]oxazinylmethyl, benzo[1,4]oxazinylethyl, benzo[1,4]oxazinylpropyl, benzo[1,4]oxazinylbutyl, benzo[1,4]oxazin-6-yl, —NH—Rx1” with Rx1 being selected from the group consisting of: “methyl, ethyl, propyl, isopropyl, tert-butyl, hexyl, allyl, propenyl, prop-2-en-1-yl, cyclopropyl, cyclopropylmethyl, cyclopropylethyl, cyclopropylpropyl, cyclopropylbutyl, cyclopentyl, cyclopentylmethyl, cyclopentylethyl, cyclopentylpropyl, cyclopentylbutyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, cyclohexylbutyl, phenyl, naphthalenyl, naphthalen-1-yl, naphthalen-2-yl, benzyl, phenyl-ethyl, isoxazol, pyridinyl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyrazolyl, pyrazol-3-yl, pyrazol-4-yl, quinolinyl, quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-8-yl, thiophenyl, thiophen-2-yl, thiophen-3-yl, furanyl, furan-2-yl, furan-3-yl, pyrimidinyl, pyrimidin-5-yl, imidazolyl, imidazol-4-yl, imidazol-3-yl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-b]pyridin-5-yl, indolyl, 1H-indol-2-yl, dibenzofuranyl, dibenzofuran-4-yl, piperidinyl, piperidinylmethyl, piperidinylethyl, piperidinylpropyl, piperidinylbutyl, piperidin-1-yl, piperidin-3-yl, piperidin-4-yl, piperazinyl, piperazinylmethyl, piperazinylethyl, piperazinylpropyl, piperazinylbutyl, piperazin-1-yl, diazepanyl, diazepanylmethyl, diazepanylethyl, diazepanyl-propyl, diazepanylbuytl, diazepan-1-yl, morpholinyl, morpholinylmethyl, morpholinylethyl, morpholinylpropyl, morpholinylbuytyl, morpholin-4-yl, 2-morpholin-4-yl-ethyl, 1,2,3,4-tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydro-isoquinolinylmethyl, 1,2,3,4-tetrahydro-isoquinolinylethyl, 1,2,3,4-tetrahydro-isoquinolinylpropyl, 1,2,3,4-tetrahydro-isoquinolinylbutyl, 1,2,3,4-tetrahydro-isoquinolin-7-yl, benzo[1,3]dioxolyl, benzo[1,3]dioxolylmethyl, benzo[1,3]dioxolylethyl, benzo[1,3]dioxolylpropyl, benzo[1,3]dioxolylbutyl, benzo[1,3]dioxol-5-yl, benzo[1,4]oxazinyl, benzo[1,4]oxazinylmethyl, benzo[1,4]oxazinylethyl, benzo[1,4]oxazinylpropyl, benzo[1,4]oxazinylbutyl, benzo[1,4]oxazin-6-yl”;
        
            where above substituents of substituents group (i)—if not hydrogen or nitrogen—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-I, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-C1, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
        
        
    
    


radical R2 independently is “hydrogen”;
radical R3 independently is selected from the group consisting of:

    
    
        (i) “—NH—C(O)—NH—C(O)—O—Rx2, —NH—C(S)—NH—Rx3, —NH—C(═NH)—Rx4, —NH—C(O)—C(O)—Rx5”, with Rx2, Rx3, Rx4, Rx5 independently from each other being selected from the group consisting of: “methyl, ethyl, propyl, isopropyl, tert-butyl, hexyl, allyl, propenyl, prop-2-en-1-yl, cyclopropyl, cyclopropylmethyl, cyclopropylethyl, cyclopropylpropyl, cyclopropylbutyl, cyclopentyl, cyclopentylmethyl, cyclopentylethyl, cyclopentylpropyl, cyclopentylbutyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, cyclohexylbutyl, phenyl, naphthalenyl, naphthalen-1-yl, naphthalen-2-yl, benzyl, phenyl-ethyl, isoxazol, pyridinyl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyrazolyl, pyrazol-3-yl, pyrazol-4-yl, quinolinyl, quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-8-yl, thiophenyl, thiophen-2-yl, thiophen-3-yl, furanyl, furan-2-yl, furan-3-yl, pyrimidinyl, pyrimidin-5-yl, imidazolyl, imidazol-4-yl, imidazol-3-yl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-b]pyridin-5-yl, indolyl, 1H-indol-2-yl, dibenzofuranyl, dibenzofuran-4-yl, piperidinyl, piperidinylmethyl, piperidinylethyl, piperidinylpropyl, piperidinylbutyl, piperidin-1-yl, piperidin-3-yl, piperidin-4-yl, piperazinyl, piperazinylmethyl, piperazinylethyl, piperazinylpropyl, piperazinylbutyl, piperazin-1-yl, diazepanyl, diazepanylmethyl, diazepanylethyl, diazepanylpropyl, diazepanylbuytl, diazepan-1-yl, morpholinyl, morpholinylmethyl, morpholinylethyl, morpholinylpropyl, morpholinylbuytyl, morpholin-4-yl, 2-morpholin-4-yl-ethyl, 1,2,3,4-tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydro-isoquinolinylmethyl, 1,2,3,4-tetrahydro-isoquinolinylethyl, 1,2,3,4-tetrahydro-isoquinolinylpropyl, 1,2,3,4-tetrahydro-isoquinolinylbutyl, 1,2,3,4-tetrahydro-isoquinolin-7-yl, benzo[1,3]dioxolyl, benzo[1,3]dioxolylmethyl, benzo[1,3]dioxolylethyl, benzo[1,3]dioxolylpropyl, benzo[1,3]dioxolylbutyl, benzo[1,3]dioxol-5-yl, benzo[1,4]oxazinyl, benzo[1,4]oxazinylmethyl, benzo[1,4]oxazinylethyl, benzo[1,4]oxazinylpropyl, benzo[1,4]oxazinylbutyl, benzo[1,4]oxazin-6-yl”;
        where above substituents of substituents group (i)—if not hydrogen or nitrogen—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-I, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-C1, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
    
    


radical R4 independently is selected from the group consisting of:

    
    
        (i) “hydrogen, methyl, ethyl, propyl, isopropyl, tert-butyl, hexyl, allyl, propenyl, prop-2-en-1-yl, cyclopropyl, cyclopropylmethyl, cyclopropylethyl, cyclopropylpropyl, cyclopropylbutyl, cyclopentyl, cyclopentylmethyl, cyclopentylethyl, cyclopentylpropyl, cyclopentylbutyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, cyclohexylbutyl, phenyl, naphthalenyl, naphthalen-1-yl, naphthalen-2-yl, benzyl, phenyl-ethyl, isoxazol, pyridinyl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyrazolyl, pyrazol-3-yl, pyrazol-4-yl, quinolinyl, quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-8-yl, thiophenyl, thiophen-2-yl, thiophen-3-yl, furanyl, furan-2-yl, furan-3-yl, pyrimidinyl, pyrimidin-5-yl, imidazolyl, imidazol-4-yl, imidazol-3-yl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-b]pyridin-5-yl, indolyl, 1H-indol-2-yl, dibenzofuranyl, dibenzofuran-4-yl, piperidinyl, piperidinylmethyl, piperidinylethyl, piperidinylpropyl, piperidinylbutyl, piperidin-1-yl, piperidin-3-yl, piperidin-4-yl, piperazinyl, piperazinylmethyl, piperazinylethyl, piperazinylpropyl, piperazinylbutyl, piperazin-1-yl, diazepanyl, diazepanylmethyl, diazepanylethyl, diazepanylpropyl, diazepanylbuytl, diazepan-1-yl, morpholinyl, morpholinylmethyl, morpholinylethyl, morpholinylpropyl, morpholinylbuytyl, morpholin-4-yl, 2-morpholin-4-yl-ethyl, 1,2,3,4-tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydro-isoquinolinylmethyl, 1,2,3,4-tetrahydro-isoquinolinylethyl, 1,2,3,4-tetrahydro-isoquinolinylpropyl, 1,2,3,4-tetrahydro-isoquinolinylbutyl, 1,2,3,4-tetrahydro-isoquinolin-7-yl, benzo[1,3]dioxolyl, benzo[1,3]dioxolylmethyl, benzo[1,3]dioxolylethyl, benzo[1,3]dioxolylpropyl, benzo[1,3]dioxolylbutyl, benzo[1,3]dioxol-5-yl, benzo[1,4]oxazinyl, benzo[1,4]oxazinylmethyl, benzo[1,4]oxazinylethyl, benzo[1,4]oxazinylpropyl, benzo[1,4]oxazinylbutyl, benzo[1,4]oxazin-6-yl, —NH—Rx6” with Rx6 being selected from the group consisting of: “methyl, ethyl, propyl, isopropyl, tert-butyl, hexyl, allyl, propenyl, prop-2-en-1-yl, cyclopropyl, cyclopropylmethyl, cyclopropylethyl, cyclopropylpropyl, cyclopropylbutyl, cyclopentyl, cyclopentylmethyl, cyclopentylethyl, cyclopentylpropyl, cyclopentylbutyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, cyclohexylbutyl, phenyl, naphthalenyl, naphthalen-1-yl, naphthalen-2-yl, benzyl, phenyl-ethyl, isoxazol, pyridinyl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyrazolyl, pyrazol-3-yl, pyrazol-4-yl, quinolinyl, quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-8-yl, thiophenyl, thiophen-2-yl, thiophen-3-yl, furanyl, furan-2-yl, furan-3-yl, pyrimidinyl, pyrimidin-5-yl, imidazolyl, imidazol-4-yl, imidazol-3-yl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-b]pyridin-5-yl, indolyl, 1H-indol-2-yl, dibenzofuranyl, dibenzofuran-4-yl, piperidinyl, piperidinylmethyl, piperidinylethyl, piperidinylpropyl, piperidinylbutyl, piperidin-1-yl, piperidin-3-yl, piperidin-4-yl, piperazinyl, piperazinylmethyl, piperazinylethyl, piperazinylpropyl, piperazinylbutyl, piperazin-1-yl, diazepanyl, diazepanylmethyl, diazepanylethyl, diazepanylpropyl, diazepanylbuytl, diazepan-1-yl, morpholinyl, morpholinylmethyl, morpholinylethyl, morpholinylpropyl, morpholinylbuytyl, morpholin-4-yl, 2-morpholin-4-yl-ethyl, 1,2,3,4-tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydro-isoquinolinylmethyl, 1,2,3,4-tetrahydro-isoquinolinylethyl, 1,2,3,4-tetrahydro-isoquinolinylpropyl, 1,2,3,4-tetrahydro-isoquinolinylbutyl, 1,2,3,4-tetrahydro-isoquinolin-7-yl, benzo[1,3]dioxolyl, benzo[1,3]dioxolylmethyl, benzo[1,3]dioxolylethyl, benzo[1,3]dioxolylpropyl, benzo[1,3]dioxolylbutyl, benzo[1,3]dioxol-5-yl, benzo[1,4]oxazinyl, benzo[1,4]oxazinylmethyl, benzo[1,4]oxazinylethyl, benzo[1,4]oxazinylpropyl, benzo[1,4]oxazinylbutyl, benzo[1,4]oxazin-6-yl”;
        where above substituents of substituents group (i)—if not hydrogen or nitrogen—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-I, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-Cl, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
    
    


radical R5 independently is “hydrogen”.
In a further preferred embodiment, pyrido[2,3-b]pyrazine derivatives according to above general formula (I) and preferred embodiments and subsets are provided, wherein:
radical R1 independently is selected from the group consisting of:

    
    
        (i) “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, —NH-alkyl, —NH—(C9-C30)alkyl, —NH-cycloalkyl, —NH-cycloalkylalkyl, —NH-aryl, —NH-arylalkyl, —NH-heteroaryl, —NH-heteroarylalkyl, —NH-heterocyclyl, —NH-heterocyclylalkyl”;
        
            where above substituents of substituents group (i)—if not hydrogen or nitrogen—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-I, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-C1, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
        
        
    
    


radical R2 independently is “hydrogen”;
radical R3 independently is selected from the group consisting of:

    
    
        (i) “—NH—C(O)—NH2, —NH—C(O)—NH-alkyl, —NH—C(O)—NH—(C9-C30)alkyl, —NH—C(O)—NH-cycloalkyl, —NH—C(O)—NH-cycloalkylalkyl, —NH—C(O)—NH-aryl, NH—C(O)—NH-arylalkyl, —NH—C(O)—NH-heteroaryl, —NH—C(O)—NH-heteroarylalkyl, —NH—C(O)—NH-heterocyclyl, —NH—C(O)—NH-heterocyclylalkyl, —NH—C(O)—O-alkyl, —NH—C(O)—O—(C9-C30)alkyl, —NH—C(O)—O-cycloalkyl, —NH—C(O)—O-cycloalkylalkyl, —NH—C(O)—O-aryl, —NH—C(O)—O-arylalkyl, —NH—C(O)—O-heteroaryl, —NH—C(O)—O-heteroarylalkyl, —NH—C(O)—O-heterocyclyl, —NH—C(O)—O-heterocyclylalkyl, —NH—C(O)-alkyl, —NH—C(O)—(C9-C30)alkyl, —NH—C(O)-cycloalkyl, —NH—C(O)-cycloalkylalkyl, —NH—C(O)-aryl, —NH—C(O)-arylalkyl, —NH—C(O)-heteroaryl, —NH—C(O)-heteroarylalkyl, —NH—C(O)-heterocyclyl, —NH—C(O)-heterocyclylalkyl, —NH—S(O2)-alkyl, —NH—S(O2)—(C9-C30)alkyl, —NH—S(O2)-cycloalkyl, —NH—S(O2)-cycloalkylalkyl, —NH—S(O2)-aryl, —NH—S(O2)-arylalkyl, —NH—S(O2)-heteroaryl, —NH—S(O2)-heteroarylalkyl, —NH—S(O2)-heterocyclyl, —NH—S(O2)-heterocyclylalkyl;
        
            where above substituents of substituents group (i)—if not hydrogen, nitrogen or sulphur—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-I, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-Cl, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
        
        
    
    


radical R4 independently is selected from the group consisting of:

    
    
        (i) “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, —NH-alkyl, —NH—(C9-C30)alkyl, —NH-cycloalkyl, —NH-cycloalkylalkyl, —NH-aryl, —NH-arylalkyl, —NH-heteroaryl, —NH-heteroarylalkyl, —NH-heterocyclyl, —NH-heterocyclylalkyl”;
        
            where above substituents of substituents group (i)—if not hydrogen or nitrogen—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-I, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-C1, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
        
        
    
    


radical R5 independently is selected from the group consisting of:

    
    
        (i) “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl”;
        
            where above substituents of substituents group (i)—if not hydrogen—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-I, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-Cl, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”.
        
        
    
    


In a yet further preferred embodiment, pyrido[2,3-b]pyrazine derivatives according to above general formula (I) and preferred embodiments and subsets are provided, wherein:
radical R1 independently is selected from the group consisting of:

    
    
        (i) “hydrogen, methyl, ethyl, propyl, isopropyl, tert-butyl, hexyl, allyl, propenyl, prop-2-en-1-yl, cyclopropyl, cyclopropylmethyl, cyclopropylethyl, cyclopropyl-propyl, cyclopropylbutyl, cyclopentyl, cyclopentylmethyl, cyclopentylethyl, cyclopentylpropyl, cyclopentylbutyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, cyclohexylbutyl, phenyl, naphthalenyl, naphthalen-1-yl, naphthalen-2-yl, benzyl, phenyl-ethyl, isoxazol, pyridinyl, pyridin-3-yl, pyridin-4-yl, pyrazolyl, pyrazol-3-yl, pyrazol-4-yl, quinolinyl, quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-8-yl, thiophenyl, thiophen-2-yl, thiophen-3-yl, furanyl, furan-2-yl, furan-3-yl, pyrimidinyl, pyrimidin-5-yl, imidazolyl, imidazol-4-yl, imidazol-3-yl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-b]pyridin-5-yl, indolyl, 1H-indol-2-yl, dibenzofuranyl, dibenzofuran-4-yl, piperidinyl, piperidinylmethyl, piperidinylethyl, piperidinylpropyl, piperidinylbutyl, piperidin-1-yl, piperidin-3-yl, piperidin-4-yl, piperazinyl, piperazinylmethyl, piperazinylethyl, piperazinylpropyl, piperazinylbutyl, piperazin-1-yl, diazepanyl, diazepanylmethyl, diazepanylethyl, diazepanylpropyl, diazepanylbuytl, diazepan-1-yl, morpholinyl, morpholinyl-methyl, morpholinylethyl, morpholinylpropyl, morpholinylbuytyl, morpholin-4-yl, 2-morpholin-4-yl-ethyl, 1,2,3,4-tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydro-isoquinolinylmethyl, 1,2,3,4-tetrahydro-isoquinolinylethyl, 1,2,3,4-tetrahydro-isoquinolinylpropyl, 1,2,3,4-tetrahydro-isoquinolinylbutyl, 1,2,3,4-tetrahydro-isoquinolin-7-yl, benzo[1,3]dioxolyl, benzo[1,3]dioxolylmethyl, benzo[1,3]dioxolylethyl, benzo[1,3]dioxolylpropyl, benzo[1,3]dioxolylbutyl, benzo[1,3]dioxol-5-yl, benzo[1,4]oxazinyl, benzo[1,4]oxazinylmethyl, benzo[1,4]oxazinylethyl, benzo[1,4]oxazinylpropyl, benzo[1,4]oxazinylbutyl, benzo[1,4]oxazin-6-yl, —NH—Ry1” with Ry1 being selected from the group consisting of: “methyl, ethyl, propyl, isopropyl, tert-butyl, hexyl, allyl, propenyl, prop-2-en-1-yl, cyclopropyl, cyclopropylmethyl, cyclopropylethyl, cyclopropylpropyl, cyclopropylbutyl, cyclopentyl, cyclopentylmethyl, cyclopentylethyl, cyclopentyl-propyl, cyclopentylbutyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, cyclohexylbutyl, phenyl, naphthalenyl, naphthalen-1-yl, naphthalen-2-yl, benzyl, phenyl-ethyl, isoxazol, pyridinyl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyrazolyl, pyrazol-3-yl, pyrazol-4-yl, quinolinyl, quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-8-yl, thiophenyl, thiophen-2-yl, thiophen-3-yl, furanyl, furan-2-yl, furan-3-yl, pyrimidinyl, pyrimidin-5-yl, imidazolyl, imidazol-4-yl, imidazol-3-yl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-b]pyridin-5-yl, indolyl, 1H-indol-2-yl, dibenzofuranyl, dibenzofuran-4-yl, piperidinyl, piperidinylmethyl, piperidinylethyl, piperidinylpropyl, piperidinylbutyl, piperidin-1-yl, piperidin-3-yl, piperidin-4-yl, piperazinyl, piperazinylmethyl, piperazinylethyl, piperazinylpropyl, piperazinylbutyl, piperazin-1-yl, diazepanyl, diazepanylmethyl, diazepanylethyl, diazepanylpropyl, diazepanylbuytl, diazepan-1-yl, morpholinyl, morpholinylmethyl, morpholinylethyl, morpholinylpropyl, morpholinylbuytyl, morpholin-4-yl, 2-morpholin-4-yl-ethyl, 1,2,3,4-tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydro-isoquinolinylmethyl, 1,2,3,4-tetrahydro-isoquinolinylethyl, 1,2,3,4-tetrahydro-isoquinolinylpropyl, 1,2,3,4-tetrahydro-isoquinolinylbutyl, 1,2,3,4-tetrahydro-isoquinolin-7-yl, benzo[1,3]dioxolyl, benzo[1,3]dioxolylmethyl, benzo[1,3]dioxolylethyl, benzo[1,3]dioxolylpropyl, benzo[1,3]dioxolylbutyl, benzo[1,3]dioxol-5-yl, benzo[1,4]oxazinyl, benzo[1,4]oxazinylmethyl, benzo[1,4]oxazinylethyl, benzo[1,4]oxazinylpropyl, benzo[1,4]oxazinylbutyl, benzo[1,4]oxazin-6-yl”;
        
            where above substituents of substituents group (i)—if not hydrogen or nitrogen—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-I, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-C1, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
        
        
    
    


radical R2 independently is “hydrogen”;
radical R3 independently is selected from the group consisting of:

    
    
        (i) “—NH—C(O)—NH2, —NH—C(O)—NH—Ry2, —NH—C(O)—O—Ry3, —NH—C(O)—Ry4, —NH—S(O2)—Ry5”;
        
            with Ry2, Ry3, Ry4, Ry5 independently from each other being selected from the group consisting of: “methyl, ethyl, propyl, isopropyl, tert-butyl, hexyl, allyl, propenyl, prop-2-en-1-yl, cyclopropyl, cyclopropylmethyl, cyclopropylethyl, cyclopropylpropyl, cyclopropylbutyl, cyclopentyl, cyclopentylmethyl, cyclopentylethyl, cyclopentylpropyl, cyclopentylbutyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, cyclohexylbutyl, phenyl, naphthalenyl, naphthalen-1-yl, naphthalen-2-yl, benzyl, phenyl-ethyl, isoxazol, pyridinyl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyrazolyl, pyrazol-3-yl, pyrazol-4-yl, quinolinyl, quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-8-yl, thiophenyl, thiophen-2-yl, thiophen-3-yl, furanyl, furan-2-yl, furan-3-yl, pyrimidinyl, pyrimidin-5-yl, imidazolyl, imidazol-4-yl, imidazol-3-yl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-b]pyridin-5-yl, indolyl, 1H-indol-2-yl, dibenzofuranyl, dibenzofuran-4-yl, piperidinyl, piperidinylmethyl, piperidinylethyl, piperidinylpropyl, piperidinylbutyl, piperidin-1-yl, piperidin-3-yl, piperidin-4-yl, piperazinyl, piperazinylmethyl, piperazinylethyl, piperazinylpropyl, piperazinylbutyl, piperazin-1-yl, diazepanyl, diazepanylmethyl, diazepanylethyl, diazepanylpropyl, diazepanylbuytl, diazepan-1-yl, morpholinyl, morpholinylmethyl, morpholinylethyl, morpholinylpropyl, morpholinylbuytyl, morpholin-4-yl, 2-morpholin-4-yl-ethyl, 1,2,3,4-tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydro-isoquinolinylmethyl, 1,2,3,4-tetrahydro-isoquinolinylethyl, 1,2,3,4-tetrahydro-isoquinolinylpropyl, 1,2,3,4-tetrahydro-isoquinolinylbutyl, 1,2,3,4-tetrahydro-isoquinolin-7-yl, benzo[1,3]dioxolyl, benzo[1,3]dioxolylmethyl, benzo[1,3]dioxolylethyl, benzo[1,3]dioxolylpropyl, benzo[1,3]dioxolylbutyl, benzo[1,3]dioxol-5-yl, benzo[1,4]oxazinyl, benzo[1,4]oxazinylmethyl, benzo[1,4]oxazinylethyl, benzo[1,4]oxazinylpropyl, benzo[1,4]oxazinylbutyl, benzo[1,4]oxazin-6-yl”;
            where above substituents of substituents group (i)—if not hydrogen, nitrogen or sulphur—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-I, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-Cl, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
        
        
    
    


radical R4 independently is selected from the group consisting of:

    
    
        (i) “hydrogen, methyl, ethyl, propyl, isopropyl, tert-butyl, hexyl, allyl, propenyl, prop-2-en-1-yl, cyclopropyl, cyclopropylmethyl, cyclopropylethyl, cyclopropyl-propyl, cyclopropylbutyl, cyclopentyl, cyclopentylmethyl, cyclopentylethyl, cyclopentylpropyl, cyclopentylbutyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, cyclohexylbutyl, phenyl, naphthalenyl, naphthalen-1-yl, naphthalen-2-yl, benzyl, phenyl-ethyl, isoxazol, pyridinyl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyrazolyl, pyrazol-3-yl, pyrazol-4-yl, quinolinyl, quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-8-yl, thiophenyl, thiophen-2-yl, thiophen-3-yl, furanyl, furan-2-yl, furan-3-yl, pyrimidinyl, pyrimidin-5-yl, imidazolyl, imidazol-4-yl, imidazol-3-yl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-b]pyridin-5-yl, indolyl, 1H-indol-2-yl, dibenzofuranyl, dibenzofuran-4-yl, piperidinyl, piperidinylmethyl, piperidinylethyl, piperidinylpropyl, piperidinylbutyl, piperidin-1-yl, piperidin-3-yl, piperidin-4-yl, piperazinyl, piperazinylmethyl, piperazinylethyl, piperazinylpropyl, piperazinylbutyl, piperazin-1-yl, diazepanyl, diazepanylmethyl, diazepanylethyl, diazepanylpropyl, diazepanylbuytl, diazepan-1-yl, morpholinyl, morpholinyl-methyl, morpholinylethyl, morpholinylpropyl, morpholinylbuytyl, morpholin-4-yl, 2-morpholin-4-yl-ethyl, 1,2,3,4-tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydro-isoquinolinylmethyl, 1,2,3,4-tetrahydro-isoquinolinylethyl, 1,2,3,4-tetrahydro-isoquinolinylpropyl, 1,2,3,4-tetrahydro-isoquinolinylbutyl, 1,2,3,4-tetrahydro-isoquinolin-7-yl, benzo[1,3]dioxolyl, benzo[1,3]dioxolylmethyl, benzo[1,3]dioxolylethyl, benzo[1,3]dioxolylpropyl, benzo[1,3]dioxolylbutyl, benzo[1,3]dioxol-5-yl, benzo[1,4]oxazinyl, benzo[1,4]oxazinylmethyl, benzo[1,4]oxazinylethyl, benzo[1,4]oxazinylpropyl, benzo[1,4]oxazinylbutyl, benzo[1,4]oxazin-6-yl, —NH—Ry6” with Ry6 being selected from the group consisting of: “methyl, ethyl, propyl, isopropyl, tert-butyl, hexyl, allyl, propenyl, prop-2-en-1-yl, cyclopropyl, cyclopropylmethyl, cyclopropylethyl, cyclopropylpropyl, cyclopropylbutyl, cyclopentyl, cyclopentylmethyl, cyclopentylethyl, cyclopentylpropyl, cyclopentylbutyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, cyclohexylbutyl, phenyl, naphthalenyl, naphthalen-1-yl, naphthalen-2-yl, benzyl, phenyl-ethyl, isoxazol, pyridinyl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyrazolyl, pyrazol-3-yl, pyrazol-4-yl, quinolinyl, quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-8-yl, thiophenyl, thiophen-2-yl, thiophen-3-yl, furanyl, fu-ran-2-yl, furan-3-yl, pyrimidinyl, pyrimidin-5-yl, imidazolyl, imidazol-4-yl, imidazol-3-yl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-b]pyridin-5-yl, indolyl, 1H-indol-2-yl, dibenzofuranyl, dibenzofuran-4-yl, piperidinyl, piperidinylmethyl, piperidinylethyl, piperidinylpropyl, piperidinylbutyl, piperidin-1-yl, piperidin-3-yl, piperidin-4-yl, piperazinyl, piperazinylmethyl, piperazinylethyl, piperazinylpropyl, piperazinylbutyl, piperazin-1-yl, diazepanyl, diazepanylmethyl, diazepanylethyl, diazepanyl-propyl, diazepanylbuytl, diazepan-1-yl, morpholinyl, morpholinylmethyl, morpholinylethyl, morpholinylpropyl, morpholinylbuytyl, morpholin-4-yl, 2-morpholin-4-yl-ethyl, 1,2,3,4-tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydro-isoquinolinylmethyl, 1,2,3,4-tetrahydro-isoquinolinylethyl, 1,2,3,4-tetrahydro-isoquinolinylpropyl, 1,2,3,4-tetrahydro-isoquinolinylbutyl, 1,2,3,4-tetrahydro-isoquinolin-7-yl, benzo[1,3]dioxolyl, benzo[1,3]dioxolylmethyl, benzo[1,3]dioxolylethyl, benzo[1,3]dioxolylpropyl, benzo[1,3]dioxolylbutyl, benzo[1,3]dioxol-5-yl, benzo[1,4]oxazinyl, benzo[1,4]oxazinylmethyl, benzo[1,4]oxazinylethyl, benzo[1,4]oxazinylpropyl, benzo[1,4]oxazinylbutyl, benzo[1,4]oxazin-6-yl”;
        
            where above substituents of substituents group (i)—if not hydrogen or nitrogen—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-I, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-C1, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
        
        
    
    


radical R5 independently is selected from the group consisting of:

    
    
        (i) “hydrogen, methyl, ethyl, propyl, isopropyl, tert-butyl, hexyl, allyl, propenyl, prop-2-en-1-yl, cyclopropyl, cyclopropylmethyl, cyclopropylethyl, cyclopropylpropyl, cyclopropylbutyl, cyclopentyl, cyclopentylmethyl, cyclopentylethyl, cyclopentylpropyl, cyclopentylbutyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, cyclohexylbutyl, phenyl, naphthalenyl, naphthalen-1-yl, naphthalen-2-yl, benzyl, phenyl-ethyl, isoxazol, pyridinyl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyrazolyl, pyrazol-3-yl, pyrazol-4-yl, quinolinyl, quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-8-yl, thiophenyl, thiophen-2-yl, thiophen-3-yl, furanyl, furan-2-yl, furan-3-yl, pyrimidinyl, pyrimidin-5-yl, imidazolyl, imidazol-4-yl, imidazol-3-yl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-b]pyridin-5-yl, indolyl, 1H-indol-2-yl, dibenzofuranyl, dibenzofuran-4-yl, piperidinyl, piperidinylmethyl, piperidinylethyl, piperidinylpropyl, piperidinylbutyl, piperidin-1-yl, piperidin-3-yl, piperidin-4-yl, piperazinyl, piperazinylmethyl, piperazinylethyl, piperazinylpropyl, piperazinylbutyl, piperazin-1-yl, diazepanyl, diazepanylmethyl, diazepanylethyl, diazepanylpropyl, diazepanylbuytl, diazepan-1-yl, morpholinyl, morpholinyl-methyl, morpholinylethyl, morpholinylpropyl, morpholinylbuytyl, morpholin-4-yl, 2-morpholin-4-yl-ethyl, 1,2,3,4-tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydro-isoquinolinylmethyl, 1,2,3,4-tetrahydro-isoquinolinylethyl, 1,2,3,4-tetrahydro-isoquinolinylpropyl, 1,2,3,4-tetrahydro-isoquinolinylbutyl, 1,2,3,4-tetrahydro-isoquinolin-7-yl, benzo[1,3]dioxolyl, benzo[1,3]dioxolylmethyl, benzo[1,3]dioxolylethyl, benzo[1,3]dioxolylpropyl, benzo[1,3]dioxolylbutyl, benzo[1,3]dioxol-5-yl, benzo[1,4]oxazinyl, benzo[1,4]oxazinylmethyl, benzo[1,4]oxazinylethyl, benzo[1,4]oxazinylpropyl, benzo[1,4]oxazinylbutyl, benzo[1,4]oxazin-6-yl;
        
            where above substituents of substituents group (i)—if not hydrogen or nitrogen—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-I, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-Cl, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
        
        
    
    


In another preferred embodiment, pyrido[2,3-b]pyrazine derivatives according to above general formula (I) and preferred embodiments and subsets are provided, wherein:
radical R1 independently is selected from the group consisting of:

    
    
        (i) “—NH—C(O)—NH2, —NH—C(S)—NH2, —NH—C(O)—NH-alkyl, —NH—C(O)—NH—(C9-C30)alkyl, —NH—C(O)—NH-cycloalkyl, —NH—C(O)—NH-cycloalkylalkyl, —NH—C(O)—NH-aryl, —NH—C(O)—NH-arylalkyl, —NH—C(O)—NH-heteroaryl, —NH—C(O)—NH-heteroarylalkyl, —NH—C(O)—NH-heterocyclyl, —NH—C(O)—NH-heterocyclylalkyl, —NH—C(S)—NH-alkyl, —NH—C(S)—NH—(C9-C30)alkyl, —NH—C(S)—NH-cycloalkyl, —NH—C(S)—NH-cycloalkylalkyl, —NH—C(S)—NH-aryl, —NH—C(S)—NH-arylalkyl, —NH—C(S)—NH-heteroaryl, —NH—C(S)—NH-heteroarylalkyl, —NH—C(S)—NH-heterocyclyl, —NH—C(S)—NH-heterocyclylalkyl, —NH—C(O)-alkyl, —NH—C(O)—(C9-C30)alkyl, —NH—C(O)-cycloalkyl, —NH—C(O)-cycloalkylalkyl, —NH—C(O)-aryl, —NH—C(O)-arylalkyl, —NH—C(O)-heteroaryl, —NH—C(O)-heteroarylalkyl, —NH—C(O)-heterocyclyl, —NH—C(O)—heterocyclylalkyl, —NH—C(S)-alkyl, —NH—C(S)—(C9-C30)alkyl, —NH—C(S)-cycloalkyl, —NH—C(S)-cycloalkylalkyl, —NH—C(S)-aryl, —NH—C(S)-arylalkyl, —NH—C(S)-heteroaryl, —NH—C(S)-heteroarylalkyl, —NH—C(S)-heterocyclyl, —NH—C(S)-heterocyclylalkyl”;
        
            where above substituents of substituents group (i)—if not hydrogen, nitrogen or sulphur—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-1, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-Cl, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
        
        
    
    


radical R2 independently is “hydrogen”;
radical R3 independently is selected from the group consisting of:

    
    
        (i) “alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, —NH-alkyl, —NH—(C9-C30)alkyl, —NH-cycloalkyl, —NH-cycloalkylalkyl, —NH-aryl, —NH-arylalkyl, —NH-heteroaryl, —NH-heteroarylalkyl, —NH-heterocyclyl, —NH-heterocyclylalkyl”;
        
            where above substituents of substituents group (i)—if not hydrogen or nitrogen—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-I, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-Cl, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
        
        
    
    


radical R4 independently is selected from the group consisting of:

    
    
        (i) “hydrogen, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, —NH-alkyl, —NH—(C9-C30)alkyl, —NH-cycloalkyl, —NH-cycloalkylalkyl, —NH-aryl, —NH-arylalkyl, —NH-heteroaryl, —NH-heteroarylalkyl, —NH-heterocyclyl, —NH-heterocyclylalkyl”;
        
            where above substituents of substituents group (i)—if not hydrogen or nitrogen—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-I, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-Cl, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
        
        
    
    


radical R5 independently is “hydrogen”.
In yet another preferred embodiment, pyrido[2,3-b]pyrazine derivatives according to above general formula (I) and preferred embodiments and subsets are provided, wherein:
radical R1 independently is selected from the group consisting of:

    
    
        (i) “—NH—C(O)—NH2, —NH—C(S)—NH2, —NH—C(O)—NH—Rz1, —NH—C(S)—NH—Rz2, —NH—C(O)—Ry3, —NH—C(S)—NH—Rz4”, with Rz1, Rz2, Rz3, Rz4 independently from each other being selected from the group consisting of: “methyl, ethyl, propyl, isopropyl, tert-butyl, hexyl, allyl, propenyl, prop-2-en-1-yl, cyclopropyl, cyclopropylmethyl, cyclopropylethyl, cyclopropylpropyl, cyclopropylbutyl, cyclopentyl, cyclopentylmethyl, cyclopentylethyl, cyclopentylpropyl, cyclopentylbutyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, cyclohexylbutyl, phenyl, naphthalenyl, naphthalen-1-yl, naphthalen-2-yl, benzyl, phenyl-ethyl, isoxazol, pyridinyl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyrazolyl, pyrazol-3-yl, pyrazol-4-yl, quinolinyl, quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-8-yl, thiophenyl, thiophen-2-yl, thiophen-3-yl, furanyl, furan-2-yl, furan-3-yl, pyrimidinyl, pyrimidin-5-yl, imidazolyl, imidazol-4-yl, imidazol-3-yl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-b]pyridin-5-yl, indolyl, 1H-indol-2-yl, dibenzofuranyl, dibenzofuran-4-yl, piperidinyl, piperidinylmethyl, piperidinylethyl, piperidinylpropyl, piperidinylbutyl, piperidin-1-yl, piperidin-3-yl, piperidin-4-yl, piperazinyl, piperazinylmethyl, piperazinylethyl, piperazinylpropyl, piperazinylbutyl, piperazin-1-yl, diazepanyl, diazepanylmethyl, diazepanylethyl, diazepanylpropyl, diazepanylbuytl, diazepan-1-yl, morpholinyl, morpholinylmethyl, morpholinylethyl, morpholinylpropyl, morpholinylbuytyl, morpholin-4-yl, 2-morpholin-4-yl-ethyl, 1,2,3,4-tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydro-isoquinolinylmethyl, 1,2,3,4-tetrahydro-isoquinolinylethyl, 1,2,3,4-tetrahydro-isoquinolinylpropyl, 1,2,3,4-tetrahydro-isoquinolinylbutyl, 1,2,3,4-tetrahydro-isoquinolin-7-yl, benzo[1,3]dioxolyl, benzo[1,3]dioxolylmethyl, benzo[1,3]dioxolylethyl, benzo[1,3]dioxolylpropyl, benzo[1,3]dioxolylbutyl, benzo[1,3]dioxol-5-yl, benzo[1,4]oxazinyl, benzo[1,4]oxazinylmethyl, benzo[1,4]oxazinylethyl, benzo[1,4]oxazinylpropyl, benzo[1,4]oxazinylbutyl, benzo[1,4]oxazin-6-yl”;
        
            where above substituents of substituents group (i)—if not hydrogen, nitrogen or sulphur—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-C1, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-I, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-C1, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
        
        
    
    


radical R2 independently is “hydrogen”;
radical R3 independently is selected from the group consisting of:

    
    
        (i) “methyl, ethyl, propyl, isopropyl, tert-butyl, hexyl, allyl, propenyl, prop-2-en-1-yl, cyclopropyl, cyclopropylmethyl, cyclopropylethyl, cyclopropylpropyl, cyclopropylbutyl, cyclopentyl, cyclopentylmethyl, cyclopentylethyl, cyclopentylpropyl, cyclopentylbutyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, cyclohexylbutyl, phenyl, naphthalenyl, naphthalen-1-yl, naphthalen-2-yl, benzyl, phenyl-ethyl, isoxazol, pyridinyl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyrazolyl, pyrazol-3-yl, pyrazol-4-yl, quinolinyl, quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-8-yl, thiophenyl, thiophen-2-yl, thiophen-3-yl, furanyl, furan-2-yl, furan-3-yl, pyrimidinyl, pyrimidin-5-yl, imidazolyl, imidazol-4-yl, imidazol-3-yl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-b]pyridin-5-yl, indolyl, 1H-indol-2-yl, dibenzofuranyl, dibenzofuran-4-yl, piperidinyl, piperidinylmethyl, piperidinylethyl, piperidinylpropyl, piperidinylbutyl, piperidin-1-yl, piperidin-3-yl, piperidin-4-yl, piperazinyl, piperazinylmethyl, piperazinylethyl, piperazinylpropyl, piperazinylbutyl, piperazin-1-yl, diazepanyl, diazepanylmethyl, diazepanylethyl, diazepanylpropyl, diazepanylbuytl, diazepan-1-yl, morpholinyl, morpholinylmethyl, morpholinylethyl, morpholinylpropyl, morpholinylbuytyl, morpholin-4-yl, 2-morpholin-4-yl-ethyl, 1,2,3,4-tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydro-isoquinolinylmethyl, 1,2,3,4-tetrahydro-isoquinolinylethyl, 1,2,3,4-tetrahydro-isoquinolinylpropyl, 1,2,3,4-tetrahydro-isoquinolinylbutyl, 1,2,3,4-tetrahydro-isoquinolin-7-yl, benzo[1,3]dioxolyl, benzo[1,3]dioxolylmethyl, benzo[1,3]dioxolylethyl, benzo[1,3]dioxolylpropyl, benzo[1,3]dioxolylbutyl, benzo[1,3]dioxol-5-yl, benzo[1,4]oxazinyl, benzo[1,4]oxazinylmethyl, benzo[1,4]oxazinylethyl, benzo[1,4]oxazinylpropyl, benzo[1,4]oxazinylbutyl, benzo[1,4]oxazin-6-yl, —NH—Rz5” with Rz5 being selected from the group consisting of: “methyl, ethyl, propyl, isopropyl, tert-butyl, hexyl, allyl, propenyl, prop-2-en-1-yl, cyclopropyl, cyclopropylmethyl, cyclopropylethyl, cyclopropylpropyl, cyclopropylbutyl, cyclopentyl, cyclopentylmethyl, cyclopentylethyl, cyclopentylpropyl, cyclopentylbutyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, cyclohexylbutyl, phenyl, naphthalenyl, naphthalen-1-yl, naphthalen-2-yl, benzyl, phenyl-ethyl, isoxazol, pyridinyl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyrazolyl, pyrazol-3-yl, pyrazol-4-yl, quinolinyl, quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-8-yl, thiophenyl, thiophen-2-yl, thiophen-3-yl, furanyl, furan-2-yl, furan-3-yl, pyrimidinyl, pyrimidin-5-yl, imidazolyl, imidazol-4-yl, imidazol-3-yl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-b]pyridin-5-yl, indolyl, 1H-indol-2-yl, dibenzofuranyl, dibenzofuran-4-yl, piperidinyl, piperidinylmethyl, piperidinylethyl, piperidinylpropyl, piperidinylbutyl, piperidin-1-yl, piperidin-3-yl, piperidin-4-yl, piperazinyl, piperazinylmethyl, piperazinylethyl, piperazinylpropyl, piperazinylbutyl, piperazin-1-yl, diazepanyl, diazepanylmethyl, diazepanylethyl, diazepanylpropyl, diazepanylbuytl, diazepan-1-yl, morpholinyl, morpholinylmethyl, morpholinylethyl, morpholinylpropyl, morpholinylbuytyl, morpholin-4-yl, 2-morpholin-4-yl-ethyl, 1,2,3,4-tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydro-isoquinolinylmethyl, 1,2,3,4-tetrahydro-isoquinolinylethyl, 1,2,3,4-tetrahydro-isoquinolinylpropyl, 1,2,3,4-tetrahydro-isoquinolinylbutyl, 1,2,3,4-tetrahydro-isoquinolin-7-yl, benzo[1,3]dioxolyl, benzo[1,3]dioxolylmethyl, benzo[1,3]dioxolylethyl, benzo[1,3]dioxolylpropyl, benzo[1,3]dioxolylbutyl, benzo[1,3]dioxol-5-yl, benzo[1,4]oxazinyl, benzo[1,4]oxazinylmethyl, benzo[1,4]oxazinylethyl, benzo[1,4]oxazinylpropyl, benzo[1,4]oxazinylbutyl, benzo[1,4]oxazin-6-yl”;
        
            where above substituents of substituents group (i)—if not hydrogen or nitrogen—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-1, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-C1, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
        
        
    
    


radical R4 independently is selected from the group consisting of:

    
    
        (i) “hydrogen, methyl, ethyl, propyl, isopropyl, tert-butyl, hexyl, allyl, propenyl, prop-2-en-1-yl, cyclopropyl, cyclopropylmethyl, cyclopropylethyl, cyclopropyl-propyl, cyclopropylbutyl, cyclopentyl, cyclopentylmethyl, cyclopentylethyl, cyclopentylpropyl, cyclopentylbutyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, cyclohexylbutyl, phenyl, naphthalenyl, naphthalen-1-yl, naphthalen-2-yl, benzyl, phenyl-ethyl, isoxazol, pyridinyl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyrazolyl, pyrazol-3-yl, pyrazol-4-yl, quinolinyl, quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-8-yl, thiophenyl, thiophen-2-yl, thiophen-3-yl, furanyl, furan-2-yl, furan-3-yl, pyrimidinyl, pyrimidin-5-yl, imidazolyl, imidazol-4-yl, imidazol-3-yl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-b]pyridin-5-yl, indolyl, 1H-indol-2-yl, dibenzofuranyl, dibenzofuran-4-yl, piperidinyl, piperidinylmethyl, piperidinylethyl, piperidinylpropyl, piperidinylbutyl, piperidin-1-yl, piperidin-3-yl, piperidin-4-yl, piperazinyl, piperazinylmethyl, piperazinylethyl, piperazinylpropyl, piperazinylbutyl, piperazin-1-yl, diazepanyl, diazepanylmethyl, diazepanylethyl, diazepanylpropyl, diazepanylbuytl, diazepan-1-yl, morpholinyl, morpholinyl-methyl, morpholinylethyl, morpholinylpropyl, morpholinylbuytyl, morpholin-4-yl, 2-morpholin-4-yl-ethyl, 1,2,3,4-tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydro-isoquinolinylmethyl, 1,2,3,4-tetrahydro-isoquinolinylethyl, 1,2,3,4-tetrahydro-isoquinolinylpropyl, 1,2,3,4-tetrahydro-isoquinolinylbutyl, 1,2,3,4-tetrahydro-isoquinolin-7-yl, benzo[1,3]dioxolyl, benzo[1,3]dioxolylmethyl, benzo[1,3]dioxolylethyl, benzo[1,3]dioxolylpropyl, benzo[1,3]dioxolylbutyl, benzo[1,3]dioxol-5-yl, benzo[1,4]oxazinyl, benzo[1,4]oxazinylmethyl, benzo[1,4]oxazinylethyl, benzo[1,4]oxazinylpropyl, benzo[1,4]oxazinylbutyl, benzo[1,4]oxazin-6-yl”;
        
            where above substituents of substituents group (i)—if not hydrogen or nitrogen—may, optionally, additionally be substituted with at least one substituent selected from the group consisting of: “—F, —Cl, —Br, —I, —CN, —CF3, —N3, —NH2, —NO2, —OH, ═O, —OCF3, —OCHF2, —SH, —O—SO3H, —OP(O)(OH)2, —CHO, —COOH, —C(O)NH2, —SO3H, —P(O)(OH)2, —NHC(O)—NH2, —C(NH)—NH2, —C(O)—C(O)—NH2, —C(O)—CF3, alkyl, (C9-C30)alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkyl-OH, alkyl-CN, alkyl-COOH, alkyl-P(O)(O-alkyl)2, cycloalkyl-CN, aryl-OH, aryl(—OH)(-alkyl), —C(O)-alkyl, —C(O)-heterocyclyl, —C(O)—O-alkyl, —C(O)—O-heterocyclyl, —P(O)(O-alkyl-O—C(O)-alkyl)2, —OP(O)(O-alkyl)2, —OS(O2)-alkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-arylalkyl, —O-heterocyclyl, —O-heterocyclylalkyl, —O-arylalkyl-(O-alkyl)2, —O-alkyl-O-alkyl, —O-alkyl-N(alkyl)2, —O-alkyl-halogen, —O-alkyl-Cl, —O-alkyl-F, —O-alkyl-Br, —O-alkyl-1, —OC(O)-alkyl, —OC(O)—N(alkyl)2, —OC(O)—NH-alkyl, —OC(O)—(C9-C30)alkyl, —OC(O)—O-alkyl, —OC(O)—O-alkyl-O-alkyl, —OC(O)—O-aryl, —N(alkyl)2, —N(aryl)2, —NHC(O)-alkyl, —NHC(O)-alkyl-NH-alkyl, —NHC(O)-alkyl-C(O)—O-alkyl, —NHC(O)—O-alkyl, —NHC(O)—O-alkyl-O-alkyl, —NHC(O)—O-alkyl-O-alkyl-O-alkyl-O-alkyl, —NHC(O)—NH-alkyl, —NHC(O)—NH-aryl, —NHC(O)—NH-heteroaryl, —NHC(O)—NH-heterocyclyl, —NHC(O)—NH-heterocyclylalkyl, —NHC(O)—NH-alkyl-halogen, —NHC(O)—NH-alkyl-Cl, —NHC(O)—N(alkyl)2, —NHS(O2)-alkyl”;
        
        
    
    


radical R5 independently is “hydrogen”.
In another preferred embodiment, pyrido[2,3-b]pyrazine derivatives according to general formula (I) and above preferred embodiments and subsets are provided that are selected from the group consisting of:












Com-




pound
Structure
Name







 1




1-Ethyl-3-(6-p- tolylamino-pyrido[2,3- b]pyrazin-3-yl)-urea


 


 2




1-[6-(4-Amino-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


 3




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-phenyl-urea


 


 4




1-Ethyl-3-(6-phenyl- pyrido[2,3-b]pyrazin- 3-yl)-urea


 


 5




1-Ethyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


 6




1-[6-(4-Chloro- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3- ethyl-urea


 


 7




1-Ethyl-3-(6-pyridin- 4-yl-pyrido[2,3- b]pyrazin-3-yl)-urea


 


 8




1-[6-(3-Chloro-4- hydroxy-5-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3- ethyl-urea


 


 9




1-[6-(3,5-Dichloro-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


 10




1-Ethyl-3-[6-(1- methyl-1H-pyrazol-4- yl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


 11




1-Ethyl-3-[6-(4- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


 12




1-Ethyl-3-[6-(3- isopropoxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


 13




1-Ethyl-3-(6- phenylamino- pyrido[2,3-b]pyrazin- 3-yl)-urea


 


 14




1-Phenyl-3-(6- phenylamino- pyrido[2,3-b]pyrazin- 3-yl)-urea


 


 15




1-[6-(3,5-Dichloro-4- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


 16




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-propyl-urea


 


 17




1-Cyclohexyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


 18




1-Allyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


 19




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-isopropyl-urea


 


 20




1-Cyclopentyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


 21




1-Ethyl-3-[6-(4- hydroxy-3-methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


 22




1-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3- ethyl-urea


 


 23




1-Ethyl-3-[6-(3,4,5- trimethoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


 24




1-Ethyl-3-[6-(4- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


 25




1-Ethyl-3-(6-p- tolylamino-pyrido[2,3- b]pyrazin-3-yl)- thiourea


 


 26




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-phenethyl- urea


 


 27




1-(3,5-Dimethyl- isoxazol-4-yl)-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


 28




1-tert-Butyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


 29




1-Benzyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


 30




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-1-[1-(2,2,2- trifluoro-acetyl)- piperidin-4-yl]-urea


 


 31




1-[6-(3-Chloro-4- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


 32




1-Ethyl-3-[6-(quinolin- 3-ylamino)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


 33




2,2-Dimethyl- propionic acid(2,2- dimethyl- propionyloxymeth- oxy)-[4-(3-{3-[4-(2,2- dimethyl-propionyl- oxy)-3-methoxy- phenyl]-pyrido[2,3- b]pyrazin-6-yl}- ureido)-butyl]- phosphinoyloxy- methyl ester


 


 34




Phosphoric acid di- ethyl ester 4-[6-(3- ethyl-ureido)- pyrido[2,3-b]-pyrazin- 3-yl]-2-methoxy- phenyl ester


 


 35




1-Ethyl-3-[3-(4- methyl-3,4-dihydro- 2H-benzo[1,4]oxazin- 6-yl)-pyrido[2, 3-b]pyrazin-6-yl]-urea


 


 36




N-[3-(3-Isopropoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-acetamide


 


 37




Methanesulfonic acid 2-chloro-4-[6-(3-ethyl- ureido)-pyrido[2,3- b]pyrazin-3-yl]-6- methoxy-phenyl ester


 


 38




[3-(3-Isopropoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-carbamic acid ethyl ester


 


 39




1-{3-[4-(2-Chloro- ethoxy)-3-methoxy- phenyl]-pyrido[2,3- b]pyrazin-6-yl}- 3-ethyl-urea


 


 40




{4-[6-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-yl]-2-methoxy- phenyl}-carbamic acid 2-methoxy-ethyl ester


 


 41




Phosphoric acid mono-{4-[6-(3-ethyl- ureido)-pyrido-[2,3- b]pyrazin-3-yl]-2- methoxy-phenyl} es- ter; sodium salt


 


 42




1-[3-(2,2-Difluoro- benzo[1,3]dioxol-5- ylamino)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


 43




Methanesulfonic acid 4-[6-(3-ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-yl]-2-methoxy- phenyl ester


 


 44




{4-[6-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-yl]-2-methoxy- phenyl}-carbamic acid 2-[2-(2-methoxy- ethoxy)-ethoxy]-ethyl ester


 


 45




{3-[6-(3-Ethyl-ureido)- pyrido[2,3-b]-pyrazin- 3-ylamino]-phenyl}- acetic acid


 


 46




1-Ethyl-3-[3-(3- hydroxy-4-methoxy- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


 47




1-[3-(3-Bromo-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


 48




1-Ethyl-3-{3-[4- (morpholine-4- carbonyl)- phenylamino]- pyrido[2,3-b]-pyrazin- 6-yl}-urea


 


 49




1-Cyclopropyl-3-[3- (3-isopropoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


 50




5-[6-(3-Ethyl-ureido)- pyrido[2,3-b]-pyrazin- 3-ylamino]-2-hydroxy- benzoic acid methyl ester


 


 51




1-Ethyl-3-[3-(2- isopropoxy-pyridin-3- yl)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


 52




1-Ethyl-3-[3-(2H- pyrazol-3-yl)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


 53




1-Ethyl-3-[3-(3- methyl-3H-imidazol- 4-yl)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


 54




Acetic acid 4-[6-(3- ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-yl]-2-methoxy- phenyl ester


 


 55




1-Ethyl-3-[3-(2- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


 56




1-Ethyl-3-[3-(3- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


 57




1-[3-(2-Benzyloxy- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


 58




1-[3-(1-Benzyl-1H- pyrazol-4-yl)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


 59




1-Ethyl-3-[3-(1- isobutyl-1H-pyrazol- 4-yl)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


 60




1-Ethyl-3-{3-[1-(2- morpholin-4-yl-ethyl)- 1H-pyrazol-4-yl]- pyrido[2,3-b]pyrazin- 6-yl}-urea


 


 61




1-Ethyl-3-[3-(1H- pyrrolo[2,3-b]pyridin- 5-yl)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


 62




1-Ethyl-3-[3-(2- isobutoxy-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


 63




1-Ethyl-3-{3-[3- methoxy-4-(3- morpholin-4-yl- propoxy)-phenyl]- pyrido[2,3-b]pyrazin- 6-yl}-urea


 


 64




1-Ethyl-3-(3- phenylamino-pyrido- [2,3-b]pyrazin-6-yl)- urea


 


 65




1-[3-(3-Isopropoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-(4-morpholin- 4-yl-butyl)-urea


 


 66




2-Acetylamino-N-(3- p-tolylamino-pyr- ido[2,3-b]pyrazin-6- yl)-acetamide


 


 67




1-[3-(3-Bromo-2- isoporopoxy-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


 68




1-[3-(2,3-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


 70




1-Ethyl-3-[3-(1H- indol-2-yl)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


 71




1-(3-Dibenzofuran-4- yl-pyrido[2,3- b]pyrazin-6-yl)-3- ethyl-urea


 


 72




1-[3-(2-Amino- pyrimidin-5-yl)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


 73




1-[3-(3- Difluoromethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


 74




1-{3-[4-(1,1-Dioxo- 1lambda*6*- thiomorpholin-4- ylmethyl)- phenylamino]- pyrido[2,3-b]pyrazin- 6-yl}-3-ethyl-urea


 


 75




1-Ethyl-3-[3-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-6-yl]- thiourea


 


 76




N-{4-[6-(3-Ethyl- ureido)-pyrido[2,3- b]pyrazin-3-yl]- phenyl}-succinamic acid methyl ester


 


 77




N-{4-[6-(3-Ethyl- ureido)-pyrido[2,3- b]pyrazin-3-yl]-2- methoxy-phenyl}- acetamide


 


 78




1-[3-(4-Amino-3-nitro- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


 79




1-[3-(5-Acetyl-2- fluoro-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


 80




1-Ethyl-3-[3-(4- methoxy-3,5- dimethyl-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


 81




1-Ethyl-3-[3-(3,4,5- trifluoro-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


 82




1-[3-(3,5-Dimethyl- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


 83




1-Ethyl-3-[3-(3-fluoro- 4-methyl-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


 84




1-Ethyl-3-[3-(3-fluoro- biphenyl-4-yl)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


 85




1-Ethyl-3-[3-(4- methyl-3-nitro- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


 86




1-Ethyl-3-[3-(4- hydroxy-3-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


 87




4-[6-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-2- methoxy-benzoic acid methyl ester


 


 88




1,1′-(3,3′-(4-(2- (dimethyl- amino)ethoxy)phenyl azanediyl)bis(pyrido [2,3-b]pyrazin-6,3- diyl))bis(3-ethylurea)


 


 89




1-Ethyl-3-[3-(3- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


 90




1-[3-(3,5-Dichloro- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


 91




1-[3-(5-Chloro-2- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


 92




1-[3-(2,5-Dichloro- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


 93




1-Ethyl-3-[3-(5-fluoro- 2-methoxy-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


 94




1-[3-(3-Bromo-5- methyl-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


 95




1-[3-(3,4-Difluoro- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


 96




1-[3-(5-Chloro-2- fluoro-3-methyl- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


 97




1-Ethyl-3-[3-(2- trifluoromethyl- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


 98




1-Ethyl-3-[3-(4- methoxy-2-methyl- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


 99




1-[3-(3-Chloro-2- fluoro-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


100




1-Ethyl-3-(3-m-tolyl- pyrido[2,3-b]pyrazin- 6-yl)-urea


 


101




1-Ethyl-3-[3-(3-nitro- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


102




1-[3-(2-Ethoxy- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


103




1-Ethyl-3-[3-(2-fluoro- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


104




1-[3-(2-Chloro- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


105




1-Ethyl-3-(3-o-tolyl- pyrido[2,3-b]pyrazin- 6-yl)-urea


 


106




1-Ethyl-3-[3-(5-fluoro- 2-methyl-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


107




1-[3-(2,3-Dimethyl- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


108




1-[3-(2,3-Dichloro- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


109




1-[3-(2-Benzyloxy-3- bromo-5-methyl- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


110




1-[3-(3-Bromo-2- methoxy-5-methyl- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


111




1-[3-(3-Chloro- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


112




1-[3-(2-Ethoxy-4- fluoro-phenyl)-pyr- ido[2,3-b]pyrazin-6- yl]-3-ethyl-urea


 


113




1-Ethyl-3-[3-(1- methyl-1H-pyrazol-4- yl)-pyrido[2,3- b]pyrazin-6-yl]- thiourea


 


114




1-[3-(3-Cyano- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


115




1-Ethyl-3-[3-(3- hydroxymethyl- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


116




1-(3-Biphenyl-3-yl- pyrido[2,3-b]pyrazin- 6-yl)-3-ethyl-urea


 


117




1-Ethyl-3-[3-(3- methylsulfanyl- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


118




1-Ethyl-3-[3-(3- trifluoromethoxy- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


119




3-[6-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-yl]-benzoic acid ethyl ester


 


120




N-{3-[6-(3-Ethyl- ureido)-pyrido[2,3- b]pyrazin-3-yl]- phenyl}- methanesulfonamide


 


121




1-{3-[3-(3,5- Dimethoxy- benzyloxy)-phenyl]- pyrido[2,3-b]pyrazin- 6-yl}-3-ethyl-urea


 


122




1-[3-(4-Chloro- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


123




1-(3-Biphenyl-4-yl- pyrido[2,3-b]pyrazin- 6-yl)-3-ethyl-urea


 


124




1-Ethyl-3-(3-p-tolyl- pyrido[2,3-b]pyrazin- 6-yl)-thiourea


 


125




1-Ethyl-3-[3-(4- hydroxy-3,5-dimethyl- phenyl)-pyrido[2,3- b]pyrazin-6-yl]- thiourea


 


126




1-Ethyl-3-(3-p- tolylamino-pyrido[2,3- b]pyrazin-6-yl)- thiourea


 


127




1-Ethyl-3-[3-(3- isopropoxy-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


128




1-[3-(4- Diphenylamino- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


129




1-Ethyl-3-[3-(3-fluoro- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


130




1-[3-(3-Ethoxy- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


131




1-Ethyl-3-[3-(4-nitro- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


132




4-[6-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-yl]-benzoic acid methyl ester


 


133




1-Ethyl-3-[3-(4- propoxy-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


134




1-Ethyl-3-[3-(3,4,5- trimethoxy-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


135




1-Ethyl-3-[3-(2- methylsulfanyl- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


136




1-[3-(3-Cyano- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


137




1-[3-(2-Chloro-6- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


138




1-[3-(3,5-Dichloro-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


139




1-[3-(3-Chloro-4- hydroxy-5-methoxy- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-thiourea


 


140




1-[3-(4-Amino-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


141




1-Ethyl-3-(3- thiophen-3-yl- pyrido[2,3-b]pyrazin- 6-yl)-urea


 


142




1-[3-(3,4-Dimethyl- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


143




4-[6-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-yl]-2-fluoro-benzoic acid methyl ester


 


144




1-[3-(3- Dimethylamino- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


145




1-[3-(2,5-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


146




1-[3-(3-Ethoxy-2- fluoro-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


147




1-Ethyl-3-[3-(3- hydroxy-4-methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


148




1-Ethyl-3-(3- phenylamino- pyrido[2,3-b]pyrazin- 6-yl)-thiourea


 


149




1-Ethyl-3-[3-(2- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


150




1-Ethyl-3-[3-(4- hydroxy-3-methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


151




1-Ethyl-3-[3-(3,4,5- trimethyl-phenyl)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


152




1-Ethyl-3-(3- thiophen-2-yl- pyrido[2,3-b]pyrazin- 6-yl)-urea


 


153




1-Ethyl-3-[3-(2- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


154




1-Ethyl-3-[3-(3- hydroxymethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


155




1-Ethyl-3-[3-(3- phenoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


156




1-Ethyl-3-[3-(3- hydroxy-4-methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


157




1-[3-(3,5-Dimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-ethyl-thiourea


 


158




1-[3-(3-Chloro-4- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


159




1-[3-(3-Chloro-4- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


160




1-Ethyl-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


161




1-Ethyl-3-[3-(4- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


162




1-Ethyl-3-[3-(3- methoxy-4-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


163




1-Ethyl-3-[3-(3- isopropoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


164




1-Ethyl-3-[3-(4- [1,2,4]triazol-1-yl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


165




N-{5-[6-(3-Ethyl- thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-2-methyl- phenyl}- methanesulfonamide


 


166




1-[3-(3,5-Dichloro-4- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


167




1-[3-(3-Chloro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


168




1-Ethyl-3-[3- (naphthalen-2- ylamino)-pyrido[2,3- b]pyrazin-6-yl]- thiourea


 


169




1-[3-(4- Dimethylamino- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


170




1-[3-(3-Acetyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


171




[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


172




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-methyl-urea


 


173




1-(2-Chloro-ethyl)-3- [6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


174




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(2-morpholin- 4-yl-ethyl)-urea


 


175







 


176




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-pyridin-4-yl- urea


 


177




1-Ethyl-3-[6-(3- isopropoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


178




1-Ethyl-3-(6-p-tolyl- pyrido[2,3-b]pyrazin- 3-yl)-urea


 


179




1-[6-(3-Amino- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3- ethyl-urea


 


180




1-[6-(3-Amino-4- methyl-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


181




1-Ethyl-3-[6-(4- hydroxy-3,5-dimethyl- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


182




1-Ethyl-3-[6-(4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


183




1-[6-(5-Acetyl- thiophen-2-yl)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


184




1-[6-(5-Acetyl- thiophen-2-yl)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-thiourea


 


185




1-Ethyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- thiourea


 


186




1-[6-(3,5-Dichloro-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-thiourea


 


187




1-[6-(3-Chloro-4- hydroxy-5-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3- ethyl-thiourea


 


188




1-Ethyl-3-[6-(3- isopropoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


189




1-Ethyl-3-(6-p-tolyl- pyrido[2,3-b]pyrazin- 3-yl)-thiourea


 


190




1-Ethyl-3-[6-(4- hydroxy-3,5-dimethyl- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- thiourea


 


191




1-Ethyl-3-[6-(3,4,5- trimethoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


192




1-[6-(4-Amino-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-thiourea


 


193




1-Ethyl-3-[6-(1- methyl-1H-pyrazol-4- yl)-pyrido[2,3- b]pyrazin-3-yl]- thiourea


 


194




{3-[3-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 6-ylamino]-phenyl}- acetic acid


 


195




{3-[3-(3-Ethyl- thioureido)- pyrido[2,3-b]pyrazin- 6-ylamino]-phenyl}- acetic acid


 


196




1-Ethyl-3-[6-(2- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


197




1-Ethyl-3-[6-(2- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


198




1-Ethyl-3-[6-(4- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


199




1-Ethyl-3-[6-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


200




1-Ethyl-3-[6-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


201




1-[6-(3-Chloro-4- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


202




1-[6-(3-Chloro-4- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-thiourea


 


203




1-Ethyl-3-[6-(4- hydroxy-3-methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


204




1-Ethyl-3-[6-(3- hydroxy-4-methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


205




1-Ethyl-3-[6-(3- hydroxy-4-methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


206




N-{5-[3-(3-Ethyl- ureido)-pyrido[2,3- b]pyrazin-6-ylamino]- 2-methyl-phenyl}- methanesulfonamide


 


207




N-{5-[3-(3-Ethyl- thioureido)- pyrido[2,3-b]pyrazin- 6-ylamino]-2-methyl- phenyl}- methanesulfonamide


 


208




1-[6-(3-Chloro-4- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-thiourea


 


209




1-Ethyl-3-[6-(3- methoxy-4-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


210




1-Ethyl-3-[6-(3- methoxy-4-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


211




1-[6-(3-Amino-5- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


212




1-[6-(3-Amino-5- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-thiourea


 


213




1-Ethyl-3-[6-(quinolin- 3-ylamino)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


214




1-Ethyl-3-[6- (naphthalen-2- ylamino)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


215




1-Ethyl-3-[6- (naphthalen-2- ylamino)-pyrido[2,3- b]pyrazin-3-yl]- thiourea


 


216




1-[6-(4-Chloro- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


217




1-[6-(4-Chloro- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-thiourea


 


218




1-Ethyl-3-[6-(4- piperidin-1-ylmethyl- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


219




1-Ethyl-3-[6-(4- piperidin-1-ylmethyl- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


220




1-Ethyl-3-[6-(3- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


221




1-Ethyl-3-[6-(3- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


222




1-[6-(3- Difluoromethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


223




1-[6-(3- Difluoromethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-thiourea


 


224




1-Ethyl-3-(6- phenylamino- pyrido[2,3-b]pyrazin- 3-yl)-thiourea


 


225




1-Ethyl-3-(6- morpholin-4-yl- pyrido[2,3-b]pyrazin- 3-yl)-urea


 


226




1-Ethyl-3-(6- morpholin-4-yl- pyrido[2,3-b]pyrazin- 3-yl)-thiourea


 


227




1-Ethyl-3-[6-(4- methyl-piperazin-1- yl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


228




1-Ethyl-3-[6-(4- methyl-piperazin-1- yl)-pyrido[2,3- b]pyrazin-3-yl]- thiourea


 


229




1-Ethyl-3-[6-(2- methoxy-ethylamino)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


230




1-Ethyl-3-[6-(2- methoxy-ethylamino)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


231




1-[6- (cyclopropylmethyl- amino)-pyrido[2,3- b]pyrazin-3-yl]-3- ethyl-urea


 


232




1-[6- (Cyclopropylmethyl- amino)-pyrido[2,3- b]pyrazin-3-yl]-3- ethyl-thiourea


 


233




1-Ethyl-3-[6-(4- methyl-[1,4]diazepan- 1-yl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


234




1-Ethyl-3-[6-(4- methyl-[1,4]diazepan- 1-yl)-pyrido[2,3- b]pyrazin-3-yl]- thiourea


 


235




1-Ethyl-3-[6-(4- hydroxy-piperidin-1- yl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


236




1-Ethyl-3-[6-(4- hydroxy-piperidin-1- yl)-pyrido[2,3- b]pyrazin-3-yl]- thiourea


 


237




1-Ethyl-3-{6-[4-(4- hydroxy-3-methoxy- phenyl)-piperazin-1- yl]-pyrido[2,3- b]pyrazin-3-yl}-urea


 


238




1-Ethyl-3-{6-[4-(4- hydroxy-3-methoxy- phenyl)-piperazin-1- yl]-pyrido[2,3- b]pyrazin-3-yl}- thiourea


 


239




1-(6-Benzylamino- pyrido[2,3-b]pyrazin- 3-yl)-3-ethyl-urea


 


240




1-(6-Benzylamino- pyrido[2,3-b]pyrazin- 3-yl)-3-ethyl-thiourea


 


241




1-Ethyl-3-[6-(4- methyl-benzylamino)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


242




1-Ethyl-3-[6-(4- methyl-benzylamino)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


243




1-Ethyl-3-[6-(pyridin- 3-ylamino)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


244




1-Ethyl-3-[6-(pyridin- 3-ylamino)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


245




1-Ethyl-3-[6-(pyridin- 4-ylamino)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


246




1-Ethyl-3-[6-(pyridin- 4-ylamino)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


247




1-Ethyl-3-(6- phenethylamino- pyrido[2,3-b]pyrazin- 3-yl)-urea


 


248




1-Ethyl-3-(6- phenethylamino- pyrido[2,3-b]pyrazin- 3-yl)-thiourea


 


249




1-Ethyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-2-yl]-urea


 


250




1-Ethyl-3-[7-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-2-yl]-urea


 


251




1-Ethyl-3-[8-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-2-yl]-urea


 


252




1-Ethyl-3-[7-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


253




1-Ethyl-3-[8-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


254




1-{6-[4-(Cyano- dimethyl-methyl)- phenylamino]- pyrido[2,3-b]pyrazin- 3-yl}-3-ethyl-urea


 


255




1-{6-[4-(Cyano- dimethyl-methyl)- phenylamino]- pyrido[2,3-b]pyrazin- 3-yl}-3-ethyl-thiourea


 


256




1-{6-[4-(1-Cyano- cyclopentyl)- phenylamino]- pyrido[2,3-b]pyrazin- 3-yl}-3-ethyl-urea


 


257




1-{6-[4-(1-Cyano- cyclopentyl)- phenylamino]- pyrido[2,3-b]pyrazin- 3-yl}-3-ethyl-thiourea


 


258




1-[4-(Cyano-dimethyl- methyl)-phenyl]-3-[6- (4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


259




1-[4-(Cyano-dimethyl- methyl)-phenyl]-3-[6- (4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


260




1-[4-(1-Cyano- cyclopentyl)-phenyl]- 3-[6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


261




1-[4-(1-Cyano- cyclopentyl)-phenyl]- 3-[6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


262




[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-carbamic acid ethyl ester


 


263




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-propionamidine


 


264




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-4-methyl- benzamidine


 


265




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-furan-2- carboxamidine


 


266




2-(4-Chloro-phenyl)- N-[6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-acetamidine


 


267




4-Bromo-N-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- benzamidine


 


268




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-2-phenyl- acetamidine


 


269




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-4-methoxy- benzamidine


 


270




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-benzamidine


 


271




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-nicotinamidine


 


272




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]- cyclohexanecarbox- amidine


 


273




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-methylamino- propionamidine


 


274




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-quinoline-3- carboxamidine


 


275




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]- methanesulfonamide


 


276




4-Fluoro-N-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- benzenesulfonamide


 


277




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-4-methyl- benzenesulfonamide


 


278




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-4-carboxy- benzenesulfonamide


 


279




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-2,5-dimethoxy- benzenesulfonamide


 


280




C,C,C-Trifluoro-N-[6- (4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]- methanesulfonamide


 


281




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-4-methoxy- benzenesulfonamide


 


282




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]- benzenesulfonamide


 


283




Quinoline-8-sulfonic acid [6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


284




5-Dimethylamino- naphthalene-1- sulfonicacid[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-amide


 


285




2-Chloro- ethanesulfonic acid[6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


286




2-Morphloin-4-yl- ethanesulfonicacid[6- (4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


287




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3,4-dimethoxy- benzenesulfonamide


 


288




2-(2,2,2-Trifluoro- acetyl)-1,2,3,4- tetrahydro- isoquinoline-7- sulfonic acid [6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-amide


 


289




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3,5-bis- trifluoromethyl- benzenesulfonamide


 


290




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-4- trifluoromethoxy- benzenesulfonamide


 


291




Cyclopropanesulfonic acid [6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


292




Cyclohexanesulfonic acid [6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


293




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-4-methyl- benzenesulfonamide


 


294




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-C-phenyl- methanesulfonamide


 


295




(E)-2-Phenyl- ethenesulfonic acid [6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


296




Hexane-1-sulfonic acid [6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


297




Propane-1-sulfonic acid [6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


298




Ethanesulfonic acid [6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


299




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-4-isopropyl- benzenesulfonamide


 


300




3-{4-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-ylsulfamoyl]- phenyl}-propionic acid


 


301




C-Cyclopentyl-N-[6- (4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]- methanesulfonamide


 


302




Prop-2-ene-1-sulfonic acid [6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


303




Pyridine-2-sulfonic acid [6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


304




N-Ethyl-N′-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- guanidine


 


305




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-butyramide


 


306




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-benzamide


 


307




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-2-phenyl- acetamide


 


308




But-3-enoic acid [6- (4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


309




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-phenyl- propionamide


 


310




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-nicotinamide


 


311




Cyclohexanecarbox- ylic acid [6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-amide


 


312




But-3-enoic acid [6- (4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


313




Sodium; 2-chloro-4- [3-(3-ethyl-ureido)- pyrido[2,3-b]pyrazin- 6-yl]-6-methoxy- phenolate


 


314




1-Allyl-3-[6-(4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


315




Phosphoric acid mono-{4-[3-(3-ethyl- ureido)-pyrido[2,3- b]pyrazin-6-yl]-2- methoxy-phenyl} es- ter


 


316




Carbonic acid 4-[3-(3- ethyl-ureido)- pyrido[2,3-b]pyrazin- 6-yl]-phenyl ester 2- methoxy-ethyl ester


 


317




1-Ethyl-3-{6-[4-(3- ethyl-ureido)-phenyl]- pyrido[2,3-b]pyrazin- 3-yl}-urea


 


318




N-{5-[3-(3-Ethyl- ureido)-pyrido[2,3- b]pyrazin-6-ylamino]- 2-methyl-phenyl}- methanesulfonamid


 


319




N-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-2-methylamino- acetamide


 


320




1-Ethyl-3-[2-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


321




1-Ethyl-3-[2-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- thiourea


 


322




1-Ethyl-3-[3-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-2-yl]-urea


 


323




1-Ethyl-3-[3-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-2-yl]- thiourea


 


324




1-Ethyl-3-(2-p- tolylamino-pyrido[2,3- b]pyrazin-3-yl)-urea


 


325




1-Ethyl-3-(3-p- tolylamino-pyrido[2,3- b]pyrazin-2-yl)-urea


 


326




N-[2-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-4-methyl- benzenesulfonamide


 


327




N-[3-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 2-yl]-4-methyl- benzenesulfonamide


 


328




N-Ethyl-N′-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- oxalamide


 


329




1-[3-(3-Chloro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


330




1-Ethyl-3-[3-(3- phenoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


331




1-Ethyl-3-[3-(4- hydroxy-3-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


332




1-Ethyl-3-[3-(2- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


333




1-[3-(3-Acertyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


334




1-Ethyl-3-[3-(3- hydroxymethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


335




1-[3-(4- Dimethylamino- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


336




1-[3-(5-tert-Butyl-2- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


337




1-[3-(5-tert-Butyl-2- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


338




1-Ethyl-3-[3-(4- hydroxy-biphenyl-3- ylamino)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


339




1-Ethyl-3-[3-(4- hydroxy-biphenyl-3- ylamino)-pyrido[2,3- b]pyrazin-6-yl]- thiourea


 


340




1-Ethyl-3-[3-(2′- hydroxy- [1,1′;3′,1′′]terphenyl- 5′-ylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


341




1-Ethyl-3-[3-(2′- hydroxy- [1,1′;3′,1′′]terphenyl- 5′-ylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


342




1-Ethyl-3-[3-(2-nitro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


343




1-Ethyl-3-[3-(2-nitro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


344




1-[3-(Biphenyl-2- ylmino)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


345




1-[3-(Biphenyl-2- ylamino)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-thiourea


 


346




1-[3-(2-Acetyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


347




1-[3-(2-Acetyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


348




1-Ethyl-3-[3-(2- isopropyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


349




1-Ethyl-3-[3-(2- isopropyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


350




1-Ethyl-3-[3-(2- trifluoromethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


351




1-Ethyl-3-[3-(2- trifluoromethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


352




1-Ethyl-3-[3-(2- morpholin-4-yl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


353




1-Ethyl-3-[3-(2- morpholin-4-yl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


354




1-Ethyl-3-[3-(2- ethynyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


355




1-Ethyl-3-[3-(2- ethynyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


356




1-Ethyl-3-[3-(3-nitro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


357




1-Ethyl-3-[3-(3-nitro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


358




3-[6-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]- benzamidine


 


359




3-[6-(3-Ethyl- thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]- benzamidine


 


360




2-[6-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzoic acid methyl ester


 


361




2-[6-(3-Ethyl- thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzoic acid methyl ester


 


362




4-[6-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzoic acid ethyl ester


 


363




4-[6-(3-Ethyl- thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzoic acid ethyl ester


 


364




1-[3-(Biphenyl-4- ylamino)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-urea


 


365




1-[3-(Biphenyl-4- ylamino)-pyrido[2,3- b]pyrazin-6-yl]-3- ethyl-thiourea


 


366




1-Ethyl-3-[3-(4- trifluoromethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


367




1-Ethyl-3-[3-(4- trifluoromethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


368




{4-[6-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzyl}- phosphonic acid di- ethyl ester


 


369




{4-[6-(3-Ethyl- thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzyl}- phosphonic acid di- ethyl ester


 


370




{4-[6-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-phenyl}- acetic acid


 


371




{4-[6-(3-Ethyl- thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-phenyl}- acetic acid


 


372




1-[3-(2,3-Dichloro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


373




1-[3-(2,3-Dichloro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


374




1-[3-(3- Dimethylamino- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


375




1-[3-(3- Dimethylamino- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


376




1-Ethyl-3-[3-(2- methyl-3-nitro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


377




1-Ethyl-3-[3-(2- methyl-3-nitro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


378




1-[3-(2,3-Dimethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


379




1-[3-(2,3-Dimethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


380




1-Ethyl-3-[3-(3- hydroxy-2-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


381




1-Ethyl-3-[3-(3- hydroxy-2-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


382




2-Chloro-6-[6-(3- ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzoic acid


 


383




2-Chloro-6-[6-(3- ethyl-thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzoic acid


 


384




1-Ethyl-3-[3-(2-fluoro- 3-trifluoromethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


385




1-Ethyl-3-[3-(2-fluoro- 3-trifluoromethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


386




1-Ethyl-3-[3-(3- hydroxymethyl-2- methyl-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


387




1-Ethyl-3-[3-(3- hydroxymethyl-2- methyl-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


388




1-Ethyl-3-[3-(4- methoxy-2-nitro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


389




1-Ethyl-3-[3-(4- methoxy-2-nitro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


390




1-[3-(2-Bromo-4- methyl-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


391




1-[3-(2-Bromo-4- methyl-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


392




1-[3-(4-Chloro-2- trifluoromethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


393




1-[3-(4-Chloro-2- trifluoromethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


394




1-Ethyl-3-[3-(4- hydroxy-2-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


395




1-Ethyl-3-[3-(4- hydroxy-2-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


396




1-[3-(5-Chloro-2- hydroxymethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


397




1-[3-(5-Chloro-2- hydroxymethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


398




1-[3-(2,4-Dimethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


399




1-[3-(2,4-Dimethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


400




1-Ethyl-3-[3-(2-fluoro- 5-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


401




1-Ethyl-3-[3-(2-fluoro- 5-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


402




1-[3-(2,5-Dichloro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


403




1-[3-(2,5-Dichloro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


404




4-Chloro-3-[6-(3- ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzoic acid


 


405




4-Chloro-3-[6-(3- ethyl-thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzoic acid


 


406




1-[3-(5-Chloro-2- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


407




1-[3-(5-Chloro-2- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


408




1-[3-(5-tert-Butyl-2- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


409




1-[3-(5-tert-Butyl-2- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


410




1-Ethyl-3-[3-(5-fluoro- 2-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


411




1-Ethyl-3-[3-(5-fluoro- 2-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


412




1-[3-(2-Chloro-5- cyano-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


413




1-[3-(2-Chloro-5- cyano-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


414




1-[3-(5-Chloro-2- phenoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


415




1-[3-(5-Chloro-2- phenoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


416




4-Chloro-3-[6-(3- ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]- benzamide


 


417




4-Chloro-3-[6-(3- ethyl-thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]- benzamide


 


418




1-Ethyl-3-[3-(4- hydroxy-biphenyl-3- ylamino)-pyrido[2,3- b]pyrazin-6-yl]-urea


 


419




1-Ethyl-3-[3-(4- hydroxy-biphenyl-3- ylamino)-pyrido[2,3- b]pyrazin-6-yl]- thiourea


 


420




1-[3-(2-Cyano-5- methyl-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


421




1-[3-(2-Cyano-5- methyl-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


422




1-[3-(2-Chloro-5- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


423




1-[3-(2-Chloro-5- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


424




1-[3-(2-Chloro-6- methyl-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


425




1-[3-(2-Chloro-6- methyl-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


426




2-[6-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-3-hydroxy- benzoic acid


 


427




2-[6-(3-Ethyl- thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-3-hydroxy- benzoic acid


 


428




1-Ethyl-3-[3-(2- methyl-6-nitro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


429




1-Ethyl-3-[3-(2- methyl-6-nitro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


430




1-Ethyl-3-[3-(2- hydroxymethyl-6- methyl-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


431




1-Ethyl-3-[3-(2- hydroxymethyl-6- methyl-phenylamino)- pyrido[2,3-b]pyrain- 6-yl]-thiourea


 


432




1-[3-(3,4-Difluoro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


433




1-[3-(3,4-Difluoro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


434




2-Chloro-5-[6-(3- ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzoic acid


 


435




2-Chloro-5-[6-(3- ethyl-thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzoic acid


 


436




1-[3-(3-Cyano-4- methyl-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


437




1-[3-(3-Cyano-4- methyl-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


438




2-Chloro-5-[6-(3- ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]- benzenesulfonic acid


 


439




2-Chloro-5-[6-(3- ethyl-thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]- benzenesulfonic acid


 


440




1-[3-(3-Chloro-4- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


441




1-[3-(3-Chloro-4- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


442




1-[3-(3,5-Dichloro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


443




1-[3-(3,5-Dichloro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


444




2,5-Dichloro-3-[6-(3- ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzoic acid


 


445




2,5-Dichloro-3-[6-(3- ethyl-thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzoic acid


 


446




1-Ethyl-3-[3-(4- hydroxy-2,5-dimethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


447




1-Ethyl-3-[3-(4- hydroxy-2,5-dimethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


448




2-[6-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-4,5- dimethoxy-benzoic acid


 


449




2-[6-(3-Ethyl- thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-4,5- dimethoxy-benzoic acid


 


450




1-[3-(2,5-Dichloro-4- nitro-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


451




1-[3-(2,5-Dichloro-4- nitro-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


452




1-[3-(2,4-Dichloro-5- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


453




1-[3-(2,4-Dichlorro-5- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


454




1-Ethyl-3-[3-(2,4,6- trichloro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


455




1-Ethyl-3-[3-(2,4,6- trichloro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


456




1-Ethyl-3-[3-(2,4,6- trimethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


457




1-Ethyl-3-[3-(2,4,6- trimethyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


458




1-[3-(2-Bromo-4,6- difluoro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


459




1-[3-(2-Bromo-4,6- difluoro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


460




1-[3-(2-Chloro-6- cyano-4-nitro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


461




1-[3-(2-Chloro-6- cyano-4-nitro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


462




1-[3-(4-Acetyl-2,6- dichloro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


463




1-[3-(4-Acetyl-2,6- dichloro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


464




1-Ethyl-3-[3-(3,4,5- trichloro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


465




1-Ethyl-3-[3-(3,4,5- trichloro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


466




1-[3-(4-Acetyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


467




1-[3-(4-Acetyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


468




1-Ethyl-3-[3-(2- hydroxy-4-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


469




1-Ethyl-3-[3-(2- hydroxy-4-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


470




1-Ethyl-3-[3-(4- methoxy-2-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


471




1-Ethyl-3-[3-(4- methoxy-2-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


472




5-Bromo-2-[6-(3- ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzoic acid methyl ester


 


473




5-Bromo-2-[6-(3- ethyl-thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzoic acid methyl ester


 


474




2-[6-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-5-hydroxy- benzoic acid


 


475




2-[6-(3-Ethyl- thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-5-hydroxy- benzoic acid


 


476




1-Ethyl-3-[3-(4- methyl-2-nitro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


477




1-Ethyl-3-[3-(4- methyl-2-nitro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


478




1-Ethyl-3-[3-(5-fluoro- 2-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


479




1-Ethyl-3-[3-(5-fluoro- 2-methyl- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiorea


 


480




3-[6-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-4-hydroxy- benzoic acid


 


481




3-[6-(3-Ethyl- thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-4-hydroxy- benzoic acid


 


482




1-[3-(2,6-Dichloro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


483




1-[3-(2,6-Dichloro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


484




2-Chloro-4-[6-(3- ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzoic acid


 


485




2-Chloro-4-[6-(3- ethyl-thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-benzoic acid


 


486




4-[6-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-2-hydroxy- benzoic acid


 


487




4-[6-(3-Ethyl- thioureido)- pyrido[2,3-b]pyrazin- 3-ylamino]-2-hydroxy- benzoic acid


 


488




1-Ethyl-3-[3-(4-fluoro- 3-nitro-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


489




1-Ethyl-3-[3-(4-fluoro- 3-nitro-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


490




1-Ethyl-3-[3-(4- hydroxy-3-nitro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


491




1-Ethyl-3-[3-(4- hydroxy-3-nitro- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


492




1-[3-(4,5-Dimethyl-2- nitro-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-urea


 


493




1-[3-(4,5-Dimethyl-2- nitro-phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-ethyl-thiourea


 


494




1-[3-(4-Hydroxy-3- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-propyl-urea


 


495




1-[3-(4-Hydroxy-3- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-propyl- thiourea


 


496




1-[3-(3-Hydroxy-4- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-propyl-urea


 


497




1-[3-(3-Hydroxy-4- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-propyl- thiourea


 


498




1-[3-(4-Hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-propyl-urea


 


499




1-[3-(4-Hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-propyl- thiourea


 


500




1-Propyl-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


501




1-Propyl-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


502




1-Cyclopentyl-3-[3-(4- hydroxy-3-methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


503




1-Cyclopentyl-3-[3-(4- hydroxy-3-methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


504




1-Cyclopentyl-3-[3-(3- hydroxy-4-methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


505




1-Cyclopentyl-3-[3-(3- hydroxy-4-methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


506




1-Cyclopentyl-3-[3-(4- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


507




1-Cyclopentyl-3-[3-(4- hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


508




1-Cyclopentyl-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


509




1-Cyclopentyl-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


510




1-[3-(4-Hydroxy-3- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-phenyl-urea


 


511




1-[3-(4-Hydroxy-3- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-phenyl- thiourea


 


512




1-[3-(3-Hydroxy-4- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-phenyl-urea


 


513




1-[3-(3-Hydroxy-4- methoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-phenyl- thiourea


 


514




1-[3-(4-Hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-phenyl-urea


 


515




1-[3-(4-Hydroxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-3-phenyl- thiourea


 


516




1-Phenyl-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


517




1-Phenyl-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


518




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-propyl- thiourea


 


519




1-Cyclopentyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- thiourea


 


520




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-phenyl- thiourea


 


521




1-Allyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- thiourea


 


522




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-phenethyl- thiourea


 


523




1-Benzyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- thiourea


 


524




1-Cyclohexyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- thiourea


 


525




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-isopropyl- thiourea


 


526




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-methyl- thiourea


 


527




[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


528




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-pyridin-4-yl- thiourea


 


529




1-(4-Chloro-phenyl)- 3-[6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


530




1-(4-Chloro-phenyl)- 3-[6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


531




1-(3,4-Dichloro- phenyl)-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


532




1-(3,4-Dichloro- phenyl)-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- thiourea


 


533




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-p-tolyl-urea


 


534




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-p-tolyl- thiourea


 


535




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(3-methoxy- phenyl)-urea


 


536




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(3-methoxy- phenyl)-thiourea


 


537




2-{3-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-ureido}-benzoic acid methyl ester


 


538




2-{3-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-thioureido}- benzoic acid methyl ester


 


539




1-(2-Chloro-phenyl)- 3-[6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


540




1-(2-Chloro-phenyl)- 3-[6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


541




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(4- trifluoromethyl- phenyl)-urea


 


542




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(4- trifluoromethyl- phenyl)-thiourea


 


543




1-(3,5-Dimethyl- phenyl)-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


544




1-(3,5-Dimethyl- phenyl)-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- thiourea


 


545




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(2,4,6- trichloro-phenyl)-urea


 


546




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(2,4,6- trichloro-phenyl)- thiourea


 


547




1-(2-Fluoro-5-methyl- phenyl)-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


548




1-(2-Fluoro-5-methyl- phenyl)-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- thiourea


 


549




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-naphthalen-1- yl-urea


 


550




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-naphthalen-1- yl-thiourea


 


551




1-[6-(3,5-Dichloro-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-propyl-urea


 


552




1-[6-(3,5-Dichloro-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-isopropyl-urea


 


553




1-tert-Butyl-3-[6-(3,5- dichloro-4-hydroxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


554




1-tert-Butyl-3-[6-(3,5- dichloro-4-hydroxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


555




1-[6-(3,5-Dichloro-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(4- dimethylamino- phenyl)-urea


 


556




1-Cyclooctyl-3-[6-(3,5- dichloro-4-hydroxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


557




1-[6-(3,5-Dichloro-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-methyl-urea


 


558




1-Cyclohexyl-3-[6- (3,5-dichloro-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


559




1-[6-(3,5-Dichloro-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(4-fluoro- phenyl)-urea


 


560




1-[6-(3,5-Dichloro-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-thiophen-2-yl- urea


 


561




1-[6-(3,5-Dichloro-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(2-nitro- phenyl)-urea


 


562




1-[6-(3,5-Dichloro-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(3,5-dimethyl- isoxazol-4-yl)-urea


 


563




1-Cyclopentyl-3-[6- (3,5-dichloro-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


564




1-[6-(3,5-Dichloro-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-phenethyl-urea


 


565




1-[6-(3,5-Dichloro-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-[4-(2,5-dioxo- 2,5-dihydro-pyrrol-1- yl)-phenyl]-urea


 


566




1-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3- methyl-urea


 


567




1-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3- isopropyl-urea


 


568




1-tert-Butyl-3-[6-(3,4- dimethoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


569




1-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3-(4- dimethylamino- phenyl)-urea


 


570




1-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3- propyl-urea


 


571




1-Cyclohexyl-3-[6- (3,4-dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


572




1-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3-(4- fluoro-phenyl)-urea


 


573




1-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3-(3,5- dimethyl-isoxazol-4- yl)-urea


 


574




[6-(4-Benzyloxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


575




1-Allyl-3-[6-(3,4- dimethoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


576




1-Cyclopentyl-3-[6- (3,4-dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


577




1-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3- phenethyl-urea


 


578




1-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3-p- tolyl-urea


 


579




1-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3-[4- (2,5-dioxo-2,5- dihydro-pyrrol-1-yl)- phenyl]-urea


 


580




1-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3- phenyl-urea


 


581




1-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3-[1- (2,2,2-trifluoro-acetyl)- piperidin-4-yl]-urea


 


582




1-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-1,3- diethyl-urea


 


583




1-Ethyl-3-[6-(4- hydroxy-3,5-dimethyl- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


584




1-(4-Dimethylamino- phenyl)-3-[6-(4- hydroxy-3,5-dimethyl- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


585




1-Cyclohexyl-3-[6-(4- hydroxy-3,5-dimethyl- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


586




1-Ethyl-3-[6-(4- methoxy-3,5-dimethyl- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


587




1-Allyl-3-[6-(4- hydroxy-3,5-dimethyl- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


588




1-[6-(4-Hydroxy-3,5- dimethyl-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-phenethyl-urea


 


589




1-[6-(4-Hydroxy-3,5- dimethyl-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-[1-(2,2,2- trifluoro-acetyl)- piperidin-4-yl]-urea


 


590




1-(3,5-Dimethyl- isoxazol-4-yl)-3-[6-(4- hydroxy-3,5-dimethyl- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


591




1-[6-(4-Hydroxy-3,5- dimethyl-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-methyl-urea


 


592




1-[6-(4-Hydroxy-3,5- dimethyl-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-isopropyl-urea


 


593




1-tert-Butyl-3-[6-(4- hydroxy-3,5-dimethyl- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


594




1-(4-Fluoro-phenyl)-3- [6-(4-hydroxy-3,5- dimethyl-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


595




1-[6-(4-Hydroxy-3,5- dimethyl-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-phenyl-urea


 


596




1-[6-(3,5-Di-tert-butyl- 4-hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


597




1-Ethyl-3-[6-(4- isopropoxy-3,5- dimethyl-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


598




1-[6-(3,5-Dimethyl-4- propoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


599




1-[6-(4-Butoxy-3,5- dimethyl-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


600




1-(4-Fluoro-phenyl)-3- [6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


601




4-{3-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-ureido}-benzoic acid ethyl ester


 


602




1-(4-Dimethylamino- phenyl)-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


603




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-((1R,2S)-2- phenyl-cyclopropyl)- urea


 


604




1-Cyclooctyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-ul]-urea


 


605




1-Adamantan-1-yl-3- [6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


606




4-{3-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-ureido}- piperidine-1- carboxylic acid benzyl ester


 


607




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(2-morpholin-4- yl-pyridin-4-yl)-urea


 


608




1-Cycloheptyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


609




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-thiophen-2-yl- urea


 


610




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-[1-(2,2,2- trifluoro-acetyl)- piperidin-3-yl]-urea


 


611




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-pyridin-3-yl- urea


 


612




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(4-methyl- cyclohexyl)-urea


 


613




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(1,1,3,3- tetramethyl-butyl)- urea


 


614




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-thiophen-2-yl- urea


 


615




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(4-piperidin-1- yl-phenyl)-urea


 


616




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(4-nitro- phenyl)-urea


 


617




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(2-nitro- phenyl)-urea


 


618




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(3-nitro- phenyl)-urea


 


619




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(3-pyrrol-1-yl- phenyl)-urea


 


620




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-[4-(4-methyl- piperazin-1-yl)- phenyl]-urea


 


621




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(1-methyl-1H- indol-4-yl)-urea


 


622




1-[4-(2,5-Dioxo-2,5- dihydro-pyrrol-1-yl)- phenyl]-3-[6-(4- hydroxy-4-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


623




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(4-pyrrol-1-yl- phenyl)-urea


 


624




1-(4-Ethoxy-phenyl)- 3-[6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


625




1-(4-Methoxy-phenyl)- 3-[6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


626




1-(4-Cyano-phenyl)-3- [6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


627




1-Hexyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


628




1-Cyclododecyl-3-[6- (4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


629




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(3-phenyl- propyl)-urea


 


630




1-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-(4-phenyl- butyl)-urea


 


631




1-Butyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


632




1,1-Diethyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


633




3-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-1,1-diphenyl- urea


 


634




3-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-1-methyl-1-(4- trifluoromethyl- phenyl)-urea


 


635




3-[6-(4-Hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-1-(4-isopropyl- phenyl)-1-methyl-urea


 


636




1-(4-Chloro-phenyl)-3- [6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-1-methyl-urea


 


637




1-[6-(3-Chloro-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


638




1-Ethyl-3-[6-(3- hydroxy-4-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


639




1-[6-(3-Bromo-2- methoxy-5-methyl- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3-ethyl- urea


 


640




1-Ethyl-3-[6-(3-fluoro- 4-trifluoromethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-urea


 


641




1-[6-(3-Bromo-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


642




1-[6-(3-Chloro-4- hydroxy-5-methyl- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3-ethyl- urea


 


643




1-[6-(3,5-Di-tert-butyl- 4-hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


644




4-[3-(3-Ethyl-ureido)- pyrido[2,3-b]pyrazin- 6-yl]-2-hydroxy- benzoic acid methyl ester


 


645




1-[6-(3,5-Di-bromo-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


646




1-[6-(3,5-Di-fluoro-4- hydroxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


647




1-Ethyl-3-(6-phenyl- pyrido[2,3-b]pyrazin- 3-yl)-thiourea


 


648




1-[6-(4-Amino-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-thiourea


 


649




1-Ethyl-3-[6-(3- isopropoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


650




1-Ethyl-3-[6-(3,4,5- trimethoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


651




1-Ethyl-3-(6-p-tolyl- pyrido[2,3-b]pyrazin- 3-yl)-thiourea


 


652




1-tert-Butyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- thiourea


 


653




1-Cyclooctyl-3-[6-(4- hydroxy-3-methoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- thiourea


 


654




1-Adamantan-1-yl-3- [6-(4-hydroxy-3- methoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


655




1-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-2-yl]-3-ethyl- urea


 


656




1-[7-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-2-yl]-3-ethyl- urea


 


657




1-[8-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-2-yl]-3-ethyl- urea


 


658




1-Ethyl-3-[7-(3,4- Dimethoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


659




1-Ethyl-3-[8-(3,4- Dimethoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-urea


 


660




N-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- benzamide


 


661




Cyclohexanecarbox- ylic acid [6-(3,4- dimethoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


662




[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- carbamic acid ethyl ester


 


663




N-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- propionamide


 


664




[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- carbamic acid phenyl ester


 


665




[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- carbamic acid benzyl ester


 


666




[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- carbamic acid allyl ester


 


667




[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- carbamic acid methyl ester


 


668




[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- carbamic acid cyclopentyl ester


 


669




N-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- benzenesulfonamide


 


670




N-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-C- phenyl- methanesulfonamide


 


671




Cyclohexanesulfonic acid [6-(3,4- dimethoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


672




Hexane-1-sulfonic acid [6-(3,4- dimethoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


673




Prop-2-ene-1-sulfonic acid [6-(3,4- dimethoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


674




Cyclopropanesulfonic acid [6-(3,4- dimethoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-amide


 


675




N-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-4- methyl- benzenesulfonamide


 


676




N-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- acetamidine


 


677




N-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- benzamidine


 


678




N-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- cyclohexanecarbox- amidine


 


679




N-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-2,2- dimethyl- propionamidine


 


680




N-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- isobutyramidine


 


681




N-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-2- phenyl-acetamidine


 


682




N-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-4- hydroxy-benzamidine


 


683




N-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- guanidine


 


684




N-Cyclohexyl-N′-[6- (3,4-dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]- guanidine


 


685




N-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-N′- ethyl-guanidine


 


686




1-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3-ethyl- 1-methyl-urea


 


687




1-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-1,3,3- trimethyl-urea


 


688




1-Benzyl-1-[6-(3,4- dimethoxy-phenyl)- pyrido[2,3-b]pyrazin- 3-yl]-3-ethyl-urea


 


689




1-[6-(3,4-Dimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3-yl]-3-ethyl- 1-phenethyl-urea


 


690




1-Cyclohexyl-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


691




1-Cyclooctyl-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


692




1-Methyl-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


693




1-Allyl-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


694




1-tert-Butyl-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


695




1-(3,5-Dimethyl- isoxazol-4-yl)-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


696




1-Cyclohexylmethyl-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


697




1-Benzyl-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


698




1-(4-Methyl-benzyl)-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


699




1-Phenethyl-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


700




1-(2-Piperidin-1-yl- ethyl)-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


701




1-(4-Fluoro-benzyl)-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


702




1-Pentyl-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


703




1-(2-Morpholin-4-yl- ethyl)-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


704




1-(3-Phenyl-propyl)-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


705




1-(2-Methoxy-ethyl)-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


706




1-Ethyl-3-{3-[methyl- (3,4,5-trimethoxy- phenyl)-amino]- pyrido[2,3-b]pyrazin- 6-yl}-thiourea


 


707




1-Cyclopropyl-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


708




1-Furan-2-ylmethyl-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


709




3-{3-[3-(3,4,5- Trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thioureido}- propionic acid ethyl ester


 


710




1-(3-Methoxy-propyl)- 3-[3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


711




1-(1-Phenyl-ethyl)-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


712




1-(1,1,3,3- Tetramethyl-butyl)-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


713




1-Prop-2-ynyl-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]thiourea


 


714




1-(1-Ethyl-propyl)-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


715




1-(2-Chloro-ethyl)-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


716




1-(2-Bromo-ethyl)-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


717




1-Methoxymethyl-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


718




1-Cyclopropylmethyl- 3-[3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


719




1-(3-Diethylamino- propyl)-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


720




1-Ethyl-3-[2-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


721




1-Ethyl-3-[2-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 7-yl]-thiourea


 


722




1-Ethyl-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 7-yl]-thiourea


 


723




1-Ethyl-3-[2-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 8-yl]-thiourea


 


724




1-Ethyl-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 8-yl]-thiourea


 


725




1-Ethyl-3-[2-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 3-yl]-thiourea


 


726




1-Ethyl-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 2-yl]-thiourea


 


727




1-Ethyl-1-methyl-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


728




3-Ethyl-1-methyl-1-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


729




1-Ethyl-1,3-dimethyl- 3-[3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


730




1-Ethyl-1,3-dimethyl- 3-{3-[methyl-(3,4,5- trimethoxy-phenyl)- amino]-pyrido[2,3- b]pyrazin-6-yl}- thiourea


 


731




N-[3-(3,4,5- Trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-propionamide


 


732




N-[3-(3,4,5- Trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-benzamide


 


733




N*6*-Ethyl-N*3*- (3,4,5-trimethoxy- phenyl)-pyrido[2,3- b]pyrazin-3,6- diamine


 


734




N-[3-(3,4,5- Trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]- benzenesulfonamide


 


735




Cyclohexanesulfonic acid [3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-amide


 


736




Propane-1-sulfonic acid [3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-amide


 


737




N-Ethyl-N′-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-guanidine


 


738




1-Phenyl-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


739




1-(4-Fluoro-phenyl)-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


740




1-(3-Methyl-benzyl)-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


741




1-(3-Methoxy-benzyl)- 3-[3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


742




1-(3-Fluoro-benzyl)-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


743




1-(3-Chloro-benzyl)-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]thiourea


 


744




1-(2-Methyl-benzyl)-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


745




1-(2-Fluoro-benzyl)-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


746




1-(2-Chloro-benzyl)-3- [3-(3,4,5-trimerthoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


747




1-(2-Methoxy-benzyl)- 3-[3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


748




1-(3,4-Dimethoxy- benzyl)-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


749




1-(2,3-Dimethoxy- benzyl)-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


750




1-Benzo[1,3]dioxol-5- ylmethyl-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


751




1-(3,4-Dichloro- benzyl)-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


752




1-(2-Fluoro-propyl)-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


753




1-(3-Fluoro-propyl)-3- [3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


754




1-(2-Fluoro- cyclobutyl)-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


755




1-Cyclobutyl-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


756




1-(2-Fluoro- cyclopentyl)-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


757




1-(2-Fluoro- cyclohexyl)-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


758




1-Piperidin-4-yl-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


759




1-(1-Methyl-piperidin- 4-yl)-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


760




1-(3-Fluoro-piperidin- 4-yl)-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


761




1-(3-Fluoro-1-methyl- piperidin-4-yl)-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


762




[3-(3,4,5-Trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


763




1-Octyl-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


764




1-Decyl-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


765




1-Ethyl-3-{3-[methyl- (3,4,5-trimethoxy- phenyl)-amino]- pyrido[2,3-b]pyrazin- 6-yl}-thiourea


 


766




Namensgebung mit Autonom nicht möglich


 


767




1-(1-Oxy-piperidin-4- yl)-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


768




1-(1-Methyl-1-oxy- piperidin-4-yl)-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


769




1-(3-Fluoro-1-oxy- piperidin-4-yl)-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


770




1-(3-Fluoro-1-methyl- 1-oxy-piperidin-4-yl)- 3-[3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-thiourea


 


771




1-(1-Oxy-piperidin-4- yl)-3-[3-(3,4,5- trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


772




1-(1-Methyl-1-oxy- piperidin-4-yl)-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


773




1-(3-Fluoro-1-oxy- piperidin-4-yl)-3-[3- (3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea


 


774




1-(3-Fluoro-1-methyl- 1-oxy-piperidin-4-yl)- 3-[3-(3,4,5-trimethoxy- phenylamino)- pyrido[2,3-b]pyrazin- 6-yl]-urea









For the avoidance of doubt, if chemical name and chemical structure of the above illustrated compounds do not correspond by mistake, the chemical structure is regarded to unambigously define the compound.

All the above generically or explicitly disclosed pyrido[2,3-b]pyrazine derivatives, including preferred subsets/embodiments of general formula (I) and Compounds 1 to 774 are hereinafter referred to as compounds of the (present) invention.
The terms indicated for explanation of the above compounds of the invention always, unless indicated otherwise in the description or in the claims, have the following meanings:
The term “unsubstituted” means that the corresponding radical, group or moiety has no substituents.
The term “substituted” means that the corresponding radical, group or moiety has one or more substituents. Where a radical has a plurality of substituents, and a selection of various substituents is specified, the substituents are selected independently of one another and do not need to be identical.
The term “alkyl” for the purposes of this invention refers to acyclic saturated or unsaturated hydrocarbon radicals which may be branched or straight-chain and have 1 to 8 carbon atoms, i.e. C1-8-alkanyls, C2-8-alkenyls and C2-8-alkynyls. Alkenyls have at least one C—C double bond and alkynyls at least one C—C triple bond. Alkynyls may additionally also have at least one C—C double bond. Examples of suitable alkyl radicals are methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, iso-pentyl, neo-pentyl, tert-pentyl, 2- or 3-methyl-pentyl, n-hexyl, 2-hexyl, isohexyl, n-heptyl, n-octyl, n-nonyl, n-decyl, n-undecyl, n-dodecyl, n-tetradecyl, n-hexadecyl, n-octadecyl, n-icosanyl, n-docosanyl, ethylenyl (vinyl), propenyl (—CH2CH═CH2; —CH═CH—CH3, —C(═CH2)—CH3), butenyl, pentenyl, hexenyl, heptenyl, octenyl, octadienyl, octadecenyl, octadec-9-enyl, icosenyl, icos-11-enyl, (Z)-icos-11-enyl, docosnyl, docos-13-enyl, (Z)-docos-13-enyl, ethynyl, propynyl (—CH2—C≡CH, —C≡C—CH3), butynyl, pentynyl, hexynyl, heptynyl, octynyl.
The term “(C9-C30)alkyl” for the purposes of this invention refers to acyclic saturated or unsaturated hydrocarbon radicals which may be branched or straight-chain and have 9 to 30 carbon atoms, i.e. C9-30-alkanyls, C9-30-alkenyls and C9-30-alkynyls. C9-30-Alkenyls have at least one C—C double bond and C9-30-alkynyls at least one C—C triple bond. C9-30-Alkynyls may additionally also have at least one C—C double bond. Examples of suitable (C9-C30)alkyl radicals are tetradecyl, hexadecyl, octadecyl, eicosanyl, cis-13-docosenyl (erucyl), trans-13-docosenyl (brassidyl), cis-15-tetracosenyl (nervonyl) and trans-15-tetracosenyl.
The term “cycloalkyl” for the purposes of this invention refers to saturated and partially unsaturated non-aromatic cyclic hydrocarbon groups/radicals, having 1 to 3 rings, that contain 3 to 20, preferably 3 to 12, most preferably 3 to 8 carbon atoms. The cycloalkyl radical may also be part of a bi- or polycyclic system, where, for example, the cycloalkyl radical is fused to an aryl, heteroaryl or heterocyclyl radical as defined herein by any possible and desired ring member(s). The bonding to the compounds of the general formula (I) can be effected via any possible ring member of the cycloalkyl radical. Examples of suitable cycloalkyl radicals are cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclodecyl, cyclohexenyl, cyclopentenyl and cyclooctadienyl.
The term “heterocyclyl” for the purposes of this invention refers to a mono- or poly-cyclic system of 3 to 20, preferably 5 or 6 to 14 ring atoms comprising carbon atoms and 1, 2, 3, 4, or 5 heteroatoms, in particular nitrogen, oxygen and/or sulfur which are identical or different. The cyclic system may be saturated, mono- or polyunsaturated but may not be aromatic. In the case of a cyclic system consisting of at least two rings the rings may be fused or spiro- or otherwise connected. Such “heterocyclyl” radicals can be linked via any ring member. The term “heterocyclyl” also includes systems in which the heterocycle is part of a bi- or polycyclic saturated, partially unsaturated and/or aromatic system, such as where the heterocycle is fused to an “aryl”, “cycloalkyl”, “heteroaryl” or “heterocyclyl” group as defined herein via any desired and possible ring member of the heterocycyl radical. The bonding to the compounds of the general formula (I) can be effected via any possible ring member of the heterocycyl radical. Examples of suitable “heterocyclyl” radicals are pyrrolidinyl, thiapyrrolidinyl, piperidinyl, piperazinyl, oxapiperazinyl, oxapiperidinyl, oxadiazolyl, tetrahydrofuryl, imidazolidinyl, thiazolidinyl, tetrahydropyranyl, morpholinyl, tetrahydrothiophenyl, dihydropyranyl.
The term “aryl” for the purposes of this invention refers to aromatic hydrocarbon systems having 3 to 14, preferably 5 to 14, more preferably 6 to 14 carbon atoms. The term “aryl” also includes systems in which the aromatic cycle is part of a bi- or poly-cyclic saturated, partially unsaturated and/or aromatic system, such as where the aromatic cycle is fused to an “aryl”, “cycloalkyl”, “heteroaryl” or “heterocyclyl” group as defined herein via any desired and possible ring member of the aryl radical. The bonding to the compounds of the general formula (I) can be effected via any possible ring member of the aryl radical. Examples of suitable “aryl” radicals are phenyl, biphenyl, naphthyl and anthracenyl, but likewise indanyl, indenyl, or 1,2,3,4-tetrahydronaphthyl.
The term “heteroaryl” for the purposes of this invention refers to a 3 to 14, preferably 5 to 14, more preferably 5-, 6- or 7-membered cyclic aromatic hydrocarbon radical which comprises at least 1, where appropriate also 2, 3, 4 or 5 heteroatoms, preferably nitrogen, oxygen and/or sulfur, where the heteroatoms are identical or different. The number of nitrogen atoms is preferably 0, 1, 2, or 3, and that of the oxygen and sulfur atoms is independently 0 or 1. The term “heteroaryl” also includes systems in which the aromatic cycle is part of a bi- or polycyclic saturated, partially unsaturated and/or aromatic system, such as where the aromatic cycle is fused to an “aryl”, “cycloalkyl”, “heteroaryl” or “heterocyclyl” group as defined herein via any desired and possible ring member of the heteroaryl radical. The bonding to the compounds of the general formula (I) can be effected via any possible ring member of the heteroaryl radical. Examples of suitable “heteroaryl” are pyrrolyl, thienyl, furyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, oxadiazolyl, isoxazolyl, pyrazolyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, indolyl, quinolinyl, isoquinolinyl, imidazolyl, triazolyl, triazinyl, tetrazolyl, phthalazinyl, indazolyl, indolizinyl, quinoxalinyl, quinazolinyl, pteridinyl, carbazolyl, phenazinyl, phenoxazinyl, phenothiazinyl, acridinyl.
For the purposes of the present invention, the terms “alkyl-cycloalkyl”, “cycloalkylalkyl”, “alkyl-heterocyclyl”, “heterocyclylalkyl”, “alkyl-aryl”, “arylalkyl”, “alkyl-heteroaryl” and “heteroarylalkyl” mean that alkyl, cycloalkyl, heterocycl, aryl and heteroaryl are each as defined above, and the cycloalkyl, heterocyclyl, aryl and heteroaryl radical is bonded to the compounds of the general formula (I) via an alkyl radical, preferably C1-C8-alkyl radical, more preferably C1-C4-alkyl radical.
The term “halogen”, “halogen atom” or “halogen substituent” (Hal-) for the purposes of this invention refers to one, where appropriate, a plurality of fluorine (F, fluoro), bromine (Br, bromo), chlorine (Cl, chloro), or iodine (I, iodo) atoms. The designations “di-halogen”, “trihalogen” and “perhalogen” refer respectively to two, three and four substituents, where each substituent can be selected independently from the group consisting of fluorine, chlorine, bromine and iodine. “Halogen” preferably means a fluorine, chlorine or bromine atom.
All stereoisomers of the compounds of the invention are contemplated, either in a mixture or in pure or substantially pure form. The compounds of the invention can have asymmetric centers at any of the carbon atoms. Consequently, they can exist in the form of their racemates, in the form of the pure enantiomers and/or diastereomers or in the form of mixtures of these enantiomers and/or diastereomers. The mixtures may have any desired mixing ratio of the stereoisomers.
Thus, for example, the compounds of the invention which have one or more centers of chirality and which occur as racemates or as diastereomer mixtures can be fractionated by methods known per se into their optical pure isomers, i.e. enantiomers or diastereomers. The separation of the compounds of the invention can take place by column separation on chiral or nonchiral phases or by recrystallization from an optionally optically active solvent or with use of an optically active acid or base or by derivatization with an optically active reagent such as, for example, an optically active alcohol, and subsequent elimination of the radical.
The compounds of the invention may be present in the form of their double bond isomers as “pure” E or Z isomers, or in the form of mixtures of these double bond isomers.
Where possible, the compounds of the invention may be in the form of the tautomers.
It is likewise possible for the compounds of the invention to be in the form of any desired prodrugs such as, for example, esters, carbonates, carbamates, ureas, amides, N-oxides or phosphates, in which cases the actually biologically active form is released only through metabolism. Any compound that can be converted in vivo to provide the bioactive agent (i.e. compounds of the invention) is a prodrug within the scope and spirit of the invention.
Various forms of prodrugs are well known in the art and are described for instance in:

    (i) Wermuth C G et al., Chapter 31: 671-696, The Practice of Medicinal Chemistry, Academic Press 1996;
    (ii) Bundgaard H, Design of Prodrugs, Elsevier 1985; and
    (iii) Bundgaard H, Chapter 5: 131-191, A Textbook of Drug Design and Development, Harwood Academic Publishers 1991.


Said references are incorporated herein by reference.
It is further known that chemical substances are converted in the body into metabolites which may where appropriate likewise elicit the desired biological effect—in some circumstances even in more pronounced form.
Any biologically active compound that was converted in vivo by metabolism from any of the compounds of the invention is a metabolite within the scope and spirit of the invention.
Corresponding prodrugs and metabolites of the compounds of the invention should be considered to be part of the invention.
The compounds of the invention can, if they have a sufficiently basic group such as, for example, a secondary or tertiary amine, be converted with inorganic and organic acids into salts. The pharmaceutically acceptable salts of the compounds of the invention are preferably formed with hydrochloric acid, hydrobromic acid, iodic acid, sulfuric acid, phosphoric acid, methanesulfonic acid, p-toluenesulfonic acid, carbonic acid, formic acid, acetic acid, sulfoacetic acid, trifluoroacetic acid, oxalic acid, malonic acid, maleic acid, succinic acid, tartaric acid, racemic acid, malic acid, embonic acid, mandelic acid, fumaric acid, lactic acid, citric acid, taurocholic acid, glutaric acid, stearic acid, glutamic acid or aspartic acid. The salts which are formed are, inter alia, hydrochlorides, chlorided, hydrobromides, bromides, iodides, sulfates, phosphates, methanesulfonates, tosylates, carbonates, bicarbonates, formates, acetates, sulfoacetates, triflates, oxalates, malonates, maleates, succinates, tartrates, malates, embonates, mandelates, fumarates, lactates, citrates, glutarates, stearates, aspartates and glutamates. The stoichiometry of the salts formed from the compounds of the invention may moreover be an integral or non-integral multiple of one.
The compounds of the invention can, if they contain a sufficiently acidic group such as, for example, the carboxy, sulfonic acid, phosphoric acid or a phenolic group, be converted with inorganic and organic bases into their physiologically tolerated salts. Examples of suitable inorganic bases are ammonium, sodium hydroxide, potassium hydroxide, calcium hydroxide, and of organic bases are ethanolamine, diethanolamine, triethanolamine, ethylenediamine, t-butylamine, t-octylamine, dehydroabietylamine, cyclohexylamine, dibenzylethylene-diamine and lysine. The stoichiometry of the salts formed from the compounds of the invention can moreover be an integral or non-integral multiple of one.
It is likewise possible for the compounds of the invention to be in the form of their solvates and, in particular, hydrates which can be obtained for example by crystallization from a solvent or from aqueous solution. It is moreover possible for one, two, three or any number of solvate or water molecules to combine with the compounds of the invention to give solvates and hydrates.
It is known that chemical substances form solids which exist in different order states which are referred to as polymorphic forms or modifications. The various modifications of a polymorphic substance may differ greatly in their physical properties. The compounds of the invention can exist in various polymorphic forms and certain modifications may moreover be metastable. All these polymorphic forms of the compounds are to be regarded as belonging to the invention.
It has now been found in a surprising and advantageous manner that the compounds of the invention can also act, i.e. have a modulating or inhibiting effect, on two or more signal transduction pathways or enzymes of such pathways. It has been found that the compounds of the invention act, i.e. modulate or inhibit, with high selectivity.
Such a simultaneous, for example dual, modulation or inhibition of two or more signal transduction pathways, for example ras-Raf-Mek-Erk signal pathway, PI3K-Akt signal pathway and/or SAPK signal pathway, more specifically Erk1/Erk2 and/or PI3K and/or Jnk and/or p38, is advantageous over the only single modulation or inhibition of one signal transduction pathway, since synergistic therapeutic effects can be brought about, for example enhanced apoptosis and more rapid and efficient tumor regression.
The surprising advantageous effects of the compounds of the invention enable multiple therapeutic approaches to be pursued in the physiological and/or pathophysiological states or conditions which are sensitive to the treatment or modulation of, or are mediated by, two or more signal transduction pathways.
It has also been found in a surprising and advantageous manner that the compounds of the invention can also act, i.e. have modulating or inhibiting action, with high selectivity on the ras-Raf-Mek-Erk signal transduction pathway or enzymes thereof, and that the multiple mechanisms of action and therapeutic approaches detailed above can also find use with this signal pathway or enzymes.
It has also been found in a surprising and advantageous manner that the compounds of the invention can also act, i.e. have modulating or inhibiting action, with high selectivity on the PI3K-Akt signal transduction pathway or enzymes thereof, and that the multiple mechanisms of action and therapeutic approaches detailed above can also find use with this signal pathway or enzymes.
It has also been found in a surprising and advantageous manner that the compounds of the invention can also act, i.e. have modulating or inhibiting action, with high selectivity on the SAPK signal transduction pathway or enzymes thereof, and that the multiple mechanisms of action and therapeutic approaches detailed above can also find use with this signal pathway or enzymes.
It has additionally been found in a surprising and advantageous manner that the compounds of the invention can also act, i.e. have a modulating or inhibiting action, with high selectivity on enzymes such as ATM, ATR, mTOR, DNA-PK and/or hSMG-1, and that the multiple mechanisms of action and therapeutic approaches detailed above can also find use with these enzymes.
According to the invention, the term “modulation” is understood to mean the following: “activation, partial activation, inhibition, partial inhibition”. It is within the technical knowledge of the average person skilled in the art to measure and to determine such an activation, partial activation, inhibition or partial inhibition by means of the customary measurement and determination methods. For example, a partial activation can be measured and determined in relation to a full activation; and likewise a partial inhibition in relation to a full inhibition.
According to the invention, the term “inhibition” is understood to mean the following: “partial or full inhibition”. It is within the technical knowledge of the average person skilled in the art to measure and to determine such a partial or full inhibition by means of the customary measurement and determination methods. For example, partial inhibition can be measured and determined in relation to full inhibition.
The terms “modulation” and “inhibition” relate, in connection with “enzymes” and/or “kinases” in the context of this invention, both to the inactive form (enzymatically inactive) and/or active form (enzymatically active) of the particular enzyme and/or kinase. This means in the context of this invention that a compound of the invention can display its modulating action on the inactive form, active form or both forms of the enzyme and/or kinase.
In a further aspect, the object of the invention has surprisingly been solved by providing the compounds of the present invention or pharmaceutical compositions as described herein for use as a medicament.
In another aspect, the object of the present invention has surprisingly been solved by providing the use of the compounds of the invention or pharmaceutical compositions as described herein for the manufacture of a medicament for the treatment or prophylaxis of the physiological and/or pathological conditions described herein.
In a further aspect, the object of the invention has surprisingly been solved by providing the compounds of the invention for use in the manufacture of a medicament for modulating misdirected cellular signal transduction processes, especially for influencing the function of active and inactive receptor tyrosine kinases, and also cytoplasmic tyrosine, serine/threonine and lipid kinases, such as c-Raf, B-Raf, Mek, MAPKs, PDGFRbeta, Flt-3, IGF1R, PI3K, PKB/Akt1, c-Kit, c-Abl, FGFR1 and KDR.
In a further aspect, the object of the invention has surprisingly been solved by providing the compounds of the invention for use in the manufacture of a medicament for the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, that are mediated by one or more signal transduction pathways selected from the group consisting of: “ras-Raf-Mek-Erk signal transduction pathway, PI3K-Akt signal transduction pathway and/or SAPK signal transduction pathway”.
In a further aspect, the object of the invention has surprisingly been solved by providing the compounds of the invention for use in the manufacture of a medicament for the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals mediated by one or more enzymes selected from the group consisting of: “ATM, ATR, mTOR, DNA-PK, hSMG-1”.
In a further aspect, the object of the invention has surprisingly been solved by providing the compounds of the invention for use in the manufacture of a medicament for the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, where the treatment or prophylaxis is brought about by modification of one or more enzymes selected from the group consisting of: “ATM, ATR, mTOR, DNA-PK, hSMG-1”.
In a preferred embodiment, the compounds of the invention are provided for use in the manufacture of a medicament for the treatment or prophylaxis of physiological and/or pathophysiological conditions mediated by ras-Raf-Mek-Erk signal transduction pathway and PI3K-Akt signal transduction pathway in mammals, and/or for the manufacture of a medicament for the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, where the treatment or prophylaxis is brought about by modulation of ras-Raf-Mek-Erk signal transduction pathway and of PI3K-Akt signal transduction pathway.
In a further aspect, the object of the invention has surprisingly been solved by providing the compounds of the invention for use in the manufacture of a medicament for the treatment or prophylaxis of physiological and/or pathophysiological conditions mediated by ras-Raf-Mek-Erk signal transduction pathway in mammals.
In a further aspect, the object of the invention has surprisingly been solved by providing the compounds of the invention for use in the manufacture of a medicament for the treatment or prophylaxis of physiological and/or pathophysiological conditions mediated by PI3K-Akt signal transduction pathway in mammals.
In a further aspect, the object of the invention has surprisingly been solved by providing the compounds of the invention for use in the manufacture of a medicament for the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, where the treatment or prophylaxis is brought about by modulation of PI3K-Akt signal transduction pathway.
In a preferred embodiment, the compounds of the invention are provided for use in the manufacture of a medicament for the treatment or prophylaxis of physiological and/or pathophysiological conditions mediated by SAPK signal transduction pathway and PI3K-Akt signal transduction pathway in mammals, and/or for the manufacture of a medicament for the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, where the treatment or prophylaxis is brought about by modulation of SAPK signal transduction pathway and of PI3K-Akt signal transduction pathway.
In a further aspect, the object of the invention has surprisingly been solved by providing the compounds of the invention for use in the manufacture of a medicament for the treatment or prophylaxis of physiological and/or pathophysiological conditions mediated by SAPK signal transduction pathway in mammals.
In a further aspect, the object of the invention has surprisingly been solved by providing the compounds of the invention for use in the manufacture of a medicament for the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, where the treatment or prophylaxis is brought about by modulation of SAPK signal transduction pathway.
In a preferred embodiment, the compounds of the invention are provided for the uses detailed above, where the modulation of ras-Raf-Mek-Erk signal transduction pathway is brought about by modulation of one or more enzymes selected from the group consisting of: “tyrosine kinase, serine/threonine kinase, receptor tyrosine kinase, cytoplasmic tyrosine kinase, cytoplasmic serine/threonine kinase” and preferably selected from the group consisting of “Erk, Erk1, Erk2”.
In a further preferred embodiment, the compounds of the invention are provided for the uses as detailed above, where the modulation of PI3K-Akt signal transduction pathway is brought about by modulation of one or more enzymes selected from the group consisting of “lipid kinases” and preferably selected from the group consisting of: “PI3K, PI3Kalpha, PI3 Kbeta, PI3 Kgamma, PI3 Kdelta, PI3K-C2alpha, PI3K-C2beta, PI3K-Vps34p”.
In a further preferred embodiment, the compounds of the invention are provided for the uses as detailed above, where the modulation of SAPK signal transduction pathway is brought about by modulation of one or more enzymes selected from the group consisting of: “tyrosine kinase, serine/threonine kinase, receptor tyrosine kinase, cytoplasmatic tyrosine kinase, cytoplasmatic serine/threonine kinase” and preferably selected from the group consisting of: “Jnk, Jnk1, Jnk2, Jnk3, p38, p38alpha, p38beta, p38gamma, p38delta”.
In a further aspect, the object of the invention has surprisingly been solved by providing a process of manufacturing the compounds of the invention.
In a further aspect, the object of the invention has surprisingly been solved by providing the compounds of the invention according to the aspects, preferred embodiments and uses detailed above for use in the manufacture of a medicament for the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, where the treatment or prophylaxis is brought about by modulation of two or more enzymes.
In a more preferred embodiment, the compounds of the invention are provided for the uses detailed above, where at least one enzyme in the treatment or prophylaxis brought about by modulation of two or more enzymes is selected from the group consisting of: “Erk, Erk1, Erk2” and at least one enzyme is selected from the group consisting of: “PI3K, PI3Kalpha, PI3 Kbeta, PI3 Kgamma, PI3 Kdelta, PI3K-C2alpha, PI3K-C2beta, PI3K-Vps34p”.
In a more preferred embodiment, the compounds of the invention are provided for the uses detailed above, where at least one enzyme in the treatment or prophylaxis brought about by modulation of two or more enzymes is selected from the group consisting of: “Jnk, Jnk1, Jnk2, Jnk3, p38, p38alpha, p38beta, p38gamma, p38delta” and at least one enzyme is selected from the group consisting of: “PI3K, PI3Kalpha, PI3 Kbeta, PI3 Kgamma, PI3 Kdelta, PI3K-C2alpha, PI3K-C2beta, PI3K-Vps34p”.
In a more preferred embodiment, the compounds of the invention are provided for the uses detailed above, where at least one enzyme in the treatment or prophylaxis brought about by modulation of two or more enzymes is selected from the group consisting of: “Erk, Erk1, Erk2” and at least one enzyme is selected from the group consisting of: “ATM, ATR, mTOR, DNA-PK, hSMG-1”.
In a more preferred embodiment, the compounds of the invention are provided for the uses detailed above, where at least one enzyme in the treatment or prophylaxis brought about by modulation of two or more enzymes is selected from the group consisting of: “Jnk, Jnk1, Jnk2, Jnk3, p38, p38alpha, p38beta, p38gamma, p38delta” and at least one enzyme is selected from the group consisting of: “ATM, ATR, mTOR, DNA-PK, hSMG-1”.
In a more preferred embodiment, the compounds of the invention are provided for the uses detailed above, where at least one enzyme in the treatment or prophylaxis brought about by modulation of two or more enzymes is selected from the group consisting of: “PI3K, PI3Kalpha, PI3 Kbeta, PI3 Kgamma, PI3 Kdelta, PI3K-C2alpha, PI3K-C2beta, PI3K-Vps34p” and at least one enzyme is selected from the group consisting of: “ATM, ATR, mTOR, DNA-PK, hSMG-1”.
In another preferred embodiment, the compounds of the invention are provided for the uses detailed above, where the modulation is an inhibition.
Likewise, corresponding medicaments comprising at least one compound of the invention or at least one pharmaceutical composition as described herein for use in the treatment or prophylaxis of the herein disclosed physiological and/or pathological conditions are also comprised by the present invention.
For the purpose of the present invention, the compounds of the invention may be administered to all known mammals, especially to the human, for treatment and/or prophylaxis.
Preferably, such mammals are selected from the group consisting of “human, domestic animals, cattle, livestock, pets, cow, sheep, pig, goat, horse, pony, donkey, hinny, mule, hare, rabbit, cat, dog, guinea pig, hamster, rat, mouse”. More preferably, such mammals are human.
For the purpose of the present invention, the compounds of the invention may be used for the treatment or prophylaxis of all known physiological and/or pathophysiological conditions.
In a preferred embodiment, the compounds of the invention are provided for the uses detailed above, where the physiological and/or pathophysiological conditions are selected from the group consisting of: “malignant tumors, benign tumors, inflammatory disorders, inflammations, pain, rheumatic disorders, arthritic disorders, HIV infections, neurological or neurodegenerative disorders, rheumatism, arthritis, AIDS, ARC (AIDS related complex), Kaposi's sarcoma, tumors originating in the brain and/or nervous system and/or meninges (refer to WO 99/01764), dementia, Alzheimer's disease, hyperproliferative disorders, psoriasis, endometriosis, scar formation, benign prostate hyperplasia (BPH), disorders of the immune system, autoimmune disorders, immune deficiency disorders, colon tumor, stomach tumor, intestine tumor, lung tumor, pancreas tumor, ovarian tumor, prostate tumor, leukemia, melanoma, liver tumor, kidney tumor, head tumor, throat tumor, glioma, breast tumor, uterine cancer, endometrial cancer, cervical cancer, brain tumor, adenocanthoma, bladder cancer, colorectal tumor, esophageal cancer, gynecological tumor, ovarian tumor, thyroid cancer, lymphoma, chronic leukemia, acute leukemia, restenosis, diabetes, diabetic nephropathy, fibrotic disorders, cystic fibrosis, malignant nephrosclerosis, thrombotic microangiopathy syndrome, organ transplant rejection, glomerulopathies, disorders of the metabolism, solid tumors, rheumatic arthritis, diabetic retinopathy, asthma, allergies, allergic disorders, chronic obstructive pulmonary disorders, inflammatory bowel disorder, fibrosis, atherosclerosis, cardiac disorders, cardiovascular disorders, disorders of the heart muscle, vascular disorders, angiogenetic disorders, kidney disorders, rhinitis, Grave's disease, focal ischemia, heart failure, ischemia, cardiac hypertrophy, kidney failure, cardiac myocyte dysfunction, high blood pressure, vascular constriction, stroke, anaphylactic shock, blood platelet agglutination, skeletal muscular atrophy, obesity, excess weight, glucose homeostasis, congestive heart failure, angina, heart attack, myocardial infarction, hyperglycemia, hypoglycemia, hypertension”.
In a further aspect of the present invention, the object of the invention has surprisingly been solved by providing the compounds of the invention according to the aspects, preferred embodiments and uses detailed above for use in the manufacture of a medicament for the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, where the medicament comprises at least one further pharmacologically active substance.
In a further aspect of the present invention, the object of the invention has surprisingly been solved by providing the compounds of the invention according to the aspects, preferred embodiments and uses detailed above for use in the manufacture of a medicament for the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, where the medicament is administered before and/or during and/or after the treatment with at least one further pharmacologically active substance.
In a further aspect of the present invention, the object of the invention has surprisingly been solved by providing the compounds of the invention according to the aspects, preferred embodiments and uses detailed above for use in the manufacture of a medicament for the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, where the medicament is administered before and/or during and/or after the treatment with radiation therapy and/or surgery.
In the context of the present invention, the compounds of the invention may be administered with all known pharmacologically active substances in a combination therapy as detailed.
In a preferred embodiment, the compounds of the invention are provided for the uses detailed above, where the further pharmacologically active substance is selected from the group consisting of: “DNA topoisomerase I and/or II inhibitors, DNA intercalators, alkylating agents, microtubuli destabilizers, hormone and/or growth factor receptor agonists and/or antagonists, antibodies against growth factors and their receptors, kinase inhibitors, antimetabolites”.
In a preferred embodiment, the compounds of the invention are provided for the above uses, where the further pharmacologically active substance is selected from the group consisting of: “asparaginase, bleomycin, carboplatin, carmustine, chlorambucil, cisplatin, colaspase, cyclophosphamide, cytarabine, dacarbazine, dactinomycin, daunorubicin, doxorubicin (adriamycin), epirubicin, etoposide, 5-fluorouracil, hexamethylmelamine, hydroxyurea, ifosfamide, irinotecan, leucovorin, lomustine mechlorethamine, 6-mercaptopurine, mesna, methotrexate, mitomycin C, mitoxantrone, prednisolone, prednisone, procarbazine, raloxifen, streptozocin, tamoxifen, thioguanine, topotecan, vinblastine, vincristine, vindesine, aminoglutethimide, L-asparaginase, azathioprine, 5-azacytidine cladribine, busulfan, diethylstilbestrol, 2′,2′-difluorodeoxycytidine, docetaxel, erythrohydroxynonyladenine, ethynylestradiol, 5-fluorodeoxyuridine, 5-fluorodeoxyuridine monophosphate, fludarabine phosphate, fluoxymesterone, flutamide, hydroxyprogesterone caproate, idarubicin, interferon, medroxyprogesterone acetate, megestrol acetate, melphalan, mitotane, paclitaxel, oxaliplatin, pentostatin, N-phosphonoacetyl-L-aspartate (PALA), plicamycin, semustine, teniposide, testosterone propionate, thiotepa, trimethylmelamine, uridine, vinorelbine, epothilone, gemcitabine, taxotere, BCNU, CCNU, DTIC, 5-fluorouarcil, herceptin, avastin, erbitux, sorafenib, gleevec, iressa, tarceva, rapamycin, actinomycin D, sunitinib (sutent)”.
The compounds of the present invention and/or where appropriate additional pharmacologically active substances or pharmaceutical compositions as described herein can be administered in a known manner. The route of administration may thereby be any route which effectively transports the active compound to the appropriate or desired site of action, for example orally or non-orally, in particular topically, transdermally, pulmonary, rectally, intravaginally, nasally or parenteral or by implantation. Oral administration is preferred.
The compounds of the present invention and/or where appropriate additional pharmacologically active substances or pharmaceutical compositions as described herein can be administered as liquid, semisolid and solid medicinal forms. This takes place in the manner suitable in each case in the form of aerosols, powders, dusting powders and epipastics, tablets including coated tablets, emulsions, foams, solutions, suspensions, gels, ointments, pastes, pills, pastilles, capsules or suppositories. They can be administered in a suitable dosage form to the skin, epicutaneously as solution, suspension, emulsion, foam, ointment, paste or plaster; via the oral and lingual mucosa, buccally, lingually or sublingually as tablet, pastille, coated tablet, linctus or gargle; via the gastric and intestinal mucosa, enterally as tablet, coated tablet, capsule, solution, suspension or emulsion; via the rectal mucosa, rectally as suppository, rectal capsule or ointment; via the nasal mucosa, nasally as drops, ointments or spray; via the bronchial and alveolar epithelium, by the pulmonary route or by inhalation as aerosol or inhalant; via the conjunctiva, conjunctivally as eyedrops, eye ointment, eye tablets, lamellae or eye lotion; via the mucosa of the genital organs, intravaginally as vaginal suppositories, ointments and douche, by the intrauterine route as uterine pessary; via the urinary tract, intraurethrally as irrigation, ointment or bougie; into an artery, intraarterially as injection; into a vein, intravenously as injection or infusion; into the skin, intracutaneously as injection or implant; under the skin, subcutaneously as injection or implant; into the muscle, intramuscularly as injection or implant; into the abdominal cavity, intraperitoneally as injection or infusion.
As already explained above, the compounds of the invention can also be combined with other pharmaceutically active substances. It is possible for the purpose of a combination therapy to administer the individual active ingredients simultaneously or separately, in particular either by the same route (for example orally) or by separate routes (for example orally and as injection). They may be present and administered in identical or different amounts in a unit dose. It is also possible to use a particular dosage regimen when this appears appropriate. It is also possible in this way to combine a plurality of the novel compounds according to the invention with one another.
The compounds of the invention and/or where appropriate additional pharmacologically active substances are converted into a form which can be administered and are mixed where appropriate with pharmaceutically acceptable carriers and/or auxiliaries and/or diluents. Suitable excipients and carriers are described for example in Zanowiak P, Ullmann's Encyclopedia of Industrial Chemistry 2005, Pharmaceutical Dosage Forms, 1-33; Spiegel A J et al., Journal of Pharmaceutical Sciences 1963, 52: 917-927; Czetsch-Lindenwald H, Pharm. Ind. 1961, 2: 72-74; Fiedler H P, Lexikon der Hilfsstoffe für Pharmazie, Kosmetik and angrenzende Gebiete 2002, Editio Cantor Verlag, p65-68.
Oral administration can take place for example in solid form as tablet, capsule, gel capsule, coated tablet, granulation or powder, but also in the form of a drinkable solution or emulsion. The compounds of the invention can for oral administration be combined with known and ordinarily used, physiologically acceptable auxiliaries and carriers, such as, for example, gum arabic, talc, starch, sugars such as, for example, mannitol, methylcellulose, lactose, gelatin, surface-active agents, magnesium stearate, cyclodextrins, aqueous or nonaqueous carriers, diluents, dispersants, emulsifiers, lubricants, preservatives and flavorings (e.g. essential oils). The compounds of the invention can also be dispersed in a microparticulate, e.g. nanoparticulate, composition.
Non-oral administration can take place for example by intravenous, subcutaneous, intramuscular injection of sterile aqueous or oily solutions, suspensions or emulsions, by means of implants or by ointments, creams or suppositories. Administration as sustained release form is also possible where appropriate. Implants may comprise inert materials, e.g. biodegradable polymers or synthetic silicones such as, for example, silicone rubber. Intravaginal administration is possible for example by means of vaginal rings. Intrauterine administration is possible for example by means of diaphragms or other suitable intrauterine devices. Transdermal administration is additionally provided, in particular by means of a formulation suitable for this purpose and/or suitable means such as, for example, patches.
The dosage may vary within a wide range depending on type and/or severity of the disease, physiological and/or pathological condition, the mode of administration, the age, gender, bodyweight and sensitivity of the subject to be treated. It is within the ability of a skilled worker to determine a “pharmacologically effective amount” of a compound of the invention and/or additional pharmacologically active substance. Administration can take place in a single dose or a plurality of separate dosages.
A suitable unit dose is, for example, from 0.001 mg to 100 mg of the active ingredient, i.e. at least one compound of the invention and, where appropriate, at least one additional pharmacologically active substance, per kg of a patient's bodyweight.
In another aspect, the present invention relates to a pharmaceutical composition comprising a pharmacologically active amount of at least one compound of the invention, preferably a compound of the invention selected from the group consisting of: compound 1, 2, 3, 4, 5, 6, 7, B, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 80, 81, 82, 83, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 325, 326, 327, 328, 329, 330, 331, 332, 333, 334, 335, 336, 337, 338, 339, 340, 341, 342, 343, 344, 345, 346, 347, 348, 349, 350, 351, 352, 353, 354, 355, 356, 357, 358, 359, 360, 361, 362, 363, 364, 365, 366, 367, 368, 369, 370, 371, 372, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 404, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 451, 452, 453, 454, 455, 456, 457, 458, 459, 460, 461, 462, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 479, 480, 481, 482, 483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 495, 496, 497, 498, 499, 500, 501, 502, 503, 504, 505, 506, 507, 508, 509, 510, 511, 512, 513, 514, 515, 516, 517, 518, 519, 520, 521, 522, 523, 524, 525, 526, 527, 528, 529, 530, 531, 532, 533, 534, 535, 536, 537, 538, 539, 540, 541, 542, 543, 544, 545, 546, 547, 548, 549, 550, 551, 552, 553, 554, 555, 556, 557, 558, 559, 560, 561, 562, 563, 564, 565, 566, 567, 568, 569, 570, 571, 572, 573, 574, 575, 576, 577, 578, 579, 580, 581, 582, 583, 584, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594, 595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 605, 606, 607, 608, 609, 610, 611, 612, 613, 614, 615, 616, 617, 618, 619, 620, 621, 622, 623, 624, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635, 636, 637, 638, 639, 640, 641, 642, 643, 644, 645, 646, 647, 648, 649, 650, 651, 652, 653, 654, 655, 656, 657, 658, 659, 660, 661, 662, 663, 664, 665, 666, 667, 668, 669, 670, 671, 672, 673, 674, 675, 676, 677, 678, 679, 680, 681, 682, 683, 684, 685, 686, 687, 688, 689, 690, 691, 692, 693, 694, 695, 696, 697, 698, 699, 700, 701, 702, 703, 704, 705, 706, 707, 708, 709, 710, 711, 712, 713, 714, 715, 716, 717, 718, 719, 720, 721, 722, 723, 724, 725, 726, 727, 728, 729, 730, 731, 732, 733, 734, 735, 736, 737, 738, 739, 740, 741, 742, 743, 744, 745, 746, 747, 748, 749, 750, 751, 752, 753, 754, 755, 756, 757, 758, 759, 760, 761, 762, 763, 764, 765, 766, 767, 768, 769, 770, 771, 772, 773 and/or compound 774.
In a further aspect, such a pharmaceutical composition additionally comprises at least one pharmaceutically acceptable carrier and/or auxiliary and/or comprises at least one further pharmacologically active substance.
In a preferred embodiment, such further pharmacologically active substance is selected from the group consisting of: “DNA topoisomerase I and/or II inhibitors, DNA intercalators, alkylating agents, microtubuli destabilizers, hormone and/or growth factor receptor agonists and/or antagonists, antibodies against growth factors and their receptors, kinase inhibitors, antimetabolites” and preferably is selected from the group consisting of: “asparaginase, bleomycin, carboplatin, carmustine, chlorambucil, cisplatin, colaspase, cyclophosphamide, cytarabine, dacarbazine, dactinomycin, daunorubicin, doxorubicin (adriamycin), epirubicin, etoposide, 5-fluorouracil, hexamethylmelamine, hydroxyurea, ifosfamide, irinotecan, leucovorin, lomustine mechlorethamine, 6-mercaptopurine, mesna, methotrexate, mitomycin C, mitoxantrone, prednisolone, prednisone, procarbazine, raloxifen, streptozocin, tamoxifen, thioguanine, topotecan, vinblastine, vincristine, vindesine, aminoglutethimide, L-asparaginase, azathioprine, 5-azacytidine cladribine, busulfan, diethylstilbestrol, 2′,2′-difluorodeoxycytidine, docetaxel, erythrohydroxynonyladenine, ethynylestradiol, 5-fluorodeoxyuridine, 5-fluorodeoxyuridine monophosphate, fludarabine phosphate, fluoxymesterone, flutamide, hydroxyprogesterone caproate, idarubicin, interferon, medroxyprogesterone acetate, megestrol acetate, melphalan, mitotane, paclitaxel, oxaliplatin, pentostatin, N-phosphonoacetyl-L-aspartate (PALA), plicamycin, semustine, teniposide, testosterone propionate, thiotepa, trimethylmelamine, uridine, vinorelbine, epothilone, gemcitabine, taxotere, BCNU, CCNU, DTIC, 5-fluorouarcil, herceptin, avastin, erbitux, sorafenib, gleevec, iressa, tarceva, rapamycin, actinomycin D, sunitinib (sutent)”.
Concerning the pharmaceutical compositions of the invention, at least one of the compounds of the invention is present in a pharmacologically effective amount, preferably in a unit dose, e.g. the aforementioned unit dose, specifically and preferably in an administration form which makes oral administration possible. Furthermore, reference may be made to that already said in connection with the possible uses and administrations of the compounds of the invention.
In a further aspect of the present invention, the object of the invention has surprisingly been solved by providing a kit comprising a pharmacologically active amount of at least one compound of the invention as detailed above and/or at least one pharmaceutical composition as detailed above and a pharmacologically active amount of at least one further pharmacologically active substance as defined above.
General Synthesis Methods for the Compounds of the Invention:
The processes for preparing the substituted pyrido[2,3-b]pyrazine compounds of the invention are illustrated below.
The compounds of the invention are obtainable according to the following schemes (schemes 1-12) and corresponding processes known to those skilled in the art:
The definition of the R1 to R18 and X2, X3, X9 and X41 radicals shown in the following schemes corresponds to the substituents defined above in connection with the general formula (I), for example Z radicals, R radicals, X radicals, Y radicals, etc. The individual assignment can be accomplished in a simple manner by the person skilled in the art on the basis of his or her average technical knowledge.




Precursors for selected examples of the compounds of the invention in which the substituent R6 is not to be H are, for example, obtainable by the process in scheme 2 or a corresponding process known to those skilled in the art.




The precursors 5a, 5b, 6a and 6b from schemes 1 and 2 can be converted to the compounds of the invention, for example, by the process in schemes 3 and 4 or a corresponding process known to those skilled in the art.








Selected examples of the compounds of the invention in which the substituents R1, R2 and/or R5 may be selected substituted aryl, heteroaryl, alkyl, alkenyl or alkynyl radicals are, for example, obtainable by the process in scheme 5 or corresponding processes known to those skilled in the art.





Selected examples of the compounds of the invention in which the substituents R1, R2 and/or R5 may be selected NH2 or NX2X3-substituted radicals are, for example, obtainable by the process in scheme 6 or corresponding processes known to those skilled in the art.




Selected examples of the compounds of the invention in which the substituents R1 may be selected O—X9 or S—X41-substituted radicals are, for example, obtainable by the process in scheme 7 or corresponding processes known to those skilled in the art.




Precursors for selected examples of the compounds of the invention in which the substituents R3 and R4 are to be substituted by hydrogen are, for example, obtainable by the process in scheme 8 or a corresponding process known to those skilled in the art.




The precursors 36a and 36b from scheme 8 can be converted to the compounds of the invention, for example, by the process in schemes 9-12 or a corresponding process known to those skilled in the art.
















The starting compounds and intermediates are either commercially available or can be prepared by procedures known per se or known to those skilled in the art. The reactants 5-18 and 36-48 are valuable intermediates for the preparation of the compounds of the invention.
For the preparation of the starting compounds, intermediates and the compounds of the invention, reference is made inter alia to the patents WO 2004/104002 and WO 2004/104003, and also, for example, to the following primary literature whose contents are hereby incorporated into the disclosure of the present application:

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Under some of the reaction conditions specified, OH, SH and NH2 groups may possibly enter into undesired side reactions. It is therefore preferred to provide them with protecting groups or, in the case of NH2, to replace it with NO2, and then to eliminate the protecting group or to reduce the NO2 group. For instance, in a modification of the above-described processes, at least one OH group in the starting compounds can be replaced, for example, by a benzyloxy group, and/or at least one SH group can be replaced, for example, by an S-benzyl group and/or at least one NH2 group can be replaced, for example, by an NH-benzyl group or by an NO2 group. Subsequently, at least one—preferably all—benzyloxy group(s) or NH-benzyl group(s) can be eliminated, for example, with hydrogen and palladium on carbon, and/or at least one—preferably all—S-benzyl group(s) can be eliminated, for example, with sodium in ammonia, and/or at least one—preferably all—NO2 group(s) can be reduced, for example, with hydrogen and Raney nickel to NH2.
Under some of the reaction conditions mentioned, OH, NH2 and COOH groups may possibly enter into undesired side reactions. It is therefore preferred to convert starting compounds and intermediates which contain at least one OH group and/or at least one NH2 group and/or at least one COOH group to corresponding carboxylic ester and carboxamide derivatives. In a modification of the above-described processes, starting compounds and intermediates which have at least one OH group and/or which have at least one NH2 group can be converted to carboxylic ester or carboxamide derivatives by reaction with an activated carboxylic acid group, for example a carbonyl chloride group. In a modification of the above-described processes, starting compounds and intermediates which contain at least one COOH can be converted to carboxylic ester or carboxamide derivatives by reaction with an activating agent, for example thionyl chloride or carbonyldiimidazole, and subsequent reaction with a suitable alcohol or amine. Subsequently, at least one—preferably all—carboxylic ester or carboxamide group(s) in the starting compounds and intermediates can be detached, for example, with dilute aqueous acids or bases, in order to release one—preferably all—OH group(s) and/or NH2 group(s) and/or COOH group(s).
The compounds of the invention were named using the AutoNom 2000 software (ISISTM/Draw 2.5; MDL).
The contents of all cited references are hereby incorporated by reference in their entirety. The invention is explained in more detail by means of the following examples without, however, being restricted thereto.
EXAMPLES
I) Preparation and Physicochemical Characterization of Selected Compounds of the Invention
The general synthesis methods which are based on the synthesis schemes 1-12 were used to synthesize the following compounds of the invention. In addition, their NMR spectroscopy data and mass spectrometry data and melting points are included, respectively.
The precursors used for the preparation of the compounds of the invention can—unless stated otherwise—be synthesized by processes known to those skilled in the art.
The chemicals and solvents used were obtained commercially from the conventional suppliers (Acros, Aldrich, Fluka, Lancaster, Maybridge, Merck, Sigma, TCI, etc.) or synthesized.
Example 1
1-(6-Chloro-pyrido[2,3-b]pyrazin-3-yl)-3-ethyl-urea




A total of 5.0 g 6-Chloro-pyrido[2,3-b]pyrazin-3-ylamine (27.7 mmol; 1 eq) was suspended in 150 mL of dry 1,4-dioxane. 2.63 g (33.2 mmol; 1.2 eq) ethyl isocyanate was added and the reaction mixture was stirred at 100° C. for 4 hours. Additional 1.97 g (27.7 mmol; 1 eq) of ethyl isocyanate were added and the resulting solution was stirred at 100° C. for further 4 hours. After cooling to room temperature, the precipitate was filtered of and dried in vacuo to afford 6.5 g (93.3% yield) of 1-(6-Chloro-pyrido[2,3-b]pyrazin-3-yl)-3-ethyl-urea.
m.p.: 240° C.
ESI-MS: found: 252.0 (M+H+); calculated: 251.68 g/mol
1H-NMR (DMSO-d6) δ=10.38 (s, 1H), 9.00 (s, 1H), 8.42 (m, 2H), 7.69 (d, 1H), 3.30 (m, 2H), 1.15 (t, 3H) ppm
Example 2
1-(6-Chloro-pyrido[2,3-b]pyrazin-3-yl)-3-ethyl-thiourea




A total of 5.0 g 6-Chloro-pyrido[2,3-b]pyrazin-3-ylamine (27.7 mmol; 1 eq) was dissolved in 150 mL of dry DMF. 1.32 g NaH (60% dispersion in mineral oil; 33.2 mmol; 1.2 eq) was added and the dark brown solution was stirred at room temperature for 1 hour. 2.4 g (27.7 mmol; 1 eq) ethyl isothiocyanate was then added and the resulting mixture was stirred at room temperature for 3 h. The reaction mixture was then poured into 500 mL of water. The solution was neutralized with 1 N HCl whereas the product crystallizes. The brown solid was filtered of and recrystallised from dichloromethane/diethyl ether to afford 3.6 g (48.5% yield) of 1-(6-Chloro-pyrido[2,3-b]pyrazin-3-yl)-3-ethyl-thiourea.
m.p.: 215° C.
ESI-MS: found: 268.1 (M+H+); calculated: 267.74 g/mol
1H-NMR (DMSO-d6) δ=11.55 (s, 1H), 11.40 (s, 1H), 8.88 (s, 1H), 8.44 (d, 1H), 7.75 (d, 1H), 3.75 (m, 2H), 1.30 (t, 3H) ppm
Example 3
4-(3-Amino-pyrido[2,3-b]pyrazin-6-yl)-2-methoxy-phenol




To a suspension of 1.13 g 6-Chloro-pyrido[2,3-b]pyrazin-3-ylamine (5.94 mmol; 1 eq) and 1.67 g 2-Methoxy-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenol (6.55 mmol; 1.1 eq.) in ethylene glycol dimethyl ether (45 mL) under Ar, a solution of 6.29 g sodium carbonate (59.3 mmol; 10 eq.) in water (20 mL) and a suspension of 378 mg FluoroFlash catalyst (0.24 mmol; 0.04 eq.) in undecafluoro(trifluoromethyl)cyclohexane (45 mL) were added. The mixture was heated to 75° C. for 5 hours. Additional 0.76 g (2.97 mmol; 0.5 eq) of 2-Methoxy-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenol were added and the resulting mixture was stirred at 75° C. for 7.5 hours. After cooling to room temperature, the aqueous and organic phase were separated from the fluorous phase and concentrated in vacuo. The residue was dissolved in methanol and methylene dichloride and filtered. The black solution was again concentrated in vacuo. The residue was taken up in water and the resulting solution was neutralized with 1N HCl whereas the product crystallizes. The brown solid was filtered of, washed with water and dried in vacuo to afford 1.5 g (80.2% yield) of 4-(3-Amino-pyrido[2,3-b]pyrazin-6-yl)-2-methoxy-phenol.
ESI-MS: found: 269.0 (M+H+); calculated: 268.28 g/mol
1H-NMR (DMSO-d6) δ=9.47 (s, 1H), 8.29 (s, 1H), 8.15 (d, 1H), 7.91 (d, 1H), 7.84 (s, 1H), 7.67 (d, 1H), 7.34 (s, 2H), 6.90 (d, 1H), 3.89 (s, 3H) ppm
Example 4
Compound 1—1-Ethyl-3-(6-p-tolylamino-pyrido[2,3-b]pyrazin-3-yl)-urea
A total of 100 mg 1-(6-Chloro-pyrido[2,3-b]pyrazin-3-yl)-3-ethyl-urea/example 1 (0.40 mmol; 1 eq) was suspended in 3 ml of n-propanole. To this suspension 51 mg p-toluidine (0.48 mmol; 1.2 eq) was added and the reaction mixture was stirred at 100° C. for 5 hours. After cooling to room temperature, the precipitate formed was filtered and washed with diethyl ether. The brown crystals were dissolved in dichloromethane, washed with 0.5 N HCl and NaHCO3. The solution was dried over MgSO4 and the solvent was removed to afford 74 mg (52.4% yield) of 1-Ethyl-3-(6-p-tolylamino-pyrido[2,3-b]pyrazin-3-yl)-urea (compound 1) as yellow powder.
m.p.: 235° C.
ESI-MS: found: 323.0 (M+H+); calculated: 322.37 g/mol
1H-NMR (DMSO-d6) δ=9.97 (s, 1H), 9.14 (s, 1H), 8.72 (s, 1H), 8.23 (s, 1H), 8.00 (d, 1H), 7.86 (d, 2H), 7.16 (d, 2H), 7.09 (d, 1H), 3.27 (m, 2H), 1.18 (t, 3H) ppm
Example 5
Compound 2—1-[6-(4-Amino-3-methoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-3-ethyl-urea
To a suspension of 100 mg 1-(6-Chloro-pyrido[2,3-b]pyrazin-3-yl)-3-ethyl-urea/example 1 (0.39 mmol; 1 eq) and 108 mg 2-Methoxy-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenylamine (0.43 mmol; 1.1 eq.) in ethylene glycol dimethyl ether (4 mL) under Ar, a solution of 414 mg sodium carbonate (3.9 mmol; 10 eq.) in water (1.5 mL) and a suspension of 12 mg FluoroFlash catalyst (0.01 mmol; 0.02 eq.) in undecafluoro(trifluoromethyl)cyclohexane (4 mL) were added. The mixture was heated to 60° C. for 4 hours. After cooling to room temperature, the aqueous and organic phase were separated from the fluorous phase and concentrated in vacuo. The residue was dissolved in methanol and methylene dichloride and filtered. The black solution was again concentrated in vacuo. The residue was taken up in water and the resulting solution was neutralized with 1 N HCl whereas the product crystallizes. The brown solid was filtered of, washed with water and dried in vacuo to afford 120 mg (86.4% yield) of 1-[6-(4-Amino-3-methoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-3-ethyl-urea (compound 2).
m.p.: >310° C.
ESI-MS: found: 339.1 (M+H+); calculated: 338.37 g/mol
1H-NMR (DMSO-d6) δ=10.15 (s, 1H), 8.88 (s, 1H), 8.55 (s, 1H), 8.26 (d, 1H), 8.13 (d, 1H), 7.78 (s, 1H), 7.71 (d, 1H), 6.75 (s, 1H), 5.38 (d, 2H), 3.91 (s, 3H), 3.27 (m, 2H), 1.18 (t, 3H) ppm
Example 6
Compound 3—1-[6-(4-Hydroxy-3-methoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-3-phenyl-urea
In dry 1,4-dioxane (6 mL) was stirred 111.3 mg 4-(3-Amino-pyrido[2,3-b]pyrazin-6-yl)-2-methoxy-phenol/example 3 (0.35 mmol; 1 eq.). The mixture was heated to 70° C. 120 mg (0.99 mmol; 2.8 eq) Phenyl isocyanate was added and the reaction mixture was stirred at 70° C. for 4 hours. Additional 64 mg (0.53 mmol; 1.5 eq) of Phenyl isocyanate were added and the resulting mixture was stirred at 70° C. for 4 hours. After cooling to room temperature, the mixture was concentrated in vacuo and the residue was stirred in ethanol. Diethyl ether was added and the product was collected by filtration. The solid was washed with ethanol, methylene dichloride and diethyl ether and dried in vacuo to afford 92.5 mg (67.7% yield) of 1-[6-(4-Hydroxy-3-methoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-3-phenyl-urea (compound 3).
m.p.: 240° C.
ESI-MS: found: 388.3 (M+H+); calculated: 387.40 g/mol
1H-NMR (DMSO-d6) δ=10.98 (s, 1H), 10.45 (s, 1H), 9.62 (s, 1H), 9.07 (s, 1H), 8.40 (d, 1H), 8.26 (d, 1H), 7.96 (s, 1H), 7.82 (d, 1H), 7.61 (d, 2H), 7.39 (t, 2H), 7.11 (t, 1H), 6.96 (d, 1H), 3.94 (s, 3H) ppm
The following examples were synthesized according to the Compounds 1-3 and the general schemes 1-12:
Example 7
Compound 4—1-Ethyl-3-(6-phenyl-pyrido[2,3-b]pyrazin-3-yl)-urea
ESI-MS: found: 294.1 (M+H+); calculated: 293.0 g/mol
1H-NMR (DMSO-d6) δ=10.27 (s, 1H); 8.97 (s, 1H); 8.65 (s, 1H); 8.45 (d, 1H); 8.29 (dd, 2H); 8.26 (d, 1H); 7.53-7.60 (m, 3H); 3.32-3.36 (m, 2H); 1.20 (t, 3H) ppm.
Example 8
Compound 5—1-Ethyl-3-[6-(4-hydroxy-3-methoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-urea
ESI-MS: found: 340.2 (M+H+); calculated: 339.0 g/mol
1H-NMR (DMSO-d6) δ=10.21 (s, 1H); 9.58 (s, 1H); 8.94 (s, 1H); 8.55 (s, 1H); 8.35 (d, 1H); 8.20 (dd, 1H); 7.89 (d, 1H); 7.78 (dd, 1H); 6.94 (d, 1H); 3.92 (s, 3H); 3.29-3.35 (m, 2H); 1.19 (t, 3H) ppm.
Example 9
Compound 6—1-[6-(4-Chloro-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-3-ethyl-urea
m.p.: 276° C.
ESI-MS: found: 328.2 (M+H+); calculated: 327.0 g/mol
1H-NMR (DMSO-d6) δ=10.29 (s, 1H); 8.97 (s, 1H); 8.65 (s, 1H); 8.45 (d, 1H); 8.33 (dd, 1H); 8.27 (d, 1H); 7.64 (d, 2H); 3.31-3.35 (m, 2H); 1.19 (t, 3H) ppm.
Example 10
Compound 7—1-Ethyl-3-(6-pyridin-4-yl-pyrido[2,3-b]pyrazin-3-yl)-urea
m.p.: 211° C.
ESI-MS: found: 295.2 (M+H+); calculated: 294.0 g/mol
1H-NMR (DMSO-d6) δ=10.35 (s, 1H); 9.03 (s, 1H); 8.80 (d, 2H); 8.62 (s, 1H); 8.54 (d, 1H); 8.36 (d, 1H); 8.23 (d, 2H); 3.31-3.36 (m, 2H); 1.20 (t, 3H) ppm.
Example 11
Compound 8—1-[6-(3-Chloro-4-hydroxy-5-methoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-3-ethyl-urea
ESI-MS: found: 374.3 (M+H+); calculated: 373.0 g/mol
1H-NMR (DMSO-d6) δ=10.23 (s, 1H); 10.00 (s, 1H); 8.97 (s, 1H); 8.53 (s, 1H); 8.38 (d, 1H); 8.28 (d, 1H); 7.94 (d, 1H); 7.87 (d, 1H); 3.98 (s, 3H); 3.31-3.35 (m, 2H); 1.19 (t, 3H) ppm.
Example 12
Compound 9—1-[6-(3,5-Dichloro-4-hydroxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-3-ethyl-urea
m.p.: >300° C.
ESI-MS: found: 378.4 (M+H+); calculated: 377.0 g/mol
1H-NMR (DMSO-d6) δ=10.00 (s, 1H); 8.71 (s, 1H); 8.66 (s, 1H); 8.05 (d, 1H); 8.00 (s, 2H); 7.92 (d, 1H); 3.31-3.35 (m, 2H); 1.18 (t, 3H) ppm.
Example 13
Compound 10—1-Ethyl-3-[6-(1-methyl-1H-pyrazol-4-yl)-pyrido[2,3-b]pyrazin-3-yl]-urea
m.p.: 211° C.
ESI-MS: found: 298.2 (M+H+); calculated: 297.0 g/mol
1H-NMR (DMSO-d6) δ=10.17 (s, 1H); 8.85 (s, 1H); 8.65 (s, 1H); 8.51 (s, 1H); 8.29 (d, 1H); 8.19 (s, 1H); 7.91 (d, 1H); 3.94 (s, 3H); 3.31-3.35 (m, 2H); 1.19 (t, 3H) ppm.
Example 14
Compound 11—1-Ethyl-3-[6-(4-methoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-urea
m.p.: 244° C.
ESI-MS: found: 323.9 (M+H+); calculated: 323.0 g/mol
1H-NMR (DMSO-d6) δ=10.22 (s, 1H); 8.92 (s, 1H); 8.65 (s, 1H); 8.38 (d, 1H); 8.27 (d, 2H); 8.20 (d, 1H); 7.12 (d, 2H); 3.86 (s, 3H); 3.31-3.36 (m, 2H); 1.19 (t, 3H) ppm.
Example 15
Compound 12—1-Ethyl-3-[6-(3-isopropoxy-phenylamino)-pyrido[2,3-b]pyrazin-3-yl]-urea
ESI-MS: found: 367.0 (M+H+); calculated: 366.0 g/mol
1H-NMR (DMSO-d6) δ=10.02 (s, 1H); 9.77 (s, 1H); 8.67 (s, 1H); 8.47 (s, 1H); 8.03 (d, 1H); 7.97 (s, 1H); 7.20-7.22 (m, 2H); 7.11 (d, 1H); 6.57-6.60 (m, 1H); 4.57-4.63 (m, 1H); 3.26-3.31 (m, 2H); 1.30 (d, 6H); 1.19 (t, 3H) ppm.
Example 16
Compound 13—1-Ethyl-3-(6-phenylamino-pyrido[2,3-b]pyrazin-3-yl)-urea
m.p.: 202° C.
ESI-MS: found: 309.1 (M+H+); calculated: 308.0 g/mol
1H-NMR (DMSO-d6) δ=10.00 (s, 1H); 9.81 (s, 1H); 8.74 (s, 1H); 8.22 (s, 1H); 8.03 (d, 1H); 7.98 (d, 2H); 7.35 (dd, 2H); 7.13 (d, 1H); 7.02 (dd, 1H); 3.24-3.30 (m, 2H); 1.18 (t, 3H) ppm.
Example 17
Compound 14—1-Phenyl-3-(6-phenylamino-pyrido[2,3-b]pyrazin-3-yl)-urea
m.p.: 251° C.
ESI-MS: found: 357.3 (M+H+); calculated: 356.0 g/mol
1H-NMR (DMSO-d6) δ=11.13 (s, 1H); 10.31 (s, 1H); 9.90 (s, 1H); 8.75 (s, 1H); 8.08 (d, 1H); 8.06 (d, 2); 7.59 (d, 2H); 7.37-7.42 (m, 4H); 7.18 (d, 1H); 7.09 (dd, 1H); 7.06 (dd, 1H) ppm.
Example 18
Compound 15—1-[6-(3,5-Dichloro-4-hydroxy-phenylamino)-pyrido[2,3-b]pyrazin-3-yl]-3-ethyl-urea
m.p.: 272° C.
ESI-MS: found: 393.3 (M+H+); calculated: 392.0 g/mol
1H-NMR (DMSO-d6) δ=10.06 (s, 1H); 9.85 (s, 1H); 9.72 (s, 1H); 8.69 (s, 1H); 8.42 (s, 1H); 8.09 (s, 2H); 8.04 (d, 1H); 7.04 (d, 1H); 3.25-3.30 (m, 2H); 1.22 (t, 3H) ppm.
Example 19
Compound 16—1-[6-(4-Hydroxy-3-methoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-3-propyl-urea
m.p.: 220-222° C.
ESI-MS: found: 354.1 (M+H+); calculated: 353.38 g/mol
1H-NMR (DMSO-d6) δ=10.25 (s, 1H), 9.59 (s, 1H), 8.90 (bs, 1H), 8.87 (s, 1H), 8.34 (d, 1H), 8.20 (d, 1H), 7.92 (s, 1H), 7.77 (d, 1H), 6.94 (d, 1H), 3.91 (s, 3H), 3.27-3.33 (m, 2H), 1.60 (m, 2H), 1.04 (t, 3H) ppm
Example 20
Compound 17—1-Cyclohexyl-3-[6-(4-hydroxy-3-methoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-urea
m.p.: 232-235° C.
ESI-MS: found: 394.2 (M+H+); calculated: 393.44 g/mol
1H-NMR (DMSO-d6) δ=10.19 (s, 1H), 9.60 (s, 1H), 9.10 (bs, 1H), 8.85 (s, 1H), 8.34 (d, 1H), 8.21 (d, 1H), 7.94 (s, 1H), 7.77 (d, 1H), 6.94 (d, 1H), 3.91 (s, 3H), 3.78 (m, 1H), 1.75-1.85 (m, 4H), 1.40-1.54 (m, 6H) ppm
Example 21
Compound 18—1-Allyl-3-[6-(4-hydroxy-3-methoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-urea
m.p.: 211-213° C.
ESI-MS: found: 352.0 (M+H+); calculated: 351.36 g/mol
1H-NMR (DMSO-d6) δ=10.33 (s, 1H), 9.59 (s, 1H), 8.94 (bs, 1H), 8.90 (bs, 1H), 8.35 (d, 1H), 8.21 (d, 1H), 7.89 (s, 1H), 7.77 (d, 1H), 6.94 (d, 1H), 6.00 (m, 1H), 5.38 (d, 1H), 5.19 (d, 1H), 3.97 (t, 2H), 3.91 (s, 3H) ppm
Example 22
Compound 19—1-[6-(4-Hydroxy-3-methoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-3-isopropyl-urea
m.p.: 212-214° C.
ESI-MS: found: 354.0 (M+H+); calculated: 353.38 g/mol
1H-NMR (DMSO-d6) δ=10.10 (s, 1H), 9.59 (s, 1H), 8.94 (s, 1H), 8.58 (bs, 1H), 8.34 (d, 1H), 8.21 (d, 1H), 7.92 (s, 1H), 7.77 (d, 1H), 6.94 (d, 1H), 3.92 (m, 1H), 3.91 (s, 3H), 1.24 (d, 6H) ppm
Example 23
Compound 20—1-Cyclopentyl-3-[6-(4-hydroxy-3-methoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-urea
m.p.: 222-225° C.
ESI-MS: found: 380.1 (M+H+); calculated: 379.42 g/mol
1H-NMR (DMSO-d6) δ=10.15 (s, 1H), 9.60 (s, 1H), 9.09 (bs, 1H), 8.85 (s, 1H), 8.34 (d, 1H), 8.20 (d, 1H), 7.96 (s, 1H), 7.77 (d, 1H), 6.94 (d, 1H), 4.15 (m, 1H), 3.91 (s, 3H), 1.92 (m, 2H), 1.81 (m, 2H), 1.66 (m, 2H), 1.57 (m, 2H) ppm
Example 24
Compound 21—1-Ethyl-3-[6-(4-hydroxy-3-methoxy-phenylamino)-pyrido[2,3-b]pyrazin-3-yl]-urea
m.p.: 255° C.
ESI-MS: found: 355.0 (M+H+); calculated: 354.37 g/mol
1H-NMR (DMSO-d6) δ=9.94 (bs, 1H), 9.59 (s, 1H), 8.68 (bs, 2H), 8.55 (s, 1H), 7.95 (d, 1H), 7.83 (s, 1H), 7.19 (d, 1H), 7.04 (d, 1H), 6.75 (d, 1H), 3.82 (s, 3H), 3.27 (m, 2H), 1.15 (t, 3H) ppm
Example 25
Compound 22—1-[6-(3,4-Dimethoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-3-ethyl-urea
m.p.: >235° C.
ESI-MS: found: 354.1 (M+H+); calculated: 353.38 g/mol
1H-NMR (DMSO-d6) δ=10.23 (s, 1H), 8.98 (s, 1H), 8.53 (bs, 1H), 8.38 (d, 1H), 8.25 (d, 1H), 7.90 (s, 1H), 7.88 (d, 1H), 7.14 (d, 1H), 3.91 (s, 3H), 3.86 (s, 3H), 3.32 (m, 2H), 1.19 (t, 3H) ppm
Example 26
Compound 23—1-Ethyl-3-[6-(3,4,5-trimethoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-urea
m.p.: >230° C.
ESI-MS: found: 384.1 (M+H+); calculated: 383.41 g/mol
1H-NMR (DMSO-d6) δ=10.25 (s, 1H), 9.03 (s, 1H), 8.44 (bs, 1H), 8.42 (d, 1H), 8.32 (d, 1H), 7.60 (s, 2H), 3.93 (s, 6H), 3.76 (s, 3H), 3.32 (m, 2H), 1.19 (t, 3H) ppm
Example 27
Compound 24—1-Ethyl-3-[6-(4-hydroxy-phenylamino)-pyrido[2,3-b]pyrazin-3-yl]-urea
m.p.: 277° C.
ESI-MS: found: 325.1 (M+H+); calculated: 324.34 g/mol
1H-NMR (DMSO-d6) δ=9.92 (s, 1H), 9.59 (s, 1H), 9.16 (bs, 1H), 8.65 (s, 1H), 8.34 (bs, 1H), 7.94 (d, 1H), 7.70 (d, 2H), 7.04 (d, 1H), 6.76 (d, 2H), 3.26 (m, 2H), 1.16 (t, 3H) ppm
Example 28
Compound 25—1-Ethyl-3-(6-p-tolylamino-pyrido[2,3-b]pyrazin-3-yl)-thiourea
m.p.: 195° C.
ESI-MS: found: 339.0 (M+H+); calculated: 338.44 g/mol
1H-NMR (DMSO-d6) δ=11.97 (t, 1H), 11.14 (s, 1H), 9.81 (s, 1H), 8.48 (s, 1H), 8.02 (d, 1H), 7.87 (d, 2H), 7.13-7.15 (d, 3H), 3.67 (m, 2H), 2.29 (s, 3H), 1.36 (t, 3H) ppm
Example 29
Compound 26—1-[6-(4-Hydroxy-3-methoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-3-phenethyl-urea
m.p.: 235-237° C.
ESI-MS: found: 416.2 (M+H+); calculated: 415.46 g/mol
1H-NMR (DMSO-d6) δ=10.26 (s, 1H), 9.59 (s, 1H), 8.89 (s, 1H), 8.74 (s, 1H), 8.35 (d, 1H), 8.22 (d, 1H), 7.93 (s, 1H), 7.80 (d, 1H), 7.44 (d, 2H), 7.27 (t, 2H), 7.18 (t, 1H), 6.95 (d, 1H), 3.88 (s, 3H), 3.53 (m, 2H), 2.92 (t, 2H) ppm
Example 30
Compound 27—1-(3,5-Dimethyl-isoxazol-4-yl)-3-[6-(4-hydroxy-3-methoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-urea
m.p.: 249-252° C.
ESI-MS: found: 407.2 (M+H+); calculated: 406.40 g/mol
1H-NMR (DMSO-d6) δ=10.64 (s, 1H), 10.10 (s, 1H), 9.61 (s, 1H), 9.01 (s, 1H), 8.40 (d, 1H), 8.26 (d, 1H), 7.90 (s, 1H), 7.79 (d, 1H), 6.94 (d, 1H), 3.91 (s, 3H), 2.40 (s, 3H), 2.25 (s, 3H) ppm
Example 31
Compound 28—1-tert-Butyl-3-[6-(4-hydroxy-3-methoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-urea
m.p.: 219-222° C.
ESI-MS: found: 368.1 (M+H+); calculated: 367.41 g/mol.
1H-NMR (DMSO-d6) δ=10.01 (s, 1H), 9.58 (s, 1H), 8.96 (s, 1H), 8.86 (s, 1H), 8.33 (d, 1H), 8.20 (d, 1H), 7.94 (s, 1H), 7.77 (d, 1H), 6.93 (d, 1H), 3.90 (s, 3H), 1.43 (s, 9H) ppm
Example 32
Compound 29—1-Benzyl-3-[6-(4-hydroxy-3-methoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-urea
m.p.: 229-231° C.
ESI-MS: found: 402.2 (M+H+); calculated: 401.43 g/mol
1H-NMR (DMSO-d6) δ=10.36 (s, 1H), 9.58 (s, 1H), 9.11 (s, 1H), 8.94 (s, 1H), 8.35 (d, 1H), 8.20 (d, 1H), 7.85 (s, 1H), 7.75 (d, 1H), 7.43 (d, 2H), 7.38 (t, 2H), 7.29 (t, 1H), 6.93 (d, 1H), 4.54 (d, 2H), 3.88 (s, 3H) ppm
Example 33
Compound 30—1-[6-(4-Hydroxy-3-methoxy-phenyl)-pyrido[2,3-b]pyrazin-3-yl]-3-[1-(2,2,2-trifluoro-acetyl)-piperidin-4-yl]-urea
m.p.: 236-239° C.
ESI-MS: found: 491.2 (M+H+); calculated: 490.45 g/mol
1H-NMR (DMSO-d6) δ=10.29 (s, 1H), 9.60 (s, 1H), 9.19 (s, 1H), 8.89 (s, 1H), 8.35 (d, 1H), 8.22 (d, 1H), 7.92 (s, 1H), 7.76 (d, 1H), 6.92 (d, 1H), 4.04 (m, 2H), 3.88 (s, 3H), 3.83 (m, 1H), 3.57 (m, 1H), 3.48 (m, 1H), 2.06 (m, 2H), 1.63 (m, 2H) ppm
Example 34
Compound 31—1-[6-(3-Chloro-4-hydroxy-phenylamino)-pyrido[2,3-b]pyrazin-3-yl]-3-ethyl-urea
m.p: 277-280° C.
ESI-MS: found: 359.1 (M+H+); calculated: 358.79 g/mol
1H-NMR (DMSO-d6) δ=10.00 (s, 1H), 9.78 (s, 1H), 9.71 (s, 1H), 8.65 (s, 1H), 8.46 (s, 1H), 7.99 (d, 1H), 7.35 (m, 1H), 7.05 (d, 1H), 6.94 (d, 1H), 3.26 (m, 2H), 1.20 (m, 3H) ppm
Example 35
Compound 32—1-Ethyl-3-[6-(quinolin-3-ylamino)-pyrido[2,3-b]pyrazin-3-yl]-urea
m.p.: 265-270° C.
ESI-MS: found: 360.4 (M+H+); calculated: 359.39 g/mol
1H-NMR (DMSO-d6) δ=10.31 (s, 1H), 10.09 (s, 1H), 9.34 (d, 1H), 9.05 (d, 1H), 8.75 (s, 1H), 8.52 (s, 1H), 8.14 (d, 1H), 7.96 (d, 1H), 7.84 (d, 1H), 7.60 (m, 2H), 7.25 (d, 1H), 3.33 (m, 2H), 1.26 (m, 3H) ppm
Example 36
Compound 33
ESI-MS: found: 760.5 (M+H+); calculated: 759.79 g/mol
Example 37
Compound 34
m.p.: 182-184° C.
ESI-MS: found: 476.3 (M+H+); calculated: 475.44 g/mol
Example 38
Compound 35
m.p.: 245-247° C.
ESI-MS: found: 365.2 (M+H+); calculated: 364.41 g/mol
Example 39
Compound 36
m.p.: 177° C.
ESI-MS: found: 338.3 (M+H+); calculated: 337.38 g/mol
Example 40
Compound 37
m.p.: 247-249° C.
ESI-MS: found: 452.2 (M+H+); calculated: 451.89 g/mol
Example 41
Compound 38
ESI-MS: found: 368.2 (M+H+); calculated: 367.41 g/mol.
Example 42
Compound 39
ESI-MS: found: 402.2 (M+H+); calculated: 401.85 g/mol.
Example 43
Compound 40
m.p.: >240° C.
ESI-MS: found: 441.4 (M+H+); calculated: 440.46 g/mol.
Example 44
Compound 41
m.p.: >350° C.
ESI-MS: found: 420.3 (M+H+); calculated: 463.30 g/mol.
Example 45
Compound 42
m.p.: 238-241° C.
ESI-MS: found: 389.3 (M+H+); calculated: 388.33 g/mol.
Example 46
Compound 43
m.p.: 246-249° C.
ESI-MS: found: 418.2 (M+H+); calculated: 417.44 g/mol.
Example 47
Compound 44
m.p.: >330° C.
ESI-MS: found: 529.3 (M+H+); calculated: 528.56 g/mol.
Example 48
Compound 45
ESI-MS: found: 367.2 (M+H+); calculated: 366.38 g/mol.
Example 49
Compound 46
m.p.: >270° C.
ESI-MS: found: 340.3 (M+H+); calculated: 339.35 g/mol.
Example 50
Compound 47
m.p.: 337-339° C.
ESI-MS: found: 390.2, 388.3 (M+H+); calculated: 388.22 g/mol.
Example 51
Compound 48
m.p.: 276-279° C.
ESI-MS: found: 422.3 (M+H+); calculated: 421.46 g/mol.
Example 52
Compound 49
m.p.: 134° C.
ESI-MS: found: 379.4 (M+H+); calculated: 378.43 g/mol.
Example 53
Compound 50
m.p.: 195-200° C.
ESI-MS: found: 383.2 (M+H+); calculated: 382.38 g/mol.
Example 54
Compound 51
m.p.: 231-232° C.
ESI-MS: found: 353.1 (M+H+); calculated: 352.40 g/mol.
Example 55
Compound 52
m.p.: 218-220° C.
ESI-MS: found: 284.1 (M+H+); calculated: 283.29 g/mol.
Example 56
Compound 53
m.p.: 257-259° C.
ESI-MS: found: 298.3 (M+H+); calculated: 297.32 g/mol.
Example 57
Compound 54
m.p.: 227-229° C.
ESI-MS: found: 382.1 (M+H+); calculated: 381.39 g/mol.
Example 58
Compound 55
m.p.: 243-246° C.
ESI-MS: found: 325.2 (M+H+); calculated: 324.34 g/mol.
Example 59
Compound 56
m.p.: 270-273° C.
ESI-MS: found: 325.3 (M+H+); calculated: 324.34 g/mol.
Example 60
Compound 57
m.p.: 181-183° C.
ESI-MS: found: 400.3 (M+H+); calculated: 399.45 g/mol.
Example 61
Compound 58
m.p.: 258-261° C.
ESI-MS: found: 374.2 (M+H+); calculated: 373.42 g/mol.
Example 62
Compound 59
m.p.: 189-191° C.
ESI-MS: found: 340.3 (M+H+); calculated: 339.40 g/mol.
Example 63
Compound 60
m.p.: 223-226° C.
ESI-MS: found: 397.3 (M+H+); calculated: 396.45 g/mol.
Example 64
Compound 61
m.p.: 270-274° C.
ESI-MS: found: 334.2 (M+H+); calculated: 333.35 g/mol.
Example 65
Compound 62
m.p.: 179-181° C.
ESI-MS: found: 366.2 (M+H+); calculated: 365.43 g/mol.
Example 66
Compound 63
m.p.: 225-227° C.
ESI-MS: found: 467.3 (M+H+); calculated: 466.54 g/mol.
Example 67
Compound 64
m.p.: 229-231° C.
ESI-MS: found: 309.2 (M+H+); calculated: 308.34 g/mol.
Example 68
Compound 65
ESI-MS: found: 480.3 (M+H+); calculated: 479.58 g/mol.
Example 69
Compound 66
m.p.: 276-279° C.
ESI-MS: found: 351.2 (M+H+); calculated: 350.38 g/mol.
Example 70
Compound 67
m.p.: 200-202° C.
ESI-MS: found: 432.0 (M+H+); calculated: 430.30 g/mol.
Example 71
Compound 68
m.p.: 182-185° C.
ESI-MS: found: 354.1 (M+H+); calculated: 353.38 g/mol.
Example 73
Compound 70
m.p.: >300° C.
ESI-MS: found: 333.2 (M+H+); calculated: 332.37 g/mol.
Example 74
Compound 71
m.p.: >300° C.
ESI-MS: found: 384.2 (M+H+); calculated: 383.41 g/mol.
Example 75
Compound 72
m.p.: >300° C.
ESI-MS: found: 311.0 (M+H+); calculated: 310.32 g/mol.
Example 76
Compound 73
ESI-MS: found: 375.2 (M+H+); calculated: 374.35 g/mol.
Example 77
Compound 74
ESI-MS: found: 456.2 (M+H+); calculated: 455.54 g/mol.
Example 78
Compound 75
ESI-MS: found: 356.2 (M+H+); calculated: 355.42 g/mol.
Example 79
Compound 76
m.p.: 253° C.
ESI-MS: found: 423.2 (M+H+); calculated: 422.44 g/mol.
Example 80
Compound 77
m.p.: >300° C.
ESI-MS: found: 381.2 (M+H+); calculated: 380.41 g/mol.
Example 81
Compound 78
m.p.: >350° C.
ESI-MS: found: 354.2 (M+H+); calculated: 353.34 g/mol.
Example 82
Compound 79
m.p.: 238.1-241.8° C.
ESI-MS: found: 354.2 (M+H+); calculated: 353.36 g/mol.
Example 83
Compound 80
m.p.: 255.3-258.2° C.
ESI-MS: found: 351.8 (M+H+); calculated: 351.41 g/mol.
Example 84
Compound 81
m.p.: 305.4-307.2° C.
ESI-MS: found: 348.2 (M+H+); calculated: 347.30 g/mol.
Example 85
Compound 82
m.p.: 255.3-257.9° C.
ESI-MS: found: 321.8 (M+H+); calculated: 321.38 g/mol.
Example 86
Compound 83
m.p.: 247.8-252.4° C.
ESI-MS: found: 326.2 (M+H+); calculated: 325.35 g/mol.
Example 87
Compound 84
m.p.: 263.9-265.6° C.
ESI-MS: found: 388.3 (M+H+); calculated: 387.42 g/mol.
Example 88
Compound 85
m.p.: 253.3-256.2° C.
ESI-MS: found: 353.2 (M+H+); calculated: 352.35 g/mol.
Example 89
Compound 86
m.p.: 277-280° C.
ESI-MS: found: 339.3 (M+H+); calculated: 338.37 g/mol.
Example 90
Compound 87
m.p.: 256-259° C.
ESI-MS: found: 397.2 (M+H+); calculated: 396.40 g/mol.
Example 91
Compound 88
m.p.: 240-242° C.
ESI-MS: found: 306.5 (M+H+); calculated: 610.68 g/mol.
Example 92
Compound 89
m.p.: 216-219° C.
ESI-MS: found: 339.0 (M+H+); calculated: 338.37 g/mol.
Example 93
Compound 90
m.p.: 298-305° C.
ESI-MS: found: 362.3 (M+H+); calculated: 362.22 g/mol.
Example 94
Compound 91
m.p.: 254-257° C.
ESI-MS: found: 358.1 (M+H+); calculated: 357.80 g/mol.
Example 95
Compound 92
m.p.: 264-269° C.
ESI-MS: found: 362.2 (M+H+); calculated: 362.22 g/mol.
Example 96
Compound 93
m.p.: 253-258° C.
ESI-MS: found: 342.1 (M+H+); calculated: 341.34 g/mol.
Example 97
Compound 94
m.p.: 270-274° C.
ESI-MS: found: 386.2 (M+H+); calculated: 386.25 g/mol.
Example 98
Compound 95
m.p.: 259-262° C.
ESI-MS: found: 330.3 (M+H+); calculated: 329.31 g/mol.
Example 99
Compound 96
m.p.: 258-259° C.
ESI-MS: found: 360.2 (M+H+); calculated: 359.79 g/mol.
Example 100
Compound 97
m.p.: 240-243° C.
ESI-MS: found: 361.9 (M+H+); calculated: 361.33 g/mol.
Example 101
Compound 98
m.p.: 223-225° C.
ESI-MS: found: 338.0 (M+H+); calculated: 337.38 g/mol.
Example 102
Compound 99
m.p.: 275° C.
ESI-MS: found: 346.2 (M+H+); calculated: 345.76 g/mol.
Example 103
Compound 100
m.p.: 232-234° C.
ESI-MS: found: 307.9 (M+H+); calculated: 307.36 g/mol.
Example 104
Compound 101
m.p.: 249-253° C.
ESI-MS: found: 339.1 (M+H+); calculated: 338.33 g/mol.
Example 105
Compound 102
m.p.: 220-222° C.
ESI-MS: found: 337.8 (M+H+); calculated: 337.38 g/mol.
Example 106
Compound 103
m.p.: 226-228° C.
ESI-MS: found: 311.8 (M+H+); calculated: 311.32 g/mol.
Example 107
Compound 104
m.p.: 310° C.
ESI-MS: found: 328.2 (M+H+); calculated: 327.77 g/mol.
Example 108
Compound 105
m.p.: 218-220° C.
ESI-MS: found: 307.9 (M+H+); calculated: 307.36 g/mol.
Example 109
Compound 106
m.p.: 270° C.
ESI-MS: found: 326.0 (M+H+); calculated: 325.35 g/mol.
Example 110
Compound 107
m.p.: 260° C.
ESI-MS: found: 321.9 (M+H+); calculated: 321.38 g/mol.
Example 111
Compound 108
m.p.: >350° C.
ESI-MS: found: 362.2 (M+H+); calculated: 362.22 g/mol.
Example 112
Compound 109
m.p.: 236-238° C.
ESI-MS: found: 494.0, 492.0 (M+H+); calculated: 492.37 g/mol.
Example 113
Compound 110
m.p.: 228-230° C.
ESI-MS: found: 417.9, 416.1 (M+H+); calculated: 416.28 g/mol.
Example 114
Compound 111
m.p.: 262-264° C.
ESI-MS: found: 328.1 (M+H+); calculated: 327.77 g/mol.
Example 115
Compound 112
m.p.: 229-231° C.
ESI-MS: found: 356.1 (M+H+); calculated: 355.37 g/mol.
Example 116
Compound 113
m.p.: 242° C.
ESI-MS: found: 314.2 (M+H+); calculated: 313.39 g/mol.
Example 117
Compound 114
m.p.: 253-257° C.
ESI-MS: found: 318.9 (M+H+); calculated: 318.34 g/mol.
Example 118
Compound 115
m.p.: 200-202° C.
ESI-MS: found: 323.9 (M+H+); calculated: 323.35 g/mol.
Example 119
Compound 116
m.p.: 251-255° C.
ESI-MS: found: 370.3 (M+H+); calculated: 369.43 g/mol.
Example 120
Compound 117
m.p.: 221-224° C.
ESI-MS: found: 340.0 (M+H+); calculated: 339.42 g/mol.
Example 121
Compound 118
m.p.: 239-240° C.
ESI-MS: found: 378.1 (M+H+); calculated: 377.32 g/mol.
Example 122
Compound 119
m.p.: 222-223° C.
ESI-MS: found: 366.0 (M+H+); calculated: 365.39 g/mol.
Example 123
Compound 120
m.p.: 224-228° C.
ESI-MS: found: 387.1 (M+H+); calculated: 386.43 g/mol.
Example 124
Compound 121
m.p.: 212-217° C.
ESI-MS: found: 460.1 (M+H+); calculated: 459.50 g/mol.
Example 125
Compound 122
m.p.: 244-247° C.
ESI-MS: found: 328.0 (M+H+); calculated: 327.77 g/mol.
Example 126
Compound 123
m.p.: 280° C.
ESI-MS: found: 370.2 (M+H+); calculated: 369.43 g/mol.
Example 127
Compound 124
m.p.: 246° C.
ESI-MS: found: 324.0 (M+H+); calculated: 323.42 g/mol.
Example 128
Compound 125
m.p.: 244° C.
ESI-MS: found: 354.2 (M+H+); calculated: 353.45 g/mol.
Example 129
Compound 126
m.p.: 278° C.
ESI-MS: found: 339.1 (M+H+); calculated: 338.44 g/mol.
Example 130
Compound 127
m.p.: 227° C.
ESI-MS: found: 368.0 (M+H+); calculated: 367.47 g/mol.
Example 131
Compound 128
m.p.: 269-273° C.
ESI-MS: found: 461.4 (M+H+); calculated: 460.54 g/mol.
Example 132
Compound 129
m.p.: 283-286° C.
ESI-MS: found: 311.9 (M+H+); calculated: 311.32 g/mol.
Example 133
Compound 130
m.p.: 220-223° C.
ESI-MS: found: 337.8 (M+H+); calculated: 337.38 g/mol.
Example 134
Compound 131
m.p.: >350° C.
ESI-MS: found: 339.1 (M+H+); calculated: 338.33 g/mol.
Example 135
Compound 132
m.p.: 260° C.
ESI-MS: found: 351.9 (M+H+); calculated: 351.36 g/mol.
Example 136
Compound 133
m.p.: 258.7° C.
ESI-MS: found: 351.8 (M+H+); calculated: 351.41 g/mol.
Example 137
Compound 134
m.p.: 230° C.
ESI-MS: found: 400.3 (M+H+); calculated: 399.47 g/mol.
Example 138
Compound 135
m.p.: 182-185° C.
ESI-MS: found: 340.0 (M+H+); calculated: 339.42 g/mol.
Example 139
Compound 136
m.p.: 256-260° C.
ESI-MS: found: 319.1 (M+Fr); calculated: 318.34 g/mol.
Example 140
Compound 137
m.p.: 236-239° C.
ESI-MS: found: 342.0 (M+H+); calculated: 341.34 g/mol.
Example 141
Compound 138
ESI-MS: found: 394.4 (M+H+); calculated: 394.28 g/mol.
Example 142
Compound 139
ESI-MS: found: 390.3 (M+H+); calculated: 389.87 g/mol.
Example 143
Compound 140
ESI-MS: found: 355.3 (M+H+); calculated: 354.44 g/mol.
Example 144
Compound 141
m.p.: 250° C.
ESI-MS: found: 299.9 (M+H+); calculated: 299.36 g/mol.
Example 145
Compound 142
m.p.: 247-249° C.
ESI-MS: found: 321.9 (M+H+); calculated: 321.38 g/mol.
Example 146
Compound 143
m.p.: 250-252° C.
ESI-MS: found: 370.2 (M+H+); calculated: 369.35 g/mol.
Example 147
Compound 144
m.p.: 240-244° C.
ESI-MS: found: 336.9 (M+H+); calculated: 336.40 g/mol.
Example 148
Compound 145
m.p.: 207-209° C.
ESI-MS: found: 353.9 (M+H+); calculated: 353.38 g/mol.
Example 149
Compound 146
m.p.: 202-204° C.
ESI-MS: found: 356.0 (M+H+); calculated: 355.37 g/mol.
Example 150
Compound 147
m.p.: 272° C.
ESI-MS: found: 371.3 (M+H+); calculated: 370.44 g/mol.
Example 151
Compound 148
m.p.: 285° C.
ESI-MS: found: 325.1 (M+H+); calculated: 324.41 g/mol.
Example 152
Compound 149
m.p.: 280° C.
ESI-MS: found: 341.2 (M+H+); calculated: 340.41 g/mol.
Example 153
Compound 150
m.p.: 269° C.
ESI-MS: found: 371.1 (M+H+); calculated: 370.44 g/mol.
Example 154
Compound 151
m.p.: 228-233° C.
ESI-MS: found: 335.7 (M+H+); calculated: 335.41 g/mol.
Example 155
Compound 152
m.p.: 227-228° C.
ESI-MS: found: 300.0 (M+H+); calculated: 299.36 g/mol.
Example 156
Compound 153
m.p.: 225° C.
ESI-MS: found: 339.0 (M+H+); calculated: 338.37 g/mol.
Example 157
Compound 154
m.p.: 238° C.
ESI-MS: found: 339.0 (M+H+); calculated: 338.37 g/mol.
Example 158
Compound 155
m.p.: 230° C.
ESI-MS: found: 401.0 (M+H+); calculated: 400.44 g/mol.
Example 159
Compound 156
m.p.: 281° C.
ESI-MS: found: 355.1 (M+H+); calculated: 354.37 g/mol.
Example 160
Compound 157
m.p.: 265° C.
ESI-MS: found: 385.1 (M+H+); calculated: 384.46 g/mol.
Example 161
Compound 158
ESI-MS: found: 375.1 (M+H+); calculated: 374.85 g/mol.
Example 162
Compound 159
m.p.: 276° C.
ESI-MS: found: 389.1 (M+H+); calculated: 388.88 g/mol.
Example 163
Compound 160
m.p.: 268° C.
ESI-MS: found: 415.1 (M+H+); calculated: 414.49 g/mol.
Example 164
Compound 161
m.p.: 262° C.
ESI-MS: found: 341.1 (M+H+); calculated: 340.41 g/mol.
Example 165
Compound 162
m.p.: 288° C.
ESI-MS: found: 369.1 (M+H+); calculated: 368.46 g/mol.
Example 166
Compound 163
m.p.: 238° C.
ESI-MS: found: 383.1 (M+H+); calculated: 382.49 g/mol.
Example 167
Compound 164
m.p.: 294° C.
ESI-MS: found: 392.2 (M+H+); calculated: 391.46 g/mol.
Example 168
Compound 165
m.p.: 268° C.
ESI-MS: found: 432.2 (M+H+); calculated: 431.54 g/mol.
Example 169
Compound 166
m.p.: 278° C.
ESI-MS: found: 409.4 (M+H+); calculated: 409.30 g/mol.
Example 170
Compound 167
m.p.: 253° C.
ESI-MS: found: 343.0 (M+H+); calculated: 342.79 g/mol.
Example 171
Compound 168
m.p.: 289° C.
ESI-MS: found: 375.4 (M+H+); calculated: 374.47 g/mol.
Example 172
Compound 169
m.p.: 228° C.
ESI-MS: found: 351.8 (M+H+); calculated: 351.41 g/mol.
Example 173
Compound 170
m.p.: 243° C.
ESI-MS: found: 350.9 (M+H+); calculated: 350.38 g/mol.
Example 174
Compound 172
m.p.: 242-244° C.
ESI-MS: found: 326.1 (M+H+); calculated: 325.33 g/mol.
Example 175
Compound 173
m.p.: 215-218° C.
ESI-MS: found: 374.1 (M+H+); calculated: 373.80 g/mol.
Example 176
Compound 176
m.p.: 234-237° C.
ESI-MS: found: 389.2 (M+H+); calculated: 388.39 g/mol.
Example 177
Compound 177
m.p.: 234-237° C.
ESI-MS: found: 351.9 (M+H+); calculated: 351.41 g/mol.
Example 178
Compound 178
m.p.: 227-228° C.
ESI-MS: found: 308.0 (M+H+); calculated: 307.36 g/mol.
Example 179
Compound 179
m.p.: >320° C.
ESI-MS: found: 309.2 (M+H+); calculated: 308.34 g/mol.
Example 180
Compound 180
m.p.: >320° C.
ESI-MS: found: 323.0 (M+H+); calculated: 322.37 g/mol.
Example 181
Compound 181
m.p.: >240° C.
ESI-MS: found: 338.2 (M+H+); calculated: 337.38 g/mol.
Example 182
Compound 182
m.p.: 277-279° C.
ESI-MS: found: 310.2 (M+H+); calculated: 309.33 g/mol.
Example 183
Compound 183
m.p.: >250° C.
ESI-MS: found: 342.8 (M+H+); calculated: 341.39 g/mol.
Example 184
Compound 194
m.p.: 305-308° C.
ESI-MS: found: 367.2 (M+H+); calculated: 366.38 g/mol.
Example 185
Compound 195
m.p.: 248° C.
ESI-MS: found: 383.2 (M+H+); calculated: 382.45 g/mol.
Example 186
Compound 197
m.p.: 211° C.
ESI-MS: found: 341.2 (M+H+); calculated: 340.41 g/mol.
Example 187
Compound 198
m.p.: 258° C.
ESI-MS: found: 341.1 (M+H+); calculated: 340.41 g/mol.
Example 188
Compound 200
m.p.: 238° C.
ESI-MS: found: 415.3 (M+H+); calculated: 414.49 g/mol.
Example 189
Compound 201
m.p.: 260° C.
ESI-MS: found: 373.1 (M+H+); calculated: 372.81 g/mol.
Example 190
Compound 202
m.p.: 225° C.
ESI-MS: found: 389.2 (M+H+); calculated: 388.88 g/mol.
Example 191
Compound 203
m.p.: 166° C.
ESI-MS: found: 371.2 (M+H+); calculated: 370.44 g/mol.
Example 192
Compound 205
m.p.: 166° C.
ESI-MS: found: 371.2 (M+H+); calculated: 370.44 g/mol.
Example 193
Compound 207
m.p.: 236° C.
ESI-MS: found: 432.2 (M+H+); calculated: 431.54 g/mol.
Example 194
Compound 208
m.p.: 203° C.
ESI-MS: found: 375.2 (M+H+); calculated: 374.85 g/mol.
Example 195
Compound 209
m.p.: 255° C.
ESI-MS: found: 353.1 (M+H+); calculated: 352.40 g/mol.
Example 196
Compound 210
m.p.: 148° C.
ESI-MS: found: 369.0 (M+H+); calculated: 368.46 g/mol.
Example 197
Compound 217
m.p.: 185° C.
ESI-MS: found: 359.0 (M+H+); calculated: 358.86 g/mol.
Example 198
Compound 221
m.p.: 189° C.
ESI-MS: found: 355.2 (M+H+); calculated: 354.44 g/mol.
Example 199
Compound 225
m.p.: 243-245° C.
ESI-MS: found: 303.2 (M+H+); calculated: 302.34 g/mol.
Example 200
Compound 227
m.p.: 214-216° C.
ESI-MS: found: 316.3 (M+H+); calculated: 315.34 g/mol.
Example 201
Compound 231
m.p.: 201-203° C.
ESI-MS: found: 287.1 (M+H+); calculated: 286.34 g/mol.
Example 202
Compound 233
m.p.: 199-201° C.
ESI-MS: found: 330.3 (M+H+); calculated: 329.41 g/mol.
Example 203
Compound 235
m.p.: 249-251° C.
ESI-MS: found: 317.2 (M+H+); calculated: 316.36 g/mol.
Example 204
Compound 239
m.p.: 211-213° C.
ESI-MS: found: 323.2 (M+H+); calculated: 322.37 g/mol.
Example 205
Compound 241
ESI-MS: found: 337.2 (M+H+); calculated: 336.40 g/mol.
Example 206
Compound 255
ESI-MS: found: 392.4 (M+H+); calculated: 391.50 g/mol.
Example 207
Compound 257
m.p.: 216° C.
ESI-MS: found: 418.1 (M+H+); calculated: 417.54 g/mol.
Example 208
Compound 329
m.p.: >220° C.
ESI-MS: found: 359.3 (M+H+); calculated: 358.86 g/mol.
Example 209
Compound 331
m.p.: 258° C.
ESI-MS: found: 355.3 (M+H+); calculated: 354.44 g/mol.
Example 210
Compound 332
m.p.: 232° C.
ESI-MS: found: 355.1 (M+H+); calculated: 354.44 g/mol.
Example 211
Compound 336
m.p.: 255° C.
ESI-MS: found: 381.2 (M+H+)-free Base; calculated: 416.91 g/mol.
Example 212
Compound 341
m.p.: 235° C.
ESI-MS: found: 477.4 (M+H+)— free base; calculated: 513.00 g/mol.
Example 213
Compound 374
m.p.: 215° C.
ESI-MS: found: 352.0 (M+H+); calculated: 351.41 g/mol.
Example 214
Compound 378
m.p.: 225° C.
ESI-MS: found: 336.8 (M+H+); calculated: 336.44 g/mol.
Example 215
Compound 380
ESI-MS: found: 339.2 (M+H+); calculated: 338.37 g/mol.
Example 216
Compound 394
m.p.: 272° C.
ESI-MS: found: 339.2 (M+H+); calculated: 338.37 g/mol.
Example 217
Compound 398
m.p.: 210° C.
ESI-MS: found: 336.8 (M+H+); calculated: 336.40 g/mol.
Example 218
Compound 399
m.p.: 215° C.
ESI-MS: found: 353.1 (M+H+); calculated: 352.46 g/mol.
Example 219
Compound 433
m.p.: 265° C.
ESI-MS: found: 361.2 (M+H+); calculated: 360.39 g/mol.
Example 220
Compound 434
m.p.: 324-329° C.
ESI-MS: found 387.1 (M+H+); calculated: 386.80 g/mol.
Example 221
Compound 441
m.p.: 220° C.
ESI-MS: found: 375.3 (M+H+); calculated: 374.85 g/mol.
Example 222
Compound 443
m.p.: 270° C.
ESI-MS: found: 394.1 (M+H+); calculated: 393.30 g/mol.
Example 223
Compound 446
m.p.: 222° C.
ESI-MS: found: 353.0 (M+H+); calculated: 352.40 g/mol.
Example 224
Compound 465
m.p.: 277° C.
ESI-MS: found: 428.3 (M+H+); calculated: 427.75 g/mol.
Example 225
Compound 467
m.p.: 232° C.
ESI-MS: found: 367.1 (M+H+); calculated: 366.45 g/mol.
Example 226
Compound 489
m.p.: 260° C.
ESI-MS: found: 388.2 (M+H+); calculated: 387.40 g/mol.
Example 227
Compound 491
m.p.: 250° C.
ESI-MS: found: 386.4 (M+H+); calculated: 385.41 g/mol.
Example 228
Compound 501
m.p.: 243° C.
ESI-MS: found: 429.2 (M+H+); calculated: 428.51 g/mol.
Example 229
Compound 509
m.p.: 246° C.
ESI-MS: found: 455.1 (M+H+); calculated: 454.55 g/mol.
Example 230
Compound 518
m.p.: 245-238° C.
ESI-MS: found: 370.4 (M+H+); calculated: 369.45 g/mol.
Example 231
Compound 519
m.p.: 233-235° C.
ESI-MS: found: 396.3 (M+H+); calculated: 395.48 g/mol.
Example 232
Compound 521
m.p.: 261-262° C.
ESI-MS: found: 368.2 (M+H+); calculated: 367.43 g/mol.
Example 233
Compound 524
m.p.: 253-254° C.
ESI-MS: found: 410.4 (M+H+); calculated: 409.51 g/mol.
Example 234
Compound 526
m.p.: 279-280° C.
ESI-MS: found: 342.0 (M+H+); calculated: 341.39 g/mol.
Example 235
Compound 529
m.p.: 224-226° C.
ESI-MS: found: 422.3 (M+H+); calculated: 421.84 g/mol.
Example 236
Compound 533
ESI-MS: found: 402.4 (M+H+); calculated: 401.42 g/mol.
Example 237
Compound 541
ESI-MS: found: 456.4 (M+H+); calculated: 455.39 g/mol.
Example 238
Compound 551
m.p.: 265-268° C.
ESI-MS: found: 392.2 (M+H+); calculated: 392.24 g/mol.
Example 239
Compound 552
m.p.: 259-261° C.
ESI-MS: found: 392.2 (M+H+); calculated: 392.24 g/mol.
Example 240
Compound 553
m.p.: 251-253° C.
ESI-MS: found: 406.2 (M+H+); calculated: 406.27 g/mol.
Example 241
Compound 554
m.p.: 226-230° C.
ESI-MS: found: 530.2 (M+H+); calculated: 529.30 g/mol.
Example 242
Compound 555
m.p.: 259-262° C.
ESI-MS: found: 469.3 (M+H+); calculated: 469.33 g/mol.
Example 243
Compound 556
m.p.: 261-263° C.
ESI-MS: found: 460.3 (M+H+); calculated: 460.36 g/mol.
Example 244
Compound 557
m.p.: 247-249° C.
ESI-MS: found: 364.2 (M+H+); calculated: 364.19 g/mol.
Example 245
Compound 558
m.p.: 272-275° C.
ESI-MS: found: 432.2 (M+H+); calculated: 432.31 g/mol.
Example 246
Compound 559
m.p.: 289-291° C.
ESI-MS: found: 444.3 (M+H+); calculated: 444.25 g/mol.
Example 247
Compound 560
m.p.: 253-255° C.
ESI-MS: found: 432.3 (M+H+); calculated: 432.29 g/mol.
Example 248
Compound 561
m.p.: >300° C.
ESI-MS: found: 471.0 (M+H+); calculated: 471.26 g/mol.
Example 249
Compound 562
m.p.: 257-260° C.
ESI-MS: found: 445.1 (M+H+); calculated: 445.26 g/mol.
Example 250
Compound 563
m.p.: 262-264° C.
ESI-MS: found: 418.1 (M+H+); calculated: 418.28 g/mol.
Example 251
Compound 564
m.p.: 280-282° C.
ESI-MS: found: 454.3 (M+H+); calculated: 454.32 g/mol.
Example 252
Compound 565
m.p.: >300° C.
ESI-MS: found: 521.3 (M+H+); calculated: 521.32 g/mol.
Example 253
Compound 566
m.p.: 253-255° C.
ESI-MS: found: 340.1 (M+H+); calculated: 339.35 g/mol.
Example 254
Compound 567
m.p.: 233-236° C.
ESI-MS: found: 368.2 (M+H+); calculated: 367.41 g/mol.
Example 255
Compound 568
m.p.: 230-233° C.
ESI-MS: found: 382.2 (M+H+); calculated: 381.43 g/mol.
Example 256
Compound 569
m.p.: 262-263° C.
ESI-MS: found: 445.3 (M+H+); calculated: 444.49 g/mol.
Example 257
Compound 570
m.p.: 246-248° C.
ESI-MS: found: 368.2 (M+H+); calculated: 367.41 g/mol.
Example 258
Compound 571
m.p.: 262-264° C.
ESI-MS: found: 408.3 (M+H+); calculated: 407.47 g/mol.
Example 259
Compound 572
m.p.: 269-271° C.
ESI-MS: found: 420.4 (M+H+); calculated: 419.41 g/mol.
Example 260
Compound 573
m.p.: 265-267° C.
ESI-MS: found: 421.3 (M+H+); calculated: 420.43 g/mol.
Example 261
Compound 574
m.p.: 188-191° C.
ESI-MS: found: 402.2 (M+H+); calculated: 401.42 g/mol.
Example 262
Compound 575
m.p.: 236-238° C.
ESI-MS: found: 366.1 (M+H+); calculated: 365.39 g/mol.
Example 263
Compound 576
m.p.: 261-264° C.
ESI-MS: found: 394.3 (M+H+); calculated: 393.44 g/mol.
Example 264
Compound 577
m.p.: 254-257° C.
ESI-MS: found: 430.2 (M+H+); calculated: 429.48 g/mol.
Example 265
Compound 578
m.p.: 263-266° C.
ESI-MS: found: 416.2 (M+H+); calculated: 415.48 g/mol.
Example 266
Compound 579
m.p.: 279-283° C.
ESI-MS: found: 497.1 (M+H+); calculated: 496.48 g/mol.
Example 267
Compound 580
m.p.: 248-251° C.
ESI-MS: found: 402.1 (M+H+); calculated: 401.42 g/mol.
Example 268
Compound 581
m.p.: 239-242° C.
ESI-MS: found: 505.0 (M+H+); calculated: 504.47 g/mol.
Example 269
Compound 582
ESI-MS: found: 382.3 (M+H+); calculated: 381.43 g/mol.
Example 270
Compound 583
m.p.: 273-275° C.
ESI-MS: found: 429.2 (M+H+); calculated: 428.49 g/mol.
Example 271
Compound 584
m.p.: 247-250° C.
ESI-MS: found: 392.4 (M+H+); calculated: 391.47 g/mol.
Example 272
Compound 585
ESI-MS: found: 351.9 (M+H+); calculated: 351.41 g/mol.
Example 273
Compound 586
m.p.: 240-241° C.
ESI-MS: found: 351.9 (M+H+); calculated: 351.41 g/mol.
Example 274
Compound 587
m.p.: 210-212° C.
ESI-MS: found: 350.1 (M+H+); calculated: 349.39 g/mol.
Example 275
Compound 588
m.p.: 267-269° C.
ESI-MS: found: 414.2 (M+H+); calculated: 413.48 g/mol.
Example 276
Compound 589
m.p.: 251-253° C.
ESI-MS: found: 489.0 (M+H+); calculated: 488.47 g/mol.
Example 277
Compound 590
m.p.: 242-244° C.
ESI-MS: found: 405.2 (M+H+); calculated: 404.43 g/mol.
Example 278
Compound 591
ESI-MS: found: 324.1 (M+H+); calculated: 323.35 g/mol.
Example 279
Compound 592
ESI-MS: found: 351.9 (M+H+); calculated: 351.41 g/mol.
Example 280
Compound 593
ESI-MS: found: 366.0 (M+H+); calculated: 365.43 g/mol.
Example 281
Compound 594
ESI-MS: found: 404.3 (M+H+); calculated: 403.42 g/mol.
Example 282
Compound 595
m.p.: 271-273° C.
ESI-MS: found: 386.2 (M+H+); calculated: 385.43 g/mol.
Example 283
Compound 596
m.p.: 263° C.
ESI-MS: found: 422.2 (M+H+); calculated: 421.54 g/mol.
Example 284
Compound 597
m.p.: 221° C.
ESI-MS: found: 380.2 (M+H+); calculated: 379.46 g/mol.
Example 285
Compound 598
m.p.: 232° C.
ESI-MS: found: 380.1 (M+H+); calculated: 379.46 g/mol.
Example 286
Compound 599
m.p.: 233° C.
ESI-MS: found: 394.1 (M+H+); calculated: 393.49 g/mol.
Example 287
Compound 600
m.p.: 244-246° C.
ESI-MS: found: 406.3 (M+H+); calculated: 405.39 g/mol.
Example 288
Compound 601
ESI-MS: found: 460.5 (M+H+); calculated: 459.46 g/mol.
Example 289
Compound 602
m.p.: 287-290° C.
ESI-MS: found: 431.2 (M+H+); calculated: 430.47 g/mol.
Example 290
Compound 603
m.p.: 233-236° C.
ESI-MS: found: 428.3 (M+H+); calculated: 427.46 g/mol.
Example 291
Compound 604
m.p.: 232-234° C.
ESI-MS: found: 422.4 (M+H+); calculated: 421.50 g/mol.
Example 292
Compound 605
m.p.: 252-254° C.
ESI-MS: found: 446.4 (M+H+); calculated: 445.52 g/mol.
Example 293
Compound 606
m.p.: 210-212° C.
ESI-MS: found: 529.4 (M+H+); calculated: 528.57 g/mol.
Example 294
Compound 607
m.p.: 260-263° C.
ESI-MS: found: 474.5 (M+H+); calculated: 473.49 g/mol.
Example 295
Compound 608
ESI-MS: found: 408.4 (M+H+); calculated: 407.47 g/mol.
Example 296
Compound 609
m.p.: 257-259° C.
ESI-MS: found: 444.3 (M+H+); calculated: 443.49 g/mol.
Example 297
Compound 610
ESI-MS: found: 491.5 (M+H+); calculated: 490.44 g/mol.
Example 298
Compound 611
m.p.: 245-248° C.
ESI-MS: found: 389.4 (M+H+); calculated: 388.39 g/mol.
Example 299
Compound 612
m.p.: 272-273° C.
ESI-MS: found: 408.4 (M+H+); calculated: 407.47 g/mol.
Example 300
Compound 613
m.p.: 232-236° C.
ESI-MS: found: 424.4 (M+H+); calculated: 423.51 g/mol.
Example 301
Compound 614
m.p.: 216-219° C.
ESI-MS: found: 394.4 (M+H+); calculated: 393.43 g/mol.
Example 302
Compound 615
ESI-MS: found: 471.4 (M+H+); calculated: 470.53 g/mol.
Example 303
Compound 616
m.p.: 247-250° C.
ESI-MS: found: 433.3 (M+H+); calculated: 432.39 g/mol.
Example 304
Compound 617
m.p.: 220-222° C.
ESI-MS: found: 433.4 (M+H+); calculated: 432.39 g/mol.
Example 305
Compound 618
m.p.: 274-276° C.
ESI-MS: found: 433.1 (M+H+); calculated: 432.39 g/mol.
Example 306
Compound 619
m.p.: 214-217° C.
ESI-MS: found: 453.4 (M+H+); calculated: 452.43 g/mol.
Example 307
Compound 620
m.p.: 207-210° C.
ESI-MS: found: 486.3 (M+H+); calculated: 485.55 g/mol.
Example 308
Compound 621
m.p.: 248-251° C.
ESI-MS: found: 441.5 (M+H+); calculated: 440.46 g/mol.
Example 309
Compound 622
m.p.: 290-293° C.
ESI-MS: found: 483.5 (M+H+); calculated: 482.45 g/mol.
Example 310
Compound 623
m.p.: 263-265° C.
ESI-MS: found: 453.4 (M+H+); calculated: 452.47 g/mol.
Example 311
Compound 624
m.p.: 242-245° C.
ESI-MS: found: 432.2 (M+H+); calculated: 431.45 g/mol.
Example 312
Compound 625
m.p.: 235-238° C.
ESI-MS: found: 418.1 (M+H+); calculated: 417.42 g/mol.
Example 313
Compound 626
m.p.: 259-261° C.
ESI-MS: found: 413.3 (M+H+); calculated: 412.41 g/mol.
Example 314
Compound 627
m.p.: 234-235° C.
ESI-MS: found: 396.4 (M+H+); calculated: 395.46 g/mol.
Example 315
Compound 628
m.p.: 233-235° C.
ESI-MS: found: 478.4 (M+H+); calculated: 477.61 g/mol.
Example 316
Compound 629
m.p.: 233-236° C.
ESI-MS: found: 430.3 (M+H+); calculated: 429.48 g/mol.
Example 317
Compound 630
m.p.: 208-210° C.
ESI-MS: found: 444.4 (M+H+); calculated: 443.50 g/mol.
Example 318
Compound 631
m.p.: 223-226° C.
ESI-MS: found: 368.2 (M+H+); calculated: 367.41 g/mol.
Example 319
Compound 632
m.p.: 214-216° C.
ESI-MS: found: 368.2 (M+H+); calculated: 367.41 g/mol.
Example 320
Compound 633
ESI-MS: found: 464.4 (M+H+); calculated: 463.49 g/mol.
Example 321
Compound 634
ESI-MS: found: 470.1 (M+H+); calculated: 469.42 g/mol.
Example 322
Compound 635
m.p.: 226-228° C.
ESI-MS: found: 444.1 (M+H+); calculated: 443.50 g/mol.
Example 323
Compound 636
ESI-MS: found: 436.1 (M+H+); calculated: 435.87 g/mol.
Example 324
Compound 637
m.p.: >270° C.
ESI-MS: found: 344.6 (M+H+); calculated: 343.77 g/mol.
Example 325
Compound 638
ESI-MS: found: 340.1 (M+H+); calculated: 339.35 g/mol.
Example 326
Compound 639
m.p.: 250-252° C.
ESI-MS: found: 416.9 (M+H+); calculated: 416.77 g/mol.
Example 327
Compound 640
m.p.: 262° C.
ESI-MS: found: 396.2 (M+H+); calculated: 395.31 g/mol.
Example 328
Compound 641
m.p.: 291° C.
ESI-MS: found: 388.2 (M+H+); calculated: 388.22 g/mol.
Example 329
Compound 642
m.p.: 266° C.
ESI-MS: found: 358.2 (M+H+); calculated: 357.80 g/mol.
Example 330
Compound 643
m.p.: 263° C.
ESI-MS: found: 422.2 (M+H+); calculated: 421.54 g/mol.
Example 331
Compound 644
m.p.: 225° C.
ESI-MS: found: 354.1 (M+H+); calculated: 353.34 g/mol.
Example 332
Compound 647
ESI-MS: found: 310.2 (M+H+); calculated: 309.40 g/mol.
Example 333
Compound 648
ESI-MS: found: 355.3 (M+H+); calculated: 354.44 g/mol.
Example 334
Compound 649
ESI-MS: found: 368.1 (M+H+); calculated: 367.47 g/mol.
Example 335
Compound 650
m.p.: 218-219° C.
ESI-MS: found: 400.2 (M+H+); calculated: 399.47 g/mol.
Example 336
Compound 651
m.p.: 230-231° C.
ESI-MS: found: 324.1 (M+H+); calculated: 323.42 g/mol.
Example 337
Compound 652
m.p.: 213-215° C.
ESI-MS: found: 384.3 (M+H+); calculated: 383.47 g/mol.
Example 338
Compound 653
m.p.: 250-251° C.
ESI-MS: found: 438.4 (M+H+); calculated: 437.57 g/mol.
Example 339
Compound 654
m.p.: 238-240° C.
ESI-MS: found: 462.4 (M+H+); calculated: 461.59 g/mol.
Example 340
Compound 655
ESI-MS: found: 354.0 (M+H+); calculated: 353.38 g/mol.
Example 341
Compound 660
m.p.: 168-170° C.
ESI-MS: found: 387.1 (M+H+); calculated: 386.41 g/mol.
Example 342
Compound 661
ESI-MS: found: 393.3 (M+H+); calculated: 392.46 g/mol.
Example 343
Compound 686
ESI-MS: found: 368.1 (M+H+); calculated: 367.41 g/mol.
Example 344
Compound 690
m.p.: 248° C.
ESI-MS: found: 469.2 (M+H+); calculated: 468.58 g/mol.
Example 345
Compound 691
m.p.: 250° C.
ESI-MS: found: 497.3 (M+H+); calculated: 496.63 g/mol.
Example 346
Compound 692
m.p.: 258-261° C.
ESI-MS: found: 401.1 (M+H+); calculated: 400.46 g/mol.
Example 347
Compound 693
m.p.: 230-234° C.
ESI-MS: found: 427.3 (M+H+); calculated: 426.50 g/mol.
Example 348
Compound 694
m.p.: 218-220° C.
ESI-MS: found: 443.2 (M+H+); calculated: 442.54 g/mol.
Example 349
Compound 695
m.p.: 247° C.
ESI-MS: found: 482.3 (M+H+); calculated: 481.53 g/mol.
Example 350
Compound 696
m.p.: 347° C.
ESI-MS: found: 483.1 (M+H+); calculated: 482.61 g/mol.
Example 351
Compound 697
m.p.: 250-252° C.
ESI-MS: found: 477.0 (M+H+); calculated: 476.56 g/mol.
Example 352
Compound 698
m.p.: 248-250° C.
ESI-MS: found: 491.1 (M+H+); calculated: 490.59 g/mol.
Example 353
Compound 699
m.p.: 197-200° C.
ESI-MS: found: 491.3 (M+H+); calculated: 490.59 g/mol.
Example 354
Compound 700
m.p.: 206° C.
ESI-MS: found: 498.1 (M+H+); calculated: 497.62 g/mol.
Example 355
Compound 701
m.p.: 255° C.
ESI-MS: found: 495.1 (M+H+); calculated: 494.55 g/mol.
Example 356
Compound 702
m.p.: 210° C.
ESI-MS: found: 457.4 (M+H+); calculated: 456.57 g/mol.
Example 357
Compound 703
m.p.: 196° C.
ESI-MS: found: 500.2 (M+H+); calculated: 499.59 g/mol.
Example 358
Compound 704
m.p.: 195-198° C.
ESI-MS: found: 505.3 (M+H+); calculated: 504.61 g/mol.
Example 359
Compound 705
m.p.: 243-245° C.
ESI-MS: found: 445.4 (M+H+); calculated: 444.51 g/mol.
Example 359
Compound 706
m.p.: 222° C.
ESI-MS: found: 428.9 (M+H+); calculated: 428.51 g/mol.
Example 360
Compound 707
m.p.: 248° C.
ESI-MS: found: 427.3 (M+H+); calculated: 426.50 g/mol.
Example 361
Compound 708
m.p.: 228° C.
ESI-MS: found: 467.3 (M+H+); calculated: 466.52 g/mol.
Example 362
Compound 709
m.p.: 244° C.
ESI-MS: found: 487.2 (M+H+); calculated: 486.55 g/mol.
Example 363
Compound 710
m.p.: 246° C.
ESI-MS: found: 459.4 (M+H+); calculated: 458.54 g/mol.
Example 364
Compound 711
m.p.: 248° C.
ESI-MS: found: 491.4 (M+H+); calculated: 490.59 g/mol.
Example 365
Compound 733
m.p.: 110° C.
ESI-MS: found: 356.0 (M+H+); calculated: 355.40 g/mol.
II) Biological Effects of the Compounds of the Invention
II.1) Cell-Free Kinase Assays (by Means of Alpha Technology)
The inhibitory effect of the compounds of the invention was tested on various human serine/threonine kinases, tyrosine kinases and lipid kinases in enzymatic assays. Recombinant human kinases, for example PI3Kalpha, -beta, -gamma, -delta, Erk2, p38alpha, p38gamma, Jnk1, Jnk2 and others were used, in some cases as full-length kinases, in some cases as truncated fragments—but at least consisting of the functional kinase domains. The commercial kinase proteins (Proqinase, Upstate) were used as recombinant fusion proteins with GST (glutathione S-transferase) tag or His tag. Depending on the substrate type, the different kinase reactions were quantified by suitable ALPHATM beads (PerkinElmer).
Testing
The kinase assays for PI3K and Erk are described in detail and selected test results are cited below. To determine the IC50 value, the potential inhibitor substances were investigated at 10 half-logarithmically graduated concentrations of 3.16 nM-100 μM.

    
    
        a) PI3K-ALPHA (e.g. PI3Kalpha): The test substance, 1 ng of PI3Kalpha (#14-602, Upstate), 100 μM ATP and 20 μM PIP2 substrate (#P4508, Echelon) were incubated on a 384-well Optiplate (Perkin Elmer) for 60 minutes in 50 mM Hepes, 50 mM NaCl, 5 mM MgCl2, 0.05% Chaps, 5 mM DTT at pH 7.4. Subsequently, the kinase reaction was stopped by adding the ALPHA bead mix (10 μg/ml, #6760603/PerkinElmer), preincubated with 1 nM GST:Grp1 fusion protein (Upstate) and 15 nM biotinylated PIP3 (#C-39B6/Echelon) in 50 mM Hepes, 50 mM NaCl, 50 mM EDTA and 0.1% BSA, and left to stand overnight.
        b) Erk2-ALPHA: The test substance, 0.625 ng of Erk2 (#14-173, Upstate), 10 μM ATP and 15 nM biotinylated MBP (myelin basic protein) substrate were incubated on a 384-well Optiplate (Perkin Elmer) in a volume of 15 μl for 1 h in 25 mM Tris, 10 mM MgCl2, 0.1% Tween-20, 100 μM NaVO4, 2 mM DTT at pH 7.5. The kinase reaction was stopped by adding 10 μl of the ALPHA bead mix (10 μg/ml, #6760617/PerkinElmer), pre-incubated with anti-phospho MBP antibody (320 μM, #05-429/Up-state), in 25 mM Tris, 200 mM NaCl, 100 mM EDTA and 0.3% BSA, and left to stand overnight.
    
    


The luminiscence was detected the next morning in a FusionTMalpha instrument (Perkin Elmer).
Evaluation
The calculation of % inhibition values per substance concentration was done by means of the following formula from the raw data determined in the FusionTMalpha:




  
    %
    ⁢
    
      
    
    ⁢
    kinase
    ⁢
    
      
    
    ⁢
    
      inhibition
      
        (
        sample
        )
      
    
  
  =
  
    100
    -
    
      (
      
        100
        ×
        
          
            
              mean
              
                (
                sample
                )
              
            
            -
            
              mean
              
                (
                
                  0
                  ⁢
                  %
                  ⁢
                  
                    
                  
                  ⁢
                  control
                
                )
              
            
          
          
            
              mean
              
                (
                
                  100
                  ⁢
                  %
                  ⁢
                  
                    
                  
                  ⁢
                  control
                
                )
              
            
            -
            
              mean
              
                (
                
                  0
                  ⁢
                  %
                  ⁢
                  
                    
                  
                  ⁢
                  control
                
                )
              
            
          
        
      
      )
    
  




The controls were determined 8 fold and the substance samples 2 fold. 0% control contained neither any ATP nor any substrate. The 100% control contained no test substance. The IC50 values were determined with GraphPadPrism.
The compounds of the invention exhibited effective inhibition of PI3Kalpha, Erk2, p38alpha and Jnk1+Jnk2 with IC50 values of <500 nM (see Table 1).







TABLE 1







PI3Kalpha and MAPK kinase assay test results (IC50 [μM]


at 10 μM or 100 μM* ATP)











Compound
PI3Kalpha*
Erk2
p38alpha
Jnk1 + Jnk2














5
<0.5
>100
>100
>10


20
<1
>100
>100
>100


30
<1
<10
<10
<31.6


46
<5
<0.5
>100
<1


50
<1
>100
>100
>100


54
<5
<0.5
>100
<31.6


55
<5
>100
<10
>100


56
<5
<10
<10
>10


73
<5
>100
>10
>100


147
<1
>100
>100
>31.6


160
<1
<31.6
<50
>100


173
<1
<50
<50
<31.6


176
<1
>31.6
<50
<50


181
<5
>100
<50
>100


509
<1
>100
>100
>100


526
<1
>100
<50
>100


553
<5
>100
>100
<100


563
<1
>100
—
—


566
<5
>100
>31.6
>100


614
<1
<31.6
<10
<31.6


637
<5
>100
>100
>100









Especially compound 5 and derivatives are characterized by low IC50 values against PI3K and high selectivity against the other kinases.
Also pyridopyrazines, substituted by —NH-heteroaryl at the pyrazine ring (for example, compounds 50, 55, 56 and 73), show PI3K inhibition, but no or only moderate MAPK inhibition.
Pyridopyrazines, substituted by heteroaryl at the pyrazine ring (for example, compounds 46 and 54) exhibit a dual mode of kinase inhibition at least, namely an inhibition of PI3K and Erk2.
II.2) Cellular Assay: Testing for Anti-Proliferate Activity (XTT Assay)
The principle of this test is based on the intracellular reduction of the tetrazolium dye XTT (sodium 3′-[1-(phenylaminocarbonyl)-3,4-tetrazolium]bis(4-methoxy-6-nitro)benzenesulphonic acid, Sigma) to a formazan dye by mitochondrial dehydrogenases. The dye is formed only by metabolically active cells. Its photometrically measurable intensity is a quantitative indicator for the presence of living cells. The reduction in the dye formation as a result of incubation of the cells with substances serves as a parameter for the anti-proliferative activity.
Testing
The tumour cell lines (ATCC) were seeded in 96-well microtitre plates in a defined cell count (5000 cells/well for Hct116; 10000 cells/well for MDA MB468), and incubated overnight at 37° C., 5% CO2 and 95% air humidity. The test substances were made up as stock solutions (10 mM) in DMSO. To determine the EC50 values, the potential inhibitor substances were added to the cells in quarter-logarithmically graded dilutions, so as to result in final concentrations of 0.28 μM-50 μM. The cell plates were then incubated for 45 h at 37° C., 5% CO2 and 95% air humidity.
For the detection reaction, the XTT substrate was mixed with PMS (N-methyldibenzopyrazine methylsulphate, Sigma) and added to the cells, to result in a final concentration of 325 μg of XTT/ml and 2.5 μg PMS/ml. The mixture was then incubated for 3 h at 37° C., 95% air humidity. Subsequently the formazan salt formed by cellular dehydrogenases was quantified at an absorption of 490 nm.
Evaluation
The evaluation of the % inhibition values was done by means of the following formula from the values for the optical densities measured in each case at 490 nm:




  
    %
    ⁢
    
      
    
    ⁢
    inhibition
    ⁢
    
      
    
    ⁢
    of
    ⁢
    
      
    
    ⁢
    cell
    ⁢
    
      
    
    ⁢
    
      proliferation
      
        (
        sample
        )
      
    
  
  =
  
    100
    -
    
      (
      
        100
        ×
        
          
            
              mean
              
                (
                sample
                )
              
            
            -
            
              mean
              
                (
                
                  0
                  ⁢
                  %
                  ⁢
                  
                    
                  
                  ⁢
                  control
                
                )
              
            
          
          
            
              mean
              
                (
                
                  100
                  ⁢
                  %
                  ⁢
                  
                    
                  
                  ⁢
                  control
                
                )
              
            
            -
            
              mean
              
                (
                
                  0
                  ⁢
                  %
                  ⁢
                  
                    
                  
                  ⁢
                  control
                
                )
              
            
          
        
      
      )
    
  




The controls were determined 8 fold, the substance samples 2 fold. 0% control contained no cells and the 100% control contained no test substance. The EC50 values were determined with GraphPadPrism.
The compounds of the invention exhibited effective inhibition of cell proliferation in some cases with EC50 values<1 μM (see Table 2).







TABLE 2







XTT assay test results (EC50 [μM])









Compound
MDA-MB468
Hct116












5
<1
<2


46
<10
<10


50
<10
<5


54
<5
<5


55
<5
<5


56
<5
<10


73
<5
<5


89
<5
<5


113
<5
<5


126
<5
<5


134
<5
<5


138
<10
<10


140
<5
<5


147
<5
<5


148
<5
<10


150
<5
<5


152
<10
<10


160
<1
<1


173
<1
<1


176
<1
<1


181
<10
<10


509
<5
<5


526
<1
<5


553
<5
<5


563
<1
<1


566
<5
<5


614
<5
<5


637
<10
<10









Especially compound 5 and derivatives display high anti-proliferative potencies against human tumor cell lines, as they show EC50 values in the nanomolar range
II.3) Cellular Assay: Testing of Substrate Inhibition (Western Blotting)
This method enables a statement of whether the kinase modulator investigated achieves the desired effect in a cellular context too, i.e., in this case, a substrate protein downstream of the target kinase is examined for its phosphorylation status. To this end, the cells incubated with substance are lysed and the overall protein is separated on a reducing polyacrylamide gel. Subsequently, the proteins are transferred to a PVDF membrane by Western blotting and the substrate bands sought are made visible with specific antibodies and a suitable detection method. The substrate proteins down-stream of the target kinases are detected simultaneously with an anti-phospho antibody which is specific in each case and a total antibody which recognizes the substrate total protein. The duplex technology of the ODYSSEY imager (LiCOR) enables this simultaneous measurement. The intensity of the total substrate bands is employed to normalize and quantify the phosphorylation inhibition or activation.
Testing
Suitable tumor cell lines (e.g. BxPC3, Hct116 or MDA MB468) were seeded into 6-well microtitre plates in a defined cell count (e.g. 350 000 cells/well for BxPC3 and Hct116) in the particular standard complete media and then incubated overnight at 37° C., 5% CO2 and 95% air humidity. Afterwards, the cells were incubated for 24 h under serum-reduced conditions, i.e. in the particular medium except at only 0.25% serum. The test substances were made up as stock solutions (10 mM) in DMSO and incubated with the cells at final concentrations of 5, 15.8 and 50 μM for 5 h. This was followed by cell lysis in 25 mM Tris, 150 mM NaCl, 10 mM sodium pyrophosphate, 2 mM EGTA, 25 mM beta-glycerophosphate, 25 mM NaF, 10% glycerol, 0.75% NP-40, 100 μM NaVO4 buffer. After protein quantification using the BCA (bicinchonic acid protein assay kit, Sigma) assay, amounts of protein of about 20 μg per track were separated on a Lämmli polyacrylamide gel and then transferred onto a PVDF membrane (Millipore) by semi-dry Western blotting at 0.8 mA/cm2 for 1 h. This was followed by prehybridization of the membrane for 1 hour in I-block reagent (Applied Biosystems) and overnight simultaneous incubation with the specific antibodies. To determine the Erk and PI3K inhibition, the next substrates Rsk1 downstream were detected with the total antibody (Rsk #sc-231g C-21, Santa Cruz) and the phospho antibody (Phospho-p90RSK (S380) #9341, NEB Cell Signalling) and Akt with the total antibody (Akt1 #sc-1618 C-20, Santa Cruz) and the phospho antibody (Phospho-Akt (Ser 473) #9271, NEB Cell Signaling). After the membrane had been washed, the secondary antibodies were incubated with anti-rabbit IR Dye 800 (#611-732-127, Rockland) for the phospho antibodies and anti-goat Alexa Fluor 680 (#A-21081, Molecular samples) for the total protein antibodies. After incubation for 30 min at room temperature in the dark, the hybridization of the detection antibody was detected on the membrane by scanning in an ODYSSEY imager (LiCOR).
Evaluation
At concentrations of 5-50 μM, the compounds of the invention exhibited selective inhibition of PI3K or dual inhibition of Erk (MAPK1/2) and of PI3K (see Table 3), which is indicated by inhibition of the phospho-band intensity of the downstream substrates Rsk1 and Akt.







TABLE 3







Inhibition of cellular substrate phosphorylation (at 50 μM)









Compound
PI3K →pAkt
Erk →pRsk












5
100%
0%


46
 40%
100% 


50
100%
0%


54
100%
90% 


55
 90%
0%


56
100%
0%









Especially, pyridopyrazines such as compound 5 show total inhibition of cellular phospho-Akt at compound concentrations<50 μM. The Raf-Mek-Erk pathway is not affected by these derivatives, as phospho-Rsk is not inhibited.
Also, pyridopyrazines, substituted by —NH-heteroaryl at the pyrazine ring (for example, compounds 50, 55 and 56), exhibit cellular PI3K selectivity, as they do not block the Raf-Mek-Erk pathway or show inhibition of phospho-Rsk respectively.
Pyridopyrazines, substituted by heteroaryl at the pyrazine ring (for example, compounds 46 and 54) exhibit a dual mode of kinase inhibition, as they inhibit both, the PI3K-Akt and the Raf-Mek-Erk-Rsk pathways.
ABBREVIATIONS


    Akt from: murine Akt8 retrovirus or protein kinase B (PKB)
    Ask1 apoptosis signal-regulating kinase
    ATR ataxia-telangiectasia and Rad3-related
    ATM ataxia-telangiectasia mutated
    Bag1 Bcl-2 associated athanogene-1
    Bcl-2 B-cell leukaemia/lymhoma-2 gene
    DNA-PK DNA-dependent protein kinase
    Erk extracellular signal-regulated kinase
    Flt-3 fms like tyrosine kinase 3
    GSK-3 glycogen synthase kinase-3
    hSMG-1 human orthologue of product of seven nematode gene-1
    JAK-3 Janus kinase 3
    JNK c-jun N-terminal kinase
    MAPK mitogen activated protein kinase
    Mek MAP or Erk kinase
    mTOR mammalian target of rapamycin
    PDGFR platelet derived growth factor receptor
    PI3K phosphoinositol 3-kinase
    PIKK phosphoinositol 3-kinase related kinase
    PIP2 phosphatidylinositol biphosphate
    PIP3 phosphatidylinositol triphosphate
    PtdIns phosphatidylinositol
    Raf rapid accelerated fibrosarcoma
    Ras rat sarcoma
    RTK receptor tyrosine kinase
    SAPK stress-activated protein kinase
    Ser serine
    Syk spleen tyrosine kinase
    Thr threonine
    Tyr tyrosine
    VEGFR vascular endothelial growth factor receptor

## Claims

1. A compound 1-ethyl-3-(3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-yl)thiourea.

2. A pharmaceutical composition comprising 1-ethyl-3-(3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-yl)thiourea and a pharmaceutically acceptable carrier and/or pharmaceutically acceptable auxiliary.

3. The pharmaceutical composition according to claim 2, wherein 1-ethyl-3-(3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-yl)thiourea is present in a unit dose of from 0.001 mg to 100 mg per kg of body weight of a patient.