Abstract:
The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I):  
                         
 
     that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G.  
     This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

Description:
CROSS REFERENCE TO RELATED APPLICATIONS  
       [0001]    This application is a continuation-in-part application of U.S. Ser. No. 09/692,023, Filed Oct. 19, 2000, entitled “ACYLSEMICARBAZIDES AND THEIR USES”, which is a non-provisional filing of provisional application 60/160,713, filed Oct. 20, 1999, entitled “ACYLSEMICARBAZIDES AS CYCLIN DEPENDENT KINASE INHIBITORS USEFUL AS ANTI-CANCER AND ANTI-PROLIFERATIVE AGENTS” which applications are herein incorporated by reference in their entirity as though set forth in full. 
     
    
     
       FIELD OF THE INVENTION  
         [0002]    This invention relates generally to novel 5-substituted-indeno[1,2-c]pyrazol-4-ones which are useful as cyclin dependent kinase (cdk) inhibitors, pharmaceutical compositions comprising the same, methods for using the same for treating proliferative diseases, and intermediates and processes for making the same.  
         BACKGROUND OF THE INVENTION  
         [0003]    One of the most important and fundamental processes in biology is the division of cells mediated by the cell cycle. This process ensures the controlled production of subsequent generations of cells with defined biological function. It is a highly regulated phenomenon and responds to a diverse set of cellular signals both within the cell and from external sources. A complex network of tumor promoting and suppressing gene products are key components of this cellular signaling process. Over expression of the tumor promoting components or the subsequent loss of the tumor suppressing products will lead to unregulated cellular proliferation and the generation of tumors (Pardee, Science 246:603-608, 1989).  
           [0004]    Cyclin dependent kinases (cdks) play a key role in regulating the cell cycle machinery. These complexes consist of two components: a catalytic subunit (the kinase) and a regulatory subunit (the cyclin). To date, six kinase subunits (cdk 1-7) have been identified along with several regulatory subunits (cyclins A-H). Each kinase associates with a specific regulatory partner and together make up the active catalytic moiety. Each transition of the cell cycle is regulated by a particular cdk complex: G1/S by cdk2/cyclin E, cdk4/cyclin D1 and cdk6/cyclinD2; S/G2 by cdk2/cyclin A and cdk1/cyclin A; G2/M by cdk1/B. The coordinated activity of these kinases guides the individual cells through the replication process and ensures the vitality of each subsequent generation (Sherr, Cell 73:1059-1065, 1993; Draetta, Trends Biochem. Sci. 15:378-382, 1990)  
           [0005]    An increasing body of evidence has shown a link between tumor development and cdk related malfunctions. Over expression of the cyclin regulatory proteins and subsequent kinase hyperactivity have been linked to several types of cancers (Jiang, Proc. Natl. Acad. Sci. USA 90:9026-9030, 1993; Wang, Nature 343:555-557, 1990). More recently, endogenous, highly specific protein inhibitors of cdks were found to have a major affect on cellular proliferation (Kamb et al, Science 264:436-440, 1994; Beach, Nature 336:701-704, 1993). These inhibitors include p16 INK4  (an inhibitor of cdk4/D1), p21 CIP1  (a general cdk inhibitor), and p27 KIP1  (a specific cdk2/E inhibitor). A recent crystal structure of p27 bound to cdk2/A revealed how these proteins effectively inhibit the kinase activity through multiple interactions with the cdk complex (Pavletich, Nature 382:325-331, 1996). These proteins help to regulate the cell cycle through specific interactions with their corresponding cdk complexes. Cells deficient in these inhibitors are prone to unregulated growth and tumor formation.  
           [0006]    This body of evidence has led to an intense search for small molecule inhibitors of the cdk family as an approach to cancer chemotherapy.  
           [0007]    A series of indeno[1,2-c]pyrazoles having anticancer activity are described in JP 60130521 and JP 62099361 with the following generic structure:  
                         
 
           [0008]    A series of indeno[1,2-c]pyrazoles having herbicidal activity are described in GB 2223946 with the following generic structure:  
                         
 
           [0009]    A series of 1-(6′-substituted-4′-methylquinol-2′-yl)-3-methylindeno[1,2-c]pyrazoles having CNS activity are described by Quraishi, Farmaco 44:753-8, 1989 with the following generic structure:  
                         
 
           [0010]    There is a continuing unmet need for cdk inhibitors with which to treat proliferative diseases.  
         SUMMARY OF THE INVENTION  
         [0011]    The present invention describes a novel class of indeno[1,2-c]pyrazol-4-ones or pharmaceutically acceptable salt forms thereof that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk 1-7 and their regulatory subunits know as cyclins A-H.  
           [0012]    The present invention is also directed to a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof.  
           [0013]    A novel method of treating cancer or other proliferative diseases, which comprises administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents is also described herein.  
           [0014]    The present invention also describes compounds of formula (I):  
                         
 
           [0015]    wherein R 1 , R 2  and X are defined below or pharmaceutically acceptable salts thereof as cyclin dependent kinase inhibitors.  
         DETAILED DESCRIPTION OF PREFERRED EMBODIMENTS  
         [0016]    The invention pertains to novel cyclin dependent kinase inhibitors (cdks) and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. The inhibitors of this invention are indeno[1,2-c]pyrazol-4-one analogs. Certain analogs were selective for their activity against cdks and their cyclin bound complexes and were less active against other known serine/threonine kinases such as Protein Kinase A (PKA) and Protein Kinase C (PKC). In addition, these inhibitors were less active against tyrosine kinases such as c-Abl.  
           [0017]    As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently would be useful in modulating cell-cycle progression, which would ultimately control cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation, such as the treatment of cancer, psoriasis, immunological disorders involving unwanted leukocyte proliferation, in the treatment of restinosis and other smooth muscle cell disorders, and the like.  
           [0018]    The present invention, in a first embodiment, describes a novel compound of formula (I):  
                         
 
           [0019]    or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein:  
           [0020]    X is selected from the group: O, S, and NR;  
           [0021]    R is selected from the group: H, C 1-4  alkyl, and NR 5 R 5a ;  
           [0022]    R 1  is selected from the group: H. C 1-10  alkyl substituted with 0-3 R c , C 2-10  alkenyl substituted with 0-3 R c , C 2-10  alkynyl substituted with 0-3 R c , C 1-10  alkoxy, -NHR 4 , C 3-10  carbocycle substituted with 0-5 R a , and 3-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S and substituted with 0-5 R b ;  
           [0023]    R 2  is selected from the group: H, C 1-10  alkyl substituted with 0-3 R c , C 2-10  alkenyl substituted with 0-3 R c , C 2-10  alkynyl substituted with 0-3 R c , —(CF 2 ) m CF 3 , C 3-10  carbocycle substituted with 0-5 R a , and 3-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S and substituted with 0-5 R b ;  
           [0024]    R 3  is selected from the group: H, halo, —CN, NO 2 , C 1-4  haloalkyl, NR 5 R 5a , NR 5 NR 5 R 5a , NR 5 C(O)OR 5 , NR 5 C(O)R 5 , ═O, OR 5 , COR 5 , CO 2 R 5 , CONR 5 R 5a , NHC(O)NR 5 R 5a , NHC(S)NR 5 R 5a , SO 2 NR 5 R 5a , SO 2 R 5b , C 1-4  alkyl, phenyl, benzyl, C 1-4  alkyl substituted with 1-3 R c , C 5-10  alkyl substituted with C 2-10  alkenyl optionally substituted with 0-3 R 6 , C 2-10  alkynyl substituted with 0-3 R 6 , —(CF 2 ) m CF 3 , C 3-10  carbocycle substituted with 0-5 R 6 , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S, substituted with 0-3 R 6 ; and  
           [0025]    provided that if R 3  is phenyl, it is substituted with 1-5 R a ;  
           [0026]    R 4  is independently at each occurrence selected from the group: H, —CN, C 1-4  alkyl, C 1-4  haloalkyl, NR 3 R 3a , NR 3 C(O)OR 3 , NR 3 C(O)R 3 , OR 3 , COR 3 , CO 2 R 3 , CONR 3 R 3a , NHC(O)NR 3 R 3a , NHC(S)NR 3 R 3a , SO 2 NR 3 R 3a , SO 2 R 3b , C 3-10  carbocycle substituted with 0-5 R a , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S, substituted with 0-3 R 3 ;  
           [0027]    provided that at least one R 3  is present and that this R 3  is selected from the group: C 1-4  alkyl substituted with 1-3 R 6 , C 5-10  alkyl substituted with C 2-10  alkenyl optionally substituted with 0-3 R 6 , C 2-10  alkynyl substituted with 0-3 R 6 , —(CF 2 ) m CF 3 , C 3-10  carbocycle substituted with 0-5 R 6 , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S, substituted with 0-3 R 6 ;  
           [0028]    R a  is independently at each occurrence selected from the group: halo, —CN , N 3 , NO 2 , C 1-4  alkyl, C 1-4  haloalkyl, NR 3 R 3a , ═O, OR 3 , COR 3 , CO 2 R 3 , CONR 3 R 3a , NHC(O)NR 3 R 3a , NHC(S)NR 3 R 3a , NR 3 C(O)OR 3 , NR 3 C(O)R 3 , SO 2 NR 3 R 3a , SO 2 R 3b , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S;  
           [0029]    alternatively, when two R 2 , are present on adjacent carbon atoms they combine to form —OCH 2 O— or —OCH 2 CH 2 O—;  
           [0030]    R b  is independently at each occurrence selected from the group: halo, —CN, NO 2 , C 1-4  alkyl, C 1-4  haloalkyl, NR 3 R 3a , NR 3 C(O)OR 3 , NR 3 C(O)R 3 , OR 3 , COR 3 , CO 2 R 3 , CONR 3 R 3a , NHC(O)NR 3 R 3a , NHC(S)NR 3 R 3a , SO 2 NR 3 R 3a , and SO 2 R 3b ;  
           [0031]    R c  is independently at each occurrence selected from the group: halo, —CN, NO 2 , C 1-4  alkyl, C 1-4  haloalkyl, NR 3 R 3a , NR 5 NR 5 R 5a , NR 3 C(O)OR 3 , NR 3 C(O)R 3 , ═O, OR 3 , COR 3 , CO 2 R 3 , CONR 3 R 3a , NHC(O)NR 3 R 3a , NHC(S)NR 3 R 3a , SO 2 NR 3 R 3a , SO 2 R 3b , C 3-10  carbocycle substituted with 0-5 R a , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S, substituted with 0-3 R 3 ;  
           [0032]    R 3a  is selected from the group: H, C 1-4  alkyl, phenyl, and benzyl;  
           [0033]    alternatively, R 3  and R 3a , together with the nitrogen atom to which they are attached, form a heterocycle having 4-8 atoms in the ring containing an additional 0-1 N, S, or O atom and substituted with 0-3 R 3c ;  
           [0034]    R 3b  is selected from the group: H, C 1-4  alkyl, phenyl, and benzyl;  
           [0035]    R 3c  is independently at each occurrence selected from the group: halo, —CN , N 3 , NO 2 , C 1-4  alkyl, C 1-4  haloalkyl, NR 3 R 3b , ═O, OR 3 , COR 3 , CO 2 R 3 , CONR 3 R 3     b   , NHC(O)NR 3 R 3     b   , NHC(S)NR 3 R 3     b   , NR 3 C(O)OR 3 , NR 3 C(O)R 3 , SO 2 NR 3 R 3     b   , SO 2 R 3b , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S;  
           [0036]    R 5  is independently selected from the group: H, C 1-4  alkyl, phenyl and benzyl;  
           [0037]    R 5a  is independently selected from the group: H, C 1-4  alkyl, phenyl and benzyl;  
           [0038]    R 5b  is independently selected from the group: H, C 1-4  alkyl, phenyl and benzyl;  
           [0039]    R 6  is independently at each occurrence selected from the group: halo, —CN, NO 2 , C 1-4  alkyl, C 1-4  haloalkyl, NR 5 R 5 , NR 5 NR 5 R 5a , NR 5 C(O)OR 5 , NR 5 C(O)R 5 , ═O, OR 5 , COR 5 , CO 2 R 5 , CONR 5 R 5a , NHC(O)NR 5 R 5a , NHC(S)NR 5 R 5a , SO 2 NR 5 R 5a , SO 2 R 5b , C 3-10  carbocycle substituted with 0-5 R 5 , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S, substituted with 0-3 R 5 ; and  
           [0040]    m is selected from 0, 1, 2, and 3.  
           [0041]    In another embodiment of the present invention, the compounds of formula (I) are selected from:  
           [0042]    3-(4-methoxyphenyl)-5-(2-benzoylhydrazinecarboxamido)indeno[1,2-c]pyrazol-4-one;  
           [0043]    3-(4-methoxyphenyl)-5-(2-isonicotinoylhydrazinecarboxamido)indeno[1,2-c]pyrazol-4-one;  
           [0044]    3-(4-methoxyphenyl)-5-(2-nictinoylhydrazinecarbox amido)indeno[1,2-c]pyrazol-4-one;  
           [0045]    3-(4-methoxyphenyl)-5-(2-(3,4-dihydroxybenzoyl)hydrazine carboxamido)indeno[1,2-c]pyrazol-4-one;  
           [0046]    3-(4-methoxyphenyl)-5(2-(4-hydroxybenzoyl)hydrazine carboxamido)indeno[1,2-c]pyrazol-4-one;  
           [0047]    3-(4-methoxyphenyl)-5-(2-(3-aminobenzoyl) hydrazine carboxamido) indeno[1,2-c]pyrazol-4-one;  
           [0048]    3-(4-methoxyphenyl)-5-(2-(4-aminobenzoyl)hydrazine carboxamido)indeno[1,2-c]pyrazol-4-one;  
           [0049]    3-(4-methoxyphenyl)-5-(2-(2-aminobenzoyl)hydrazine carboxamido)indeno[1,2-c]pyrazol-4-one;  
           [0050]    3-(4-methoxyphenyl)-5-(2-(4-N,N-dimethylaminobenzoyl) hydrazinecarboxamido) indeno [1, 2-c]pyrazol-4-one;  
           [0051]    3-(4-methoxyphenyl)-5-(2-phenethylacetylhydrazine carboxamido) indeno[1,2-c]pyrazol-4-one;  
           [0052]    3-(4-methoxyphenyl)-5-(2-(2-hydroxybenzoyl)hydrazine carboxamido)indeno[1,2-c]pyrazol-4-one; and  
           [0053]    3-(4-methoxyphenyl)-5-(2-methoxycarbonyl hydrazinecarboxamido)indeno[1,2-c]pyrazol-4-one;  
           [0054]    1-[3-(4-methoxy-phenyl)-4-oxo-2,4-dihydro-indeno[1,2-c]pyrazol-5-yl]-3-morpholin-4-yl-urea;  
           [0055]    [3-(4-methoxy-phenyl)-4-oxo-2,4-dihydro-indeno[1,2-c]pyrazol-5-yl]-urea;  
           [0056]    1-(2-amino-cyclohexyl)-3-[3-(4-methoxy-phenyl)-4-oxo-2,4-dihydro-indeno[1,2-c]pyrazol-5-yl]-urea;  
           [0057]    2-(4-aminomethyl-piperidin-1-yl)-N-[3-(4-methoxy-phenyl)-4-oxo-2,4-dihydro-indeno[1,2-c]pyrazol-5-yl]-acetamide;  
           [0058]    1-[3-(4-methoxy-phenyl)-4-oxo-2,4-dihydro-indeno[1,2-c]pyrazol-5-yl]-3-morpholin-4-yl-urea.  
           [0059]    or pharmaceutically acceptable salt form thereof.  
           [0060]    Another embodiment of the present invention is a pharmaceutical composition comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of formula (I).  
           [0061]    Another embodiment of the present invention is a method of treating cancer and proliferative diseases comprising: administering to a host in need of such treatment a therapeutically effective amount of a compound of formula (I), or a pharmaceutically effective salt form thereof.  
         DEFINITIONS  
         [0062]    As used herein, the following terms and expressions have the indicated meanings. The compounds of the present invention may contain an asymmetrically substituted carbon atom, and may be isolated in optically active or racemic forms. It is well known in the art how to prepare optically active forms, such as by resolution of racemic forms or by synthesis from optically active starting materials. All chiral, diastereomeric, racemic forms and all geometric isomeric forms of a structure are intended, unless the specific stereochemistry or isomer form is specifically indicated.  
           [0063]    The term “alkyl” is intended to include both branched and straight-chain saturated aliphatic hydrocarbon groups having the specified number of carbon atoms. Examples of alkyl include, but are not limited to, methyl, ethyl, n-propyl, i-propyl, n-butyl, s-butyl, t-butyl, n-pentyl, and s-pentyl. In addition, the term is intended to include both unsubstituted and substituted alkyl groups, the latter referring to alkyl moieties having one or more hydrogen substituents replaced by, but not limited to halogen, hydroxyl, carbonyl, alkoxy, ester, ether, cyano, phosphoryl, amino, imino, amido, sulfhydryl, alkythio, thioester, sulfonyl, nitro, heterocyclo, aryl or heteroaryl. It will also be understood by those skilled in the art that the substituted moieties themselves can be substituted as well when appropriate.  
           [0064]    The terms “halo” or “halogen” as used herein refer to fluoro, chloro, bromo and iodo. The term “aryl” is intended to mean an aromatic moiety containing the specified number of carbon atoms, such as, but not limited to phenyl, indanyl or naphthyl. The terms “cycloalkyl” and “bicycloalkyl” are intended to mean any stable ring system, which may be saturated or partially unsaturated. Examples of such include, but are not limited to, cyclopropyl, cyclopentyl, cyclohexyl, norbornyl, bicyclo[2.2.2]nonane, adamantly, or tetrahydronaphthyl (tetralin).  
           [0065]    As used herein, “carbocycle” or “carbocyclic residue” is intended to mean any stable 3- to 7-membered monocyclic or bicyclic or 7- to 13-membered bicyclic or tricyclic, any of which may be saturated, partially unsaturated, or aromatic. Examples of such carbocycles include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, adamantyl, cyclooctyl,; [3.3.0]bicyclooctane, [4.3.0]bicyclononane, [4.4.0]bicyclodecane (decalin), [2.2.2]bicyclooctane, fluorenyl, phenyl, naphthyl, indanyl, adamantyl, or tetrahydronaphthyl (tetralin).  
           [0066]    As used herein, the term “heterocycle” or “heterocyclic system” is intended to mean a stable 5- to 7- membered monocyclic or bicyclic or 7- to 10-membered bicyclic heterocyclic ring which is saturated partially unsaturated or unsaturated (aromatic), and which consists of carbon atoms and from 1 to 4 heteroatoms independently selected from the group consisting of N, O and S and including any bicyclic group in which any of the above-defined heterocyclic rings is fused to a benzene ring. The nitrogen and sulfur heteroatoms may optionally be oxidized. The heterocyclic ring may be attached to its pendant group at any heteroatom or carbon atom which results in a stable structure. The heterocyclic rings described herein may be substituted on carbon or on a nitrogen atom if the resulting compound is stable. If specifically noted, a nitrogen in the heterocycle may optionally be quaternized. It is preferred that when the total number of S and O atoms in the heterocycle exceeds 1, then these heteroatoms are not adjacent to one another. It is preferred that the total number of S and O atoms in the heterocycle is not more than 1. As used herein, the term “aromatic heterocyclic system” is intended to mean a stable 5- to 7- membered monocyclic or bicyclic or 7- to 10-membered bicyclic heterocyclic aromatic ring which consists of carbon atoms and from 1 to 4 heterotams independently selected from the group consisting of N, O and S. It is preferred that the total number of S and O atoms in the aromatic heterocycle is not more than 1.  
           [0067]    Examples of heterocycles include, but are not limited to, 1H-indazole, 2-pyrrolidonyl, 2H,6H-1,5,2-dithiazinyl, 2H-pyrrolyl, 3H-indolyl, 4-piperidonyl, 4aH-carbazole, 4H-quinolizinyl, 6H-1,2,5-thiadiazinyl, acridinyl, azocinyl, benzimidazolyl, benzofuranyl, benzothiofuranyl, benzothiophenyl, benzoxazolyl, benzthiazolyl, benztriazolyl, benztetrazolyl, benzisoxazolyl, benzisothiazolyl, benzimidazalonyl, carbazolyl, 4aH-carbazolyl, b-carbolinyl, chromanyl, chromenyl, cinnolinyl, decahydroquinolinyl, 2H,6H-1,5,2-dithiazinyl, dihydrofuro[2,3-b]tetrahydrofuran, furanyl, furazanyl, imidazolidinyl, imidazolinyl, imidazolyl, 1H-indazolyl, indolenyl, indolinyl, indolizinyl, indolyl, isobenzofuranyl, isochromanyl, isoindazolyl, isoindolinyl, isoindolyl, isoquinolinyl, isothiazolyl, isoxazolyl, morpholinyl, naphthyridinyl, octahydroisoquinolinyl, oxadiazolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazolyl, oxazolidinyl., oxazolyl, oxazolidinylperimidinyl, phenanthridinyl, phenanthrolinyl, phenarsazinyl, phenazinyl, phenothiazinyl, phenoxathiinyl, phenoxazinyl, phthalazinyl, piperazinyl, piperidinyl, pteridinyl, piperidonyl, 4-piperidonyl, pteridinyl, purinyl, pyranyl, pyrazinyl, pyrazolidinyl, pyrazolinyl, pyrazolyl, pyridazinyl, pyridooxazole, pyridoimidazole, pyridothiazole, pyridinyl, pyridyl, pyrimidinyl, pyrrolidinyl, pyrrolinyl, pyrrolyl, quinazolinyl, quinolinyl, 4H-quinolizinyl, quinoxalinyl, quinuclidinyl, carbolinyl, tetrahydrofuranyl, tetrahydroisoquinolinyl, tetrahydroquinolinyl, 6H-1,2,5-thiadiazinyl, 1,2,3-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,5-thiadiazolyl, 1,3,4-thiadiazolyl, thianthrenyl, thiazolyl, thienyl, thienothiazolyl, thienooxazolyl, thienoimidazolyl, thiophenyl, triazinyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,5-triazolyl, 1,3,4-triazolyl, xanthenyl. Preferred heterocycles include, but are not limited to, pyridinyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, indolyl, benzimidazolyl, 1H-indazolyl, oxazolidinyl, benzotriazolyl, benzisoxazolyl, oxindolyl, benzoxazolinyl, or isatinoyl. Also included are fused ring and spiro compounds containing, for example, the above heterocycles.  
           [0068]    As used herein, “pharmaceutically acceptable salts” refer to derivatives of the disclosed compounds wherein the parent compound is modified by making acid or base salts thereof. Examples of pharmaceutically acceptable salts include, but are not limited to, mineral or organic acid salts of basic residues such as amines; alkali or organic salts of acidic residues such as carboxylic acids; and the like. The pharmaceutically acceptable salts include the conventional non-toxic salts or the quaternary ammonium salts of the parent compound formed, for example, from non-toxic inorganic or organic acids. For example, such conventional non-toxic salts include those derived from inorganic acids such as hydrochloric, hydrobromic, sulfuric, sulfamic, phosphoric, nitric and the like; and the salts prepared from organic acids such as acetic, propionic, succinic, glycolic, stearic, lactic, malic, tartaric, citric, ascorbic, pamoic, maleic, hydroxymaleic, phenylacetic, glutamic, benzoic, salicylic, sulfanilic, 2-acetoxybenzoic, fumaric, toluenesulfonic, methanesulfonic, ethane disulfonic, oxalic, isethionic, and the like.  
           [0069]    The pharmaceutically acceptable salts of the present invention can be synthesized from the parent compound which contains a basic or acidic moiety by conventional chemical methods. Generally, such salts can be prepared by reacting the free acid or base forms of these compounds with a stoichiometric amount of the appropriate base or acid in water or in an organic solvent, or in a mixture of the two; generally, nonaqueous media like ether, ethyl acetate, ethanol, isopropanol, or acetonitrile are preferred. Lists of suitable salts are found in Remington&#39;s Pharmaceutical Sciences, 18th ed., Mack Publishing Company, Easton, Pa., 1990, p. 1445, the disclosure of which is hereby incorporated by reference.  
           [0070]    The phrase “pharmaceutically acceptable” is employed herein to refer to those compounds, materials, compositions, and/or dosage forms which are, within the scope of sound medical judgment, suitable for use in contact with the tissues of human beings and animals without excessive toxicity, irritation, allergic response, or other problem or complication commensurate with a reasonable benefit/risk ratio.  
           [0071]    “Prodrugs”, as the term is used herein, are intended to include any covalently bonded carriers which release an active parent drug of the present invention in vivo when such prodrug is administered to a mammalian subject. Since prodrugs are known to enhance numerous desirable qualities of pharmaceuticals (i.e., solubility, bioavailability, manufacturing, etc.) the compounds of the present invention may be delivered in prodrug form. Thus, the present invention is intended to cover prodrugs of the presently claimed compounds, methods of delivering the same, and compositions containing the same. Prodrugs of the present invention are prepared by modifying functional groups present in the compound in such a way that the modifications are cleaved, either in routine manipulation or in vivo, to the parent compound. Prodrugs include compounds of the present invention wherein a hydroxy, amino, or sulfhydryl group is bonded to any group that, when the prodrug of the present invention is administered to a mammalian subject, it cleaves to form a free hydroxyl, free amino, or free sulfydryl group, respectively. Examples of prodrugs include, but are not limited to, acetate, formate, and benzoate derivatives of alcohol and amine functional groups in the compounds of the present invention.  
           [0072]    “Substituted” is intended to indicate that one or more hydrogens on the atom indicated in the expression using “substituted” is replaced with a selection from the indicated group(s), provided that the indicated atom&#39;s normal valency is not exceeded, and that the substitution results in a stable compound. When a substituent is keto (i.e., ═O) group, then 2 hydrogens on the atom are replaced.  
           [0073]    As used herein, the term “anti cancer” or “anti-proliferative” agent includes, but is not limited to, altretamine, busulfan, chlorambucil, cyclophosphamide, ifosfamide, mechlorethamine, melphalan, thiotepa, cladribine, fluorouracil, floxuridine, gemcitabine, thioguanine, pentostatin, methotrexate, 6-mercaptopurine, cytarabine, carmustine, lomustine, streptozotocin, carboplatin, cisplatin, oxaliplatin, iproplatin, tetraplatin, lobaplatin, JM216, JM335, fludarabine, aminoglutethimide, flutamide, goserelin, leuprolide, megestrol acetate, cyproterone acetate, tamoxifen, anastrozole, bicalutamide, dexamethasone, diethylstilbestrol, prednisone, bleomycin, dactinomycin, daunorubicin, doxirubicin, idarubicin, mitoxantrone, losoxantrone, mitomycin-c, plicamycin, paclitaxel, docetaxel, topotecan, irinotecan, 9-amino camptothecan, 9-nitro camptothecan, GS-211, etoposide, teniposide, vinblastine, vincristine, vinorelbine, procarbazine, asparaginase, pegaspargase, octreotide, estramustine, hydroxyurea.  
         SYNTHESIS  
         [0074]    The compounds of the present invention can be synthesized using the methods described below, together with synthetic methods known in the art of synthetic organic chemistry, or variations thereon as appreciated by those skilled in the art. Preferred methods include, but are not limited to, those methods described below. Each of the references cited below are hereby incorporated herein by reference.  
                         
 
           [0075]    An approach to preparing indeno[1,2-c]pyrazol-4-ones is presented in Scheme 1 and can be used to prepare compounds of the present invention. The nitro group of dimethyl 3-nitrophthalate was reduced to the amine using catalytic hydrogenation. The aniline was acylated using acetic anhydride and pyridine as a base. A mixture of the resulting acetamide 2 and an acetophenone were treated with a strong base in an appropriate solvent at elevated temperature to give the desired triketone 3. Additional means of preparing triketones are known to one skilled in the art as described in Kilgore et al, Industrial and Engineering Chemistry 34:494-497, 1946, the contents of which are hereby incorporated herein by reference. The triketone was treated with hydrazine at elevated temperature in an appropriate solvent to give the indeno[1,2-c]pyrazol-4-one ring system. Additional means of preparing indeno[1,2-c]pyrazol-4-ones are known to one skilled in the art as described in Lemke et al., J. Heterocyclic Chem. 19:1335-1340, 1982; Mosher and Soeder, J. Heterocyclic Chem. 8:855-59, 1971; Hrnciar and Svanygova Collect. Czech. Chem. Commun. 59:2734-40, 1994 the contents of which are hereby incorporated herein by reference. The amide was deacylated by heating with a strong acid in an appropriate solvent to give aniline 4. This aniline was acylated under standard conditions using an acid chloride in an appropriate solvent to give the desired product 5. 
                         
 
           [0076]    An alternative method for making compounds of the present invention is shown in Scheme 2. The intermediate triketone 3 can be deacylated with strong acid and reacylated with an appropriate acid chloride using methods known to those skilled in the art. Subsequently, triketone 6 can the be converted to the indeno[1,2-c]pyrazol-4-one ring system using the same conditions described previously in Scheme 1. 
                         
 
           [0077]    Another method for preparing the triketones 6 of Scheme 2 employs the condensation of a 1,3-diketone 6a with 3-nitrophthalic anhydride as described in Rotberg and Oshkaya, Zh. Organ. Khim. 8:84-87, 1972; Zh. Organ. Khim. 9:2548-2550, 1973, the contents of which are hereby incorporated herein by reference. The 1,3-diketones, when not commercially available can be readily prepared by one skilled in the art by the acetylation or trifluoroacetylation of the requisite methyl ketone, R 1 COCH 3 . Reduction of the nitro derivative 6b to the aniline 6c can be accomplished in a variety of ways including catalyic hydrogenation, treatment with zinc or iron under acidic conditions, or treatment with other reducing agents such as sodium dithionite or stannous chloride. Subsequently the aniline 6c can be converted to the indeno[1,2-c]pyrazol-4-ones of this invention by acylation followed by treatment with hydrazine as described previously in Scheme 2. 
                         
 
           [0078]    Another method for making the indeno[1,2-c]pyrazol-4-one ring system is shown in Scheme 4. Dimethyl hydrazine was reacted with 3-acetylpyridine with no solvent to give the hydrazone 7. This was treated in a similar fashion as described in Scheme 1 to give the desired intermediate 8. Additional means of preparing similar intermediates are known to one skilled in the art as described in Rappoport, J. Org. Chem. 49:2948-2953, 1984, the contents of which are hereby incorporated herein by reference. This intermediate was carried through the sequence in a similar fashion as described in Scheme 1. 
                         
 
           [0079]    Another approach to preparing indeno[1,2-c]pyrazol-4-ones is presented in Scheme 5 and can be used to prepare compounds of the present invention. Treating the intermediate 5-aminoindeno[1,2-c]pyrazol-4-one with 2-(trimethylsilyl) ethoxymethylmethyl chloride (SEMCl) and a suitable base in an inert solvent under reflux gives the SEM protected intermediate. The aniline is converted to the carbamate with phenylchloroformate using methods known to those skilled in the art. This intermediate is reacted with carbaztes in DMSO at elevated temperatures and then the SEM group is removed by treating with acid in a polar protic solvent to give the desired acylsemicarbazide-containing indenopyrazole analogs.  
           [0080]    Other features of the invention will become apparent during the following descriptions of exemplary embodiments which are given for illustration of the invention and are not intended to be limiting thereof. 
       
    
    
     EXAMPLES  
       [0081]    Abbreviations used in the Examples are defined as follows: “° C.” for degrees Celsius, “CIMS” for chemical ionization mass spectroscopy, “eq” for equivalent or equivalents, “g” for gram or grams, “h” for hour or hours, “mg” for milligram or milligrams, “mL” for milliliter or milliliters, “mmol” for millimolar, “M” for molar, “min” for minute or minutes, “p-TsOH” for para-toluenesulphonic acid, “DMF” for dimethylformamide, and “TFA” for trifluoroacetic acid.  
       Example I  
     Preparation of 3-(4-methoxyphenyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0082]    [0082]                           
         [0083]    Step 1. Synthesis of 2 from dimethyl 3-nitrophthalate.  
         [0084]    A solution of dimethyl 3-nitrophthalate (25 g, 105 mmol) in methanol (100 mL) was treated with 5% Pd/C (2.5 g) and hydrogenated on a Parr Shaker at 50 psi for 2 h. The solution was filtered (Celite), the filtrate collected and the solvent removed at reduced pressure. The residue was dissolved in acetic anhydride (20 mL) treated with pyridine (0.05 mL) and heated to 80° C. for 1 min. The reaction was cooled and stirred at 25° C. for 2 h. The solvent was removed at reduced pressure and the residue recrystallized from ethanol to give the product as a white solid (21 g, 79%). mp 104-105° C.; CIMS m/e calc&#39;d for C 12 H 14 NO 5 : 252.0872, found 252.0888; Analysis calc&#39;d for C 12 H 13 NO 5 : C, 57.37; H, 5.22; N, 5.58; found: C, 57.67; H, 5.29; N, 5.77.  
         [0085]    Step 2. Synthesis of triketone 11 from 2.  
         [0086]    A solution of 2 (1 g, 4.0 mmol) in dry DMF (2 mL) was treated with sodium hydride (0.15 g, 60% suspension in oil, 0.4 mmol) in one portion. After 1 h, 4-methoxyacetophenone (0.6 g, 4.0 mmol) was added in one portion and the reaction heated to 90° C. A second portion of sodium hydride (0.15 g, 60% suspension in oil, 0.4 mmol) was added and the exothermic reaction turns deep red. After 20 min, the reaction was cooled to 25° C. diluted with water (20 mL), extracted with EtOAc (10 mL) and the aqueous phase separated. The aqueous phase was acidified with 2 N HCl to pH 2 and the crude product collected. Recrystalization with ethanol gave the desired product as a yellow solid (0.4 g, 30%). mp 174-175° C.; CIMS m/e calc&#39;d for C 19 H 16 NO 5 : 338.1028, found 338.1022; Analysis calc&#39;d for C 19 H 15 NO 5 : C, 67.65; H, 4.48; N, 4.15; found: C, 67.87; H, 4.29; N, 3.99.  
         [0087]    Step 3. Synthesis of 12 from 11.  
         [0088]    A solution of 11 (0.2 g, 0.6 mmol) in EtOH (5 mL) was treated with hydrazine hydrate (0.1 mL, 1.8 mmol) and p-TsOH (3 mg). The reaction was heated to reflux and stirred for 2 h. The reaction was cooled to 25° C. and the product collected as a yellow solid (0.1 g, 50%). mp 268° C.; CIMS m/e calc&#39;d for C 19 H 16 N 3 O 3 : 334.1192, found: 334.1168; Analysis calc&#39;d for C 19 H 15 N 3 O 3 : C, 68.46; H, 4.54; N, 12.61; found: C, 68.81; H, 4.39; N, 12.45.  
       Example II  
     Preparation of 3-(4-methoxyphenyl)-5-(chloroacetamido)indeno[1,2-c]pyrazol-4-one  
       [0089]    [0089]                           
         [0090]    Step 1. Synthesis of 13 from 12.  
         [0091]    A suspension of 12 (1.0 g, 3.0 mmol) in MeOH (10 mL) was treated with conc. HCl (1 mL) and heated to reflux. After 2 h, the reaction was cooled and the product was collected as a greenish solid (0.7 g, 81%). mp 273° C.; CIMS m/e calc&#39;d for C 17 H 13 N 3 O 2 :292.1086, found: 292.1080; Analysis calc&#39;d for C 17 H 14 N 3 O 2 : C, 69.85; H, 4.83; N, 14.37; found: C, 69.99; H, 4.59; N, 14.44.  
         [0092]    Step 2. Synthesis of 14 from 13.  
         [0093]    A suspension of 13 (20 mg, 0.07 mmol) in dioxane (2 mL) was treated with aqueous sat. NaHCO 3  (1 mL) and chloroacetyl chloride (30 mL, 0.21 mmol). The reaction was heated to 50° C. and stirred for 2 h. The reaction was cooled, poured into water (2 mL), extracted with EtOAc (10 mL), the organic layer separated, dried (MgSO 4 ) and the solvent removed at reduced pressure. The solid residue was recrystallized from EtOH to give the product as a yellow solid (9 mg, 35%). mp 274° C.; CIMS m/e calc&#39;d for C 19 H 15 N 3 O 3 Cl:368.0802, found: 368.0818.  
       Example III  
     Preparation of 3-(4-methoxyphenyl)-5-(cyclopropylamido)indeno[1,2-c]pyrazol-4-one  
       [0094]    Prepared in a similar fashion as described for example II using cyclopropylacetyl chloride as the starting material. mp 289° C.; CIMS m/e calc&#39;d for C 21 H 18 N 3 O 3 : 360.1348, found: 360.1330.  
       Example IV  
     Preparation of 3-(4-methoxyphenyl)-5-(isopropylamido)indeno[1,2-c]pyrazol-4-one  
       [0095]    Prepared in a similar fashion as described for example II using isopropylacetyl chloride as the starting material. mp 288° C.; CIMS m/e calc&#39;d for C 21 H 20 N 3 O 3 : 362.1505, found: 362.1535.  
       Example V  
     Preparation of 3-(4-methoxyphenyl)-5-(ethylamido)indeno[1,2-c]pyrazol-4-one  
       [0096]    Prepared in a similar fashion as described for example II using propionyl chloride as the starting material. mp 287 ° C.; CIMS m/e calc&#39;d for C 20 H 18 N 3 O 3 : 348.1348, found: 348.1313.  
       Example VI  
     Preparation of 3-(4-methoxyphenyl)-5-(cyclopentylamido)indeno[1,2-c]pyrazol-4-one  
       [0097]    Prepared in a similar fashion as described for example II using cyclopentylacetyl chloride as the starting material. mp 267° C.; CIMS m/e calc&#39;d for C 23 H 22 N 3 O 3 : 388.1661, found: 388.1626.  
       Example VII  
     Preparation of 3-(4-methoxyphenyl)-5-(cyclobutylamido)indeno[1,2-c]pyrazol-4-one  
       [0098]    Prepared in a similar fashion as described for example II using cyclobutylacetyl chloride as the starting material. mp 297° C.; CIMS m/e calc&#39;d for C 22 H 20 N 3 O 3 : 374.1505, found: 374.1530.  
       Example VIII  
     Preparation of 3-(4-methoxyphenyl)-5-(phenylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0099]    Prepared in a similar fashion as described for example II using phenylacetyl chloride as the starting material. mp 280° C.; CIMS m/e calc&#39;d for C 25 H 20 N 3 O 3 : 410.1505, found: 410.1533.  
       Example IX  
     Preparation of 3-(4-methoxyphenyl)-5-(butylamido)indeno[1,2-c]pyrazol-4-one  
       [0100]    Prepared in a similar fashion as described for example II using butyryl chloride as the starting material. mp 282° C.; CIMS m/e calc&#39;d for C 21 H 20 N 3 O 3 : 362.1505, found: 362.1500.  
       Example X  
     Preparation of 3-(4-methoxyphenyl)-5-((4-chlorophenyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0101]    Prepared in a similar fashion as described for example II using 4-chlorophenylacetyl chloride as the starting material. mp 238° C.; CIMS m/e calc&#39;d for C 25 H 19 N 3 O 3 Cl: 444.1115, found: 444.1110.  
       Example XI  
     Preparation of 3-(4-methoxyphenyl)-5-((3-methoxyphenyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0102]    Prepared in a similar fashion as described for example II using 3-methoxyphenylacetyl chloride as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 26 H 22 N 3 O 4 : 440.1610, found: 440.1620.  
       Example XII  
     Preparation of 3-(4-methoxyphenyl)-5-((4-methoxyphenyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0103]    Prepared in a similar fashion as described for example II using 4-methoxyphenylacetyl chloride as the starting material. mp 280° C.; CIMS m/e calc&#39;d for C 26 H 22 N 3 O 4 : 440.1610, found: 440.1630.  
       Example XIII  
     Preparation of 3-(4-methoxyphenyl)-5-((3,4-dimethoxyphenyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0104]    Prepared in a similar fashion as described for example II using 3,4-dimethoxyphenylacetyl chloride as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 27 H 24 N 3 O 5 : 470.1716, found: 470.1731.  
       Example XIV  
     Preparation of 3-(4-methoxyphenyl)-5-((2,5-dimethoxyphenyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0105]    Prepared in a similar fashion as described for example II using 2,5-dimethoxyphenylacetyl chloride as the starting material. mp 226° C.; CIMS m/e calc&#39;d for C 27 H 24 N 3 O 5 : 470.1716, found: 470.1739.  
       Example XV  
     Preparation of 3-(2-methoxyphenyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0106]    Prepared in a similar fashion as described for example I using 2-methoxyacetophenone as the starting material. mp 276° C.; CIMS m/e calc&#39;d for C 19 H 16 N 3 O 3 : 334.1192, found: 334.1169.  
       Example XVI  
     Preparation of 3-(3,4-dimethoxyphenyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0107]    Prepared in a similar fashion as described for example I using 3,4-dimethoxyacetophenone as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 20 H 18 N 3 O 4 : 364.1297, found: 364.1288.  
       Example XVII  
     Preparation of 3-(4-methoxyphenyl)-5-((3,4-ethylenedioxyphenyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0108]    [0108]                           
         [0109]    Step 1. Synthesis of 15 from 11.  
         [0110]    A suspension of 11 (5 g, 14.8 mmol) in MeOH (50 mL) was treated with conc. HCl (3 mL) and heated to reflux. After stirring for 2 h, the reaction was cooled to 0° C. and the product collected as a yellow solid (4.2 g, 96%). mp 173° C.; CIMS m/e calc&#39;d for C 17 H 14 NO 4 : 296.0923, Found: 296.0901.  
         [0111]    Step 2. Synthesis of 16 from 15.  
         [0112]    A suspension of 15 (20 mg, 0.07 mmol) in acetone (2 mL) was treated with NaHCO 3  (10 mg) and the acid chloride of (3,4-methylenedioxyphenyl)acetic acid (prepared by heating the acid in a benzene:thionyl chloride 4:1 mixture at 50° C. for 2 h, removing the volatile components at reduced pressure, and using the crude acid chloride without further purification). The reaction was heated to 50° C. and stirred for 2 h. The reaction was cooled, poured into water (4 mL), extracted with EtOAc (10 mL), dried (MgSO 4 ), filtered and concentrated. The crude triketone was suspended in EtOH (2 mL), treated with hydrazine hydrate (0.05 mL) and p-TsOH (1 mg) and heated to reflux for 2 h. The reaction was cooled to 0° C. and the product filtered to give a yellow solid (6.5 mg, 20%). mp 297° C.; CIMS m/e calc&#39;d for C 26 H 20 N 3 O 5 : 454.1403, Found: 454.1398.  
       Example XVIII  
     Preparation of 3-(4-dimethoxyphenyl)-5-((3-thiophene)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0113]    Prepared in a similar fashion as described for example XVII using the acid chloride of 3-thiopheneacetic acid as the starting material. mp 293° C.; CIMS m/e calc&#39;d for C 23 H 18 N 3 O 3 S: 416.1069, found: 416.1088.  
       Example XIX  
     Preparation of 3-(4-methoxyphenyl)-5-((2-methoxyphenyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0114]    Prepared in a similar fashion as described for example XVII using the acid chloride of 2-methoxyphenylacetic acid as the starting material. mp 255° C.; CIMS m/e calc&#39;d for C 26 H 22 N 3 O 4 : 440.1610, found: 440.1622.  
       Example XX  
     Preparation of 3-(4-methoxyphenyl)-5-((3,4-dichlorophenyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0115]    Prepared in a similar fashion as described for example XVII using the acid chloride of 3,4-dichlorophenylacetic acid as the starting material. mp 299° C.; CIMS m/e calc&#39;d for C 25 H 18 N 3 O 3 Cl 2 : 478.0725, found: 478.0744.  
       Example XXI  
     Preparation of 3-(4-methoxyphenyl)-5-((2,4-dichlorophenyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0116]    Prepared in a similar fashion as described for example XVII using the acid chloride of 2,4-dichlorophenylacetic acid as the starting material. mp 286° C.; CIMS m/e calc&#39;d for C 25 H 18 N 3 O 3 Cl 2 : 478.0725, found: 478.0734.  
       Example XXII  
     Preparation of 3-(4-methoxyphenyl)-5-((2-chlorophenyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0117]    Prepared in a similar fashion as described for example XVII using the acid chloride of 2-chlorophenylacetic acid as the starting material. mp 300° C.; CIMS m/e calc&#39;d for C 25 H 19 N 3 O 3 Cl: 444.1115, found: 444.1111.  
       Example XXIII  
     Preparation of 3-(4-methoxyphenyl)-5-(aminoacetamido)indeno[1,2-c]pyrazol-4-one  
       [0118]    [0118]                           
         [0119]    A suspension of 14 (15 mg, 0.04 mmol) in EtOH (1 mL) was treated with conc. NH 4 OH (1 mL), placed in a sealed tube and heated to 80° C. for 3 h. The reaction was cooled and the solvent removed at reduced pressure. The residue was recrystallized from EtOH to give the product as a yellow solid (9 mg, 62%). mp &gt;300° C.; CIMS m/e calc&#39;d for C 20 H 19 N 4 O 3 : 363.1457, Found: 363.1431.  
       Example XXIV  
     Preparation of 3-(4-methoxyphenyl)-5-((2-hydroxyethyl)aminoacetamido)indeno[1,2-c]pyrazol-4-one  
       [0120]    Prepared in a similar fashion as described for example XXIII using hydroxylamine as the starting material. mp 243° C.; CIMS m/e calc&#39;d for C 21 H 21 N 4 O 4 : 393.1563, found: 393.1539.  
       Example XXV  
     Preparation of 3-(4-methoxyphenyl)-5-(N,N-dimethylaminoacetamido)indeno[1,2-c]pyrazol-4-one  
       [0121]    Prepared in a similar fashion as described for example XXIII using dimethylamine as the starting material. mp 279° C.; CIMS m/e calc&#39;d for C 21 H 21 N 4 O 3 : 377.1614, found: 377.1640.  
       Example XXVI  
     Preparation of 3-(4-methoxyphenyl)-5-(piperazinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0122]    Prepared in a similar fashion as described for example XXIII using piperazine as the starting material. mp 277° C.; CIMS m/e calc&#39;d for C 23 H 24 N 5 O 3 : 418.1879, found: 418.1899.  
       Example XXVII  
     Preparation of 3-(4-methoxyphenyl)-5-(4-methylpiperazinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0123]    Prepared in a similar fashion as described for example XXIII using 4-methylpiperizine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 24 H 26 N 5 O 3 : 432.2036, found: 432.2030.  
       Example XXVIII  
     Preparation of 3-(4-methoxyphenyl)-5-(4-(2-hydroxyethyl)piperazinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0124]    Prepared in a similar fashion as described for example XXIII using 4-hydroxyethylpiperizine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 25 H 28 N 5 O 4 : 462.2141, found: 462.2128.  
       Example XXIX  
     Preparation of 3-(4-methoxyphenyl)-5-(piperidinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0125]    Prepared in a similar fashion as described for example XXIII using piperidine as the starting material. mp 291° C.; CIMS m/e calc&#39;d for C 24 H 25 N 4 O 3 : 417.1927, found: 417.1955.  
       Example XXX  
     Preparation of 3-(4-methoxyphenyl)-5-(4-aminomethylpiperidinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0126]    Prepared in a similar fashion as described for example XXIII using 4-aminomethylpiperidine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 25 H 28 N 5 O 3 : 446.2192, found: 446.2166.  
       Example XXXI  
     Preparation of 3-(4-methoxyphenyl)-5-(ethylaminoacetamido)indeno[1,2-c]pyrazol-4-one  
       [0127]    Prepared in a similar fashion as described for example XXIII using ethylamine as the starting material. mp 250° C.; CIMS m/e calc&#39;d for C 21 H 21 N 4 O 3 : 377.1614, found: 377.1644.  
       Example XXXII  
     Preparation of 3-(4-methoxyphenyl)-5-(thiomorpholinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0128]    Prepared in a similar fashion as described for example XXIII using thiomorpholine as the starting material. mp 298° C.; CIMS m/e calc&#39;d for C 23 H 23 N 4 O 3 S: 435.1491, found: 435.1477.  
       Example XXXIII  
     Preparation of 3-(4-methoxyphenyl)-5-(morpholinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0129]    Prepared in a similar fashion as described for example XXIII using morpholine as the starting material. mp 295° C.; CIMS m/e calc&#39;d for C 23 H 23 N 4 O 4 : 419.1719, found: 419.1744.  
       Example XXXIV  
     Preparation of 3-(4-methoxyphenyl)-5-(pyrrolidinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0130]    Prepared in a similar fashion as described for example XXIII using pyyrolidine as the starting material. mp 279° C.; CIMS m/e calc&#39;d for C 23 H 23 N 4 O 3 : 403.1770, found: 403.1761.  
       Example XXXV  
     Preparation of 3-(4-methoxyphenyl)-5-(4-pyridinylaminomethylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0131]    Prepared in a similar fashion as described for example XXIII using 4-aminomethylpyridine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 25 H 22 N 5 O 3 : 440.1723, found: 440.1762.  
       Example XXXVI  
     Preparation of 3-(4-methoxyphenyl)-5-((4-acetamidophenyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0132]    [0132]                           
         [0133]    A suspension of 18 (10 mg, 0.02 mmol) in dioxane (1 mL) was treated with aqueous sat. NaHCO 3  (0.5 mL) and acetyl chloride (0.01 mL) and heated at 50° C. for 1 h. The reaction was cooled, poured into water (5 mL), extracted with EtOAc (10 mL), the organic layer separated, dried (MgSO 4 ) and the solvent removed at reduced pressure. The residue was recrystallized from EtOH to give the product as a yellow solid (5.6 mg, 61%). mp 268° C.; CIMS m/e calc&#39;d for C 27 H 23 N 4 O 4 : 467.1719, Found: 467.1730.  
       Example XXXVII  
     Preparation of 3-(4-methoxyphenyl)-5-((4-methoxycarbonylaminophenyl)acetamido) indeno[1,2-c]pyrazol-4-one  
       [0134]    Prepared in a similar fashion as described for example XXXII using methylchloroformate as the starting material. mp 257° C.; CIMS m/e calc&#39;d for C 27 H 23 N 4 O 5 : 483.1668, found: 483.1633.  
       Example XXXVIII  
     Preparation of 3-(4-methoxyphenyl)-5-((4-aminomethylcarbonylaminophenyl)acetamido) indeno[1,2-c]pyrazol-4-one  
       [0135]    Prepared in a similar fashion as described for example XXIII and XXXII using chloroacetyl chloride and conc. NH 4 OH as the starting materias. mp 228° C.; CIMS m/e calc&#39;d for C 27 H 24 N 5 O 4 : 482.1828, found: 482.1844.  
       Example XXXIX  
     Preparation of 3-(4-methoxyphenyl)-5-((4-N,N-dimethylaminomethylcarbonylaminophenyl)acetamido) indeno[1,2-c]pyrazol-4-one  
       [0136]    Prepared in a similar fashion as described for example XXIII and XXXII using chloroacetyl chloride and dimethyl amine as the starting materias. mp &gt;300° C.; CIMS m/e calc&#39;d for C 29 H 28 N 5 O 4 : 510.2141, found: 510.2121.  
       Example XL  
     Preparation of 3-(4-methoxyphenyl)-5-((4-azidophenyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0137]    A solution of example XXXVI (20 mg, 0.04 mmol) in DMF (2 mL) was treated with 5% palladium on carbon (5 mg) and hydrogentaed at atmospheric pressure using a hydrogen baloon. After 2 h, the solution was filtered (Celite), and the solvent removed at reduced pressure. The residue was recrystallized from EtOH to give the product as a yellow solid (15 mg, 78%). mp &gt;300° C.; CIMS m/e calc&#39;d for C 25 H 19 N 6 O 3 : 451.1519, found: 451.1544.  
       Example XLI  
     Preparation of 3-(4-methoxyphenyl)-5-((4-aminophenyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0138]    Prepared in a similar fashion as described for example XXVII using the acid chloride of 4-azidophenylacetic acid as the starting material. mp 283° C.; CIMS m/e calc&#39;d for C 25 H 21 N 4 O 3 : 425.1614, found: 425.1643.  
       Example XLII  
     Preparation of 3-(4-methoxyphenyl)-5-(phenylcarbamoyl)aminoindeno [1,2-c]pyrazol-4-one  
       [0139]    [0139]                           
         [0140]    Step 1. Synthesis of 20 from 15.  
         [0141]    A suspension of 15 (0.5 g, 1.7 mmol) in acetone (10 mL) was treated with NaHCO 3  (0.5 g) and phenyl chloroformate. The mixture was heated to 50° C. for 2 h. The reaction was cooled, poured into water (20 mL), extracted with EtOAc (40 mL), the organic layer separated, dried (MgSO 4 ) and the solvent removed at reduced pressure. The residue was suspended in EtOH (10 mL) and treated with hydrazine hydrate (0.16 mL, 5.1 mmol) and p-TsOH (10 mg). The mixture was heated to reflux and stirred for 3 h. The reaction was cooled to 0° C. and the product collected as a yellow solid (0.25 g, 36%). mp 195° C.; CIMS m/e calc&#39;d for C 24 H 18 N 3 O 4 : 412.1297, Found: 412.1308.  
         [0142]    Step 2. Synthesis of 21 from 20.  
         [0143]    A solution of 20 (20 mg, 0.05 mmol) in DMSO (2 mL) was treated with aniline (20 mL, mmol) and dimethylaminopyridine (1 mg). The mixture was heated to 80° C. for 2 h. The reaction was cooled, poured into water (4 mL), extracted with EtOAc (15 mL), the organic layer separated, dried (MgSO 4 ) and the solvent removed at reduced pressure. The residue was recrystallized from EtOH to give the product as a yellow solid (9 mg, 44%). mp &gt;300° C.; CIMS m/e calc&#39;d for C 24 H 19 N 4 O 3 : 411.1457, Found: 411.1432.  
       Example XLIII  
     Preparation of 3-(4-methoxyphenyl)-5-(butylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0144]    Prepared in a similar fashion as described for example XLII using butyl amine as the starting material. mp 252° C.; CIMS m/e calc&#39;d for C 21 H 21 N 4 O 3 : 377.1614, found: 377.1633.  
       Example XLIV  
     Preparation of 3-(4-methoxyphenyl)-5-(4-aminobenzylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0145]    Prepared in a similar fashion as described for example XLII using 4-aminobenzyl amine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 25 H 22 N 5 O 3 : 440.1723, found: 440.1700.  
       Example XLV  
     Preparation of 3-(4-methoxyphenyl)-5-(4-pyridylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0146]    Prepared in a similar fashion as described for example XLII using 4-aminomethylpyridine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 24 H 20 N 5 O 3 : 426.1566, found: 426.1533.  
       Example XLVI  
     Preparation of 3-(4-hydroxyphenyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0147]    [0147]                           
         [0148]    A suspension of 12 (20 mg, 0.07 mmol) in CH 2 Cl 2  (2 mL) was treated with excess BBr 3  (1.0 mL, 1.0 M in CH 2 Cl 2 ) and stirred for 20 h. The reaction was slowly poured into aqueous sat. NaHCO 3  (5 mL), extracted with EtOAc (10 mL), dried (MgSO 4 ) and concentrated. The residue was recrystallized from EtOH to give the desired product as a yellow solid (7.5 mg, 33%). mp &gt;300° C.; CIMS m/e calc&#39;d for C 18 H 14 N 3 O 3 : 320.1035, Found: 320.1050.  
       Example XLVII  
     Preparation of 3-(4-methoxyphenyl)-5-(formamido)indeno[1,2-c]pyrazol-4-one  
       [0149]    [0149]                           
         [0150]    A suspension of 13 (20 mg, 0.06 mmol) in formic acid (2 mL) was heated to 100° C. for 2 h. The reaction mixture was cooled and the solvent removed at reduced pressure. The residue was recrystallized from EtOH to give the desired product as a yellow solid (12 mg, 63%). mp 280° C.; CIMS m/e calc&#39;d for C 18 H 14 N 3 O 3 : 320.1035, Found: 320.1040.  
       Example XLVIII  
     Preparation of 3-(3-pyridyl)-5-(acetamido)indeno [1,2-c]pyrazol-4-one  
       [0151]    [0151]                           
         [0152]    Step 1. Synthesis of 24 from 3-acetylpyridine.  
         [0153]    A solution of 3-acetylpyridine (1.0 g, 8.3 mmol) in benzene (3 mL) was treated with 1,1-dimethylhydrazine (0.62 mL, 8.3 mmol) and p-TsOH (5 mg). The mixture was heated to 85° C. and stirred for 3 h. The reaction was cooled and the solvent removed at reduced pressure. This crude hydrazone was treated with 1.0 M NaN(TMS) 2  in THF (16.6 mL, 16.6 mmol) at 25° C. over 5 min. After 30 min dimethyl 3-acetamidophthalate (2.1 g, 8.3 mmol) was added in one portion and the reaction heated to reflux. Stirring was continued for 6 h. The reaction was cooled and quenched by the slow addition of TFA. The solvent was removed at reduced pressure and the residue chromatographed (silica, 2.5-5% MeOH/CH 2 Cl 2 ) to give the product as a yellow solid (0.35 g, 14%). mp 265° C.; CIMS m/e calc&#39;d for C 17 H 13 N 2 O 4 : 309.0875, Found: 309.0888.  
         [0154]    Step 2. Synthesis of 25 from 24.  
         [0155]    A suspension of 24 (30 mg, 0.09 mmol) in EtOH (2 mL) was treated with hydrazine hydrate (0.05 mL) and p-TsOH (1 mg) and heated to reflux. After stirring for 2 h. the reaction was cooled and the product filtered to give a yellow solid (12 mg, 44%). mp &gt;300° C.; CIMS m/e calc&#39;d for C 17 H 13 N 4 O 2 : 305.1039, Found: 305.1048.  
       Example XLIX  
     Preparation of 3-(4-pyridyl)-5-(acetamido)indeno [1,2-c]pyrazol-4-one  
       [0156]    Prepared in a similar fashion as described for example XLVIII using 4-acetylpyridine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 17 H 13 N 4 O 2 : 305.1039, found: 305.1046.  
       Example L  
     Preparation of 3-(4-pyridyl)-5-(formamido)indeno [1,2-c]pyrazol-4-one  
       [0157]    Prepared in a similar fashion as described for example XLVII using 4-acetylpyridine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 16 H 11 N 4 O 2 : 291.0882, found: 291.0882.  
       Example LI  
     Preparation of 3-phenyl-5-(acetamido)indeno [1,2-c]pyrazol-4-one  
       [0158]    Prepared in a similar fashion as described for example I using acetophenone as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 18 H 13 N 3 O 2 : 304.1065, found: 304.1086.  
       Example LII  
     Preparation of 3-(4-methylthiophenyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0159]    Prepared in a similar fashion as described for example I using 4′-methylthioacetophenone as the starting material. mp 283° C.; CIMS m/e calc&#39;d for C 19 H 15 N 3 O 2 S: 350.0956, found: 350.0963.  
       Example LIII  
     Preparation of 3-(4-methylsulphonylphenyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0160]    Prepared by oxidation of the product of example LII. mp &gt;300° C.; CIMS m/e calc&#39;d for C 19 H 15 N 3 O 4 S: 382.0860, found: 382.0862.  
       Example LIV  
     Preparation of 3-(4-N,N-dimethylaminophenyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0161]    Prepared in a similar fashion as described for example I using 4′-N,N,-dimethylaminoacetophenone as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 20 H 18 N 4 O 2 : 347.1496, found: 347.1508.  
       Example LV  
     Preparation of 3-(4-N,N-dimethylaminophenyl)-5-(morpholinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0162]    Prepared in a similar fashion as described for examples II and XXIII employing the product of example LIV and morpholine as the starting materials. mp &gt;300° C.; CIMS m/e calc&#39;d for C 24 H 26 N 5 O 3 : 432.2036, found: 432.2020.  
       Example LVI  
     Preparation of 3-(4-N,N-dimethylaminophenyl)-5-(dimethylaminoacetamido)indeno[1,2-c]pyrazol-4-one  
       [0163]    Prepared in a similar fashion as described for examples II and XXIII employing the product of example LIV and dimethylamine as the starting materials. mp &gt;300° C.; CIMS m/e calc&#39;d for C 22 H 24 N 5 O 2 : 390.1930, found: 390.1948.  
       Example LVII  
     Preparation of 3-(4-(1-piperidinyl)phenyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0164]    Prepared in a similar fashion as described for example I using 4′-(1-piperidinyl)acetophenone as the starting material. mp 291° C.; CIMS m/e calc&#39;d for C 23 H 22 N 4 O 2 : 387.1801, found: 387.1821.  
       Example LVIII  
     Preparation of 3-(4-morpholinyl)phenyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0165]    Prepared in a similar fashion as described for example I using 4′-morpholinylacetophenone as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 22 H 20 N 4 O 3 : 388.1528, found: 388.1535.  
       Example LIX  
     Preparation of 3-(4-ethoxyphenyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0166]    Prepared in a similar fashion as described for example I using 4′-ethoxyacetophenone as the starting material. mp 288° C.; CIMS m/e calc&#39;d for C 20 H 17 N 3 O 3 : 348.1325, found: 348.1348.  
       Example LX  
     Preparation of 3-(4-butylphenyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0167]    Prepared in a similar fashion as described for example I using 4′-butylacetophenone as the starting material. mp 259° C.; CIMS m/e calc&#39;d for C 22 H 21 N 3 O 2 : 360.1701, found: 360.1712.  
       Example LXI  
     Preparation of 3-(4-ethylphenyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0168]    Prepared in a similar fashion as described for example I using 4′-ethylacetophenone as the starting material. mp 294° C.; CIMS m/e calc&#39;d for C 20 H 17 N 3 O 2 : 331.1310, found: 331.1321.  
       Example LXII  
     Preparation of 3-(4-n-propylphenyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0169]    Prepared in a similar fashion as described for example I using 4′-n-propylacetophenone as the starting material. mp 269° C.; CIMS m/e calc&#39;d for C 21 H 19 N 3 O 2 : 346.1555, found: 346.1554.  
       Example LXIII  
     Preparation of 3-(4-methoxyphenyl)-5-carbamoylaminoindeno[1,2-c]pyrazol-4-one  
       [0170]    Prepared in a similar fashion as described for example XLII using concentrated ammonium hydroxide as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 18 H 15 N 4 O 3 : 335.1144, found: 335.1113.  
       Example LXIV  
     Preparation of 3-(4-methoxyphenyl)-5-(dimethylaminocarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0171]    Prepared in a similar fashion as described for example XLII using dimethylamino hydrazine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 20 H 20 N 5 O 3 : 378.1566, found: 378.1555.  
       Example LXV  
     Preparation of 3-(4-methoxyphenyl)-5-(methylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0172]    Prepared in a similar fashion as described for example XLII using methylamine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 19 H 17 N 4 O 3 : 349.1300, found: 349.1311.  
       Example LXVI  
     Preparation of 3-(4-methoxyphenyl)-5-(morpholinocarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0173]    Prepared in a similar fashion as described for example XLII using N-aminomorpholine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 22 H 22 N 5 O 4 : 420.1671, found: 420.1655.  
       Example LXVII  
     Preparation of 3-(4-methoxyphenyl)-5-(cis-2-aminocyclohexanylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0174]    Prepared in a similar fashion as described for example XLII using cis-1,2-diaminocyclohexane as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 24 H 26 N 5 O 3 : 432.2035, found: 432.2020.  
       Example LXVIII  
     Preparation of 3-(4-methoxyphenyl)-5-(4-methylpiperazinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0175]    Prepared in a similar fashion as described for example XLII using (4-amino)methylpiperazine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 23 H 25 N 6 O 3 : 433.1987, found: 433.1999.  
       Example LXIX  
     Preparation of 3-(4-methoxyphenyl)-5-(4-uridomethylpiperadinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0176]    Prepared in a similar fashion as described for example XXIII using example XXX as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 26 H 29 N 6 O 4 : 489.2250, found: 489.2209.  
       Example LXX  
     Preparation of 3-(4-methoxyphenyl)-5-(4-(2-pyridyl)piperazinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0177]    Prepared in a similar fashion as described for example XXIII using 4-(2-pyridyl)piperazine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 28 H 27 N 6 O 3 : 495.2144, found: 495.2111.  
       Example LXXI  
     Preparation of 3-(4-methoxyphenyl)-5-(4-(aminoethyl)piperazinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0178]    Prepared in a similar fashion as described for example XXIII using 4-(aminoethyl)piperazine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 25 H 29 N 6 O 3 : 461.2300, found: 461.2333.  
       Example LXXII  
     Preparation of 3-(4-methoxyphenyl)-5-(4-amidopiperadinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0179]    Prepared in a similar fashion as described for example XXIII using isonipecotamide as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 25 H 26 N 5 O 4 : 460.1984, found: 460.1998.  
       Example LXXIII  
     Preparation of 3-(4-methoxyphenyl)-5-(4-hydroxypiperadinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0180]    Prepared in a similar fashion as described for example XXIII using 4-hydroxypiperadine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 24 H 25 N 4 O 4 : 433.1875, found: 433.1844.  
       Example LXXIV  
     Preparation of 3-(4-methoxyphenyl)-5-(4-hydroxmethylypiperadinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0181]    Prepared in a similar fashion as described for example XXIII using 4-hydroxmethylypiperadine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 25 H 27 N 4 O 4 : 447.2032, found:447.2002.  
       Example LXXV  
     Preparation of 3-(4-methoxyphenyl)-5-(4-amidopiperazinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0182]    Prepared in a similar fashion as described for example XXIII using 4-amidopiperazine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 24 H 25 N 6 O 6 : 493.1835, found:493.1802.  
       Example LXXVI  
     Preparation of 3-(4-methoxyphenyl)-5-(4-dimethylaminopiperadinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0183]    Prepared in a similar fashion as described for example XXIII using 4-dimethylaminopiperadine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 26 H 30 N 5 O 5 : 492.2246, found:492.2220.  
       Example LXXVII  
     Preparation of 3-(4-methoxyphenyl)-5-(4-aminopiperadinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0184]    Prepared in a similar fashion as described for example XXIII using 4-aminopiperadine as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 24 H 26 N 5 O 5 : 464.1933, found:464.1975.  
       Example LXXVIII  
     Preparation of 3-(4-(dimethylamino)phenyl)-5-((4-methyl-1-piperazinyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0185]    Prepared in a similar fashion as described for examples II and XXIII employing the product of example LIV and 1-methylpiperazine as the starting materials. mp &gt;300° C.; ESI-MS m/e calc&#39;d for C 25 H 29 N 6 O 2 : 445.2352, found: 445.2359.  
       Example LXXIX  
     Preparation of 3-(4-(dimethylamino)phenyl)-5-((4-amino methyl-1-piperidinyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0186]    Prepared in a similar fashion as described for examples II and XXIII employing the product of example LIV and 4-(aminomethyl)piperidine as the starting materials. ESI-MS m/e calc&#39;d for C 26 H 31 N 6 O 2 : 459.2508, found: 459.2508.  
       Example LXXX  
     Preparation of 3-(4-(dimethylamino)phenyl)-5-((4-hydroxy-1-piperidinyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0187]    Prepared in a similar fashion as described for examples II and XXIII employing the product of example LIV and 4-hydroxypiperidine as the starting materials. mp 267° C.; ESI-MS m/e calc&#39;d for C 25 H 28 N 5 O 3 : 446.2192, found: 446.2206.  
       Example LXXXI  
     Preparation of 3-(4-(4-morpholinyl)phenyl)-5-(4-morpholinyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0188]    Prepared in a similar fashion as described for examples II and XXIII employing the product of example LVIII and morpholine as the starting materials. mp 258° C.; ESI-MS m/e calc&#39;d for C 26 H 28 N 5 O 4 : 474.2141, found: 474.2151.  
       Example LXXXII  
     Preparation of 3-(4-(4-morpholinyl)phenyl)-5-((4-methyl-1-piperazinyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0189]    Prepared in a similar fashion as described for examples II and XXIII employing the product of example LVIII and 1-methylpiperazine as the starting materials. mp 258° C.; ESI-MS m/e calc&#39;d for C 27 H 31 N 6 O 3 : 487.2457, found: 487.2447.  
       Example LXXXIII  
     Preparation of 3-(4-(4-morpholinyl)phenyl)-5-((4-hydroxy-1-piperidinyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0190]    Prepared in a similar fashion as described for examples II and XXIII employing the product of example LVIII and 4-hydroxypiperidine as the starting materials. mp 245° C.; ESI-MS m/e calc&#39;d for C 27 H 30 N 5 O 4 : 488.2298, found: 488.2290.  
       Example LXXXIV  
     Preparation of 3-(4-(4-morpholinyl)phenyl)-5-((4-amino methyl-1-piperidinyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0191]    Prepared in a similar fashion as described for examples II and XXIII employing the product of example LVIII and 4-(aminomethyl)piperidine as the starting materials. mp 240° C.; ESI-MS m/e calc&#39;d for C 28 H 33 N 6 O 3 : 501.2614, found: 501.2619.  
       Example LXXXV  
     Preparation of 3-(4-(dimethylamino)phenyl)-5-((((4-methyl-1-piperazinyl)amino)carbonyl)amino)indeno[1,2-c]pyrazol-4-one  
       [0192]    Prepared in a similar fashion as described for examples I, XXVII, and XLII employing the 4-(dimethylamino) acetophenone and 1-amino-4-methylpiperazine as the starting materials. mp &gt;300° C.; ESI-MS m/e calc&#39;d for C 24 H 28 N 7 O 2 : 446.2304, found: 446.2310.  
       Example LXXXVI  
     Preparation of 3-(i-propyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0193]    [0193]                           
         [0194]    Step 1. Synthesis of 26 from 3-nitrophthalic anhydride.  
         [0195]    A solution of 3-nitrophthalic anhydride (9.7 g, 50 mmol) and 1,1,1-trifluoro-5-methyl-2,4-hexanedione (9.1 g, 50 mmol) in acetic anhydride (28.3 mL, 300 mmol) was treated with triethylamine (13.95 mL, 100 mmol) and stirred at 25° C. for 4 h. The solution was diluted with 1 N HCl (200 mL) and the precipate collected and washed with water (200 mL) and hexane (400 mL) to give the product as a yellow solid (11.1 g, 85%). mp 127-129° C.; CIMS (M+H) calc&#39;d for C 13 H 12 NO 5 : 262.0715, found: 262.0694.  
         [0196]    Step 2. Synthesis of triketone 27 from 26.  
         [0197]    A solution of 26 (11 g, 42 mmol) in EtOH (224 mL) and water (56 mL) was treated with zinc (90 g, 1.4 mol) and calcium chloride (3 g, 27 mmol) and heated to reflux for 16 h. The reaction was filtered (Celite) and the filtrate was concentrated at reduced pressure to give an aqueous residue which was extracted with EtOAc (100 mL). The organic layer was separated and washed with sat. EDTA (100 ml) and brine (100 mL), dried (MgSO 4 ), filtered, and concentrated at reduced pressure to give a yellow solid. Trituration with hexane gave the product as a yellow solid (7.1 g, 73%). mp 241-243° C.; CIMS (M+H) calc&#39;d for C 13 H 14 NO 3 : 232.0974, found: 232.0962.  
         [0198]    Step 3. Synthesis of 28 from 27.  
         [0199]    A solution of 27 (500 mg, 2.16 mmol) in CH2Cl2 (5 mL) was treated with Et3N (0.36 mL, 2.59 mmol) and stirred at 25° C. for 15 min. The reaction mixture was treated with acetyl chloride (0.18 mL, 2.38 mmol) and stirred at 25° C. for 1 h. The reaction mixture was quenched with 1 N HCl (20 mL) and extracted with EtOAc (20 mL). The organic layer was separated, dried (MgSO4), filtered, and concentrated at reduced pressure to give a brown residue. Trituration with hexane gave the product as a tan solid (484 mg, 82%). mp 241-243° C.; CIMS (M+H) calc&#39;d for C 15 H 16 NO 4 : 274.1079, found: 274.1093.  
         [0200]    Step 4. Synthesis of 29 from 28.  
         [0201]    A solution of 28 (240 mg, 0.88 mmol) in BuOH (5 mL) was treated with hydrazine hydrate (0.055 mL, 1.76 mmol) and p-TsOH (8.4 mg, 0.044 mmol). The reaction was heated to reflux and stirred for 4 h. The reaction was cooled to 25° C. and the solvent removed at reduced pressure. Recrystalization with i-propyl alcohol gave the product collected as an off-white solid (173 mg, 73%). mp &gt;250° C.; ESIMS (M+H) calc&#39;d for C 15 H 16 N 3 O 2 : 270.1242, found: 270.1258.  
       Example LXXXVII  
     Preparation of 3-(c-propyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0202]    Prepared in a similar fashion as described for example LXXXVI using the c-propyl analog of 26 as the starting material. mp 220-221° C.; CIMS (M+H) calc&#39;d for C 15 H 14 N 3 O 2 : 268.1086, found: 268.1078.  
       Example LXXXVIII  
     Preparation of 3-(t-butyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0203]    Prepared in a similar fashion as described for example LXXXVI using the t-butyl analog of 26 as the starting material. mp &gt;250° C.; CIMS (M+H) calc&#39;d for C 16 H 18 N 3 O 2 : 284.1399, found: 284.1395.  
       Example LXXXIX  
     Preparation of 3-(2-thienyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0204]    Prepared in a similar fashion as described for example LXXXVI using the 2-thienyl analog of 26 as the starting material. mp 269° C.; CIMS (M+H) calc&#39;d for C 16 H 12 N 3 O 2 S: 310.0650, found: 310.0635.  
       Example XC  
     Preparation of 3-(3-methyl-2-thienyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0205]    Prepared in a similar fashion as described for example LXXXVI using the 3-methyl-2-thienyl analog of 26 as the starting material. mp 275° C.; ESIMS (M+H) calc&#39;d for C 17 H 14 N 3 O 2 S: 324.0811, found: 324.0807.  
       Example XCI  
     Preparation of 3-(ethyl)-5-(carbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0206]    Prepared in a similar fashion as described for example LXXXVI using ammonia and the ethyl analog of 15 as the starting materials. mp &gt;250° C.; CIMS (M+H) calc&#39;d for C 13 H 13 N 4 O 2 : 257.1039, found: 257.1033.  
       Example XCII  
     Preparation of 3-(n-propyl)-5-(carbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0207]    Prepared in a similar fashion as described for example LXXXVI using ammonia and the n-propyl analog of 15 as the starting materials. mp 187-189° C.; CIMS (M+H) calc&#39;d for C 14 H 15 N 4 O 2 : 271.1195, found: 271.1187.  
       Example XCIII  
     Preparation of 3-(i-propyl)-5-(carbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0208]    Prepared in a similar fashion as described for example LXXXVI using ammonia and the i-propyl analog of 15 as the starting materials. mp &gt;250° C.; CIMS (M+H) calc&#39;d for C 14 H 15 N 4 O 2 : 271.1195, found: 271.1196.  
       Example XCIV  
     Preparation of 3-(c-propyl)-5-(carbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0209]    Prepared in a similar fashion as described for example LXXXVI using ammonia and the c-propyl analog of 15 as the starting materials. mp 252-253° C.; ESIMS (M-H) calc&#39;d for C 14 H 11 N 4 O 2 : 267.0881, found: 267.0884.  
       Example XCV  
     Preparation of 3-(c-hexyl)-5-(carbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0210]    Prepared in a similar fashion as described for example LXXXVI using ammonia and the c-hexyl analog of 15 as the starting materials. mp 178-179° C.; ESIMS (M+H) calc&#39;d for C 17 H 19 N 4 O 2 : 311.1507, found: 311.1500.  
       Example XCVI  
     Preparation of 3-(2-thienyl)-5-(carbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0211]    Prepared in a similar fashion as described for example LXXXVI using ammonia and the 2-thienyl analog of 15 as the starting materials. mp 214° C.; CIMS m+ calc&#39;d for C 15 H 10 N 4 O 2 S: 310.0517, found: 310.0524.  
       Example XCVII  
     Preparation of 3-(3-methyl-2-thienyl)-5-(carbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0212]    Prepared in a similar fashion as described for example LXXXVI using ammonia and the 3-methyl-2-thienyl analog of 15 as the starting materials. mp 270° C.; ESIMS (M+H) calc&#39;d for C 16 H 13 N 4 O 2 S: 325.0759, found: 325.0744.  
       Example XCVIII  
     Preparation of 3-(5-methyl-2-thienyl)-5-(carbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0213]    Prepared in a similar fashion as described for example LXXXVI using ammonia and the 5-methyl-2-thienyl analog of 15 as the starting materials. mp &gt;280° C.; ESIMS (M+H) calc&#39;d for C 16 H 13 N 4 O 2 S: 325.0759, found: 325.0761.  
       Example XCIX  
     Preparation of 3-(5-ethylcarboxyl-2-thienyl)-5-(carbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0214]    Prepared in a similar fashion as described for example LXXXVI using ammonia and the 5-ethylcarboxyl-2-thienyl analog of 15 as the starting materials. mp &gt;280° C.; ESIMS (M+H) calc&#39;d for C 18 H 15 N 4 O 4 S: 383.0813, found: 383.0788.  
       Example C  
     Preparation of 3-(3-thienyl)-5-(carbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0215]    Prepared in a similar fashion as described for example LXXXVI using ammonia and the 3-thienyl analog of 15 as the starting materials. mp &gt;280° C.; ESIMS (M+H) calc&#39;d for C 15 H 11 N 4 O 2 S: 311.0603, found: 311.0594.  
       Example CI  
     Preparation of 3-(5-chloro-3-thienyl)-5-(carbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0216]    Prepared in a similar fashion as described for example LXXXVI using ammonia and the 5-chloro-3-thienyl analog of 15 as the starting materials. mp &gt;300° C.; ESIMS (M+H) calc&#39;d for C 15 H 10 N 4 O 2 SCl: 345.0209, found: 345.0213.  
       Example CII  
     Preparation of 3-(2,5-dimethyl-3-thienyl)-5-(carbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0217]    Prepared in a similar fashion as described for example LXXXVI using ammonia and the 2,5-dimethyl-3-thienyl analog of 15 as the starting materials. mp &gt;280° C.; ESIMS (M+H) calc&#39;d for C 17 H 15 N 4 O 2 S: 339.0916, found: 339.0905.  
       Example CIII  
     Preparation of 3-(2-furanyl)-5-(carbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0218]    Prepared in a similar fashion as described for example LXXXVI using ammonia and the 2-furanyl analog of 15 as the starting materials. mp 278° C.; ESIMS (M+H) calc&#39;d for C 15 H 11 N 4 O 3 : 295.0831, found: 295.0838.  
       Example CIV  
     Preparation of 3-(i-propyl)-5-(N,N-dimethylaminocarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0219]    Prepared in a similar fashion as described for example LXXXVI using 1,1-dimethylhydrazine and the i-propyl analog of 15 as the starting materials. mp 231-233° C.; ESIMS (M+H) calc&#39;d for C 16 H 20 N 5 O 2 : 314.1616, found: 314.1599.  
       Example CV  
     Preparation of 3-(c-propyl)-5-(N,N-dimethylaminocarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0220]    Prepared in a similar fashion as described for example LXXXVI using 1,1-dimethylhydrazine and the c-propyl analog of 15 as the starting materials. mp XXX ° C.; ESIMS (M+H) calc&#39;d for C 16 H 18 N 5 O 2 : 312.1460, found: 312.1487.  
       Example CVI  
     Preparation of 3-(c-hexyl)-5-(N,N-dimethylaminocarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0221]    Prepared in a similar fashion as described for example LXXXVI using 1,1-dimethylhydrazine and the c-hexyl analog of 15 as the starting materials. mp 229-231° C.; ESIMS (M+H) calc&#39;d for C 19 H 24 N 5 O 2 : 354.1929, found: 354.1932.  
       Example CVII  
     Preparation of 3-(2-thienyl)-5-(N,N-dimethylaminocarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0222]    Prepared in a similar fashion as described for example LXXXVI using 1,1-dimethylhydrazine and the 2-thienyl analog of 15 as the starting materials. mp 279° C.; ESIMS (M+H) calc&#39;d for C 17 H 16 N 5 O 2 S: 354.1024, found: 354.1025.  
       Example CVIII  
     Preparation of 3-(5-methoxy-2-thienyl)-5-(N,N-dimethylaminocarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0223]    Prepared in a similar fashion as described for example LXXXVI using 1,l-dimethylhydrazine and the 5-methoxy-2-thienyl analog of 15 as the starting materials. mp 280° C.; ESIMS (M+H) calc&#39;d for C 18 H 18 N 5 O 3 S: 384.1130, found: 384.1119.  
       Example CIX  
     Preparation of 3-(5-methyl-2-thienyl)-5-(N,N-dimethylaminocarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0224]    Prepared in a similar fashion as described for example LXXXVI using 1,1-dimethylhydrazine and the 5-methyl-2-thienyl analog of 15 as the starting materials. mp &gt;280° C.; ESIMS (M+H) calc&#39;d for C 18 H 18 N 5 O 2 S: 368.1181, found: 368.1171.  
       Example CX  
     Preparation of 3-(5-ethylcarboxyl-2-thienyl)-5-(N,N-dimethylaminocarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0225]    Prepared in a similar fashion as described for example LXXXVI using 11-dimethylhydrazine and the 5-ethylcarboxyl-2-thienyl analog of 15 as the starting materials. mp 252° C.; ESIMS (M+H) calc&#39;d for C 20 H 20 N 5 O 4 S: 426.1236, found: 426.1251.  
       Example CXI  
     Preparation of 3-(3-thienyl)-5-(N,N-dimethylaminocarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0226]    Prepared in a similar fashion as described for example LXXXVI using 1,1-dimethylhydrazine and the 3-thienyl analog of 15 as the starting materials. mp 202° C.; ESIMS (M+H) calc&#39;d for C 17 H 16 N 5 O 2 S: 354.1025, found: 354.1031.  
       Example CXII  
     Preparation of 3-(1-methyl-3-pyrrolyl)-5-(carbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0227]    Prepared in a similar fashion as described for example LXXXVI using ammonia and the 1-methyl-3-pyrrolyl analog of 15 as the starting materials. mp &gt;300° C.; ESIMS (M+H) calc&#39;d for C 16 H 14 N 5 O 2 : 308.1147, found: 308.1166.  
       Example CXIII  
     Preparation of 3-(2,5-dimethyl-3-thienyl)-5-(N,N-dimethylaminocarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0228]    Prepared in a similar fashion as described for example LXXXVI using 1,1-dimethylhydrazine and the 2,5-dimethyl-3-thienyl analog of 15 as the starting materials. mp 252° C.; ESIMS (M+H) calc&#39;d for C 19 H 20 N 5 O 2 S: 382.1338, found: 382.1357.  
       Example CXIV  
     Preparation of 3-(2-furanyl)-5-(N,N-dimethylaminocarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0229]    Prepared in a similar fashion as described for example LXXXVI using 1,1-dimethylhydrazine and the 2-furanyl analog of 15 as the starting materials. mp 202° C.; ESIMS (M+H) calc&#39;d for C 17 H 16 N 5 O 3 : 338.1253, found: 338.1248.  
       Example CXV  
     Preparation of 3-(i-propyl)-5-(4-carbamoylpiperidinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0230]    Prepared in a similar fashion as described for example XXIII using isonipecotamide and the i-propyl analog of 14 as the starting materials. mp 224-225° C.; ESIMS (M+H) calc&#39;d for C 21 H 26 N 5 O 3 : 396.2035, found: 396.2036.  
       Example CXVI  
     Preparation of 3-(c-hexyl)-5-(4-carbamoylpiperidinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0231]    Prepared in a similar fashion as described for example XXIII using isonipecotamide and the c-hexyl analog of 14 as the starting materials. mp 228-229° C.; ESIMS (M+H) calc&#39;d for C 24 H 30 N 5 O 3 : 436.2348, found: 436.2345.  
       Example CXVII  
     Preparation of 3-(ethyl)-5-(4-aminomethylpiperidinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0232]    Prepared in a similar fashion as described for example XXIII using 4-(aminomethyl)piperidine and the ethyl analog of 14 as the starting materials. mp 174-176° C.; ESIMS (M+H) calc&#39;d for C 20 H 26 N 5 O 2 : 368.2086, found: 368.2078.  
       Example CXVIII  
     Preparation of 3-(i-propyl)-5-(4-aminomethylpiperidinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0233]    Prepared in a similar fashion as described for example XXIII using 4-(aminomethyl)piperidine and the i-propyl analog of 14 as the starting materials. mp 218-220° C.; ESIMS (M+H) calc&#39;d for C 21 H 28 N 5 O 2 : 382.2242, found: 382.2227.  
       Example CXIX  
     Preparation of 3-(c-propyl)-5-(4-aminomethylpiperidinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0234]    Prepared in a similar fashion as described for example XXIII using 4-(aminomethyl)piperidine and the c-propyl analog of 14 as the starting materials. mp 138-140° C.; ESIMS (M+H) calc&#39;d for C 21 H 26 N 5 O 2 : 380.2086, found: 380.2079.  
       Example CXX  
     Preparation of 3-(c-hexyl)-5-(4-aminomethylpiperidinylacetamido)indeno[1,2-c]pyrazol-4-one  
       [0235]    Prepared in a similar fashion as described for example XXIII using 4-(aminomethyl)piperidine and the c-hexyl analog of 14 as the starting materials. mp 196-198° C.; ESIMS (M+H) calc&#39;d for C 24 H 32 N 5 O 2 : 422.2555, found: 422.2540.  
       Example CXXI  
     Preparation of 3-(i-propyl)-5-(4-methylpiperazinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0236]    Prepared in a similar fashion as described for example LXXXVI using 1-amino-4-methylpiperazine and the i-propyl analog of 15 as the starting materials. mp 231-233° C.; ESIMS (M+H) calc&#39;d for C 19 H 25 N 6 O 2 : 369.2038, found: 369.2039.  
       Example CXXII  
     Preparation of 3-(5-ethylcarboxyl-2-thienyl)-5-(4-methylpiperazinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0237]    Prepared in a similar fashion as described for example LXXXVI using 1-amino-4-methylpiperazine and the 5-ethylcarboxyl-2-thienyl analog of 15 as the starting materials. mp 249° C.; ESIMS (M+H) calc&#39;d for C 23 H 25 N 6 O 4 S: 481.1657, found: 481.1642.  
       Example CXXIII  
     Preparation of 3-(5-carboxyl-2-thienyl)-5-(4-methylpiperazinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0238]    A solution of CXXII (30 mg, 0.05 mmol) in 3:1 THF/water (2 mL) was treated with LiOH (23 mg, 0.5 mmol) and the reaction was stirred at 25° C. for 12 h and then heated to reflux for 1 h. The organic solvent was removed at reduced pressure and the residue was partioned between EtOAc (5 mL) and water (5 mL). The organic layer was separated and the aqueous phase was adjusted to pH=2 with 1 M HCl and re-extracted with EtOAc (5 mL). The combined organic layers were dried (Na2SO4), filtered and concentrated at reduced pressure to give a crude residue. Purification by reverse phase HPLC gave the product as a yellow solid (10.4 mg, 46%). mp 270° C.; ESIMS (M+H) calc&#39;d for C 21 H 21 N 6 O 4 S: 453.1344, found: 453.1353.  
       Example CXXIV  
     Preparation of 3-(2,5-dimethyl-3-thienyl)-5-(4-methylpiperazinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0239]    Prepared in a similar fashion as described for example LXXXVI using 1-amino-4-methylpiperazine and the 2,5-dimethyl-3-thienyl analog of 15 as the starting materials. mp 250° C.; ESIMS (M+H) calc&#39;d for C 22 H 25 N 6 O 2 S: 437.1760, found: 437.1771.  
       Example CXXV  
     Preparation of 3-(i-propyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0240]    Prepared in a similar fashion as described for example LXXXVI using 4-aminomorpholine and the i-propyl analog of 15 as the starting materials. mp 256-258° C.; ESIMS (M−H) calc&#39;d for C 18 H 20 N 5 O 3 : 354.1566, found: 354.1543.  
       Example CXXVI  
     Preparation of 3-(N-methylcarbamoyl-4-piperidinyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0241]    Prepared in a similar fashion as described for example LXXXVI using 4-aminomorpholine and the N-methylcarbamoyl-4-piperidinyl analog of 15 as the starting materials. mp 216-218° C.; ESIMS (M+H) calc&#39;d for C 22 H 27 N 6 O 5 : 455.2042, found: 455.2036.  
       Example CXXVII  
     Preparation of 3-(5-methyl-2-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0242]    Prepared in a similar fashion as described for example LXXXVI using 4-aminomorpholine and the 5-methyl-2-thienyl analog of 15 as the starting materials. mp 261° C.; ESIMS (M+H) calc&#39;d for C 20 H 20 N 5 O 3 S: 410.1287, found: 410.1308.  
       Example CXXVIII  
     Preparation of 3-(5-chloro-3-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0243]    Prepared in a similar fashion as described for example LXXXVI using 4-aminomorpholine and the 5-chloro-3-thienyl analog of 15 as the starting materials. mp 259° C.; ESIMS (M+H) calc&#39;d for C 19 H 17 N 5 O 3 SCl: 430.0741, found: 430.0757.  
       Example CXXIX  
     Preparation of 3-(2,5-dimethyl-3-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0244]    Prepared in a similar fashion as described for example LXXXVI using 4-aminomorpholine and the 2,5-dimethyl-3-thienyl analog of 15 as the starting materials. mp &gt;280° C.; ESIMS (M+H) calc&#39;d for C 21 H 22 N 5 O 3 S: 424.1443, found: 424.1431.  
       Example CXXX  
     Preparation of 3-(5-ethylcarboxyl-2-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0245]    Prepared in a similar fashion as described for example LXXXVI using 4-aminomorpholine and the 5-ethylcarboxyl-2-thienyl analog of 15 as the starting materials. mp 258° C.; ESIMS (M+H) calc&#39;d for C 22 H 22 N 5 O 5 S: 468.1341, found: 468.1331.  
       Example CXXXI  
     Preparation of 3-(5-carboxyl-2-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0246]    Prepared in a similar fashion as described for example LXXXVI (HYDROLYSIS OF PREVIOUS ESTER). mp 273° C.; ESIMS (M+H) calc&#39;d for C 20 H 18 N 5 O 5 S: 440.1028, found: 440.1026.  
       Example CXXXII  
     Preparation of 3-(5-benzylcarboxamido-2-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0247]    A solution of benzylamine (0.01 mL, 0.09 mmol) in DMF (1 mL) was treated with acid CXXXI (40 mg, 0.09 mmol) and stirred at 25° C.. The reaction was treated with TBTU (29 mg, 0.09 mmol) and stirred at 25° C. for 30 min. Triethylamine (0.01 mL, 0.09 mmol) was added and the reaction stirred at 25° C. for 12 h. After adding more TBTU (15 mg, 0.045 mmol) and triethylamine (0.01 mL, 0.09 mmol) the reaction was stirred at 25° C. for an additional 4 h. The reaction was diluted with EtOAc (10 mL) and water (10 mL) and the aqueous layer was extracted with EtOAc (5×10 mL). The combined organic layers were dried (Na2SO4), filtered, and the solvent removed at reduced pressure. Purification of the residue using reverse phase HPLC gave the product as a yellow solid (21 mg, 42%). mp 275° C.; ESIMS (M+H) calc&#39;d for C 27 H 25 N 5 O 4 S: 529.1659, found: 529.1682.  
       Example CXXXIII  
     Preparation of 3-(5-(4-methylpiperazinyl)carboxamido-2-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0248]    Prepared in a similar fashion as described for example CXXXII using 1-amino-4-methylpiperazine as the starting material. mp 190° C.; ESIMS (M+H) calc&#39;d for C 25 H 29 N 8 O 4 S: 537.2032, found: 537.2055.  
       Example CXXXIV  
     Preparation of 3-(5-(2-(1-methylpyrrolidinyl)ethyl)carboxamido-2-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0249]    Prepared in a similar fashion as described for example CXXXII using 2-(2-aminoethyl)-1-methylpyrrolidine as the starting material. mp 235° C.; ESIMS (M+H) calc&#39;d for C 27 H 32 N 7 O 4 S: 550.2236, found: 550.2229.  
       Example CXXXV  
     Preparation of 3-(5-(N,N-dimethylamino)carboxamido-2-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0250]    Prepared in a similar fashion as described for example CXXXII using 1,1-dimethylhydrazine as the starting material. mp 201° C.; ESIMS (M+H) calc&#39;d for C 22 H 24 N 7 O 4 S: 482.1610, found: 482.1588.  
       Example CXXXVI  
     Preparation of 3-(5-(2-(N,N-dimethylamino)ethyl)carboxamido-2-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0251]    Prepared in a similar fashion as described for example CXXXII using N,N-dimethylethylenediamine as the starting material. mp 190° C.; ESIMS (M+H) calc&#39;d for C 24 H 28 N 7 O 4 S: 510.1923, found: 510.1922.  
       Example CXXXVII  
     Preparation of 3-(5-(2-(pyrrolidinyl)ethyl)carboxamido-2-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0252]    Prepared in a similar fashion as described for example CXXXII using 1-(2-aminoethyl)pyrrolidine as the starting material. mp 224° C.; ESIMS (M+H) calc&#39;d for C 26 H 30 N 7 O 4 S: 536.2080, found: 536.2091.  
       Example CXXXVIII  
     Preparation of 3-(5-(2-(morpholinyl)ethyl)carboxamido-2-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0253]    Prepared in a similar fashion as described for example CXXXII using 4-(2-aminoethyl)morpholine as the starting material. mp 241° C.; ESIMS (M+H) calc&#39;d for C 26 H 30 N 7 O 5 S: 552.2029, found: 552.2043.  
       Example CXXXIX  
     Preparation of 3-(5-morpholinylcarboxamido-2-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0254]    Prepared in a similar fashion as described for example CXXXII using 4-aminomorpholine as the starting material. mp 271° C.; ESIMS (M+H) calc&#39;d for C 24 H 26 N 7 O 5 S: 524.1716, found: 524.1719.  
       Example CXL  
     Preparation of 3-(5-(3-(pyrrolidonyl)propyl)carboxamido-2-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0255]    Prepared in a similar fashion as described for example CXXXII using 1-(3-aminopropyl)-2-pyrrolidinone as the starting material. mp 260° C.; ESIMS (M+H) calc&#39;d for C 27 H 30 N 7 O 5 S: 564.2029, found: 564.2031.  
       Example CXLI  
     Preparation of 3-(5-(2-(3-pyridyl)ethyl)carboxamido-2-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0256]    Prepared in a similar fashion as described for example CXXXII using 3-(2-aminoethyl)pyridine as the starting material. mp 203° C.; ESIMS (M+H) calc&#39;d for C 27 H 26 N 7 O 4 S: 544.1766, found: 544.1760.  
       Example CXLII  
     Preparation of 3-(5-(3-(imidazolyl)propyl)carboxamido-2-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0257]    Prepared in a similar fashion as described for example CXXXII using 1-(3-aminopropyl)imidazole as the starting material. mp 263° C.; ESIMS (M+H) calc&#39;d for C 26 H 27 N 8 O 4 S: 547.1875, found: 547.1872.  
       Example CXLIII  
     Preparation of 3-(5-(2-(2-pyridyl)ethyl)carboxamido-2-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0258]    Prepared in a similar fashion as described for example CXXXII using 2-(2-aminoethyl)pyridine as the starting material. mp &gt;280° C.; ESIMS (M+H) calc&#39;d for C 27 H 26 N 7 O 4 S: 544.1767, found: 544.1778.  
       Example CXLIV  
     Preparation of 3-(5-((2-pyridyl)methyl)carboxamido-2-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0259]    Prepared in a similar fashion as described for example CXXXII using 2-(aminomethyl)pyridine as the starting material. mp 239° C.; ESIMS (M+H) calc&#39;d for C 26 H 24 N 7 O 4 S: 530.1610, found: 530.1603.  
       Example CXLV  
     Preparation of 3-(5-(2-(piperidinyl)ethyl)carboxamido-2-thienyl)-5-(morpholinylcarbamoyl)aminoindeno[1,2-c]pyrazol-4-one  
       [0260]    Prepared in a similar fashion as described for example CXXXII using 1-(2-aminoethyl)piperidine as the starting material. mp 228° C.; ESIMS (M+H) calc&#39;d for C 27 H 32 N 7 O 4 S: 550.2236, found: 550.2236.  
       Example CXLVI  
     Preparation of 3-(4-(trifluoromethyl)phenyl)-5-(acetamido)indeno[1,2-c]pyrazol-4-one  
       [0261]    Prepared in a similar fashion as described for example LXXXVI employing 1-(4-(trifluoromethyl)phenyl)-4,4,4-trifluoro-1,3-butanedione as the starting material. mp &gt;300° C.; ESI − -MS m/e calc&#39;d for C 19 H 11 N 3 O 2 : 370.0804, found: 370.0809.  
       Example CXLVII  
     Preparation of 3-(4-(4-t-butoxycarbonyl-1-piperazinyl)phenyl)-5-(((4-morpholinylamino)carbonyl)amino)indeno[1,2-c]pyrazol-4-one  
       [0262]    [0262]                           
         [0263]    Step 1. Synthesis of 30.  
         [0264]    A solution of 4-piperazinoacetophenone (24.8 g, 121 mmol) and di-tert-butyl dicarbonate (27.8 g, 128 mmol) in 480 mL of tetrahydrofuran was refluxed for 16 h. After cooling to room temperature the solution was concentrated under vacuum. The resulting solids were washed with hexane and dried under vacuum to afford 29.4 g (80%) of the product as an off-white solid. NMR (CDCl 3 ) δ7.89 (d, 2 H, J=9 Hz), 6.87 (d, 2 H, J=9 Hz), 3.59 (m, 4 H), 3.33 (m, 4 H), 2.53 (s, 3 H), 1.49 (s, 9 H).  
         [0265]    Step 2. Synthesis of 31 from 30.  
         [0266]    To a solution of 30 (11.35 g, 37 mmol) and ethyl trifluoroacetate (5.40 mL, 45 mmol) in 50 mL of tetrahydrofuran at 25° C. was added dropwise over 15 min. 21% sodium ethoxide in ethanol (16.8 mL, 45 mmol), and the resulting solution then was stirred at 25° C. for 14 h. The reaction mixture was diluted with water, adjusted to pH 5 with conc. hydrochloric acid, and extracted with ethyl acetate. The combined extracts was washed with water and brine, dried over anhydrous sodium sulfate, filtered, and concentrated under vacuum. The resulting solid was washed with diethyl ether and dried to furnish 12.1 g (81%) of the product as an orange solid. NMR (CDCl 3 ) δ7.87 (d, 2 H, J=9 Hz), 6.87 (d, 2 H, J=9 Hz), 6.45 (s, 1 H), 3.60 (m, 4 H), 3.41 (m, 4 H), 1.48 (s, 9 H).  
         [0267]    Step 3. Synthesis of CXLVII from 31.  
         [0268]    Prepared in a similar fashion as described for examples LXXVI and XLII employing 31 and 4-aminomorpholine as starting materials. mp 242° C.; ESI-MS m/e calc&#39;d for C 30 H 36 N 7 O 5 574.2778, found: 574.2762.  
       Example CXLVIII  
     Preparation of 3-(4-(1-piperazinyl)phenyl)-5-(((4-morpholinylamino)carbonyl)amino)indeno[1,2-c]pyrazol-4-one  
       [0269]    A solution of CXLVII (0.58 g, 1.0 mmol) in 20 mL of trifluoroacetic acid was stirred at 25° C. for 2 h. The reaction mixture was concentrated under vacuum, and the residue was recrystallized from ethanol to provide 0.53 g (89%) of the yellow product as its TFA-salt. mp 263° C.; ESI-MS m/e calc&#39;d for C 25 H 28 N 7 O 3 : 474.2254, found: 474.2280.  
       Example CXLIX  
     Preparation of 3-(4-(1-piperazinyl)phenyl)-5-((aminocarbonyl)amino)indeno[1,2-c]pyrazol-4-one  
       [0270]    Prepared in a similar fashion as described for examples XLII and CXLVIII employing 2-(4-(4-t-butoxycarbonyl-1-piperazinyl)benzoyl)-4-amino-1,3-indanedione obtained in example CXLVII and ammonia as the starting materials. mp 257° C.; ESI-MS m/e calc&#39;d for C 21 H 21 N 6 O 2 : 389.1726, found: 389.1724.  
       Example CL  
     Preparation of 3-(4-(1-piperazinyl)phenyl)-5-((hydrazinocarbonyl)amino)indeno[1,2-c]pyrazol-4-one  
       [0271]    Prepared in a similar fashion as described for examples XLII and CXLVIII employing 2-(4-(4-t-butoxycarbonyl-1-piperazinyl)benzoyl)-4-amino-1,3-indanedione obtained in example CXLVII and hydrazine as the starting materials. mp 257° C.; ESI-MS m/e calc&#39;d for C 21 H 22 N 7 O 2 : 404.1835, found: 404.1834.  
       Example CLI  
     Preparation of 3-(4-(1-piperazinyl)phenyl)-5-((dimethylamino)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0272]    Prepared employing 2-(4-(4-t-butoxycarbonyl-1-piperazinyl)benzoyl)-4-amino-1,3-indanedione obtained in example CXLVII as the starting material. Chloroacetylation and treatment with dimethylamine in a similar fashion as described for examples II and XXIII, followed by treatment with hydrazine and removal of the t-butoxycarbonyl group in a similar fashion as described for examples I and CXLVIII, afforded the example compound. mp 243° C.; ESI-MS m/e calc&#39;d for C 24 H 27 N 6 O 2 : 431.2196, found: 431.2198.  
       Example CLII  
     Preparation of 3-(4-(1-piperazinyl)phenyl)-5-((4-morpholinyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0273]    Prepared employing 2-(4-(4-t-butoxycarbonyl-1-piperazinyl)benzoyl)-4-amino-1,3-indanedione obtained in example CXLVII as the starting material. Chloroacetylation and treatment with morpholine in a similar fashion as described for examples II and XXIII, followed by treatment with hydrazine and removal of the t-butoxycarbonyl group in a similar fashion as described for examples I and CXLVIII, afforded the example compound. mp 259° C.; ESI-MS m/e calc&#39;d for C 26 H 29 N 6 O 3 : 473.2301, found: 473.2302.  
       Example CLIII  
     Preparation of 3-(4-(1-piperazinyl)phenyl)-5-((4-methyl-1-piperazinyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0274]    Prepared employing 2-(4-(4-t-butoxycarbonyl-1-piperazinyl)benzoyl)-4-amino-1,3-indanedione obtained in example CXLVII as the starting material. Chloroacetylation and treatment with 1-methylpiperazine in a similar fashion as described for examples II and XXIII, followed by treatment with hydrazine and removal of the t-butoxycarbonyl group in a similar fashion as described for examples I and CXLVIII, afforded the example compound. ESI-MS m/e calc&#39;d for C 27 H 32 N 7 O 2 : 486.2618, found: 486.2608.  
       Example CLIV  
     Preparation of 3-(4-(1-piperazinyl)phenyl)-5-((4-amino methyl-1-piperidinyl)acetamido)indeno[1,2-c]pyrazol-4-one  
       [0275]    Prepared employing 2-(4-(4-t-butoxycarbonyl-1-piperazinyl)benzoyl)-4-amino-1,3-indanedione obtained in example CXLVII as the starting material. Chloroacetylation and treatment with 4-(aminomethyl)piperidine in a similar fashion as described for examples II and XXIII, followed by treatment with hydrazine and removal of the t-butoxycarbonyl group in a similar fashion as described for examples I and CXLVIII, afforded the example compound. mp 239° C.; ESI-MS m/e calc&#39;d for C 28 H 34 N 7 O 2 : 500.2774, found: 500.2772.  
       Example CLV  
     Preparation of 3-(4-(4-methyl-1-piperazinyl)phenyl)-5-(((4-morpholinylamino)carbonyl)amino)indeno[1,2-c]pyrazol-4-one  
       [0276]    [0276]                           
         [0277]    To a solution of CXLVIII (0.17 g, 0.29 mmol) in 10 mL of methanol and 2 mL of water at 25° C. was added sequentially 37% aqueous formaldehyde (0.45 g, 5.8 mmol), sodium cyanoborohydride (0.18 g, 2.9 mmol), and 4 drops of acetic acid. The resulting solution was stirred at 25° C. for 16 h. The mixture was diluted with water. It then was made acidic (˜pH 1) with conc. hydrochloric acid and stirred for 10 min. The solution next was made basic (˜pH 13) with 50% aqueous sodium hydroxide and finally adjusted to pH 10 with 1 N hydrochloric acid. The mixture was extracted with 4:1 chloroform/isopropanol. The combined extracts were washed with water and brine, dried over anhydrous sodium sulfate, and filtered. To the filtrate was added excess trifluoroacetic acid, and the solution was concentrated under vacuum. The residue was recrystallized from isopropanol to furnish 0.16 g (92%) of the yellow product as its TFA-salt. mp 245° C.; ESI-MS m/e calc&#39;d for C 26 H 30 N 7 O 3 : 488.2410, found: 488.2420.  
       Example CLVI  
     Preparation of 3-(4-(4-ethyl-1-piperazinyl)phenyl)-5-(((4-morpholinylamino)carbonyl)amino)indeno[1,2-c]pyrazol-4-one  
       [0278]    Prepared in a similar fashion as described for example CLV employing CXLVIII and acetaldehyde as the starting materials. mp 245° C.; ESI-MS m/e calc&#39;d for C 27 H 32 N 7 O 3 : 502.2567, found: 502.2555.  
       Example CLVII  
     Preparation of 3-(4-(4-isopropyl-1-piperazinyl)phenyl)-5-(((4-morpholinylamino)carbonyl)amino)indeno[1,2-c]pyrazol-4-one  
       [0279]    Prepared in a similar fashion as described for example CLV employing CXLVIII and acetone as the starting materials. mp 253° C.; ESI-MS m/e calc&#39;d for C 28 H 34 N 7 O 3 : 516.2723, found: 516.2726.  
       Example CLVIII  
     Preparation of 3-(4-methoxyphenyl)-5-(2-benzoylhydrazinecarboxamido)indeno[1,2-c]pyrazol-4-one  
       [0280]    Step 1. Synthesis of 31 from 13. 
                         
 
         [0281]    A suspension of aniline 31 (0.5 g, 1.7 mmol) in dioxane (10 mL) was treated with triethylamine (0.48 mL, 3.4 mmol) in one portion at room temperature. Then 2-(trimethylsilyl) ethyloxy chloride (SEMCl) (0.48 mL, 2.6 mmol) was added in one portion and the mixture heated to reflux for 2 h. The reaction was cooled, diluted with EtOAc (20 mL) washed with water (10 mL), dried (MgSO4) and the solvent removed at reduced pressure. The residue was taken up in benzene (3 mL), applied to a plug of silica gel (10 g) and eluted with EtOAc/Hexane (1:3) until all the yellow color was washed from the silica gel plug. The solvent was evaporated and the residue taken on to the next step. This material was dissolved in dioxane (10 mL) and treated with K2CO3 (0.36 g, 2.6 mmol) in one portion. Then phenylchloroformate (0.27 mL, 2.23 mmol) was added in one portion and the reaction heated to 50 C. for 2 h. The reaction was cooled and the solvent removed at reduced pressure. The residue was recrystalized from EtOH to give a yellow solid (0.4 g, 43%). mp ° C.; CIMS m/e calculated for C 30 H 32 N 3 O5Si: 542.2111, found: 542.2101;  
         [0282]    Step 2. Synthesis of Ex. CLVIII from 31.  
         [0283]    Compound 31 (0.015 g, 0.03 mmol) in DMSO (0.2 mL) was treated with phenylcarbazte (0.008 g, 0.06 mmol) in one portion and heated to 80 C. for 30 minutes. The solvent was removed at reduced pressure heating to 65 C. The residue was disolved in EtOH (0.5 mL) and treated with 4N HCl/dioxane (0.4 mL). The mixture was heated to 80 C. for 20 minutes and then cooled. The desired product was filtered and air dried (0.008g, 62%). mp &gt;300° C.; CIMS m/e calculated for C 26 H 27 N 4 O 4 : 459.2032, found: 459.1999;  
       Example CLIX  
     Preparation of 3-(4-methoxyphenyl)-5-(2-isonicotinoylhydrazinecarboxamido)indeno[1,2-c]pyrazol-4-one  
       [0284]    Prepared in a similar fashion as described for example CLVIII using 4-pyridylcarbazate as the starting material. mp 248° C.; CIMS m/e calculated for C 24 H 19 N 6 O 4 : 455.1468, found: 455.1400;  
       Example CLX  
     Preparation of 3-(4-methoxyphenyl)-5-(2-nictinoylhydrazinecarboxamido)indeno[1,2-c]pyrazol-4-one  
       [0285]    Prepared in a similar fashion as described for example CLVIII using 3-pyridylcarbazate as the starting material. mp 227° C.; CIMS m/e calc&#39;d for C 24 H 19 N 6 O 4 : 455.1468, found: 455.1487;  
       Example CLXI  
     Preparation of 3-(4-methoxyphenyl)-5-(2-(3,4-dihydroxy benzoyl)hydrazinecarboxamido)indeno[1,2-c]pyrazol-4-one  
       [0286]    Prepared in a similar fashion as described for example CLVIII using 3,4-dihydroxyphenyl carbazate as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 25 H 20 N 5 O 6 : 486.1414, found: 486.1497;  
       Example CLXII  
     Preparation of 3-(4-methoxyphenyl)-5-(2-(4-hydroxy benzoyl)hydrazinecarboxamido)indeno[1,2-c]pyrazol-4-one  
       [0287]    Prepared in a similar fashion as described for example CLVIII using 4-hydroxyphenyl carbazate as the starting material. mp 283° C.; CIMS m/e calc&#39;d for C 25 H 20 N 5 O 5 : 470.1464, found: 470.1544;  
       Example CLXIII  
     Preparation of 3-(4-methoxyphenyl)-5-(2-(3-aminobenzoyl)hydrazinecarboxamido)indeno[1,2-c]pyrazol-4-one  
       [0288]    Prepared in a similar fashion as described for example CLVIII using 3-aminophenyl carbazate as the starting material. mp 250° C.; CIMS m/e calc&#39;d for C 25 H 21 N 6 O 4 : 469.1624, found: 469.1513;  
       Example CLXIV  
     Preparation of 3-(4-methoxyphenyl)-5-(2-(4-aminobenzoyl)hydrazinecarboxamido)indeno[1,2-c]pyrazol-4-one  
       [0289]    Prepared in a similar fashion as described for example CLVIII using 4-aminophenyl carbazate as the starting material. mp 247° C.; CIMS m/e calc&#39;d for C 25 H 21 N 6 O 4 : 469.1624, found: 469.1528;  
       Example CLXV  
     Preparation of 3-(4-methoxyphenyl)-5-(2-(2-aminobenzoyl)hydrazinecarboxamido)indeno[1,2-c]pyrazol-4-one  
       [0290]    Prepared in a similar fashion as described for example CLVIII using 2-aminophenyl carbazate as the starting material. mp 257° C.; CIMS m/e calc&#39;d for C 25 H 21 N 6 O 4 : 469.1624, found: 469.1548;  
       Example CLXVI  
     Preparation of 3-(4-methoxyphenyl)-5-(2-(4-N,N-dimethylamino benzoyl)hydrazinecarboxamido)indeno[1,2-c]pyrazol-4-one  
       [0291]    Prepared in a similar fashion as described for example CLVIII using 4-N,N-dimethylaminophenyl carbazate as the starting material. mp 259° C.; CIMS m/e calc&#39;d for C 27 H 25 N 6 O 4 : 497.1937, found: 497.1876;  
       Example CLXVII  
     Preparation of 3-(4-methoxyphenyl)-5-(2-phenethylacetyl hydrazinecarboxamido)indeno[1,2-c]pyrazol-4-one  
       [0292]    Prepared in a similar fashion as described for example CLVIII using benzyl carbazate as the starting material. mp 269° C.; CIMS m/e calc&#39;d for C 26 H 22 N 5 O 4 : 468.1672, found: 468.1313;  
       Example CLXVIII  
     Preparation of 3-(4-methoxyphenyl)-5-(2-(2-hydroxy benzoyl)hydrazinecarboxamido)indeno[1,2-c]pyrazol-4-one  
       [0293]    Prepared in a similar fashion as described for example CLVIII using 2-hydroxyphenyl carbazate as the starting material. mp 280° C.; CIMS m/e calc&#39;d for C 25 H 20 N 5 O 5 : 470.1464, found: 470.1419;  
       Example CLXIX  
     Preparation of 3-(4-methoxyphenyl)-5-(2-methoxycarbonyl hydrazinecarboxamido)indeno[1,2-c]pyrazol-4-one  
       [0294]    Prepared in a similar fashion as described for example CLVIII using carbazic acid methyl ester as the starting material. mp &gt;300° C.; CIMS m/e calc&#39;d for C 20 H 28 N 5 O 5 : 408.1308, found: 408.1397;  
       EXAMPLE CLXX  
     Preparation of Intermediate CLXX  
       [0295]    The preparation of intermediate CLXX, (N-[2-(4-Methoxy-benzoyl)-1,3-dioxo-indan-4-yl]-acetamide) is described in Nugiel, D. A.; Etzkorn, A. M.; Vidwans, A.; Benfield, P. A.; Boisclair, M.; Burton, C. R.; Cox, S.; Czerniak, P. M.; Doleniak, D.; Seitz, S. P. J. Med. Chem. 2001, 44, 1334-1336 which is herein incorporated by reference in it&#39;s entirety as though set forth in full.  
       EXAMPLE CLXXI  
     Preparation of Intermediate CLXXI  
       [0296]    Synthesis of 4-Amino-2-(4-methoxy-benzoyl)-indan-1,3-dione: The compound prepared in example 1 (2.0 g, 5.93 mmol) is dissolved in 20% HCl in methanol (50 mL). This solution is stirred at reflux for a period of 3 h. It is then allowed to cool to room temperature and stirred overnight. The product is filtered off, washed with ethanol (20 mL) and air dried to give the product as a yellow solid (1.5 g, 85.7%). mp 268-269° C.;  1 H NMR (DMSOd 6 ) δ8.17 (d, J=8.8 Hz, 2H), 7.49 (t, 1H), 7.12 (d, J=8.7 Hz, 2H), 6.98 (m, 2H), 3.88 (s, 1H).  
       EXAMPLE CLXXII  
     Preparation of Intermediate CLXXII  
       [0297]    Synthesis of [2-(4-Methoxybenzoyl)-1,3-dioxo-indan-4-yl]-carbamic acid phenyl ester: The product prepared in Example CLXXI (1.5 g, 5.08 mmol) is dissolved in acetone (40 mL) and treated with sodium carbonate (1.26 g, 15.24 mmol) and phenyl chloroformate (1.19 g, 7.62 mmol). The suspension is stirred at 50° C. for 3 h. The reaction mixture is diluted with water (120 mL), and extracted with ethyl acetate (2×100 mL). The organic layer is separated, washed with brine (50 mL), dried (Na 2 SO 4 ) and the solvent removed at reduced pressure to give a gummy orange residue. Cold ethyl ether (100 mL) is added to this residue to give a precipitate. The precipitate is collected and washed with ethyl ether (2×10 mL) to give desired product as a yellow solid (1.65 g. 78%). mp 256-258° C.;  1 HNMR (DMSOd 6 ) δ10.83 (s, 1H), 8.08 (d, J=8.0 Hz, 1H), 7.57 (d, J=2.9 Hz, 2H), 7.54 (m, 3H), 7.28 (m, 3H), 7.09 (t, 1H), 6.89 (d, J=10.8 Hz, 2H), 3.81 (s, 3H).  
       EXAMPLE CLXXIII  
     Preparation of 1-[3-(4-methoxy-phenyl)-4-oxo-2,4-dihydro-indeno[1,2-c]pyrazol-5-yl]-3-morpholin-4-yl-urea  
       [0298]    [0298]                           
         [0299]    The product prepared in Example CLXXII (0.03 g, 0.072 mmol) in anhydrous DMSO (2 mL) is treated with 4-aminomorpholine (0.0084 g, 0.082 mmol) and 4-dimethylaminopyridine (0.005 g, 0.04 mmol) and heated to 80° C. for 3 h. The solvent is removed under reduced pressure and the residue triturated with ethanol to give a dark solid. The solid is collected and washed with ethanol (5 mL) to give a tricarbonyl urea (0.03 g, 100%). The tricarbonyl urea intermediate (0.03 g, 0.078 mmol) is treated with hydrazine hydrate (0.1 mL, 3.21 mmol) and p-toluenesulfonic acid monohydrate (0.01 g, 0.05 mmol) in refluxing ethanol (4 mL) for a period of 3 h. The reaction mixture is cooled to room temperature, the solid collected, washed with cold ethanol (2×2 mL), and air dried to give the product as a yellowish solid (0.012 g, 41.3%). mp 290-291° C.;  1 H NMR (DMSO-d 6 ) δ8.27 (d, J=6.8 Hz, 2H), 8.16 (d, J=8.8 Hz, 2H), 7.42 (m, 1H), 7.12 (m, 3H), 3.81 (s, 3H), 2.90 (s, 4H), 2.70 (s, 4H), HRMS calcd. for C 22 H 22 N 5 O 4  (M+H + ) 420.1672; found 420.1688;  
       EXAMPLE CLXXIV  
     Preparation of [3-(4-methoxy-phenyl)-4-oxo-2,4-dihydro-indeno[1,2-c]pyrazol-5-yl]-urea  
       [0300]    [0300]                           
         [0301]    The product prepared in Example CLXXII (0.03 g, 0.072 mmol) in anhydrous DMSO (2 mL) is treated with excess ammonium hydroxide solution and 4-dimethylaminopyridine (0.005 g, 0.04 mmol) and is heated to 80° C. for 3 h. The solvent is removed under reduced pressure and the residue triturated with ethanol to give a dark solid. The solid is collected and washed with ethanol (5 mL) to give urea (0.03 g, 100%). The tricarbonyl urea intermediate (0.03 g, 0.078 mmol) is treated with hydrazine hydrate (0.1 mL, 3.21 mmol) and p-toluenesulfonic acid monohydrate (0.01 g, 0.05 mmol) in refluxing ethanol (4 mL) for a period of 3 h. The reaction mixture is cooled to room temperature, the solid collected, washed with cold ethanol (2×2 mL), and air dried to give the product as a yellowish solid (0.018 g, 62.4%). mp 267-269° C.;  1 H NMR (DMSO-d 6 ) δ9.35 (s, 1H), 8.22 (m, 3H), 7.38 (m, 1H), 7.10 (d, J=8.8 Hz, 2H), 7.02 (d, J =7 Hz, 1H), 3.81 (s, 3H); HRMS calcd. for C 18 H 15 N 4 O 3  (M+H + ) 335.1144; found 335.1162;  
       EXAMPLE CLXXV  
     Preparation of 1-(2-amino-cyclohexyl)-3-[3-(4-methoxy-phenyl)-4-oxo-2,4-dihydro-indeno[1,2-c]pyrazol-5-yl]-urea  
       [0302]    [0302]                           
         [0303]    The product prepared in Example CLXXII (0.03 g, 0.072 mmol) in anhydrous DMSO (2 mL) is treated with 1,2-diaminocyclohexane (0.01 g, 0.082 mmol) and 4-dimethylaminopyridine (0.005 g, 0.04 mmol) and heated to 80° C. for 3 h. The solvent is removed under reduced pressure and the residue triturated with ethanol to give a dark solid. The solid is collected and washed with ethanol (5 mL) to give a tricarbonyl urea (0.03 g, 100%). The tricarbonyl urea intermediate (0.03 g, 0.078 mmol) is treated with hydrazine hydrate (0.1 mL, 3.21 mmol) and p-toluenesulfonic acid monohydrate (0.01 g, 0.05 mmol) in refluxing ethanol (4 mL) for a period of 3 h. The reaction mixture is cooled to room temperature, the solid collected, washed with cold ethanol (2×2 mL), and air dried to give the product as a yellowish solid (0.01 g, 30.6%).  1 HNMR (DMSO-d 6 ) δ9.56 (s, 1H), 8.27 (d, 1H), 8.19 (d, 2H), 7.41 (t, 1H), 7.10 (m, 3H), 4.10 (s, 1H), 3.81 (s, 3H), 3.23 (s, 1H), 1.63 (m, 5H), 1.40 (m, 3H).  
       EXAMPLE CLXXVI  
     Preparation of 5-Amino-3-(4-methoxyphenyl)-2-phenyl-2H-indeno-[1,2-c]pyrazol-4-one:  
       [0304]    [0304]                           
         [0305]    A suspension of N-[3-(4-Methoxy-phenyl)-4-oxo-2,4-dihydro-indeno[1,2-c]pyrazol-5-yl]-acetamide (as produced according to Nugiel, D. A.; Etzkorn, A. M.; Vidwans, A.; Benfield, P. A.; Boisclair, M.; Burton, C. R.; Cox, S.; Czerniak, P. M.; Doleniak, D.; Seitz, S. P. J. Med. Chem. 2001, 44, 1334-1336) (1.0 g, 3.0 mmol) in MeOH (10 mL) was treated with concentrated HCl (1 mL) and heated to reflux. After stirring the mixture for 2 h the reaction was cooled and the product was collected by filtration and obtained as a greenish solid (0.7 g, 81%). mp 273° C.; NMR (DMSO-d 6 ) δ13.6 (bs, 1 H), 8.3 (d, J=8.4 Hz, 1 H), 8.1 (d, J=8.8 Hz, 2 H), 7.5 (t, J=7.7 Hz 1 H), 7.2 (d, J=7.0 Hz, 1 H), 7.1 (d, J=8.8 Hz, 2 H), 3.8 (s, 3 H); HRMS m/e calc&#39;d for C 17 H 14 N 3 O 2  (M +H): 292.1086, found: 292.1080.  
       EXAMPLE CLXXVII  
     Preparation of 2-Chloro-N-[3-(4-methoxyphenyl)-4-oxo-2,4-dihydro-indeno[1,2-c]pyrazol-5-yl]-acetamide  
       [0306]    [0306]                           
         [0307]    A suspension of the product prepared in Example CLXXVI (0.2 g, 0.7 mmol) in dioxane (10 mL) was treated with aqueous saturated NaHCO 3  (3 mL) and chloroacetyl chloride (3 mL, 0.21 mmol). The reaction was heated to 50° C. and stirred for 2 h. The reaction is then cooled, poured into water (20 mL), extracted with EtOAc (100 mL), the organic layer separated, dried (MgSO 4 ) and the solvent removed at reduced pressure. The residue is recrystallized from EtOH to give the product as a yellow solid (0.09 g, 35%). mp &gt;300° C.; NMR (DMSO-d 6 ) δ13.6 (bs, 1 H), 11.3 (s, 1 H), 8.3 (d, J=8.4 Hz, 1 H), 8.1 (d, J=8.8 Hz, 2 H), 7.5 (t, J=7.7 Hz 1 H), 7.2 (d, J=7.0 Hz, 1 H), 7.1 (d, J=8.8 Hz, 2 H), 4.5 (s, 2 H), 3.8 (s, 3 H); HRMS m/e calc&#39;d for C 19 H 15 N 3 O 3 Cl (M+H): 368.0802, found: 368.0818.  
       EXAMPLE CLXXVIII  
     Preparation of 2-(4-aminomethyl-piperidin-1-yl)-N-[3-(4-methoxy-phenyl)-4-oxo-2,4-dihydro-indeno[1,2-c]pyrazol-5-yl]-acetamide  
       [0308]    [0308]                           
         [0309]    A suspension of product prepared according to Example CLXXVII (0.015 g, 0.04 mmol) in EtOH (1 mL) is treated with 4-aminomethylpiperdine (0.75 mL), placed in a sealed tube and heated to 80° C. for 3 h. The reaction is cooled and the solvent removed at reduced pressure. The residue is recrystallized from EtOH to give the product as a yellow solid (0.009 g, 62%) .mp &gt;300° C.; NMR (DMSO-d 6 ) δ13.6 (bs, 1 H), 11.3 (s, 1 H), 8.35 (d, J=8.4 Hz, 1 H), 8.1 (d, J=8.8 Hz, 2 H), 7.5 (t, J=7.7 Hz 1 H), 7.2 (d, J=7.0 Hz, 1 H), 7.1 (d, J=8.8 Hz, 2 H), 3.8 (s, 3 H), 3.2 (bs, 2 H), 2.9(bs, 2 H), 2.5 (d, J=8.0 Hz, 2 H), 2.2 (t, J=8.0 Hz, 2 H), 1.6 (m, 5 H); HRMS m/e calc&#39;d for C 25 H 28 N 5 O 3  (M+H): 446.2192, found: 446.2169; Anal. (C 25 H 27 N 5 O 3 ) C, H, N.  
       EXAMPLE CLXXIX  
     Preparation of 2-(4-Methoxybenzoyl)-3-methoxycarbonylamino-indan-1,3-dione  
       [0310]    [0310]                           
         [0311]    A solution of 3-methoxycarbonylamino-phthalic acid dimethyl ester (1 g, 4.8 mmol) and 4-methoxyacetophenone (0.72 g, 4.8 mmol) in dry DMF (3 mL) was heated to 90° C. Sodium hydride (0.21 g, 60% suspension in oil, 5.2 mmol) is added in one portion and the exothermic reaction turns deep red. After 20 min, the reaction is cooled to room temperature, diluted with water (25 mL) extracted with EtOAc (10 mL) and the aqueous phase separated. The aqueous phase is acidified to pH 2 with 2N HCl and the crude product collected. Recrystallization with ethanol gives the desired product as a yellow solid (0.4 g, 30%). ESIMS 352 (M−H, 100%).  
       EXAMPLE CLXXX  
     Preparation of 3-(4-Methoxyphenyl)-5-methoxycarbonylamino-2H-indeno-[1,2-c]pyrazol-4-one  
       [0312]    [0312]                           
         [0313]    A solution of 2-(4-methoxybenzoyl)-3-methoxycarbonylamino-indan-1,3-dione (0.2 g, 0.6 mmol) in EtOH (5 mL) is treated with hydrazine hydrate (0.1 mL, 1.8 mmol) and p-TsOH (3 mg). The reaction is heated to reflux and stirred for 2 h. The reaction is cooled to room temperature and the product crystallized from the reaction mixture. The product is collected by filtration as a yellow solid (0.1 g, 50%). mp &gt;300° C.; HRMS m/e calc&#39;d for C 19 H 16 N 3 O 4  (M+H): 350.1141, found: 350.1168.  
       UTILITY  
     Inhibition of Kinase/Cyclin Complex Enzymatic Activity  
       [0314]    Several of the compounds disclosed in this invention were assayed for their inhibitory activity against cdk4/D1 and cdk2/E kinase complexes. Briefly, the in vitro assays employ cell lysates from insect cells expressing either of the kinases and subsequently their corresponding regulatory units. The cdk2/cyclinE is purified from insect cells expressing His-tagged cdk2 and cyclin E. The cdk/cyclin lysate is combined in a microtitre-type plate along with a kinase compatible buffer,  32 P-labeled ATP at a concentration of 50 mM, a GST-Rb fusion protein and the test compound at varying concentrations. The kinase reaction is allowed to proceeded with the radiolabled ATP, then effectively stopped by the addition of a large excess of EDTA and unlabeled ATP. The GST-Rb labeled protein is sequestered on a GSH-Sepharose bead suspension, washed, resuspended in scintillant, and the  32 P activity detected in a scintillation counter. The compound concentration which inhibits 50% of the kinase activity was calculated for each compound. A compound was considered active if its IC 50  was found to be less than 1 μM.  
       Inhibition of HCT 116 Cancer Cell Proliferation  
       [0315]    To test the cellular activity of several compounds disclosed in this invention, we examined the effect of these compounds on cultured HCT116 cells and determined their effect on cell-cycle progression by the calorimetric cytotoxcity test using sulforhodamine B (Skehan et al. J. Natl. Cancer Inst. 82:1107-12, 1990). Briefly, HCT116 cells are cultured in the presence of test compounds at increasing concentrations. At selected time points, groups of cells are fixed with trichloroacetic acid and stained with sulforhodamine B (SRB). Unbound dye was removed by washing and protein-bound dye was extracted for determination of optical density. A compound was considered active if its IC 50  was found to be less than 10 μM.  
                                                           TABLE 1                                                                                  Example           mass   mp       #   R 1     R 2     (M + H)   (° C.)                    I   Methyl   4-MeOC 6 H 4     334   268       II   ClCH 2     4-MeOC 6 H 4     382   274       III   Cyclopropyl   4-MeOC 6 H 4     360   289       IV   Isopropyl   4-MeOC 6 H 4     362   288       V   Ethyl   4-MeOC 6 H 4     348   287       VI   Cyclopentyl   4-MeOC 6 H 4     388   267       VII   Cyclobutyl   4-MeOC 6 H 4     374   297       VIII   Benzyl   4-MeOC 6 H 4     410   280       IX   n-propyl   4-MeOC 6 H 4     362   282       X   4-ClC 6 H 4 CH 2     4-MeOC 6 H 4     444   238       XI   3-MeOC 6 H 4 CH 2     4-MeOC 6 H 4     440   &gt;300       XII   4-MeOC 6 H 4 CH 2     4-MeOC 6 H 4     440   280       XIII   3,4-diMeOC 6 H 4 CH 2     4-MeOC 6 H 4     470   &gt;300       XIV   2,5-diMeOC 6 H 4 CH 2     4-MeOC 6 H 4     470   226       XV   Methyl   2-MeOC 6 H 4     334   276       XVI   Methyl   3,4-diMeOC 6 H 4     364   &gt;300       XVII   3,4-(OCH 2 O)C 6 H 4 CH 2     4-MeOC 6 H 4     454   297       XVIII   3-thiophenylCH 2     4-MeOC 6 H 4     416   293       XIX   2-MeOC 6 H 4 CH 2     4-MeOC 6 H 4     440   255       XX   3,4-diClOC 6 H 4 CH 2     4-MeOC 6 H 4     479   299       XXI   2,4-diClOC 6 H 4 CH 2     4-MeOC 6 H 4     479   286       XXII   2-ClC 6 H 4 CH 2     4-MeOC 6 H 4     444   300       XXIII   H 2 NCH 2     4-MeOC 6 H 4     349   &gt;300       XXIV   HOCH 2 CH 2 NHCH 2     4-MeOC 6 H 4     393   243       XXV   Me 2 NCH 2     4-MeOC 6 H 4     377   279       XXVI   piperazinylCH 2     4-MeOC 6 H 4     418   277       XXVII   4-Me-piperazinylCH 2     4-MeOC 6 H 4     432   &gt;300       XXVIII   4-HOCH 2 CH 2 -   4-MeOC 6 H 4     462   &gt;300           piperazinylCH 2         XXIX   piperidinylCH 2     4-MeOC 6 H 4     417   291       XXX   4-NH 2 CH 2 -   4-MeOC 6 H 4     446   &gt;300           piperidinylCH 2         XXXI   CH 3 CH 2 NHCH 2     4-MeOC 6 H 4     377   250       XXXII   ThiomorpholinylCH 2     4-MeOC 6 H 4     435   298       XXXIII   morpholinylCH 2     4-MeOC 6 H 4     419   295       XXXIV   pyrrolidinylCH 2     4-MeOC 6 H 4     403   279       XXXV   4-pyridylCH 2 NHCH 2     4-MeOC 6 H 4     440   &gt;300       XXXVI   4-CH 3 CONHC 6 H 4 CH 2     4-MeOC 6 H 4     467   268       XXXVII   4-CH 3 OCONHC 6 H 4 CH 2     4-MeOC 6 H 4     483   257       XXXVIII   4-NH 2 CH 2 CONHC 6 H 4 CH 2     4-MeOC 6 H 4     482   228       XXXIX   4-Me 2 NCH 2 CONHC 6 H 4 CH 2     4-MeOC 6 H 4     510   &gt;300       XL   4-N 3 C 6 H 4 CH 2     4-MeOC 6 H 4     451   &gt;300       XLI   4-NH 2 C 6 H 4 CH 2     4-MeOC 6 H 4     425   283       XLII   C 6 H 5 NH   4-MeOC 6 H 4     411   &gt;300       XLIII   CH 3 CH 2 CH 2 NH   4-MeOC 6 H 4     377   252       XLIV   4-NH 2 C 6 H 4 CH 2 NH   4-MeOC 6 H 4     440   &gt;300       XLV   4-pyridylCH 2 NH   4-MeOC 6 H 4     426   &gt;300       XLVI   Methyl   4-HOC 6 H 4     320   &gt;300       XLVII   H   4-MeOC 6 H 4     320   280       XLVIII   Methyl   3-pyridyl   305   &gt;300       XLIX   Methyl   4-pyridyl   305   &gt;300       L   H   4-pyridyl   291   &gt;300       LI   Methyl   C 6 H 5     305   &gt;300       LII   Methyl   4-MeSC 6 H 4     351   283       LIII   Methyl   4-MeSO 2 C 6 H 4     383   &gt;300       LVI   Methyl   4-Me 2 NC 6 H 4     348   &gt;300       LV   morpholinylCH 2     4-Me 2 NC 6 H 4     432   &gt;300       LVI   Me 2 NCH 2     4-Me 2 NC 6 H 4     390   &gt;300       LVII   Methyl   4-(piperdinyl)C 6 H 4     388   291       LVIII   Methyl   4-(morpholinyl)C 6 H 4     389   &gt;300       LIX   Methyl   4-CH 3 CH 2 OC 6 H 4     349   288       LX   Methyl   4-CH 3 CH 2 CH 2 CH 2 C 6 H 4     361   259       LXI   Methyl   4-CH 3 CH 2 C 6 H 4     332   294       LXII   Methyl   4-CH 3 CH 2 CH 2 C 6 H 4     347   269       LXIII   NH 2     4-MeOC 6 H 4     335   &gt;300       LXIV   Me2NNH   4-MeOC 6 H 4     378   &gt;300       LXV   MeNH   4-MeOC 6 H 4     349   &gt;300       LXVI   MorpholinylNH   4-MeOC 6 H 4     420   &gt;300       LXVII   cis-1,2-   4-MeOC 6 H 4     432   &gt;300           diaminocyclohexanyl       LXVIII   4-methyl-   4-MeOC 6 H 4     433   &gt;300           piperazinylNH       LXVIX   4-uridomethyl-   4-MeOC 6 H 4     489   &gt;300           piperadinylCH 2         LXX   4-(2-pyridyl)-   4-MeOC 6 H 4     495   &gt;300           piperazinyl CH 2         LXXI   4-(aminoethyl)-   4-MeOC 6 H 4     461   &gt;300           piperazinyl CH 2         LXXII   4-amidopiperidinylCH 2     4-MeOC 6 H 4     460   &gt;300       LXXIII   4-hydroxy-   4-MeOC 6 H 4     433   &gt;300           piperidinylCH 2         LXXIV   4-hydroxy-   4-MeOC 6 H 4     447   &gt;300           methylpiperidinylCH 2         LXXV   4-amidopiperazinylCH 2     4-MeOC 6 H 4     493   &gt;300       LXXVI   4-dimethyl-   4-MeOC 6 H 4     492   &gt;300           aminopiperadinylCH 2         LXXVII   4-aminopiperadinylCH 2     4-MeOC 6 H 4     464   &gt;300       LXXVIII   4-Me-piperazinylCH 2     4-Me 2 NC 6 H 4     445   &gt;300       LXXIX   4-NH 2 CH 2 -   4-Me 2 NC 6 H 4     459   NA           piperidinylCH 2         LXXX   4-OH-piperidinylCH 2     4-Me 2 NC 6 H 4     446   267       LXXXI   morpholinylCH 2     4-(morpholinyl)C 6 H 4     474   258       LXXXII   4-Me-piperazinylCH 2     4-(morpholinyl)C 6 H 4     487   258       LXXXIII   4-OH-piperidinylCH 2     4-(morpholinyl)C 6 H 4     488   245       LXXXIV   4-NH 2 CH 2 -   4-(morpholinyl)C 6 H 4     501   240           piperidinylCH 2         LXXXV   4-Me-piperazinylNH   4-Me 2 NC 6 H 4     446   &gt;300       LXXXVI   Methyl   i-propyl   270   &gt;250       LXXXVII   Methyl   c-propyl   268   220       LXXXVIII   Methyl   t-butyl   284   &gt;250       LXXXIX   Methyl   2-thienyl   310   269       XC   Methyl   3-Me-2-thienyl   324   275       XCI   NH 2     Ethyl   257   &gt;250       XCII   NH 2     n-propyl   271   187       XCIII   NH 2     i-propyl   271   &gt;250       XCIV   NH 2     c-propyl   267   252                   (M − H)       XCV   NH 2     c-hexyl   311   178       XCVI   NH 2     2-thienyl   310   214                   (M+)       XCVII   NH 2     3-Me-2-thienyl   325   270       XCVIII   NH 2     5-Me-2-thienyl   325   &gt;280       XCIX   NH 2     5-CO 2 Et-2-thienyl   383   &gt;280       C   NH 2     3-thienyl   311   &gt;280       CI   NH 2     5-Cl-3-thienyl   345   &gt;300       CII   NH 2     2,5-diMe-3-thienyl   339   &gt;280       CIII   NH 2     2-furanyl   295   278       CIV   Me 2 NNH   i-propyl   314   231       CV   Me 2 NNH   c-propyl   312       CVI   Me 2 NNH   c-hexyl   354   229       CVII   Me 2 NNH   2-thienyl   354   279       CVIII   Me 2 NNH   5-MeO-2-thienyl   384   280       CIX   Me 2 NNH   5-Me-2-thienyl   368   &gt;280       CX   Me 2 NNH   5-CO 2 Et-2-thienyl   426   252       CXI   Me 2 NNH   3-thienyl   354   202       CXII   NH 2     1-methyl-3-   308   &gt;300               pyrrolyl       CXIII   Me 2 NNH   2,5-diMe-3-thienyl   382   252       CXIV   Me 2 NNH   2-furanyl   338   202       CXV   4-NH 2 CO-   i-propyl   396   224           piperidinylCH 2         CXVI   4-NH 2 CO-   c-hexyl   436   228           piperidinylCH 2         CXVII   4-NH 2 CH 2 -   ethyl   368   174           piperidinylCH 2         CXVIII   4-NH 2 CH 2 -   1-propyl   382   218           piperidinylCH 2         CXVIX   4-NH 2 CH 2 -   c-propyl   380   138           piperidinylCH 2         CXX   4-NH 2 CH 2 -   c-hexyl   422   196           piperidinylCH 2         CXXI   4-CH 3 -piperazinylNH   i-propyl   369   231       CXXII   4-CH 3 -piperazinylNH   5-CO 2 Et-2-thienyl   481   249       CXXIII   4-CH 3 -piperazinylNH   5-CO 2 H-2-thienyl   453   270       CXXIV   4-CH 3 -piperazinylNH   2,5-diMe-3-thienyl   437   250       CXXV   MorpholinylNH   i-propyl   354   256                   (M − H)       CXXVI   MorpholinylNH   4-CO 2 Me-   455   216               piperidinyl       CXXVII   MorpholinylNH   5-Me-2-thienyl   410   261       CXXVIII   MorpholinylNH   5-Cl-3-thienyl   430   259       CXXIX   MorpholinylNH   2,5-diMe-3-thienyl   424   &gt;280       CXXX   MorpholinylNH   5-CO 2 Et-2-thienyl   468   258       CXXXI   MorpholinylNH   5-CO 2 H-2-thienyl   440   273       CXXXII   MorpholinylNH   5-CONHBn-2-thienyl   529   275       CXXXIII   MorpholinylNH   5-CONH(4-Me-   537   190               piperazinyl)-2-               thienyl       CXXXIV   MorpholinylNH   5-CONHCH 2 CH 2 (1-Me-   550   235               2-pyrrolidinyl)-2-thienyl       CXXXV   MorpholinylNH   5-CONHNMe 2 -2-thienyl   482   201       CXXXVI   MorpholinylNH   5-CONHCH 2 CH 2 NMe 2 -   510   190               2-thienyl       CXXXVII   MorpholinylNH   5-CONHCH 2 CH 2 (1-   536   224               pyrrolidinyl)-2-thienyl       CXXXVIII   MorpholinylNH   5-CONHCH 2 CH 2 (1-   552   241               morpholinyl)-2-thienyl       CXXXIX   MorpholinylNH   5-CONHmorpholinyl-2-thienyl   524   271       CXL   MorpholinylNH   5-CONHCH 2 CH 2 CH 2 (1-   564   260               pyrrolidonyl)-2-thienyl       CXLI   MorpholinylNH   5-CONHCH 2 CH 2 (3-   544   203               pyridyl)-2-thienyl       CXLII   MorpholinylNH   5-CONHCH 2 CH 2 CH 2 (1-   547   263               imidazolyl)-2-thienyl       CXLIII   MorpholinylNH   5-CONHCH 2 CH 2 (2-   544   &gt;280               pyridyl)-2-thienyl       CXLIV   MorpholinylNH   5-CONHCH 2 (3-   530   239               pyridyl)-2-thienyl       CXLV   MorpholinylNH   5-CONHCH 2 CH 2 (1-   550   228               piperidinyl)-2-thienyl       CXLVI   Methyl   4-CF 3 C 6 H 4     370   &gt;300                   (M − H)       CXLVII   MorpholinylNH   4-(4-Boc-   574   242               piperazinyl)C 6 H 4         CXLVIII   MorpholinylNH   4-(piperazinyl)C 6 H 4     474   263       CXLIX   NH 2     4-(piperazinyl)C 6 H 4     389   257       CL   NH 2 NH   4-(piperazinyl)C 6 H 4     404   257       CLI   Me 2 NCH 2     4-(piperazinyl)C 6 H 4     431   243       CLII   morpholinylCH 2     4-(piperazinyl)C 6 H 4     473   259       CLIII   4-Me-piperazinylCH 2     4-(piperazinyl)C 6 H 4     486   NA       CLIV   4-NH 2 CH 2 -   4-(piperazinyl)C 6 H 4     500   239           piperidinylCH 2         CLV   MorpholinylNH   4-(4-Me-   488   245               piperazinyl)C 6 H 4         CLVI   MorpholinylNH   4-(4-Et-   502   245               piperazinyl)C 6 H 4         CLVII   MorpholinylNH   4-(4-i-Pr-   516   253               piperazinyl)C 6 H 4         CLVIII   C 6 H 5 C(O)NHNH   4-MeOC 6 H 4     459   &gt;300       CLIX   4-pyridylC(O)NHNH   4-MeOC 6 H 4     455   248       CLX   3-pyridylC(O)NHNH   4-MeOC 6 H 4     455   227       CLXI   3,4-dihydroxy-   4-MeOC 6 H 4     486   &gt;300           C 6 H 3 C(O)NHNH       CLXII   4-hydroxy-   4-MeOC 6 H 4     470   283           C 6 H 4 C(O)NHNH       CLXIII   3-amino-C 6 H 4 C(O)NHNH   4-MeOC 6 H 4     469   250       CLXIV   4-amino-C 6 H 4 C(O)NHNH   4-MeOC 6 H 4     469   247       CLXV   2-amino-C 6 H 4 C(O)NHNH   4-MeOC 6 H 4     469   257       CLXVI   4-N,N-dimethylamino-   4-MeOC 6 H 4     497   259           C 6 H 4 C(O)NHNH       CLXVII   C 6 H 5 CH 2 C(O)NHNH   4-MeOC 6 H 4     468   269       CLXVIII   2-hydroxy-   4-MeOC 6 H 4     470   280           C 6 H 4 C(O)NHNH       CLXIX   MeOC(O)NHNH   4-MeOC 6 H 4     408   &gt;300                  
 
         [0316]    [0316]                                           TABLE 2                                                                                  Example               Number   R 1     R 2                      100   2-pyridylmethyl   4-MeOC 6 H 4         101   2-pyridylmethyl   3-MeOC 6 H 4         102   2-pyridylmethyl   4-NH 2 C 6 H 4         103   2-pyridylmethyl   3-NH 2 C 6 H 4         104   2-pyridylmethyl   2-NH 2 C 6 H 4         105   2-pyridylmethyl   4-Me 2 NC 6 H 4         106   2-pyridylmethyl   3-Me 2 NC 6 H 4         107   2-pyridylmethyl   2-Me 2 NC 6 H 4         108   2-pyridylmethyl   4-pyridyl       109   2-pyridylmethyl   3-pyridyl       110   2-pyridylmethyl   2-pyridyl       111   2-pyridylmethyl   2-thiazolyl       112   2-pyridylmethyl   2-pyrazolyl       113   2-pyridylmethyl   5-isoquinolyl       114   2-pyridylmethyl   3,4-methylenedioxyC 6 H 3         115   2-pyridylmethyl   3,4-ethylenedioxyC 6 H 3         116   2-pyridylmethyl   2-imidazolyl       117   2-pyridylmethyl   2-oxazolyl       118   2-pyridylmethyl   4-isoxazolyl       119   2-pyridylmethyl   4-HOC 6 H 4         120   2-pyridylmethyl   3-HOC 6 H 4         121   2-pyridylmethyl   3,4-diHOC 6 H 4         122   2-pyridylmethyl   4-NH 2 CH 2 C 6 H 4         123   2-pyridylmethyl   3-NH 2 CH 2 C 6 H 4         124   3-pyridylmethyl   4-MeOC 6 H 4         125   3-pyridylmethyl   3-MeOC 6 H 4         126   3-pyridylmethyl   4-NH 2 C 6 H 4         127   3-pyridylmethyl   3-NH 2 C 6 H 4         128   3-pyridylmethyl   2-NH 2 C 6 H 4         129   3-pyridylmethyl   4-Me 2 NC 6 H 4         130   3-pyridylmethyl   3-Me 2 NC 6 H 4         131   3-pyridylmethyl   2-Me 2 NC 6 H 4         132   3-pyridylmethyl   4-pyridyl       133   3-pyridylmethyl   3-pyridyl       134   3-pyridylmethyl   2-pyridyl       135   3-pyridylmethyl   2-thiazolyl       136   3-pyridylmethyl   2-pyrazolyl       137   3-pyridylmethyl   5-isoquinolyl       138   3-pyridylmethyl   3,4-methylenedioxyC 6 H 3         139   3-pyridylmethyl   3,4-ethylenedioxyC 6 H 3         140   3-pyridylmethyl   2-imidazolyl       141   3-pyridylmethyl   2-oxazolyl       142   3-pyridylmethyl   4-isoxazolyl       143   3-pyridylmethyl   4-HOC 6 H 4         144   3-pyridylmethyl   3-HOC 6 H 4         145   3-pyridylmethyl   3,4-diHOC 6 H 4         146   3-pyridylmethyl   4-NH 2 CH 2 C 6 H 4         147   3-pyridylmethyl   3-NH 2 CH 2 C 6 H 4         148   4-pyridylmethyl   4-MeOC 6 H 4         149   4-pyridylmethyl   3-MeOC 6 H 4         150   4-pyridylmethyl   4-NH 2 C 6 H 4         151   4-pyridylmethyl   3-NH 2 C 6 H 4         152   4-pyridylmethyl   2-NH 2 C 6 H 4         153   4-pyridylmethyl   4-Me 2 NC 6 H 4         154   4-pyridylmethyl   3-Me 2 NC 6 H 4         155   4-pyridylmethyl   2-Me 2 NC 6 H 4         156   4-pyridylmethyl   4-pyridyl       157   4-pyridylmethyl   3-pyridyl       158   4-pyridylmethyl   2-pyridyl       159   4-pyridylmethyl   2-thiazolyl       160   4-pyridylmethyl   2-pyrazolyl       161   4-pyridylmethyl   5-isoquinolyl       162   4-pyridylmethyl   3,4-methylenedioxyC 6 H 3         163   4-pyridylmethyl   3,4-ethylenedioxyC 6 H 3         164   4-pyridylmethyl   2-imidazolyl       165   4-pyridylmethyl   2-oxazolyl       166   4-pyridylmethyl   4-isoxazolyl       167   4-pyridylmethyl   4-HOC 6 H 4         168   4-pyridylmethyl   3-HOC 6 H 4         169   4-pyridylmethyl   3,4-diHOC 6 H 4         170   4-pyridylmethyl   4-NH 2 CH 2 C 6 H 4         171   4-pyridylmethyl   3-NH 2 CH 2 C 6 H 4         172   2-NH 2 C 6 H 4 CH 2     4-MeOC 6 H 4         173   2-NH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         174   2-NH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         175   2-NH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         176   2-NH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         177   2-NH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         178   2-NH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         179   2-NH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         180   2-NH 2 C 6 H 4 CH 2     4-pyridyl       181   2-NH 2 C 6 H 4 CH 2     3-pyridyl       182   2-NH 2 C 6 H 4 CH 2     2-pyridyl       183   2-NH 2 C 6 H 4 CH 2     2-thiazolyl       184   2-NH 2 C 6 H 4 CH 2     2-pyrazolyl       185   2-NH 2 C 6 H 4 CH 2     5-isoquinolyl       186   2-NH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         187   2-NH 2 C 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         188   2-NH 2 C 6 H 4 CH 2     2-imidazolyl       189   2-NH 2 C 6 H 4 CH 2     2-oxazolyl       190   2-NH 2 C 6 H 4 CH 2     4-isoxazolyl       191   2-NH 2 C 6 H 4 CH 2     4-HOC 6 H 4         192   2-NH 2 C 6 H 4 CH 2     3-HOC 6 H 4         193   2-NH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         194   2-NH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         195   2-NH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         196   3-NH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         197   3-NH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         198   3-NH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         199   3-NH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         200   3-NH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         201   3-NH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         202   3-NH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         203   3-NH 2 C 6 H 4 CH 2     4-pyridyl       204   3-NH 2 C 6 H 4 CH 2     3-pyridyl       205   3-NH 2 C 6 H 4 CH 2     2-pyridyl       206   3-NH 2 C 6 H 4 CH 2     2-thiazolyl       207   3-NH 2 C 6 H 4 CH 2     2-pyrazolyl       208   3-NH 2 C 6 H 4 CH 2     5-isoquinolyl       209   3-NH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         210   3-NH 2 C 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         211   3-NH 2 C 6 H 4 CH 2     2-imidazolyl       212   3-NH 2 C 6 H 4 CH 2     2-oxazolyl       213   3-NH 2 C 6 H 4 CH 2     4-isoxazolyl       214   3-NH 2 C 6 H 4 CH 2     4-HOC 6 H 4         215   3-NH 2 C 6 H 4 CH 2     3-HOC 6 H 4         216   3-NH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         217   3-NH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         218   3-NH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         219   4-NH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         220   4-NH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         221   4-NH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         222   4-NH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         223   4-NH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         224   4-NH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         225   4-NH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         226   4-NH 2 C 6 H 4 CH 2     4-pyridyl       227   4-NH 2 C 6 H 4 CH 2     3-pyridyl       228   4-NH 2 C 6 H 4 CH 2     2-pyridyl       229   4-NH 2 C 6 H 4 CH 2     2-thiazolyl       230   4-NH 2 C 6 H 4 CH 2     2-pyrazolyl       231   4-NH 2 C 6 H 4 CH 2     5-isoquinolyl       232   4-NH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         233   4-NH 2 C 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         234   4-NH 2 C 6 H 4 CH 2     2-imidazolyl       235   4-NH 2 C 6 H 4 CH 2     2-oxazolyl       236   4-NH 2 C 6 H 4 CH 2     4-isoxazolyl       237   4-NH 2 C 6 H 4 CH 2     4-HOC 6 H 4         238   4-NH 2 C 6 H 4 CH 2     3-HOC 6 H 4         239   4-NH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         240   4-NH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         241   4-NH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         242   2-MeOC 6 H 4 CH 2     3-MeOC 6 H 4         243   2-MeOC 6 H 4 CH 2     4-NH 2 C 6 H 4         244   2-MeOC 6 H 4 CH 2     3-NH 2 C 6 H 4         245   2-MeOC 6 H 4 CH 2     2-NH 2 C 6 H 4         246   2-MeOC 6 H 4 CH 2     4-Me 2 NC 6 H 4         247   2-MeOC 6 H 4 CH 2     3-Me 2 NC 6 H 4         248   2-MeOC 6 H 4 CH 2     2-Me 2 NC 6 H 4         249   2-MeOC 6 H 4 CH 2     4-pyridyl       250   2-MeOC 6 H 4 CH 2     3-pyridyl       251   2-MeOC 6 H 4 CH 2     2-pyridyl       252   2-MeOC 6 H 4 CH 2     2-thiazolyl       253   2-MeOC 6 H 4 CH 2     2-pyrazolyl       254   2-MeOC 6 H 4 CH 2     5-isoquinolyl       255   2-MeOC 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         256   2-MeOC 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         257   2-MeOC 6 H 4 CH 2     2-imidazolyl       258   2-MeOC 6 H 4 CH 2     2-oxazolyl       259   2-MeOC 6 H 4 CH 2     4-isoxazolyl       260   2-MeOC 6 H 4 CH 2     4-HOC 6 H 4         261   2-MeOC 6 H 4 CH 2     3-HOC 6 H 4         262   2-MeOC 6 H 4 CH 2     3,4-diHOC 6 H 4         263   2-MeOC 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         264   2-MeOC 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         265   3-MeOC 6 H 4 CH 2     3-MeOC 6 H 4         266   3-MeOC 6 H 4 CH 2     4-NH 2 C 6 H 4         267   3-MeOC 6 H 4 CH 2     3-NH 2 C 6 H 4         268   3-MeOC 6 H 4 CH 2     2-NH 2 C 6 H 4         269   3-MeOC 6 H 4 CH 2     4-Me 2 NC 6 H 4         270   3-MeOC 6 H 4 CH 2     3-Me 2 NC 6 H 4         271   3-MeOC 6 H 4 CH 2     2-Me 2 NC 6 H 4         272   3-MeOC 6 H 4 CH 2     4-pyridyl       273   3-MeOC 6 H 4 CH 2     3-pyridyl       274   3-MeOC 6 H 4 CH 2     2-pyridyl       275   3-MeOC 6 H 4 CH 2     2-thiazolyl       276   3-MeOC 6 H 4 CH 2     2-pyrazolyl       277   3-MeOC 6 H 4 CH 2     5-isoquinolyl       278   3-MeOC 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         279   3-MeOC 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         280   3-MeOC 6 H 4 CH 2     2-imidazolyl       281   3-MeOC 6 H 4 CH 2     2-oxazolyl       282   3-MeOC 6 H 4 CH 2     4-isoxazolyl       283   3-MeOC 6 H 4 CH 2     4-HOC 6 H 4         284   3-MeOC 6 H 4 CH 2     3-HOC 6 H 4         285   3-MeOC 6 H 4 CH 2     3,4-diHOC 6 H 4         286   3-MeOC 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         287   3-MeOC 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         288   4-MeOC 6 H 4 CH 2     3-MeOC 6 H 4         289   4-MeOC 6 H 4 CH 2     4-NH 2 C 6 H 4         290   4-MeOC 6 H 4 CH 2     3-NH 2 C 6 H 4         291   4-MeOC 6 H 4 CH 2     2-NH 2 C 6 H 4         292   4-MeOC 6 H 4 CH 2     4-Me 2 NC 6 H 4         293   4-MeOC 6 H 4 CH 2     3-Me 2 NC 6 H 4         294   4-MeOC 6 H 4 CH 2     2-Me 2 NC 6 H 4         295   4-MeOC 6 H 4 CH 2     4-pyridyl       296   4-MeOC 6 H 4 CH 2     3-pyridyl       297   4-MeOC 6 H 4 CH 2     2-pyridyl       298   4-MeOC 6 H 4 CH 2     2-thiazolyl       299   4-MeOC 6 H 4 CH 2     2-pyrazolyl       300   4-MeOC 6 H 4 CH 2     5-isoquinolyl       301   4-MeOC 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         302   4-MeOC 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         303   4-MeOC 6 H 4 CH 2     2-imidazolyl       304   4-MeOC 6 H 4 CH 2     2-oxazolyl       305   4-MeOC 6 H 4 CH 2     4-isoxazolyl       306   4-MeOC 6 H 4 CH 2     4-HOC 6 H 4         307   4-MeOC 6 H 4 CH 2     3-HOC 6 H 4         308   4-MeOC 6 H 4 CH 2     3,4-diHOC 6 H 4         309   4-MeOC 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         310   4-MeOC 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         311   2-HOC 6 H 4 CH 2     4-MeOC 6 H 4         312   2-HOC 6 H 4 CH 2     3-MeOC 6 H 4         313   2-HOC 6 H 4 CH 2     4-NH 2 C 6 H 4         314   2-HOC 6 H 4 CH 2     3-NH 2 C 6 H 4         315   2-HOC 6 H 4 CH 2     2-NH 2 C 6 H 4         316   2-HOC 6 H 4 CH 2     4-Me 2 NC 6 H 4         317   2-HOC 6 H 4 CH 2     3-Me 2 NC 6 H 4         318   2-HOC 6 H 4 CH 2     2-Me 2 NC 6 H 4         319   2-HOC 6 H 4 CH 2     4-pyridyl       320   2-HOC 6 H 4 CH 2     3-pyridyl       321   2-HOC 6 H 4 CH 2     2-pyridyl       322   2-HOC 6 H 4 CH 2     2-thiazolyl       323   2-HOC 6 H 4 CH 2     2-pyrazolyl       324   2-HOC 6 H 4 CH 2     5-isoquinolyl       325   2-HOC 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         326   2-HOC 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         327   2-HOC 6 H 4 CH 2     2-imidazolyl       328   2-HOC 6 H 4 CH 2     2-oxazolyl       329   2-HOC 6 H 4 CH 2     4-isoxazolyl       330   2-HOC 6 H 4 CH 2     4-HOC 6 H 4         331   2-HOC 6 H 4 CH 2     3-HOC 6 H 4         332   2-HOC 6 H 4 CH 2     3,4-diHOC 6 H 4         333   2-HOC 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         334   2-HOC 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         335   3-HOC 6 H 4 CH 2     4-MeOC 6 H 4         336   3-HOC 6 H 4 CH 2     3-MeOC 6 H 4         337   3-HOC 6 H 4 CH 2     4-NH 2 C 6 H 4         338   3-HOC 6 H 4 CH 2     3-NH 2 C 6 H 4         339   3-HOC 6 H 4 CH 2     2-NH 2 C 6 H 4         340   3-HOC 6 H 4 CH 2     4-Me 2 NC 6 H 4         341   3-HOC 6 H 4 CH 2     3-Me 2 NC 6 H 4         342   3-HOC 6 H 4 CH 2     2-Me 2 NC 6 H 4         343   3-HOC 6 H 4 CH 2     4-pyridyl       344   3-HOC 6 H 4 CH 2     3-pyridyl       345   3-HOC 6 H 4 CH 2     2-pyridyl       346   3-HOC 6 H 4 CH 2     2-thiazolyl       347   3-HOC 6 H 4 CH 2     2-pyrazolyl       348   3-HOC 6 H 4 CH 2     5-isoquinolyl       349   3-HOC 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         350   3-HOC 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         351   3-HOC 6 H 4 CH 2     2-imidazolyl       352   3-HOC 6 H 4 CH 2     2-oxazolyl       353   3-HOC 6 H 4 CH 2     4-isoxazolyl       354   3-HOC 6 H 4 CH 2     4-HOC 6 H 4         355   3-HOC 6 H 4 CH 2     3-HOC 6 H 4         356   3-HOC 6 H 4 CH 2     3,4-diHOC 6 H 4         357   3-HOC 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         358   3-HOC 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         359   4-HOC 6 H 4 CH 2     4-MeOC 6 H 4         360   4-HOC 6 H 4 CH 2     3-MeOC 6 H 4         361   4-HOC 6 H 4 CH 2     4-NH 2 C 6 H 4         362   4-HOC 6 H 4 CH 2     3-NH 2 C 6 H 4         363   4-HOC 6 H 4 CH 2     2-NH 2 C 6 H 4         364   4-HOC 6 H 4 CH 2     4-Me 2 NC 6 H 4         365   4-HOC 6 H 4 CH 2     3-Me 2 NC 6 H 4         366   4-HOC 6 H 4 CH 2     2-Me 2 NC 6 H 4         367   4-HOC 6 H 4 CH 2     4-pyridyl       368   4-HOC 6 H 4 CH 2     3-pyridyl       369   4-HOC 6 H 4 CH 2     2-pyridyl       370   4-HOC 6 H 4 CH 2     2-thiazolyl       371   4-HOC 6 H 4 CH 2     2-pyrazolyl       372   4-HOC 6 H 4 CH 2     5-isoquinolyl       373   4-HOC 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         374   4-HOC 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         375   4-HOC 6 H 4 CH 2     2-imidazolyl       376   4-HOC 6 H 4 CH 2     2-oxazolyl       377   4-HOC 6 H 4 CH 2     4-isoxazolyl       378   4-HOC 6 H 4 CH 2     4-HOC 6 H 4         379   4-HOC 6 H 4 CH 2     3-HOC 6 H 4         380   4-HOC 6 H 4 CH 2     3,4-diHOC 6 H 4         381   4-HOC 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         382   4-HOC 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         383   4-ClC 6 H 4 CH 2     3-MeOC 6 H 4         384   4-ClC 6 H 4 CH 2     4-NH 2 C 6 H 4         385   4-ClC 6 H 4 CH 2     3-NH 2 C 6 H 4         386   4-ClC 6 H 4 CH 2     2-NH 2 C 6 H 4         387   4-ClC 6 H 4 CH 2     4-Me 2 NC 6 H 4         388   4-ClC 6 H 4 CH 2     3-Me 2 NC 6 H 4         389   4-ClC 6 H 4 CH 2     2-Me 2 NC 6 H 4         390   4-ClC 6 H 4 CH 2     4-pyridyl       391   4-ClC 6 H 4 CH 2     3-pyridyl       392   4-ClC 6 H 4 CH 2     2-pyridyl       393   4-ClC 6 H 4 CH 2     2-thiazolyl       394   4-ClC 6 H 4 CH 2     2-pyrazolyl       395   4-ClC 6 H 4 CH 2     5-isoquinolyl       396   4-ClC 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         397   4-ClC 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         398   4-ClC 6 H 4 CH 2     2-imidazolyl       399   4-ClC 6 H 4 CH 2     2-oxazolyl       400   4-ClC 6 H 4 CH 2     4-isoxazolyl       401   4-ClC 6 H 4 CH 2     4-HOC 6 H 4         402   4-ClC 6 H 4 CH 2     3-HOC 6 H 4         403   4-ClC 6 H 4 CH 2     3,4-diHOC 6 H 4         404   4-ClC 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         405   4-ClC 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         406   2-NH 2 CH 2 C 6 H 4 CH 2     4-MeOC 6 H 4         407   2-NH 2 CH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         408   2-NH 2 CH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         409   2-NH 2 CH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         410   2-NH 2 CH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         411   2-NH 2 CH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         412   2-NH 2 CH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         413   2-NH 2 CH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         414   2-NH 2 CH 2 C 6 H 4 CH 2     4-pyridyl       415   2-NH 2 CH 2 C 6 H 4 CH 2     3-pyridyl       416   2-NH 2 CH 2 C 6 H 4 CH 2     2-pyridyl       417   2-NH 2 CH 2 C 6 H 4 CH 2     2-thiazolyl       418   2-NH 2 CH 2 C 6 H 4 CH 2     2-pyrazolyl       419   2-NH 2 CH 2 C 6 H 4 CH 2     5-isoquinolyl       420   2-NH 2 CH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         421   2-NH 2 CH 2 C 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         422   2-NH 2 CH 2 C 6 H 4 CH 2     2-imidazolyl       423   2-NH 2 CH 2 C 6 H 4 CH 2     2-oxazolyl       424   2-NH 2 CH 2 C 6 H 4 CH 2     4-isoxazolyl       425   2-NH 2 CH 2 C 6 H 4 CH 2     4-HOC 6 H 4         426   2-NH 2 CH 2 C 6 H 4 CH 2     3-HOC 6 H 4         427   2-NH 2 CH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         428   2-NH 2 CH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         429   2-NH 2 CH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         430   3-NH 2 CH 2 C 6 H 4 CH 2     4-MeOC 6 H 4         431   3-NH 2 CH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         432   3-NH 2 CH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         433   3-NH 2 CH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         434   3-NH 2 CH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         435   3-NH 2 CH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         436   3-NH 2 CH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         437   3-NH 2 CH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         438   3-NH 2 CH 2 C 6 H 4 CH 2     4-pyridyl       439   3-NH 2 CH 2 C 6 H 4 CH 2     3-pyridyl       440   3-NH 2 CH 2 C 6 H 4 CH 2     2-pyridyl       441   3-NH 2 CH 2 C 6 H 4 CH 2     2-thiazolyl       442   3-NH 2 CH 2 C 6 H 4 CH 2     2-pyrazolyl       443   3-NH 2 CH 2 C 6 H 4 CH 2     5-isoquinolyl       444   3-NH 2 CH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         445   3-NH 2 CH 2 C 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         446   3-NH 2 CH 2 C 6 H 4 CH 2     2-imidazolyl       447   3-NH 2 CH 2 C 6 H 4 CH 2     2-oxazolyl       448   3-NH 2 CH 2 C 6 H 4 CH 2     4-isoxazolyl       449   3-NH 2 CH 2 C 6 H 4 CH 2     4-HOC 6 H 4         450   3-NH 2 CH 2 C 6 H 4 CH 2     3-HOC 6 H 4         451   3-NH 2 CH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         452   3-NH 2 CH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         453   3-NH 2 CH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         454   4-NH 2 CH 2 C 6 H 4 CH 2     4-MeOC 6 H 4         455   4-NH 2 CH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         456   4-NH 2 CH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         457   4-NH 2 CH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         458   4-NH 2 CH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         459   4-NH 2 CH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         460   4-NH 2 CH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         461   4-NH 2 CH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         462   4-NH 2 CH 2 C 6 H 4 CH 2     4-pyridyl       463   4-NH 2 CH 2 C 6 H 4 CH 2     3-pyridyl       464   4-NH 2 CH 2 C 6 H 4 CH 2     2-pyridyl       465   4-NH 2 CH 2 C 6 H 4 CH 2     2-thiazolyl       466   4-NH 2 CH 2 C 6 H 4 CH 2     2-pyrazolyl       467   4-NH 2 CH 2 C 6 H 4 CH 2     5-isoquinolyl       468   4-NH 2 CH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         469   4-NH 2 CH 2 C 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         470   4-NH 2 CH 2 C 6 H 4 CH 2     2-imidazolyl       471   4-NH 2 CH 2 C 6 H 4 CH 2     2-oxazolyl       472   4-NH 2 CH 2 C 6 H 4 CH 2     4-isoxazolyl       473   4-NH 2 CH 2 C 6 H 4 CH 2     4-HOC 6 H 4         474   4-NH 2 CH 2 C 6 H 4 CH 2     3-HOC 6 H 4         475   4-NH 2 CH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         476   4-NH 2 CH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         477   4-NH 2 CH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         478   2-Me 2 NCH 2 C 6 H 4 CH 2     4-MeOC 6 H 4         479   2-Me 2 NCH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         480   2-Me 2 NCH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         481   2-Me 2 NCH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         482   2-Me 2 NCH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         483   2-Me 2 NCH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         484   2-Me 2 NCH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         485   2-Me 2 NCH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         486   2-Me 2 NCH 2 C 6 H 4 CH 2     4-pyridyl       487   2-Me 2 NCH 2 C 6 H 4 CH 2     3-pyridyl       488   2-Me 2 NCH 2 C 6 H 4 CH 2     2-pyridyl       489   2-Me 2 NCH 2 C 6 H 4 CH 2     2-thiazolyl       490   2-Me 2 NCH 2 C 6 H 4 CH 2     2-pyrazolyl       491   2-Me 2 NCH 2 C 6 H 4 CH 2     5-isoquinolyl       492   2-Me 2 NCH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         493   2-Me 2 NCH 2 C 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         494   2-Me 2 NCH 2 C 6 H 4 CH 2     2-imidazolyl       495   2-Me 2 NCH 2 C 6 H 4 CH 2     2-oxazolyl       496   2-Me 2 NCH 2 C 6 H 4 CH 2     4-isoxazolyl       497   2-Me 2 NCH 2 C 6 H 4 CH 2     4-HOC 6 H 4         498   2-Me 2 NCH 2 C 6 H 4 CH 2     3-HOC 6 H 4         499   2-Me 2 NCH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         500   2-Me 2 NCH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         501   2-Me 2 NCH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         502   3-Me 2 NCH 2 C 6 H 4 CH 2     4-MeOC 6 H 4         503   3-Me 2 NCH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         504   3-Me 2 NCH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         505   3-Me 2 NCH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         506   3-Me 2 NCH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         507   3-Me 2 NCH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         508   3-Me 2 NCH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         509   3-Me 2 NCH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         510   3-Me 2 NCH 2 C 6 H 4 CH 2     4-pyridyl       511   3-Me 2 NCH 2 C 6 H 4 CH 2     3-pyridyl       512   3-Me 2 NCH 2 C 6 H 4 CH 2     2-pyridyl       513   3-Me 2 NCH 2 C 6 H 4 CH 2     2-thiazolyl       514   3-Me 2 NCH 2 C 6 H 4 CH 2     2-pyrazolyl       515   3-Me 2 NCH 2 C 6 H 4 CH 2     5-isoquinolyl       516   3-Me 2 NCH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         517   3-Me 2 NCH 2 C 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         518   3-Me 2 NCH 2 C 6 H 4 CH 2     2-imidazolyl       519   3-Me 2 NCH 2 C 6 H 4 CH 2     2-oxazolyl       520   3-Me 2 NCH 2 C 6 H 4 CH 2     4-isoxazolyl       521   3-Me 2 NCH 2 C 6 H 4 CH 2     4-HOC 6 H 4         522   3-Me 2 NCH 2 C 6 H 4 CH 2     3-HOC 6 H 4         523   3-Me 2 NCH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         524   3-Me 2 NCH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         525   3-Me 2 NCH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         526   4-Me 2 NCH 2 C 6 H 4 CH 2     4-MeOC 6 H 4         527   4-Me 2 NCH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         528   4-Me 2 NCH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         529   4-Me 2 NCH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         530   4-Me 2 NCH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         531   4-Me 2 NCH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         532   4-Me 2 NCH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         533   4-Me 2 NCH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         534   4-Me 2 NCH 2 C 6 H 4 CH 2     4-pyridyl       535   4-Me 2 NCH 2 C 6 H 4 CH 2     3-pyridyl       536   4-Me 2 NCH 2 C 6 H 4 CH 2     2-pyridyl       537   4-Me 2 NCH 2 C 6 H 4 CH 2     2-thiazolyl       538   4-Me 2 NCH 2 C 6 H 4 CH 2     2-pyrazolyl       539   4-Me 2 NCH 2 C 6 H 4 CH 2     5-isoquinolyl       540   4-Me 2 NCH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         541   4-Me 2 NCH 2 C 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         542   4-Me 2 NCH 2 C 6 H 4 CH 2     2-imidazolyl       543   4-Me 2 NCH 2 C 6 H 4 CH 2     2-oxazolyl       545   4-Me 2 NCH 2 C 6 H 4 CH 2     4-isoxazolyl       546   4-Me 2 NCH 2 C 6 H 4 CH 2     4-HOC 6 H 4         547   4-Me 2 NCH 2 C 6 H 4 CH 2     3-HOC 6 H 4         548   4-Me 2 NCH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         549   4-Me 2 NCH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         550   4-Me 2 NCH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         551   H   3-MeOC 6 H 4         552   H   4-NH 2 C 6 H 4         553   H   3-NH 2 C 6 H 4         554   H   2-NH 2 C 6 H 4         555   H   4-Me 2 NC 6 H 4         556   H   3-Me 2 NC 6 H 4         557   H   2-Me 2 NC 6 H 4         558   H   3-pyridyl       559   H   2-pyridyl       560   H   2-thiazolyl       561   H   2-pyrazolyl       562   H   5-isoquinolyl       563   H   3,4-methylenedioxyC 6 H 3         564   H   3,4-ethylenedioxyC 6 H 3         565   H   2-imidazolyl       566   H   2-oxazolyl       567   H   4-isoxazolyl       568   H   4-HOC 6 H 4         569   H   3-HOC 6 H 4         570   H   3,4-diHOC 6 H 4         571   H   4-NH 2 CH 2 C 6 H 4         572   H   3-NH 2 CH 2 C 6 H 4         573   Me   3-MeOC 6 H 4         574   Me   4-NH 2 C 6 H 4         575   Me   3-NH 2 C 6 H 4         576   Me   2-NH 2 C 6 H 4         577   Me   4-Me 2 NC 6 H 4         578   Me   3-Me 2 NC 6 H 4         579   Me   2-Me 2 NC 6 H 4         580   Me   3-pyridyl       581   Me   2-pyridyl       582   Me   2-thiazolyl       583   Me   2-pyrazolyl       584   Me   5-isoquinolyl       585   Me   3,4-ethylenedioxyC 6 H 3         586   Me   2-imidazolyl       587   Me   2-oxazolyl       588   Me   4-isoxazolyl       589   Me   3-HOC 6 H 4         590   Me   3,4-diHOC 6 H 4         591   Me   4-NH 2 CH 2 C 6 H 4         592   Me   3-NH 2 CH 2 C 6 H 4         593   Et   3-MeOC 6 H 4         594   Et   4-NH 2 C 6 H 4         595   Et   3-NH 2 C 6 H 4         596   Et   2-NH 2 C 6 H 4         597   Et   4-Me 2 NC 6 H 4         598   Et   3-Me 2 NC 6 H 4         599   Et   2-Me 2 NC 6 H 4         600   Et   4-pyridyl       601   Et   3-pyridyl       602   Et   2-pyridyl       603   Et   2-thiazolyl       604   Et   2-pyrazolyl       605   Et   5-isoquinolyl       606   Et   3,4-methylenedioxyC 6 H 3         607   Et   3,4-ethylenedioxyC 6 H 3         608   Et   2-imidazolyl       609   Et   2-oxazolyl       610   Et   4-isoxazolyl       611   Et   4-HOC 6 H 4         612   Et   3-HOC 6 H 4         613   Et   3,4-diHOC 6 H 4         614   Et   4-NH 2 CH 2 C 6 H 4         615   Et   3-NH 2 CH 2 C 6 H 4         616   Me 2 NCH 2     3-MeOC 6 H 4         617   Me 2 NCH 2     4-NH 2 C 6 H 4         618   Me 2 NCH 2     3-NH 2 C 6 H 4         619   Me 2 NCH 2     2-NH 2 C 6 H 4         620   Me 2 NCH 2     4-Me 2 NC 6 H 4         621   Me 2 NCH 2     3-Me 2 NC 6 H 4         622   Me 2 NCH 2     2-Me 2 NC 6 H 4         623   Me 2 NCH 2     4-pyridyl       624   Me 2 NCH 2     3-pyridyl       625   Me 2 NCH 2     2-pyridyl       626   Me 2 NCH 2     2-thiazolyl       627   Me 2 NCH 2     2-pyrazolyl       628   Me 2 NCH 2     5-isoquinolyl       629   Me 2 NCH 2     3,4-methylenedioxyC 6 H 3         630   Me 2 NCH 2     3,4-ethylenedioxyC 6 H 3         631   Me 2 NCH 2     2-imidazolyl       632   Me 2 NCH 2     2-oxazolyl       633   Me 2 NCH 2     4-isoxazolyl       634   Me 2 NCH 2     4-HOC 6 H 4         635   Me 2 NCH 2     3-HOC 6 H 4         636   Me 2 NCH 2     3,4-diHOC 6 H 4         637   Me 2 NCH 2     4-NH 2 CH 2 C 6 H 4         638   Me 2 NCH 2     3-NH 2 CH 2 C 6 H 4         639   EtNHCH 2     3-MeOC 6 H 4         640   EtNHCH 2     4-NH 2 C 6 H 4         641   EtNHCH 2     3-NH 2 C 6 H 4         642   EtNHCH 2     2-NH 2 C 6 H 4         643   EtNHCH 2     4-Me 2 NC 6 H 4         644   EtNHCH 2     3-Me 2 NC 6 H 4         645   EtNHCH 2     2-Me 2 NC 6 H 4         646   EtNHCH 2     4-pyridyl       647   EtNHCH 2     3-pyridyl       648   EtNHCH 2     2-pyridyl       649   EtNHCH 2     2-thiazolyl       650   EtNHCH 2     2-pyrazolyl       651   EtNHCH 2     5-isoquinolyl       652   EtNHCH 2     3,4-methylenedioxyC 6 H 3         653   EtNHCH 2     3,4-ethylenedioxyC 6 H 3         654   EtNHCH 2     2-imidazolyl       655   EtNHCH 2     2-oxazolyl       656   EtNHCH 2     4-isoxazolyl       657   EtNHCH 2     4-HOC 6 H 4         658   EtNHCH 2     3-HOC 6 H 4         659   EtNHCH 2     3,4-diHOC 6 H 4         660   EtNHCH 2     4-NH 2 CH 2 C 6 H 4         661   EtNHCH 2     3-NH 2 CH 2 C 6 H 4         662   HOCH 2 CH 2 NHCH 2     3-MeOC 6 H 4         663   HOCH 2 CH 2 NHCH 2     4-NH 2 C 6 H 4         664   HOCH 2 CH 2 NHCH 2     3-NH 2 C 6 H 4         665   HOCH 2 CH 2 NHCH 2     2-NH 2 C 6 H 4         666   HOCH 2 CH 2 NHCH 2     4-Me 2 NC 6 H 4         667   HOCH 2 CH 2 NHCH 2     3-Me 2 NC 6 H 4         668   HOCH 2 CH 2 NHCH 2     2-Me 2 NC 6 H 4         669   HOCH 2 CH 2 NHCH 2     4-pyridyl       670   HOCH 2 CH 2 NHCH 2     3-pyridyl       671   HOCH 2 CH 2 NHCH 2     2-pyridyl       672   HOCH 2 CH 2 NHCH 2     2-thiazolyl       673   HOCH 2 CH 2 NHCH 2     2-pyrazolyl       674   HOCH 2 CH 2 NHCH 2     5-isoquinolyl       675   HOCH 2 CH 2 NHCH 2     3,4-methylenedioxyC 6 H 3         676   HOCH 2 CH 2 NHCH 2     3,4-ethylenedioxyC 6 H 3         677   HOCH 2 CH 2 NHCH 2     2-imidazolyl       678   HOCH 2 CH 2 NHCH 2     2-oxazolyl       679   HOCH 2 CH 2 NHCH 2     4-isoxazolyl       680   HOCH 2 CH 2 NHCH 2     4-HOC 6 H 4         681   HOCH 2 CH 2 NHCH 2     3-HOC 6 H 4         682   HOCH 2 CH 2 NHCH 2     3,4-diHOC 6 H 4         683   HOCH 2 CH 2 NHCH 2     4-NH 2 CH 2 C 6 H 4         684   HOCH 2 CH 2 NHCH 2     3-NH 2 CH 2 C 6 H 4         685   H 2 NCH 2 CH 2 NHCH 2     4-MeOC 6 H 4         686   H 2 NCH 2 CH 2 NHCH 2     3-MeOC 6 H 4         687   H 2 NCH 2 CH 2 NHCH 2     4-NH 2 C 6 H 4         688   H 2 NCH 2 CH 2 NHCH 2     3-NH 2 C 6 H 4         689   H 2 NCH 2 CH 2 NHCH 2     2-NH 2 C 6 H 4         690   H 2 NCH 2 CH 2 NHCH 2     4-Me 2 NC 6 H 4         691   H 2 NCH 2 CH 2 NHCH 2     3-Me 2 NC 6 H 4         692   H 2 NCH 2 CH 2 NHCH 2     2-Me 2 NC 6 H 4         693   H 2 NCH 2 CH 2 NHCH 2     4-pyridyl       694   H 2 NCH 2 CH 2 NHCH 2     3-pyridyl       695   H 2 NCH 2 CH 2 NHCH 2     2-pyridyl       696   H 2 NCH 2 CH 2 NHCH 2     2-thiazolyl       697   H 2 NCH 2 CH 2 NHCH 2     2-pyrazolyl       698   H 2 NCH 2 CH 2 NHCH 2     5-isoquinolyl       699   H 2 NCH 2 CH 2 NHCH 2     3,4-methylenedioxyC 6 H 3         700   H 2 NCH 2 CH 2 NHCH 2     3,4-ethylenedioxyC 6 H 3         701   H 2 NCH 2 CH 2 NHCH 2     2-imidazolyl       702   H 2 NCH 2 CH 2 NHCH 2     2-oxazolyl       703   H 2 NCH 2 CH 2 NHCH 2     4-isoxazolyl       704   H 2 NCH 2 CH 2 NHCH 2     4-HOC 6 H 4         705   H 2 NCH 2 CH 2 NHCH 2     3-HOC 6 H 4         706   H 2 NCH 2 CH 2 NHCH 2     3,4-diHOC 6 H 4         707   H 2 NCH 2 CH 2 NHCH 2     4-NH 2 CH 2 C 6 H 4         708   H 2 NCH 2 CH 2 NHCH 2     3-NH 2 CH 2 C 6 H 4         709   Me 2 NCH 2 CH 2 NHCH 2     4-MeOC 6 H 4         710   Me 2 NCH 2 CH 2 NHCH 2     3-MeOC 6 H 4         711   Me 2 NCH 2 CH 2 NHCH 2     4-NH 2 C 6 H 4         712   Me 2 NCH 2 CH 2 NHCH 2     3-NH 2 C 6 H 4         713   Me 2 NCH 2 CH 2 NHCH 2     2-NH 2 C 6 H 4         714   Me 2 NCH 2 CH 2 NHCH 2     4-Me 2 NC 6 H 4         715   Me 2 NCH 2 CH 2 NHCH 2     3-Me 2 NC 6 H 4         716   Me 2 NCH 2 CH 2 NHCH 2     2-Me 2 NC 6 H 4         717   Me 2 NCH 2 CH 2 NHCH 2     4-pyridyl       718   Me 2 NCH 2 CH 2 NHCH 2     3-pyridyl       719   Me 2 NCH 2 CH 2 NHCH 2     2-pyridyl       720   Me 2 NCH 2 CH 2 NHCH 2     2-thiazolyl       721   Me 2 NCH 2 CH 2 NHCH 2     2-pyrazolyl       722   Me 2 NCH 2 CH 2 NHCH 2     5-isoquinolyl       723   Me 2 NCH 2 CH 2 NHCH 2     3,4-methylenedioxyC 6 H 3         724   Me 2 NCH 2 CH 2 NHCH 2     3,4-ethylenedioxyC 6 H 3         725   Me 2 NCH 2 CH 2 NHCH 2     2-imidazolyl       726   Me 2 NCH 2 CH 2 NHCH 2     2-oxazolyl       727   Me 2 NCH 2 CH 2 NHCH 2     4-isoxazolyl       728   Me 2 NCH 2 CH 2 NHCH 2     4-HOC 6 H 4         729   Me 2 NCH 2 CH 2 NHCH 2     3-HOC 6 H 4         730   Me 2 NCH 2 CH 2 NHCH 2     3,4-diHOC 6 H 4         731   Me 2 NCH 2 CH 2 NHCH 2     4-NH 2 CH 2 C 6 H 4         732   Me 2 NCH 2 CH 2 NHCH 2     3-NH 2 CH 2 C 6 H 4         733   1-morpholinylmethyl   3-MeOC 6 H 4         734   1-morpholinylmethyl   4-NH 2 C 6 H 4         735   1-morpholinylmethyl   3-NH 2 C 6 H 4         736   1-morpholinylmethyl   2-NH 2 C 6 H 4         737   1-morpholinylmethyl   4-Me 2 NC 6 H 4         738   1-morpholinylmethyl   3-Me 2 NC 6 H 4         739   1-morpholinylmethyl   2-Me 2 NC 6 H 4         740   1-morpholinylmethyl   4-pyridyl       741   1-morpholinylmethyl   3-pyridyl       742   1-morpholinylmethyl   2-pyridyl       743   1-morpholinylmethyl   2-thiazolyl       744   1-morpholinylmethyl   2-pyrazolyl       745   1-morpholinylmethyl   5-isoquinolyl       746   1-morpholinylmethyl   3,4-methylenedioxyC 6 H 3         747   1-morpholinylmethyl   3,4-ethylenedioxyC 6 H 3         748   1-morpholinylmethyl   2-imidazolyl       749   1-morpholinylmethyl   2-oxazolyl       750   1-morpholinylmethyl   4-isoxazolyl       751   1-morpholinylmethyl   4-HOC 6 H 4         752   1-morpholinylmethyl   3-HOC 6 H 4         753   1-morpholinylmethyl   3,4-diHOC 6 H 4         754   1-morpholinylmethyl   4-NH 2 CH 2 C 6 H 4         755   1-morpholinylmethyl   3-NH 2 CH 2 C 6 H 4         756   1-thiomorpholinylmethyl   3-MeOC 6 H 4         757   1-thiomorpholinylmethyl   4-NH 2 C 6 H 4         758   1-thiomorpholinylmethyl   3-NH 2 C 6 H 4         759   1-thiomorpholinylmethyl   2-NH 2 C 6 H 4         760   1-thiomorpholinylmethyl   4-Me 2 NC 6 H 4         761   1-thiomorpholinylmethyl   3-Me 2 NC 6 H 4         762   1-thiomorpholinylmethyl   2-Me 2 NC 6 H 4         763   1-thiomorpholinylmethyl   4-pyridyl       764   1-thiomorpholinylmethyl   3-pyridyl       765   1-thiomorpholinylmethyl   2-pyridyl       766   1-thiomorpholinylmethyl   2-thiazolyl       767   1-thiomorpholinylmethyl   2-pyrazolyl       768   1-thiomorpholinylmethyl   5-isoquinolyl       769   1-thiomorpholinylmethyl   3,4-methylenedioxyC 6 H 3         770   1-thiomorpholinylmethyl   3,4-ethylenedioxyC 6 H 3         771   1-thiomorpholinylmethyl   2-imidazolyl       772   1-thiomorpholinylmethyl   2-oxazolyl       773   1-thiomorpholinylmethyl   4-isoxazolyl       774   1-thiomorpholinylmethyl   4-HOC 6 H 4         775   1-thiomorpholinylmethyl   3-HOC 6 H 4         776   1-thiomorpholinylmethyl   3,4-diHOC 6 H 4         777   1-thiomorpholinylmethyl   4-NH 2 CH 2 C 6 H 4         778   1-thiomorpholinylmethyl   3-NH 2 CH 2 C 6 H 4         779   1-piperazinylmethyl   3-MeOC 6 H 4         780   1-piperazinylmethyl   4-NH 2 C 6 H 4         781   1-piperazinylmethyl   3-NH 2 C 6 H 4         782   1-piperazinylmethyl   2-NH 2 C 6 H 4         783   1-piperazinylmethyl   4-Me 2 NC 6 H 4         784   1-piperazinylmethyl   3-Me 2 NC 6 H 4         785   1-piperazinylmethyl   2-Me 2 NC 6 H 4         786   1-piperazinylmethyl   4-pyridyl       787   1-piperazinylmethyl   3-pyridyl       788   1-piperazinylmethyl   2-pyridyl       789   1-piperazinylmethyl   2-thiazolyl       790   1-piperazinylmethyl   2-pyrazolyl       791   1-piperazinylmethyl   5-isoquinolyl       792   1-piperazinylmethyl   3,4-methylenedioxyC 6 H 3         793   1-piperazinylmethyl   3,4-ethylenedioxyC 6 H 3         794   1-piperazinylmethyl   2-imidazolyl       795   1-piperazinylmethyl   2-oxazolyl       796   1-piperazinylmethyl   4-isoxazolyl       797   1-piperazinylmethyl   4-HOC 6 H 4         798   1-piperazinylmethyl   3-HOC 6 H 4         799   1-piperazinylmethyl   3,4-diHOC 6 H 4         800   1-piperazinylmethyl   4-NH 2 CH 2 C 6 H 4         801   1-piperazinylmethyl   3-NH 2 CH 2 C 6 H 4                      
         [0317]    [0317]                                           TABLE 3                                                                                  Example               Number   R 1     R 2                      802   2-pyridylmethyl   4-MeOC 6 H 4         803   2-pyridylmethyl   3-MeOC 6 H 4         804   2-pyridylmethyl   4-NH 2 C 6 H 4         805   2-pyridylmethyl   3-NH 2 C 6 H 4         806   2-pyridylmethyl   2-NH 2 C 6 H 4         807   2-pyridylmethyl   4-Me 2 NC 6 H 4         808   2-pyridylmethyl   3-Me 2 NC 6 H 4         809   2-pyridylmethyl   2-Me 2 NC 6 H 4         810   2-pyridylmethyl   4-pyridyl       811   2-pyridylmethyl   3-pyridyl       812   2-pyridylmethyl   2-pyridyl       813   2-pyridylmethyl   2-thiazolyl       814   2-pyridylmethyl   2-pyrazolyl       815   2-pyridylmethyl   5-isoquinolyl       816   2-pyridylmethyl   3,4-methylenedioxyC 6 H 3         817   2-pyridylmethyl   3,4-ethylenedioxyC 6 H 3         818   2-pyridylmethyl   2-imidazolyl       819   2-pyridylmethyl   2-oxazolyl       820   2-pyridylmethyl   4-isoxazolyl       821   2-pyridylmethyl   4-HOC 6 H 4         822   2-pyridylmethyl   3-HOC 6 H 4         823   2-pyridylmethyl   3,4-diHOC 6 H 4         824   2-pyridylmethyl   4-NH 2 CH 2 C 6 H 4         825   2-pyridylmethyl   3-NH 2 CH 2 C 6 H 4         826   3-pyridylmethyl   4-MeOC 6 H 4         827   3-pyridylmethyl   3-MeOC 6 H 4         828   3-pyridylmethyl   4-NH 2 C 6 H 4         829   3-pyridylmethyl   3-NH 2 C 6 H 4         830   3-pyridylmethyl   2-NH 2 C 6 H 4         831   3-pyridylmethyl   4-Me 2 NC 6 H 4         832   3-pyridylmethyl   3-Me 2 NC 6 H 4         833   3-pyridylmethyl   2-Me 2 NC 6 H 4         834   3-pyridylmethyl   4-pyridyl       835   3-pyridylmethyl   3-pyridyl       836   3-pyridylmethyl   2-pyridyl       837   3-pyridylmethyl   2-thiazolyl       838   3-pyridylmethyl   2-pyrazolyl       839   3-pyridylmethyl   5-isoquinolyl       840   3-pyridylmethyl   3,4-methylenedioxyC 6 H 3         841   3-pyridylmethyl   3,4-ethylenedioxyC 6 H 3         842   3-pyridylmethyl   2-imidazolyl       843   3-pyridylmethyl   2-oxazolyl       844   3-pyridylmethyl   4-isoxazolyl       845   3-pyridylmethyl   4-HOC 6 H 4         846   3-pyridylmethyl   3-HOC 6 H 4         847   3-pyridylmethyl   3,4-diHOC 6 H 4         848   3-pyridylmethyl   4-NH 2 CH 2 C 6 H 4         849   3-pyridylmethyl   3-NH 2 CH 2 C 6 H 4         850   4-pyridylmethyl   4-MeOC 6 H 4         851   4-pyridylmethyl   3-MeOC 6 H 4         852   4-pyridylmethyl   4-NH 2 C 6 H 4         853   4-pyridylmethyl   3-NH 2 C 6 H 4         854   4-pyridylmethyl   2-NH 2 C 6 H 4         855   4-pyridylmethyl   4-Me 2 NC 6 H 4         856   4-pyridylmethyl   3-Me 2 NC 6 H 4         857   4-pyridylmethyl   2-Me 2 NC 6 H 4         858   4-pyridylmethyl   4-pyridyl       859   4-pyridylmethyl   3-pyridyl       860   4-pyridylmethyl   2-pyridyl       861   4-pyridylmethyl   2-thiazolyl       862   4-pyridylmethyl   2-pyrazolyl       863   4-pyridylmethyl   5-isoquinolyl       864   4-pyridylmethyl   3,4-methylenedioxyC 6 H 3         865   4-pyridylmethyl   3,4-ethylenedioxyC 6 H 3         866   4-pyridylmethyl   2-imidazolyl       867   4-pyridylmethyl   2-oxazolyl       868   4-pyridylmethyl   4-isoxazolyl       869   4-pyridylmethyl   4-HOC 6 H 4         870   4-pyridylmethyl   3-HOC 6 H 4         871   4-pyridylmethyl   3,4-diHOC 6 H 4         872   4-pyridylmethyl   4-NH 2 CH 2 C 6 H 4         873   4-pyridylmethyl   3-NH 2 CH 2 C 6 H 4         874   2-NH 2 C 6 H 4     4-MeOC 6 H 4         875   2-NH 2 C 6 H 4     3-MeOC 6 H 4         876   2-NH 2 C 6 H 4     4-NH 2 C 6 H 4         877   2-NH 2 C 6 H 4     3-NH 2 C 6 H 4         878   2-NH 2 C 6 H 4     2-NH 2 C 6 H 4         879   2-NH 2 C 6 H 4     4-Me 2 NC 6 H 4         880   2-NH 2 C 6 H 4     3-Me 2 NC 6 H 4         881   2-NH 2 C 6 H 4     2-Me 2 NC 6 H 4         882   2-NH 2 C 6 H 4     4-pyridyl       883   2-NH 2 C 6 H 4     3-pyridyl       884   2-NH 2 C 6 H 4     2-pyridyl       885   2-NH 2 C 6 H 4     2-thiazolyl       886   2-NH 2 C 6 H 4     2-pyrazolyl       887   2-NH 2 C 6 H 4     5-isoquinolyl       888   2-NH 2 C 6 H 4     3,4-methylenedioxyC 6 H 3         889   2-NH 2 C 6 H 4     3,4-ethylenedioxyC 6 H 3         890   2-NH 2 C 6 H 4     2-imidazolyl       891   2-NH 2 C 6 H 4     2-oxazolyl       892   2-NH 2 C 6 H 4     4-isoxazolyl       893   2-NH 2 C 6 H 4     4-HOC 6 H 4         894   2-NH 2 C 6 H 4     3-HOC 6 H 4         895   2-NH 2 C 6 H 4     3,4-diHOC 6 H 4         896   2-NH 2 C 6 H 4     4-NH 2 CH 2 C 6 H 4         897   2-NH 2 C 6 H 4     3-NH 2 CH 2 C 6 H 4         898   3-NH 2 C 6 H 4     4-MeOC 6 H 4         899   3-NH 2 C 6 H 4     3-MeOC 6 H 4         900   3-NH 2 C 6 H 4     4-NH 2 C 6 H 4         901   3-NH 2 C 6 H 4     3-NH 2 C 6 H 4         902   3-NH 2 C 6 H 4     2-NH 2 C 6 H 4         903   3-NH 2 C 6 H 4     4-Me 2 NC 6 H 4         904   3-NH 2 C 6 H 4     3-Me 2 NC 6 H 4         905   3-NH 2 C 6 H 4     2-Me 2 NC 6 H 4         906   3-NH 2 C 6 H 4     4-pyridyl       907   3-NH 2 C 6 H 4     3-pyridyl       908   3-NH 2 C 6 H 4     2-pyridyl       909   3-NH 2 C 6 H 4     2-thiazolyl       910   3-NH 2 C 6 H 4     2-pyrazolyl       911   3-NH 2 C 6 H 4     5-isoquinolyl       912   3-NH 2 C 6 H 4     3,4-methylenedioxyC 6 H 3         913   3-NH 2 C 6 H 4     3,4-ethylenedioxyC 6 H 3         914   3-NH 2 C 6 H 4     2-imidazolyl       915   3-NH 2 C 6 H 4     2-oxazolyl       916   3-NH 2 C 6 H 4     4-isoxazolyl       917   3-NH 2 C 6 H 4     4-HOC 6 H 4         918   3-NH 2 C 6 H 4     3-HOC 6 H 4         919   3-NH 2 C 6 H 4     3,4-diHOC 6 H 4         920   3-NH 2 C 6 H 4     4-NH 2 CH 2 C 6 H 4         921   3-NH 2 C 6 H 4     3-NH 2 CH 2 C 6 H 4         922   4-NH 2 C 6 H 4     4-MeOC 6 H 4         923   4-NH 2 C 6 H 4     3-MeOC 6 H 4         924   4-NH 2 C 6 H 4     4-NH 2 C 6 H 4         925   4-NH 2 C 6 H 4     3-NH 2 C 6 H 4         926   4-NH 2 C 6 H 4     2-NH 2 C 6 H 4         927   4-NH 2 C 6 H 4     4-Me 2 NC 6 H 4         928   4-NH 2 C 6 H 4     3-Me 2 NC 6 H 4         930   4-NH 2 C 6 H 4     2-Me 2 NC 6 H 4         931   4-NH 2 C 6 H 4     4-pyridyl       932   4-NH 2 C 6 H 4     3-pyridyl       933   4-NH 2 C 6 H 4     2-pyridyl       934   4-NH 2 C 6 H 4     2-thiazolyl       935   4-NH 2 C 6 H 4     2-pyrazolyl       936   4-NH 2 C 6 H 4     5-isoquinolyl       937   4-NH 2 C 6 H 4     3,4-methylenedioxyC 6 H 3         938   4-NH 2 C 6 H 4     3,4-ethylenedioxyC 6 H 3         939   4-NH 2 C 6 H 4     2-imidazolyl       940   4-NH 2 C 6 H 4     2-oxazolyl       941   4-NH 2 C 6 H 4     4-isoxazolyl       942   4-NH 2 C 6 H 4     4-HOC 6 H 4         943   4-NH 2 C 6 H 4     3-HOC 6 H 4         944   4-NH 2 C 6 H 4     3,4-diHOC 6 H 4         945   4-NH 2 C 6 H 4     4-NH 2 CH 2 C 6 H 4         946   4-NH 2 C 6 H 4     3-NH 2 CH 2 C 6 H 4         947   2-MeOC 6 H 4     4-MeOC 6 H 4         948   2-MeOC 6 H 4     3-MeOC 6 H 4         949   2-MeOC 6 H 4     4-NH 2 C 6 H 4         950   2-MeOC 6 H 4     3-NH 2 C 6 H 4         951   2-MeOC 6 H 4     2-NH 2 C 6 H 4         952   2-MeOC 6 H 4     4-Me 2 NC 6 H 4         953   2-MeOC 6 H 4     3-Me 2 NC 6 H 4         954   2-MeOC 6 H 4     2-Me 2 NC 6 H 4         955   2-MeOC 6 H 4     4-pyridyl       956   2-MeOC 6 H 4     3-pyridyl       957   2-MeOC 6 H 4     2-pyridyl       958   2-MeOC 6 H 4     2-thiazolyl       959   2-MeOC 6 H 4     2-pyrazolyl       960   2-MeOC 6 H 4     5-isoquinolyl       961   2-MeOC 6 H 4     3,4-methylenedioxyC 6 H 3         962   2-MeOC 6 H 4     3-4-ethylenedioxyC 6 H 3         963   2-MeOC 6 H 4     2-imidazolyl       964   2-MeOC 6 H 4     2-oxazolyl       965   2-MeOC 6 H 4     4-isoxazolyl       966   2-MeOC 6 H 4     4-HOC 6 H 4         967   2-MeOC 6 H 4     3-HOC 6 H 4         968   2-MeOC 6 H 4     3,4-diHOC 6 H 4         969   2-MeOC 6 H 4     4-NH 2 CH 2 C 6 H 4         970   2-MeOC 6 H 4     3-NH 2 CH 2 C 6 H 4         971   3-MeOC 6 H 4     4-MeOC 6 H 4         972   3-MeOC 6 H 4     3-MeOC 6 H 4         973   3-MeOC 6 H 4     4-NH 2 C 6 H 4         974   3-MeOC 6 H 4     3-NH 2 C 6 H 4         975   3-MeOC 6 H 4     2-NH 2 C 6 H 4         976   3-MeOC 6 H 4     4-Me 2 NC 6 H 4         977   3-MeOC 6 H 4     3-Me 2 NC 6 H 4         978   3-MeOC 6 H 4     2-Me 2 NC 6 H 4         979   3-MeOC 6 H 4     4-pyridyl       980   3-MeOC 6 H 4     3-pyridyl       981   3-MeOC 6 H 4     2-pyridyl       982   3-MeOC 6 H 4     2-thiazolyl       983   3-MeOC 6 H 4     2-pyrazolyl       984   3-MeOC 6 H 4     5-isoquinolyl       985   3-MeOC 6 H 4     3,4-methylenedioxyC 6 H 3         986   3-MeOC 6 H 4     3,4-ethylenedioxyC 6 H 3         987   3-MeOC 6 H 4     2-imidazolyl       988   3-MeOC 6 H 4     2-oxazolyl       989   3-MeOC 6 H 4     4-isoxazolyl       990   3-MeOC 6 H 4     4-HOC 6 H 4         991   3-MeOC 6 H 4     3-HOC 6 H 4         992   3-MeOC 6 H 4     3,4-diHOC 6 H 4         993   3-MeOC 6 H 4     4-NH 2 CH 2 C 6 H 4         994   3-MeOC 6 H 4     3-NH 2 CH 2 C 6 H 4         995   4-MeOC 6 H 4     4-MeOC 6 H 4         996   4-MeOC 6 H 4     3-MeOC 6 H 4         997   4-MeOC 6 H 4     4-NH 2 C 6 H 4         998   4-MeOC 6 H 4     3-NH 2 C 6 H 4         999   4-MeOC 6 H 4     2-NH 2 C 6 H 4         1000   4-MeOC 6 H 4     4-Me 2 NC 6 H 4         1001   4-MeOC 6 H 4     3-Me 2 NC 6 H 4         1002   4-MeOC 6 H 4     2-Me 2 NC 6 H 4         1003   4-MeOC 6 H 4     4-pyridyl       1004   4-MeOC 6 H 4     3-pyridyl       1005   4-MeOC 6 H 4     2-pyridyl       1006   4-MeOC 6 H 4     2-thiazolyl       1007   4-MeOC 6 H 4     2-pyrazolyl       1008   4-MeOC 6 H 4     5-isoquinolyl       1009   4-MeOC 6 H 4     3,4-methylenedioxyC 6 H 3         1010   4-MeOC 6 H 4     3,4-ethylenedioxyC 6 H 3         1011   4-MeOC 6 H 4     2-imidazolyl       1012   4-MeOC 6 H 4     2-oxazolyl       1013   4-MeOC 6 H 4     4-isoxazolyl       1014   4-MeOC 6 H 4     4-HOC 6 H 4         1015   4-MeOC 6 H 4     3-HOC 6 H 4         1016   4-MeOC 6 H 4     3,4-diHOC 6 H 4         1017   4-MeOC 6 H 4     4-NH 2 CH 2 C 6 H 4         1018   4-MeOC 6 H 4     3-NH 2 CH 2 C 6 H 4         1019   2-HOC 6 H 4     4-MeOC 6 H 4         1020   2-HOC 6 H 4     3-MeOC 6 H 4         1021   2-HOC 6 H 4     4-NH 2 C 6 H 4         1022   2-HOC 6 H 4     3-NH 2 C 6 H 4         1023   2-HOC 6 H 4     2-NH 2 C 6 H 4         1024   2-HOC 6 H 4     4-Me 2 NC 6 H 4         1025   2-HOC 6 H 4     3-Me 2 NC 6 H 4         1026   2-HOC 6 H 4     2-Me 2 NC 6 H 4         1027   2-HOC 6 H 4     4-pyridyl       1028   2-HOC 6 H 4     3-pyridyl       1029   2-HOC 6 H 4     2-pyridyl       1030   2-HOC 6 H 4     2-thiazolyl       1031   2-HOC 6 H 4     2-pyrazolyl       1032   2-HOC 6 H 4     5-isoquinolyl       1033   2-HOC 6 H 4     3,4-methylenedioxyC 6 H 3         1034   2-HOC 6 H 4     3,4-ethylenedioxyC 6 H 3         1035   2-HOC 6 H 4     2-imidazolyl       1036   2-HOC 6 H 4     2-oxazolyl       1037   2-HOC 6 H 4     4-isoxazolyl       1038   2-HOC 6 H 4     4-HOC 6 H 4         1039   2-HOC 6 H 4     3-HOC 6 H 4         1040   2-HOC 6 H 4     3,4-diHOC 6 H 4         1041   2-HOC 6 H 4     4-NH 2 CH 2 C 6 H 4         1042   2-HOC 6 H 4     3-NH 2 CH 2 C 6 H 4         1043   3-HOC 6 H 4     4-MeOC 6 H 4         1044   3-HOC 6 H 4     3-MeOC 6 H 4         1045   3-HOC 6 H 4     4-NH 2 C 6 H 4         1046   3-HOC 6 H 4     3-NH 2 C 6 H 4         1047   3-HOC 6 H 4     2-NH 2 C 6 H 4         1048   3-HOC 6 H 4     4-Me 2 NC 6 H 4         1049   3-HOC 6 H 4     3-Me 2 NC 6 H 4         1050   3-HOC 6 H 4     2-Me 2 NC 6 H 4         1051   3-HOC 6 H 4     4-pyridyl       1052   3-HOC 6 H 4     3-pyridyl       1053   3-HOC 6 H 4     2-pyridyl       1054   3-HOC 6 H 4     2-thiazolyl       1055   3-HOC 6 H 4     2-pyrazolyl       1056   3-HOC 6 H 4     5-isoquinolyl       1057   3-HOC 6 H 4     3,4-methylenedioxyC 6 H 3         1058   3-HOC 6 H 4     3,4-ethylenedioxyC 6 H 3         1059   3-HOC 6 H 4     2-imidazolyl       1060   3-HOC 6 H 4     2-oxazolyl       1061   3-HOC 6 H 4     4-isoxazolyl       1062   3-HOC 6 H 4     4-HOC 6 H 4         1063   3-HOC 6 H 4     3-HOC 6 H 4         1064   3-HOC 6 H 4     3,4-diHOC 6 H 4         1065   3-HOC 6 H 4     4-NH 2 CH 2 C 6 H 4         1066   3-HOC 6 H 4     3-NH 2 CH 2 C 6 H 4         1067   4-HOC 6 H 4     4-MeOC 6 H 4         1068   4-HOC 6 H 4     3-MeOC 6 H 4         1069   4-HOC 6 H 4     4-NH 2 C 6 H 4         1070   4-HOC 6 H 4     3-NH 2 C 6 H 4         1071   4-HOC 6 H 4     2-NH 2 C 6 H 4         1072   4-HOC 6 H 4     4-Me 2 NC 6 H 4         1073   4-HOC 6 H 4     3-Me 2 NC 6 H 4         1074   4-HOC 6 H 4     2-Me 2 NC 6 H 4         1075   4-HOC 6 H 4     4-pyridyl       1076   4-HOC 6 H 4     3-pyridyl       1077   4-HOC 6 H 4     2-pyridyl       1078   4-HOC 6 H 4     2-thiazolyl       1079   4-HOC 6 H 4     2-pyrazolyl       1080   4-HOC 6 H 4     5-isoquinolyl       1081   4-HOC 6 H 4     3,4-methylenedioxyC 6 H 3         1082   4-HOC 6 H 4     3,4-ethylenedioxyC 6 H 3         1083   4-HOC 6 H 4     2-imidazolyl       1084   4-HOC 6 H 4     2-oxazolyl       1085   4-HOC 6 H 4     4-isoxazolyl       1086   4-HOC 6 H 4     4-HOC 6 H 4         1087   4-HOC 6 H 4     3-HOC 6 H 4         1088   4-HOC 6 H 4     3,4-diHOC 6 H 4         1089   4-HOC 6 H 4     4-NH 2 CH 2 C 6 H 4         1090   4-HOC 6 H 4     3-NH 2 CH 2 C 6 H 4         1091   4-ClC 6 H 4     4-MeOC 6 H 4         1092   4-ClC 6 H 4     3-MeOC 6 H 4         1093   4-ClC 6 H 4     4-NH 2 C 6 H 4         1094   4-ClC 6 H 4     3-NH 2 C 6 H 4         1095   4-ClC 6 H 4     2-NH 2 C 6 H 4         1096   4-ClC 6 H 4     4-Me 2 NC 6 H 4         1097   4-ClC 6 H 4     3-Me 2 NC 6 H 4         1098   4-ClC 6 H 4     2-Me 2 NC 6 H 4         1099   4-ClC 6 H 4     4-pyridyl       1100   4-ClC 6 H 4     3-pyridyl       1101   4-ClC 6 H 4     2-pyridyl       1102   4-ClC 6 H 4     2-thiazolyl       1103   4-ClC 6 H 4     2-pyrazolyl       1104   4-ClC 6 H 4     5-isoquinolyl       1105   4-ClC 6 H 4     3,4-methylenedioxyC 6 H 3         1106   4-ClC 6 H 4     3,4-ethylenedioxyC 6 H 3         1107   4-ClC 6 H 4     2-imidazolyl       1108   4-ClC 6 H 4     2-oxazolyl       1109   4-ClC 6 H 4     4-isoxazolyl       1110   4-ClC 6 H 4     4-HOC 6 H 4         1111   4-ClC 6 H 4     3-HOC 6 H 4         1112   4-ClC 6 H 4     3,4-diHOC 6 H 4         1113   4-ClC 6 H 4     4-NH 2 CH 2 C 6 H 4         1114   4-ClC 6 H 4     3-NH 2 CH 2 C 6 H 4         1115   2-NH 2 CH 2 C 6 H 4     4-MeOC 6 H 4         1116   2-NH 2 CH 2 C 6 H 4     3-MeOC 6 H 4         1117   2-NH 2 CH 2 C 6 H 4     4-NH 2 C 6 H 4         1118   2-NH 2 CH 2 C 6 H 4     3-NH 2 C 6 H 4         1119   2-NH 2 CH 2 C 6 H 4     2-NH 2 C 6 H 4         1120   2-NH 2 CH 2 C 6 H 4     4-Me 2 NC 6 H 4         1121   2-NH 2 CH 2 C 6 H 4     3-Me 2 NC 6 H 4         1122   2-NH 2 CH 2 C 6 H 4     2-Me 2 NC 6 H 4         1123   2-NH 2 CH 2 C 6 H 4     4-pyridyl       1124   2-NH 2 CH 2 C 6 H 4     3-pyridyl       1125   2-NH 2 CH 2 C 6 H 4     2-pyridyl       1126   2-NH 2 CH 2 C 6 H 4     2-thiazolyl       1127   2-NH 2 CH 2 C 6 H 4     2-pyrazolyl       1128   2-NH 2 CH 2 C 6 H 4     5-isoquinolyl       1129   2-NH 2 CH 2 C 6 H 4     3,4-methylenedioxyC 6 H 3         1130   2-NH 2 CH 2 C 6 H 4     3,4-ethylenedioxyC 6 H 3         1131   2-NH 2 CH 2 C 6 H 4     2-imidazolyl       1132   2-NH 2 CH 2 C 6 H 4     2-oxazolyl       1133   2-NH 2 CH 2 C 6 H 4     4-isoxazolyl       1134   2-NH 2 CH 2 C 6 H 4     4-HOC 6 H 4         1135   2-NH 2 CH 2 C 6 H 4     3-HOC 6 H 4         1136   2-NH 2 CH 2 C 6 H 4     3,4-diHOC 6 H 4         1137   2-NH 2 CH 2 C 6 H 4     4-NH 2 CH 2 C 6 H 4         1138   2-NH 2 CH 2 C 6 H 4     3-NH 2 CH 2 C 6 H 4         1139   3-NH 2 CH 2 C 6 H 4     4-MeOC 6 H 4         1140   3-NH 2 CH 2 C 6 H 4     3-MeOC 6 H 4         1141   3-NH 2 CH 2 C 6 H 4     4-NH 2 C 6 H 4         1142   3-NH 2 CH 2 C 6 H 4     3-NH 2 C 6 H 4         1143   3-NH 2 CH 2 C 6 H 4     2-NH 2 C 6 H 4         1144   3-NH 2 CH 2 C 6 H 4     4-Me 2 NC 6 H 4         1145   3-NH 2 CH 2 C 6 H 4     3-Me 2 NC 6 H 4         1146   3-NH 2 CH 2 C 6 H 4     2-Me 2 NC 6 H 4         1147   3-NH 2 CH 2 C 6 H 4     4-pyridyl       1148   3-NH 2 CH 2 C 6 H 4     3-pyridyl       1149   3-NH 2 CH 2 C 6 H 4     2-pyridyl       1150   3-NH 2 CH 2 C 6 H 4     2-thiazolyl       1151   3-NH 2 CH 2 C 6 H 4     2-pyrazolyl       1152   3-NH 2 CH 2 C 6 H 4     5-isoquinolyl       1153   3-NH 2 CH 2 C 6 H 4     3,4-methylenedioxyC 6 H 3         1154   3-NH 2 CH 2 C 6 H 4     3,4-ethylenedioxyC 6 H 3         1155   3-NH 2 CH 2 C 6 H 4     2-imidazolyl       1156   3-NH 2 CH 2 C 6 H 4     2-oxazolyl       1157   3-NH 2 CH 2 C 6 H 4     4-isoxazolyl       1158   3-NH 2 CH 2 C 6 H 4     4-HOC 6 H 4         1159   3-NH 2 CH 2 C 6 H 4     3-HOC 6 H 4         1160   3-NH 2 CH 2 C 6 H 4     3,4-diHOC 6 H 4         1161   3-NH 2 CH 2 C 6 H 4     4-NH 2 CH 2 C 6 H 4         1162   3-NH 2 CH 2 C 6 H 4     3-NH 2 CH 2 C 6 H 4         1163   4-NH 2 CH 2 C 6 H 4     4-MeOC 6 H 4         1164   4-NH 2 CH 2 C 6 H 4     3-MeOC 6 H 4         1165   4-NH 2 CH 2 C 6 H 4     4-NH 2 C 6 H 4         1166   4-NH 2 CH 2 C 6 H 4     3-NH 2 C 6 H 4         1167   4-NH 2 CH 2 C 6 H 4     2-NH 2 C 6 H 4         1168   4-NH 2 CH 2 C 6 H 4     4-Me 2 NC 6 H 4         1169   4-NH 2 CH 2 C 6 H 4     3-Me 2 NC 6 H 4         1170   4-NH 2 CH 2 C 6 H 4     2-Me 2 NC 6 H 4         1171   4-NH 2 CH 2 C 6 H 4     4-pyridyl       1172   4-NH 2 CH 2 C 6 H 4     3-pyridyl       1173   4-NH 2 CH 2 C 6 H 4     2-pyridyl       1174   4-NH 2 CH 2 C 6 H 4     2-thiazolyl       1175   4-NH 2 CH 2 C 6 H 4     2-pyrazolyl       1176   4-NH 2 CH 2 C 6 H 4     5-isoquinolyl       1177   4-NH 2 CH 2 C 6 H 4     3,4-methylenedioxyC 6 H 3         1178   4-NH 2 CH 2 C 6 H 4     3,4-ethylenedioxyC 6 H 3         1179   4-NH 2 CH 2 C 6 H 4     2-imidazolyl       1180   4-NH 2 CH 2 C 6 H 4     2-oxazolyl       1181   4-NH 2 CH 2 C 6 H 4     4-isoxazolyl       1182   4-NH 2 CH 2 C 6 H 4     4-HOC 6 H 4         1183   4-NH 2 CH 2 C 6 H 4     3-HOC 6 H 4         1184   4-NH 2 CH 2 C 6 H 4     3,4-diHOC 6 H 4         1185   4-NH 2 CH 2 C 6 H 4     4-NH 2 CH 2 C 6 H 4         1186   4-NH 2 CH 2 C 6 H 4     3-NH 2 CH 2 C 6 H 4         1187   2-Me 2 NCH 2 C 6 H 4     4-MeOC 6 H 4         1188   2-Me 2 NCH 2 C 6 H 4     3-MeOC 6 H 4         1189   2-Me 2 NCH 2 C 6 H 4     4-NH 2 C 6 H 4         1190   2-Me 2 NCH 2 C 6 H 4     3-NH 2 C 6 H 4         1191   2-Me 2 NCH 2 C 6 H 4     2-NH 2 C 6 H 4         1192   2-Me 2 NCH 2 C 6 H 4     4-Me 2 NC 6 H 4         1193   2-Me 2 NCH 2 C 6 H 4     3-Me 2 NC 6 H 4         1194   2-Me 2 NCH 2 C 6 H 4     2-Me 2 NC 6 H 4         1195   2-Me 2 NCH 2 C 6 H 4     4-pyridyl       1196   2-Me 2 NCH 2 C 6 H 4     3-pyridyl       1197   2-Me 2 NCH 2 C 6 H 4     2-pyridyl       1198   2-Me 2 NCH 2 C 6 H 4     2-thiazolyl       1199   2-Me 2 NCH 2 C 6 H 4     2-pyrazolyl       1200   2-Me 2 NCH 2 C 6 H 4     5-isoquinolyl       1201   2-Me 2 NCH 2 C 6 H 4     3,4-methylenedioxyC 6 H 3         1202   2-Me 2 NCH 2 C 6 H 4     3,4-ethylenedioxyC 6 H 3         1203   2-Me 2 NCH 2 C 6 H 4     2-imidazolyl       1204   2-Me 2 NCH 2 C 6 H 4     2-oxazolyl       1205   2-Me 2 NCH 2 C 6 H 4     4-isoxazolyl       1206   2-Me 2 NCH 2 C 6 H 4     4-HOC 6 H 4         1207   2-Me 2 NCH 2 C 6 H 4     3-HOC 6 H 4         1208   2-Me 2 NCH 2 C 6 H 4     3,4-diHOC 6 H 4         1209   2-Me 2 NCH 2 C 6 H 4     4-NH 2 CH 2 C 6 H 4         1210   2-Me 2 NCH 2 C 6 H 4     3-NH 2 CH 2 C 6 H 4         1211   3-Me 2 NCH 2 C 6 H 4     4-MeOC 6 H 4         1212   3-Me 2 NCH 2 C 6 H 4     3-MeOC 6 H 4         1213   3-Me 2 NCH 2 C 6 H 4     4-NH 2 C 6 H 4         1214   3-Me 2 NCH 2 C 6 H 4     3-NH 2 C 6 H 4         1215   3-Me 2 NCH 2 C 6 H 4     2-NH 2 C 6 H 4         1216   3-Me 2 NCH 2 C 6 H 4     4-Me 2 NC 6 H 4         1217   3-Me 2 NCH 2 C 6 H 4     3-Me 2 NC 6 H 4         1218   3-Me 2 NCH 2 C 6 H 4     2-Me 2 NC 6 H 4         1219   3-Me 2 NCH 2 C 6 H 4     4-pyridyl       1220   3-Me 2 NCH 2 C 6 H 4     3-pyridyl       1221   3-Me 2 NCH 2 C 6 H 4     2-pyridyl       1222   3-Me 2 NCH 2 C 6 H 4     2-thiazolyl       1223   3-Me 2 NCH 2 C 6 H 4     2-pyrazolyl       1224   3-Me 2 NCH 2 C 6 H 4     5-isoquinolyl       1225   3-Me 2 NCH 2 C 6 H 4     3,4-methylenedioxyC 6 H 3         1226   3-Me 2 NCH 2 C 6 H 4     3,4-ethylenedioxyC 6 H 3         1227   3-Me 2 NCH 2 C 6 H 4     2-imidazolyl       1228   3-Me 2 NCH 2 C 6 H 4     2-oxazolyl       1229   3-Me 2 NCH 2 C 6 H 4     4-isoxazolyl       1230   3-Me 2 NCH 2 C 6 H 4     4-HOC 6 H 4         1231   3-Me 2 NCH 2 C 6 H 4     3-HOC 6 H 4         1232   3-Me 2 NCH 2 C 6 H 4     3,4-diHOC 6 H 4         1233   3-Me 2 NCH 2 C 6 H 4     4-NH 2 CH 2 C 6 H 4         1234   3-Me 2 NCH 2 C 6 H 4     3-NH 2 CH 2 C 6 H 4         1235   4-Me 2 NCH 2 C 6 H 4     4-MeOC 6 H 4         1236   4-Me 2 NCH 2 C 6 H 4     3-MeOC 6 H 4         1237   4-Me 2 NCH 2 C 6 H 4     4-NH 2 C 6 H 4         1238   4-Me 2 NCH 2 C 6 H 4     3-NH 2 C 6 H 4         1239   4-Me 2 NCH 2 C 6 H 4     2-NH 2 C 6 H 4         1240   4-Me 2 NCH 2 C 6 H 4     4-Me 2 NC 6 H 4         1241   4-Me 2 NCH 2 C 6 H 4     3-Me 2 NC 6 H 4         1242   4-Me 2 NCH 2 C 6 H 4     2-Me 2 NC 6 H 4         1243   4-Me 2 NCH 2 C 6 H 4     4-pyridyl       1244   4-Me 2 NCH 2 C 6 H 4     3-pyridyl       1245   4-Me 2 NCH 2 C 6 H 4     2-pyridyl       1246   4-Me 2 NCH 2 C 6 H 4     2-thiazolyl       1247   4-Me 2 NCH 2 C 6 H 4     2-pyrazolyl       1248   4-Me 2 NCH 2 C 6 H 4     5-isoquinolyl       1249   4-Me 2 NCH 2 C 6 H 4     3,4-methylenedioxyC 6 H 3         1250   4-Me 2 NCH 2 C 6 H 4     3,4-ethylenedioxyC 6 H 3         1251   4-Me 2 NCH 2 C 6 H 4     2-imidazolyl       1252   4-Me 2 NCH 2 C 6 H 4     2-oxazolyl       1253   4-Me 2 NCH 2 C 6 H 4     4-isoxazolyl       1254   4-Me 2 NCH 2 C 6 H 4     4-HOC 6 H 4         1255   4-Me 2 NCH 2 C 6 H 4     3-HOC 6 H 4         1256   4-Me 2 NCH 2 C 6 H 4     3,4-diHOC 6 H 4         1257   4-Me 2 NCH 2 C 6 H 4     4-NH 2 CH 2 C 6 H 4         1258   4-Me 2 NCH 2 C 6 H 4     3-NH 2 CH 2 C 6 H 4         1259   H   4-MeOC 6 H 4         1260   H   3-MeOC 6 H 4         1261   H   4-NH 2 C 6 H 4         1262   H   3-NH 2 C 6 H 4         1263   H   2-NH 2 C 6 H 4         1264   H   4-Me 2 NC 6 H 4         1265   H   3-Me 2 NC 6 H 4         1266   H   2-Me 2 NC 6 H 4         1267   H   4-pyridyl       1268   H   3-pyridyl       1269   H   2-pyridyl       1270   H   2-thiazolyl       1271   H   2-pyrazolyl       1272   H   5-isoquinolyl       1273   H   3,4-methylenedioxyC 6 H 3         1274   H   3,4-ethylenedioxyC 6 H 3         1275   H   2-imidazolyl       1276   H   2-oxazolyl       1277   H   4-isoxazolyl       1278   H   4-HOC 6 H 4         1279   H   3-HOC 6 H 4         1280   H   3,4-diHOC 6 H 4         1281   H   4-NH 2 CH 2 C 6 H 4         1282   H   3-NH 2 CH 2 C 6 H 4         1283   Me   4-MeOC 6 H 4         1284   Me   3-MeOC 6 H 4         1285   Me   4-NH 2 C 6 H 4         1286   Me   3-NH 2 C 6 H 4         1287   Me   2-NH 2 C 6 H 4         1288   Me   4-Me 2 NC 6 H 4         1289   Me   3-Me 2 NC 6 H 4         1290   Me   2-Me 2 NC 6 H 4         1291   Me   4-pyridyl       1292   Me   3-pyridyl       1293   Me   2-pyridyl       1294   Me   2-thiazolyl       1295   Me   2-pyrazolyl       1296   Me   5-isoquinolyl       1297   Me   3,4-methylenedioxyC 6 H 3         1298   Me   3,4-ethylenedioxyC 6 H 3         1299   Me   2-imidazolyl       1300   Me   2-oxazolyl       1301   Me   4-isoxazolyl       1302   Me   4-HOC 6 H 4         1303   Me   3-HOC 6 H 4         1304   Me   3,4-diHOC 6 H 4         1305   Me   4-NH 2 CH 2 C 6 H 4         1306   Me   3-NH 2 CH 2 C 6 H 4         1307   Et   4-MeOC 6 H 4         1308   Et   3-MeOC 6 H 4         1309   Et   4-NH 2 C 6 H 4         1310   Et   3-NH 2 C 6 H 4         1311   Et   2-NH 2 C 6 H 4         1312   Et   4-Me 2 NC 6 H 4         1313   Et   3-Me 2 NC 6 H 4         1314   Et   2-Me 2 NC 6 H 4         1315   Et   4-pyridyl       1316   Et   3-pyridyl       1317   Et   2-pyridyl       1318   Et   2-thiazolyl       1319   Et   2-pyrazolyl       1320   Et   5-isoquinolyl       1321   Et   3,4-methylenedioxyC 6 H 3         1322   Et   3,4-ethylenedioxyC 6 H 3         1323   Et   2-imidazolyl       1324   Et   2-oxazolyl       1325   Et   4-isoxazolyl       1326   Et   4-HOC 6 H 4         1327   Et   3-HOC 6 H 4         1328   Et   3,4-diHOC 6 H 4         1329   Et   4-NH 2 CH 2 C 6 H 4         1330   Et   3-NH 2 CH 2 C 6 H 4         1331   2-NH 2 C 6 H 4 CH 2     4-MeOC 6 H 4         1332   2-NH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         1333   2-NH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         1334   2-NH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         1335   2-NH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         1336   2-NH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         1337   2-NH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         1338   2-NH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         1339   2-NH 2 C 6 H 4 CH 2     4-pyridyl       1340   2-NH 2 C 6 H 4 CH 2     3-pyridyl       1341   2-NH 2 C 6 H 4 CH 2     2-pyridyl       1342   2-NH 2 C 6 H 4 CH 2     2-thiazolyl       1343   2-NH 2 C 6 H 4 CH 2     2-pyrazolyl       1344   2-NH 2 C 6 H 4 CH 2     5-isoquinolyl       1345   2-NH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         1346   2-NH 2 C 6 H 4 CH 2     3-4-ethylenedioxyC 6 H 3         1347   2-NH 2 C 6 H 4 CH 2     2-imidazolyl       1348   2-NH 2 C 6 H 4 CH 2     2-oxazolyl       1349   2-NH 2 C 6 H 4 CH 2     4-isoxazolyl       1350   2-NH 2 C 6 H 4 CH 2     4-HOC 6 H 4         1351   2-NH 2 C 6 H 4 CH 2     3-HOC 6 H 4         1352   2-NH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         1353   2-NH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         1354   2-NH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         1355   3-NH 2 C 6 H 4 CH 2     4-MeOC 6 H 4         1356   3-NH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         1357   3-NH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         1358   3-NH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         1359   3-NH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         1360   3-NH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         1361   3-NH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         1362   3-NH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         1363   3-NH 2 C 6 H 4 CH 2     4-pyridyl       1364   3-NH 2 C 6 H 4 CH 2     3-pyridyl       1365   3-NH 2 C 6 H 4 CH 2     2-pyridyl       1366   3-NH 2 C 6 H 4 CH 2     2-thiazolyl       1367   3-NH 2 C 6 H 4 CH 2     2-pyrazolyl       1367   3-NH 2 C 6 H 4 CH 2     5-isoquinolyl       1369   3-NH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         1370   3-NH 2 C 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         1371   3-NH 2 C 6 H 4 CH 2     2-imidazolyl       1372   3-NH 2 C 6 H 4 CH 2     2-oxazolyl       1373   3-NH 2 C 6 H 4 CH 2     4-isoxazolyl       1374   3-NH 2 C 6 H 4 CH 2     4-HOC 6 H 4         1375   3-NH 2 C 6 H 4 CH 2     3-HOC 6 H 4         1376   3-NH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         1377   3-NH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         1378   3-NH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         1379   4-NH 2 C 6 H 4 CH 2     4-MeOC 6 H 4         1380   4-NH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         1381   4-NH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         1382   4-NH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         1383   4-NH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         1384   4-NH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         1385   4-NH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         1386   4-NH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         1387   4-NH 2 C 6 H 4 CH 2     4-pyridyl       1388   4-NH 2 C 6 H 4 CH 2     3-pyridyl       1389   4-NH 2 C 6 H 4 CH 2     2-pyridyl       1390   4-NH 2 C 6 H 4 CH 2     2-thiazolyl       1391   4-NH 2 C 6 H 4 CH 2     2-pyrazolyl       1392   4-NH 2 C 6 H 4 CH 2     5-isoquinolyl       1393   4-NH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         1394   4-NH 2 C 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         1395   4-NH 2 C 6 H 4 CH 2     2-imidazolyl       1396   4-NH 2 C 6 H 4 CH 2     2-oxazolyl       1397   4-NH 2 C 6 H 4 CH 2     4-isoxazolyl       1398   4-NH 2 C 6 H 4 CH 2     4-HOC 6 H 4         1399   4-NH 2 C 6 H 4 CH 2     3-HOC 6 H 4         1400   4-NH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         1401   4-NH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         1402   4-NH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         1403   2-MeOC 6 H 4 CH 2     4-MeOC 6 H 4         1404   2-MeOC 6 H 4 CH 2     3-MeOC 6 H 4         1405   2-MeOC 6 H 4 CH 2     4-NH 2 C 6 H 4         1406   2-MeOC 6 H 4 CH 2     3-NH 2 C 6 H 4         1407   2-MeOC 6 H 4 CH 2     2-NH 2 C 6 H 4         1408   2-MeOC 6 H 4 CH 2     4-Me 2 NC 6 H 4         1409   2-MeOC 6 H 4 CH 2     3-Me 2 NC 6 H 4         1410   2-MeOC 6 H 4 CH 2     2-Me 2 NC 6 H 4         1411   2-MeOC 6 H 4 CH 2     4-pyridyl       1412   2-MeOC 6 H 4 CH 2     3-pyridyl       1413   2-MeOC 6 H 4 CH 2     2-pyridyl       1414   2-MeOC 6 H 4 CH 2     2-thiazolyl       1415   2-MeOC 6 H 4 CH 2     2-pyrazolyl       1416   2-MeOC 6 H 4 CH 2     5-isoquinolyl       1417   2-MeOC 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         1418   2-MeOC 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         1419   2-MeOC 6 H 4 CH 2     2-imidazolyl       1420   2-MeOC 6 H 4 CH 2     2-oxazolyl       1421   2-MeOC 6 H 4 CH 2     4-isoxazolyl       1422   2-MeOC 6 H 4 CH 2     4-HOC 6 H 4         1423   2-MeOC 6 H 4 CH 2     3-HOC 6 H 4         1424   2-MeOC 6 H 4 CH 2     3,4-diHOC 6 H 4         1425   2-MeOC 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         1426   2-MeOC 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         1427   3-MeOC 6 H 4 CH 2     4-MeOC 6 H 4         1428   3-MeOC 6 H 4 CH 2     3-MeOC 6 H 4         1429   3-MeOC 6 H 4 CH 2     4-NH 2 C 6 H 4         1430   3-MeOC 6 H 4 CH 2     3-NH 2 C 6 H 4         1431   3-MeOC 6 H 4 CH 2     2-NH 2 C 6 H 4         1432   3-MeOC 6 H 4 CH 2     4-Me 2 NC 6 H 4         1433   3-MeOC 6 H 4 CH 2     3-Me 2 NC 6 H 4         1434   3-MeOC 6 H 4 CH 2     2-Me 2 NC 6 H 4         1435   3-MeOC 6 H 4 CH 2     4-pyridyl       1436   3-MeOC 6 H 4 CH 2     3-pyridyl       1437   3-MeOC 6 H 4 CH 2     2-pyridyl       1438   3-MeOC 6 H 4 CH 2     2-thiazolyl       1439   3-MeOC 6 H 4 CH 2     2-pyrazolyl       1440   3-MeOC 6 H 4 CH 2     5-isoquinolyl       1441   3-MeOC 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         1442   3-MeOC 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         1443   3-MeOC 6 H 4 CH 2     2-imidazolyl       1444   3-MeOC 6 H 4 CH 2     2-oxazolyl       1445   3-MeOC 6 H 4 CH 2     4-isoxazolyl       1446   3-MeOC 6 H 4 CH 2     4-HOC 6 H 4         1447   3-MeOC 6 H 4 CH 2     3-HOC 6 H 4         1448   3-MeOC 6 H 4 CH 2     3,4-diHOC 6 H 4         1449   3-MeOC 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         1450   3-MeOC 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         1451   4-MeOC 6 H 4 CH 2     4-MeOC 6 H 4         1452   4-MeOC 6 H 4 CH 2     3-MeOC 6 H 4         1453   4-MeOC 6 H 4 CH 2     4-NH 2 C 6 H 4         1454   4-MeOC 6 H 4 CH 2     3-NH 2 C 6 H 4         1455   4-MeOC 6 H 4 CH 2     2-NH 2 C 6 H 4         1456   4-MeOC 6 H 4 CH 2     4-Me 2 NC 6 H 4         1457   4-MeOC 6 H 4 CH 2     3-Me 2 NC 6 H 4         1458   4-MeOC 6 H 4 CH 2     2-Me 2 NC 6 H 4         1459   4-MeOC 6 H 4 CH 2     4-pyridyl       1460   4-MeOC 6 H 4 CH 2     3-pyridyl       1461   4-MeOC 6 H 4 CH 2     2-pyridyl       1462   4-MeOC 6 H 4 CH 2     2-thiazolyl       1463   4-MeOC 6 H 4 CH 2     2-pyrazolyl       1464   4-MeOC 6 H 4 CH 2     5-isoquinolyl       1465   4-MeOC 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         1466   4-MeOC 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         1467   4-MeOC 6 H 4 CH 2     2-imidazolyl       1468   4-MeOC 6 H 4 CH 2     2-oxazolyl       1469   4-MeOC 6 H 4 CH 2     4-isoxazolyl       1470   4-MeOC 6 H 4 CH 2     4-HOC 6 H 4         1471   4-MeOC 6 H 4 CH 2     3-HOC 6 H 4         1472   4-MeOC 6 H 4 CH 2     3,4-diHOC 6 H 4         1473   4-MeOC 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         1474   4-MeOC 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         1475   2-HOC 6 H 4 CH 2     4-MeOC 6 H 4         1476   2-HOC 6 H 4 CH 2     3-MeOC 6 H 4         1477   2-HOC 6 H 4 CH 2     4-NH 2 C 6 H 4         1478   2-HOC 6 H 4 CH 2     3-NH 2 C 6 H 4         1479   2-HOC 6 H 4 CH 2     2-NH 2 C 6 H 4         1480   2-HOC 6 H 4 CH 2     4-Me 2 NC 6 H 4         1481   2-HOC 6 H 4 CH 2     3-Me 2 NC 6 H 4         1482   2-HOC 6 H 4 CH 2     2-Me 2 NC 6 H 4         1483   2-HOC 6 H 4 CH 2     4-pyridyl       1484   2-HOC 6 H 4 CH 2     3-pyridyl       1485   2-HOC 6 H 4 CH 2     2-pyridyl       1486   2-HOC 6 H 4 CH 2     2-thiazolyl       1487   2-HOC 6 H 4 CH 2     2-pyrazolyl       1488   2-HOC 6 H 4 CH 2     5-isoquinolyl       1489   2-HOC 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         1490   2-HOC 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         1491   2-HOC 6 H 4 CH 2     2-imidazolyl       1492   2-HOC 6 H 4 CH 2     2-oxazolyl       1493   2-HOC 6 H 4 CH 2     4-isoxazolyl       1494   2-HOC 6 H 4 CH 2     4-HOC 6 H 4         1495   2-HOC 6 H 4 CH 2     3-HOC 6 H 4         1496   2-HOC 6 H 4 CH 2     3,4-diHOC 6 H 4         1497   2-HOC 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         1498   2-HOC 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         1499   3-HOC 6 H 4 CH 2     4-MeOC 6 H 4         1500   3-HOC 6 H 4 CH 2     3-MeOC 6 H 4         1501   3-HOC 6 H 4 CH 2     4-NH 2 C 6 H 4         1502   3-HOC 6 H 4 CH 2     3-NH 2 C 6 H 4         1503   3-HOC 6 H 4 CH 2     2-NH 2 C 6 H 4         1504   3-HOC 6 H 4 CH 2     4-Me 2 NC 6 H 4         1505   3-HOC 6 H 4 CH 2     3-Me 2 NC 6 H 4         1506   3-HOC 6 H 4 CH 2     2-Me 2 NC 6 H 4         1507   3-HOC 6 H 4 CH 2     4-pyridyl       1508   3-HOC 6 H 4 CH 2     3-pyridyl       1509   3-HOC 6 H 4 CH 2     2-pyridyl       1510   3-HOC 6 H 4 CH 2     2-thiazolyl       1511   3-HOC 6 H 4 CH 2     2-pyrazolyl       1512   3-HOC 6 H 4 CH 2     5-isoquinolyl       1513   3-HOC 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         1514   3-HOC 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         1514   3-HOC 6 H 4 CH 2     2-imidazolyl       1516   3-HOC 6 H 4 CH 2     2-oxazolyl       1517   3-HOC 6 H 4 CH 2     4-isoxazolyl       1518   3-HOC 6 H 4 CH 2     4-HOC 6 H 4         1519   3-HOC 6 H 4 CH 2     3-HOC 6 H 4         1520   3-HOC 6 H 4 CH 2     3,4-diHOC 6 H 4         1521   3-HOC 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         1522   3-HOC 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         1523   4-HOC 6 H 4 CH 2     4-MeOC 6 H 4         1524   4-HOC 6 H 4 CH 2     3-MeOC 6 H 4         1525   4-HOC 6 H 4 CH 2     4-NH 2 C 6 H 4         1526   4-HOC 6 H 4 CH 2     3-NH 2 C 6 H 4         1527   4-HOC 6 H 4 CH 2     2-NH 2 C 6 H 4         1528   4-HOC 6 H 4 CH 2     4-Me 2 NC 6 H 4         1529   4-HOC 6 H 4 CH 2     3-Me 2 NC 6 H 4         1530   4-HOC 6 H 4 CH 2     2-Me 2 NC 6 H 4         1531   4-HOC 6 H 4 CH 2     4-pyridyl       1532   4-HOC 6 H 4 CH 2     3-pyridyl       1533   4-HOC 6 H 4 CH 2     2-pyridyl       1534   4-HOC 6 H 4 CH 2     2-thiazolyl       1535   4-HOC 6 H 4 CH 2     2-pyrazolyl       1536   4-HOC 6 H 4 CH 2     5-isoquinolyl       1537   4-HOC 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         1538   4-HOC 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         1539   4-HOC 6 H 4 CH 2     2-imidazolyl       1540   4-HOC 6 H 4 CH 2     2-oxazolyl       1541   4-HOC 6 H 4 CH 2     4-isoxazolyl       1542   4-HOC 6 H 4 CH 2     4-HOC 6 H 4         1543   4-HOC 6 H 4 CH 2     3-HOC 6 H 4         1544   4-HOC 6 H 4 CH 2     3,4-diHOC 6 H 4         1545   4-HOC 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         1546   4-HOC 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         1547   4-ClC 6 H 4 CH 2     4-MeOC 6 H 4         1548   4-ClC 6 H 4 CH 2     3-MeOC 6 H 4         1549   4-ClC 6 H 4 CH 2     4-NH 2 C 6 H 4         1550   4-ClC 6 H 4 CH 2     3-NH 2 C 6 H 4         1551   4-ClC 6 H 4 CH 2     2-NH 2 C 6 H 4         1552   4-ClC 6 H 4 CH 2     4-Me 2 NC 6 H 4         1553   4-ClC 6 H 4 CH 2     3-Me 2 NC 6 H 4         1554   4-ClC 6 H 4 CH 2     2-Me 2 NC 6 H 4         1555   4-ClC 6 H 4 CH 2     4-pyridyl       1556   4-ClC 6 H 4 CH 2     3-pyridyl       1557   4-ClC 6 H 4 CH 2     2-pyridyl       1558   4-ClC 6 H 4 CH 2     2-thiazolyl       1559   4-ClC 6 H 4 CH 2     2-pyrazolyl       1560   4-ClC 6 H 4 CH 2     5-isoquinolyl       1561   4-ClC 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         1562   4-ClC 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         1563   4-ClC 6 H 4 CH 2     2-imidazolyl       1564   4-ClC 6 H 4 CH 2     2-oxazolyl       1565   4-ClC 6 H 4 CH 2     4-isoxazolyl       1566   4-ClC 6 H 4 CH 2     4-HOC 6 H 4         1567   4-ClC 6 H 4 CH 2     3-HOC 6 H 4         1568   4-ClC 6 H 4 CH 2     3,4-diHOC 6 H 4         1569   4-ClC 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         1570   4-ClC 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         1571   2-NH 2 CH 2 C 6 H 4 CH 2     4-MeOC 6 H 4         1572   2-NH 2 CH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         1573   2-NH 2 CH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         1574   2-NH 2 CH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         1575   2-NH 2 CH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         1576   2-NH 2 CH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         1577   2-NH 2 CH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         1578   2-NH 2 CH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         1579   2-NH 2 CH 2 C 6 H 4 CH 2     4-pyridyl       1580   2-NH 2 CH 2 C 6 H 4 CH 2     3-pyridyl       1581   2-NH 2 CH 2 C 6 H 4 CH 2     2-pyridyl       1582   2-NH 2 CH 2 C 6 H 4 CH 2     2-thiazolyl       1583   2-NH 2 CH 2 C 6 H 4 CH 2     2-pyrazolyl       1584   2-NH 2 CH 2 C 6 H 4 CH 2     5-isoquinolyl       1585   2-NH 2 CH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         1586   2-NH 2 CH 2 C 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         1587   2-NH 2 CH 2 C 6 H 4 CH 2     2-imidazolyl       1588   N-NH 2 CH 2 C 6 H 4 CH 2     2-oxazolyl       1589   2-NH 2 CH 2 C 6 H 4 CH 2     4-isoxazolyl       1590   2-NH 2 CH 2 C 6 H 4 CH 2     4-HOC 6 H 4         1591   2-NH 2 CH 2 C 6 H 4 CH 2     3-HOC 6 H 4         1592   2-NH 2 CH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         1593   2-NH 2 CH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         1594   2-NH 2 CH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         1595   3-NH 2 CH 2 C 6 H 4 CH 2     4-MeOC 6 H 4         1596   3-NH 2 CH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         1597   3-NH 2 CH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         1598   3-NH 2 CH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         1599   3-NH 2 CH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         1600   3-NH 2 CH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         1601   3-NH 2 CH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         1602   3-NH 2 CH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         1603   3-NH 2 CH 2 C 6 H 4 CH 2     4-pyridyl       1604   3-NH 2 CH 2 C 6 H 4 CH 2     3-pyridyl       1605   3-NH 2 CH 2 C 6 H 4 CH 2     2-pyridyl       1606   3-NH 2 CH 2 C 6 H 4 CH 2     2-thiazolyl       1607   3-NH 2 CH 2 C 6 H 4 CH 2     2-pyrazolyl       1608   3-NH 2 CH 2 C 6 H 4 CH 2     5-isoquinolyl       1609   3-NH 2 CH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         1610   3-NH 2 CH 2 C 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         1611   3-NH 2 CH 2 C 6 H 4 CH 2     2-imidazolyl       1612   3-NH 2 CH 2 C 6 H 4 CH 2     2-oxazolyl       1613   3-NH 2 CH 2 C 6 H 4 CH 2     4-isoxazolyl       1614   3-NH 2 CH 2 C 6 H 4 CH 2     4-HOC 6 H 4         1615   3-NH 2 CH 2 C 6 H 4 CH 2     3-HOC 6 H 4         1616   3-NH 2 CH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         1617   3-NH 2 CH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         1618   3-NH 2 CH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         1619   4-NH 2 CH 2 C 6 H 4 CH 2     4-MeOC 6 H 4         1620   4-NH 2 CH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         1621   4-NH 2 CH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         1622   4-NH 2 CH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         1623   4-NH 2 CH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         1624   4-NH 2 CH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         1625   4-NH 2 CH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         1626   4-NH 2 CH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         1627   4-NH 2 CH 2 C 6 H 4 CH 2     4-pyridyl       1628   4-NH 2 CH 2 C 6 H 4 CH 2     3-pyridyl       1629   4-NH 2 CH 2 C 6 H 4 CH 2     2-pyridyl       1630   4-NH 2 CH 2 C 6 H 4 CH 2     2-thiazolyl       1631   4-NH 2 CH 2 C 6 H 4 CH 2     2-pyrazolyl       1632   4-NH 2 CH 2 C 6 H 4 CH 2     5-isoquinolyl       1633   4-NH 2 CH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         1634   4-NH 2 CH 2 C 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         1635   4-NH 2 CH 2 C 6 H 4 CH 2     2-imidazolyl       1636   4-NH 2 CH 2 C 6 H 4 CH 2     2-oxazolyl       1637   4-NH 2 CH 2 C 6 H 4 CH 2     4-isoxazolyl       1638   4-NH 2 CH 2 C 6 H 4 CH 2     4-HOC 6 H 4         1639   4-NH 2 CH 2 C 6 H 4 CH 2     3-HOC 6 H 4         1640   4-NH 2 CH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         1641   4-NH 2 CH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         1642   4-NH 2 CH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         1643   2-Me 2 NCH 2 C 6 H 4 CH 2     4-MeOC 6 H 4         1644   2-Me 2 NCH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         1645   2-Me 2 NCH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         1646   2-Me 2 NCH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         1647   2-Me 2 NCH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         1648   2-Me 2 NCH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         1649   2-Me 2 NCH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         1650   2-Me 2 NCH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         1651   2-Me 2 NCH 2 C 6 H 4 CH 2     4-pyridyl       1652   2-Me 2 NCH 2 C 6 H 4 CH 2     3-pyridyl       1653   2-Me 2 NCH 2 C 6 H 4 CH 2     2-pyridyl       1654   2-Me 2 NCH 2 C 6 H 4 CH 2     2-thiazolyl       1655   2-Me 2 NCH 2 C 6 H 4 CH 2     2-pyrazolyl       1656   2-Me 2 NCH 2 C 6 H 4 CH 2     5-isoquinolyl       1657   2-Me 2 NCH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         1658   2-Me 2 NCH 2 C 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         1659   2-Me 2 NCH 2 C 6 H 4 CH 2     2-imidazolyl       1660   2-Me 2 NCH 2 C 6 H 4 CH 2     2-oxazolyl       1661   2-Me 2 NCH 2 C 6 H 4 CH 2     4-isoxazolyl       1662   2-Me 2 NCH 2 C 6 H 4 CH 2     4-HOC 6 H 4         1663   2-Me 2 NCH 2 C 6 H 4 CH 2     3-HOC 6 H 4         1664   2-Me 2 NCH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         1665   2-Me 2 NCH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         1666   2-Me 2 NCH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         1667   3-Me 2 NCH 2 C 6 H 4 CH 2     4-MeOC 6 H 4         1668   3-Me 2 NCH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         1669   3-Me 2 NCH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         1670   3-Me 2 NCH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         1671   3-Me 2 NCH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         1672   3-Me 2 NCH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         1673   3-Me 2 NCH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         1674   3-Me 2 NCH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         1675   3-Me 2 NCH 2 C 6 H 4 CH 2     4-pyridyl       1676   3-Me 2 NCH 2 C 6 H 4 CH 2     3-pyridyl       1677   3-Me 2 NCH 2 C 6 H 4 CH 2     2-pyridyl       1678   3-Me 2 NCH 2 C 6 H 4 CH 2     2-thiazolyl       1679   3-Me 2 NCH 2 C 6 H 4 CH 2     2-pyrazolyl       1680   3-Me 2 NCH 2 C 6 H 4 CH 2     5-isoquinolyl       1681   3-Me 2 NCH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         1682   3-Me 2 NCH 2 C 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         1683   3-Me 2 NCH 2 C 6 H 4 CH 2     2-imidazolyl       1684   3-Me 2 NCH 2 C 6 H 4 CH 2     2-oxazolyl       1685   3-Me 2 NCH 2 C 6 H 4 CH 2     4-isoxazolyl       1686   3-Me 2 NCH 2 C 6 H 4 CH 2     4-HOC 6 H 4         1687   3-Me 2 NCH 2 C 6 H 4 CH 2     3-HOC 6 H 4         1688   3-Me 2 NCH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         1689   3-Me 2 NCH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         1690   3-Me 2 NCH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4         1691   4-Me 2 NCH 2 C 6 H 4 CH 2     4-MeOC 6 H 4         1692   4-Me 2 NCH 2 C 6 H 4 CH 2     3-MeOC 6 H 4         1693   4-Me 2 NCH 2 C 6 H 4 CH 2     4-NH 2 C 6 H 4         1694   4-Me 2 NCH 2 C 6 H 4 CH 2     3-NH 2 C 6 H 4         1695   4-Me 2 NCH 2 C 6 H 4 CH 2     2-NH 2 C 6 H 4         1696   4-Me 2 NCH 2 C 6 H 4 CH 2     4-Me 2 NC 6 H 4         1697   4-Me 2 NCH 2 C 6 H 4 CH 2     3-Me 2 NC 6 H 4         1698   4-Me 2 NCH 2 C 6 H 4 CH 2     2-Me 2 NC 6 H 4         1699   4-Me 2 NCH 2 C 6 H 4 CH 2     4-pyridyl       1700   4-Me 2 NCH 2 C 6 H 4 CH 2     3-pyridyl       1701   4-Me 2 NCH 2 C 6 H 4 CH 2     2-pyridyl       1702   4-Me 2 NCH 2 C 6 H 4 CH 2     2-thiazolyl       1703   4-Me 2 NCH 2 C 6 H 4 CH 2     2-pyrazolyl       1704   4-Me 2 NCH 2 C 6 H 4 CH 2     5-isoquinolyl       1705   4-Me 2 NCH 2 C 6 H 4 CH 2     3,4-methylenedioxyC 6 H 3         1706   4-Me 2 NCH 2 C 6 H 4 CH 2     3,4-ethylenedioxyC 6 H 3         1707   4-Me 2 NCH 2 C 6 H 4 CH 2     2-imidazolyl       1708   4-Me 2 NCH 2 C 6 H 4 CH 2     2-oxazolyl       1709   4-Me 2 NCH 2 C 6 H 4 CH 2     4-isoxazolyl       1710   4-Me 2 NCH 2 C 6 H 4 CH 2     4-HOC 6 H 4         1711   4-Me 2 NCH 2 C 6 H 4 CH 2     3-HOC 6 H 4         1712   4-Me 2 NCH 2 C 6 H 4 CH 2     3,4-diHOC 6 H 4         1713   4-Me 2 NCH 2 C 6 H 4 CH 2     4-NH 2 CH 2 C 6 H 4         1714   4-Me 2 NCH 2 C 6 H 4 CH 2     3-NH 2 CH 2 C 6 H 4                      
         [0318]    [0318]                             TABLE 4                                                                                  Example               Number   R 1     R 2                 1715   Methyl   4-MeOC 6 H 4         1716   ClCH 2     4-MeOC 6 H 4         1717   Cyclopropyl   4-MeOC 6 H 4         1718   Isopropyl   4-MeOC 6 H 4         1719   Ethyl   4-MeOC 6 H 4         1720   Cyclopentyl   4-MeOC 6 H 4         1721   Cyclobutyl   4-MeOC 6 H 4         1722   Benzyl   4-MeOC 6 H 4         1723   n-propyl   4-MeOC 6 H 4         1724   4-ClC 6 H 4 CH 2     4-MeOC 6 H 4         1725   3-MeOC 6 H 4 CH 2     4-MeOC 6 H 4         1726   4-MeOC 6 H 4 CH 2     4-MeOC 6 H 4         1727   3,4-diMeOC 6 H 4 CH 2     4-MeOC 6 H 4         1728   2,5-diMeOC 6 H 4 CH 2     4-MeOC 6 H 4         1729   Methyl   2-MeOC 6 H 4         1730   Methyl   3,4-diMeOC 6 H 4         1731   3,4-(OCH 2 O)C 6 H 4 CH 2     4-MeOC 6 H 4         1732   3-thiophenylCH 2     4-MeOC 6 H 4         1733   2-MeOC 6 H 4 CH 2     4-MeOC 6 H 4         1734   3,4-diClOC 6 H 4 CH 2     4-MeOC 6 H 4         1735   2,4-diClOC 6 H 4 CH 2     4-MeOC 6 H 4         1736   2-ClC 6 H 4 CH 2     4-MeOC 6 H 4         1737   H 2 NCH 2     4-MeOC 6 H 4         1738   HOCH 2 NHCH 2 CH 2     4-MeOC 6 H 4         1739   Me 2 NCH 2     4-MeOC 6 H 4         1740   PiperazinylCH 2     4-MeOC 6 H 4         1741   4-Me-piperazinylCH 2     4-MeOC 6 H 4         1742   4-HOCH 2 CH 2 -piperazinylCH 2     4-MeOC 6 H 4         1743   PiperidinylCH 2     4-MeOC 6 H 4         1744   4-NH 2 CH 2 -piperidinylCH 2     4-MeOC 6 H 4         1745   CH 3 CH 2 NHCH 2     4-MeOC 6 H 4         1746   ThiomorpholinylCH 2     4-MeOC 6 H 4         1747   MorpholinylCH 2     4-MeOC 6 H 4         1748   PyyrolidinylCH 2     4-MeOC 6 H 4         1749   4-pyridylCH 2 NHCH 2     4-MeOC 6 H 4         1750   4-CH 3 CONHC 6 H 4 CH 2     4-MeOC 6 H 4         1751   4-CH 3 OCONHC 6 H 4 CH 2     4-MeOC 6 H 4         1752   4-NH 2 CH 2 CONHC 6 H 4 CH 2     4-MeOC 6 H 4         1753   4-Me 2 NCH 2 CONHC 6 H 4 CH 2     4-MeOC 6 H 4         1754   4-N 3 C 6 H 4 CH 2     4-MeOC 6 H 4         1755   4-NH 2 C 6 H 4 CH 2     4-MeOC 6 H 4         1756   C 6 H 5 NH   4-MeOC 6 H 4         1757   CH 3 CH 2 CH 2 NH   4-MeOC 6 H 4         1758   4-NH 2 C 6 H 4 CH 2 NH   4-MeOC 6 H 4         1759   4-pyridyCH 2 NH   4-MeOC 6 H 4         1760   Methyl   4-HOC 6 H 4         1761   H   4-MeOC 6 H 4         1762   Methyl   3-pyridyl       1763   Methyl   4-pyridyl       1764   H   4-pyridyl       1765   Methyl   C 6 H 5         1766   Methyl   4-MeSC 6 H 4         1767   Methyl   4-MeSO 2 C 6 H 4         1768   Methyl   4-Me 2 NC 6 H 4         1769   MorpholinylCH 2     4-Me 2 NC 6 H 4         1770   Me 2 NCH 2     4-Me 2 NC 6 H 4         1771   Me 2 NCH 2     4-(piperdinyl)C 6 H 4         1772   Me 2 NCH 2     4-(morpholinyl)C 6 H 4         1773   Me 2 NCH 2     4-CH 3 CH 2 OC 6 H 4         1774   Me 2 NCH 2     4-CH 3 CH 2 CH 2 CH 2 C 6 H 4         1775   Me 2 NCH 2     4-CH 3 CH 2 C 6 H 4         1776   Me 2 NCH 2     4-CH 3 CH 2 CH 2 C 6 H 4