The present application relates to the compounds of formula (I), and the N-oxides, stereoisomers, tautomers and agriculturally or veterinarily acceptable salts thereof wherein the variables are defined in the claims. The compounds of formula (I), as well as the N-oxides, stereoisomers tautomers and agriculturally or veterinarily acceptable salts thereof are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The application also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.

Invertebrate pests and in particular insects, arachnids and nematodes destroy growing and harvested crops and attack wooden dwelling and commercial structures, thereby causing large economic loss to the food supply and to property. Accordingly, there is an ongoing need for new agents for combating invertebrate pests.

Carbamoylated and thiocarbamoylated oxime derivatives are known for pesticidal use, for example, in patent publications WO 2016/156076, semi-carbazones and thiosemicarbazones derivatives are known for pesticidal use in patent publication WO 2016/116445.

Due to the ability of target pests to develop resistance to pesticidally-active agents, there is an ongoing need to identify further compounds, which are suitable for combating invertebrate pests such as insects, arachnids and nematodes. Furthermore, there is a need for new compounds having a high pesticidal activity and showing a broad activity spectrum against a large number of different invertebrate pests, especially against difficult to control insects, arachnids and nematodes.

It is therefore an object of the present invention to identify and provide compounds, which exhibit a high pesticidal activity and have a broad activity spectrum against invertebrate pests.

It has been found that these objects can be achieved by substituted bicyclic compounds of formula I, as depicted and defined below, including their stereoisomers, their salts, in particular their agriculturally or veterinarily acceptable salts, their tautomers and their N-oxides.

In a first aspect, the present invention relates to the compounds of formula I,

Moreover, the present invention also relates to processes and intermediates for preparing compounds of formula I and to active compound combinations comprising them. Moreover, the present invention relates to agricultural or veterinary compositions comprising the compounds of formula I, and to the use of the compounds of formula I or compositions comprising them for combating or controlling invertebrate pests and/or for protecting crops, plants, plant propagation material and/or growing plants from attack and/or infestation by invertebrate pests. The present invention also relates to methods of applying the compounds of formula I. The present invention also relates to method for protecting crops, plants, plant propagation material and/or growing plants from attack or infestation by invertebrate pests comprising contacting or treating the crops, plants, plant propagation material and growing plants, or soil, material, surface, space, area or water in which the crops, plants, plant propagation material is stored or the plant is growing, with a pesticidally effective amount of at least one compound of formula (I) as defined above or a composition comprising at least one compound of formula (I);

Furthermore, the present invention relates to seed comprising compounds of formula I. Wherein the compounds of formula I includes N-oxides, stereoisomers, tautomers and agriculturally or veterinarily acceptable salts thereof.

With due modification of the starting compounds, the compounds of formula I can be prepared by procedures as given in below schemes.

Compounds of the formula S1-2 can be prepared in amide coupling reactions between an aryl carboxylic acid (ArCOOH) and compounds of the formula S1-1 using a coupling reagent such as HATU as described by, for example, Tobinaga, et al WO 2018/021447 (Scheme 1). Alternatively, an aryl carboxylic acid (ArCOOH) can be pre-activated as an acid chloride by reaction with, for example, SOCl2, prior to reaction with an amine (S1-1) in the presence of a base (e.g. Et3N) to form compounds of the formula S1-2. Compounds of the formula S1-3 can, in turn, be prepared by reaction of compounds of the formula S1-2 with a thionating reagent such at P2S5as described by, for example, Carroll et al, WO 2008/130953. Compounds of the formula S1-4 can be synthesized by reaction of compounds of the formula S1-2 with a reducing agent such as BH3.SMe2as described by, for example, Chen et al, WO 2009/135299.

Compounds of the formula S2-2 can be prepared from compounds of the formula S2-1 by reaction with, for example, hydroxylamine hydrochloride in the presence of a base (e.g. NaOH, pyridine, triethylamine, K2CO3, NaH) as described by, for example, Sanders et al, J. Am. Chem. Soc. 2011, 133, 949-957 (Scheme 2). Compounds of the formula S2-3 can be prepared from compounds of the formula S2-2 by reaction with a chlorinating reagent (e.g. N-chlorosuccinimide, NaOCl, t-butylhypochlorite) as described by, for example, Sanders et al, J. Am. Chem. Soc. 2011, 133, 949-957. Compounds of the formula S2-4 can be prepared from compounds of the formula S2-3 by reaction with an amine nucleophile (ArNHR2) as described by, for example, Altug et al, Tetrahedron Lett. 2009, 50, 7392-7394. Compounds of the formula S2-5 can be prepared from compounds of the formula S2-4 by reaction with an electrophile (e.g. methyl iodide, cyanogen bromide, acetyl chloride etc.) in the presence of a base (e.g. NaOH, pyridine, triethylamine, K2CO3, NaH) as described by, for example, Lui et al, Pest. Manag. Sci. 2009, 65, 229-234.

Compounds of the formula S3-2 (R=Me, Et) can be prepared from compounds of the formula S3-1 by reaction with, for example, hydrochloric acid in methanol as described by, for example, Laurent et al, Molecules, 2010, 15, 4283-4293 (Scheme 3). Compounds of the formula S3-3 can be prepared from compounds of the formula S3-2 by reaction with an amine nucleophile (ArNHR2) as described by, for example, Arnold et al, WO 2008/124849.

Compounds of the formula S4-2 can be prepared via compounds of the formula S4-1 by reaction of compounds of the formula S1-2 with a chlorinating agent (e.g. N-chlorosuccinimide, NaOCl, t-butylhypochlorite) followed by a hydrazine [H2NN(R32] as described by, for example, Crimmin et al, Dalton Trans., 2011, 42, 514-522 (Scheme 4). Compounds of the formula S4-2 can also be prepared from compounds of the formula S1-3 by reaction with, for example, a hydrazine [H2NN(R3)2] as described by, for example, Burlison et al, WO 2009/158026.

Compounds of the formula S5-3 can be prepared by reaction of compounds of the formula S5-1 with a reducing agent, for example, LiAlH4. The resultant compounds of the formula S5-2 can then by reacted with aryl alcohol (ArOH) under Mitsonobu conditions to form compounds of the formula S5-3 (Scheme 5). Compounds for the formula S5-5 can be prepared by reaction of compounds of the formula S5-2 with a chlorinating reagent (e.g. SOCl2, POCl3) as described by, for example, Miyahara et al, WO 2017/209155. The resultant compounds of the formula S5-4 can then be converted into compounds of the formula S5-2 by reaction with an arylthiol (ArSH). Compounds of the formula of the formula S5-6 can, in turn, be prepared by reaction of compounds of the formula S5-5 with an oxidizing agent (e.g. MCPBA). Compounds of the formula S1-4 can also be prepared by reducing compounds of the formula of the formula S5-1 with, e.g. DIBAL. The resultant compounds of the formula S2-1 can then be reacted with an amine (ArNHR2) in a reductive amination with, e.g. Na(CN)BH3to form compounds of the formula S1-4.

Compounds of the formula S6-3 can be prepared by treating compounds of the formula S6-1 with a halogenating agent (e.g. POCl3, PBr3) (Scheme 6). The resultant compounds of the formula S6-2 can then be reacted with an amine (R2NH2) in an SNAr reaction or palladium-catalyzed amination as described by, for example, Ojida et al, WO 2018/084321 or Hatakeyama et al, WO 2018/110497, respectively. Alternatively, the resultant compounds of the formula S6-3 can be acylated with an aryl acid (or chloride) to form compounds of the formula S6-4.

Compounds of the formula S7-1, S7-2, S7-3 and S7-4 are isomers of compounds depicted in Scheme 1-4 and, as such, can be synthesized using analogous procedures are those described above (Scheme 7).

Compounds of the formula S8-1 can be prepared in analogy to compounds of the formula S6-3 (Scheme 8). Compounds of the formula S8-2 can be prepared from compounds of the formula S6-2 by reaction with an alcohol [ArC(R9)(R10)OH] in an SNAr reaction or copper-catalyzed ether formation reaction as described by, for example, Long et al, WO 2018/059534 or Gao et al WO 2016/150193, respectively. Compounds of the formula S8-3 can be prepared from compounds of the formula S6-2 by reaction with a thiol [ArC(R9)(R10)SH] in an SNAr reaction or palladium-catalyzed thioether formation reaction as described by, for example, Wang et al, WO 2017/198196 or Barrow et al, WO 2016/123577.

Compounds of the formula S9-3 can also be prepared by a Suzuki-type aryl coupling reaction as depicted in scheme 9, where X is halogen such as chlorine or bromine and Lg is a boron containing radical such as B(OH2) or the corresponding di-C1-C4-alkyl ester. The reaction of the compound of formula S9-1 with the compound of formula S9-2 can be performed e.g. by analogy to the reaction described in WO 2014/007217 or in Org. Lett., 2009, 11(24), 5666-5669 (Scheme 9).

Similarly, compounds of the formula S10-3 can also be prepared by a Suzuki-type aryl coupling reaction as depicted in scheme 10, where X is halogen such as chlorine or bromine and Lg is a boron containing radical such as B(OH2) or the corresponding di-C1-C4-alkyl ester. The reaction of the compound of formula S10-1 with the compound of formula S10-2 can be performed e.g. by analogy to the reaction described in WO 2014/007217 or in Org. Lett., 2009, 11(24), 5666-5669 (Scheme 10).

Compounds of the formula S11-2 (R=Me, Et) can be prepared in a palladium-catalyzed carbonylation of compounds of the formula S11-1 using CO (g) and MeOH or EtOH as described by, for example, Evans et al, WO 2017/214269 (Scheme 11). Compounds of the formula S11-4 can, in turn, be prepared from Compounds of the formula S11-2 by, e.g. basic hydrolysis. Compounds of the formula S11-3 can also be prepared from compounds of the formula S11-2 by reduction with, e.g. DIBAL.

Compounds of the formula S11-4, S11-3 and S12-1 can be converted in known syntheses into compounds on the formula (I) as described by, for example, Crouse et al, WO 2009/102736, Crouse et al, WO 2010/093764, Crouse et al, US 2012/0202687, Crouse et al, WO 2013/009791, Baum et al, WO 2013/116052, Fischer et al, WO 2013/116053, Crouse et al, WO 2014/011429, Jeanguenat et al, WO 2016/116445 and Narine et al, WO 2018/177781 (Scheme 12).

Individual compounds of formula I can also be prepared by derivatisation of other compounds of formula I or the intermediates thereof.

If the synthesis yields mixtures of isomers, a separation is generally not necessarily required since in some cases the individual isomers can be interconverted during work-up for use or during application (for example under the action of light, acids or bases). Such conversions may also take place after use, for example in the treatment of plants in the treated plant, or in the harmful fungus to be controlled.

A skilled person will readily understand that the preferences for the substituents, also in particular the ones given in the tables below for the respective substituents, given herein in connection with compounds I apply for the intermediates accordingly. Thereby, the substituents in each case have independently of each other or more preferably in combination the meanings as defined herein.

Unless otherwise indicated, the term “compound(s) according to the invention” or “compound(s) of the invention” or “compound(s) of formula (I)”, refers to the compounds of formula I.

The term “compound(s) according to the invention”, or “compounds of formula I” comprises the compound(s) as defined herein as well as a stereoisomer, salt, tautomer or N-oxide thereof. The term “compound(s) of the present invention” is to be understood as equivalent to the term “compound(s) according to the invention”, therefore also comprising a stereoisomer, salt, tautomer or N-oxide thereof.

The term “composition(s) according to the invention” or “composition(s) of the present invention” encompasses composition(s) comprising at least one compound of formula I according to the invention as defined above. The compositions of the invention are preferably agricultural or veterinary compositions.

Depending on the substitution pattern, the compounds according to the invention may have one or more centers of chirality, in which case they are present as mixtures of enantiomers or diastereomers. The invention provides both the single pure enantiomers or pure diastereomers of the compounds according to the invention, and their mixtures and the use according to the invention of the pure enantiomers or pure diastereomers of the compounds according to the invention or their mixtures. Suitable compounds according to the invention also include all possible geometrical stereoisomers (cis/trans isomers) and mixtures thereof. Cis/trans isomers may be present with respect to an alkene, carbon-nitrogen double-bond or amide group. The term “stereoisomer(s)” encompasses both optical isomers, such as enantiomers or diastereomers, the latter existing due to more than one center of chirality in the molecule, as well as geometrical isomers (cis/trans isomers). The present invention relates to every possible stereoisomer of the compounds of formula I, i.e. to single enantiomers or diastereomers, as well as to mixtures thereof.

The compounds according to the invention may be amorphous or may exist in one or more different crystalline states (polymorphs) which may have different macroscopic properties such as stability or show different biological properties such as activities. The present invention relates to amorphous and crystalline compounds according to the invention, mixtures of different crystalline states of the respective compounds according to the invention, as well as amorphous or crystalline salts thereof.

The term “tautomers” encompasses isomers, which are derived from the compounds of formula I by the shift of an H-atom involving at least one H-atom located at a nitrogen, oxygen or sulphur atom. Examples of tautomeric forms are keto-enol forms, imine-enamine forms, urea-isourea forms, thiourea-isothiourea forms, (thio)amide-(thio)imidate forms etc.

The term “stereoisomers” encompasses both optical isomers, such as enantiomers or diastereomers, the latter existing due to more than one center of chirality in the molecule, as well as geometrical isomers (cis/trans isomers).

Depending on the substitution pattern, the compounds of the formula I may have one or more centers of chirality, in which case they are present as mixtures of enantiomers or diastereomers. One center of chirality is the carbon ring atom of the isothiazoline ring carrying radical R1. The invention provides both the pure enantiomers or diastereomers and their mixtures and the use according to the invention of the pure enantiomers or diastereomers of the compound I or its mixtures. Suitable compounds of the formula I also include all possible geometrical stereoisomers (cis/trans isomers) and mixtures thereof.

The term N-oxides relates to a form of compounds I in which at least one nitrogen atom is present in oxidized form (as NO). To be more precise, it relates to any compound of the present invention which has at least one tertiary nitrogen atom that is oxidized to an N-oxide moiety. N-oxides of compounds I can in particular be prepared by oxidizing e.g. the ring nitrogen atom of an N-heterocycle, e.g. a pyridine or pyrimidine ring present in Ar or R11, or an imino-nitrogen present in central tricyclic core, with a suitable oxidizing agent, such as peroxo carboxylic acids or other peroxides. The person skilled in the art knows if and in which positions compounds of the present invention may form N-oxides.

Salts of the compounds of the formula I are preferably agriculturally and veterinarily acceptable salts. They can be formed in a customary method, e.g. by reacting the compound with an acid of the anion in question if the compound of formula I has a basic functionality or by reacting an acidic compound of formula I with a suitable base.

Suitable agriculturally or veterinarily acceptable salts are especially the salts of those cations or the acid addition salts of those acids whose cations and anions, which are known and accepted in the art for the formation of salts for agricultural or veterinary use respectively, and do not have any adverse effect on the action of the compounds according to the present invention. Suitable cations are in particular the ions of the alkali metals, preferably lithium, sodium and potassium, of the alkaline earth metals, preferably calcium, magnesium and barium, and of the transition metals, preferably manganese, copper, zinc and iron, and also ammonium (NH4+) and substituted ammonium in which one to four of the hydrogen atoms are replaced by C1-C4-alkyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkyl, hydroxy-C1-C4-alkoxy-C1-C4-alkyl, phenyl or —CH2-phenyl. Examples of substituted ammonium ions comprise methylammonium, isopropylammonium, dimethylammonium, diisopropylammonium, trimethylammonium, tetramethylammonium, tetraethylammonium, tetrabutylammonium, 2-hydroxyethylammonium, 2-(2-hydroxyethoxy)ethylammonium, bis(2-hydroxyethyl)ammonium, benzyltrimethylammonium and benzyl-triethylammonium, furthermore phosphonium ions, sulfonium ions, preferably tri(C1-C4-alkyl)sulfonium, and sulfoxonium ions, preferably tri(C1-C4-alkyl)sulfoxonium. Suitable acid addition veterinarily acceptable salts, e.g. formed by compounds of formula I containing a basic nitrogen atom, e.g. an amino group, include salts with inorganic acids, for example hydrochlorides, sulphates, phosphates, and nitrates and salts of organic acids for example acetic acid, maleic acid, dimaleic acid, fumaric acid, difumaric acid, methane sulfenic acid, methane sulfonic acid, and succinic acid.

Anions of useful acid addition salts are primarily chloride, bromide, fluoride, hydrogen sulfate, sulfate, dihydrogen phosphate, hydrogen phosphate, phosphate, nitrate, hydrogen carbonate, carbonate, hexafluorosilicate, hexafluorophosphate, benzoate, and the anions of C1-C4-alkanoic acids, preferably formate, acetate, propionate and butyrate. They can be formed by reacting a compound of formulae I with an acid of the corresponding anion, preferably of hydrochloric acid, hydrobromic acid, sulfuric acid, phosphoric acid or nitric acid.

The term “invertebrate pest” as used herein encompasses animal populations, such as insects, arachnids and nematodes, which may attack plants, thereby causing substantial damage to the plants attacked, as well as ectoparasites which may infest animals, in particular warm blooded animals such as e.g. mammals or birds, or other higher animals such as reptiles, amphibians or fish, thereby causing substantial damage to the animals infested.

The term “plant propagation material” is to be understood to denote all the generative parts of the plant such as seeds and vegetative plant material such as cuttings and tubers (e. g. potatoes), which can be used for the multiplication of the plant. This includes seeds, roots, fruits, tubers, bulbs, rhizomes, shoots, sprouts and other parts of plants, including seedlings and young plants, which are to be transplanted after germination or after emergence from soil. The plant propagation materials may be treated prophylactically with a plant protection compound either at or before planting or transplanting. Said young plants may also be protected before transplantation by a total or partial treatment by immersion or pouring.

The term “plants” comprises any types of plants including “modified plants” and in particular “cultivated plants”.

The term “modified plants” refers to any wild type species or related species or related genera of a cultivated plant.

The term “cultivated plants” is to be understood as including plants which have been modified by breeding, mutagenesis or genetic engineering including but not limiting to agricultural biotech products on the market or in development (cf. http://www.bio.org/speeches/pubs/er/agri_products.asp). Genetically modified plants are plants, which genetic material has been so modified by the use of recombinant DNA techniques that under natural circumstances cannot readily be obtained by cross breeding, mutations or natural recombination. Typically, one or more genes have been integrated into the genetic material of a genetically modified plant in order to improve certain properties of the plant. Such genetic modifications also include but are not limited to targeted post-translational modification of protein(s), oligo- or polypeptides e. g. by glycosylation or polymer additions such as prenylated, acetylated or farnesylated moieties or PEG moieties.

Plants that have been modified by breeding, mutagenesis or genetic engineering, e. g. have been rendered tolerant to applications of specific classes of herbicides, such as auxin herbicides such as dicamba or 2,4-D; bleacher herbicides such as hydroxylphenylpyruvate dioxygenase (HPPD) inhibitors or phytoene desaturase (PDS) inhibitors; acetolactate synthase (ALS) inhibitors such as sulfonyl ureas or imidazolinones; enolpyruvylshikimate-3-phosphate synthase (EPSPS) inhibitors, such as glyphosate; glutamine synthetase (GS) inhibitors such as glufosinate; protoporphyrinogen-IX oxidase inhibitors; lipid biosynthesis inhibitors such as acetyl CoA carboxylase (ACCase) inhibitors; or oxynil (i. e. bromoxynil or ioxynil) herbicides as a result of conventional methods of breeding or genetic engineering. Furthermore, plants have been made resistant to multiple classes of herbicides through multiple genetic modifications, such as resistance to both glyphosate and glufosinate or to both glyphosate and a herbicide from another class such as ALS inhibitors, HPPD inhibitors, auxin herbicides, or ACCase inhibitors. These herbicide resistance technologies are e. g. described in Pest Managem. Sci. 61, 2005, 246; 61, 2005, 258; 61, 2005, 277; 61, 2005, 269; 61, 2005, 286; 64, 2008, 326; 64, 2008, 332; Weed Sci. 57, 2009, 108; Austral. J. Agricult. Res. 58, 2007, 708; Science 316, 2007, 1185; and references quoted therein. Several cultivated plants have been rendered tolerant to herbicides by conventional methods of breeding (mutagenesis), e. g. Clearfield® summer rape (Canola, BASF SE, Germany) being tolerant to imidazolinones, e. g. imazamox, or ExpressSun® sunflowers (DuPont, USA) being tolerant to sulfonyl ureas, e. g. tribenuron. Genetic engineering methods have been used to render cultivated plants such as soybean, cotton, corn, beets and rape, tolerant to herbicides such as glyphosate and glufosinate, some of which are commercially available under the trade names RoundupReady® (glyphosate-tolerant, Monsanto, U.S.A.), Cultivance® (imidazolinone tolerant, BASF SE, Germany) and LibertyLink® (glufosinate-tolerant, Bayer CropScience, Germany).

Furthermore, plants are also covered that are by the use of recombinant DNA techniques capable to synthesize one or more insecticidal proteins, especially those known from the bacterial genusBacillus, particularly fromBacillus thuringiensis, such as 5-endotoxins, e. g. CryIA(b), CryIA(c), CryIF, CryIF(a2), CryIIA(b), CryIIIA, CryIIIB(b1) or Cry9c; vegetative insecticidal proteins (VIP), e. g. VIP1, VIP2, VIP3 or VIP3A; insecticidal proteins of bacteria colonizing nematodes, e. g.Photorhabdusspp. orXenorhabdusspp.; toxins produced by animals, such as scorpion toxins, arachnid toxins, wasp toxins, or other insect-specific neurotoxins; toxins produced by fungi, such Streptomycetes toxins, plant lectins, such as pea or barley lectins; agglutinins; proteinase inhibitors, such as trypsin inhibitors, serine protease inhibitors, patatin, cystatin or papain inhibitors; ribosome-inactivating proteins (RIP), such as ricin, maize-RIP, abrin, luffin, saporin or bryodin; steroid metabolism enzymes, such as 3-hydroxysteroid oxidase, ecdysteroid-IDP-glycosyl-transferase, cholesterol oxidases, ecdysone inhibitors or HMG-CoA-reductase; ion channel blockers, such as blockers of sodium or calcium channels; juvenile hormone esterase; diuretic hormone receptors (helicokinin receptors); stilben synthase, bibenzyl synthase, chitinases or glucanases. In the context of the present invention these insecticidal proteins or toxins are to be understood expressly also as pre-toxins, hybrid proteins, truncated or otherwise modified proteins. Hybrid proteins are characterized by a new combination of protein domains, (see, e. g. WO 02/015701). Further examples of such toxins or genetically modified plants capable of synthesizing such toxins are disclosed, e. g., in EP-A 374 753, WO 93/007278, WO 95/34656, EP-A 427 529, EP-A 451 878, WO 03/18810 und WO 03/52073. The methods for producing such genetically modified plants are generally known to the person skilled in the art and are described, e. g. in the publications mentioned above. These insecticidal proteins contained in the genetically modified plants impart to the plants producing these proteins tolerance to harmful pests from all taxonomic groups of athropods, especially to beetles (Coelop-tera), two-winged insects (Diptera), and moths (Lepidoptera) and to nematodes (Nematoda). Genetically modified plants capable to synthesize one or more insecticidal proteins are, e. g., described in the publications mentioned above, and some of which are commercially available such as YieldGard® (corn cultivars producing the Cry1Ab toxin), YieldGard® Plus (corn cultivars producing Cry1Ab and Cry3Bb1 toxins), Starlink© (corn cultivars producing the Cry9c toxin), Herculex® RW (corn cultivars producing Cry34Ab1, Cry35Ab1 and the enzyme Phosphinothricin-N-Acetyltransferase [PAT]); NuCOTN® 33B (cotton cultivars producing the Cry1Ac toxin), Bollgard® I (cotton cultivars producing the Cry1Ac toxin), Bollgard® II (cotton cultivars producing Cry1Ac and Cry2Ab2 toxins); VIPCOT® (cotton cultivars producing a VIP-toxin); NewLeaf® (potato cultivars producing the Cry3A toxin); Bt-Xtra®, NatureGard®, KnockOut®, BiteGard®, Protecta®, Bt11 (e. g. Agrisure® CB) and Bt176 from Syngenta Seeds SAS, France, (corn cultivars producing the Cry1Ab toxin and PAT enzyme), MIR604 from Syngenta Seeds SAS, France (corn cultivars producing a modified version of the Cry3A toxin, c.f. WO 03/018810), MON 863 from Monsanto Europe S.A., Belgium (corn cultivars producing the Cry3Bb1 toxin), IPC 531 from Monsanto Europe S.A., Belgium (cotton cultivars producing a modified version of the Cry1Ac toxin) and 1507 from Pioneer Overseas Corporation, Belgium (corn cultivars producing the Cry1F toxin and PAT enzyme).

Furthermore, plants are also covered that are by the use of recombinant DNA techniques capable to synthesize one or more proteins to increase the resistance or tolerance of those plants to bacterial, viral or fungal pathogens. Examples of such proteins are the so-called “pathogenesis-related proteins” (PR proteins, see, e. g. EP-A 392 225), plant disease resistance genes (e. g. potato cultivars, which express resistance genes acting againstPhytophthora infestansderived from the mexican wild potatoSolanum bulbocastanum) or T4-lysozym (e. g. potato cultivars capable of synthesizing these proteins with increased resistance against bacteria such asErwinia amylvora). The methods for producing such genetically modified plants are generally known to the person skilled in the art and are described, e. g. in the publications mentioned above.

Furthermore, plants are also covered that are by the use of recombinant DNA techniques capable to synthesize one or more proteins to increase the productivity (e. g. bio mass production, grain yield, starch content, oil content or protein content), tolerance to drought, salinity or other growth-limiting environmental factors or tolerance to pests and fungal, bacterial or viral pathogens of those plants.

Furthermore, plants are also covered that contain by the use of recombinant DNA techniques a modified amount of substances of content or new substances of content, specifically to improve human or animal nutrition, e. g. oil crops that produce health-promoting long-chain omega-3 fatty acids or unsaturated omega-9 fatty acids (e. g. Nexera® rape, DOW Agro Sciences, Canada).

Furthermore, plants are also covered that contain by the use of recombinant DNA techniques a modified amount of substances of content or new substances of content, specifically to improve raw material production, e. g. potatoes that produce increased amounts of amylopectin (e. g. Amflora® potato, BASF SE, Germany).

The organic moieties mentioned in the above definitions of the variables are—like the term halogen—collective terms for individual listings of the individual members. The prefix Cn-Cmindicates in each case the possible number of carbon atoms in the group.

The term halogen denotes in each case F, Br, Cl or I, in particular F, Cl or Br.

The term “haloalkyl” as used herein, which is also expressed as “alkyl which is partially or fully halogenated”, refers to straight-chain or branched alkyl groups having 1 to 2 (“C1-C2-haloalkyl”), 1 to 3 (“C1-C3-haloalkyl”), 1 to 4 (“C1-C4-haloalkyl”) or 1 to 6 (“C1-C6-haloalkyl”) carbon atoms (as mentioned above), where some or all of the hydrogen atoms in these groups are replaced by halogen atoms as mentioned above: in particular C1-C2-haloalkyl, such as chloromethyl, bromomethyl, dichloromethyl, trichloromethyl, fluoromethyl, difluoromethyl, trifluoromethyl, chlorofluoromethyl, dichlorofluoromethyl, chlorodifluoromethyl, 1-chloroethyl, 1-bromoethyl, 1-fluoroethyl, 2-fluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, 2-chloro-2-fluoroethyl, 2-chloro-2,2-difluoroethyl, 2,2-dichloro-2-fluoroethyl, 2,2,2-trichloroethyl or pentafluoroethyl. C1-C3-haloalkyl is additionally, for example, 1-fluoropropyl, 2-fluoropropyl, 3-fluoropropyl, 1,1-difluoropropyl, 2,2-difluoropropyl, 1,2-difluoropropyl, 3,3-difluoropropyl, 3,3,3-trifluoropropyl, heptafluoropropyl, 1,1,1-trifluoroprop-2-yl, 3-chloropropyl and the like. Examples for C1-C4-haloalkyl are, apart those mentioned for C1-C3-haloalkyl, 4-chlorobutyl and the like.

The term “alkylene” (or alkanediyl) as used herein in each case denotes an alkyl radical as defined above, wherein one hydrogen atom at any position of the carbon backbone is replaced by one further binding site, thus forming a bivalent moiety. Alkylene has preferably 1 to 6 carbon atoms (C1-C6-alkylene), 2 to 6 carbon atoms (C2-C6-alkylene), in particular 1 to 4 carbon atoms (C1-C4-alkylene) or 2 to 4 carbon atoms (C2-C4-alkylene). Examples of alkylene are methylene (CH2), 1,1-ethandiyl, 1,2-ethandiyl, 1,3-propandiyl, 1,2-propandiyl, 2,2-propandiyl, 1,4-butandiyl, 1,2-butandiyl, 1,3-butandiyl, 2,3-butandiyl, 2,2-butandiyl, 1,5-pentandiyl, 2,2-dimethylpropan-1,3-diyl, 1,3-dimethyl-1,3-propandiyl, 1,6-hexandiyl etc.

The term “cycloalkyl” as used herein refers to mono- or bi- or polycyclic saturated hydrocarbon radicals having in particular 3 to 6 (“C3-C6-cycloalkyl”) or 3 to 5 (“C3-C5-cycloalkyl”) or 3 to 4 (“C3-C4-cycloalkyl”) carbon atoms. Examples of monocyclic radicals having 3 to 4 carbon atoms comprise cyclopropyl and cyclobutyl. Examples of monocyclic radicals having 3 to 5 carbon atoms comprise cyclopropyl, cyclobutyl and cyclopentyl. Examples of monocyclic radicals having 3 to 6 carbon atoms comprise cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl. Examples of monocyclic radicals having 3 to 8 carbon atoms comprise cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl. Examples of bicyclic radicals having 7 or 8 carbon atoms comprise bicyclo[2.2.1]heptyl, bicyclo[3.1.1]heptyl, bicyclo[2.2.2]octyl and bicyclo[3.2.1]octyl. Preferably, the term cycloalkyl denotes a monocyclic saturated hydrocarbon radical.

The term “cycloalkoxy” as used herein refers to a cycloalkyl radical, in particular a monocyclic cycloalkyl radical, as defined above having in particular 3 to 6 (“C3-C6-cycloalkoxy”) or 3 to 5 (“C3-C5-cycloalkoxy”) or 3 to 4 (“C3-C4-cycloalksoxy”) carbon atoms, which is bound via an oxygen atom to the remainder of the molecule.

The term “cycloalkyl-C1-C4-alkyl” refers to a C3-C8-cycloalkyl (“C3-C8-cycloalkyl-C1-C4-alkyl”), preferably a C3-C6-cycloalkyl (“C3-C6-cycloalkyl-C1-C4-alkyl”), more preferably a C3-C4-cycloalkyl (“C3-C4-cycloalkyl-C1-C4-alkyl”) as defined above (preferably a monocyclic cycloalkyl group) which is bound to the remainder of the molecule via a C1-C4-alkyl group, as defined above. Examples for C3-C4-cycloalkyl-C1-C4-alkyl are cyclopropylmethyl, cyclopropylethyl, cyclopropylpropyl, cyclobutylmethyl, cyclobutylethyl and cyclobutylpropyl, Examples for C3-C6-cycloalkyl-C1-C4-alkyl, apart those mentioned for C3-C4-cycloalkyl-C1-C4-alkyl, are cyclopentylmethyl, cyclopentylethyl, cyclopentylpropyl, cyclohexylmethyl, cyclohexylethyl and cyclohexylpropyl.

The term “alkoxyalkoxy” as used herein refers to an alkoxyalkyl radical, in particular a C1-C6-alkoxy-C1-C4-alkyl radical, as defined above, which is bound via an oxygen atom to the remainder of the molecule. Examples thereof are OCH2—OCH3, OCH2—OC2H5, n-propoxymethoxy, OCH2—OCH(CH3)2, n-butoxymethoxy, (1-methylpropoxy)methoxy, (2-methylpropoxy)methoxy, OCH2—OC(CH3)3, 2-(methoxy)ethoxy, 2-(ethoxy)ethoxy, 2-(n-propoxy)ethoxy, 2-(1-methylethoxy)ethoxy, 2-(n-butoxy)ethoxy, 2-(1-methylpropoxy)ethoxy, 2-(2-methylpropoxy)ethoxy, 2-(1,1-dimethylethoxy)ethoxy, etc.

The substituent “oxo” replaces a CH2by a C(═O) group.

The term “aryl” relates to phenyl and bi- or polycyclic carbocycles having at least one fused phenylene ring, which is bound to the remainder of the molecule. Examples of bi- or polycyclic carbocycles having at least one phenylene ring include naphthyl, tetrahydronaphthyl, indanyl, indenyl, anthracenyl, fluorenyl etc.

The term “aryl-C1-C4-alkyl” relates to C1-C4-alkyl, as defined above, wherein one hydrogen atom has been replaced by an aryl radical, in particular a phenyl radical. Particular examples of aryl-C1-C4-alkyl include —CH2-phenyl, 1-phenethyl, 2-phenetyl, 1-phenylpropyl, 2-phenylpropyl, 3-phenyl-1-propyl and 2-phenyl-2-propyl.

The term “aryloxy-C1-C4-alkyl” relates to C1-C4-alkyl, as defined above, wherein one hydrogen atom has been replaced by an aryloxy radical, in particular a phenoxy radical. Particular examples of aryloxy-C1-C4-alkyl include phenoxymethyl, 1-phenoxyethyl, 2-phenoxyetyl, 1-phenoxypropyl, 2-phenoxypropyl, 3-phenoxy-1-propyl and 2-phenoxy-2-propyl.

The term “aryl-C1-C4-carbonyl” relates to aryl as defined above, in particular a phenyl radical, which is bound by a carbonyl to the remainder of the molecule. Particular examples of arylcarbonyl include benzoyl, 1-naphthoyl and 2-naphthoyl.

The term “hetaryl-C1-C4-alkyl” relates to C1-C4-alkyl, as defined above, wherein one hydrogen atom has been replaced by a hetaryl radical, in particular a pyridyl radical. Particular examples of hetaryl-C1-C4-alkyl include 2-pyridylmethyl, 3-pyridylmethyl, 4-pyridylmethyl, 1-(2-pyridyl)ethyl, 2-(2-pyridyl)ethyl, 1-(3-pyridyl)ethyl, 2-(3-pyridyl)ethyl, 1-(4-pyridyl)ethyl, 2-(4-pyridyl)ethyl etc.

The term “hetaryloxy-C1-C4-alkyl” relates to C1-C4-alkyl, as defined above, wherein one hydrogen atom has been replaced by an hetaryloxy radical, in particular a pyridyloxy radical. Particular examples of hetaryloxy-C1-C4-alkyl include 2-pyridyloxymethyl, 3-pyridyloxymethyl, 4-pyridyloxymethyl, 1-(2-pyridyloxy)ethyl, 2-(2-pyridyloxy)ethyl, 1-(3-pyridyloxy)ethyl, 2-(3-pyridyloxy)ethyl, 1-(4-pyridyloxy)ethyl, 2-(4-pyridyloxy)ethyl etc.

The term “hetaryl-C1-C4-carbonyl” relates to hetaryl as defined above, in particular a C-bound hetaryl radical, e.g. 2-, 3- or 4-pyridyl, 2- or 3-thienyl, 2- or 3-furyl, 1-, 2- or 3-pyrrolyl, 2- or 4-pyrimidinyl, pyridazinyl, 1-, 3- or 4-pyrazolyl, 1-, 2- or 4-imidazolyl radical, which is bound by a carbonyl to the remainder of the molecule.

The term “substituted” if not specified otherwise refers to substituted with 1, 2, or maximum possible number of substituents. If substituents as defined in compounds of formula I are more than one then they are independently from each other are same or different if not mentioned otherwise.

With respect to the variables, the embodiments of the compounds of the formula I are,

In one preferred embodiment, A is N;

In another preferred embodiment, A and D are N;

In another preferred embodiment, B1and D are N;

In another preferred embodiment, E and D are N;

In another preferred embodiment, A is N, B1is CRB1, E is CRE, and D is CRD;

In another preferred embodiment, A and D are N, B1is CRB1, and E is CRE.

In another preferred embodiment, B1is N, A is CRA, D is ORD, and E is CRE.

In another preferred embodiment, B1and D are N, A is CRA, and E is CRE;

In another preferred embodiment, E and D are N, A is CRA, and B1is CRB1.

In another preferred embodiment, A and D are N, B1is CRB1, E is CRE, B2is CRB2, B3is CRB3, and B4is CRB4;

In another preferred embodiment, B1and D are N, A is CRA, E is CRE, B2is CRB2, B3is CRB3, and B4is CRB4;

In another preferred embodiment, E and D are N, A is CRA, B1is CRB1, B2is CRB2, B3is CRB3, and B4is CRB4;

In another preferred embodiment, RAis H, halogen, C1-C6-alkyl, C3-C6-cycloalkyl, wherein the alkyl or cycloalkyl moieties are unsubstituted or substituted with halogen.

In one preferred embodiment, RB1, RB2, RB3, and RB4independently of each other are H, halogen, or C1-C6-alkyl;

In one preferred embodiment, Q is —C(R4R5)—O—, wherein C is bound to Ar.

In another preferred embodiment, Q is —C(R4R5)—O—, wherein 0 is bound to Ar.

In another preferred embodiment, Q is —C(═O)—O—, wherein C is bound to Ar.

In another preferred embodiment, Q is —C(═O)—O—, wherein 0 is bound to Ar.

In another preferred embodiment, Q is —S(═O)m—C(R7R8)—, wherein S is bound to Ar.

In another preferred embodiment, Q is —S(═O)m—C(R7R8)—, wherein C is bound to Ar.

In another preferred embodiment, Q is —N(R2)—S(═O)m—, wherein N is bound to Ar.

In another preferred embodiment, Q is —N(R2)—S(═O)m—, wherein S is bound to Ar.

In another preferred embodiment, Q is —N(R2)—C(R9R10)—, wherein N is bound to Ar.

In another preferred embodiment, Q is —N(R2)—C(R9R10)—, wherein C is bound to Ar.

In another preferred embodiment, Q is —C(═O)—C(R19R20)—, wherein C(═O) is bound to Ar.

In another preferred embodiment, Q is —C(═O)—C(R19R20)—, wherein C(R19R20) is bound to Ar.

In another preferred embodiment, Q is —N(R2)—C(═O)—, wherein N is bound to Ar.

In another preferred embodiment, Q is —N(R2)—, wherein N is bound to Ar.

In another preferred embodiment, Q is —N(R2)—C(═O)—, wherein C is bound to Ar.

In another preferred embodiment, Q is —N(R2)—C(═S)—, wherein N is bound to Ar.

In another preferred embodiment, Q is —N(R2)—C(═S)—, wherein C is bound to Ar.

In another preferred embodiment, Q is —N═C(X)—, wherein N is bound to Ar.

In another preferred embodiment, Q is —N═C(X)—, wherein C is bound to Ar.

In another preferred embodiment, Q is —N(R2)—C(═NR)—, wherein N is bound to Ar.

In another preferred embodiment, Q is —N(R2)—C(═NR)—, wherein C is bound to Ar.

In another preferred embodiment, Q is —C(R13R14)—C(R15R16)—.

In another preferred embodiment, Q is —C(R17)═C(R18)—.

In another preferred embodiment, Q is —C(R4R5)—O—, —N(R2)—S(═O)m—, —N(R2)—C(R9R10)—, —N(R2)—C(═O)—, —N(R2)—C(═S)—, —N═C(X)—, or —N(R2)—C(═NR)—, wherein Ar is bound to either side of Q; In another preferred embodiment, Q is —C(R4R5)—O—, —N(R2)—C(R9R10)—, —N(R2)—, —N(R2)—C(═O)—, —N═C(X)—, or —N(R2)—C(═NR)—; wherein Ar is bound to either side of Q.

In another preferred embodiment, Q is —C(R4R5)—O—, —N(R2)—C(R9R10)—, —N(R2)—, —N(R2)—C(═O)—, or —N(R2)—C(═NR)—; wherein Ar is bound to either side of Q.

In another preferred embodiment, Q is —C(R4R5)—O—, —N(R2)—C(R9R10)—, —N(R2)—C(═O)—, —N(R2)—C(═NR)—, wherein Ar is bound to either side of Q;

In one preferred embodiment, X is H or N(R3)2;

In another preferred embodiment, X is H;

In another preferred embodiment, X is N(R3)2;

In another preferred embodiment, R is H, CN, C1-C6-alkyl, or OR8;

In another preferred embodiment, R is H, or C1-C6-alkyl;

In another preferred embodiment, R is H, CH3, C2H5, n-C3H7, or isopropyl;

In one preferred embodiment, Ar is phenyl which is unsubstituted or substituted with RArIn another preferred embodiment, Ar is 5- or 6-membered hetaryl, which is unsubstituted or substituted with RAr.

In more preferred embodiment, Ar is phenyl, pyrimidinyl, pyridazinyl, or pyridyl, which are unsubstituted or substituted with RAr.

Particularly preferred Ar are listed in Table A below.

Particularly preferred Ar is selected from Ar-1 to Ar-20;

also particularly preferred Ar is selected from Ar-1 to Ar-13;

also particularly preferred Ar is selected from Ar-1 to Ar-13 and Ar-17 to Ar-18;

also particularly preferred Ar is selected from Ar-1, Ar-2, Ar-3, Ar-4, Ar-10, Ar-17, and Ar-18.

also particularly preferred Ar is selected from Ar-17 and Ar-18;

also particularly preferred Ar is selected from Ar-1, Ar-2, Ar-5, Ar-21 and Ar-22;

also particularly preferred Ar is Ar-17;

also particularly preferred Ar is Ar-18;

In one preferred embodiment, R1is Y—Z-T-R11.

In one preferred embodiment, Y is —CRya═N—, wherein the N is bound to Z.

In another preferred embodiment, Y is —NRyc—C(═S)—, wherein C(═S) is bound to Z.

In another preferred embodiment, Y is —NRyc—C(═O)—, wherein C(═O) is bound to Z.

In one preferred embodiment, Y is —CRya═N— and Z is a single bond;

—NRzc—C(═O)—, wherein C(═O) is bound to T;

—NRzc—C(═S)—, wherein C(═S) is bound to T;

—N═C(S—Rza)—, wherein T is bound to the carbon atom; or

—NRzc—C(S—Rza)═, wherein T is bound to the carbon atom;

In another preferred embodiment, Z is —NRzc—C(═S)—, wherein C(═S) is bound to T.

In another preferred embodiment, Z is —NRzc—C(═O)—, wherein C(═O) is bound to T.

In another preferred embodiment, Z is-N═C(S—Rza)—, wherein T is bound to the carbon atom.

In another preferred embodiment, Z is-NRzc—C(S—Rza)═, wherein T is bound to the carbon atom.

In another preferred embodiment, Z is —O—C(═O)—, wherein T is bound to the carbon atom;

In another preferred embodiment, Z is a single bond.

In one preferred embodiment, T is O.

In another preferred embodiment, T is N—RT.

In another preferred embodiment, T is N.

In one preferred embodiment, Ryais H, halogen, C1-C6-alkyl, C1-C6-alkoxy, which are unsubstituted or substituted with halogen, phenyl, or —CH2-phenyl, wherein the phenyl rings are unsubstituted or substituted with Rf.

In more preferred embodiment, Ryais H, halogen, C1-C6-alkyl, C1-C6-alkoxy, which are unsubstituted or substituted with halogen, or phenyl which is unsubstituted or substituted with Rf.

In further most preferred embodiment, Ryais H or CH3;

In one embodiment, Ryc, Rzcare H, C1-C6-alkyl, C3-C6-cycloalkyl, which are unsubstituted or substituted with halogen, phenyl, or —CH2-phenyl, wherein the rings are unsubstituted or substituted with Rf.

In more preferred embodiment, Rycand Rzcare H, C1-C6-alkyl, C1-C6-haloalkyl, or phenyl which is unsubstituted or substituted with Rf.

In further most preferred embodiment, Rycand Rzcare H or CH3;

In one preferred embodiment, RTis H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C4-alkyl-C1-C6-alkoxy, which are unsubstituted or substituted with halogen, C(═O)—NRbRc, C(═O)—Rd, SO2NRbRc, S(═O)mRe, phenyl, or —CH2-phenyl, wherein the phenyl rings are unsubstituted or substituted with Rf.

In more preferred embodiment, RTis H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C4-alkyl-C1-C6-alkoxy, which are unsubstituted or substituted with halogen.

In most preferred embodiment, RTis H or C1-C6-alkyl.

In another preferred embodiment, Rzctogether with RTif present, forms C1-C6-alkylene or a linear C2-C6-alkenylene group, where in the linear C1-C6-alkylene and the linear C2-C6-alkenylene a CH2moiety may be replaced by a carbonyl or a C═N—R′ and/or wherein 1 or 2 CH2moieties may be replaced by O or S and/or wherein the linear C1-C6-alkylene and the linear C2-C6-alkenylene may be unsubstituted or substituted with Rh.

In more preferred embodiment, Rzctogether with RTif present, forms C1-C6-alkylene or a linear C2-C6-alkenylene group, where in the linear C1-C6-alkylene and the linear C2-C6-alkenylene a CH2moiety is replaced by a carbonyl group.

In another more preferred embodiment, Rzctogether with RTif present, forms C1-C6-alkylene or a linear C2-C6-alkenylene group, where in the linear C1-C6-alkylene and the linear C2-C6-alkenylene a CH2moiety is replaced by a C═N—R′ and wherein 1 or 2 CH2moieties may be replaced by O or S and/or wherein the linear C1-C6-alkylene and the linear C2-C6-alkenylene may be unsubstituted or substituted with Rh.

In another more preferred embodiment, Rzctogether with RTif present, forms C1-C6-alkylene or a linear C2-C6-alkenylene group, where in the linear C1-C6-alkylene and the linear C2-C6-alkenylene 1 or 2 CH2moieties are replaced by O or S and/or wherein the linear C1-C6-alkylene and the linear C2-C6-alkenylene may be unsubstituted or substituted with Rh.

In another preferred embodiment, Rzatogether with RTif present, forms C1-C6-alkylene or a linear C2-C6-alkenylene group, where in the linear C1-C6-alkylene and the linear C2-C6-alkenylene a CH2moiety may be replaced by a carbonyl or a C═N—R′ and/or wherein 1 or 2 CH2moieties may be replaced by O or S and/or wherein the linear C1-C6-alkylene and the linear C2-C6-alkenylene may be unsubstituted or substituted with Rh;

In more preferred embodiment, RZatogether with RTif present, forms C1-C6-alkylene or a linear C2-C6-alkenylene group, where in the linear C1-C6-alkylene and the linear C2-C6-alkenylene a CH2moiety is replaced by a carbonyl group.

In another more preferred embodiment, Rzatogether with RTif present, forms C1-C6-alkylene or a linear C2-C6-alkenylene group, where in the linear C1-C6-alkylene and the linear C2-C6-alkenylene a CH2moiety is replaced by a C═N—R′ and wherein 1 or 2 CH2moieties may be replaced by O or S and/or wherein the linear C1-C6-alkylene and the linear C2-C6-alkenylene may be unsubstituted or substituted with Rh.

In another more preferred embodiment, Rzatogether with RTif present, forms C1-C6-alkylene or a linear C2-C6-alkenylene group, where in the linear C1-C6-alkylene and the linear C2-C6-alkenylene 1 or 2 CH2moieties are replaced by O or S and/or wherein the linear C1-C6-alkylene and the linear C2-C6-alkenylene may be unsubstituted or substituted with Rh.

In a preferred embodiment, Ra, Rband Rcare H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, which are unsubstituted or substituted with halogen, C1-C6-alkylene-CN, phenyl, or —CH2-phenyl, wherein the phenyl rings are unsubstituted or substituted with Rf;

In more preferred embodiment, Ra, Rband Rcare H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, which are unsubstituted or substituted with halogen, phenyl, or —CH2-phenyl, wherein the phenyl rings are unsubstituted or substituted with Rf.

In a preferred embodiment, Rdis H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, which are unsubstituted or substituted with halogen, phenyl, or —CH2-phenyl, wherein the phenyl rings are unsubstituted or substituted with Rf.

In more preferred embodiment, Rdis H, C1-C6-alkyl, C1-C6-haloalkyl, or phenyl which is unsubstituted or substituted with Rf.

In one preferred embodiment, Reis C1-C6-alkyl, C1-C6-haloalkyl, C3-C6-cycloalkyl, C3-C6-halocycloalkyl, phenyl, or —CH2-phenyl, wherein the phenyl rings are unsubstituted or substituted with Rf.

In more preferred embodiment, Reis H, C1-C6-alkyl, C1-C6-haloalkyl, or phenyl unsubstituted or substituted with Rf.

In one embodiment, m is 0.

In another embodiment, m is 1.

In another embodiment, m is 2.

In another embodiment, m is 0 or 1.

In another embodiment, m is 1 or 2.

In more preferred embodiment, R1are formulas Y-1 to Y-9 whereindenotes attachment to the remaining part of the compound, D is R11or R12and wherein RT, R11, R12, R RYa, Rzaand Rzcare as defined in compounds of formula I.

In more preferred embodiment, R1are formulas Y-1 to Y-8 whereindenotes attachment to use the remaining part of the compound, D is R11or R12and wherein RT, R11, R12, Rya, Ryc, Rzaand Rzcare as defined in compounds of formula I.

Also in more preferred embodiment, R1are formulas Y-1, Y-5 or Y-6 whereindenotes attachment to the remaining part of the compound, D is R11or R12and wherein RT, R11, R12, Rya, Ryc, Rzaand Rzcare as defined in compounds of formula I.

In another more preferred embodiment, R1are below formulas YZT-1 to YZT-9, whereindenotes attachment to the remaining part of the compound and R11, R12, RT, R Rzaand Rzcare as defined in compounds of formula I.

In another more preferred embodiment, R1are formulas YZT-1 to YZT-8, whereindenotes attachment to the remaining part of the compound and R11, R12, RT, Rya, Rzaand Rzcare as defined in compounds of formula I.

In most preferred embodiment, R1are formulas Y-1A to Y-9A, whereindenotes attachment to the remaining part of the compound, D is R11or R12.

In most preferred embodiment, R1are formulas Y-1A to Y-8B, whereindenotes attachment to the remaining part of the compound, D is R11or R12.

In more preferred embodiment, R11is C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, which are unsubstituted or substituted with halogen, aryl, arylcarbonyl, aryl-C1-C4-alkyl, aryloxy-C1-C4-alkyl, hetaryl, carbonylhetaryl, C1-C4-alkyl-hetaryl and C1-C4-alkyl-hetaryloxy, where the rings are unsubstituted or substituted with Rgand wherein the hetaryl is a 5- or 6-membered monocyclic hetaryl or a 8-, 9- or 10-membered bicyclic hetaryl.

In most preferred embodiment, R11is aryl, aryl-C1-C4-alkyl, hetaryl, or hetaryl-C1-C4-alkyl, wherein the rings are unsubstituted or substituted with Rgand where hetaryl in hetaryl or hetaryl-C1-C4-alkyl, is preferably a 5- or 6-membered monocyclic hetaryl such as pyridyl, pyrimidinyl, pyridazinyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, isoxazolyl or isothiazolyl which is unsubstituted or substituted with R9.

Examples of particularly preferred radicals R11are the radicals R11-1 to R11-29 summarized in Table A-1 below.

In another preferred embodiment of the invention, R11is R11-1, R11-10, or R11-29;

In one embodiment, R12is a radical of the formula (A1),

wherein # indicates the point of attachment to T and wherein R121, R122, R123and R124are as defined above and wherein R121, R122, R123and R124independently of each other and especially in combination preferably have the following meanings:R121is C1-C4-alkoxy, in particular OCH3, OC2H5;R122is C1-C4-alkoxy, such as OCH3, OC2H5, n-propoxyx or isopropoxy, or C3-C4-alkenyloxy, such as allyloxy, with R122in particular being OCH3, OC2H5, or n-propoxy;R123is OH, C1-C4-alkoxy, such as OCH3, OC2H5, or C3-C4-alkenyloxy, such as allyloxy, with R123in particular being OCH3, OC2H5;R124is C1-C4-alkyl, such as CH3or C2H5, or C1-C4-alkoxy-C1-C4-alkyl, such as methoxymethyl, ethoxymethyl, 2-methoxyethyl or 2-ethoxyethyl, with R124in particular being methyl.

In more preferred embodiment, R12is in particular a radical of the formula (A11), e.g. (A11-a) or (A11-b)

wherein # indicates the point of attachment to T and wherein R121, R122, R123and R124are as defined above and wherein R121, R122, R123and R124independently of each other and especially in combination preferably have the following meanings:R121is C1-C4-alkoxy, in particular OCH3or OC2H5;R122is C1-C4-alkoxy, such as OCH3, OC2H5, n-propoxyx or isopropoxy, or C3-C4-alkenyloxy, such as allyloxy, with R122in particular being OCH3, OC2H5or n-propoxy;R123is OH, C1-C4-alkoxy, such as OCH3or OC2H5, or C3-C4-alkenyloxy, such as allyloxy, with R123in particular being OCH3or OC2H5;R124is C1-C4-alkyl, such as CH3or C2H5, or C1-C4-alkoxy-C1-C4-alkyl, such as methoxymethyl, ethoxymethyl, 2-methoxyethyl or 2-ethoxyethyl, with R124in particular being methyl.

In a more preferred embodiment compounds of formula I are selected from compounds of formula A.1 to A.36.

wherein, Ar is phenyl or 5- or 6-membered hetaryl ring which is substituted with RAr;RAris halogen, OH, CN, NO2, SCN, C1-C6-alkyl, C1-C6-alkoxy, or S—Re, wherein the alkyl and alkoxy are unsubstituted or substituted with halogen;RAis H, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C3-C6-cycloalkyl, or C3-C6-halocycloalkyl;RB1, RB2, RB3, and RB4independently of each other are H, halogen, or C1-C6-alkyl;Q Is —C(R4R5)—O—, —N(R2)—S(═O)m—, —N(R2)—C(R9R10)—, —N(R2)—C(═O)—, —N(R2)—C(═S)—,—N═C(X)—, —N(R2)—C(═NR)—; wherein Ar is bound to either side of Q;X is N(R3)2;and R1is Y—Z-T-R11or Y—Z-T-R12, as defined in formula I.

Also more preferred are the compound of formula I, whereinA and D are N, B1is CRB1, E is CRE, B2is CRB2, B3is CRB3, and B4is CRB4;RB1, RE, independently of each other are H, halogen, or C1-C6-alkyl;RB2, RB3, and RB4independently of each other are H, halogen, C1-C6-alkyl;Q is —C(R4R5)—O—, —N(R2)—C(R9R10)—, —N(R2)—, —N(R2)—C(═O)—, or —N(R2)—C(═NR)—; wherein Ar is bound to either side of Q;m is 0, 1, or 2;R is H, CN, or C1-C6-alkyl;R2is H or C1-C6-alkyl;R4, R5, R9, R10, are identical or different H or C1-C6-alkyl;Ar is Ar1, Ar2, Ar3, Ar4, Ar10, Ar17, or Ar18;R1is Y-1A, Y-3C, Y-5A, Y-6A, Y-8A, or Y-9A;D is R11or R12;R11is R11-1 or R11-10;R12is A1-1b or A11-3b;

Also more preferred are the compound of formula I, whereinB1is N, A is CRA, O is ORD, E is CRE, B2is CRB2, B3is CRB3, and B4is CRB4;RA, RE, RDindependently of each other are H, halogen, or C1-C6-alkyl;RB2, RB3, and RB4independently of each other are H, halogen, C1-C6-alkyl;Q is —C(R4R5)—O—, —N(R2)—C(R9R10)—, —N(R2)—, —N(R2)—C(═O)—, or —N(R2)—C(═NR)—; wherein Ar is bound to either side of Q;m is 0, 1, or 2;R is H, CN, or C1-C6-alkyl;R2is H or C1-C6-alkyl;R4, R5, R9, R10, are identical or different H or C1-C6-alkyl;Ar is Ar1, Ar2, Ar3, Ar4, Ar10, Ar17, or Ar18;R1is Y-1A, Y-3C, Y-5A, Y-6A, Y-8A, or Y-9A;D is R11or R12;R11is R11-1 or R11-10;R12is A1-1b or A11-3b;

Also more preferred are the compound of formula I, whereinB1and D are N, A is CRA, E is CRE, B2is CRB2, B3is CRB3, and B4is CRB4;RA, RE, independently of each other are H, halogen, or C1-C6-alkyl;RB2, RB3, and RB4independently of each other are H, halogen, C1-C6-alkyl;Q is —C(R4R5)—O—, —N(R2)—C(R9R10)—, —N(R2)—, —N(R2)—C(═O)—, or —N(R2)—C(═NR)—; wherein Ar is bound to either side of Q;m is 0, 1, or 2;R is H, CN, or C1-C6-alkyl;R2is H or C1-C6-alkyl;R4, R5, R9, R10, are identical or different H or C1-C6-alkyl;Ar is Ar1, Ar2, Ar3, Ar4, Ar10, Ar17, or Ar18;R1is Y-1A, Y-3C, Y-5A, Y-6A, Y-8A, or Y-9A;D is R11or R12;R11is R11-1 or R11-10;R12is A1-1b or A11-3b;

Also more preferred are the compound of formula I, whereinE and D are N, A is CRA, B1is CRB1, B2is CRB2, B3is CRB3, and B4is CRB4;RA, R B1independently of each other are H, halogen, or C1-C6-alkyl;RB2, RB3, and RB4independently of each other are H, halogen, C1-C6-alkyl;Q is —C(R4R5)—O—, —N(R2)—C(R9R10)—, —N(R2)—, —N(R2)—C(═O)—, or —N(R2)—C(═NR)—; wherein Ar is bound to either side of Q;m is 0, 1, or 2;R is H, CN, or C1-C6-alkyl;R2is H or C1-C6-alkyl;R4, R5, R9, R10, are identical or different H or C1-C6-alkyl;Ar is Ar1, Ar2, Ar3, Ar4, Ar10, Ar17, or Ar18;R1is Y-1A, Y-3C, Y-5A, Y-6A, Y-8A, or Y-9A;D is R11or R12;R11is R11-1 or R11-10;R12is A1-1b or A11-3b;

Also more preferred are the compound of formula I, whereinA, B1, E, D independently are selected from N or CH, wherein at least one of the A, B1, E, and D is N; and when A and D are N, B1is CH;B2, B3, B4are CH;Q is —C(R4R5)—O—, —N(R2)—C(R9R10)—, —N(R2)—, —N(R2)—C(═O)—, —N═C(X)—, or —N(R2)—C(═NR)—; wherein Ar is bound to either side of Q.Ar is Ar-1 or Ar-2;m is 0, 1, or 2;R is H, CN, or C1-C6-alkyl;R2is H or C1-C6-alkyl;R4, R5, R9, R10, are identical or different H or C1-C6-alkyl;Ar is Ar1, Ar2, Ar3, Ar4, Ar10, Ar17, or Ar18;R1is Y-1A, Y-5A, Y-6A or Y-8A;D is R11or R12;R11is R11-1 or R11-29;R12is A1-1b or A11-3b;

Particular compounds of formula I are the compounds of the formulae I.1 to I.48 that are compiled in the following tables 1 to 3888, wherein the combination of variables B2, B3, B4, Ar, and D for each compound of tables 1 to 3888 corresponds to each line of Table B. Each of the groups mentioned for a substituent in the tables is furthermore per se, independently of the combination in which it is mentioned, a particularly preferred aspect of the substituent in question.

Table 1945. Compounds of formula I.37 wherein R1is Y-1A, R is NH, and R2is H.

Table 1946. Compounds of formula I.37 wherein R1is Y-1B, R is NH, and R2is H.

Table 1947. Compounds of formula I.37 wherein R1is Y-2A, R is NH, and R2is H.

Table 1948. Compounds of formula I.37 wherein R1is Y-2B, R is NH, and R2is H.

Table 1949. Compounds of formula I.37 wherein R1is Y-3A, R is NH, and R2is H.

Table 1950. Compounds of formula I.37 wherein R1is Y-3B, R is NH, and R2is H.

Table 1951. Compounds of formula I.37 wherein R1is Y-3C, R is NH, and R2is H.

Table 1952. Compounds of formula I.37 wherein R1is Y-3D, R is NH, and R2is H.

Table 1953. Compounds of formula I.37 wherein R1is Y-4A, R is NH, and R2is H.

Table 1954. Compounds of formula I.37 wherein R1is Y-4B, R is NH, and R2is H.

Table 1955. Compounds of formula I.37 wherein R1is Y-4C, R is NH, and R2is H.

Table 1956. Compounds of formula I.37 wherein R1is Y-4D, R is NH, and R2is H.

Table 1957. Compounds of formula I.37 wherein R1is Y-5A, R is NH, and R2is H.

Table 1958. Compounds of formula I.37 wherein R1is Y-5B, R is NH, and R2is H.

Table 1959. Compounds of formula I.37 wherein R1is Y-6A, R is NH, and R2is H.

Table 1960. Compounds of formula I.37 wherein R1is Y-6B, R is NH, and R2is H.

Table 1961. Compounds of formula I.37 wherein R1is Y-8A, R is NH, and R2is H.

Table 1962. Compounds of formula I.37 wherein R1is Y-8B, R is NH, and R2is H.

Table 1963. Compounds of formula I.37 wherein R1is Y-1A, R is NH, and R2is CH3.

Table 1964. Compounds of formula I.37 wherein R1is Y-1B, R is NH, and R2is CH3.

Table 1965. Compounds of formula I.37 wherein R1is Y-2A, R is NH, and R2is CH3.

Table 1966. Compounds of formula I.37 wherein R1is Y-2B, R is NH, and R2is CH3.

Table 1967. Compounds of formula I.37 wherein R1is Y-3A, R is NH, and R2is CH3.

Table 1968. Compounds of formula I.37 wherein R1is Y-3B, R is NH, and R2is CH3.

Table 1969. Compounds of formula I.37 wherein R1is Y-3C, R is NH, and R2is CH3.

Table 1970. Compounds of formula I.37 wherein R1is Y-3D, R is NH, and R2is CH3.

Table 1971. Compounds of formula I.37 wherein R1is Y-4A, R is NH, and R2is CH3.

Table 1972. Compounds of formula I.37 wherein R1is Y-4B, R is NH, and R2is CH3.

Table 1973. Compounds of formula I.37 wherein R1is Y-4C, R is NH, and R2is CH3.

Table 1974. Compounds of formula I.37 wherein R1is Y-4D, R is NH, and R2is CH3.

Table 1975. Compounds of formula I.37 wherein R1is Y-5A, R is NH, and R2is CH3.

Table 1976. Compounds of formula I.37 wherein R1is Y-5B, R is NH, and R2is CH3.

Table 1977. Compounds of formula I.37 wherein R1is Y-6A, R is NH, and R2is CH3.

Table 1978. Compounds of formula I.37 wherein R1is Y-6B, R is NH, and R2is CH3.

Table 1979. Compounds of formula I.37 wherein R1is Y-8A, R is NH, and R2is CH3.

Table 1980. Compounds of formula I.37 wherein R1is Y-8B, R is NH, and R2is CH3.

Table 1981. Compounds of formula I.37 wherein R1is Y-1A, R is NH, and R2is c-C3H5.

Table 1982. Compounds of formula I.37 wherein R1is Y-1B, R is NH, and R2is c-C3H5.

Table 1983. Compounds of formula I.37 wherein R1is Y-2A, R is NH, and R2is c-C3H5.

Table 1984. Compounds of formula I.37 wherein R1is Y-2B, R is NH, and R2is c-C3H5.

Table 1985. Compounds of formula I.37 wherein R1is Y-3A, R is NH, and R2is c-C3H5.

Table 1986. Compounds of formula I.37 wherein R1is Y-3B, R is NH, and R2is c-C3H5.

Table 1987. Compounds of formula I.37 wherein R1is Y-3C, R is NH, and R2is c-C3H5.

Table 1988. Compounds of formula I.37 wherein R1is Y-3D, R is NH, and R2is c-C3H5.

Table 1989. Compounds of formula I.37 wherein R1is Y-4A, R is NH, and R2is c-C3H5.

Table 1990. Compounds of formula I.37 wherein R1is Y-4B, R is NH, and R2is c-C3H5.

Table 1991. Compounds of formula I.37 wherein R1is Y-4C, R is NH, and R2is c-C3H5.

Table 1992. Compounds of formula I.37 wherein R1is Y-4D, R is NH, and R2is c-C3H5.

Table 1993. Compounds of formula I.37 wherein R1is Y-5A, R is NH, and R2is c-C3H5.

Table 1994. Compounds of formula I.37 wherein R1is Y-5B, R is NH, and R2is c-C3H5.

Table 1995. Compounds of formula I.37 wherein R1is Y-6A, R is NH, and R2is c-C3H5.

Table 1996. Compounds of formula I.37 wherein R1is Y-6B, R is NH, and R2is c-C3H5.

Table 1997. Compounds of formula I.37 wherein R1is Y-8A, R is NH, and R2is c-C3H5.

Table 1998. Compounds of formula I.37 wherein R1is Y-8B, R is NH, and R2is c-C3H5.

Table 2053. Compounds of formula I.37 wherein R1is Y-1A, R is NCN, and R2is H.

Table 2054. Compounds of formula I.37 wherein R1is Y-1B, R is NCN, and R2is H.

Table 2055. Compounds of formula I.37 wherein R1is Y-2A, R is NCN, and R2is H.

Table 2056. Compounds of formula I.37 wherein R1is Y-2B, R is NCN, and R2is H.

Table 2057. Compounds of formula I.37 wherein R1is Y-3A, R is NCN, and R2is H.

Table 2058. Compounds of formula I.37 wherein R1is Y-3B, R is NCN, and R2is H.

Table 2059. Compounds of formula I.37 wherein R1is Y-3C, R is NCN, and R2is H.

Table 2060. Compounds of formula I.37 wherein R1is Y-3D, R is NCN, and R2is H.

Table 2061. Compounds of formula I.37 wherein R1is Y-4A, R is NCN, and R2is H.

Table 2062. Compounds of formula I.37 wherein R1is Y-4B, R is NCN, and R2is H.

Table 2063. Compounds of formula I.37 wherein R1is Y-4C, R is NCN, and R2is H.

Table 2064. Compounds of formula I.37 wherein R1is Y-4D, R is NCN, and R2is H.

Table 2065. Compounds of formula I.37 wherein R1is Y-5A, R is NCN, and R2is H.

Table 2066. Compounds of formula I.37 wherein R1is Y-5B, R is NCN, and R2is H.

Table 2067. Compounds of formula I.37 wherein R1is Y-6A, R is NCN, and R2is H.

Table 2068. Compounds of formula I.37 wherein R1is Y-6B, R is NCN, and R2is H.

Table 2069. Compounds of formula I.37 wherein R1is Y-8A, R is NCN, and R2is H.

Table 2070. Compounds of formula I.37 wherein R1is Y-8B, R is NCN, and R2is H.

Table 2071. Compounds of formula I.37 wherein R1is Y-1A, R is NCN, and R2is CH3.

Table 2072. Compounds of formula I.37 wherein R1is Y-1B, R is NCN, and R2is CH3.

Table 2073. Compounds of formula I.37 wherein R1is Y-2A, R is NCN, and R2is CH3.

Table 2074. Compounds of formula I.37 wherein R1is Y-2B, R is NCN, and R2is CH3.

Table 2075. Compounds of formula I.37 wherein R1is Y-3A, R is NCN, and R2is CH3.

Table 2076. Compounds of formula I.37 wherein R1is Y-3B, R is NCN, and R2is CH3.

Table 2077. Compounds of formula I.37 wherein R1is Y-3C, R is NCN, and R2is CH3.

Table 2078. Compounds of formula I.37 wherein R1is Y-3D, R is NCN, and R2is CH3.

Table 2079. Compounds of formula I.37 wherein R1is Y-4A, R is NCN, and R2is CH3.

Table 2080. Compounds of formula I.37 wherein R1is Y-4B, R is NCN, and R2is CH3.

Table 2081. Compounds of formula I.37 wherein R1is Y-4C, R is NCN, and R2is CH3.

Table 2082. Compounds of formula I.37 wherein R1is Y-4D, R is NCN, and R2is CH3.

Table 2083. Compounds of formula I.37 wherein R1is Y-5A, R is NCN, and R2is CH3.

Table 2084. Compounds of formula I.37 wherein R1is Y-5B, R is NCN, and R2is CH3.

Table 2085. Compounds of formula I.37 wherein R1is Y-6A, R is NCN, and R2is CH3.

Table 2086. Compounds of formula I.37 wherein R1is Y-6B, R is NCN, and R2is CH3.

Table 2087. Compounds of formula I.37 wherein R1is Y-8A, R is NCN, and R2is CH3.

Table 2088. Compounds of formula I.37 wherein R1is Y-8B, R is NCN, and R2is CH3.

Table 2089. Compounds of formula I.37 wherein R1is Y-1A, R is NCN, and R2is c-C3H5.

Table 2090. Compounds of formula I.37 wherein R1is Y-1B, R is NCN, and R2is c-C3H5.

Table 2091. Compounds of formula I.37 wherein R1is Y-2A, R is NCN, and R2is c-C3H5.

Table 2092. Compounds of formula I.37 wherein R1is Y-2B, R is NCN, and R2is c-C3H5.

Table 2093. Compounds of formula I.37 wherein R1is Y-3A, R is NCN, and R2is c-C3H5.

Table 2094. Compounds of formula I.37 wherein R1is Y-3B, R is NCN, and R2is c-C3H5.

Table 2095. Compounds of formula I.37 wherein R1is Y-3C, R is NCN, and R2is c-C3H5.

Table 2096. Compounds of formula I.37 wherein R1is Y-3D, R is NCN, and R2is c-C3H5.

Table 2097. Compounds of formula I.37 wherein R1is Y-4A, R is NCN, and R2is c-C3H5.

Table 2098. Compounds of formula I.37 wherein R1is Y-4B, R is NCN, and R2is c-C3H5.

Table 2099. Compounds of formula I.37 wherein R1is Y-4C, R is NCN, and R2is c-C3H5.

Table 2100. Compounds of formula I.37 wherein R1is Y-4D, R is NCN, and R2is c-C3H5.

Table 2101. Compounds of formula I.37 wherein R1is Y-5A, R is NCN, and R2is c-C3H5.

Table 2102. Compounds of formula I.37 wherein R1is Y-5B, R is NCN, and R2is c-C3H5.

Table 2103. Compounds of formula I.37 wherein R1is Y-6A, R is NCN, and R2is c-C3H5.

Table 2104. Compounds of formula I.37 wherein R1is Y-6B, R is NCN, and R2is c-C3H5.

Table 2105. Compounds of formula I.37 wherein R1is Y-8A, R is NCN, and R2is c-C3H5.

Table 2106. Compounds of formula I.37 wherein R1is Y-8B, R is NCN, and R2is c-C3H5.

Table 2107. Compounds of formula I.38 wherein R1is Y-1A, R is NH, and R2is H.

Table 2108. Compounds of formula I.38 wherein R1is Y-1B, R is NH, and R2is H.

Table 2109. Compounds of formula I.38 wherein R1is Y-2A, R is NH, and R2is H.

Table 2110. Compounds of formula I.38 wherein R1is Y-2B, R is NH, and R2is H.

Table 2111. Compounds of formula I.38 wherein R1is Y-3A, R is NH, and R2is H.

Table 2112. Compounds of formula I.38 wherein R1is Y-3B, R is NH, and R2is H.

Table 2113. Compounds of formula I.38 wherein R1is Y-3C, R is NH, and R2is H.

Table 2114. Compounds of formula I.38 wherein R1is Y-3D, R is NH, and R2is H.

Table 2115. Compounds of formula I.38 wherein R1is Y-4A, R is NH, and R2is H.

Table 2116. Compounds of formula I.38 wherein R1is Y-4B, R is NH, and R2is H.

Table 2117. Compounds of formula I.38 wherein R1is Y-4C, R is NH, and R2is H.

Table 2118. Compounds of formula I.38 wherein R1is Y-4D, R is NH, and R2is H.

Table 2119. Compounds of formula I.38 wherein R1is Y-5A, R is NH, and R2is H.

Table 2120. Compounds of formula I.38 wherein R1is Y-5B, R is NH, and R2is H.

Table 2121. Compounds of formula I.38 wherein R1is Y-6A, R is NH, and R2is H.

Table 2122. Compounds of formula I.38 wherein R1is Y-6B, R is NH, and R2is H.

Table 2123. Compounds of formula I.38 wherein R1is Y-8A, R is NH, and R2is H.

Table 2124. Compounds of formula I.38 wherein R1is Y-8B, R is NH, and R2is H.

Table 2125. Compounds of formula I.38 wherein R1is Y-1A, R is NH, and R2is CH3.

Table 2126. Compounds of formula I.38 wherein R1is Y-1B, R is NH, and R2is CH3.

Table 2127. Compounds of formula I.38 wherein R1is Y-2A, R is NH, and R2is CH3.

Table 2128. Compounds of formula I.38 wherein R1is Y-2B, R is NH, and R2is CH3.

Table 2129. Compounds of formula I.38 wherein R1is Y-3A, R is NH, and R2is CH3.

Table 2130. Compounds of formula I.38 wherein R1is Y-3B, R is NH, and R2is CH3.

Table 2131. Compounds of formula I.38 wherein R1is Y-3C, R is NH, and R2is CH3.

Table 2132. Compounds of formula I.38 wherein R1is Y-3D, R is NH, and R2is CH3.

Table 2133. Compounds of formula I.38 wherein R1is Y-4A, R is NH, and R2is CH3.

Table 2134. Compounds of formula I.38 wherein R1is Y-4B, R is NH, and R2is CH3.

Table 2135. Compounds of formula I.38 wherein R1is Y-4C, R is NH, and R2is CH3.

Table 2136. Compounds of formula I.38 wherein R1is Y-4D, R is NH, and R2is CH3.

Table 2137. Compounds of formula I.38 wherein R1is Y-5A, R is NH, and R2is CH3.

Table 2138. Compounds of formula I.38 wherein R1is Y-5B, R is NH, and R2is CH3.

Table 2139. Compounds of formula I.38 wherein R1is Y-6A, R is NH, and R2is CH3.

Table 2140. Compounds of formula I.38 wherein R1is Y-6B, R is NH, and R2is CH3.

Table 2141. Compounds of formula I.38 wherein R1is Y-8A, R is NH, and R2is CH3.

Table 2142. Compounds of formula I.38 wherein R1is Y-8B, R is NH, and R2is CH3.

Table 2143. Compounds of formula I.38 wherein R1is Y-1A, R is NH, and R2is c-C3H5.

Table 2144. Compounds of formula I.38 wherein R1is Y-1B, R is NH, and R2is c-C3H5.

Table 2145. Compounds of formula I.38 wherein R1is Y-2A, R is NH, and R2is c-C3H5.

Table 2146. Compounds of formula I.38 wherein R1is Y-2B, R is NH, and R2is c-C3H5.

Table 2147. Compounds of formula I.38 wherein R1is Y-3A, R is NH, and R2is c-C3H5.

Table 2148. Compounds of formula I.38 wherein R1is Y-3B, R is NH, and R2is c-C3H5.

Table 2149. Compounds of formula I.38 wherein R1is Y-3C, R is NH, and R2is c-C3H5.

Table 2150. Compounds of formula I.38 wherein R1is Y-3D, R is NH, and R2is c-C3H5.

Table 2151. Compounds of formula I.38 wherein R1is Y-4A, R is NH, and R2is c-C3H5.

Table 2152. Compounds of formula I.38 wherein R1is Y-4B, R is NH, and R2is c-C3H5.

Table 2153. Compounds of formula I.38 wherein R1is Y-4C, R is NH, and R2is c-C3H5.

Table 2154. Compounds of formula I.38 wherein R1is Y-4D, R is NH, and R2is c-C3H5.

Table 2155. Compounds of formula I.38 wherein R1is Y-5A, R is NH, and R2is c-C3H5.

Table 2156. Compounds of formula I.38 wherein R1is Y-5B, R is NH, and R2is c-C3H5.

Table 2157. Compounds of formula I.38 wherein R1is Y-6A, R is NH, and R2is c-C3H5.

Table 2158. Compounds of formula I.38 wherein R1is Y-6B, R is NH, and R2is c-C3H5.

Table 2159. Compounds of formula I.38 wherein R1is Y-8A, R is NH, and R2is c-C3H5.

Table 2160. Compounds of formula I.38 wherein R1is Y-8B, R is NH, and R2is c-C3H5.

Table 2215. Compounds of formula I.38 wherein R1is Y-1A, R is NCN, and R2is H.

Table 2216. Compounds of formula I.38 wherein R1is Y-1B, R is NCN, and R2is H.

Table 2217. Compounds of formula I.38 wherein R1is Y-2A, R is NCN, and R2is H.

Table 2218. Compounds of formula I.38 wherein R1is Y-2B, R is NCN, and R2is H.

Table 2219. Compounds of formula I.38 wherein R1is Y-3A, R is NCN, and R2is H.

Table 2220. Compounds of formula I.38 wherein R1is Y-3B, R is NCN, and R2is H.

Table 2221. Compounds of formula I.38 wherein R1is Y-3C, R is NCN, and R2is H.

Table 2222. Compounds of formula I.38 wherein R1is Y-3D, R is NCN, and R2is H.

Table 2223. Compounds of formula I.38 wherein R1is Y-4A, R is NCN, and R2is H.

Table 2224. Compounds of formula I.38 wherein R1is Y-4B, R is NCN, and R2is H.

Table 2225. Compounds of formula I.38 wherein R1is Y-4C, R is NCN, and R2is H.

Table 2226. Compounds of formula I.38 wherein R1is Y-4D, R is NCN, and R2is H.

Table 2227. Compounds of formula I.38 wherein R1is Y-5A, R is NCN, and R2is H.

Table 2228. Compounds of formula I.38 wherein R1is Y-5B, R is NCN, and R2is H.

Table 2229. Compounds of formula I.38 wherein R1is Y-6A, R is NCN, and R2is H.

Table 2230. Compounds of formula I.38 wherein R1is Y-6B, R is NCN, and R2is H.

Table 2231. Compounds of formula I.38 wherein R1is Y-8A, R is NCN, and R2is H.

Table 2232. Compounds of formula I.38 wherein R1is Y-8B, R is NCN, and R2is H.

Table 2233. Compounds of formula I.38 wherein R1is Y-1A, R is NCN, and R2is CH3.

Table 2234. Compounds of formula I.38 wherein R1is Y-1B, R is NCN, and R2is CH3.

Table 2235. Compounds of formula I.38 wherein R1is Y-2A, R is NCN, and R2is CH3.

Table 2236. Compounds of formula I.38 wherein R1is Y-2B, R is NCN, and R2is CH3.

Table 2237. Compounds of formula I.38 wherein R1is Y-3A, R is NCN, and R2is CH3.

Table 2238. Compounds of formula I.38 wherein R1is Y-3B, R is NCN, and R2is CH3.

Table 2239. Compounds of formula I.38 wherein R1is Y-3C, R is NCN, and R2is CH3.

Table 2240. Compounds of formula I.38 wherein R1is Y-3D, R is NCN, and R2is CH3.

Table 2241. Compounds of formula I.38 wherein R1is Y-4A, R is NCN, and R2is CH3.

Table 2242. Compounds of formula I.38 wherein R1is Y-4B, R is NCN, and R2is CH3.

Table 2243. Compounds of formula I.38 wherein R1is Y-4C, R is NCN, and R2is CH3.

Table 2244. Compounds of formula I.38 wherein R1is Y-4D, R is NCN, and R2is CH3.

Table 2245. Compounds of formula I.38 wherein R1is Y-5A, R is NCN, and R2is CH3.

Table 2246. Compounds of formula I.38 wherein R1is Y-5B, R is NCN, and R2is CH3.

Table 2247. Compounds of formula I.38 wherein R1is Y-6A, R is NCN, and R2is CH3.

Table 2248. Compounds of formula I.38 wherein R1is Y-6B, R is NCN, and R2is CH3.

Table 2249. Compounds of formula I.38 wherein R1is Y-8A, R is NCN, and R2is CH3.

Table 2250. Compounds of formula I.38 wherein R1is Y-8B, R is NCN, and R2is CH3.

Table 2251. Compounds of formula I.38 wherein R1is Y-1A, R is NCN, and R2is c-C3H5.

Table 2252. Compounds of formula I.38 wherein R1is Y-1B, R is NCN, and R2is c-C3H5.

Table 2253. Compounds of formula I.38 wherein R1is Y-2A, R is NCN, and R2is c-C3H5.

Table 2254. Compounds of formula I.38 wherein R1is Y-2B, R is NCN, and R2is c-C3H5.

Table 2255. Compounds of formula I.38 wherein R1is Y-3A, R is NCN, and R2is c-C3H5.

Table 2256. Compounds of formula I.38 wherein R1is Y-3B, R is NCN, and R2is c-C3H5.

Table 2257. Compounds of formula I.38 wherein R1is Y-3C, R is NCN, and R2is c-C3H5.

Table 2258. Compounds of formula I.38 wherein R1is Y-3D, R is NCN, and R2is c-C3H5.

Table 2259. Compounds of formula I.38 wherein R1is Y-4A, R is NCN, and R2is c-C3H5.

Table 2260. Compounds of formula I.38 wherein R1is Y-4B, R is NCN, and R2is c-C3H5.

Table 2261. Compounds of formula I.38 wherein R1is Y-4C, R is NCN, and R2is c-C3H5.

Table 2262. Compounds of formula I.38 wherein R1is Y-4D, R is NCN, and R2is c-C3H5.

Table 2263. Compounds of formula I.38 wherein R1is Y-5A, R is NCN, and R2is c-C3H5.

Table 2264. Compounds of formula I.38 wherein R1is Y-5B, R is NCN, and R2is c-C3H5.

Table 2265. Compounds of formula I.38 wherein R1is Y-6A, R is NCN, and R2is c-C3H5.

Table 2266. Compounds of formula I.38 wherein R1is Y-6B, R is NCN, and R2is c-C3H5.

Table 2267. Compounds of formula I.38 wherein R1is Y-8A, R is NCN, and R2is c-C3H5.

Table 2268. Compounds of formula I.38 wherein R1is Y-8B, R is NCN, and R2is c-C3H5.

Table 2269. Compounds of formula I.39 wherein R1is Y-1A, R is NH, and R2is H.

Table 2270. Compounds of formula I.39 wherein R1is Y-1B, R is NH, and R2is H.

Table 2271. Compounds of formula I.39 wherein R1is Y-2A, R is NH, and R2is H.

Table 2272. Compounds of formula I.39 wherein R1is Y-2B, R is NH, and R2is H.

Table 2273. Compounds of formula I.39 wherein R1is Y-3A, R is NH, and R2is H.

Table 2274. Compounds of formula I.39 wherein R1is Y-3B, R is NH, and R2is H.

Table 2275. Compounds of formula I.39 wherein R1is Y-3C, R is NH, and R2is H.

Table 2276. Compounds of formula I.39 wherein R1is Y-3D, R is NH, and R2is H.

Table 2277. Compounds of formula I.39 wherein R1is Y-4A, R is NH, and R2is H.

Table 2278. Compounds of formula I.39 wherein R1is Y-4B, R is NH, and R2is H.

Table 2279. Compounds of formula I.39 wherein R1is Y-4C, R is NH, and R2is H.

Table 2280. Compounds of formula I.39 wherein R1is Y-4D, R is NH, and R2is H.

Table 2281. Compounds of formula I.39 wherein R1is Y-5A, R is NH, and R2is H.

Table 2282. Compounds of formula I.39 wherein R1is Y-5B, R is NH, and R2is H.

Table 2283. Compounds of formula I.39 wherein R1is Y-6A, R is NH, and R2is H.

Table 2284. Compounds of formula I.39 wherein R1is Y-6B, R is NH, and R2is H.

Table 2285. Compounds of formula I.39 wherein R1is Y-8A, R is NH, and R2is H.

Table 2286. Compounds of formula I.39 wherein R1is Y-8B, R is NH, and R2is H.

Table 2287. Compounds of formula I.39 wherein R1is Y-1A, R is NH, and R2is CH3.

Table 2288. Compounds of formula I.39 wherein R1is Y-1B, R is NH, and R2is CH3.

Table 2289. Compounds of formula I.39 wherein R1is Y-2A, R is NH, and R2is CH3.

Table 2290. Compounds of formula I.39 wherein R1is Y-2B, R is NH, and R2is CH3.

Table 2291. Compounds of formula I.39 wherein R1is Y-3A, R is NH, and R2is CH3.

Table 2292. Compounds of formula I.39 wherein R1is Y-3B, R is NH, and R2is CH3.

Table 2293. Compounds of formula I.39 wherein R1is Y-3C, R is NH, and R2is CH3.

Table 2294. Compounds of formula I.39 wherein R1is Y-3D, R is NH, and R2is CH3.

Table 2295. Compounds of formula I.39 wherein R1is Y-4A, R is NH, and R2is CH3.

Table 2296. Compounds of formula I.39 wherein R1is Y-4B, R is NH, and R2is CH3.

Table 2297. Compounds of formula I.39 wherein R1is Y-4C, R is NH, and R2is CH3.

Table 2298. Compounds of formula I.39 wherein R1is Y-4D, R is NH, and R2is CH3.

Table 2299. Compounds of formula I.39 wherein R1is Y-5A, R is NH, and R2is CH3.

Table 2300. Compounds of formula I.39 wherein R1is Y-5B, R is NH, and R2is CH3.

Table 2301. Compounds of formula I.39 wherein R1is Y-6A, R is NH, and R2is CH3.

Table 2302. Compounds of formula I.39 wherein R1is Y-6B, R is NH, and R2is CH3.

Table 2303. Compounds of formula I.39 wherein R1is Y-8A, R is NH, and R2is CH3.

Table 2304. Compounds of formula I.39 wherein R1is Y-8B, R is NH, and R2is CH3.

Table 2305. Compounds of formula I.39 wherein R1is Y-1A, R is NH, and R2is c-C3H5.

Table 2306. Compounds of formula I.39 wherein R1is Y-1B, R is NH, and R2is c-C3H5.

Table 2307. Compounds of formula I.39 wherein R1is Y-2A, R is NH, and R2is c-C3H5.

Table 2308. Compounds of formula I.39 wherein R1is Y-2B, R is NH, and R2is c-C3H5.

Table 2309. Compounds of formula I.39 wherein R1is Y-3A, R is NH, and R2is c-C3H5.

Table 2310. Compounds of formula I.39 wherein R1is Y-3B, R is NH, and R2is c-C3H5.

Table 2311. Compounds of formula I.39 wherein R1is Y-3C, R is NH, and R2is c-C3H5.

Table 2312. Compounds of formula I.39 wherein R1is Y-3D, R is NH, and R2is c-C3H5.

Table 2313. Compounds of formula I.39 wherein R1is Y-4A, R is NH, and R2is c-C3H5.

Table 2314. Compounds of formula I.39 wherein R1is Y-4B, R is NH, and R2is c-C3H5.

Table 2315. Compounds of formula I.39 wherein R1is Y-4C, R is NH, and R2is c-C3H5.

Table 2316. Compounds of formula I.39 wherein R1is Y-4D, R is NH, and R2is c-C3H5.

Table 2317. Compounds of formula I.39 wherein R1is Y-5A, R is NH, and R2is c-C3H5.

Table 2318. Compounds of formula I.39 wherein R1is Y-5B, R is NH, and R2is c-C3H5.

Table 2319. Compounds of formula I.39 wherein R1is Y-6A, R is NH, and R2is c-C3H5.

Table 2320. Compounds of formula I.39 wherein R1is Y-6B, R is NH, and R2is c-C3H5.

Table 2321. Compounds of formula I.39 wherein R1is Y-8A, R is NH, and R2is c-C3H5.

Table 2322. Compounds of formula I.39 wherein R1is Y-8B, R is NH, and R2is c-C3H5.

Table 2377. Compounds of formula I.39 wherein R1is Y-1A, R is NCN, and R2is H.

Table 2378. Compounds of formula I.39 wherein R1is Y-1B, R is NCN, and R2is H.

Table 2379. Compounds of formula I.39 wherein R1is Y-2A, R is NCN, and R2is H.

Table 2380. Compounds of formula I.39 wherein R1is Y-2B, R is NCN, and R2is H.

Table 2381. Compounds of formula I.39 wherein R1is Y-3A, R is NCN, and R2is H.

Table 2382. Compounds of formula I.39 wherein R1is Y-3B, R is NCN, and R2is H.

Table 2383. Compounds of formula I.39 wherein R1is Y-3C, R is NCN, and R2is H.

Table 2384. Compounds of formula I.39 wherein R1is Y-3D, R is NCN, and R2is H.

Table 2385. Compounds of formula I.39 wherein R1is Y-4A, R is NCN, and R2is H.

Table 2386. Compounds of formula I.39 wherein R1is Y-4B, R is NCN, and R2is H.

Table 2387. Compounds of formula I.39 wherein R1is Y-4C, R is NCN, and R2is H.

Table 2388. Compounds of formula I.39 wherein R1is Y-4D, R is NCN, and R2is H.

Table 2389. Compounds of formula I.39 wherein R1is Y-5A, R is NCN, and R2is H.

Table 2390. Compounds of formula I.39 wherein R1is Y-5B, R is NCN, and R2is H.

Table 2391. Compounds of formula I.39 wherein R1is Y-6A, R is NCN, and R2is H.

Table 2392. Compounds of formula I.39 wherein R1is Y-6B, R is NCN, and R2is H.

Table 2393. Compounds of formula I.39 wherein R1is Y-8A, R is NCN, and R2is H.

Table 2394. Compounds of formula I.39 wherein R1is Y-8B, R is NCN, and R2is H.

Table 2395. Compounds of formula I.39 wherein R1is Y-1A, R is NCN, and R2is CH3.

Table 2396. Compounds of formula I.39 wherein R1is Y-1B, R is NCN, and R2is CH3.

Table 2397. Compounds of formula I.39 wherein R1is Y-2A, R is NCN, and R2is CH3.

Table 2398. Compounds of formula I.39 wherein R1is Y-2B, R is NCN, and R2is CH3.

Table 2399. Compounds of formula I.39 wherein R1is Y-3A, R is NCN, and R2is CH3.

Table 2400. Compounds of formula I.39 wherein R1is Y-3B, R is NCN, and R2is CH3.

Table 2401. Compounds of formula I.39 wherein R1is Y-3C, R is NCN, and R2is CH3.

Table 2402. Compounds of formula I.39 wherein R1is Y-3D, R is NCN, and R2is CH3.

Table 2403. Compounds of formula I.39 wherein R1is Y-4A, R is NCN, and R2is CH3.

Table 2404. Compounds of formula I.39 wherein R1is Y-4B, R is NCN, and R2is CH3.

Table 2405. Compounds of formula I.39 wherein R1is Y-4C, R is NCN, and R2is CH3.

Table 2406. Compounds of formula I.39 wherein R1is Y-4D, R is NCN, and R2is CH3.

Table 2407. Compounds of formula I.39 wherein R1is Y-5A, R is NCN, and R2is CH3.

Table 2408. Compounds of formula I.39 wherein R1is Y-5B, R is NCN, and R2is CH3.

Table 2409. Compounds of formula I.39 wherein R1is Y-6A, R is NCN, and R2is CH3.

Table 2410. Compounds of formula I.39 wherein R1is Y-6B, R is NCN, and R2is CH3.

Table 2411. Compounds of formula I.39 wherein R1is Y-8A, R is NCN, and R2is CH3.

Table 2412. Compounds of formula I.39 wherein R1is Y-8B, R is NCN, and R2is CH3.

Table 2413. Compounds of formula I.39 wherein R1is Y-1A, R is NCN, and R2is c-C3H5.

Table 2414. Compounds of formula I.39 wherein R1is Y-1B, R is NCN, and R2is c-C3H5.

Table 2415. Compounds of formula I.39 wherein R1is Y-2A, R is NCN, and R2is c-C3H5.

Table 2416. Compounds of formula I.39 wherein R1is Y-2B, R is NCN, and R2is c-C3H5.

Table 2417. Compounds of formula I.39 wherein R1is Y-3A, R is NCN, and R2is c-C3H5.

Table 2418. Compounds of formula I.39 wherein R1is Y-3B, R is NCN, and R2is c-C3H5.

Table 2419. Compounds of formula I.39 wherein R1is Y-3C, R is NCN, and R2is c-C3H5.

Table 2420. Compounds of formula I.39 wherein R1is Y-3D, R is NCN, and R2is c-C3H5.

Table 2421. Compounds of formula I.39 wherein R1is Y-4A, R is NCN, and R2is c-C3H5.

Table 2422. Compounds of formula I.39 wherein R1is Y-4B, R is NCN, and R2is c-C3H5.

Table 2423. Compounds of formula I.39 wherein R1is Y-4C, R is NCN, and R2is c-C3H5.

Table 2424. Compounds of formula I.39 wherein R1is Y-4D, R is NCN, and R2is c-C3H5.

Table 2425. Compounds of formula I.39 wherein R1is Y-5A, R is NCN, and R2is c-C3H5.

Table 2426. Compounds of formula I.39 wherein R1is Y-5B, R is NCN, and R2is c-C3H5.

Table 2427. Compounds of formula I.39 wherein R1is Y-6A, R is NCN, and R2is c-C3H5.

Table 2428. Compounds of formula I.39 wherein R1is Y-6B, R is NCN, and R2is c-C3H5.

Table 2429. Compounds of formula I.39 wherein R1is Y-8A, R is NCN, and R2is c-C3H5.

Table 2430. Compounds of formula I.39 wherein R1is Y-8B, R is NCN, and R2is c-C3H5.

Table 2431. Compounds of formula I.40 wherein R1is Y-1A, R is NH, and R2is H.

Table 2432. Compounds of formula I.40 wherein R1is Y-1B, R is NH, and R2is H.

Table 2433. Compounds of formula I.40 wherein R1is Y-2A, R is NH, and R2is H.

Table 2434. Compounds of formula I.40 wherein R1is Y-2B, R is NH, and R2is H.

Table 2435. Compounds of formula I.40 wherein R1is Y-3A, R is NH, and R2is H.

Table 2436. Compounds of formula I.40 wherein R1is Y-3B, R is NH, and R2is H.

Table 2437. Compounds of formula I.40 wherein R1is Y-3C, R is NH, and R2is H.

Table 2438. Compounds of formula I.40 wherein R1is Y-3D, R is NH, and R2is H.

Table 2439. Compounds of formula I.40 wherein R1is Y-4A, R is NH, and R2is H.

Table 2440. Compounds of formula I.40 wherein R1is Y-4B, R is NH, and R2is H.

Table 2441. Compounds of formula I.40 wherein R1is Y-4C, R is NH, and R2is H.

Table 2442. Compounds of formula I.40 wherein R1is Y-4D, R is NH, and R2is H.

Table 2443. Compounds of formula I.40 wherein R1is Y-5A, R is NH, and R2is H.

Table 2444. Compounds of formula I.40 wherein R1is Y-5B, R is NH, and R2is H.

Table 2445. Compounds of formula I.40 wherein R1is Y-6A, R is NH, and R2is H.

Table 2446. Compounds of formula I.40 wherein R1is Y-6B, R is NH, and R2is H.

Table 2447. Compounds of formula I.40 wherein R1is Y-8A, R is NH, and R2is H.

Table 2448. Compounds of formula I.40 wherein R1is Y-8B, R is NH, and R2is H.

Table 2449. Compounds of formula I.40 wherein R1is Y-1A, R is NH, and R2is CH3.

Table 2450. Compounds of formula I.40 wherein R1is Y-1B, R is NH, and R2is CH3.

Table 2451. Compounds of formula I.40 wherein R1is Y-2A, R is NH, and R2is CH3.

Table 2452. Compounds of formula I.40 wherein R1is Y-2B, R is NH, and R2is CH3.

Table 2453. Compounds of formula I.40 wherein R1is Y-3A, R is NH, and R2is CH3.

Table 2454. Compounds of formula I.40 wherein R1is Y-3B, R is NH, and R2is CH3.

Table 2455. Compounds of formula I.40 wherein R1is Y-3C, R is NH, and R2is CH3.

Table 2456. Compounds of formula I.40 wherein R1is Y-3D, R is NH, and R2is CH3.

Table 2457. Compounds of formula I.40 wherein R1is Y-4A, R is NH, and R2is CH3.

Table 2458. Compounds of formula I.40 wherein R1is Y-4B, R is NH, and R2is CH3.

Table 2459. Compounds of formula I.40 wherein R1is Y-4C, R is NH, and R2is CH3.

Table 2460. Compounds of formula I.40 wherein R1is Y-4D, R is NH, and R2is CH3.

Table 2461. Compounds of formula I.40 wherein R1is Y-5A, R is NH, and R2is CH3.

Table 2462. Compounds of formula I.40 wherein R1is Y-5B, R is NH, and R2is CH3.

Table 2463. Compounds of formula I.40 wherein R1is Y-6A, R is NH, and R2is CH3.

Table 2464. Compounds of formula I.40 wherein R1is Y-6B, R is NH, and R2is CH3.

Table 2465. Compounds of formula I.40 wherein R1is Y-8A, R is NH, and R2is CH3.

Table 2466. Compounds of formula I.40 wherein R1is Y-8B, R is NH, and R2is CH3.

Table 2467. Compounds of formula I.40 wherein R1is Y-1A, R is NH, and R2is c-C3H5.

Table 2468. Compounds of formula I.40 wherein R1is Y-1B, R is NH, and R2is c-C3H5.

Table 2469. Compounds of formula I.40 wherein R1is Y-2A, R is NH, and R2is c-C3H5.

Table 2470. Compounds of formula I.40 wherein R1is Y-2B, R is NH, and R2is c-C3H5.

Table 2471. Compounds of formula I.40 wherein R1is Y-3A, R is NH, and R2is c-C3H5.

Table 2472. Compounds of formula I.40 wherein R1is Y-3B, R is NH, and R2is c-C3H5.

Table 2473. Compounds of formula I.40 wherein R1is Y-3C, R is NH, and R2is c-C3H5.

Table 2474. Compounds of formula I.40 wherein R1is Y-3D, R is NH, and R2is c-C3H5.

Table 2475. Compounds of formula I.40 wherein R1is Y-4A, R is NH, and R2is c-C3H5.

Table 2476. Compounds of formula I.40 wherein R1is Y-4B, R is NH, and R2is c-C3H5.

Table 2477. Compounds of formula I.40 wherein R1is Y-4C, R is NH, and R2is c-C3H5.

Table 2478. Compounds of formula I.40 wherein R1is Y-4D, R is NH, and R2is c-C3H5.

Table 2479. Compounds of formula I.40 wherein R1is Y-5A, R is NH, and R2is c-C3H5.

Table 2480. Compounds of formula I.40 wherein R1is Y-5B, R is NH, and R2is c-C3H5.

Table 2481. Compounds of formula I.40 wherein R1is Y-6A, R is NH, and R2is c-C3H5.

Table 2482. Compounds of formula I.40 wherein R1is Y-6B, R is NH, and R2is c-C3H5.

Table 2483. Compounds of formula I.40 wherein R1is Y-8A, R is NH, and R2is c-C3H5.

Table 2484. Compounds of formula I.40 wherein R1is Y-8B, R is NH, and R2is c-C3H5.

Table 2539. Compounds of formula I.40 wherein R1is Y-1A, R is NCN, and R2is H.

Table 2540. Compounds of formula I.40 wherein R1is Y-1B, R is NCN, and R2is H.

Table 2541. Compounds of formula I.40 wherein R1is Y-2A, R is NCN, and R2is H.

Table 2542. Compounds of formula I.40 wherein R1is Y-2B, R is NCN, and R2is H.

Table 2543. Compounds of formula I.40 wherein R1is Y-3A, R is NCN, and R2is H.

Table 2544. Compounds of formula I.40 wherein R1is Y-3B, R is NCN, and R2is H.

Table 2545. Compounds of formula I.40 wherein R1is Y-3C, R is NCN, and R2is H.

Table 2546. Compounds of formula I.40 wherein R1is Y-3D, R is NCN, and R2is H.

Table 2547. Compounds of formula I.40 wherein R1is Y-4A, R is NCN, and R2is H.

Table 2548. Compounds of formula I.40 wherein R1is Y-4B, R is NCN, and R2is H.

Table 2549. Compounds of formula I.40 wherein R1is Y-4C, R is NCN, and R2is H.

Table 2550. Compounds of formula I.40 wherein R1is Y-4D, R is NCN, and R2is H.

Table 2551. Compounds of formula I.40 wherein R1is Y-5A, R is NCN, and R2is H.

Table 2552. Compounds of formula I.40 wherein R1is Y-5B, R is NCN, and R2is H.

Table 2553. Compounds of formula I.40 wherein R1is Y-6A, R is NCN, and R2is H.

Table 2554. Compounds of formula I.40 wherein R1is Y-6B, R is NCN, and R2is H.

Table 2555. Compounds of formula I.40 wherein R1is Y-8A, R is NCN, and R2is H.

Table 2556. Compounds of formula I.40 wherein R1is Y-8B, R is NCN, and R2is H.

Table 2557. Compounds of formula I.40 wherein R1is Y-1A, R is NCN, and R2is CH3.

Table 2558. Compounds of formula I.40 wherein R1is Y-1B, R is NCN, and R2is CH3.

Table 2559. Compounds of formula I.40 wherein R1is Y-2A, R is NCN, and R2is CH3.

Table 2560. Compounds of formula I.40 wherein R1is Y-2B, R is NCN, and R2is CH3.

Table 2561. Compounds of formula I.40 wherein R1is Y-3A, R is NCN, and R2is CH3.

Table 2562. Compounds of formula I.40 wherein R1is Y-3B, R is NCN, and R2is CH3.

Table 2563. Compounds of formula I.40 wherein R1is Y-3C, R is NCN, and R2is CH3.

Table 2564. Compounds of formula I.40 wherein R1is Y-3D, R is NCN, and R2is CH3.

Table 2565. Compounds of formula I.40 wherein R1is Y-4A, R is NCN, and R2is CH3.

Table 2566. Compounds of formula I.40 wherein R1is Y-4B, R is NCN, and R2is CH3.

Table 2567. Compounds of formula I.40 wherein R1is Y-4C, R is NCN, and R2is CH3.

Table 2568. Compounds of formula I.40 wherein R1is Y-4D, R is NCN, and R2is CH3.

Table 2569. Compounds of formula I.40 wherein R1is Y-5A, R is NCN, and R2is CH3.

Table 2570. Compounds of formula I.40 wherein R1is Y-5B, R is NCN, and R2is CH3.

Table 2571. Compounds of formula I.40 wherein R1is Y-6A, R is NCN, and R2is CH3.

Table 2572. Compounds of formula I.40 wherein R1is Y-6B, R is NCN, and R2is CH3.

Table 2573. Compounds of formula I.40 wherein R1is Y-8A, R is NCN, and R2is CH3.

Table 2574. Compounds of formula I.40 wherein R1is Y-8B, R is NCN, and R2is CH3.

Table 2575. Compounds of formula I.40 wherein R1is Y-1A, R is NCN, and R2is c-C3H5.

Table 2576. Compounds of formula I.40 wherein R1is Y-1B, R is NCN, and R2is c-C3H5.

Table 2577. Compounds of formula I.40 wherein R1is Y-2A, R is NCN, and R2is c-C3H5.

Table 2578. Compounds of formula I.40 wherein R1is Y-2B, R is NCN, and R2is c-C3H5.

Table 2579. Compounds of formula I.40 wherein R1is Y-3A, R is NCN, and R2is c-C3H5.

Table 2580. Compounds of formula I.40 wherein R1is Y-3B, R is NCN, and R2is c-C3H5.

Table 2581. Compounds of formula I.40 wherein R1is Y-3C, R is NCN, and R2is c-C3H5.

Table 2582. Compounds of formula I.40 wherein R1is Y-3D, R is NCN, and R2is c-C3H5.

Table 2583. Compounds of formula I.40 wherein R1is Y-4A, R is NCN, and R2is c-C3H5.

Table 2584. Compounds of formula I.40 wherein R1is Y-4B, R is NCN, and R2is c-C3H5.

Table 2585. Compounds of formula I.40 wherein R1is Y-4C, R is NCN, and R2is c-C3H5.

Table 2586. Compounds of formula I.40 wherein R1is Y-4D, R is NCN, and R2is c-C3H5.

Table 2587. Compounds of formula I.40 wherein R1is Y-5A, R is NCN, and R2is c-C3H5.

Table 2588. Compounds of formula I.40 wherein R1is Y-5B, R is NCN, and R2is c-C3H5.

Table 2589. Compounds of formula I.40 wherein R1is Y-6A, R is NCN, and R2is c-C3H5.

Table 2590. Compounds of formula I.40 wherein R1is Y-6B, R is NCN, and R2is c-C3H5.

Table 2591. Compounds of formula I.40 wherein R1is Y-8A, R is NCN, and R2is c-C3H5.

Table 2592. Compounds of formula I.40 wherein R1is Y-8B, R is NCN, and R2is c-C3H5.

Table 2593. Compounds of formula I.41 wherein R1is Y-1A, R is NH, and R2is H.

Table 2594. Compounds of formula I.41 wherein R1is Y-1B, R is NH, and R2is H.

Table 2595. Compounds of formula I.41 wherein R1is Y-2A, R is NH, and R2is H.

Table 2596. Compounds of formula I.41 wherein R1is Y-2B, R is NH, and R2is H.

Table 2597. Compounds of formula I.41 wherein R1is Y-3A, R is NH, and R2is H.

Table 2598. Compounds of formula I.41 wherein R1is Y-3B, R is NH, and R2is H.

Table 2599. Compounds of formula I.41 wherein R1is Y-3C, R is NH, and R2is H.

Table 2600. Compounds of formula I.41 wherein R1is Y-3D, R is NH, and R2is H.

Table 2601. Compounds of formula I.41 wherein R1is Y-4A, R is NH, and R2is H.

Table 2602. Compounds of formula I.41 wherein R1is Y-4B, R is NH, and R2is H.

Table 2603. Compounds of formula I.41 wherein R1is Y-4C, R is NH, and R2is H.

Table 2604. Compounds of formula I.41 wherein R1is Y-4D, R is NH, and R2is H.

Table 2605. Compounds of formula I.41 wherein R1is Y-5A, R is NH, and R2is H.

Table 2606. Compounds of formula I.41 wherein R1is Y-5B, R is NH, and R2is H.

Table 2607. Compounds of formula I.41 wherein R1is Y-6A, R is NH, and R2is H.

Table 2608. Compounds of formula I.41 wherein R1is Y-6B, R is NH, and R2is H.

Table 2609. Compounds of formula I.41 wherein R1is Y-8A, R is NH, and R2is H.

Table 2610. Compounds of formula I.41 wherein R1is Y-8B, R is NH, and R2is H.

Table 2611. Compounds of formula I.41 wherein R1is Y-1A, R is NH, and R2is CH3.

Table 2612. Compounds of formula I.41 wherein R1is Y-1B, R is NH, and R2is CH3.

Table 2613. Compounds of formula I.41 wherein R1is Y-2A, R is NH, and R2is CH3.

Table 2614. Compounds of formula I.41 wherein R1is Y-2B, R is NH, and R2is CH3.

Table 2615. Compounds of formula I.41 wherein R1is Y-3A, R is NH, and R2is CH3.

Table 2616. Compounds of formula I.41 wherein R1is Y-3B, R is NH, and R2is CH3.

Table 2617. Compounds of formula I.41 wherein R1is Y-3C, R is NH, and R2is CH3.

Table 2618. Compounds of formula I.41 wherein R1is Y-3D, R is NH, and R2is CH3.

Table 2619. Compounds of formula I.41 wherein R1is Y-4A, R is NH, and R2is CH3.

Table 2620. Compounds of formula I.41 wherein R1is Y-4B, R is NH, and R2is CH3.

Table 2621. Compounds of formula I.41 wherein R1is Y-4C, R is NH, and R2is CH3.

Table 2622. Compounds of formula I.41 wherein R1is Y-4D, R is NH, and R2is CH3.

Table 2623. Compounds of formula I.41 wherein R1is Y-5A, R is NH, and R2is CH3.

Table 2624. Compounds of formula I.41 wherein R1is Y-5B, R is NH, and R2is CH3.

Table 2625. Compounds of formula I.41 wherein R1is Y-6A, R is NH, and R2is CH3.

Table 2626. Compounds of formula I.41 wherein R1is Y-6B, R is NH, and R2is CH3.

Table 2627. Compounds of formula I.41 wherein R1is Y-8A, R is NH, and R2is CH3.

Table 2628. Compounds of formula I.41 wherein R1is Y-8B, R is NH, and R2is CH3.

Table 2629. Compounds of formula I.41 wherein R1is Y-1A, R is NH, and R2is c-C3H5.

Table 2630. Compounds of formula I.41 wherein R1is Y-1B, R is NH, and R2is c-C3H5.

Table 2631. Compounds of formula I.41 wherein R1is Y-2A, R is NH, and R2is c-C3H5.

Table 2632. Compounds of formula I.41 wherein R1is Y-2B, R is NH, and R2is c-C3H5.

Table 2633. Compounds of formula I.41 wherein R1is Y-3A, R is NH, and R2is c-C3H5.

Table 2634. Compounds of formula I.41 wherein R1is Y-3B, R is NH, and R2is c-C3H5.

Table 2635. Compounds of formula I.41 wherein R1is Y-3C, R is NH, and R2is c-C3H5.

Table 2636. Compounds of formula I.41 wherein R1is Y-3D, R is NH, and R2is c-C3H5.

Table 2637. Compounds of formula I.41 wherein R1is Y-4A, R is NH, and R2is c-C3H5.

Table 2638. Compounds of formula I.41 wherein R1is Y-4B, R is NH, and R2is c-C3H5.

Table 2639. Compounds of formula I.41 wherein R1is Y-4C, R is NH, and R2is c-C3H5.

Table 2640. Compounds of formula I.41 wherein R1is Y-4D, R is NH, and R2is c-C3H5.

Table 2641. Compounds of formula I.41 wherein R1is Y-5A, R is NH, and R2is c-C3H5.

Table 2642. Compounds of formula I.41 wherein R1is Y-5B, R is NH, and R2is c-C3H5.

Table 2643. Compounds of formula I.41 wherein R1is Y-6A, R is NH, and R2is c-C3H5.

Table 2644. Compounds of formula I.41 wherein R1is Y-6B, R is NH, and R2is c-C3H5.

Table 2645. Compounds of formula I.41 wherein R1is Y-8A, R is NH, and R2is c-C3H5.

Table 2646. Compounds of formula I.41 wherein R1is Y-8B, R is NH, and R2is c-C3H5.

Table 2701. Compounds of formula I.41 wherein R1is Y-1A, R is NCN, and R2is H.

Table 2702. Compounds of formula I.41 wherein R1is Y-1B, R is NCN, and R2is H.

Table 2703. Compounds of formula I.41 wherein R1is Y-2A, R is NCN, and R2is H.

Table 2704. Compounds of formula I.41 wherein R1is Y-2B, R is NCN, and R2is H.

Table 2705. Compounds of formula I.41 wherein R1is Y-3A, R is NCN, and R2is H.

Table 2706. Compounds of formula I.41 wherein R1is Y-3B, R is NCN, and R2is H.

Table 2707. Compounds of formula I.41 wherein R1is Y-3C, R is NCN, and R2is H.

Table 2708. Compounds of formula I.41 wherein R1is Y-3D, R is NCN, and R2is H.

Table 2709. Compounds of formula I.41 wherein R1is Y-4A, R is NCN, and R2is H.

Table 2710. Compounds of formula I.41 wherein R1is Y-4B, R is NCN, and R2is H.

Table 2711. Compounds of formula I.41 wherein R1is Y-4C, R is NCN, and R2is H.

Table 2712. Compounds of formula I.41 wherein R1is Y-4D, R is NCN, and R2is H.

Table 2713. Compounds of formula I.41 wherein R1is Y-5A, R is NCN, and R2is H.

Table 2714. Compounds of formula I.41 wherein R1is Y-5B, R is NCN, and R2is H.

Table 2715. Compounds of formula I.41 wherein R1is Y-6A, R is NCN, and R2is H.

Table 2716. Compounds of formula I.41 wherein R1is Y-6B, R is NCN, and R2is H.

Table 2717. Compounds of formula I.41 wherein R1is Y-8A, R is NCN, and R2is H.

Table 2718. Compounds of formula I.41 wherein R1is Y-8B, R is NCN, and R2is H.

Table 2719. Compounds of formula I.41 wherein R1is Y-1A, R is NCN, and R2is CH3.

Table 2720. Compounds of formula I.41 wherein R1is Y-1B, R is NCN, and R2is CH3.

Table 2721. Compounds of formula I.41 wherein R1is Y-2A, R is NCN, and R2is CH3.

Table 2722. Compounds of formula I.41 wherein R1is Y-2B, R is NCN, and R2is CH3.

Table 2723. Compounds of formula I.41 wherein R1is Y-3A, R is NCN, and R2is CH3.

Table 2724. Compounds of formula I.41 wherein R1is Y-3B, R is NCN, and R2is CH3.

Table 2725. Compounds of formula I.41 wherein R1is Y-3C, R is NCN, and R2is CH3.

Table 2726. Compounds of formula I.41 wherein R1is Y-3D, R is NCN, and R2is CH3.

Table 2727. Compounds of formula I.41 wherein R1is Y-4A, R is NCN, and R2is CH3.

Table 2728. Compounds of formula I.41 wherein R1is Y-4B, R is NCN, and R2is CH3.

Table 2729. Compounds of formula I.41 wherein R1is Y-4C, R is NCN, and R2is CH3.

Table 2730. Compounds of formula I.41 wherein R1is Y-4D, R is NCN, and R2is CH3.

Table 2731. Compounds of formula I.41 wherein R1is Y-5A, R is NCN, and R2is CH3.

Table 2732. Compounds of formula I.41 wherein R1is Y-5B, R is NCN, and R2is CH3.

Table 2733. Compounds of formula I.41 wherein R1is Y-6A, R is NCN, and R2is CH3.

Table 2734. Compounds of formula I.41 wherein R1is Y-6B, R is NCN, and R2is CH3.

Table 2735. Compounds of formula I.41 wherein R1is Y-8A, R is NCN, and R2is CH3.

Table 2736. Compounds of formula I.41 wherein R1is Y-8B, R is NCN, and R2is CH3.

Table 2737. Compounds of formula I.41 wherein R1is Y-1A, R is NCN, and R2is c-C3H5.

Table 2738. Compounds of formula I.41 wherein R1is Y-1B, R is NCN, and R2is c-C3H5.

Table 2739. Compounds of formula I.41 wherein R1is Y-2A, R is NCN, and R2is c-C3H5.

Table 2740. Compounds of formula I.41 wherein R1is Y-2B, R is NCN, and R2is c-C3H5.

Table 2741. Compounds of formula I.41 wherein R1is Y-3A, R is NCN, and R2is c-C3H5.

Table 2742. Compounds of formula I.41 wherein R1is Y-3B, R is NCN, and R2is c-C3H5.

Table 2743. Compounds of formula I.41 wherein R1is Y-3C, R is NCN, and R2is c-C3H5.

Table 2744. Compounds of formula I.41 wherein R1is Y-3D, R is NCN, and R2is c-C3H5.

Table 2745. Compounds of formula I.41 wherein R1is Y-4A, R is NCN, and R2is c-C3H5.

Table 2746. Compounds of formula I.41 wherein R1is Y-4B, R is NCN, and R2is c-C3H5.

Table 2747. Compounds of formula I.41 wherein R1is Y-4C, R is NCN, and R2is c-C3H5.

Table 2748. Compounds of formula I.41 wherein R1is Y-4D, R is NCN, and R2is c-C3H5.

Table 2749. Compounds of formula I.41 wherein R1is Y-5A, R is NCN, and R2is c-C3H5.

Table 2750. Compounds of formula I.41 wherein R1is Y-5B, R is NCN, and R2is c-C3H5.

Table 2751. Compounds of formula I.41 wherein R1is Y-6A, R is NCN, and R2is c-C3H5.

Table 2752. Compounds of formula I.41 wherein R1is Y-6B, R is NCN, and R2is c-C3H5.

Table 2753. Compounds of formula I.41 wherein R1is Y-8A, R is NCN, and R2is c-C3H5.

Table 2754. Compounds of formula I.41 wherein R1is Y-8B, R is NCN, and R2is c-C3H5.

Table 2755. Compounds of formula I.42 wherein R1is Y-1A, R is NH, and R2is H.

Table 2756. Compounds of formula I.42 wherein R1is Y-1B, R is NH, and R2is H.

Table 2757. Compounds of formula I.42 wherein R1is Y-2A, R is NH, and R2is H.

Table 2758. Compounds of formula I.42 wherein R1is Y-2B, R is NH, and R2is H.

Table 2759. Compounds of formula I.42 wherein R1is Y-3A, R is NH, and R2is H.

Table 2760. Compounds of formula I.42 wherein R1is Y-3B, R is NH, and R2is H.

Table 2761. Compounds of formula I.42 wherein R1is Y-3C, R is NH, and R2is H.

Table 2762. Compounds of formula I.42 wherein R1is Y-3D, R is NH, and R2is H.

Table 2763. Compounds of formula I.42 wherein R1is Y-4A, R is NH, and R2is H.

Table 2764. Compounds of formula I.42 wherein R1is Y-4B, R is NH, and R2is H.

Table 2765. Compounds of formula I.42 wherein R1is Y-4C, R is NH, and R2is H.

Table 2766. Compounds of formula I.42 wherein R1is Y-4D, R is NH, and R2is H.

Table 2767. Compounds of formula I.42 wherein R1is Y-5A, R is NH, and R2is H.

Table 2768. Compounds of formula I.42 wherein R1is Y-5B, R is NH, and R2is H.

Table 2769. Compounds of formula I.42 wherein R1is Y-6A, R is NH, and R2is H.

Table 2770. Compounds of formula I.42 wherein R1is Y-6B, R is NH, and R2is H.

Table 2771. Compounds of formula I.42 wherein R1is Y-8A, R is NH, and R2is H.

Table 2772. Compounds of formula I.42 wherein R1is Y-8B, R is NH, and R2is H.

Table 2773. Compounds of formula I.42 wherein R1is Y-1A, R is NH, and R2is CH3.

Table 2774. Compounds of formula I.42 wherein R1is Y-1B, R is NH, and R2is CH3.

Table 2775. Compounds of formula I.42 wherein R1is Y-2A, R is NH, and R2is CH3.

Table 2776. Compounds of formula I.42 wherein R1is Y-2B, R is NH, and R2is CH3.

Table 2777. Compounds of formula I.42 wherein R1is Y-3A, R is NH, and R2is CH3.

Table 2778. Compounds of formula I.42 wherein R1is Y-3B, R is NH, and R2is CH3.

Table 2779. Compounds of formula I.42 wherein R1is Y-3C, R is NH, and R2is CH3.

Table 2780. Compounds of formula I.42 wherein R1is Y-3D, R is NH, and R2is CH3.

Table 2781. Compounds of formula I.42 wherein R1is Y-4A, R is NH, and R2is CH3.

Table 2782. Compounds of formula I.42 wherein R1is Y-4B, R is NH, and R2is CH3.

Table 2783. Compounds of formula I.42 wherein R1is Y-4C, R is NH, and R2is CH3.

Table 2784. Compounds of formula I.42 wherein R1is Y-4D, R is NH, and R2is CH3.

Table 2785. Compounds of formula I.42 wherein R1is Y-5A, R is NH, and R2is CH3.

Table 2786. Compounds of formula I.42 wherein R1is Y-5B, R is NH, and R2is CH3.

Table 2787. Compounds of formula I.42 wherein R1is Y-6A, R is NH, and R2is CH3.

Table 2788. Compounds of formula I.42 wherein R1is Y-6B, R is NH, and R2is CH3.

Table 2789. Compounds of formula I.42 wherein R1is Y-8A, R is NH, and R2is CH3.

Table 2790. Compounds of formula I.42 wherein R1is Y-8B, R is NH, and R2is CH3.

Table 2791. Compounds of formula I.42 wherein R1is Y-1A, R is NH, and R2is c-C3H5.

Table 2792. Compounds of formula I.42 wherein R1is Y-1B, R is NH, and R2is c-C3H5.

Table 2793. Compounds of formula I.42 wherein R1is Y-2A, R is NH, and R2is c-C3H5.

Table 2794. Compounds of formula I.42 wherein R1is Y-2B, R is NH, and R2is c-C3H5.

Table 2795. Compounds of formula I.42 wherein R1is Y-3A, R is NH, and R2is c-C3H5.

Table 2796. Compounds of formula I.42 wherein R1is Y-3B, R is NH, and R2is c-C3H5.

Table 2797. Compounds of formula I.42 wherein R1is Y-3C, R is NH, and R2is c-C3H5.

Table 2798. Compounds of formula I.42 wherein R1is Y-3D, R is NH, and R2is c-C3H5.

Table 2799. Compounds of formula I.42 wherein R1is Y-4A, R is NH, and R2is c-C3H5.

Table 2800. Compounds of formula I.42 wherein R1is Y-4B, R is NH, and R2is c-C3H5.

Table 2801. Compounds of formula I.42 wherein R1is Y-4C, R is NH, and R2is c-C3H5.

Table 2802. Compounds of formula I.42 wherein R1is Y-4D, R is NH, and R2is c-C3H5.

Table 2803. Compounds of formula I.42 wherein R1is Y-5A, R is NH, and R2is c-C3H5.

Table 2804. Compounds of formula I.42 wherein R1is Y-5B, R is NH, and R2is c-C3H5.

Table 2805. Compounds of formula I.42 wherein R1is Y-6A, R is NH, and R2is c-C3H5.

Table 2806. Compounds of formula I.42 wherein R1is Y-6B, R is NH, and R2is c-C3H5.

Table 2807. Compounds of formula I.42 wherein R1is Y-8A, R is NH, and R2is c-C3H5.

Table 2808. Compounds of formula I.42 wherein R1is Y-8B, R is NH, and R2is c-C3H5.

Table 2863. Compounds of formula I.42 wherein R1is Y-1A, R is NCN, and R2is H.

Table 2864. Compounds of formula I.42 wherein R1is Y-1B, R is NCN, and R2is H.

Table 2865. Compounds of formula I.42 wherein R1is Y-2A, R is NCN, and R2is H.

Table 2866. Compounds of formula I.42 wherein R1is Y-2B, R is NCN, and R2is H.

Table 2867. Compounds of formula I.42 wherein R1is Y-3A, R is NCN, and R2is H.

Table 2868. Compounds of formula I.42 wherein R1is Y-3B, R is NCN, and R2is H.

Table 2869. Compounds of formula I.42 wherein R1is Y-3C, R is NCN, and R2is H.

Table 2870. Compounds of formula I.42 wherein R1is Y-3D, R is NCN, and R2is H.

Table 2871. Compounds of formula I.42 wherein R1is Y-4A, R is NCN, and R2is H.

Table 2872. Compounds of formula I.42 wherein R1is Y-4B, R is NCN, and R2is H.

Table 2873. Compounds of formula I.42 wherein R1is Y-4C, R is NCN, and R2is H.

Table 2874. Compounds of formula I.42 wherein R1is Y-4D, R is NCN, and R2is H.

Table 2875. Compounds of formula I.42 wherein R1is Y-5A, R is NCN, and R2is H.

Table 2876. Compounds of formula I.42 wherein R1is Y-5B, R is NCN, and R2is H.

Table 2877. Compounds of formula I.42 wherein R1is Y-6A, R is NCN, and R2is H.

Table 2878. Compounds of formula I.42 wherein R1is Y-6B, R is NCN, and R2is H.

Table 2879. Compounds of formula I.42 wherein R1is Y-8A, R is NCN, and R2is H.

Table 2880. Compounds of formula I.42 wherein R1is Y-8B, R is NCN, and R2is H.

Table 2881. Compounds of formula I.42 wherein R1is Y-1A, R is NCN, and R2is CH3.

Table 2882. Compounds of formula I.42 wherein R1is Y-1B, R is NCN, and R2is CH3.

Table 2883. Compounds of formula I.42 wherein R1is Y-2A, R is NCN, and R2is CH3.

Table 2884. Compounds of formula I.42 wherein R1is Y-2B, R is NCN, and R2is CH3.

Table 2885. Compounds of formula I.42 wherein R1is Y-3A, R is NCN, and R2is CH3.

Table 2886. Compounds of formula I.42 wherein R1is Y-3B, R is NCN, and R2is CH3.

Table 2887. Compounds of formula I.42 wherein R1is Y-3C, R is NCN, and R2is CH3.

Table 2888. Compounds of formula I.42 wherein R1is Y-3D, R is NCN, and R2is CH3.

Table 2889. Compounds of formula I.42 wherein R1is Y-4A, R is NCN, and R2is CH3.

Table 2890. Compounds of formula I.42 wherein R1is Y-4B, R is NCN, and R2is CH3.

Table 2891. Compounds of formula I.42 wherein R1is Y-4C, R is NCN, and R2is CH3.

Table 2892. Compounds of formula I.42 wherein R1is Y-4D, R is NCN, and R2is CH3.

Table 2893. Compounds of formula I.42 wherein R1is Y-5A, R is NCN, and R2is CH3.

Table 2894. Compounds of formula I.42 wherein R1is Y-5B, R is NCN, and R2is CH3.

Table 2895. Compounds of formula I.42 wherein R1is Y-6A, R is NCN, and R2is CH3.

Table 2896. Compounds of formula I.42 wherein R1is Y-6B, R is NCN, and R2is CH3.

Table 2897. Compounds of formula I.42 wherein R1is Y-8A, R is NCN, and R2is CH3.

Table 2898. Compounds of formula I.42 wherein R1is Y-8B, R is NCN, and R2is CH3.

Table 2899. Compounds of formula I.42 wherein R1is Y-1A, R is NCN, and R2is c-C3H5.

Table 2900. Compounds of formula I.42 wherein R1is Y-1B, R is NCN, and R2is c-C3H5.

Table 2901. Compounds of formula I.42 wherein R1is Y-2A, R is NCN, and R2is c-C3H5.

Table 2902. Compounds of formula I.42 wherein R1is Y-2B, R is NCN, and R2is c-C3H5.

Table 2903. Compounds of formula I.42 wherein R1is Y-3A, R is NCN, and R2is c-C3H5.

Table 2904. Compounds of formula I.42 wherein R1is Y-3B, R is NCN, and R2is c-C3H5.

Table 2905. Compounds of formula I.42 wherein R1is Y-3C, R is NCN, and R2is c-C3H5.

Table 2906. Compounds of formula I.42 wherein R1is Y-3D, R is NCN, and R2is c-C3H5.

Table 2907. Compounds of formula I.42 wherein R1is Y-4A, R is NCN, and R2is c-C3H5.

Table 2908. Compounds of formula I.42 wherein R1is Y-4B, R is NCN, and R2is c-C3H5.

Table 2909. Compounds of formula I.42 wherein R1is Y-4C, R is NCN, and R2is c-C3H5.

Table 2910. Compounds of formula I.42 wherein R1is Y-4D, R is NCN, and R2is c-C3H5.

Table 2911. Compounds of formula I.42 wherein R1is Y-5A, R is NCN, and R2is c-C3H5.

Table 2912. Compounds of formula I.42 wherein R1is Y-5B, R is NCN, and R2is c-C3H5.

Table 2913. Compounds of formula I.42 wherein R1is Y-6A, R is NCN, and R2is c-C3H5.

Table 2914. Compounds of formula I.42 wherein R1is Y-6B, R is NCN, and R2is c-C3H5.

Table 2915. Compounds of formula I.42 wherein R1is Y-8A, R is NCN, and R2is c-C3H5.

Table 2916. Compounds of formula I.42 wherein R1is Y-8B, R is NCN, and R2is c-C3H5.

Table 2917. Compounds of formula I.43 wherein R1is Y-1A, R is NH, and R2is H.

Table 2918. Compounds of formula I.43 wherein R1is Y-1B, R is NH, and R2is H.

Table 2919. Compounds of formula I.43 wherein R1is Y-2A, R is NH, and R2is H.

Table 2920. Compounds of formula I.43 wherein R1is Y-2B, R is NH, and R2is H.

Table 2921. Compounds of formula I.43 wherein R1is Y-3A, R is NH, and R2is H.

Table 2922. Compounds of formula I.43 wherein R1is Y-3B, R is NH, and R2is H.

Table 2923. Compounds of formula I.43 wherein R1is Y-3C, R is NH, and R2is H.

Table 2924. Compounds of formula I.43 wherein R1is Y-3D, R is NH, and R2is H.

Table 2925. Compounds of formula I.43 wherein R1is Y-4A, R is NH, and R2is H.

Table 2926. Compounds of formula I.43 wherein R1is Y-4B, R is NH, and R2is H.

Table 2927. Compounds of formula I.43 wherein R1is Y-4C, R is NH, and R2is H.

Table 2928. Compounds of formula I.43 wherein R1is Y-4D, R is NH, and R2is H.

Table 2929. Compounds of formula I.43 wherein R1is Y-5A, R is NH, and R2is H.

Table 2930. Compounds of formula I.43 wherein R1is Y-5B, R is NH, and R2is H.

Table 2931. Compounds of formula I.43 wherein R1is Y-6A, R is NH, and R2is H.

Table 2932. Compounds of formula I.43 wherein R1is Y-6B, R is NH, and R2is H.

Table 2933. Compounds of formula I.43 wherein R1is Y-8A, R is NH, and R2is H.

Table 2934. Compounds of formula I.43 wherein R1is Y-8B, R is NH, and R2is H.

Table 2935. Compounds of formula I.43 wherein R1is Y-1A, R is NH, and R2is CH3.

Table 2936. Compounds of formula I.43 wherein R1is Y-1B, R is NH, and R2is CH3.

Table 2937. Compounds of formula I.43 wherein R1is Y-2A, R is NH, and R2is CH3.

Table 2938. Compounds of formula I.43 wherein R1is Y-2B, R is NH, and R2is CH3.

Table 2939. Compounds of formula I.43 wherein R1is Y-3A, R is NH, and R2is CH3.

Table 2940. Compounds of formula I.43 wherein R1is Y-3B, R is NH, and R2is CH3.

Table 2941. Compounds of formula I.43 wherein R1is Y-3C, R is NH, and R2is CH3.

Table 2942. Compounds of formula I.43 wherein R1is Y-3D, R is NH, and R2is CH3.

Table 2943. Compounds of formula I.43 wherein R1is Y-4A, R is NH, and R2is CH3.

Table 2944. Compounds of formula I.43 wherein R1is Y-4B, R is NH, and R2is CH3.

Table 2945. Compounds of formula I.43 wherein R1is Y-4C, R is NH, and R2is CH3.

Table 2946. Compounds of formula I.43 wherein R1is Y-4D, R is NH, and R2is CH3.

Table 2947. Compounds of formula I.43 wherein R1is Y-5A, R is NH, and R2is CH3.

Table 2948. Compounds of formula I.43 wherein R1is Y-5B, R is NH, and R2is CH3.

Table 2949. Compounds of formula I.43 wherein R1is Y-6A, R is NH, and R2is CH3.

Table 2950. Compounds of formula I.43 wherein R1is Y-6B, R is NH, and R2is CH3.

Table 2951. Compounds of formula I.43 wherein R1is Y-8A, R is NH, and R2is CH3.

Table 2952. Compounds of formula I.43 wherein R1is Y-8B, R is NH, and R2is CH3.

Table 2953. Compounds of formula I.43 wherein R1is Y-1A, R is NH, and R2is c-C3H5.

Table 2954. Compounds of formula I.43 wherein R1is Y-1B, R is NH, and R2is c-C3H5.

Table 2955. Compounds of formula I.43 wherein R1is Y-2A, R is NH, and R2is c-C3H5.

Table 2956. Compounds of formula I.43 wherein R1is Y-2B, R is NH, and R2is c-C3H5.

Table 2957. Compounds of formula I.43 wherein R1is Y-3A, R is NH, and R2is c-C3H5.

Table 2958. Compounds of formula I.43 wherein R1is Y-3B, R is NH, and R2is c-C3H5.

Table 2959. Compounds of formula I.43 wherein R1is Y-3C, R is NH, and R2is c-C3H5.

Table 2960. Compounds of formula I.43 wherein R1is Y-3D, R is NH, and R2is c-C3H5.

Table 2961. Compounds of formula I.43 wherein R1is Y-4A, R is NH, and R2is c-C3H5.

Table 2962. Compounds of formula I.43 wherein R1is Y-4B, R is NH, and R2is c-C3H5.

Table 2963. Compounds of formula I.43 wherein R1is Y-4C, R is NH, and R2is c-C3H5.

Table 2964. Compounds of formula I.43 wherein R1is Y-4D, R is NH, and R2is c-C3H5.

Table 2965. Compounds of formula I.43 wherein R1is Y-5A, R is NH, and R2is c-C3H5.

Table 2966. Compounds of formula I.43 wherein R1is Y-5B, R is NH, and R2is c-C3H5.

Table 2967. Compounds of formula I.43 wherein R1is Y-6A, R is NH, and R2is c-C3H5.

Table 2968. Compounds of formula I.43 wherein R1is Y-6B, R is NH, and R2is c-C3H5.

Table 2969. Compounds of formula I.43 wherein R1is Y-8A, R is NH, and R2is c-C3H5.

Table 2970. Compounds of formula I.43 wherein R1is Y-8B, R is NH, and R2is c-C3H5.

Table 3025. Compounds of formula I.43 wherein R1is Y-1A, R is NCN, and R2is H.

Table 3026. Compounds of formula I.43 wherein R1is Y-1B, R is NCN, and R2is H.

Table 3027. Compounds of formula I.43 wherein R1is Y-2A, R is NCN, and R2is H.

Table 3028. Compounds of formula I.43 wherein R1is Y-2B, R is NCN, and R2is H.

Table 3029. Compounds of formula I.43 wherein R1is Y-3A, R is NCN, and R2is H.

Table 3030. Compounds of formula I.43 wherein R1is Y-3B, R is NCN, and R2is H.

Table 3031. Compounds of formula I.43 wherein R1is Y-3C, R is NCN, and R2is H.

Table 3032. Compounds of formula I.43 wherein R1is Y-3D, R is NCN, and R2is H.

Table 3033. Compounds of formula I.43 wherein R1is Y-4A, R is NCN, and R2is H.

Table 3034. Compounds of formula I.43 wherein R1is Y-4B, R is NCN, and R2is H.

Table 3035. Compounds of formula I.43 wherein R1is Y-4C, R is NCN, and R2is H.

Table 3036. Compounds of formula I.43 wherein R1is Y-4D, R is NCN, and R2is H.

Table 3037. Compounds of formula I.43 wherein R1is Y-5A, R is NCN, and R2is H.

Table 3038. Compounds of formula I.43 wherein R1is Y-5B, R is NCN, and R2is H.

Table 3039. Compounds of formula I.43 wherein R1is Y-6A, R is NCN, and R2is H.

Table 3040. Compounds of formula I.43 wherein R1is Y-6B, R is NCN, and R2is H.

Table 3041. Compounds of formula I.43 wherein R1is Y-8A, R is NCN, and R2is H.

Table 3042. Compounds of formula I.43 wherein R1is Y-8B, R is NCN, and R2is H.

Table 3043. Compounds of formula I.43 wherein R1is Y-1A, R is NCN, and R2is CH3.

Table 3044. Compounds of formula I.43 wherein R1is Y-1B, R is NCN, and R2is CH3.

Table 3045. Compounds of formula I.43 wherein R1is Y-2A, R is NCN, and R2is CH3.

Table 3046. Compounds of formula I.43 wherein R1is Y-2B, R is NCN, and R2is CH3.

Table 3047. Compounds of formula I.43 wherein R1is Y-3A, R is NCN, and R2is CH3.

Table 3048. Compounds of formula I.43 wherein R1is Y-3B, R is NCN, and R2is CH3.

Table 3049. Compounds of formula I.43 wherein R1is Y-3C, R is NCN, and R2is CH3.

Table 3050. Compounds of formula I.43 wherein R1is Y-3D, R is NCN, and R2is CH3.

Table 3051. Compounds of formula I.43 wherein R1is Y-4A, R is NCN, and R2is CH3.

Table 3052. Compounds of formula I.43 wherein R1is Y-4B, R is NCN, and R2is CH3.

Table 3053. Compounds of formula I.43 wherein R1is Y-4C, R is NCN, and R2is CH3.

Table 3054. Compounds of formula I.43 wherein R1is Y-4D, R is NCN, and R2is CH3.

Table 3055. Compounds of formula I.43 wherein R1is Y-5A, R is NCN, and R2is CH3.

Table 3056. Compounds of formula I.43 wherein R1is Y-5B, R is NCN, and R2is CH3.

Table 3057. Compounds of formula I.43 wherein R1is Y-6A, R is NCN, and R2is CH3.

Table 3058. Compounds of formula I.43 wherein R1is Y-6B, R is NCN, and R2is CH3.

Table 3059. Compounds of formula I.43 wherein R1is Y-8A, R is NCN, and R2is CH3.

Table 3060. Compounds of formula I.43 wherein R1is Y-8B, R is NCN, and R2is CH3.

Table 3061. Compounds of formula I.43 wherein R1is Y-1A, R is NCN, and R2is c-C3H5.

Table 3062. Compounds of formula I.43 wherein R1is Y-1B, R is NCN, and R2is c-C3H5.

Table 3063. Compounds of formula I.43 wherein R1is Y-2A, R is NCN, and R2is c-C3H5.

Table 3064. Compounds of formula I.43 wherein R1is Y-2B, R is NCN, and R2is c-C3H5.

Table 3065. Compounds of formula I.43 wherein R1is Y-3A, R is NCN, and R2is c-C3H5.

Table 3066. Compounds of formula I.43 wherein R1is Y-3B, R is NCN, and R2is c-C3H5.

Table 3067. Compounds of formula I.43 wherein R1is Y-3C, R is NCN, and R2is c-C3H5.

Table 3068. Compounds of formula I.43 wherein R1is Y-3D, R is NCN, and R2is c-C3H5.

Table 3069. Compounds of formula I.43 wherein R1is Y-4A, R is NCN, and R2is c-C3H5.

Table 3070. Compounds of formula I.43 wherein R1is Y-4B, R is NCN, and R2is c-C3H5.

Table 3071. Compounds of formula I.43 wherein R1is Y-4C, R is NCN, and R2is c-C3H5.

Table 3072. Compounds of formula I.43 wherein R1is Y-4D, R is NCN, and R2is c-C3H5.

Table 3073. Compounds of formula I.43 wherein R1is Y-5A, R is NCN, and R2is c-C3H5.

Table 3074. Compounds of formula I.43 wherein R1is Y-5B, R is NCN, and R2is c-C3H5.

Table 3075. Compounds of formula I.43 wherein R1is Y-6A, R is NCN, and R2is c-C3H5.

Table 3076. Compounds of formula I.43 wherein R1is Y-6B, R is NCN, and R2is c-C3H5.

Table 3077. Compounds of formula I.43 wherein R1is Y-8A, R is NCN, and R2is c-C3H5.

Table 3078. Compounds of formula I.43 wherein R1is Y-8B, R is NCN, and R2is c-C3H5.

Table 3079. Compounds of formula I.44 wherein R1is Y-1A, R is NH, and R2is H.

Table 3080. Compounds of formula I.44 wherein R1is Y-1B, R is NH, and R2is H.

Table 3081. Compounds of formula I.44 wherein R1is Y-2A, R is NH, and R2is H.

Table 3082. Compounds of formula I.44 wherein R1is Y-2B, R is NH, and R2is H.

Table 3083. Compounds of formula I.44 wherein R1is Y-3A, R is NH, and R2is H.

Table 3084. Compounds of formula I.44 wherein R1is Y-3B, R is NH, and R2is H.

Table 3085. Compounds of formula I.44 wherein R1is Y-3C, R is NH, and R2is H.

Table 3086. Compounds of formula I.44 wherein R1is Y-3D, R is NH, and R2is H.

Table 3087. Compounds of formula I.44 wherein R1is Y-4A, R is NH, and R2is H.

Table 3088. Compounds of formula I.44 wherein R1is Y-4B, R is NH, and R2is H.

Table 3089. Compounds of formula I.44 wherein R1is Y-4C, R is NH, and R2is H.

Table 3090. Compounds of formula I.44 wherein R1is Y-4D, R is NH, and R2is H.

Table 3091. Compounds of formula I.44 wherein R1is Y-5A, R is NH, and R2is H.

Table 3092. Compounds of formula I.44 wherein R1is Y-5B, R is NH, and R2is H.

Table 3093. Compounds of formula I.44 wherein R1is Y-6A, R is NH, and R2is H.

Table 3094. Compounds of formula I.44 wherein R1is Y-6B, R is NH, and R2is H.

Table 3095. Compounds of formula I.44 wherein R1is Y-8A, R is NH, and R2is H.

Table 3096. Compounds of formula I.44 wherein R1is Y-8B, R is NH, and R2is H.

Table 3097. Compounds of formula I.44 wherein R1is Y-1A, R is NH, and R2is CH3.

Table 3098. Compounds of formula I.44 wherein R1is Y-1B, R is NH, and R2is CH3.

Table 3099. Compounds of formula I.44 wherein R1is Y-2A, R is NH, and R2is CH3.

Table 3100. Compounds of formula I.44 wherein R1is Y-2B, R is NH, and R2is CH3.

Table 3101. Compounds of formula I.44 wherein R1is Y-3A, R is NH, and R2is CH3.

Table 3102. Compounds of formula I.44 wherein R1is Y-3B, R is NH, and R2is CH3.

Table 3103. Compounds of formula I.44 wherein R1is Y-3C, R is NH, and R2is CH3.

Table 3104. Compounds of formula I.44 wherein R1is Y-3D, R is NH, and R2is CH3.

Table 3105. Compounds of formula I.44 wherein R1is Y-4A, R is NH, and R2is CH3.

Table 3106. Compounds of formula I.44 wherein R1is Y-4B, R is NH, and R2is CH3.

Table 3107. Compounds of formula I.44 wherein R1is Y-4C, R is NH, and R2is CH3.

Table 3108. Compounds of formula I.44 wherein R1is Y-4D, R is NH, and R2is CH3.

Table 3109. Compounds of formula I.44 wherein R1is Y-5A, R is NH, and R2is CH3.

Table 3110. Compounds of formula I.44 wherein R1is Y-5B, R is NH, and R2is CH3.

Table 3111. Compounds of formula I.44 wherein R1is Y-6A, R is NH, and R2is CH3.

Table 3112. Compounds of formula I.44 wherein R1is Y-6B, R is NH, and R2is CH3.

Table 3113. Compounds of formula I.44 wherein R1is Y-8A, R is NH, and R2is CH3.

Table 3114. Compounds of formula I.44 wherein R1is Y-8B, R is NH, and R2is CH3.

Table 3115. Compounds of formula I.44 wherein R1is Y-1A, R is NH, and R2is c-C3H5.

Table 3116. Compounds of formula I.44 wherein R1is Y-1B, R is NH, and R2is c-C3H5.

Table 3117. Compounds of formula I.44 wherein R1is Y-2A, R is NH, and R2is c-C3H5.

Table 3118. Compounds of formula I.44 wherein R1is Y-2B, R is NH, and R2is c-C3H5.

Table 3119. Compounds of formula I.44 wherein R1is Y-3A, R is NH, and R2is c-C3H5.

Table 3120. Compounds of formula I.44 wherein R1is Y-3B, R is NH, and R2is c-C3H5.

Table 3121. Compounds of formula I.44 wherein R1is Y-3C, R is NH, and R2is c-C3H5.

Table 3122. Compounds of formula I.44 wherein R1is Y-3D, R is NH, and R2is c-C3H5.

Table 3123. Compounds of formula I.44 wherein R1is Y-4A, R is NH, and R2is c-C3H5.

Table 3124. Compounds of formula I.44 wherein R1is Y-4B, R is NH, and R2is c-C3H5.

Table 3125. Compounds of formula I.44 wherein R1is Y-4C, R is NH, and R2is c-C3H5.

Table 3126. Compounds of formula I.44 wherein R1is Y-4D, R is NH, and R2is c-C3H5.

Table 3127. Compounds of formula I.44 wherein R1is Y-5A, R is NH, and R2is c-C3H5.

Table 3128. Compounds of formula I.44 wherein R1is Y-5B, R is NH, and R2is c-C3H5.

Table 3129. Compounds of formula I.44 wherein R1is Y-6A, R is NH, and R2is c-C3H5.

Table 3130. Compounds of formula I.44 wherein R1is Y-6B, R is NH, and R2is c-C3H5.

Table 3131. Compounds of formula I.44 wherein R1is Y-8A, R is NH, and R2is c-C3H5.

Table 3132. Compounds of formula I.44 wherein R1is Y-8B, R is NH, and R2is c-C3H5.

Table 3187. Compounds of formula I.44 wherein R1is Y-1A, R is NCN, and R2is H.

Table 3188. Compounds of formula I.44 wherein R1is Y-1B, R is NCN, and R2is H.

Table 3189. Compounds of formula I.44 wherein R1is Y-2A, R is NCN, and R2is H.

Table 3190. Compounds of formula I.44 wherein R1is Y-2B, R is NCN, and R2is H.

Table 3191. Compounds of formula I.44 wherein R1is Y-3A, R is NCN, and R2is H.

Table 3192. Compounds of formula I.44 wherein R1is Y-3B, R is NCN, and R2is H.

Table 3193. Compounds of formula I.44 wherein R1is Y-3C, R is NCN, and R2is H.

Table 3194. Compounds of formula I.44 wherein R1is Y-3D, R is NCN, and R2is H.

Table 3195. Compounds of formula I.44 wherein R1is Y-4A, R is NCN, and R2is H.

Table 3196. Compounds of formula I.44 wherein R1is Y-4B, R is NCN, and R2is H.

Table 3197. Compounds of formula I.44 wherein R1is Y-4C, R is NCN, and R2is H.

Table 3198. Compounds of formula I.44 wherein R1is Y-4D, R is NCN, and R2is H.

Table 3199. Compounds of formula I.44 wherein R1is Y-5A, R is NCN, and R2is H.

Table 3200. Compounds of formula I.44 wherein R1is Y-5B, R is NCN, and R2is H.

Table 3201. Compounds of formula I.44 wherein R1is Y-6A, R is NCN, and R2is H.

Table 3202. Compounds of formula I.44 wherein R1is Y-6B, R is NCN, and R2is H.

Table 3203. Compounds of formula I.44 wherein R1is Y-8A, R is NCN, and R2is H.

Table 3204. Compounds of formula I.44 wherein R1is Y-8B, R is NCN, and R2is H.

Table 3205. Compounds of formula I.44 wherein R1is Y-1A, R is NCN, and R2is CH3.

Table 3206. Compounds of formula I.44 wherein R1is Y-1B, R is NCN, and R2is CH3.

Table 3207. Compounds of formula I.44 wherein R1is Y-2A, R is NCN, and R2is CH3.

Table 3208. Compounds of formula I.44 wherein R1is Y-2B, R is NCN, and R2is CH3.

Table 3209. Compounds of formula I.44 wherein R1is Y-3A, R is NCN, and R2is CH3.

Table 3210. Compounds of formula I.44 wherein R1is Y-3B, R is NCN, and R2is CH3.

Table 3211. Compounds of formula I.44 wherein R1is Y-3C, R is NCN, and R2is CH3.

Table 3212. Compounds of formula I.44 wherein R1is Y-3D, R is NCN, and R2is CH3.

Table 3213. Compounds of formula I.44 wherein R1is Y-4A, R is NCN, and R2is CH3.

Table 3214. Compounds of formula I.44 wherein R1is Y-4B, R is NCN, and R2is CH3.

Table 3215. Compounds of formula I.44 wherein R1is Y-4C, R is NCN, and R2is CH3.

Table 3216. Compounds of formula I.44 wherein R1is Y-4D, R is NCN, and R2is CH3.

Table 3217. Compounds of formula I.44 wherein R1is Y-5A, R is NCN, and R2is CH3.

Table 3218. Compounds of formula I.44 wherein R1is Y-5B, R is NCN, and R2is CH3.

Table 3219. Compounds of formula I.44 wherein R1is Y-6A, R is NCN, and R2is CH3.

Table 3220. Compounds of formula I.44 wherein R1is Y-6B, R is NCN, and R2is CH3.

Table 3221. Compounds of formula I.44 wherein R1is Y-8A, R is NCN, and R2is CH3.

Table 3222. Compounds of formula I.44 wherein R1is Y-8B, R is NCN, and R2is CH3.

Table 3223. Compounds of formula I.44 wherein R1is Y-1A, R is NCN, and R2is c-C3H5.

Table 3224. Compounds of formula I.44 wherein R1is Y-1B, R is NCN, and R2is c-C3H5.

Table 3225. Compounds of formula I.44 wherein R1is Y-2A, R is NCN, and R2is c-C3H5.

Table 3226. Compounds of formula I.44 wherein R1is Y-2B, R is NCN, and R2is c-C3H5.

Table 3227. Compounds of formula I.44 wherein R1is Y-3A, R is NCN, and R2is c-C3H5.

Table 3228. Compounds of formula I.44 wherein R1is Y-3B, R is NCN, and R2is c-C3H5.

Table 3229. Compounds of formula I.44 wherein R1is Y-3C, R is NCN, and R2is c-C3H5.

Table 3230. Compounds of formula I.44 wherein R1is Y-3D, R is NCN, and R2is c-C3H5.

Table 3231. Compounds of formula I.44 wherein R1is Y-4A, R is NCN, and R2is c-C3H5.

Table 3232. Compounds of formula I.44 wherein R1is Y-4B, R is NCN, and R2is c-C3H5.

Table 3233. Compounds of formula I.44 wherein R1is Y-4C, R is NCN, and R2is c-C3H5.

Table 3234. Compounds of formula I.44 wherein R1is Y-4D, R is NCN, and R2is c-C3H5.

Table 3235. Compounds of formula I.44 wherein R1is Y-5A, R is NCN, and R2is c-C3H5.

Table 3236. Compounds of formula I.44 wherein R1is Y-5B, R is NCN, and R2is c-C3H5.

Table 3237. Compounds of formula I.44 wherein R1is Y-6A, R is NCN, and R2is c-C3H5.

Table 3238. Compounds of formula I.44 wherein R1is Y-6B, R is NCN, and R2is c-C3H5.

Table 3239. Compounds of formula I.44 wherein R1is Y-8A, R is NCN, and R2is c-C3H5.

Table 3240. Compounds of formula I.44 wherein R1is Y-8B, R is NCN, and R2is c-C3H5.

Table 3241. Compounds of formula I.45 wherein R1is Y-1A, R is NH, and R2is H.

Table 3242. Compounds of formula I.45 wherein R1is Y-1B, R is NH, and R2is H.

Table 3243. Compounds of formula I.45 wherein R1is Y-2A, R is NH, and R2is H.

Table 3244. Compounds of formula I.45 wherein R1is Y-2B, R is NH, and R2is H.

Table 3245. Compounds of formula I.45 wherein R1is Y-3A, R is NH, and R2is H.

Table 3246. Compounds of formula I.45 wherein R1is Y-3B, R is NH, and R2is H.

Table 3247. Compounds of formula I.45 wherein R1is Y-3C, R is NH, and R2is H.

Table 3248. Compounds of formula I.45 wherein R1is Y-3D, R is NH, and R2is H.

Table 3249. Compounds of formula I.45 wherein R1is Y-4A, R is NH, and R2is H.

Table 3250. Compounds of formula I.45 wherein R1is Y-4B, R is NH, and R2is H.

Table 3251. Compounds of formula I.45 wherein R1is Y-4C, R is NH, and R2is H.

Table 3252. Compounds of formula I.45 wherein R1is Y-4D, R is NH, and R2is H.

Table 3253. Compounds of formula I.45 wherein R1is Y-5A, R is NH, and R2is H.

Table 3254. Compounds of formula I.45 wherein R1is Y-5B, R is NH, and R2is H.

Table 3255. Compounds of formula I.45 wherein R1is Y-6A, R is NH, and R2is H.

Table 3256. Compounds of formula I.45 wherein R1is Y-6B, R is NH, and R2is H.

Table 3257. Compounds of formula I.45 wherein R1is Y-8A, R is NH, and R2is H.

Table 3258. Compounds of formula I.45 wherein R1is Y-8B, R is NH, and R2is H.

Table 3259. Compounds of formula I.45 wherein R1is Y-1A, R is NH, and R2is CH3.

Table 3260. Compounds of formula I.45 wherein R1is Y-1B, R is NH, and R2is CH3.

Table 3261. Compounds of formula I.45 wherein R1is Y-2A, R is NH, and R2is CH3.

Table 3262. Compounds of formula I.45 wherein R1is Y-2B, R is NH, and R2is CH3.

Table 3263. Compounds of formula I.45 wherein R1is Y-3A, R is NH, and R2is CH3.

Table 3264. Compounds of formula I.45 wherein R1is Y-3B, R is NH, and R2is CH3.

Table 3265. Compounds of formula I.45 wherein R1is Y-3C, R is NH, and R2is CH3.

Table 3266. Compounds of formula I.45 wherein R1is Y-3D, R is NH, and R2is CH3.

Table 3267. Compounds of formula I.45 wherein R1is Y-4A, R is NH, and R2is CH3.

Table 3268. Compounds of formula I.45 wherein R1is Y-4B, R is NH, and R2is CH3.

Table 3269. Compounds of formula I.45 wherein R1is Y-4C, R is NH, and R2is CH3.

Table 3270. Compounds of formula I.45 wherein R1is Y-4D, R is NH, and R2is CH3.

Table 3271. Compounds of formula I.45 wherein R1is Y-5A, R is NH, and R2is CH3.

Table 3272. Compounds of formula I.45 wherein R1is Y-5B, R is NH, and R2is CH3.

Table 3273. Compounds of formula I.45 wherein R1is Y-6A, R is NH, and R2is CH3.

Table 3274. Compounds of formula I.45 wherein R1is Y-6B, R is NH, and R2is CH3.

Table 3275. Compounds of formula I.45 wherein R1is Y-8A, R is NH, and R2is CH3.

Table 3276. Compounds of formula I.45 wherein R1is Y-8B, R is NH, and R2is CH3.

Table 3277. Compounds of formula I.45 wherein R1is Y-1A, R is NH, and R2is c-C3H5.

Table 3278. Compounds of formula I.45 wherein R1is Y-1B, R is NH, and R2is c-C3H5.

Table 3279. Compounds of formula I.45 wherein R1is Y-2A, R is NH, and R2is c-C3H5.

Table 3280. Compounds of formula I.45 wherein R1is Y-2B, R is NH, and R2is c-C3H5.

Table 3281. Compounds of formula I.45 wherein R1is Y-3A, R is NH, and R2is c-C3H5.

Table 3282. Compounds of formula I.45 wherein R1is Y-3B, R is NH, and R2is c-C3H5.

Table 3283. Compounds of formula I.45 wherein R1is Y-3C, R is NH, and R2is c-C3H5.

Table 3284. Compounds of formula I.45 wherein R1is Y-3D, R is NH, and R2is c-C3H5.

Table 3285. Compounds of formula I.45 wherein R1is Y-4A, R is NH, and R2is c-C3H5.

Table 3286. Compounds of formula I.45 wherein R1is Y-4B, R is NH, and R2is c-C3H5.

Table 3287. Compounds of formula I.45 wherein R1is Y-4C, R is NH, and R2is c-C3H5.

Table 3288. Compounds of formula I.45 wherein R1is Y-4D, R is NH, and R2is c-C3H5.

Table 3289. Compounds of formula I.45 wherein R1is Y-5A, R is NH, and R2is c-C3H5.

Table 3290. Compounds of formula I.45 wherein R1is Y-5B, R is NH, and R2is c-C3H5.

Table 3291. Compounds of formula I.45 wherein R1is Y-6A, R is NH, and R2is c-C3H5.

Table 3292. Compounds of formula I.45 wherein R1is Y-6B, R is NH, and R2is c-C3H5.

Table 3293. Compounds of formula I.45 wherein R1is Y-8A, R is NH, and R2is c-C3H5.

Table 3294. Compounds of formula I.45 wherein R1is Y-8B, R is NH, and R2is c-C3H5.

Table 3349. Compounds of formula I.45 wherein R1is Y-1A, R is NCN, and R2is H.

Table 3350. Compounds of formula I.45 wherein R1is Y-1B, R is NCN, and R2is H.

Table 3351. Compounds of formula I.45 wherein R1is Y-2A, R is NCN, and R2is H.

Table 3352. Compounds of formula I.45 wherein R1is Y-2B, R is NCN, and R2is H.

Table 3353. Compounds of formula I.45 wherein R1is Y-3A, R is NCN, and R2is H.

Table 3354. Compounds of formula I.45 wherein R1is Y-3B, R is NCN, and R2is H.

Table 3355. Compounds of formula I.45 wherein R1is Y-3C, R is NCN, and R2is H.

Table 3356. Compounds of formula I.45 wherein R1is Y-3D, R is NCN, and R2is H.

Table 3357. Compounds of formula I.45 wherein R1is Y-4A, R is NCN, and R2is H.

Table 3358. Compounds of formula I.45 wherein R1is Y-4B, R is NCN, and R2is H.

Table 3359. Compounds of formula I.45 wherein R1is Y-4C, R is NCN, and R2is H.

Table 3360. Compounds of formula I.45 wherein R1is Y-4D, R is NCN, and R2is H.

Table 3361. Compounds of formula I.45 wherein R1is Y-5A, R is NCN, and R2is H.

Table 3362. Compounds of formula I.45 wherein R1is Y-5B, R is NCN, and R2is H.

Table 3363. Compounds of formula I.45 wherein R1is Y-6A, R is NCN, and R2is H.

Table 3364. Compounds of formula I.45 wherein R1is Y-6B, R is NCN, and R2is H.

Table 3365. Compounds of formula I.45 wherein R1is Y-8A, R is NCN, and R2is H.

Table 3366. Compounds of formula I.45 wherein R1is Y-8B, R is NCN, and R2is H.

Table 3367. Compounds of formula I.45 wherein R1is Y-1A, R is NCN, and R2is CH3.

Table 3368. Compounds of formula I.45 wherein R1is Y-1B, R is NCN, and R2is CH3.

Table 3369. Compounds of formula I.45 wherein R1is Y-2A, R is NCN, and R2is CH3.

Table 3370. Compounds of formula I.45 wherein R1is Y-2B, R is NCN, and R2is CH3.

Table 3371. Compounds of formula I.45 wherein R1is Y-3A, R is NCN, and R2is CH3.

Table 3372. Compounds of formula I.45 wherein R1is Y-3B, R is NCN, and R2is CH3.

Table 3373. Compounds of formula I.45 wherein R1is Y-3C, R is NCN, and R2is CH3.

Table 3374. Compounds of formula I.45 wherein R1is Y-3D, R is NCN, and R2is CH3.

Table 3375. Compounds of formula I.45 wherein R1is Y-4A, R is NCN, and R2is CH3.

Table 3376. Compounds of formula I.45 wherein R1is Y-4B, R is NCN, and R2is CH3.

Table 3377. Compounds of formula I.45 wherein R1is Y-4C, R is NCN, and R2is CH3.

Table 3378. Compounds of formula I.45 wherein R1is Y-4D, R is NCN, and R2is CH3.

Table 3379. Compounds of formula I.45 wherein R1is Y-5A, R is NCN, and R2is CH3.

Table 3380. Compounds of formula I.45 wherein R1is Y-5B, R is NCN, and R2is CH3.

Table 3381. Compounds of formula I.45 wherein R1is Y-6A, R is NCN, and R2is CH3.

Table 3382. Compounds of formula I.45 wherein R1is Y-6B, R is NCN, and R2is CH3.

Table 3383. Compounds of formula I.45 wherein R1is Y-8A, R is NCN, and R2is CH3.

Table 3384. Compounds of formula I.45 wherein R1is Y-8B, R is NCN, and R2is CH3.

Table 3385. Compounds of formula I.45 wherein R1is Y-1A, R is NCN, and R2is c-C3H5.

Table 3386. Compounds of formula I.45 wherein R1is Y-1B, R is NCN, and R2is c-C3H5.

Table 3387. Compounds of formula I.45 wherein R1is Y-2A, R is NCN, and R2is c-C3H5.

Table 3388. Compounds of formula I.45 wherein R1is Y-2B, R is NCN, and R2is c-C3H5.

Table 3389. Compounds of formula I.45 wherein R1is Y-3A, R is NCN, and R2is c-C3H5.

Table 3390. Compounds of formula I.45 wherein R1is Y-3B, R is NCN, and R2is c-C3H5.

Table 3391. Compounds of formula I.45 wherein R1is Y-3C, R is NCN, and R2is c-C3H5.

Table 3392. Compounds of formula I.45 wherein R1is Y-3D, R is NCN, and R2is c-C3H5.

Table 3393. Compounds of formula I.45 wherein R1is Y-4A, R is NCN, and R2is c-C3H5.

Table 3394. Compounds of formula I.45 wherein R1is Y-4B, R is NCN, and R2is c-C3H5.

Table 3395. Compounds of formula I.45 wherein R1is Y-4C, R is NCN, and R2is c-C3H5.

Table 3396. Compounds of formula I.45 wherein R1is Y-4D, R is NCN, and R2is c-C3H5.

Table 3397. Compounds of formula I.45 wherein R1is Y-5A, R is NCN, and R2is c-C3H5.

Table 3398. Compounds of formula I.45 wherein R1is Y-5B, R is NCN, and R2is c-C3H5.

Table 3399. Compounds of formula I.45 wherein R1is Y-6A, R is NCN, and R2is c-C3H5.

Table 3400. Compounds of formula I.45 wherein R1is Y-6B, R is NCN, and R2is c-C3H5.

Table 3401. Compounds of formula I.45 wherein R1is Y-8A, R is NCN, and R2is c-C3H5.

Table 3402. Compounds of formula I.45 wherein R1is Y-8B, R is NCN, and R2is c-C3H5.

Table 3403. Compounds of formula I.46 wherein R1is Y-1A, R is NH, and R2is H.

Table 3404. Compounds of formula I.46 wherein R1is Y-1B, R is NH, and R2is H.

Table 3405. Compounds of formula I.46 wherein R1is Y-2A, R is NH, and R2is H.

Table 3406. Compounds of formula I.46 wherein R1is Y-2B, R is NH, and R2is H.

Table 3407. Compounds of formula I.46 wherein R1is Y-3A, R is NH, and R2is H.

Table 3408. Compounds of formula I.46 wherein R1is Y-3B, R is NH, and R2is H.

Table 3409. Compounds of formula I.46 wherein R1is Y-3C, R is NH, and R2is H.

Table 3410. Compounds of formula I.46 wherein R1is Y-3D, R is NH, and R2is H.

Table 3411. Compounds of formula I.46 wherein R1is Y-4A, R is NH, and R2is H.

Table 3412. Compounds of formula I.46 wherein R1is Y-4B, R is NH, and R2is H.

Table 3413. Compounds of formula I.46 wherein R1is Y-4C, R is NH, and R2is H.

Table 3414. Compounds of formula I.46 wherein R1is Y-4D, R is NH, and R2is H.

Table 3415. Compounds of formula I.46 wherein R1is Y-5A, R is NH, and R2is H.

Table 3416. Compounds of formula I.46 wherein R1is Y-5B, R is NH, and R2is H.

Table 3417. Compounds of formula I.46 wherein R1is Y-6A, R is NH, and R2is H.

Table 3418. Compounds of formula I.46 wherein R1is Y-6B, R is NH, and R2is H.

Table 3419. Compounds of formula I.46 wherein R1is Y-8A, R is NH, and R2is H.

Table 3420. Compounds of formula I.46 wherein R1is Y-8B, R is NH, and R2is H.

Table 3421. Compounds of formula I.46 wherein R1is Y-1A, R is NH, and R2is CH3.

Table 3422. Compounds of formula I.46 wherein R1is Y-1B, R is NH, and R2is CH3.

Table 3423. Compounds of formula I.46 wherein R1is Y-2A, R is NH, and R2is CH3.

Table 3424. Compounds of formula I.46 wherein R1is Y-2B, R is NH, and R2is CH3.

Table 3425. Compounds of formula I.46 wherein R1is Y-3A, R is NH, and R2is CH3.

Table 3426. Compounds of formula I.46 wherein R1is Y-3B, R is NH, and R2is CH3.

Table 3427. Compounds of formula I.46 wherein R1is Y-3C, R is NH, and R2is CH3.

Table 3428. Compounds of formula I.46 wherein R1is Y-3D, R is NH, and R2is CH3.

Table 3429. Compounds of formula I.46 wherein R1is Y-4A, R is NH, and R2is CH3.

Table 3430. Compounds of formula I.46 wherein R1is Y-4B, R is NH, and R2is CH3.

Table 3431. Compounds of formula I.46 wherein R1is Y-4C, R is NH, and R2is CH3.

Table 3432. Compounds of formula I.46 wherein R1is Y-4D, R is NH, and R2is CH3.

Table 3433. Compounds of formula I.46 wherein R1is Y-5A, R is NH, and R2is CH3.

Table 3434. Compounds of formula I.46 wherein R1is Y-5B, R is NH, and R2is CH3.

Table 3435. Compounds of formula I.46 wherein R1is Y-6A, R is NH, and R2is CH3.

Table 3436. Compounds of formula I.46 wherein R1is Y-6B, R is NH, and R2is CH3.

Table 3437. Compounds of formula I.46 wherein R1is Y-8A, R is NH, and R2is CH3.

Table 3438. Compounds of formula I.46 wherein R1is Y-8B, R is NH, and R2is CH3.

Table 3439. Compounds of formula I.46 wherein R1is Y-1A, R is NH, and R2is c-C3H5.

Table 3440. Compounds of formula I.46 wherein R1is Y-1B, R is NH, and R2is c-C3H5.

Table 3441. Compounds of formula I.46 wherein R1is Y-2A, R is NH, and R2is c-C3H5.

Table 3442. Compounds of formula I.46 wherein R1is Y-2B, R is NH, and R2is c-C3H5.

Table 3443. Compounds of formula I.46 wherein R1is Y-3A, R is NH, and R2is c-C3H5.

Table 3444. Compounds of formula I.46 wherein R1is Y-3B, R is NH, and R2is c-C3H5.

Table 3445. Compounds of formula I.46 wherein R1is Y-3C, R is NH, and R2is c-C3H5.

Table 3446. Compounds of formula I.46 wherein R1is Y-3D, R is NH, and R2is c-C3H5.

Table 3447. Compounds of formula I.46 wherein R1is Y-4A, R is NH, and R2is c-C3H5.

Table 3448. Compounds of formula I.46 wherein R1is Y-4B, R is NH, and R2is c-C3H5.

Table 3449. Compounds of formula I.46 wherein R1is Y-4C, R is NH, and R2is c-C3H5.

Table 3450. Compounds of formula I.46 wherein R1is Y-4D, R is NH, and R2is c-C3H5.

Table 3451. Compounds of formula I.46 wherein R1is Y-5A, R is NH, and R2is c-C3H5.

Table 3452. Compounds of formula I.46 wherein R1is Y-5B, R is NH, and R2is c-C3H5.

Table 3453. Compounds of formula I.46 wherein R1is Y-6A, R is NH, and R2is c-C3H5.

Table 3454. Compounds of formula I.46 wherein R1is Y-6B, R is NH, and R2is c-C3H5.

Table 3455. Compounds of formula I.46 wherein R1is Y-8A, R is NH, and R2is c-C3H5.

Table 3456. Compounds of formula I.46 wherein R1is Y-8B, R is NH, and R2is c-C3H5.

Table 3511. Compounds of formula I.46 wherein R1is Y-1A, R is NCN, and R2is H.

Table 3512. Compounds of formula I.46 wherein R1is Y-1B, R is NCN, and R2is H.

Table 3513. Compounds of formula I.46 wherein R1is Y-2A, R is NCN, and R2is H.

Table 3514. Compounds of formula I.46 wherein R1is Y-2B, R is NCN, and R2is H.

Table 3515. Compounds of formula I.46 wherein R1is Y-3A, R is NCN, and R2is H.

Table 3516. Compounds of formula I.46 wherein R1is Y-3B, R is NCN, and R2is H.

Table 3517. Compounds of formula I.46 wherein R1is Y-3C, R is NCN, and R2is H.

Table 3518. Compounds of formula I.46 wherein R1is Y-3D, R is NCN, and R2is H.

Table 3519. Compounds of formula I.46 wherein R1is Y-4A, R is NCN, and R2is H.

Table 3520. Compounds of formula I.46 wherein R1is Y-4B, R is NCN, and R2is H.

Table 3521. Compounds of formula I.46 wherein R1is Y-4C, R is NCN, and R2is H.

Table 3522. Compounds of formula I.46 wherein R1is Y-4D, R is NCN, and R2is H.

Table 3523. Compounds of formula I.46 wherein R1is Y-5A, R is NCN, and R2is H.

Table 3524. Compounds of formula I.46 wherein R1is Y-5B, R is NCN, and R2is H.

Table 3525. Compounds of formula I.46 wherein R1is Y-6A, R is NCN, and R2is H.

Table 3526. Compounds of formula I.46 wherein R1is Y-6B, R is NCN, and R2is H.

Table 3527. Compounds of formula I.46 wherein R1is Y-8A, R is NCN, and R2is H.

Table 3528. Compounds of formula I.46 wherein R1is Y-8B, R is NCN, and R2is H.

Table 3529. Compounds of formula I.46 wherein R1is Y-1A, R is NCN, and R2is CH3.

Table 3530. Compounds of formula I.46 wherein R1is Y-1B, R is NCN, and R2is CH3.

Table 3531. Compounds of formula I.46 wherein R1is Y-2A, R is NCN, and R2is CH3.

Table 3532. Compounds of formula I.46 wherein R1is Y-2B, R is NCN, and R2is CH3.

Table 3533. Compounds of formula I.46 wherein R1is Y-3A, R is NCN, and R2is CH3.

Table 3534. Compounds of formula I.46 wherein R1is Y-3B, R is NCN, and R2is CH3.

Table 3535. Compounds of formula I.46 wherein R1is Y-3C, R is NCN, and R2is CH3.

Table 3536. Compounds of formula I.46 wherein R1is Y-3D, R is NCN, and R2is CH3.

Table 3537. Compounds of formula I.46 wherein R1is Y-4A, R is NCN, and R2is CH3.

Table 3538. Compounds of formula I.46 wherein R1is Y-4B, R is NCN, and R2is CH3.

Table 3539. Compounds of formula I.46 wherein R1is Y-4C, R is NCN, and R2is CH3.

Table 3540. Compounds of formula I.46 wherein R1is Y-4D, R is NCN, and R2is CH3.

Table 3541. Compounds of formula I.46 wherein R1is Y-5A, R is NCN, and R2is CH3.

Table 3542. Compounds of formula I.46 wherein R1is Y-5B, R is NCN, and R2is CH3.

Table 3543. Compounds of formula I.46 wherein R1is Y-6A, R is NCN, and R2is CH3.

Table 3544. Compounds of formula I.46 wherein R1is Y-6B, R is NCN, and R2is CH3.

Table 3545. Compounds of formula I.46 wherein R1is Y-8A, R is NCN, and R2is CH3.

Table 3546. Compounds of formula I.46 wherein R1is Y-8B, R is NCN, and R2is CH3.

Table 3547. Compounds of formula I.46 wherein R1is Y-1A, R is NCN, and R2is c-C3H5.

Table 3548. Compounds of formula I.46 wherein R1is Y-1B, R is NCN, and R2is c-C3H5.

Table 3549. Compounds of formula I.46 wherein R1is Y-2A, R is NCN, and R2is c-C3H5.

Table 3550. Compounds of formula I.46 wherein R1is Y-2B, R is NCN, and R2is c-C3H5.

Table 3551. Compounds of formula I.46 wherein R1is Y-3A, R is NCN, and R2is c-C3H5.

Table 3552. Compounds of formula I.46 wherein R1is Y-3B, R is NCN, and R2is c-C3H5.

Table 3553. Compounds of formula I.46 wherein R1is Y-3C, R is NCN, and R2is c-C3H5.

Table 3554. Compounds of formula I.46 wherein R1is Y-3D, R is NCN, and R2is c-C3H5.

Table 3555. Compounds of formula I.46 wherein R1is Y-4A, R is NCN, and R2is c-C3H5.

Table 3556. Compounds of formula I.46 wherein R1is Y-4B, R is NCN, and R2is c-C3H5.

Table 3557. Compounds of formula I.46 wherein R1is Y-4C, R is NCN, and R2is c-C3H5.

Table 3558. Compounds of formula I.46 wherein R1is Y-4D, R is NCN, and R2is c-C3H5.

Table 3559. Compounds of formula I.46 wherein R1is Y-5A, R is NCN, and R2is c-C3H5.

Table 3560. Compounds of formula I.46 wherein R1is Y-5B, R is NCN, and R2is c-C3H5.

Table 3561. Compounds of formula I.46 wherein R1is Y-6A, R is NCN, and R2is c-C3H5.

Table 3562. Compounds of formula I.46 wherein R1is Y-6B, R is NCN, and R2is c-C3H5.

Table 3563. Compounds of formula I.46 wherein R1is Y-8A, R is NCN, and R2is c-C3H5.

Table 3564. Compounds of formula I.46 wherein R1is Y-8B, R is NCN, and R2is c-C3H5.

Table 3565. Compounds of formula I.47 wherein R1is Y-1A, R is NH, and R2is H.

Table 3566. Compounds of formula I.47 wherein R1is Y-1B, R is NH, and R2is H.

Table 3567. Compounds of formula I.47 wherein R1is Y-2A, R is NH, and R2is H.

Table 3568. Compounds of formula I.47 wherein R1is Y-2B, R is NH, and R2is H.

Table 3569. Compounds of formula I.47 wherein R1is Y-3A, R is NH, and R2is H.

Table 3570. Compounds of formula I.47 wherein R1is Y-3B, R is NH, and R2is H.

Table 3571. Compounds of formula I.47 wherein R1is Y-3C, R is NH, and R2is H.

Table 3572. Compounds of formula I.47 wherein R1is Y-3D, R is NH, and R2is H.

Table 3573. Compounds of formula I.47 wherein R1is Y-4A, R is NH, and R2is H.

Table 3574. Compounds of formula I.47 wherein R1is Y-4B, R is NH, and R2is H.

Table 3575. Compounds of formula I.47 wherein R1is Y-4C, R is NH, and R2is H.

Table 3576. Compounds of formula I.47 wherein R1is Y-4D, R is NH, and R2is H.

Table 3577. Compounds of formula I.47 wherein R1is Y-5A, R is NH, and R2is H.

Table 3578. Compounds of formula I.47 wherein R1is Y-5B, R is NH, and R2is H.

Table 3579. Compounds of formula I.47 wherein R1is Y-6A, R is NH, and R2is H.

Table 3580. Compounds of formula I.47 wherein R1is Y-6B, R is NH, and R2is H.

Table 3581. Compounds of formula I.47 wherein R1is Y-8A, R is NH, and R2is H.

Table 3582. Compounds of formula I.47 wherein R1is Y-8B, R is NH, and R2is H.

Table 3583. Compounds of formula I.47 wherein R1is Y-1A, R is NH, and R2is CH3.

Table 3584. Compounds of formula I.47 wherein R1is Y-1B, R is NH, and R2is CH3.

Table 3585. Compounds of formula I.47 wherein R1is Y-2A, R is NH, and R2is CH3.

Table 3586. Compounds of formula I.47 wherein R1is Y-2B, R is NH, and R2is CH3.

Table 3587. Compounds of formula I.47 wherein R1is Y-3A, R is NH, and R2is CH3.

Table 3588. Compounds of formula I.47 wherein R1is Y-3B, R is NH, and R2is CH3.

Table 3589. Compounds of formula I.47 wherein R1is Y-3C, R is NH, and R2is CH3.

Table 3590. Compounds of formula I.47 wherein R1is Y-3D, R is NH, and R2is CH3.

Table 3591. Compounds of formula I.47 wherein R1is Y-4A, R is NH, and R2is CH3.

Table 3592. Compounds of formula I.47 wherein R1is Y-4B, R is NH, and R2is CH3.

Table 3593. Compounds of formula I.47 wherein R1is Y-4C, R is NH, and R2is CH3.

Table 3594. Compounds of formula I.47 wherein R1is Y-4D, R is NH, and R2is CH3.

Table 3595. Compounds of formula I.47 wherein R1is Y-5A, R is NH, and R2is CH3.

Table 3596. Compounds of formula I.47 wherein R1is Y-5B, R is NH, and R2is CH3.

Table 3597. Compounds of formula I.47 wherein R1is Y-6A, R is NH, and R2is CH3.

Table 3598. Compounds of formula I.47 wherein R1is Y-6B, R is NH, and R2is CH3.

Table 3599. Compounds of formula I.47 wherein R1is Y-8A, R is NH, and R2is CH3.

Table 3600. Compounds of formula I.47 wherein R1is Y-8B, R is NH, and R2is CH3.

Table 3601. Compounds of formula I.47 wherein R1is Y-1A, R is NH, and R2is c-C3H5.

Table 3602. Compounds of formula I.47 wherein R1is Y-1B, R is NH, and R2is c-C3H5.

Table 3603. Compounds of formula I.47 wherein R1is Y-2A, R is NH, and R2is c-C3H5.

Table 3604. Compounds of formula I.47 wherein R1is Y-2B, R is NH, and R2is c-C3H5.

Table 3605. Compounds of formula I.47 wherein R1is Y-3A, R is NH, and R2is c-C3H5.

Table 3606. Compounds of formula I.47 wherein R1is Y-3B, R is NH, and R2is c-C3H5.

Table 3607. Compounds of formula I.47 wherein R1is Y-3C, R is NH, and R2is c-C3H5.

Table 3608. Compounds of formula I.47 wherein R1is Y-3D, R is NH, and R2is c-C3H5.

Table 3609. Compounds of formula I.47 wherein R1is Y-4A, R is NH, and R2is c-C3H5.

Table 3610. Compounds of formula I.47 wherein R1is Y-4B, R is NH, and R2is c-C3H5.

Table 3611. Compounds of formula I.47 wherein R1is Y-4C, R is NH, and R2is c-C3H5.

Table 3612. Compounds of formula I.47 wherein R1is Y-4D, R is NH, and R2is c-C3H5.

Table 3613. Compounds of formula I.47 wherein R1is Y-5A, R is NH, and R2is c-C3H5.

Table 3614. Compounds of formula I.47 wherein R1is Y-5B, R is NH, and R2is c-C3H5.

Table 3615. Compounds of formula I.47 wherein R1is Y-6A, R is NH, and R2is c-C3H5.

Table 3616. Compounds of formula I.47 wherein R1is Y-6B, R is NH, and R2is c-C3H5.

Table 3617. Compounds of formula I.47 wherein R1is Y-8A, R is NH, and R2is c-C3H5.

Table 3618. Compounds of formula I.47 wherein R1is Y-8B, R is NH, and R2is c-C3H5.

Table 3673. Compounds of formula I.47 wherein R1is Y-1A, R is NCN, and R2is H.

Table 3674. Compounds of formula I.47 wherein R1is Y-1B, R is NCN, and R2is H.

Table 3675. Compounds of formula I.47 wherein R1is Y-2A, R is NCN, and R2is H.

Table 3676. Compounds of formula I.47 wherein R1is Y-2B, R is NCN, and R2is H.

Table 3677. Compounds of formula I.47 wherein R1is Y-3A, R is NCN, and R2is H.

Table 3678. Compounds of formula I.47 wherein R1is Y-3B, R is NCN, and R2is H.

Table 3679. Compounds of formula I.47 wherein R1is Y-3C, R is NCN, and R2is H.

Table 3680. Compounds of formula I.47 wherein R1is Y-3D, R is NCN, and R2is H.

Table 3681. Compounds of formula I.47 wherein R1is Y-4A, R is NCN, and R2is H.

Table 3682. Compounds of formula I.47 wherein R1is Y-4B, R is NCN, and R2is H.

Table 3683. Compounds of formula I.47 wherein R1is Y-4C, R is NCN, and R2is H.

Table 3684. Compounds of formula I.47 wherein R1is Y-4D, R is NCN, and R2is H.

Table 3685. Compounds of formula I.47 wherein R1is Y-5A, R is NCN, and R2is H.

Table 3686. Compounds of formula I.47 wherein R1is Y-5B, R is NCN, and R2is H.

Table 3687. Compounds of formula I.47 wherein R1is Y-6A, R is NCN, and R2is H.

Table 3688. Compounds of formula I.47 wherein R1is Y-6B, R is NCN, and R2is H.

Table 3689. Compounds of formula I.47 wherein R1is Y-8A, R is NCN, and R2is H.

Table 3690. Compounds of formula I.47 wherein R1is Y-8B, R is NCN, and R2is H.

Table 3691. Compounds of formula I.47 wherein R1is Y-1A, R is NCN, and R2is CH3.

Table 3692. Compounds of formula I.47 wherein R1is Y-1B, R is NCN, and R2is CH3.

Table 3693. Compounds of formula I.47 wherein R1is Y-2A, R is NCN, and R2is CH3.

Table 3694. Compounds of formula I.47 wherein R1is Y-2B, R is NCN, and R2is CH3.

Table 3695. Compounds of formula I.47 wherein R1is Y-3A, R is NCN, and R2is CH3.

Table 3696. Compounds of formula I.47 wherein R1is Y-3B, R is NCN, and R2is CH3.

Table 3697. Compounds of formula I.47 wherein R1is Y-3C, R is NCN, and R2is CH3.

Table 3698. Compounds of formula I.47 wherein R1is Y-3D, R is NCN, and R2is CH3.

Table 3699. Compounds of formula I.47 wherein R1is Y-4A, R is NCN, and R2is CH3.

Table 3700. Compounds of formula I.47 wherein R1is Y-4B, R is NCN, and R2is CH3.

Table 3701. Compounds of formula I.47 wherein R1is Y-4C, R is NCN, and R2is CH3.

Table 3702. Compounds of formula I.47 wherein R1is Y-4D, R is NCN, and R2is CH3.

Table 3703. Compounds of formula I.47 wherein R1is Y-5A, R is NCN, and R2is CH3.

Table 3704. Compounds of formula I.47 wherein R1is Y-5B, R is NCN, and R2is CH3.

Table 3705. Compounds of formula I.47 wherein R1is Y-6A, R is NCN, and R2is CH3.

Table 3706. Compounds of formula I.47 wherein R1is Y-6B, R is NCN, and R2is CH3.

Table 3707. Compounds of formula I.47 wherein R1is Y-8A, R is NCN, and R2is CH3.

Table 3708. Compounds of formula I.47 wherein R1is Y-8B, R is NCN, and R2is CH3.

Table 3709. Compounds of formula I.47 wherein R1is Y-1A, R is NCN, and R2is c-C3H5.

Table 3710. Compounds of formula I.47 wherein R1is Y-1B, R is NCN, and R2is c-C3H5.

Table 3711. Compounds of formula I.47 wherein R1is Y-2A, R is NCN, and R2is c-C3H5.

Table 3712. Compounds of formula I.47 wherein R1is Y-2B, R is NCN, and R2is c-C3H5.

Table 3713. Compounds of formula I.47 wherein R1is Y-3A, R is NCN, and R2is c-C3H5.

Table 3714. Compounds of formula I.47 wherein R1is Y-3B, R is NCN, and R2is c-C3H5.

Table 3715. Compounds of formula I.47 wherein R1is Y-3C, R is NCN, and R2is c-C3H5.

Table 3716. Compounds of formula I.47 wherein R1is Y-3D, R is NCN, and R2is c-C3H5.

Table 3717. Compounds of formula I.47 wherein R1is Y-4A, R is NCN, and R2is c-C3H5.

Table 3718. Compounds of formula I.47 wherein R1is Y-4B, R is NCN, and R2is c-C3H5.

Table 3719. Compounds of formula I.47 wherein R1is Y-4C, R is NCN, and R2is c-C3H5.

Table 3720. Compounds of formula I.47 wherein R1is Y-4D, R is NCN, and R2is c-C3H5.

Table 3721. Compounds of formula I.47 wherein R1is Y-5A, R is NCN, and R2is c-C3H5.

Table 3722. Compounds of formula I.47 wherein R1is Y-5B, R is NCN, and R2is c-C3H5.

Table 3723. Compounds of formula I.47 wherein R1is Y-6A, R is NCN, and R2is c-C3H5.

Table 3724. Compounds of formula I.47 wherein R1is Y-6B, R is NCN, and R2is c-C3H5.

Table 3725. Compounds of formula I.47 wherein R1is Y-8A, R is NCN, and R2is c-C3H5.

Table 3726. Compounds of formula I.47 wherein R1is Y-8B, R is NCN, and R2is c-C3H5.

Table 3727. Compounds of formula I.48 wherein R1is Y-1A, R is NH, and R2is H.

Table 3728. Compounds of formula I.48 wherein R1is Y-1B, R is NH, and R2is H.

Table 3729. Compounds of formula I.48 wherein R1is Y-2A, R is NH, and R2is H.

Table 3730. Compounds of formula I.48 wherein R1is Y-2B, R is NH, and R2is H.

Table 3731. Compounds of formula I.48 wherein R1is Y-3A, R is NH, and R2is H.

Table 3732. Compounds of formula I.48 wherein R1is Y-3B, R is NH, and R2is H.

Table 3733. Compounds of formula I.48 wherein R1is Y-3C, R is NH, and R2is H.

Table 3734. Compounds of formula I.48 wherein R1is Y-3D, R is NH, and R2is H.

Table 3735. Compounds of formula I.48 wherein R1is Y-4A, R is NH, and R2is H.

Table 3736. Compounds of formula I.48 wherein R1is Y-4B, R is NH, and R2is H.

Table 3737. Compounds of formula I.48 wherein R1is Y-4C, R is NH, and R2is H.

Table 3738. Compounds of formula I.48 wherein R1is Y-4D, R is NH, and R2is H.

Table 3739. Compounds of formula I.48 wherein R1is Y-5A, R is NH, and R2is H.

Table 3740. Compounds of formula I.48 wherein R1is Y-5B, R is NH, and R2is H.

Table 3741. Compounds of formula I.48 wherein R1is Y-6A, R is NH, and R2is H.

Table 3742. Compounds of formula I.48 wherein R1is Y-6B, R is NH, and R2is H.

Table 3743. Compounds of formula I.48 wherein R1is Y-8A, R is NH, and R2is H.

Table 3744. Compounds of formula I.48 wherein R1is Y-8B, R is NH, and R2is H.

Table 3745. Compounds of formula I.48 wherein R1is Y-1A, R is NH, and R2is CH3.

Table 3746. Compounds of formula I.48 wherein R1is Y-1B, R is NH, and R2is CH3.

Table 3747. Compounds of formula I.48 wherein R1is Y-2A, R is NH, and R2is CH3.

Table 3748. Compounds of formula I.48 wherein R1is Y-2B, R is NH, and R2is CH3.

Table 3749. Compounds of formula I.48 wherein R1is Y-3A, R is NH, and R2is CH3.

Table 3750. Compounds of formula I.48 wherein R1is Y-3B, R is NH, and R2is CH3.

Table 3751. Compounds of formula I.48 wherein R1is Y-3C, R is NH, and R2is CH3.

Table 3752. Compounds of formula I.48 wherein R1is Y-3D, R is NH, and R2is CH3.

Table 3753. Compounds of formula I.48 wherein R1is Y-4A, R is NH, and R2is CH3.

Table 3754. Compounds of formula I.48 wherein R1is Y-4B, R is NH, and R2is CH3.

Table 3755. Compounds of formula I.48 wherein R1is Y-4C, R is NH, and R2is CH3.

Table 3756. Compounds of formula I.48 wherein R1is Y-4D, R is NH, and R2is CH3.

Table 3757. Compounds of formula I.48 wherein R1is Y-5A, R is NH, and R2is CH3.

Table 3758. Compounds of formula I.48 wherein R1is Y-5B, R is NH, and R2is CH3.

Table 3759. Compounds of formula I.48 wherein R1is Y-6A, R is NH, and R2is CH3.

Table 3760. Compounds of formula I.48 wherein R1is Y-6B, R is NH, and R2is CH3.

Table 3761. Compounds of formula I.48 wherein R1is Y-8A, R is NH, and R2is CH3.

Table 3762. Compounds of formula I.48 wherein R1is Y-8B, R is NH, and R2is CH3.

Table 3763. Compounds of formula I.48 wherein R1is Y-1A, R is NH, and R2is c-C3H5.

Table 3764. Compounds of formula I.48 wherein R1is Y-1B, R is NH, and R2is c-C3H5.

Table 3765. Compounds of formula I.48 wherein R1is Y-2A, R is NH, and R2is c-C3H5.

Table 3766. Compounds of formula I.48 wherein R1is Y-2B, R is NH, and R2is c-C3H5.

Table 3767. Compounds of formula I.48 wherein R1is Y-3A, R is NH, and R2is c-C3H5.

Table 3768. Compounds of formula I.48 wherein R1is Y-3B, R is NH, and R2is c-C3H5.

Table 3769. Compounds of formula I.48 wherein R1is Y-3C, R is NH, and R2is c-C3H5.

Table 3770. Compounds of formula I.48 wherein R1is Y-3D, R is NH, and R2is c-C3H5.

Table 3771. Compounds of formula I.48 wherein R1is Y-4A, R is NH, and R2is c-C3H5.

Table 3772. Compounds of formula I.48 wherein R1is Y-4B, R is NH, and R2is c-C3H5.

Table 3773. Compounds of formula I.48 wherein R1is Y-4C, R is NH, and R2is c-C3H5.

Table 3774. Compounds of formula I.48 wherein R1is Y-4D, R is NH, and R2is c-C3H5.

Table 3775. Compounds of formula I.48 wherein R1is Y-5A, R is NH, and R2is c-C3H5.

Table 3776. Compounds of formula I.48 wherein R1is Y-5B, R is NH, and R2is c-C3H5.

Table 3777. Compounds of formula I.48 wherein R1is Y-6A, R is NH, and R2is c-C3H5.

Table 3778. Compounds of formula I.48 wherein R1is Y-6B, R is NH, and R2is c-C3H5.

Table 3779. Compounds of formula I.48 wherein R1is Y-8A, R is NH, and R2is c-C3H5.

Table 3780. Compounds of formula I.48 wherein R1is Y-8B, R is NH, and R2is c-C3H5.

Table 3835. Compounds of formula I.48 wherein R1is Y-1A, R is NCN, and R2is H.

Table 3836. Compounds of formula I.48 wherein R1is Y-1B, R is NCN, and R2is H.

Table 3837. Compounds of formula I.48 wherein R1is Y-2A, R is NCN, and R2is H.

Table 3838. Compounds of formula I.48 wherein R1is Y-2B, R is NCN, and R2is H.

Table 3839. Compounds of formula I.48 wherein R1is Y-3A, R is NCN, and R2is H.

Table 3840. Compounds of formula I.48 wherein R1is Y-3B, R is NCN, and R2is H.

Table 3841. Compounds of formula I.48 wherein R1is Y-3C, R is NCN, and R2is H.

Table 3842. Compounds of formula I.48 wherein R1is Y-3D, R is NCN, and R2is H.

Table 3843. Compounds of formula I.48 wherein R1is Y-4A, R is NCN, and R2is H.

Table 3844. Compounds of formula I.48 wherein R1is Y-4B, R is NCN, and R2is H.

Table 3845. Compounds of formula I.48 wherein R1is Y-4C, R is NCN, and R2is H.

Table 3846. Compounds of formula I.48 wherein R1is Y-4D, R is NCN, and R2is H.

Table 3847. Compounds of formula I.48 wherein R1is Y-5A, R is NCN, and R2is H.

Table 3848. Compounds of formula I.48 wherein R1is Y-5B, R is NCN, and R2is H.

Table 3849. Compounds of formula I.48 wherein R1is Y-6A, R is NCN, and R2is H.

Table 3850. Compounds of formula I.48 wherein R1is Y-6B, R is NCN, and R2is H.

Table 3851. Compounds of formula I.48 wherein R1is Y-8A, R is NCN, and R2is H.

Table 3852. Compounds of formula I.48 wherein R1is Y-8B, R is NCN, and R2is H.

Table 3853. Compounds of formula I.48 wherein R1is Y-1A, R is NCN, and R2is CH3.

Table 3854. Compounds of formula I.48 wherein R1is Y-1B, R is NCN, and R2is CH3.

Table 3855. Compounds of formula I.48 wherein R1is Y-2A, R is NCN, and R2is CH3.

Table 3856. Compounds of formula I.48 wherein R1is Y-2B, R is NCN, and R2is CH3.

Table 3857. Compounds of formula I.48 wherein R1is Y-3A, R is NCN, and R2is CH3.

Table 3858. Compounds of formula I.48 wherein R1is Y-3B, R is NCN, and R2is CH3.

Table 3859. Compounds of formula I.48 wherein R1is Y-3C, R is NCN, and R2is CH3.

Table 3860. Compounds of formula I.48 wherein R1is Y-3D, R is NCN, and R2is CH3.

Table 3861. Compounds of formula I.48 wherein R1is Y-4A, R is NCN, and R2is CH3.

Table 3862. Compounds of formula I.48 wherein R1is Y-4B, R is NCN, and R2is CH3.

Table 3863. Compounds of formula I.48 wherein R1is Y-4C, R is NCN, and R2is CH3.

Table 3864. Compounds of formula I.48 wherein R1is Y-4D, R is NCN, and R2is CH3.

Table 3865. Compounds of formula I.48 wherein R1is Y-5A, R is NCN, and R2is CH3.

Table 3866. Compounds of formula I.48 wherein R1is Y-5B, R is NCN, and R2is CH3.

Table 3867. Compounds of formula I.48 wherein R1is Y-6A, R is NCN, and R2is CH3.

Table 3868. Compounds of formula I.48 wherein R1is Y-6B, R is NCN, and R2is CH3.

Table 3869. Compounds of formula I.48 wherein R1is Y-8A, R is NCN, and R2is CH3.

Table 3870. Compounds of formula I.48 wherein R1is Y-8B, R is NCN, and R2is CH3.

Table 3871. Compounds of formula I.48 wherein R1is Y-1A, R is NCN, and R2is c-C3H5.

Table 3872. Compounds of formula I.48 wherein R1is Y-1B, R is NCN, and R2is c-C3H5.

Table 3873. Compounds of formula I.48 wherein R1is Y-2A, R is NCN, and R2is c-C3H5.

Table 3874. Compounds of formula I.48 wherein R1is Y-2B, R is NCN, and R2is c-C3H5.

Table 3875. Compounds of formula I.48 wherein R1is Y-3A, R is NON, and R2is c-C3H5.

Table 3876. Compounds of formula I.48 wherein R1is Y-3B, R is NON, and R2is c-C3H5.

Table 3877. Compounds of formula I.48 wherein R1is Y-3C, R is NON, and R2is c-C3H5.

Table 3878. Compounds of formula I.48 wherein R1is Y-31D, R is NON, and R2is c-C3H5.

Table 3879. Compounds of formula I.48 wherein R1is Y-4A, R is NON, and R2is c-C3H5.

Table 3880. Compounds of formula I.48 wherein R1is Y-4B, R is NON, and R2is c-C3H5.

Table 3881. Compounds of formula I.48 wherein R1is Y-4C, R is NON, and R2is c-C3H5.

Table 3882. Compounds of formula I.48 wherein R1is Y-41D, R is NON, and R2is c-C3H5.

Table 3883. Compounds of formula I.48 wherein R1is Y-5A, R is NON, and R2is c-C3H5.

Table 3884. Compounds of formula I.48 wherein R1is Y-5B, R is NON, and R2is c-C3H5.

Table 3885. Compounds of formula I.48 wherein R1is Y-6A, R is NON, and R2is c-C3H5.

Table 3886. Compounds of formula I.48 wherein R1is Y-6B, R is NON, and R2is c-C3H5.

Table 3887. Compounds of formula I.48 wherein R1is Y-8A, R is NON, and R2is c-C3H5.

Table 3888. Compounds of formula I.48 wherein R1is Y-8B, R is NON, and R2is c-C3H5.

As used herein, the term “compound(s) of the present invention” or “compound(s) according to the invention” refers to the compound(s) of formula (I) as defined above, which are also referred to as “compound(s) of formula I” or “compound(s) I” or “formula I compound(s)”, and includes their salts, tautomers, stereoisomers, and N-oxides.

Mixtures

The invention also relates to a mixture of at least one compound of the invention with at least one mixing partner. Preferred are binary mixtures of one compound of the invention as component I with one mixing partner herein as component II. Preferred weight ratios for such binary mixtures are from 5000:1 to 1:5000, preferably from 1000:1 to 1:1000, more preferably from 100:1 to 1:100, particularly from 10:1 to 1:10. In such binary mixtures, components I and II may be used in equal amounts, or an excess of component I, or an excess of component II may be used.

Mixing partners can be selected from pesticides, in particular insecticides, nematicides, and acaricides, fungicides, herbicides, plant growth regulators, fertilizers. Preferred mixing partners are insecticides, nematicides, and fungicides.

The following list M of pesticides, grouped according the Mode of Action Classification of the Insecticide Resistance Action Committee (IRAC), together with which the compounds of the invention can be used and with which potential synergistic effects might be produced, illustrates the possible combinations:

M.16 Inhibitors of the chitin biosynthesis type 1: buprofezin;

The commercially available compounds M listed above may be found in The Pesticide Manual, 18th Edition, C. MacBean, British Crop Protection Council (2018), or http://bcpcdata.com/pesticide-manual.html, http://www.alanwood.net/pesticides.

The following list of fungicides, in conjunction with which the compounds of the invention can be used, illustrates the possible combinations:

Suitable mixing partners for the compounds of the invention also include biopesticides.

Biopesticides have been defined as a form of pesticides based on micro-organisms (bacteria, fungi, viruses, nematodes, etc.) or natural products (compounds, e.g. metabolites, proteins, or extracts from biological or other natural sources) (U.S. Environmental Protection Agency: http://www.epa.gov/pesticides/biopesticides/). Biopesticides fall into two major classes, microbial and biochemical pesticides:

(1) Microbial pesticides consist of bacteria, fungi or viruses (and often include the metabolites that bacteria and fungi produce). Entomopathogenic nematodes are also classified as microbial pesticides, even though they are multi-cellular.

(2) Biochemical pesticides are naturally occurring substances or or structurally-similar and functionally identical to a naturally-occurring substance and extracts from biological sources that control pests or provide other crop protection uses as defined below, but have non-toxic mode of actions (e.g. growth or developmental regulation, attractants, repellents or defence activators (e.g. induced resistance) and are relatively non-toxic to mammals.

The following list of biopesticides, in conjunction with which the compounds of the invention can be used, illustrates the possible combinations:

The biopesticides from group L1) and/or L2) may also have insecticidal, acaricidal, molluscidal, pheromone, nematicidal, plant stress reducing, plant growth regulator, plant growth promoting and/or yield enhancing activity. The biopesticides from group L3) and/or L4) may also have fungicidal, bactericidal, viricidal, plant defense activator, plant stress reducing, plant growth regulator, plant growth promoting and/or yield enhancing activity. The biopesticides from group

According to the invention, the solid material (dry matter) of the biopesticides (with the exception of oils e.g. Neem oil) are considered as active components (e.g. to be obtained after drying or evaporation of the extraction or suspension medium in case of liquid formulations of the microbial pesticides).

In accordance with the invention, the weight ratios and percentages used herein for a biological extract e.g. Quillay extract are based on the total weight of the dry content (solid material) of the respective extract(s).

The total weight ratios of compositions comprising at least one microbial pesticide in the form of viable microbial cells including dormant forms, can be determined using the amount of CFU of the respective microorganism to calclulate the total weight of the respective active component with the following equation that 1×1010CFU equals one gram of total weight of the respective active component. Colony forming unit is measure of viable microbial cells, in particular fungal and bacterial cells. In addition, here “CFU” may also be understood as the number of (juvenile) individual nematodes in case of (entomopathogenic) nematode biopesticides, e.g.Steinernema feltiae.

When mixtures comprising microbial pesticides are employed in crop protection, the application rates range from 1×106to 5×1016(or more) CFU/ha, preferably from 1×108to 1×1013CFU/ha, and even more preferably from 1×109to 5×1015CFU/ha and in particular from 1×1012to 5×1014CFU/ha. In the case of nematodes as microbial pesticides (e.g.Steinernema feltiae), the application rates regularly range from 1×105to 1×1012(or more), preferably from 1×108to 1×1011, more preferably from 5×108to 1×1010individuals (e.g. in the form of eggs, juvenile or any other live stages, preferably in an infective juvenile stage) per ha.

When mixtures comprising microbial pesticides are employed in seed treatment, the application rates generally range from 1×101to 1×1012(or more) CFU/seed, preferably from 1×106to 1×109CFU/seed. Furthermore, the application rates with respect to seed treatment generally range from 1×107to 1×1014(or more) CFU per 100 kg of seed, preferably from 1×109to 1×1012CFU per 100 kg of seed.

The invention also relates to agrochemical compositions comprising an auxiliary and at least one compound of the invention or a mixture thereof.

An agrochemical composition comprises a pesticidally effective amount of a compound of the invention or a mixture thereof.

The compositions are prepared in a known manner, e.g. described by Mollet and Grube-mann, Formulation technology, Wiley VCH, Weinheim, 2001; or Knowles, New developments in crop protection product formulation, Agrow Reports DS243, T&F Informa, London, 2005.

Suitable anti-freezing agents are ethylene glycol, propylene glycol, urea and glycerin.

Suitable anti-foaming agents are silicones, long chain alcohols, and salts of fatty acids.

Suitable colorants (e.g. in red, blue, or green) are pigments of low water solubility and water-soluble dyes. Examples are inorganic colorants (e.g. iron oxide, titan oxide, iron hexacyanofer-rate) and organic colorants (e.g. alizarin-, azo-, and phthalocyanine colorants).

Examples for composition types and their preparation are:

10-60 wt % of a compound I according to the invention and 5-15 wt % wetting agent (e.g. alcohol alkoxylates) are dissolved in water and/or in a water-soluble solvent (e.g. alcohols) up to 100 wt %.

The active substance dissolves upon dilution with water.

5-25 wt % of a compound I according to the invention and 1-10 wt % dispersant (e.g. polyvinylpyrrolidone) are dissolved in up to 100 wt % organic solvent (e.g. cyclohexanone). Dilution with water gives a dispersion.

15-70 wt % of a compound I according to the invention and 5-10 wt % emulsifiers (e.g. calcium dodecylbenzenesulfonate and castor oil ethoxylate) are dissolved in up to 100 wt % water-insoluble organic solvent (e.g. aromatic hydrocarbon). Dilution with water gives an emulsion. iv) Emulsions (EW, EO, ES)

5-40 wt % of a compound I according to the invention and 1-10 wt % emulsifiers (e.g. calcium dodecylbenzenesulfonate and castor oil ethoxylate) are dissolved in 20-40 wt % water-insoluble organic solvent (e.g. aromatic hydrocarbon). This mixture is introduced into up to 100 wt % water by means of an emulsifying machine and made into a homogeneous emulsion. Dilution with water gives an emulsion.

In an agitated ball mill, 20-60 wt % of a compound I according to the invention are comminuted with addition of 2-10 wt % dispersants and wetting agents (e.g. sodium lignosulfonate and alcohol ethoxylate), 0,1-2 wt % thickener (e.g. xanthan gum) and up to 100 wt % water to give a fine active substance suspension. Dilution with water gives a stable suspension of the active sub-stance. For FS type composition up to 40 wt % binder (e.g. polyvinylalcohol) is added.

50-80 wt % of a compound I according to the invention are ground finely with addition of up to 100 wt % dispersants and wetting agents (e.g. sodium lignosulfonate and alcohol ethoxylate) and prepared as water-dispersible or water-soluble granules by means of technical appliances (e.g. extrusion, spray tower, fluidized bed). Dilution with water gives a stable dispersion or solution of the active substance.

50-80 wt % of a compound I according to the invention are ground in a rotor-stator mill with addition of 1-5 wt % dispersants (e.g. sodium lignosulfonate), 1-3 wt % wetting agents (e.g. alcohol ethoxylate) and up to 100 wt % solid carrier, e.g. silica gel. Dilution with water gives a stable dispersion or solution of the active substance.

In an agitated ball mill, 5-25 wt % of a compound I according to the invention are comminuted with addition of 3-10 wt % dispersants (e.g. sodium lignosulfonate), 1-5 wt % thickener (e.g. carboxymethylcellulose) and up to 100 wt % water to give a fine suspension of the active sub-stance. Dilution with water gives a stable suspension of the active substance.

5-20 wt % of a compound I according to the invention are added to 5-30 wt % organic solvent blend (e.g. fatty acid dimethylamide and cyclohexanone), 10-25 wt % surfactant blend (e.g. alkohol ethoxylate and arylphenol ethoxylate), and water up to 100%. This mixture is stirred for 1 h to produce spontaneously a thermodynamically stable microemulsion.

An oil phase comprising 5-50 wt % of a compound I according to the invention, 0-40 wt % water insoluble organic solvent (e.g. aromatic hydrocarbon), 2-15 wt % acrylic monomers (e.g. methylmethacrylate, methacrylic acid and a di- or triacrylate) are dispersed into an aqueous solution of a protective colloid (e.g. polyvinyl alcohol). Radical polymerization initiated by a radical initiator results in the formation of poly(meth)acrylate microcapsules. Alternatively, an oil phase comprising 5-50 wt % of a compound I according to the invention, 0-40 wt % water insoluble organic solvent (e.g. aromatic hydrocarbon), and an isocyanate monomer (e.g. diphenylmethene-4,4′-diisocyanatae) are dispersed into an aqueous solution of a protective colloid (e.g. polyvinyl alcohol). The addition of a polyamine (e.g. hexamethylenediamine) results in the formation of a polyurea microcapsule. The monomers amount to 1-10 wt %. The wt % relate to the total CS composition.

1-10 wt % of a compound I according to the invention are ground finely and mixed intimately with up to 100 wt % solid carrier, e.g. finely divided kaolin.

0.5-30 wt % of a compound I according to the invention is ground finely and associated with up to 100 wt % solid carrier (e.g. silicate). Granulation is achieved by extrusion, spray-drying or the fluidized bed.

1-50 wt % of a compound I according to the invention are dissolved in up to 100 wt % organic solvent, e.g. aromatic hydrocarbon.

The agrochemical compositions generally comprise between 0.01 and 95%, preferably between 0.1 and 90%, and most preferably between 0.5 and 75%, by weight of active substance.

The active substances are employed in a purity of from 90% to 100%, preferably from 95% to 100% (according to NMR spectrum).

Various types of oils, wetters, adjuvants, fertilizer, or micronutrients, and other pesticides (e.g. herbicides, insecticides, fungicides, growth regulators, safeners) may be added to the active substances or the compositions comprising them as premix or, if appropriate not until immediately prior to use (tank mix). These agents can be admixed with the compositions according to the invention in a weight ratio of 1:100 to 100:1, preferably 1:10 to 10:1.

The user applies the composition according to the invention usually from a predosage device, a knapsack sprayer, a spray tank, a spray plane, or an irrigation system. Usually, the agrochemical composition is made up with water, buffer, and/or further auxiliaries to the desired application concentration and the ready-to-use spray liquor or the agrochemical composition according to the invention is thus obtained. Usually, 20 to 2000 liters, preferably 50 to 400 liters, of the ready-to-use spray liquor are applied per hectare of agricultural useful area.

According to one embodiment, individual components of the composition of the invention e.g. parts of a kit or parts of a binary or ternary mixture may be mixed by the user himself in a spray tank and further auxiliaries may be added, if appropriate.

In a further embodiment, either individual components of the composition according to the invention or partially premixed components, e.g. components comprising compounds of the invention and/or mixing partners as defined above, may be mixed by the user in a spray tank and further auxiliaries and additives may be added.

In a further embodiment, either individual components of the composition according to the invention or partially premixed components, e.g. components comprising compounds of the invention and/or mixing partners as defined above, can be applied jointly (e.g. after tank mix) or consecutively.

The compounds of the invention are suitable for use in protecting crops, plants, plant propagation materials, e.g. seeds, or soil or water, in which the plants are growing, from attack or infestation by animal pests. Therefore, the invention also relates to a plant protection method, which comprises contacting crops, plants, plant propagation materials, e.g. seeds, or soil or water, in which the plants are growing, to be protected from attack or infestation by animal pests, with a pesticidally effective amount of a compound of the invention.

The compounds of the invention are also suitable for use in combating or controlling animal pests. Therefore, the invention also relates to a method of combating or controlling animal pests, which comprises contacting the animal pests, their habitat, breeding ground, or food supply, or the crops, plants, plant propagation materials, e.g. seeds, or soil, or the area, material or environment in which the animal pests are growing or may grow, with a pesticidally effective amount of a compound of the invention.

The compounds of the invention are effective through both contact and ingestion. Furthermore, the compounds of the invention can be applied to any and all developmental stages, e.g. egg, larva, pupa, and adult.

The compounds of the invention can be applied as such or in form of compositions comprising them as defined above. Furthermore, the compounds of the invention can be applied together with a mixing partner or in form of compositions comprising said mixtures. The components of said mixture can be applied simultaneously, jointly or separately, or in succession, that is immediately one after another and thereby creating the mixture “in situ” on the desired location, e.g. the plant, the sequence, in the case of separate application, generally not having any effect on the result of the control measures.

The application can be carried out both before and after the infestation of the crops, plants, plant propagation materials, e.g. seeds, soil, or the area, material or environment by the pests.

Suitable application methods include i.a. soil treatment, seed treatment, in furrow application, and foliar application. Soil treatment methods include drenching the soil, drip irrigation (drip application onto the soil), dipping roots, tubers or bulbs, or soil injection. Seed treatment techniques include seed dressing, seed coating, seed dusting, seed soaking, and seed pelleting. In furrow applications typically include the steps of making a furrow in cultivated land, seeding the furrow with seeds, applying the pesticidally active compound to the furrow, and closing the furrow. Foliar application refers to the application of the pesticidally active compound to plant foliage, e.g. through spray equipment. For foliar applications, it can be advantageous to modify the behavior of the pests by use of pheromones in combination with the compounds of the invention. Suitable pheromones for specific crops and pests are known and publicly available from databases of pheromones and semiochemicals, e.g. http://www.pherobase.com.

As used herein, the term “contacting” includes both direct contact (applying the compounds/compositions directly on the animal pest or plant—typically to the foliage, stem or roots of the plant) and indirect contact (applying the compounds/compositions to the locus, i.e. habitat, breeding ground, plant, seed, soil, area, material, or environment in which a pest is growing or may grow, of the animal pest or plant).

The term “animal pest” includes arthropods, gastropods, and nematodes. Preferred animal pests according to the invention are arthropods, preferably insects and arachnids, in particular insects. Insects, which are of particular relevance for crops, are typically referred to as crop insect pests.

The term “crop” refers to both, growing and harvested crops.

The term “cultivated plants” is to be understood as including plants which have been modified by mutagenesis or genetic engineering in order to provide a new trait to a plant or to modify an already present trait.

Mutagenesis includes techniques of random mutagenesis using X-rays or mutagenic chemicals, but also techniques of targeted mutagenesis, in order to create mutations at a specific locus of a plant genome. Targeted mutagenesis techniques frequently use oligonucleotides or proteins like CRISPR/Cas, zinc-finger nucleases, TALENs or meganucleases to achieve the targeting effect.

Genetic engineering usually uses recombinant DNA techniques to create modifications in a plant genome which under natural circumstances cannot readily be obtained by cross breeding, mutagenesis or natural recombination. Typically, one or more genes are integrated into the genome of a plant in order to add a trait or improve a trait. These integrated genes are also referred to as transgenes in the art, while plant comprising such transgenes are referred to as transgenic plants. The process of plant transformation usually produces several transformation events, which differ in the genomic locus in which a transgene has been integrated. Plants comprising a specific transgene on a specific genomic locus are usually described as comprising a specific “event”, which is referred to by a specific event name. Traits which have been introduced in plants or have been modified include in particular herbicide tolerance, insect resistance, increased yield and tolerance to abiotic conditions, like drought.

Herbicide tolerance has been created by using mutagenesis as well as using genetic engineering. Plants which have been rendered tolerant to ALS inhibitor herbicides by conventional methods of mutagenesis and breeding comprise plant varieties commercially available under the name Clearfield®.

Transgenes wich have been used to provide herbicide tolerance traits comprise: for tolerance to glyphosate: cp4 epsps, epsps grg23ace5, mepsps, 2mepsps, gat4601, gat4621 and goxv247, for tolerance to glufosinate: pat and bar, for tolerance to 2,4-D: aad-1 and aad-12, for tolerance to dicamba: dmo, for tolerance to oxynil herbicies: bxn, for tolerance to sulfonylurea herbicides: zm-hra, csr1-2, gm-hra, S4-HrA, for tolerance to ALS inhibitor herbicides: csr1-2, for tolerance to HPPD inhibitor herbicides: hppdPF, W336 and avhppd-03.

Insect resistance has mainly been created by transferring bacterial genes for insecticidal proteins to plants. Transgenes which have most frequently been used are toxin genes ofBacillusspec. and synthetic variants thereof, like cry1A, cry1Ab, cry1Ab-Ac, cry1Ac, cry1A.105, cry1F, cry1Fa2, cry2Ab2, cry2Ae, mcry3A, ecry3.1Ab, cry3Bb1, cry34Ab1, cry35Ab1, cry9C, vip3A(a), vip3Aa20. However, also genes of plant origin have been transferred to other plants. In particular genes coding for protease inhibitors, like CpTI and pinII. A further approach uses transgenes in order to produce double stranded RNA in plants to target and downregulate insect genes. An example for such a transgene is dvsnf7.

Transgenic soybean events comprising genes for insecticidal proteins are e.g., but not excluding others, MON87701, MON87751 and DAS-81419.

Increased yield has been created by increasing ear biomass using the transgene athb17, being present in corn event MON87403, or by enhancing photosynthesis using the transgene bbx32, being present in the soybean event MON87712.

Cultivated plants comprising a modified oil content have been created by using the transgenes: gm-fad2-1, Pj.D6D, Nc.Fad3, fad2-1A and fatb1-A. Soybean events comprising at least one of these genes are: 260-05, MON87705 and MON87769.

Tolerance to abiotic conditions, in particular to tolerance to drought, has been created by using the transgene cspB, comprised by the corn event MON87460 and by using the transgene Hahb-4, comprised by soybean event IND-00410-5.

Traits are frequently combined by combining genes in a transformation event or by combining different events during the breeding process. Preferred combination of traits are herbicide tolerance to different groups of herbicides, insect tolerance to different kind of insects, in particular tolerance to lepidopteran and coleopteran insects, herbicide tolerance with one or several types of insect resistance, herbicide tolerance with increased yield as well as a combination of herbicide tolerance and tolerance to abiotic conditions.

Plants comprising singular or stacked traits as well as the genes and events providing these traits are known (http://www.isaaa.org/gmapprovaldatabase) and (http://cera-amc.ora/GMCropDatabase).

The use of compositions according to the invention on cultivated plants may result in effects which are specific to a cultivated plant comprising a certain gene or event. These effects may comprise enhanced yield, enhanced resistance or tolerance to insects, nematodes, fungal, bacterial,mycoplasma, viral or viroid pathogens as well as early vigour, early or delayed ripening, cold or heat tolerance as well as changed amino acid or fatty acid spectrum or content.

It has been found that the pesticidal activity of the compounds of the invention may be enhanced by the insecticidal trait of a modified plant. Furthermore, it has been found that the compounds of the invention are suitable for preventing insects to become resistant to the insecticidal trait or for combating pests, which already have become resistant to the insecticidal trait of a modified plant. Moreover, the compounds of the invention are suitable for combating pests, against which the insecticidal trait is not effective, so that a complementary insecticidal activity can advantageously be used.

The term “plant propagation material” refers to all the generative parts of the plant e.g. seeds and vegetative plant material e.g. cuttings and tubers (e.g. potatoes), which can be used for the multiplication of the plant. This includes seeds, roots, fruits, tubers, bulbs, rhizomes, shoots, sprouts and other parts of plants. Seedlings and young plants, which are to be transplanted after germination or after emergence from soil, may also be included. These plant propagation materials may be treated prophylactically with a plant protection compound either at or before planting or transplanting.

The term “seed” embraces seeds and plant propagules of all kinds including but not limited to true seeds, seed pieces, suckers, corms, bulbs, fruit, tubers, grains, cuttings, cut shoots and the like, and means in a preferred embodiment true seeds.

In general, “pesticidally effective amount” means the amount of active ingredient needed to achieve an observable effect on growth, including the effects of necrosis, death, retardation, prevention, and removal, destruction, or otherwise diminishing the occurrence and activity of the target organism. The pesticidally effective amount can vary for the various compounds/compositions used in the invention. A pesticidally effective amount of the compositions will also vary according to the prevailing conditions e.g. desired pesticidal effect and duration, weather, target species, locus, mode of application.

In the case of soil treatment, in furrow application or of application to the pests dwelling place or nest, the quantity of active ingredient ranges from 0.0001 to 500 g per 100 m2, preferably from 0.001 to 20 g per 100 m2.

For use in treating crop plants, e.g. by foliar application, the rate of application of the active ingredients of this invention may be in the range of 0.0001 g to 4000 g per hectare, e.g. from 1 g to 2 kg per hectare or from 1 g to 750 g per hectare, desirably from 1 g to 100 g per hectare, more desirably from 10 g to 50 g per hectare, e.g., 10 to 20 g per hectare, 20 to 30 g per hectare, 30 to 40 g per hectare, or 40 to 50 g per hectare.

The compounds of the invention are particularly suitable for use in the treatment of seeds in order to protect the seeds from insect pests, in particular from soil-living insect pests, and the resulting seedling's roots and shoots against soil pests and foliar insects. The invention therefore also relates to a method for the protection of seeds from insects, in particular from soil insects, and of the seedling's roots and shoots from insects, in particular from soil and foliar insects, said method comprising treating the seeds before sowing and/or after pregermination with a compound of the invention. The protection of the seedling's roots and shoots is preferred. More preferred is the protection of seedling's shoots from piercing and sucking insects, chewing insects and nematodes.

The term “seed treatment” comprises e.g. seed dressing, seed coating, seed dusting, seed soaking, seed pelleting, and in-furrow application methods. Preferably, the seed treatment application of the active compound is carried out by spraying or by dusting the seeds before sowing of the plants and before emergence of the plants.

The invention also comprises seeds coated with or containing the active compound. The term “coated with and/or containing” generally signifies that the active ingredient is for the most part on the surface of the propagation product at the time of application, although a greater or lesser part of the ingredient may penetrate into the propagation product, depending on the method of application. When the said propagation product is (re)planted, it may absorb the active ingredient.

In addition, the active compound may also be used for the treatment of seeds from plants, which have been modified by mutagenisis or genetic engineering, and which e.g. tolerate the action of herbicides or fungicides or insecticides.

Conventional seed treatment formulations include e.g. flowable concentrates FS, solutions LS, suspoemulsions (SE), powders for dry treatment DS, water dispersible powders for slurry treatment WS, water-soluble powders SS and emulsion ES and EC and gel formulation GF. These formulations can be applied to the seed diluted or undiluted. Application to the seeds is carried out before sowing, either directly on the seeds or after having pregerminated the latter. Preferably, the formulations are applied such that germination is not included.

The active substance concentrations in ready-to-use formulations, which may be obtained after two-to-tenfold dilution, are preferably from 0.01 to 60% by weight, more preferably from 0.1 to 40% by weight.

In a preferred embodiment a FS formulation is used for seed treatment. Typically, a FS formulation may comprise 1-800 g/l of active ingredient, 1-200 g/l Surfactant, 0 to 200 g/l antifreezing agent, 0 to 400 g/l of binder, 0 to 200 g/l of a pigment and up to 1 liter of a solvent, preferably water.

Especially preferred FS formulations of the compounds of the invention for seed treatment usually comprise from 0.1 to 80% by weight (1 to 800 g/l) of the active ingredient, from 0.1 to 20% by weight (1 to 200 g/l) of at least one surfactant, e.g. 0.05 to 5% by weight of a wetter and from 0.5 to 15% by weight of a dispersing agent, up to 20% by weight, e.g. from 5 to 20% of an anti-freeze agent, from 0 to 15% by weight, e.g. 1 to 15% by weight of a pigment and/or a dye, from 0 to 40% by weight, e.g. 1 to 40% by weight of a binder (sticker/adhesion agent), optionally up to 5% by weight, e.g. from 0.1 to 5% by weight of a thickener, optionally from 0.1 to 2% of an anti-foam agent, and optionally a preservative e.g. a biocide, antioxidant or the like, e.g. in an amount from 0.01 to 1% by weight and a filler/vehicle up to 100% by weight.

In the treatment of seed, the application rates of the compounds of the invention are generally from 0.1 g to 10 kg per 100 kg of seed, preferably from 1 g to 5 kg per 100 kg of seed, more preferably from 1 g to 1000 g per 100 kg of seed and in particular from 1 g to 200 g per 100 kg of seed, e.g. from 1 g to 100 g or from 5 g to 100 g per 100 kg of seed.

The invention therefore also relates to seed comprising a compound of the invention, or an agriculturally useful salt thereof, as defined herein. The amount of the compound of the invention or the agriculturally useful salt thereof will in general vary from 0.1 g to 10 kg per 100 kg of seed, preferably from 1 g to 5 kg per 100 kg of seed, in particular from 1 g to 1000 g per 100 kg of seed. For specific crops e.g. lettuce the rate can be higher.

The compounds of the invention may also be used for improving the health of a plant. Therefore, the invention also relates to a method for improving plant health by treating a plant, plant propagation material and/or the locus where the plant is growing or is to grow with an effective and non-phytotoxic amount of a compound of the invention.

As used herein “an effective and non-phytotoxic amount” means that the compound is used in a quantity which allows to obtain the desired effect but which does not give rise to any phytotoxic symptom on the treated plant or on the plant grown from the treated propagule or treated soil.

“Plant health” is defined as a condition of the plant and/or its products which is determined by several aspects alone or in combination with each other e.g. yield (e.g. increased biomass and/or increased content of valuable ingredients), quality (e.g. improved content or composition of certain ingredients or shelf life), plant vigour (e.g. improved plant growth and/or greener leaves (“greening effect”), tolerance to abiotic (e.g. drought) and/or biotic stress (e.g. disease) and production efficiency (e.g., harvesting efficiency, processability).

The above identified indicators for the health condition of a plant may be interdependent and may result from each other. Each indicator is defined in the art and can be determined by methods known to a skilled person.

The compounds of the invention are also suitable for use against non-crop insect pests. For use against said non-crop pests, compounds of the invention can be used as bait composition, gel, general insect spray, aerosol, as ultra-low volume application and bed net (impregnated or surface applied). Furthermore, drenching and rodding methods can be used.

The bait can be a liquid, a solid or a semisolid preparation (e.g. a gel). The bait employed in the composition is a product, which is sufficiently attractive to incite insects e.g. ants, termites, wasps, flies, mosquitoes, crickets etc. or cockroaches to eat it. The attractiveness can be manipulated by using feeding stimulants or sex pheromones. Food stimulants are preferably chosen from animal and/or plant proteins (meat-, fish- or blood meal, insect parts, egg yolk), from fats and oils of animal and/or plant origin, or mono-, oligo- or polyorganosaccharides, especially from sucrose, lactose, fructose, dextrose, glucose, starch, pectin or even molasses or honey. Fresh or decaying parts of fruits, crops, plants, animals, insects or specific parts thereof can also serve as a feeding stimulant. Sex pheromones are known to be more insect specific. Specific pheromones are known (http://www.pherobase.com).

For use in bait compositions, the typical content of active ingredient is from 0.001 wt % to 15 wt %, desirably from 0.001 wt % to 5 wt % of active compound.

Formulations of the compounds of the invention as aerosols (e.g in spray cans), oil sprays or pump sprays are highly suitable for professional or non-professional users for controlling pests e.g. flies, fleas, ticks, bed bugs, mosquitoes or cockroaches. Aerosol recipes are preferably composed of the active compound, solvents, furthermore auxiliaries e.g. emulsifiers, perfume oils, if appropriate stabilizers, and, if required, propellants.

The oil spray formulations differ from the aerosol recipes in that no propellants are used.

For use in spray compositions, the content of active ingredient is from 0.001 to 80 wt %, preferably from 0.01 to 50 wt % and most preferably from 0.01 to 15 wt %.

The compounds of the invention and its respective compositions can also be used in mosquito and fumigating coils, smoke cartridges, vaporizer plates or long-term vaporizers and also in moth papers, moth pads or other heat-independent vaporizer systems.

Methods to control infectious diseases transmitted by insects (e.g. malaria, dengue and yellow fever, lymphatic filariasis, and leishmaniasis) with compounds of the invention and its respective compositions also comprise treating surfaces of huts and houses, air spraying and impregnation of curtains, tents, clothing items, bed nets, tsetse-fly trap. Insecticidal compositions for application to fibers, fabric, knitgoods, nonwovens, netting material or foils and tarpaulins preferably comprise a mixture including the insecticide, optionally a repellent and at least one binder.

The compounds of the invention and its compositions can be used for protecting wooden materials e.g. trees, board fences, sleepers, frames, artistic artifacts, etc. and buildings, but also construction materials, furniture, leathers, fibers, vinyl articles, electric wires and cables etc. from ants, termites and/or wood or textile destroying beetles, and for controlling ants and termites from doing harm to crops or human beings (e.g. when the pests invade into houses and public facilities or nest in yards, orchards or parks).

Customary application rates in the protection of materials are, e.g., from 0.001 g to 2000 g or from 0.01 g to 1000 g of active compound per m2treated material, desirably from 0.1 g to 50 g per m2.

Insecticidal compositions for use in the impregnation of materials typically contain from 0.001 to 95 wt %, preferably from 0.1 to 45 wt %, and more preferably from 1 to 25 wt % of at least one repellent and/or insecticide.

The compounds of the invention are especially suitable for efficiently combating animal pests e.g. arthropods, gastropods and nematodes including:

Pests from the class Symphyla e.g.Scutigerella immaculata,

Insects from the order Dermaptera, e.g.Forficula auricularia,

Insects from the order Collembola, e.g.Onychiurusspp., e.g.Onychiurus armatus,

The compounds of the invention are particularly suitable for efficiently combating

The compounds of the invention are suitable for use in treating or protecting animals against infestation or infection by parasites. Therefore, the invention also relates to the use of a compound of the invention for the manufacture of a medicament for the treatment or protection of animals against infestation or infection by parasites. Furthermore, the invention relates to a method of treating or protecting animals against infestation and infection by parasites, which comprises orally, topically or parenterally administering or applying to the animals a parasiticidally effective amount of a compound of the invention.

The invention also relates to the non-therapeutic use of compounds of the invention for treating or protecting animals against infestation and infection by parasites. Moreover, the invention relates to a non-therapeutic method of treating or protecting animals against infestation and infection by parasites, which comprises applying to a locus a parasiticidally effective amount of a compound of the invention.

The compounds of the invention are further suitable for use in combating or controlling parasites in and on animals. Furthermore, the invention relates to a method of combating or controlling parasites in and on animals, which comprises contacting the parasites with a parasitically effective amount of a compound of the invention.

The invention also relates to the non-therapeutic use of compounds of the invention for controlling or combating parasites. Moreover, the invention relates to a non-therapeutic method of combating or controlling parasites, which comprises applying to a locus a parasiticidally effective amount of a compound of the invention.

The compounds of the invention can be effective through both contact (via soil, glass, wall, bed net, carpet, blankets or animal parts) and ingestion (e.g. baits). Furthermore, the compounds of the invention can be applied to any and all developmental stages.

The compounds of the invention can be applied as such or in form of compositions comprising the compounds of the invention.

The compounds of the invention can also be applied together with a mixing partner, which acts against pathogenic parasites, e.g. with synthetic coccidiosis compounds, polyetherantibiotics e.g. Amprolium, Robenidin, Toltrazuril, Monensin, Salinomycin, Maduramicin, Lasalocid, Narasin or Semduramicin, or with other mixing partners as defined above, or in form of compositions comprising said mixtures.

The compounds of the invention and compositions comprising them can be applied orally, parenterally or topically, e.g. dermally. The compounds of the invention can be systemically or non-systemically effective.

The application can be carried out prophylactically, therapeutically or non-therapeutically. Furthermore, the application can be carried out preventively to places at which occurrence of the parasites is expected.

As used herein, the term “contacting” includes both direct contact (applying the compounds/compositions directly on the parasite, including the application directly on the animal or excluding the application directly on the animal, e.g. at it's locus for the latter) and indirect contact (applying the compounds/compositions to the locus of the parasite). The contact of the parasite through application to its locus is an example of a non-therapeutic use of the compounds of the invention.

The term “locus” means the habitat, food supply, breeding ground, area, material or environment in which a parasite is growing or may grow outside of the animal.

As used herein, the term “parasites” includes endo- and ectoparasites. In some embodiments of the invention, endoparasites can be preferred. In other embodiments, ectoparasites can be preferred. Infestations in warm-blooded animals and fish include lice, biting lice, ticks, nasal bots, keds, biting flies, muscoid flies, flies, myiasitic fly larvae, chiggers, gnats, mosquitoes and fleas.

The compounds of the invention are especially useful for combating parasites of the following orders and species, respectively:

Generally, “parasiticidally effective amount” means the amount of active ingredient needed to achieve an observable effect on growth, including the effects of necrosis, death, retardation, prevention, and removal, destruction, or otherwise diminishing the occurrence and activity of the target organism. The parasiticidally effective amount can vary for the various compounds/com-positions used in the invention. A parasiticidally effective amount of the compositions will also vary according to the prevailing conditions e.g. desired parasiticidal effect and duration, target species, mode of application.

Generally, it is favorable to apply the compounds of the invention in total amounts of 0.5 mg/kg to 100 mg/kg per day, preferably 1 mg/kg to 50 mg/kg per day.

For oral administration to warm-blooded animals, the compounds I may be formulated as animal feeds, animal feed premixes, animal feed concentrates, pills, solutions, pastes, suspensions, drenches, gels, tablets, boluses and capsules. In addition, the compounds I may be administered to the animals in their drinking water. For oral administration, the dosage form chosen should provide the animal with 0.01 mg/kg to 100 mg/kg of animal body weight per day of the compounds I, preferably with 0.5 mg/kg to 100 mg/kg of animal body weight per day.

Alternatively, the compounds I may be administered to animals parenterally, e.g., by intraruminal, intramuscular, intravenous or subcutaneous injection. The compounds I may be dispersed or dissolved in a physiologically acceptable carrier for subcutaneous injection. Alternatively, the compounds I may be formulated into an implant for subcutaneous administration. In addition the compounds I may be transdermally administered to animals. For parenteral administration, the dosage form chosen should provide the animal with 0.01 mg/kg to 100 mg/kg of animal body weight per day of the compounds I.

The compounds I may also be applied topically to the animals in the form of dips, dusts, powders, collars, medallions, sprays, shampoos, spot-on and pour-on formulations and in ointments or oil-in-water or water-in-oil emulsions. For topical application, dips and sprays usually contain 0.5 ppm to 5,000 ppm and preferably 1 ppm to 3,000 ppm of the compounds I. In addition, the compounds I may be formulated as ear tags for animals, particularly quadrupeds e.g. cattle and sheep.

Suitable preparations are:Solutions e.g. oral solutions, concentrates for oral administration after dilution, solutions for use on the skin or in body cavities, pouring-on formulations, gels;Emulsions and suspensions for oral or dermal administration; semi-solid preparations;Formulations in which the active compound is processed in an ointment base or in an oil-in-water or water-in-oil emulsion base;Solid preparations e.g. powders, premixes or concentrates, granules, pellets, tablets, boluses, capsules; aerosols and inhalants, and active compound-containing shaped articles.

Compositions suitable for injection are prepared by dissolving the active ingredient in a suitable solvent and optionally adding further auxiliaries e.g. acids, bases, buffer salts, preservatives, and solubilizers. Suitable auxiliaries for injection solutions are known in the art. The solutions are filtered and filled sterile.

Oral solutions are administered directly. Concentrates are administered orally after prior dilution to the use concentration. Oral solutions and concentrates are prepared according to the state of the art and as described above for injection solutions, sterile procedures not being necessary.

Solutions for use on the skin are trickled on, spread on, rubbed in, sprinkled on or sprayed on. Solutions for use on the skin are prepared according to the state of the art and according to what is described above for injection solutions, sterile procedures not being necessary.

Gels are applied to or spread on the skin or introduced into body cavities. Gels are prepared by treating solutions which have been prepared as described in the case of the injection solutions with sufficient thickener that a clear material having an ointment-like consistency results. Suitable thickeners are known in the art.

Pour-on formulations are poured or sprayed onto limited areas of the skin, the active compound penetrating the skin and acting systemically. Pour-on formulations are prepared by dissolving, suspending or emulsifying the active compound in suitable skin-compatible solvents or solvent mixtures. If appropriate, other auxiliaries e.g. colorants, bioabsorption-promoting substances, antioxidants, light stabilizers, adhesives are added. Suitable such auxiliaries are known in the art.

Emulsions can be administered orally, dermally or as injections. Emulsions are either of the water-in-oil type or of the oil-in-water type. They are prepared by dissolving the active compound either in the hydrophobic or in the hydrophilic phase and homogenizing this with the solvent of the other phase with the aid of suitable emulsifiers and, if appropriate, other auxiliaries e.g. colorants, absorption-promoting substances, preservatives, antioxidants, light stabilizers, viscosity-enhancing substances. Suitable hydrophobic phases (oils), suitable hydrophilic phases, suitable emulsifiers, and suitable further auxiliaries for emulsions are known in the art.

Suspensions can be administered orally or topically/dermally. They are prepared by suspending the active compound in a suspending agent, if appropriate with addition of other auxiliaries e.g. wetting agents, colorants, bioabsorption-promoting substances, preservatives, antioxidants, light stabilizers. Suitable suspending agents, and suitable other auxiliaries for suspensions including wetting agents are known in the art.

Semi-solid preparations can be administered orally or topically/dermally. They differ from the suspensions and emulsions described above only by their higher viscosity.

For the production of solid preparations, the active compound is mixed with suitable excipients, if appropriate with addition of auxiliaries, and brought into the desired form. Suitable auxiliaries for this purpose are known in the art.

The compositions which can be used in the invention can comprise generally from about 0.001 to 95% of the compound of the invention.

Ready-to-use preparations contain the compounds acting against parasites, preferably ectoparasites, in concentrations of 10 ppm to 80% by weight, preferably from 0.1 to 65% by weight, more preferably from 1 to 50% by weight, most preferably from 5 to 40% by weight.

Preparations which are diluted before use contain the compounds acting against ectoparasites in concentrations of 0.5 to 90% by weight, preferably of 1 to 50% by weight.

Furthermore, the preparations comprise the compounds of formula I against endoparasites in concentrations of 10 ppm to 2% by weight, preferably of 0.05 to 0.9% by weight, very particularly preferably of 0.005 to 0.25% by weight.

Topical application may be conducted with compound-containing shaped articles e.g. collars, medallions, ear tags, bands for fixing at body parts, and adhesive strips and foils.

Generally it is favorable to apply solid formulations which release compounds of the invention in total amounts of 10 mg/kg to 300 mg/kg, preferably 20 mg/kg to 200 mg/kg, most preferably 25 mg/kg to 160 mg/kg body weight of the treated animal in the course of three weeks.

EXAMPLES

Synthesis Examples

With appropriate modification of the starting materials, the procedures as described in the preparation examples below were used to obtain further compounds of formula I. The compounds obtained in this manner are listed in the table C that follows, together with physical data.

Compounds can be characterized e.g. by coupled High Performance Liquid Chromatography/mass spectrometry (HPLC/MS), by1H-NMR and/or by their melting points.

1H-NMR: The signals are characterized by chemical shift (ppm, 6 [delta]) vs. tetramethylsilane respectively, CDCl3for13C-NMR, by their multiplicity and by their integral (relative number of hydrogen atoms given). The following abbreviations are used to characterize the multiplicity of the signals: m=multiplet, q=quartet, t=triplet, d=doublet and s=singlet.

Abbreviations used are: d for day(s), h for hour(s), min for minute(s), r.t./room temperature for 20-25° C., Rt for retention time; DMSO for dimethyl sulfoxide, OAc for acetate, EtOAc for ethyl acetate.

A solution of 2-chloropyrimidin-4-amine (1.500 g), (4-formylphenyl)boronic acid (2.328 g), cesium fluoride (1.935 g), palladium acetate (0.130 g), triphenylphosphine-3,3′,3″-trisulfonic acid trisodium salt (0.645 g) in acetonitrile/water (1:3, 22 mL) was set under argon atmosphere. The reaction mixture was stirred for 16 h at 100° C. The reaction mixture was cooled down and water was added. The resulting precipitate was filtered and subjected to silica gel flash column chromatography, eluting with a gradient of EtOAc and cyclohexane to obtain the title compound as a solid (2.00 g). HPLC/MS (method 2): Rt: 0.551 min; m/z=199.9 (M+1)+.

To solution of 4-(4-aminopyrimidin-2-yl)benzaldehyde (0.700 g) in pyridine (20 mL) 4-(trifluoromethyl)benzoyl chloride (0.832 g) was added at 0° C. After stirring 16 h at room temperature, ethyl acetate (20 mL) was added. The resulting precipitate was was subjected to silica gel flash column chromatography eluting with a gradient of EtOAc and methanol to obtain the title compound as a solid (0.400 g). HPLC/MS (method 2): Rt: 1.143 min; m/z=371.9 (M+1)+.

Step 3: Synthesis of N-[2-[4-[(E)-[(2-isopropyl-5-methyl-phenyl)carbamothioylhydrazono]methyl]phenyl]pyrimidin-4-yl]-4-(trifluoromethyl)benzamide

N-[2-[4-[(E)-[(2-isopropyl-5-methyl-phenyl)carbamothioylhydrazono]methyl]phenyl]pyrimidin-4-yl]-4-(trifluoromethyl)benzamide (0.100 g) and methyl 2-bromoacetate (0.03 mL) were dissolved in ethanol (3.0 mL) and stirred for and stirred for 4 h at reflux temperature. After stirring 16 h at room temperature, the resulting precipitate was filtered and washed with cold ethanol to obtain the title compound as a solid (0.090 g). HPLC/MS (method 2): Rt: 1.488 min; m/z=617.2 (M+1)+.

By analogous procedures to the procedures described above for example C-5, C-12, C-13 the examples of formula I as listed in Table C were prepared.

Biological Examples

If not otherwise specified, the test solutions are prepared as follows:

The active compound is dissolved at the desired concentration in a mixture of 1:1 (vol:vol) distilled water:acetone. The test solution is prepared at the day of use.

Test solutions are prepared in general at concentrations of 1000 ppm, 500 ppm, 300 ppm, 100 ppm and 30 ppm (wt/vol).

For evaluating control of boll weevil (Anthonomus grandis) the test unit consisted of 96-well-microtiter plates containing an insect diet and 5-10A. grandiseggs.

The compounds were formulated using a solution containing 75% v/v water and 25% v/v DMSO. Different concentrations of formulated compounds were sprayed onto the insect diet at 5 μl, using a custom built micro atomizer, at two replications.

After application, microtiter plates were incubated at about 25±1° C. and about 75±5% relative humidity for 5 days. Egg and larval mortality was then visually assessed.

In this test, the following compounds at 2500 ppm showed over 75% mortality in comparison with untreated controls: C-24, C-25, C-26, C-27, C-28, C-29, C-30, C-31.

The active compound is dissolved at the desired concentration in a mixture of 1:1 (vol:vol) distilled water:acetone. Surfactant (Alkamuls® EL 620) is added at a rate of 0.1% (vol/vol). The test solution is prepared at the day of use.

Leaves of cabbage were dipped in test solution and air-dried. Treated leaves were placed in petri dish enlined with moist filter paper and inoculated with ten 3rdinstar larvae. Mortality was recorded 72 hours after treatment. Feeding damages were also recorded using a scale of 0-100%.

The active compounds were formulated in cyclohexanone as a 10,000 ppm solution supplied in tubes. The tubes were inserted into an automated electrostatic sprayer equipped with an atomizing nozzle and they served as stock solutions for which lower dilutions were made in 50% acetone:50% water (v/v). A non-ionic surfactant (Kinetic®) was included in the solution at a volume of 0.01% (v/v).

Cotton plants at the cotyledon stage (one plant per pot) were sprayed by an automated electrostatic plant sprayer equipped with an atomizing spray nozzle. The plants were dried in the sprayer fume hood and then removed from the sprayer. Each pot was placed into a plastic cup and about 10 to 12 whitefly adults (approximately 3-5 days old) were introduced. The insects were collected using an aspirator and a nontoxic Tygon® tubing connected to a barrier pipette tip. The tip, containing the collected insects, was then gently inserted into the soil containing the treated plant, allowing insects to crawl out of the tip to reach the foliage for feeding. Cups were covered with a reusable screened lid. Test plants were maintained in a growth room at about 25° C. and about 20-40% relative humidity for 3 days, avoiding direct exposure to fluorescent light (24-hour photoperiod) to prevent trapping of heat inside the cup. Mortality was assessed 3 days after treatment, compared to untreated control plants.

In this test, the following compounds at 300 ppm showed over 75% mortality in comparison with untreated controls: C-25.

The active compounds were formulated in cyclohexanone as a 10,000 ppm solution supplied in tubes. The tubes were inserted into an automated electrostatic sprayer equipped with an atomizing nozzle and they served as stock solutions for which lower dilutions were made in 50% acetone:50% water (v/v). A nonionic surfactant (Kinetic®) was included in the solution at a volume of 0.01% (v/v).

Lima bean plants (variety Sieva) were grown 2 plants to a pot and selected for treatment at the 1sttrue leaf stage. Test solutions were sprayed onto the foliage by an automated electrostatic plant sprayer equipped with an atomizing spray nozzle. The plants were dried in the sprayer fume hood and then removed from the sprayer. Each pot was placed into perforated plastic bags with a zip closure. About 10 to 11 armyworm larvae were placed into the bag and the bags zipped closed. Test plants were maintained in a growth room at about 25° C. and about 20-40% relative humidity for 4 days, avoiding direct exposure to fluorescent light (24 hour photoperiod) to prevent trapping of heat inside the bags. Mortality and reduced feeding were assessed 4 days after treatment, compared to untreated control plants.

For evaluating control of tobacco budworm (Heliothis virescens) the test unit consisted of 96-well-microtiter plates containing an insect diet and 15-25H. virescenseggs.

The compounds were formulated using a solution containing 75% v/v water and 25% v/v DMSO. Different concentrations of formulated compounds were sprayed onto the insect diet at 10 μl, using a custom built micro atomizer, at two replications.

After application, microtiter plates were incubated at about 28±1° C. and about 80±5% relative humidity for 5 days. Egg and larval mortality was then visually assessed.

For evaluating control of yellow fever mosquito (Aedes aegypti) the test unit consisted of 96-well-microtiter plates containing 200 μl of tap water per well and 5-15 freshly hatchedA. aegyptilarvae. The active compounds were formulated using a solution containing 75% (v/v) water and 25% (v/v) DMSO. Different concentrations of formulated compounds or mixtures were sprayed onto the insect diet at 2.5 μl, using a custom built micro atomizer, at two replications.

After application, microtiter plates were incubated at 28+1° C., 80+5% RH for 2 days. Larval mortality was then visually assessed.

Dichromothrips corbettiadults used for bioassay were obtained from a colony maintained continuously under laboratory conditions. For testing purposes, the test compound is diluted in a 1:1 mixture of acetone:water (vol:vol), plus Kinetic® HV at a rate of 0.01% v/v.

Thrips potency of each compound was evaluated by using a floral-immersion technique. All petals of individual, intact orchid flowers were dipped into treatment solution and allowed to dry in Petri dishes. Treated petals were placed into individual re-sealable plastic along with about 20 adult thrips. All test arenas were held under continuous light and a temperature of about 28° C. for duration of the assay. After 3 days, the numbers of live thrips were counted on each petal. The percent mortality was recorded 72 hours after treatment.

The active compounds were formulated by a Tecan liquid handler in 100% cyclohexanone as a 10,000 ppm solution supplied in tubes. The 10,000 ppm solution was serially diluted in 100% cyclohexanone to make interim solutions. These served as stock solutions for which final dilutions were made by the Tecan in 50% acetone:50% water (v/v) into 10 or 20 ml glass vials. A nonionic surfactant (Kinetic®) was included in the solution at a volume of 0.01% (v/v). The vials were then inserted into an automated electrostatic sprayer equipped with an atomizing nozzle for application to plants/insects.

Small (˜2″ in height) cotton plants are sprayed with test compounds at concentrations ranging from 300 to 0.01 ppm in acetone/water through the automated VPS. After drying, cotton leaves are removed and circular leaf discs (˜1 cm diameter) are punched from the treated surface and transferred to clean 20 mL scintillation vials. Ten Western flower thrips (FRANOC) are aspirated into each scintillation vial. The vials with the leaf discs and thrips are kept in an upright incubator at 25° C. and 50% relative humidity with a 14:10 light:dark photoperiod. Each treatment is replicated twice.

Thrips mortality is assessed at 2 DAT (days after treatment), counting all thrips both dead and alive. [The average absolute mortality is calculated for each treatment.]

In this test, the following compounds at 300 ppm showed over 75% mortality in comparison with untreated controls: C-12, C-15, C-18, C-24, C-27, C-28, C-30.