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Azaheterocycles, combinatory library, focused library, pharmaceutical composition and method for preparing (variants)
Azaheterocycles, combinatory library, focused library, pharmaceutical composition and method for preparing (variants)
IPC classes for russian patent Azaheterocycles, combinatory library, focused library, pharmaceutical composition and method for preparing (variants) (RU 2318818):
C40B40/04 -
Another patents in same IPC classes:
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Non-steroidal modulators of progesterone receptor Non-steroidal modulators of progesterone receptor / 2309155
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Bicyclic 1,4-piridotiazine-1,1-dioxides and method for production thereof Bicyclic 1,4-piridotiazine-1,1-dioxides and method for production thereof / 2307124
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Condensed pyridazine derivatives and drugs having the compounds as active ingredients Condensed pyridazine derivatives and drugs having the compounds as active ingredients / 2292337
Compound is represented by structural formula
Lactam compounds and their pharmaceutical using Lactam compounds and their pharmaceutical using / 2287530
Invention relates to novel lactam compounds of the formula (I) or their pharmaceutically acceptable salts wherein A means phenyl, thienyl, pyridyl, pyrimidinyl, pyrazinyl; R2, R3 and R4 can be similar or different and mean independently of one another hydrogen atom (H), halogen atom, -OH, (C1-C6)-alkyl, (C1-C6)-alkoxy-group, -NH2, -NO2, -CF3, phenyl that can comprise substitute(s), benzyloxy-group that can comprise substitute(s), pnehylvinyl, and one among R2, R3 and R4 means -CF3-O- and others mean H; B means phenyl that can comprises substitute(s), monocyclic aliphatic (C3-C8)-ring, dihydropyrane ring; -X- and -Y- xan be similar or different and they mean independently -O-, -NH-, -NR5-, -S-; Z means -CH2-, -NH-; W means -NR1-, -CR8R9- wherein R1 means H; R8 and R9 are similar or different and mean H; wherein R5 represents a linear alkyl group that can comprise substitute(s), (C1-C8)-linear or branched alkoxycarbonyl group, acyl group chosen from formyl group, acyl group comprising (C1-C6)-alkyl, (C1-C6)-alkenyl or (C1-C6)-alkynyl group that can comprise substitute(s), carbamoyl group comprising (C1-C6)-alkyl group at nitrogen atom that can comprise substitutes, sulfonyl group comprising (C1-C6)-alkyl group at sulfur atom that can comprise substitute(s); each among a, b and c represents position of carbon atom under condition that: (i) substitute(s) is chosen from the group comprising halogen atom, -OH, (C1-C6)-alkyl, mercapto-group, (C1-C6)-alkoxy-group, -NO2, -COOH, -CF3, phenyl, -NH2, (C1-C8)-linear or branched alkoxycarbonyl group, (C1-C8)-linear or branched acyl group, (C1-C8)-linear or branched acyloxy-group; (ii) when B represents benzene ring, each among -X- and -Y- represents -NH-, -Z- represents -CH2- and -W- represents -NH- then R2, R3 and R4 can not mean phenyl group, 4-bromophenyl group, 4-hydroxyphenyl group, 4-methoxyphenyl group, 2-hydroxyphenyl group, 3,4-dimethoxyphenyl group or 3-methoxy-4-hydroxyphenyl group. Compounds of the formula (I) show the enhanced capacity for transport of sugar and can be used in pharmaceutical compositions for prophylaxis and/or treatment of diabetes mellitus and diabetic nephropathy.
Isoxazoline derivative and herbicide comprising its as active component Isoxazoline derivative and herbicide comprising its as active component / 2286989
Invention relates to a compound of the general formula [I]: wherein R1 and R2 can be similar or different and each represents (C1-C10)-alkyl group; each among R3 and R4 represents hydrogen atom; R5 and R6 can be similar or different and each represents hydrogen atom or (C1-C10)-alkyl group; Y represents 5-6-membered aromatic heterocyclic group or condensed aromatic heterocyclic group comprising one or some heteroatoms chosen from nitrogen atom, oxygen atom and sulfur atom wherein heterocyclic group can be substituted with 0-6 of similar or different groups chosen from the following group of substitutes α, and so on; n means whole values from 0 to 2; [Group of substitutes α]: hydroxyl group, halogen atoms, (C1-C10)-alkyl groups, (C1-C10)-alkyl groups wherein each group is monosubstituted with group chosen from the following group of substitutes β, (C1-C4)-halogenalkyl groups, (C3-C8)-cycloalkyl groups, (C1-C10)-alkoxy-groups, (C1-C10)-alkoxy-groups wherein each group is monosubstituted with group chosen from the following group of substitutes and so on; [Group of substitutes β]: hydroxyl group, (C3-C8)-cycloalkyl groups that can be substituted with halogen atom or alkyl group, (C1-C10)-alkoxy-group, (C1-C10)-alkylthio-groups, (C1-C10)-alkylsulfonyl groups, (C1-C10)-alkoxycarbonyl groups, amino-group, carbamoyl group (wherein its nitrogen atom can be substituted with similar or different (C1-C10)-alkyl groups), (C1-C6)-acyl groups, (C1-C10)-alkoxyimino-groups, cyano-group, optionally substituted phenyl group; [Group of substitutes γ]: optionally substituted phenyl group, optionally substituted aromatic heterocyclic groups, cyano-group. Also, invention relates to herbicide comprising derivative of isoxazoline of the formula [I] as an active component or its pharmaceutically acceptable salt. Invention provides the development of isoxazoline derivative possessing the herbicide activity with respect to resistant weeds, selectivity for cultural crop and weed.
2-amino-4-acetyl-7-bromo-8<sup>b</sup>-hydroxy-3<sup>a</sup>,8<sup>b</sup>-dihydroxytiazolo[5,4-b]indole for liver protection from poisoning with carbon tetrachloride 2-amino-4-acetyl-7-bromo-8b-hydroxy-3a,8b-dihydroxytiazolo[5,4-b]indole for liver protection from poisoning with carbon tetrachloride / 2286348
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7-bromo-4-acetylthiazolo[5,4-b]indol-2-succinimide protecting body against hypoxia and possessing curative effect in lung toxic edema 7-bromo-4-acetylthiazolo[5,4-b]indol-2-succinimide protecting body against hypoxia and possessing curative effect in lung toxic edema / 2281951
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Method for production of e-2-aroylmethylene-1-phenyl-1,2,3,4-tetrahydroquinazolin-4-ones Method for production of e-2-aroylmethylene-1-phenyl-1,2,3,4-tetrahydroquinazolin-4-ones / 2306315
Invention relates to new method for production of E-2-aroylmethylene-1-phenyl-1,2,3,4-tetrahydroquinazolin-4-ones of general formula I wherein R represents H, methyl, Cl. Claimed method includes interaction of 5-aryl-2,3-dihydro-2,3-furandiones with N-phenylanthranyl acid amide in medium of inert aprotic solvent (preferably benzene) followed by isolation of target products. Process is carried out preferably at 79-80°C. Claimed compounds have fluorescent properties and are useful in labeling and copying agents, intermediates for synthesis of new heterocyclic compounds, etc.
Agent against acid-resistant microorganisms containing pyridone carboxylic acids as active component Agent against acid-resistant microorganisms containing pyridone carboxylic acids as active component / 2299205
Invention relates to an agent used against acid-resistant microorganisms containing derivative of pyridone carboxylic acid as an active component, its pharmaceutically acceptable salt or its hydrate that elicits high antibacterial activity against Mycobacterium tuberculosis and atypical acid-resistant microorganisms. Invention describes agent used against acid-resistant microorganisms containing compound represented by the following formula (I) its salt or its hydrate as an active component wherein R1 represents cyclic alkyl group comprising 3-6 carbon atoms that can comprise substitute(s) chosen from halogen atom; R2 represents hydrogen atom; R3 represents hydrogen atom; A1 represents incomplete structure represented by the formula (2): wherein X2 represents halogen atom, alkyl group comprising 1-6 carbon atoms or alkoxy-group comprising 1-6 carbon atoms; A1, A2 and A3 form incomplete structure of the formula: in common with carbon atoms combined with them; X1 represents halogen atom; Y represents hydrogen atom; Z represents phenylpiperazine substitute. Invention provides synthesis of pyridone carboxylic acid eliciting high antibacterial activity against Mycobacterium tuberculosis and atypical acid-resistant microorganisms in combination with good pharmacokinetics indices and safety.
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Agent against acid-resistant microorganisms containing heterocyclic derivatives of benzoxazine as active component Agent against acid-resistant microorganisms containing heterocyclic derivatives of benzoxazine as active component / 2297420
Invention relates to agent used against acid-resistant microorganisms. Invention describes agent against acid-resistant microorganisms containing as an active component the compound represented by the general formula (1) or its hydrate wherein R2 represents hydrogen atom; R3 represents hydrogen atom; A1, A2 and A3 form incomplete structure of the formula: wherein A1 represent incomplete structure of the formula: wherein X2 and above described R1 can be combined to form six-membered cyclic structure comprising part of the parent nucleus wherein formed ring can comprise oxygen atom and, except for, can comprise alkyl group having 1-6 carbon atoms as a substitute; X1 represents halogen atom, hydrogen atom or amino-group; Y represents hydrogen atom; Z represents incomplete structure of the formula: . Agent elicits high antibacterial activity of broad spectrum and possesses good pharmacokinetics and safety also.
Lactam compounds and their pharmaceutical using Lactam compounds and their pharmaceutical using / 2287530
Invention relates to novel lactam compounds of the formula (I) or their pharmaceutically acceptable salts wherein A means phenyl, thienyl, pyridyl, pyrimidinyl, pyrazinyl; R2, R3 and R4 can be similar or different and mean independently of one another hydrogen atom (H), halogen atom, -OH, (C1-C6)-alkyl, (C1-C6)-alkoxy-group, -NH2, -NO2, -CF3, phenyl that can comprise substitute(s), benzyloxy-group that can comprise substitute(s), pnehylvinyl, and one among R2, R3 and R4 means -CF3-O- and others mean H; B means phenyl that can comprises substitute(s), monocyclic aliphatic (C3-C8)-ring, dihydropyrane ring; -X- and -Y- xan be similar or different and they mean independently -O-, -NH-, -NR5-, -S-; Z means -CH2-, -NH-; W means -NR1-, -CR8R9- wherein R1 means H; R8 and R9 are similar or different and mean H; wherein R5 represents a linear alkyl group that can comprise substitute(s), (C1-C8)-linear or branched alkoxycarbonyl group, acyl group chosen from formyl group, acyl group comprising (C1-C6)-alkyl, (C1-C6)-alkenyl or (C1-C6)-alkynyl group that can comprise substitute(s), carbamoyl group comprising (C1-C6)-alkyl group at nitrogen atom that can comprise substitutes, sulfonyl group comprising (C1-C6)-alkyl group at sulfur atom that can comprise substitute(s); each among a, b and c represents position of carbon atom under condition that: (i) substitute(s) is chosen from the group comprising halogen atom, -OH, (C1-C6)-alkyl, mercapto-group, (C1-C6)-alkoxy-group, -NO2, -COOH, -CF3, phenyl, -NH2, (C1-C8)-linear or branched alkoxycarbonyl group, (C1-C8)-linear or branched acyl group, (C1-C8)-linear or branched acyloxy-group; (ii) when B represents benzene ring, each among -X- and -Y- represents -NH-, -Z- represents -CH2- and -W- represents -NH- then R2, R3 and R4 can not mean phenyl group, 4-bromophenyl group, 4-hydroxyphenyl group, 4-methoxyphenyl group, 2-hydroxyphenyl group, 3,4-dimethoxyphenyl group or 3-methoxy-4-hydroxyphenyl group. Compounds of the formula (I) show the enhanced capacity for transport of sugar and can be used in pharmaceutical compositions for prophylaxis and/or treatment of diabetes mellitus and diabetic nephropathy.
Isoxazoline derivative and herbicide comprising its as active component Isoxazoline derivative and herbicide comprising its as active component / 2286989
Invention relates to a compound of the general formula [I]: wherein R1 and R2 can be similar or different and each represents (C1-C10)-alkyl group; each among R3 and R4 represents hydrogen atom; R5 and R6 can be similar or different and each represents hydrogen atom or (C1-C10)-alkyl group; Y represents 5-6-membered aromatic heterocyclic group or condensed aromatic heterocyclic group comprising one or some heteroatoms chosen from nitrogen atom, oxygen atom and sulfur atom wherein heterocyclic group can be substituted with 0-6 of similar or different groups chosen from the following group of substitutes α, and so on; n means whole values from 0 to 2; [Group of substitutes α]: hydroxyl group, halogen atoms, (C1-C10)-alkyl groups, (C1-C10)-alkyl groups wherein each group is monosubstituted with group chosen from the following group of substitutes β, (C1-C4)-halogenalkyl groups, (C3-C8)-cycloalkyl groups, (C1-C10)-alkoxy-groups, (C1-C10)-alkoxy-groups wherein each group is monosubstituted with group chosen from the following group of substitutes and so on; [Group of substitutes β]: hydroxyl group, (C3-C8)-cycloalkyl groups that can be substituted with halogen atom or alkyl group, (C1-C10)-alkoxy-group, (C1-C10)-alkylthio-groups, (C1-C10)-alkylsulfonyl groups, (C1-C10)-alkoxycarbonyl groups, amino-group, carbamoyl group (wherein its nitrogen atom can be substituted with similar or different (C1-C10)-alkyl groups), (C1-C6)-acyl groups, (C1-C10)-alkoxyimino-groups, cyano-group, optionally substituted phenyl group; [Group of substitutes γ]: optionally substituted phenyl group, optionally substituted aromatic heterocyclic groups, cyano-group. Also, invention relates to herbicide comprising derivative of isoxazoline of the formula [I] as an active component or its pharmaceutically acceptable salt. Invention provides the development of isoxazoline derivative possessing the herbicide activity with respect to resistant weeds, selectivity for cultural crop and weed.
Phenylethenyl- or phenylethynyl-derivatives as antagonists of glutamate receptors Phenylethenyl- or phenylethynyl-derivatives as antagonists of glutamate receptors / 2284323
Invention relates to using phenylethenyl- or phenylethynyl-derivatives as antagonists of glutamates receptors. Invention describes using compound of the general formula (I):
Anellated cabamoylazaheterocycles, focused library, pharmaceutical composition and method for its preparing Anellated cabamoylazaheterocycles, focused library, pharmaceutical composition and method for its preparing / 2281947
Invention relates to novel anellated carbamoylazaheterocycles of the general formula (1) that possess inhibitory property of kinase activity and eliciting, for example, an anticancer activity. Also, compounds can be used as agonists, antagonists, receptor modulating agents, antiparasitic and antibacterial agents. Also, invention relates to a method for synthesis of compounds of the formula (1), a pharmaceutical composition based on thereof and a focused library for assay of leader-compounds. In compounds of the general formula (1) W represents 6-oxopiperazine, [1,4]-thiazepane, [1,4]-oxazepane or [1,4]-diazepane cycle anellated with at least one optionally substituted and optionally condensed heterocycle or carbocycle Q; Q represents optionally substituted thiophene, optionally substituted pyrrole, optionally substituted imidazole, optionally substituted thiazole, optionally substituted pyrrolidine, optionally substituted indole, optionally substituted benzofuran, optionally substituted pyridine, optionally substituted quinoline, optionally substituted benzene or optionally substituted naphthalene cycle; R1, R2 and R represent independently of each another hydrogen atom, inert substitute, optionally substituted (C1-C6)-alkyl, optionally substituted (C3-C8)-cycloalkyl, optionally substituted phenyl, optionally substituted aryl, optionally substituted heterocyclyl.
C-glycoside derivatives and their salts C-glycoside derivatives and their salts / 2317288
Invention relates to novel compounds representing C-glycoside derivatives and their salts of the formula: wherein ring A represents (1) benzene ring; (2) five- or six-membered monocyclic heteroaryl ring comprising 1, 2 or 4 heteroatoms chosen from nitrogen (N) and sulfur (S) atoms but with exception of tetrazoles, or (3) unsaturated nine-membered bicyclic heterocycle comprising 1 heteroatom representing oxygen atom (O); ring B represents (1) unsaturated eight-nine-membered bicyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O; (2) saturated or unsaturated five- or six-membered monocyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O; (3) unsaturated nine-membered bicyclic carbocycle, or (4) benzene ring; X represents a bond or lower alkylene wherein values for ring A, ring B and X correlate so manner that (1) when ring A represents benzene ring then ring B is not benzene ring, or (2) when ring A represents benzene ring and ring B represents unsaturated eight-nine-membered bicyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O and comprising benzene ring or unsaturated nine-membered bicyclic carbocycle comprising benzene ring then X is bound to ring B in moiety distinct from benzene ring comprised in ring B; each among R1-R4 represents separately hydrogen atom, -C(=O)-lower alkyl or lower alkylene-aryl; each R5-R11 represents separately hydrogen atom, lower alkyl, halogen atom, -OH, =O, -NH2, halogen-substituted lower alkyl-sulfonyl, phenyl, saturated six-membered monocyclic heterocycle comprising 1 or 2 heteroatoms chosen from N and O, lower alkylene-OH, lower alkyl, -COOH, -CN, -C(=O)-O-lower alkyl, -O-lower alkyl, -O-cycloalkyl, -O-lower alkylene-OH, -O-lower alkylene-O-lower alkyl, -O-lower alkylene-COOH, -O-lower alkylene-C(=O)-O-lower alkyl, -O-lower alkylene-C(=O)-NH2, -O-lower alkylene-C(=O)-N-(lower alkyl)2, -O-lower alkylene-CH(OH)-CH2(OH), -O-lower alkylene-NH, -O-lower alkylene-NH-lower alkyl, -O-lower alkylene-N-(lower alkyl)2, -O-lower alkylene-NH-C(=O)-lower alkyl, -NH-lower alkyl, -N-(lower alkyl)2, -NH-lower alkylene-OH or NH-C(=O)-lower alkyl. Indicated derivatives can be used as inhibitor of co-transporter of Na+-glucose and especially as a therapeutic and/or prophylactic agent in diabetes mellitus, such as insulin-dependent diabetes mellitus (diabetes mellitus 1 type) and non-insulin-dependent diabetes mellitus (diabetes mellitus 2 type), and in diseases associated with diabetes mellitus, such as insulin-resistant diseases and obesity.

FIELD: organic chemistry, medicine, biochemistry, pharmacy.

SUBSTANCE: invention relates to novel azaheterocycles of the general formula (I): possessing inhibitory effect on activity of tyrosine kinase and can be used in treatment of different diseases mediated by these receptors. In compound of the general formula (1) W represents azaheterocycle comprising 6-13 atoms that can be optionally annelated with at least one (C5-C7)-carbocycle and/or possibly annelated with heterocycle comprising 4-10 atoms in ring and comprising at least one heteroatom chosen from oxygen (O), sulfur (S) or nitrogen (N) atom; Ra 1 represents a substitute of amino group but not hydrogen atom, such as substituted (C1-C6)-alkyl, possibly substituted aryl and possibly substituted 5-10-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; Rb represents carbamoyl group -C(O)NHRa wherein Ra represents a substitute of amino group but not hydrogen atom, such as possibly substituted alkyl, possibly substituted aryl, possibly substituted 5-10-membered heterocyclyc comprising at least one heteroatom chosen from O, S or N; Rc represents a substitute of cyclic system, such as possibly substituted (C1-C6)-alkyl, possibly substituted aryl and possibly substituted 5-6-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; or Rb and Rc form in common aminocyanomethylene group [(=C(NH2)CN], or their pharmaceutically acceptable salts. Also, invention relates to methods for synthesis of these compounds (variants), a pharmaceutical composition, combinatory and focused libraries.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition, improved methods for synthesis and preparing.

35 cl, 16 sch, 13 tbl, 43 ex

 

The text descriptions are given in facsimile form.

1. Azaheterocycle General formula 1

where W represents azaheterocycle, including 6-13 atoms, optional annelirovannymi at least one C5-C7carbocycles and/or possibly the fused heterocycle with 4 to 10 atoms in the ring, and including at least one of the heteroatoms selected from the group O, S or N;

R1 ais a Deputy amino group, excluding hydrogen, such as, possibly substituted C1-C6alkyl, possibly substituted aryl or possibly substituted 5-10-membered heterocyclyl, including at least one of the heteroatoms selected from the group O, S or N; Rbare karbamoilnuyu group-C(O)otherain which Rais a Deputy amino group, excluding hydrogen, such as a possibly substituted alkyl, possibly substituted aryl, possibly substituted 5-10-membered heterocyclyl, including at least one of the heteroatoms selected from the group O, S or N; Rcare Deputy cyclic systems, such as possibly substituted C1-C6alkyl, perhaps C is displaced aryl or possibly substituted 5-6-membered heterocyclyl, including at least one of the heteroatoms selected from the group O, S or N, or Rband Rctogether form an amino-cyano-methylene group [(=C(NH2)CN]; or their pharmaceutically acceptable salts, including templates T-1.1 T-1.41; T-2.1-T; T-3.1 T-3.2:

in which the dotted line with its accompanying solid line (represents a single or double bond, and excluding azaheterocycle, including fragments In(1-29), azaheterocycle C1(1-6) and C2(1-17)

2. Compounds according to claim 1, which represents a substituted azaheterocycle General formula 1.1-1.5

where the dotted line with its accompanying solid line () is one the RNA or double bond; R1 a, Rband Rchave the above meaning; R2 ais a Deputy amino group, such as a hydrogen atom, possibly substituted C1-C6alkyl, each of R1 dand R2 d, R3 dand R4 dindependently from each other represent a Deputy cyclic system selected from hydrogen, possibly substituted C1-C6of alkyl, possibly substituted aryl, or

R1 dand R2 afor compounds 1.1, 1.2 and 1.3 and R2 dand R2 afor connections 1.4 and 1.5 can form together with the atoms to which they are linked, possibly substituted 4-10-membered azaheterocycles may contain additional heteroatoms selected from nitrogen, oxygen or sulfur, and possibly condensed with a benzene ring or another 5-6-membered heterocycle, in which the heteroatoms are selected from nitrogen, oxygen or sulfur, and

R3 dand R2 dfor compounds 1.3, R1 dand R2 dfor connections 1.4 and 1.5, and R4 dand R3 dfor connections 1.5 together with the atoms to which they are linked, may form a possibly substituted aliphatic cycle, containing 4-12 carbon atoms, POS is but substituted mono - or condensed barometrically cycle or possibly substituted 5-6-membered heterocycle, in which heteroatoms selected from nitrogen, oxygen or sulfur, and which may be condensed with another possibly substituted 5-6-membered heterocycle containing as heteroatoms nitrogen, oxygen or sulfur, or

Rcand R2 dfor compounds 1.2, or Rcand R3 dfor connections 1.3 and 1.4, or Rcand R4 dfor connections 1.5 together with the atoms to which they are linked, may form a possibly substituted aliphatic cycle, containing 4-12 carbon atoms or a possibly substituted 5-6-membered heterocycle, in which the heteroatoms are selected from nitrogen, oxygen or sulfur, and which may be condensed with another possibly substituted 5-6-membered heterocycle containing as heteroatoms nitrogen, oxygen or sulfur.

3. Compounds according to claim 1, which represents a substituted benzodiazepines General formula 1.6

where the dotted line with its accompanying solid line (represents a single or double bond, R1 a, R2 a, Rband Rchave the above significance, each of R1 d, R2 dand R3 dindependently from each other represent a Deputy cyclic system selected from hydrogen, possibly C is displaced C 1-C6of alkyl, possibly substituted aryl, or

R3 dand R2 dtogether with the atoms to which they are linked, may form a possibly substituted mono - or condensed barometrically cycle, possibly substituted 5-6-membered heterocycle, in which the heteroatoms are selected from nitrogen, oxygen or sulfur, and which may be condensed with another possibly substituted 5-6-membered heterocycle containing as heteroatoms nitrogen, oxygen or sulfur, or possibly substituted aliphatic cycle, containing 4-12 carbon atoms, and

R1 dand R2 amay form together with the atoms to which they are linked, possibly substituted 4-6-membered azaheterocycles may contain additional heteroatoms selected from nitrogen, oxygen or sulfur, and possibly condensed with a substituted benzene ring or another possibly substituted 5-6-membered heterocycle, in which the heteroatoms are selected from nitrogen, oxygen or sulfur.

4. Compounds according to claim 3, represents 3-oxo-2,3,4,5-tetrahydro-1H-benzo[e][1,4]benzodiazepines, General formula 1.6.1

where R1 a, R2 a, Rb, Rcand R1 dhave the above for the 1.6 value; Rn dp is ecstasy a one or two Vice-cyclic system, selected from hydrogen, possibly substituted C1-C6-alkyl, nitro, halogen, amino, C1-C6acylamino, arylsulfonyl-amino, arylenecarborane, possibly substituted 5-6-membered azaheterocycles.

5. Compounds according to claim 3 or 4, a 3-oxo-2,3,4,5-tetrahydro-1H-benzo[e][1,4]benzodiazepines, including template General formula 1.6.1.1-1.6.1.16

where Rband Rchave the above value.

6. Compounds according to claim 1, which represents a 7-oxazepan General formula 1.7

where the dotted line with its accompanying solid line (represents a single or double bond; R1 a, Rband Rchave the above meaning; R1 dand R2#x0200A; dtogether with the atoms to which they are linked, and R3 dand R4 dtogether with the atoms to which they are linked, form, respectively, possibly substituted aromatic cycle or possibly substituted 5-6-membered azaheterocycles may contain additional heteroatoms selected from nitrogen, oxygen or sulfur, and possibly condensed with a benzene ring or another 5-6-membered heterocycle, in which the heteroatoms are selected from nitrogen, oxygen, or sulfur, or a possibly substituted aliphatic cycle, containing 4-12 carbon atoms.

7. Compounds according to claim 6, representing kannelirovannye 7-oxazepine, including template General formula 1.7.1-1.7.74

where Rband Rchave the above value.

8. Compounds according to claim 1, which represents a substituted azaheterocycle General formula 1.8-1.15

where the dotted line with its accompanying solid line (represents a single or double bond, R1 a, Rband Rchave the above meaning; R2 ais a Deputy amino group, such as a hydrogen atom, possibly substituted C1-C6alkyl, each of R1 d, R2 d, R3 d, R4 dand R5 dindependently from each other represent a Deputy cyclic system selected from hydrogen, possibly substituted C1-C6of alkyl, possibly substituted aryl, or

R1 dand R2 afor connections, 1.8, 1.9, R2 aand R2 dfor connections 1.10, 1.11, R2 aand R3 dfor connections 1.12 and 1.13, R2 aand R4 dfor connections 1.14, 1.15 can form together with the atoms to which they are linked, possibly substituted 4-6-membered azaheterocycles may contain additional heteroatoms selected from nitrogen, oxygen or sulfur, and possibly condensed with a substituted benzene ring or another possibly substituted 5-6-membered heterocycle, in which the heteroatoms are selected from nitrogen, oxygen or sulfur, and

R1 dand R2 dfor connections 1.9, 1.12, 1.13, 1.14, 1.15, R2 dand R3 dfor connections 1.11, 1.14, 1.15, R4 dand R3 dfor connections 1.13, R4 dand R5 dfor connections 1.15 together with the atoms to which they are linked, may form a possibly substituted aliphatic cycle comprising 4 to 12 carbon atoms, possibly substituted mono - or condensed barometrically cycle or possibly substituted 5-6-membered heterocycle, in which the heteroatoms are selected from nitrogen, sour what kind or sulfur, and which may be condensed with another possibly substituted 5-6-membered heterocycle containing as heteroatoms nitrogen, oxygen or sulfur.

9. Compounds according to claim 1, which represents a substituted azaheterocycle General formula 1.16-1.18

where the dotted line with its accompanying solid line (represents a single or double bond, R1 a, R2 a, Rband Rchave the above meaning; R3 ais a Deputy amino group selected from the group of hydrogen, possibly substituted alkyl, possibly substituted cycloalkyl, possibly substituted aryl; R1 d, R2 d, R3 dand R4 dindependently from each other represent a cyclic system substituents selected from hydrogen, possibly substituted C1-C6of alkyl, possibly substituted aryl, or compounds 1.16 R2 dand R3 atogether with the atoms to which they are linked, may form a through R2 dand R3 apossibly substituted azaheterocycle; or for connections 1.17 independent R3 dand R3 a together with the atoms to which they are linked, may form a through R3 dand R3 apossibly substituted 4-6-membered azaheterocycles, a R1 dand R2 dtogether with the atoms to which they are linked, may form a through R1 dand R2 dpossibly substituted aromatic cycle, 5-6-membered ring possibly substituted heterocycle comprising at least one heteroatom selected from the group O, S or N, or an aliphatic cycle, comprising from 4 to 12 carbon atoms; or for connections 1.18 independent R1 dand R2 dtogether with the atoms to which they are linked, may form a through R1 dand R2 dpossibly substituted aromatic cycle, possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, or a possibly substituted aliphatic cycle, comprising from 4 to 12 carbon atoms, and R3 aand R3 dtogether with the atoms to which they are linked, may form a through R3 aand R3 dpossibly substituted 4-6-membered azaheterocycles, a R3 dand R4 dtogether with the atoms to which they are linked, may form a through R3 dand R4  dpossibly substituted aromatic cycle, possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, or a possibly substituted aliphatic cycle, comprising from 4 to 12 carbon atoms.

10. Compounds according to claim 1, which represents a substituted azaheterocycle General formula 1.19 or 1.20

where the dotted line with its accompanying solid line (represents a single or double bond, R1 a, R2 a, Rband Rchave the above meaning; R1 d, R2 d, R3 dand R4 dindependently from each other represent a Deputy cyclic system selected from hydrogen, possibly substituted C1-C6the alkyl or compounds 1.19 independent R1 dand R2 dtogether with the atoms to which they are linked, may form a through R1 dand R2 dpossibly substituted aromatic cycle, possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, or a possibly substituted aliphatic cycle, comprising from 4 to 1 carbon atoms, a R2 aand R3 dtogether with the atoms to which they are linked, may form a through R2 aand R3 dpossibly substituted 4-6-membered azaheterocycles; or for connections 1.20 independent R1 dand R2 dtogether with the atoms to which they are linked, may form a through R1 dand R2 dpossibly substituted aromatic cycle, possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, or a possibly substituted aliphatic cycle, comprising from 4 to 12 carbon atoms, R2 aand R3 dtogether with the atoms to which they are linked, may form a through R2 aand R3 dpossibly substituted 4-6-membered azaheterocycles, and R3 dand R4 dtogether with the atoms to which they are linked, may form a through R3 dand R4 dpossibly substituted aromatic cycle, possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, or a possibly substituted aliphatic cycle, comprising from 4 to 12 carbon atoms.

11. Connection of claim 10, which represents a substituted azaheterocycle the General formula 1.19.1 or 1.20.1

where the dotted line with its accompanying solid line (represents a single or double bond, R1 a, R2 a, Rb, Rc, R3 dand R4 dhave the above for 1.19 and 1.20 value, Rn drepresents one or two Vice-cyclic system selected from hydrogen, possibly substituted C1-C4-alkyl.

12. Compounds according to claim 1, which represents a substituted azaheterocycle General formula 1.21 or 1.22

where the dotted line with its accompanying solid line (represents a single or double bond, R1 a, R2 a, Rband Rchave the above meaning; R1 d, R2 d, R3 dand R4 dindependently from each other represent a Deputy cyclic system selected from hydrogen, possibly substituted C1-C6-alkyl, or for connections 1.21 independent R1 dand R2 dtogether with the atom to which they are bound, may form a through R1Ȁ dand R2 dpossibly substituted C3-C6-cycloalkyl, R2 aand R2 dtogether with the atoms to which they are linked, may form a through R2 aand R2 dpossibly substituted 5-6-membered azaheterocycles may contain additional heteroatoms selected from nitrogen, oxygen, or sulfur, a R3 dand R4 dtogether with the atoms to which they are linked, may form a through R3 dand R4 dpossibly substituted 5-6-membered azaheterocycles; or for connections 1.22 independent R1 dand R2 dtogether with the atoms, with kotorii they are linked, may form a through R1 dand R2 dpossibly substituted aromatic cycle, possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, or a possibly substituted aliphatic cycle, comprising from 4 to 12 carbon atoms; R2 aand R2 dtogether with the atoms to which they are linked, may form a through R2 aand R2 dpossibly substituted 5-6-membered azaheterocycles may contain an additional heteroatom selected from nitrogen, oxygen or sulfur, and R3Ȁ dand R4 dtogether with the atoms to which they are linked, may form a through R3 dand R4 dpossibly substituted aromatic cycle, possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, or a possibly substituted aliphatic cycle, comprising from 4 to 12 carbon atoms.

13. Connection 12, which represents a substituted azaheterocycle General formula 1.21.1 or 1.22.1

where the dotted line with its accompanying solid line (represents a single or double bond, R1 a, R2 a, Rb, Rc, R1 dand R2 dhave the above for 1.21 and 1.22 is, Rn drepresents one or two Vice-cyclic system selected from hydrogen or a possibly substituted C1-C6-alkyl.

14. Compounds according to claim 1, which represents a substituted azaheterocycle General formula 1.23-1.33

where a is an atom, O, S or NR2 a; dotted line with its accompanying solid line (represents a single or double bond; R1 a, Rband Rchave the above meaning; R2 ais a Deputy amino group, such as a hydrogen atom, possibly substituted C1-C6alkyl, each of R1 d, R2 d, R3 d, R4 d, R5 dand R6 dindependently from each other represent a Deputy cyclic system selected from hydrogen, possibly substituted C1-C6of alkyl, possibly substituted aryl, or compounds 1.23 and 1.27 R1 dand R2 dtogether with the atom to which they are bound, may form a through R1 dand R2 dpossibly substituted C5-C6cycloalkyl; for connections 1.23, 1.25, 1.27, 1.28, 1.30, 1.31, 1.33 R3 dand R4 dtogether with the atoms to which they are linked, may form a through R3 dand R4 dpossibly substituted aromatics the third cycle, possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, or a possibly substituted aliphatic cycle, comprising from 4 to 12 carbon atoms, and compounds 1.23, 1.24, 1.25, 1.26 Rcand R4 dtogether with the atoms to which they are linked, may form a through Rcand R4 dpossibly substituted cycloalkyl or possibly substituted 5-6-membered heterocycle; or for connections 1.24, 1.25, 1.26, 1.28, 1.29, 1.30, 1.31, 1.32, 1.33 independent R1 dand R2 dtogether with the atoms to which they are linked, may form a through R1 dand R2 dpossibly substituted aromatic cycle, possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, or a possibly substituted aliphatic cycle, comprising from 4 to 12 carbon atoms; for connections 1.24 R3 dand R4 dtogether with the atom to which they are bound, may form a through R3 dand R4 dpossibly substituted C5-C6cycloalkyl, a Rcand R4 dtogether with the atoms to which they are linked, may form a through Rcand R4 dpossibly substituted C5-C6cycloalkyl; or D. the I compounds 1.26 R 2 dand R3 dtogether with the atoms to which they are linked, can form, respectively, by R2 dand R3 dpossibly substituted aromatic cycle, possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, or a possibly substituted aliphatic cycle, comprising from 4 to 12 carbon atoms; for connections 1.27, 1.29, 1.30, 1.31 and 1.32 R4 dand R5 dtogether with the atoms to which they are linked, may form a through R4 dand R5 dpossibly substituted cycloalkyl; for connections 1.26,1.27, 1.29, 1.30 Rcand R5 dtogether with the atoms to which they are linked, may form a through Rcand R5 dpossibly substituted C5-C6cycloalkyl; for connections 1.28 R5 dand R6 dtogether with the atom to which they are bound, may form a through R5 dand R6 dpossibly substituted C5-C6cycloalkyl, a Rcand R6 dtogether with the atoms to which they are linked, may form a through Rcand R6 dpossibly substituted C5-C6cycloalkyl; for connections 1.31, 1.32, 1.33 R5 dand R6 d together with the atoms to which they are linked, may form a through R5 dand R6 dpossibly substituted aromatic cycle, possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, or a possibly substituted aliphatic cycle, comprising from 4 to 12 carbon atoms, a Rcand R6 dtogether with the atoms to which they are linked, may form a through Rcand R6 dpossibly substituted C5-C6cycloalkyl or possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N; or for connections 1.32, 1.33 R2 dand R3 dtogether with the atoms, with kotorii they are linked, may form a through R2 dand R3 dpossibly substituted aromatic cycle, possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, or a possibly substituted aliphatic cycle, comprising from 4 to 12 carbon atoms.

15. Compounds according to claim 1, which represents a substituted azaheterocycle General formula 1.37-1.40

where the dotted line with its accompanying solid line (represents a single or double bond, R1 a, R2 a, Rband Rchave the above meaning; R4 ais a Deputy amino group selected from a possibly substituted C1-C6of alkyl; each of R1 d, R2 d, R4 dand R5 dindependently from each other represent a Deputy cyclic system selected from hydrogen, possibly substituted C1-C6of alkyl, possibly substituted aryl, or compounds 1.37 R1 dand R2 dtogether with the atom to which they are bound, may form a through R1 dand R2 dpossibly substituted C5-C6cycloalkyl, R2 aand R4 atogether with the atoms to which they are linked, may form a through R2 aand R4 apossibly substituted 5-6-membered azaheterocycles, a Rcand R4 dtogether with the atoms to which they are linked, may form a through Rcand R4 dpossibly substituted C5-C6cycloalkyl or possibly substituted 5-6-membered heterocycle comprising, according to what ina least one of the heteroatoms selected from the group O, S or N; or for connections 1.38 independent R1 dand R2 dtogether with the atom to which they are bound, may form a through R1 dand R2 dpossibly substituted C5-C6cycloalkyl or possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, R2 aand R4 atogether with the atom to which they are bound, may form a through R2 aand R4 apossibly substituted azaheterocycle, a Rcand R4 dtogether with the atoms to which they are linked, may form a through Rcand R4 dpossibly substituted C5-6cycloalkyl or possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N; or for connections 1.39 independent R1 dand R2 dtogether with the atom to which they are bound, may form a through R1 dand R2 dpossibly substituted C5-6cycloalkyl or possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, R2 aand R4 atogether with the ohms, to which they are linked, may form a through R2 aand R4 apossibly substituted 5-6-membered azaheterocycles, independent R4 dand R5 dtogether with the atoms to which they are linked, may form a through R4 dand R5 dpossibly substituted aromatic cycle may annelirovannymi possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, or a possibly substituted aliphatic cycle, comprising from 4 to 12 carbon atoms, a Rcand R5 dtogether with the atoms to which they are linked, may form a through Rcand R5 dpossibly substituted C5-6cycloalkyl or possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N; or for connections 1.40 independent R1 dand R2 dtogether with the atom to which they are bound, may form a through R1 dand R2 dpossibly substituted cycloalkyl or possibly substituted heterocycle, R2 aand R4 atogether with the atom to which they are bound, may form a through R2 aand R4 apossibly substituted 5-6-clenn the th azaheterocycle, R4 dand R5 dtogether with the atoms to which they are linked, may form a through R4 dand R5 dpossibly substituted aromatic cycle, possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, or a possibly substituted aliphatic cycle, comprising from 4 to 12 carbon atoms, a Rcand R5 dtogether with the atoms to which they are linked, may form a through Rcand R5 dpossibly substituted cycloalkyl or possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N.

16. Azaheterocycle General formula 2.1-2.4 and their pharmaceutically acceptable acid additive salt

where R1 ais a Deputy amino group, preferably a possibly substituted C1-C6alkyl, possibly substituted aryl or possibly substituted 5-6-membered heterocyclyl, including at least one of the heteroatoms selected from the group O, S or N; R2 aand R3 aindependently from each other represent a Deputy shall stitely amino group, selected from the group of hydrogen, possibly substituted alkyl, possibly substituted aryl; R1 d, R2 d, R3 d, R4 d, R5 d, R6 d, R7 dand R8 dindependently from each other represent a Deputy cyclic system selected from hydrogen, possibly substituted C1-C6of alkyl, possibly substituted aryl or possibly substituted 5-6-membered heterocyclyl, including at least one of the heteroatoms selected from the group O, S or N, or perhaps replaced With3-6cycloalkyl; or R1 dand R2 dtogether with the carbon atom to which they are bound, may form a through R1 dand R2 dpossibly substituted C3-6cycloalkyl; or for compounds 2.1 and 2.2 R3 d, R4 d, R5 d, R6 dtogether with the atoms to which they are linked, may form a through R4 dand R5 dpossibly substituted aromatic cycle or possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, or a possibly substituted aliphatic cycle, comprising from 4 to 12 carbon atoms; or R2 atogether with the atom to which it is linked, and R3 dand R4 dtogether with the atoms to which they are linked, form a through R2 aand R3 dand R4 dpossibly substituted 5-6-membered azaheterocycles; or R3 atogether with the atom to which it is linked, and R5 dand R6 dtogether with the atoms to which they are linked, form a through R3 aand R5 dand R6 dpossibly substituted 5-6-membered azaheterocycles; or R2 atogether with the atom to which it is linked, and R3 d, R4 d, R5 dand R6 dtogether with the atoms to which they are linked, form a through R2 a, R4 dand R5 dpossibly substituted 5-6-membered azaheterocycles; or R3 atogether with the atom to which it is linked, and R3 d, R4 d, R5 dand R6 dtogether with the atoms to which they are linked, form a through R3 a, R4 dor R5 dand R6 dpossibly substituted 5-6-membered azaheterocycles; or for connections 2.3 and 2.4, R3 d, R4 d, R5 dand R6  dtogether with the atoms to which they are linked, form a through R4 dand R5 dpossibly substituted aromatic cycle, possibly substituted 5-6-membered heterocycle comprising at least one heteroatom selected from the group O, S or N, or a possibly substituted aliphatic cycle, comprising from 4 to 12 carbon atoms; or R5 d, R6 d, R7 dand R8 dtogether with the atoms to which they are linked, form a through R7 dand R5 dpossibly substituted aromatic cycle, possibly substituted 5-6-membered azaheterocycles, including at least one of the heteroatoms selected from the group O, S or N, or a possibly substituted aliphatic cycle, comprising from 4 to 12 carbon atoms, excluding piperazine E

17. Azaheterocycle General formula 3.1 or 3.2

where connections 3.1 R1 aand R2 aindependently from each other represent a Deputy amino group selected from a possibly substituted C1-6of alkyl, possibly substituted cycloalkyl, possibly substituted aryl; R1 drepresents aryl; R2 dnot only is em a hydrogen atom or a C 1-C6alkyl, or R1 dand R2 dtogether with the atom to which they are bound, form a through R1 dand R2 dcycloalkyl or 5-6-membered heterocyclyl; R3 dand R4 dindependently from each other represent a Deputy cyclic system selected from C1-C6the alkyl, or R3 dand R4 dtogether with the carbon atom to which they are bound, form a through R3 dand R4 dcycloalkyl or possibly substituted 5-6-membered azaheterocycles; for connections 3.2 R1 ais a Deputy amino group; R1 drepresents aryl or heterocyclyl; R2 drepresents a hydrogen atom or a C1-C6alkyl, or R1 dand R2 dtogether with the atom to which they are bound, form a through R1 dand R2 dC5-C6cycloalkyl or 5-6-membered heterocycle; R2 atogether with the atom to which it is linked, and R3 dtogether with the atom to which it is linked, form a through R2 aand R3 d5-6-membered azaheterocycles, excluding piperazinone General formula D

where R1 a=N, CH3; R2 a= optionally substituted alkyl; R1 daryl or optionally substituted alkyl; R2 dand R3 d= optionally substituted alkyl, or R2 dand R3 dtogether with the carbon atom to which they are connected, form a through R2 dand R3 dcyclopropane.

18. Connection 17, which represents azaheterocycle, including the fragment of the formula 3.1.1-3.1.7

19. The method of producing azaheterocycles General formula 1.1-1.5 according to claim 2 interaction bifunctional reagent of General formula 4.5(1-5)selected from the group below, or optionally N-protected amino acids of General formula 4.1(1-3)selected from the group below, and ether oxo-carboxylic acids of General formula 4.2(1-3)selected from the group below, with isonitriles General formula2and the primary amine of General formula3in the environment of an organic solvent, however, in the case of preparing compounds in which Rband Rctogether represent sabinecretella =C(other 3 a)CN, the reaction is carried out in the presence of an acid catalyst

where R' represents hydrogen or (CH3)3SOS(Oh);

R" represents alkyl or aryl;

R1 a, R2 a, R3 a, Rc, R1 d, R2 d, R3 dand R4 dhave the meanings specified above for compounds of General formula 1.1-1.5.

20. The method of producing azaheterocycles General formula 1.6 according to claim 3 interaction in the environment of organic solvent isonitrile General formula2the primary amine of General formula3and bifunctional reagent of General formula 4.7, or optionally N-protected amino acids of General formula 4.1 and halogenocarboxylic compounds of General formula 4.6, followed by cyclization of the resulting adducts, and to obtain the compounds of General formula 1.6, in which Rband Rctogether represent aminocinnamate is eh =C(other 3 a)CN, the reaction is carried out in the presence of an acid catalyst

where R1 a, R2 a, R3 a, Rc, R1 d, R2 dand R3 dhave the meanings specified above for azaheterocycles General formula 1.6; R' represents hydrogen or (CH3)3SOS(ON).

21. The method of obtaining Azarov General formula 1.7 6 interaction bifunctional reagent of General formula 4.8, isonitrile General formula2and the primary amine of General formula3in the environment of an organic solvent, whereby to obtain compounds of General formula 1.7, in which Rband Rctogether they are aminocinnamate C(other3 a)CN, the reaction is carried out in the presence of an acid catalyst

where R1 a, R3 a, Rc, R1 d, R2 d, R3 dand R4 dhave the meanings specified above for azaheterocycles General formula 1.7.

22. The method of obtaining and what heterocycles General formula 1.8-1.15 of claim 8 interaction of isonitrile General formula B 2the primary amine of General formula3in the environment of organic solvent and monoether dicarboxylic acid of General formula 4.9(1-4) and optionally protected amino-carbonyl compounds of General formula 4.10(1-3) followed by cyclization of the resulting adducts or bifunctional reagent of General formula 4.11(1-8), and to obtain the compounds of General formula 1.8-1.15, in which Rband Rctogether they are aminocinnamate C(other3 a)CN, the reaction is carried out in the presence of an acid catalyst

where R1 a, R2 a, R3 a, Rc, R1 d, R2 d, R3 d, R4 dand R5 dhave the meanings specified above for azaheterocycles General formula 1.8-1.15.

23. Ways is getting azaheterocycles General formula 1.16-1.18 according to claim 9 interaction in the environment of organic solvent isonitrile General formula 2the primary amine of General formula3and bifunctional reagent of General formula 4.12(1-3), and to obtain the compounds of General formula 1.16-1.18, in which Rband Rctogether they are aminocinnamate C(other3 a)CN, the reaction is carried out in the presence of an acid catalyst

where R1 a, R2 a, R3 a, Rc, R1 d, R2 d, R3 dand R4 dhave the meanings specified above for azaheterocycles General formula 1.16-1.18.

24. The method of producing azaheterocycles General formula 1.19, 1.20 of claim 10 interaction in the environment of organic solvent isonitrile General formula2the primary amine of General formula3and bifunctional reagent of General formula 4.13(1,2), and to obtain the compounds of General formula 1.19, 1.20, in which Rband Rctogether they are aminocinnamate C(other3 a)CN, the reaction is carried out in the presence of an acid catalyst

p num="137"> where R1 a, R2 a, R3 a, Rc, R1 d, R2 d, R3 dand R4 dhave the meanings specified above for azaheterocycles General formula 1.19,1.20.

25. The method of producing azaheterocycles General formula 1.21, 1.22 on para.12 interaction in the environment of organic solvent isonitrile General formula2the primary amine of General formula3and bifunctional reagent of General formula 4.14(1,2), and to obtain the compounds of General formula 1.21, 1.22, in which Rband Rctogether they are aminocinnamate C(other3 a)CN, the reaction is carried out in the presence of an acid catalyst

where R1 a, R2 a, R3 a, Rc, R1 d, R2 d, R3 dand R4 dhave the meanings specified above for azaheterocycles General formula 1.21, 1.22.

26. The method of producing azaheterocycles General formula 1.23-1.33 on 14 interaction of isonitrile General formula B2the primary amine of General formula3substituted acid of General formula 4.15(1-4) and the halogen-carbonyl connected to the I General formula 4.16(1-4) in an organic solvent with subsequent cyclization of the resulting adducts, moreover, to obtain the compounds of General formula 1.23-1.33, in which Rband Rctogether they are aminocinnamate C(other3 a)CN, the reaction is carried out in the presence of an acid catalyst

where R1 a, R3 a, Rc, R1 d, R2 d, R3 d, R4 d, R5 d, R6 dand a have the meanings specified above for azaheterocycles General formula 1.23-1.33.

27. The method of producing azaheterocycles General formula 1.23-1.33 on 14 interaction of isonitrile General formula2the primary amine of General formula3corresponding halogen-substituted acids of General formula 4.17(1-4) and the appropriate substituted carbonyl compounds of General formula 4.18(1-4) in an organic solvent with subsequent cyclization of the resulting adducts, and to obtain the compounds of General formula 1.23-1.33, in which Rband Rctogether they are aminocinnamate C(other3 a)CN, the reaction is carried out in prisutstvie the acid catalyst

where R1 a, R3 a, Rc, R1 d, R2 d, R3 d, R4 d, R5 d, R6 dand a have the meanings specified above for azaheterocycles General formula 1.23-1.33.

So get azaheterocycles General formula 1.23-1.33 on 14 interaction of isonitrile General formula2the primary amine of General formula3and the corresponding bifunctional reagent of General formula 4.19.1-4.19.11 in the environment of an organic solvent, whereby to obtain compounds of General formula 1.23-1.33, in which Rband Rctogether they are aminocinnamate C(other3 a)CN, the reaction is carried out in the presence of an acid catalyst

where R1 a, R3 a, Rc, R1 d, R2 d, R3 d, R4 d, R5 d, R6 dand a have the meanings specified above for azaheterocycles General formula 1.23-1.33.

29. The method of producing azaheterocycles General formula 1.37, 1.39 on clause 15 of the interaction of isonitrile General formula2the primary amine of General formula3, (2,3-disubstituted-touraid)-acetic acid of General formula 4.20 and halogen-carbonyl compounds of General formula 4.21.1 4.21.2 or in the environment of an organic solvent with subsequent cyclization of the resulting adducts, or a bifunctional reagent of General formula 4.22.1 or 4.22.2 in the environment of an organic solvent, whereby to obtain compounds of General formula 1.37, 1.39, in which Rband Rctogether they are aminocinnamate C(other4 a)CN, the reaction is carried out in the presence of an acid catalyst

where R1 a, R2 a, R3 a, R4 a, Rc, R1  d, R2 d, R3 d, R4 dand R5 dhave the meanings specified above for azaheterocycles General formula 1.37, 1.39.

30. The method of producing azaheterocycles General formula 1.38, 1.40 on clause 15 of the interaction of isonitrile General formula2the primary amine of General formula3and halogen-carbonyl compounds of General formula 4.21.1 4.21.2 or and (3,3-disubstituted-touraid)-acetic acid of General formula 4.23 in the environment of an organic solvent with subsequent cyclization of the resulting adducts or bifunctional reagent of General formula 4.24.1 or 4.24.2, and to obtain the compounds of General formula 1.38, 1.40, in which Rband Rctogether they are aminocinnamate C(other4 a)CN, the reaction is carried out in the presence of an acid catalyst

where R1 a, R2 a, R3 a, R4 a, Rc, R1 d, R2 d, R3 d, R4 dand R5 dhave the meanings specified above for azaheterocycles General formula 1.38, 1.40.

31. The method of obtaining azaheterocycle what s the General formula 2.1-2.4 P16 interaction of carbonyl compounds of General formula 4.26, isonitrile General formula2and bifunctional reagent of General formula 4.27.1 or 4.27.2 in the medium of organic solvent

where R1 a, R2 a, R3 a, R1 d, R2 d, R3 d, R4 d, R5 d, R6 d, R7 dand R8 dhave the meanings specified above for azaheterocycles General formula 2.1-2.4.

32. The method of producing azaheterocycles General formula 3.1, 3.2 on 17 interaction in the environment of organic solvent isonitrile General formula B2the primary amine of General formula3, carbonyl compounds of General formula 4.26 and optionally N-protected amino acids of General formula 4.28

where R1 a, R2 a, R3 a, R1 d, R2 d, R3 dand R4 dhave the meanings specified above for azaheterocycles General formula 3.1, 3.2; R represents a hydrogen atom or (CH3 )3SOS(ON).

33. A combinatorial library to identify compounds leaders, consisting of azaheterocyclic compounds of General formula 1 according to claim 1, and/or azaheterocyclic compounds of the General formula 2.1, 2.2, 2.3 and 2.4 in clause 16, and/or azaheterocyclic compounds of the General formula 3.1 and 3.2 by 17.

34. Focused library to identify compounds leaders, containing at least one of azaheterocyclic compound of General formula 1 according to claim 1, and/or azaheterocyclic compound of General formula 2.1, 2.2, 2.3 and 2.4 in clause 16, and/or azaheterocyclic compound of General formula 3.1 and 3.2 by 17.

35. Pharmaceutical composition having anti-cancer activity and is intended to obtain drugs for treating and preventing various diseases in animals and humans in the form of tablets, capsules, or injections, placed in pharmaceutically acceptable packing, containing as active substance pharmaceutically effective amount of at least one of azaheterocyclic compounds of General formula 1 according to claim 1, and/or azaheterocyclic compounds of General formula 2.1, 2.2, 2.3 and 2.4 in clause 16, and/or azaheterocyclic compounds of General formula 3.1 and 3.2 to 17, or its pharmaceutically acceptable salt.

 
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