New condensed heterocyclic compounds and their use

FIELD: chemistry.

SUBSTANCE: present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts. The disclosed compounds have inhibitory effect on HsEg5. In formula (I) A is C=O or CH2; B is optionally substituted C1-6alkyl, D is O or N, where O is substituted with one R8, and where N is substituted with one or more R8, R1 and R2 together with the carbon atoms with which they are bonded form optionally substituted isothiazole or isoxazole, condensed with a pyrimidine ring, optionally substituted with a substitute which is C1-6 alkyl. Values of the rest of the radicals are given in the formula of invention.

EFFECT: invention relates to use of disclosed compounds in making medicinal agents with inhibitory effect on HsEg5, to a method of obtaining inhibitory effect on HsEg5, to a pharmaceutical composition which contains the disclosed compound as an active ingredient.

22 cl, 31 ex

 

The text descriptions are given in facsimile form.

1. Compound characterized by the structural formula (I)

in which a is a C=O or CH2;
In represents an optionally substituted C1-6alkyl, substituents independently selected from-NH2, -OH, -NHC1-6of alkyl, -N(C1-6the alkyl)2, -NH-C3-6cycloalkyl, 4-6-membered saturated heterocycle containing nitrogen as heteroatom;
D represents O or N, where substituted with one R8and where N is substituted by one or more R8and when n is 0 and m is not equal to 0, R8directly attached to B;
R1and R2in combination with the carbon atoms to which they are attached, form an optionally substituted isothiazol condensed with the pyrimidine ring, which is optionally substituted by 1 Deputy, which represents a C1-6alkyl;
R3represents phenyl, optionally substituted with halogen;
R4and R5represent H;
R6and R7independently selected from H or unsubstituted C1-6of alkyl;
R8independently selected from H, unsubstituted C1-6the alkyl, unsubstituted With3-7cycloalkyl or unsubstituted 4-6 membered heterocycle, where N is a heteroatom;
R9represents an unsubstituted benzothiophene, unsubstituted naphthyl or phenyl, optionally substituted by 1 or 2 substituents, where the substituents independently selected from C1-6of alkyl, -OC1-6of alkyl, halogen or naphthyl;
or its pharmaceutically acceptable salt.

2. The compound or its pharmaceutically acceptable salt according to claim 1, where a is a C=O.

3. The compound or its pharmaceutically acceptable salt according to claim 1, where In is an optionally substituted C1-4al the sludge, the Deputy independently selected from-NH2-HE,- NCH3, -N(CH3)2, -N-cyclopropane, N-CYCLOBUTANE, azetidine, pyrrolidine or piperidine.

4. The compound or its pharmaceutically acceptable salt according to claim 1, where D represents O, substituted with one R8.

5. The compound or its pharmaceutically acceptable salt according to claim 1, where D represents N, substituted with two R8.

6. The compound or its pharmaceutically acceptable salt according to claim 1, where R1and R2together form an optionally substituted condensed isothiazol, optionally substituted stands.

7. The compound or its pharmaceutically acceptable salt according to claim 1, where R3represents optionally substituted phenyl, where specified, the Deputy Director is F.

8. The compound or its pharmaceutically acceptable salt according to claim 1, where R6and R7independently selected from H, ethyl or isopropyl.

9. The compound or its pharmaceutically acceptable salt according to claim 1, where R8independently selected from H, unsubstituted C1-6the alkyl or unsubstituted 4-6 membered heterocycle, where N is a heteroatom.

10. The compound or its pharmaceutically acceptable salt according to claim 1, where R9represents phenyl which is optionally substituted by 1 or 2 substituents, where these substituents independently selected from methyl, IU is hydroxy, F or CL.

11. The compound or its pharmaceutically acceptable salt according to claim 1,
where n is 1;
And is;
Represents a C1-6alkyl;
D represents N;
R1and R2in combination with the carbon atoms to which they are attached, form a isothiazol condensed with pyrimidine ring;
R3represents phenyl, optionally substituted by F;
R4and R5represent H;
R6and R7represent H, ethyl or isopropyl;
R8represents H or unsubstituted C1-6alkyl;
R9represents phenyl, optionally substituted stands, methoxy, CL or F.

12. The compound or its pharmaceutically acceptable salt of formula (I) according to claim 1, chosen from:
N-(3-Aminopropyl)-N-{1-[5-(4-terbisil)-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl]propyl} -4-methylbenzamide;
N-(3-Aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)propyl]-4-bromobenzene;
N-(3-Aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)propyl]-4-chlorobenzamide;
N-(3-Aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)propyl]-3-fluoro-4-methylbenzamide;
N-(3-Aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)propyl]-2,3-dichlorobenzamide;
(3-Aminopropyl)-[1-(5-benzo is l-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)propyl]amide naphthalene-2-carboxylic acid;
(3-Aminopropyl)-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)-propyl]amide benzo[b]thiophene-2-carboxylic acid;
N-Azetidin-3-ylmethyl-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)propyl]-4-methylbenzamide;
N-[1-(5-Benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)propyl]-4-methyl-N-piperidine-3-iletilmesine;
N-(2-amino-ethyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)propyl]-4-methylbenzamide;
N-[1-(5-Benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)propyl]-N-(2-dimethylaminoethyl)-4-methylbenzamide;
N-[1-(5-Benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)propyl]-N-(3-dimethylaminopropyl)-4-methylbenzamide;
N-[1-(5-Benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)propyl]-N-[3-(isopropylamino)propyl]-4-methylbenzamide;
N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)propyl]-N-[3-(cyclopropylamino)propyl]-4-methylbenzamide;
N-(3-azetidin-1-ylpropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)propyl]-4-methylbenzamide;
N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)propyl]-4-methyl-N-[3-(3-pyrrolidin-1-ylpropyl)benzamide;
N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)propyl]-4-methyl-N-[3-(methylamino)propyl]benzamide;
N-[1-(5-Benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)propyl]--(3-hydroxypropyl)-4-methylbenzamide;
N-(3-Aminopropyl)-N-[1(5-benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)propyl]-4-methylbenzamide;
N-(3-Aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl)-2-methylpropyl]-4-methylbenzamide;
N-(3-Aminopropyl)-N-{1-[5-(4-terbisil)-3-methyl-4-oxo-4,5-dihydrothiazolo[5,4-d]pyrimidine-6-yl]-2-methylpropyl}-4-methylbenzamide; and
5-Benzyl-6-{1-[(3-hydroxypropyl)-(4-methylbenzyl)amino]propyl}-3-methyl-5H-isothiazol[5,4-d]pyrimidine-4-it.

13. Compound characterized by the structural formula (I)

in which a is a C=O or CH2;
In represents an optionally substituted C1-6alkyl, substituents independently selected from-NH2, -OH, -NHC1-6of alkyl, -N(C1-6alkyl)2, -NH-C3-6cycloalkyl, 4-6 membered saturated heterocycle containing nitrogen as heteroatom;
D represents O or N, where substituted with one R8and where N is substituted by one or more R8and when n is 0 and m is not equal to 0, R8directly attached to B;
R1and R2in combination with the carbon atoms to which they are attached, form an optionally substituted isooxazolyl condensed with the pyrimidine ring, which is optionally substituted by 1 Deputy, which represents a C1-6alkyl;
R3present is employed, a phenyl, optionally substituted with halogen;
R4and R5represent H;
R6and R7independently selected from H or unsubstituted C1-6of alkyl;
R8independently selected from H, unsubstituted C1-6the alkyl, unsubstituted With3-7cycloalkyl or unsubstituted 4-6 membered heterocycle, where N is a heteroatom;
R9represents phenyl, optionally substituted by 1 or 2 substituents, where the substituents independently selected from C1-6of alkyl, -OC1-6of alkyl, halogen, or naphthyl;
or its pharmaceutically acceptable salt.

14. The compound or its pharmaceutically acceptable salt of formula (I) according to item 13, selected from:
N-(3-Aminopropyl)-N-{1-[5-(4-terbisil)-3-methyl-4-oxo-4,5-dihydroisoxazole[5,4-d]pyrimidine-6-yl]-2-methylpropyl}-4-methylbenzamide;
N-(3-Aminopropyl)-3-fluoro-N-{1-[5-(4-terbisil)-3-methyl-4-oxo-4,5-dihydroisoxazole[5,4-d]pyrimidine-6-yl]-2-methylpropyl}-4-methylbenzamide;
N-(3-Aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydroisoxazole[5,4-d]pyrimidine-6-yl)-2-methylpropyl]-3-fluoro-4-methylbenzamide;
N-(3-Aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydroisoxazole[5,4-d]pyrimidine-6-yl)-2-methylpropyl]-4-methylbenzamide;
N-(3-Aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydroisoxazole[5,4-d]pyrimidine-6-yl)propyl]-4-methylbenzamide;
N-(3-Aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydroisoxazole[5,4-d]pyrimido the-6-yl)propyl]-4-fermentated;
N-(3-Aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydroisoxazole[5,4-d]pyrimidine-6-yl)propyl]-2,3-dichlorobenzamide;
N-(3-Aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydroisoxazole[5,4-d]pyrimidine-6-yl)propyl]-3-fluoro-4-methylbenzamide; and
N-(3-Aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydroisoxazole[5,4-d]pyrimidine-6-yl)propyl]-4-methoxybenzamide.

15. The compound or its pharmaceutically acceptable salt according to any one of claims 1 to 12, having inhibitory activity against HsEg5.

16. The compound or its pharmaceutically acceptable salt according to item 13 or 14, having inhibitory activity against HsEg5.

17. The use of compound or its pharmaceutically acceptable salt according to any one of claims 1 to 12, to obtain drugs having inhibitory action against HsEg5.

18. The use of compound or its pharmaceutically acceptable salt according to item 13 or 14, to obtain drugs having inhibitory action against HsEg5.

19. The method of obtaining inhibitory effect against HsEg5, which includes contacting the specified HsEg5 with an effective amount of the compound or its pharmaceutically acceptable salt according to any one of claims 1 to 12.

20. The method of obtaining inhibitory effect against HsEg5, which includes contacting the specified HsEg5 with an effective amount of a compound or pharmaceutical is acceptable salt according to item 13 or 14.

21. Pharmaceutical composition comprising as active ingredient a compound according to any one of claims 1 to 12 or its pharmaceutically acceptable salt having inhibitory action against HsEg5, together with at least one pharmaceutically acceptable carrier, diluent or excipient.

22. Pharmaceutical composition comprising as active ingredient the compound according to item 13 or 14 or its pharmaceutically acceptable salt having inhibitory action against HsEg5, together with at least one pharmaceutically acceptable carrier, diluent or excipient.



 

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6 cl, 4 tbl, 106 ex

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23 cl, 13 dwg, 11 tbl, 26 ex

FIELD: chemistry.

SUBSTANCE: invention is related to the compound of general formula 1 or its tautomer or pharmaceutically acceptable salt, where W selected from N and CR4; X is selected from CH(R8), O, S, N(R8), C(=O), C(=O)O, C(=O)N(R8), OC(=O), N(R8)C(=O), C(R8)-CH and C(=R8); G1 - bicyclic or tricyclic condensed derivative of azepin, selected from general formulas 2-9 , or derivative of aniline of common formula 10 , where A1, A4, A7 and A10 are independently selected from CH2, C=O, O and NR10; A2, A3, A9, A11, A13, A14, A15, A19 and A20 are independently selected from CH and N; or A5 stands for covalent connection, and A6 represents S; or A5 stands for N=CH, and A6 represents covalent connection; A8 , A12 , A18 and A21 are independently selected from CH=CH, NH, NCH3 and S; A16 and A17 both represent CH2, or one from A16 and A17 represents CH2, and the one another is selected from C=O, CH(OH), CF2, O, SOc and NR10; Y is selected from CH=CH or S; R1 and R2 are independently selected from H, F, Cl, Br, alkyl, CF3 and group O-alkyl; R3 is selected from H and alkyl; R4-R7 are independently selected from H, F, Cl, Br, alkyl, CF3, OH and group O-alkyl; R8 is selected from H, (CH2)bR9 and (C=O)(CH2)bR9; R9 is selected from H, alkyl, possibly substituted aryl, possibly substituted heteroaryl, OH, groups O-alkyl, OC(=O)alkyl, NH2, NHalkyl, N(alkyl)2, CHO, CO2H, CO2alkyl, CONH2, CONHalkyl, CON(alkyl)2 and CN; R10 is selected from H, alkyl, group COalkyl and (CH2)dOH; R11 is selected from alkyl, (CH2)dAr, (CH2)dOH, (CH2)dNH2, group (CH2)aCOOalkyl, (CH2)dCOOH and (CH2)dOAr; R12 and R13 are independently selected from H, alkyl, F, CI, Br, CH(OCH3)2, CHF2, CF3, groups COOalkyl, CONHalkyl, (CH2)dNHCH2Ar, CON(alkyl)2, CHO, COOH, (CH2)dOH, (CH2)dNH2, N(alkyl)2, CONH(CH2)dAr and Ar; Ar is selected from possibly substituted heterocycles or possibly substituted phenyl; a is selected from 1, 2 and 3; b is selected from 1, 2, 3 and 4; c is selected from 0, 1 and 2; and d is selected from 0, 1, 2 and 3. Besides, the invention is related to pharmaceutical compound and to method for activation of vasopressin receptors of type 2.

EFFECT: compounds according to invention represent agonists of receptor of vasopressin V2, which stipulates for their application (another object of invention) for preparation of medicine for treatment of condition selected from polyuria, including polyuria, which is due to central diabetes insipidus, nocturnal enuresis of nocturnal polyurea, for control of enuresis, to postpone bladder emptying and for treatment of disorders related to bleeds.

21 cl, 228 ex

FIELD: medicine.

SUBSTANCE: invention offers analogues of quinazoline of the formula I

where A is bound at least with one of atoms of carbon in position 6 or 7 of the dicyclic ring; X represents N. A represents the group Q or Z including tautomeric group Z form where Q and Z, have the formulas resulted more low in which symbols and radicals, have the value specified in item 1 of the formula of the invention. R1 represents phenyl, substituted -(G)nOAr or -O(G)nAr and where phenyl is unessentially replaced by halogen or C1-C10alkyl; where G represents C1-C4alkylene, n is peer 0 or 1. And Ar represents phenyl either pyridyl or thiazolyl where Ar is unessentially substituted by 1-2 substituents chosen from halogen or C1-C10alkyl; R2 and R3 represent N. The bonds of the formula I are inhibitors of the receptor tyrosine kinases of type 1. The invention includes also a way of treatment of hyperproliferative diseases, such as a cancer, application of bonds of the formula 1 in manufacture of medical products and pharmaceutical composition on the basis of these bonds.

EFFECT: rising of efficiency of a composition and the method of treatment.

14 cl, 6 dwg, 63 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to new annelated azaheterocyclic amides, including a pyrimidine fragment, with the general formula 1, method of obtaining them and their application in the form of free bases or their pharmaceutically accepted salts as inhibitors of P13K kinase, in compounds with the general formula 1: , where: X represents an oxygen atom, sulphur atom or not necessarily substituted at the nitrogen NH group, where the substitute is selected from lower alkyls and possibly a substituted aryl; Y represents an atom of nitrogen or substituted at the carbon atom CH group, where the substitute is selected from lower alkyls; Z represents an oxygen atom; R1 represents a hydrogen atom or not necessarily substituted C1-C6alkyl, or Z represents a nitrogen atom, which is together with a carbon atom, with which it is joined, form through Z and R1 annelated imidazole cycle; R2 and R3 independently from each other represent hydrogen, not necessarily substituted with C1-C6alkyl, C3-C6cycloalkyl, not necessarily substituted with phenyl, not necessarily substituted with 6-member aza-heteroaryl, under the condition, when Y represents a nitrogen atom, or R2 and R3 independently from each other represent not necessarily substituted C1-C6alkyl, not necessarily substituted with phenyl, not necessarily substituted with 5-7-member heterocycle with 1-2 heteroatoms, selected from nitrogen and oxygen, and possibly annelated with a phenyl ring, under the condition, when Y does not necessarily represent a substituted carbon atom at the CH group, and X represents an oxygen atom, sulphur atom, or R2 represents hydrogen, and R3 represents a substituted aminoC1-C6alkyl and not necessarily substituted 5-6-member aza-heterocycloalkyl, under the condition, when Y represents a group which is substituted at the CH atom, and X represents an oxygen atom, sulphur atom, or R2 represents hydrogen, and R3 represents phenyl which is not necessarily substituted, pyridyl which is not necessarily substituted, pyrimidinyl which is not necessarily substituted, under the conditions, when R1 represents a substituted aminoC1-C6alkyl, substituted C2-C3hydroxyalkyl and aza-heterocycloalkyl not necessarily substituted, Y represents a group with CH substituted, and X represents an oxygen atom, sulphur, and the substitute of the above indicated substituted alkyl, phenyl, heterocycle, pyridyl, pyrimidyl are selected from groups of hydroxyl-, cyano-groups, hydrogen, lower alkyls, possibly mono- or di-substituted lower alkyl sulfamoyl, carbamoyl, C1-C6alkoxycarbonyl, amino, mono- or di-lower alkyl-amine, N-(lower alkyl), N-(phenylC1-C6alkyl)amine, phenyl, possibly substituted with a halogen atom, C1-C6alkyl, haloid-C1-C6alkyl; phenylC1-C6alkyl, saturated or non-saturated 5-6-member heterocycle containing 1-2-heteroatoms, selected from nitrogen, oxygen and sulphur, and possible condensation with a benzene ring R4 represents hydrogen or a lower alkyl.

EFFECT: obtaining new annelated aza-heterocyclic amides, including a pyrimidine fragment, with the general formula with the possibility of their application in the form of free bases or their pharmaceutically accepted salts as inhibitors of PI3K kinase.

16 cl, 5 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: novel chemical compounds of formula (I) or their pharmaceutically acceptable salts possess inhibiting activity with respect to kinase p-38 MAP and kinase FGFR, and can be used in treatment of such diseases as arthritis, obstructive lung disease, Alzheimer's disease or oncological and other diseases. In general formula (I) , R1 is hydrogen, R2 is 6-member oxygen-containing heterocyclyl, aryl, selected from unsubstituted phenyl or phenyl substituted with aliphatic acyl group which contains 1-6 carbon atoms, halogen cyano, hydroxyl, C1-6alkylsulfinyl, C1-6alkylsulfonyloxy, C1-6alkylsulfonyl, C1-6alkylsulfanyl, tret-butydimethylsilanyloxy, 6-member heterocyclyl, containing 1-2-heteroatoms, selected from nitrogen and oxygen, R3 is C1-6alkyl, Ar1 is phenyl, substituted with 1-2 substituents, selected from atoms of halogen, C1-6alkyl, C1-6alkoxy, C1-6alkylamino, di(C1-6alkyl)amino, X1 is oxygen and X2 is chemical bond.

EFFECT: efficient application of invention compounds in pharmaceutical composition.

13 cl, 1 tbl, 64 ex

FIELD: chemistry.

SUBSTANCE: claimed are novel pyrazole derivatives of formula II or its pharmaceutically acceptable salts, where C ring is selected from phenyl or pyridinyl ring and R2, R2', Rx and Ry are such as said in given description. C ring has ortho-substituent and is optionally substituted in non-ortho positions. R2 and R2' , optionally taken with their intermediate atoms, form condensed ring system, such s indazole ring, and Rx and Ry, optionally taken together with their intermediate atoms, form condensed ring system, such a quinazoline ring.

EFFECT: possibility to use compositions as inhibitors of protein kinases as inhibitors GSK-3 and other kinases and apply them for protein kinase-mediated diseases.

41 cl, 8 tbl, 423 ex

FIELD: chemistry.

SUBSTANCE: invention relates to application of the substituted esters of 1,2,3,7-tetrahydro-pyrrolo [3,2-f][1,3]benzoxazine-5-carboxylic acid of general formula 1 or their racemoids, or their pharmaceutically acceptable and/or hydrates as substances of pharmaceutical compositions having anti-influenza virus activity: , where: R1 and R4 independently represent amines substitute selected from hydrogen, optionally substituted by liner or branched alkyl, containing 3-12 carbon atoms, optionally substituted cycloalkyl containing 3-10 carbon atoms, optionally substituted aryl, and probably, annelated heterocyclyl, which can be aromatic or non-aromatic and contains from 3 to 10 atoms in the ring, with one or several heteroatoms selected from nitrogen, oxygen or sulphur or their oxides; R2 represents alkyl substitute selected from hydrogen, optionally substituted mercapto group, optionally substituted amino group, optionally substituted hydroxyl; R3 represents lower alkyl; R5 represents substitute of the cyclic system selected from hydrogen, optionally substituted linear or branched alkyl, containing 3-12 carbon atoms, optionally substituted cycloalkyl containing 3-10 carbon atoms optionally substituted aryl or optionally substituted and optionally substituted annelated heterocyclyl, which can be aromatic or non-aromatic and contains from 3 to 10 atoms in the ring with one or several heteroatoms selected from nitrogen, hydrogen or sulphur or their oxides; R6 represents substitute of cyclic system selected from hydrogen, halogen atom, cyano group, optionally substituted aryl or optionally substituted annelated heterocycle, which can be aromatic or non-aromatic and contains from 3 to 10 atoms in the ring with one or several heteroatoms selected from nitrogen, hydrogen or sulphur or their oxides.

EFFECT: production of the pharmaceutical compositions having anti-influenza virus activity.

12 cl, 2 dwg, 2 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention pertains to non-peptide antagonists GnRH, with general formula 1 , where each of A1, A2 and A3 are independently chosen from A5 and A6; and A4 represents either a covalent bond, or A5; under the condition that, if A4 is a covalent bond, then one of A1-A3 represent A6, and the other two represent A5, and that, if A4 represents A5, then all of A1-A3 represent A5; A5 is chosen from C-R13 and N; A6 is chosen from N-R14, S and O; R1 is chosen from H, NHY1 and COY2, and R2 represents H; or and R1, and R2 represents methyl or together represent =O; each of R3, R4 and R5 independently represents H or low alkyl; each of R6, R7, R8, R9, R10, R11 and R12 are independently chosen from H, NH2, F, CI, Br, O-alkyl and CH2NMe2; R13 is chosen from H, F, CI, Br, NO2, NH2, OH, Me, Et, OMe and NMe2; R14 is chosen from H, methyl and ethyl; W is chosen from CH and N; X is chosen from CH2, O and NH; Y1 is chosen from CO-low alkyl, CO(CH2)bY3, CO(CH2)bCOY3 and CO(CH2)bNHCOY3; Y2 is chosen from OR15, NRI6R17 and NH(CH2)cCOY3; Y3 is chosen from alkyl, OR15 and NR16R17; R15 represents H; each of R16 and R17 is independently chosen from H, low alkyl and (CH2)aR18, or together represent -(CH2)2-Z-(CH2)2-; R18 is chosen from OH, pyridyl, pyrizinyl and oxadiazolyl; Z represents NH; a represents 0-4; and b and c represent 1-3. The invention also relates to use of formula 1 a compound as a therapeutic agent and pharmaceutical composition, with antagonistic effect to GnRH receptor. Description is also given of the method of obtaining compounds with the given formula.

EFFECT: obtaining new compounds, with useful biological properties.

27 cl, 70 ex

FIELD: chemistry.

SUBSTANCE: invention relates to new compounds of the formula (1a) or its pharmaceutically acceptable salt, esters or imides where A is a thiophenyl group containing, probably, substitution, the thiophenyl group A containing, probably, substitution with one or several groups as follows: alkyl, halo or arylalkyl, Y is O, S or NR2 where R2 is hydrogen or alkyl group containing 1 to 6 carbon atoms, and R1 is an non-ramified alkyl group containing 6 to 25 carbon atoms, ramified alkyl group containing 6 to 25 carbon atoms, aryl alkyl group where the alkyl group contains 2 to 25 carbon atoms or phenyl group containing substitution with one or several groups as follows: phenyloxy, phenylthio, SO2-phenyl, alkylphenyl, CO-phenyl, CONR16- phenyl, NR16CO-phenyl or NR16 -phenyl containing, probably, substitution where R16 is hydrogen or alkyl group containing 1 to 4 carbon atoms, the groups phenyloxy, phenylthio, SO2-phenyl, alkylphenyl, CO-phenyl, CONR-phenyl or NR-phenyl containing, probably, substitution with one or several groups as follows: halo, alkyl, alkylhalo or phenyl group containing substitution with one or several groups or alkyl groups provided the above compound is not 5-methyl-2-(4-metoxyphenyl)amino-4H-thieno[2,3-d][1,3]oxazine-4-on, 6-amyl-2-(4-chlorophenyl)amino-4H-thieno[2,3-d][1,3]oxazine-4-on or 6-amyl-2-(4-metoxyphenyl)amino-4H-thieno[2,3-d][1,3]oxazine-4-on Invention also relates to method of obtaining compounds of the formula (Ia) or (IIa), to pharmaceutical compound and application, as well as cosmetic technique.

EFFECT: obtaining of new biologically active compounds and pharmaceutical compounds based on them.

27 cl, 4 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to a new derivative of sulfonamide substituted imidazoquinolines, and specifically to N-{2-[4-amino-2-(ethoxymethyl)-1H-imidazo-[4,5-c]-qunolin-1-yl]-1,1-dimethylethyl}-methanesulfonamide and its pharmaceutically acceptable salts, as well as to a pharmaceutical composition based on this compound.

EFFECT: invention also relates to a method of inducing biosynthesis of cytokines in an animal organism and methods of treating viral and oncological diseases in animals using said compound and pharmaceutical composition based on said compound.

5 cl, 1 tbl, 39 ex

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