Aminopyrimidines and pyridines

FIELD: organic chemistry.

SUBSTANCE: invention relates to new compounds of general formula I , wherein one from V or X is N and another is CRa or both V and X are CRa (each CRa is independently hydrogen atom); Y is O, S; Z is N(R2)(R3); R1 is hydrogen, C1-C10-alkyl, C3-C7-cycloalkyl, etc.; R4 is hydrogen, C1-C6-alkyl, C3-C7-cycloalkyl, etc.; A is hydrogen, C1-C10-alkyl, halo-C1-C6-alkyl, etc.; B is optionally substituted 5-membered aromatic ring containing at least one nitrogen atom and 0-3 additional heteroatoms; U is -NR5; meanings of the rest substituents are as defined in specification, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical composition and intermediates of formula I.

EFFECT: new biologically active compounds and pharmaceutical compositions based on the same having inhibition activity in relates to IKK-β enzyme.

26 cl, 13 ex

 

The text descriptions are listed faxing

1. The compound of formula (I):

in which one of V or X is N and the other means CRa/sub> or both V and X mean CRa(in which each of Raindependently represents hydrogen);

Y represents O, S;

Z represents N(R2)(R3);

R1represents hydrogen, (C1-C10)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6) alkyl, (C1-C10)heteroalkyl, heterocyclyl, heterocyclyl(C1-C6)alkyl or (C1-C6) alkylen-C(O)R11;

R11represents hydrogen or NR12R13(in which R12and R13independently represent a (C1-C6)alkyl);

R2and R3represent hydrogen;

R4represents hydrogen, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl;

the fragment represents a hydrogen, (C1-C10)alkyl, halogen(C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, (C1-C10)heteroalkyl, heterocyclyl, heterocyclyl (C1-C6) alkyl, heterothermy (C3-C7)cycloalkyl, aryl, aryl(C1-C4)alkyl, aryl(C1-C4)heteroalkyl, heteroaryl, heteroaryl(C1-C4)alkyl, heteroaryl 1-C4)heteroalkyl or RaRbNC(=X)-, in which Raand Rbindependently represent aryl, X represents S;

the fragment represents a substituted or unsubstituted five-membered aromatic ring containing at least one nitrogen atom and 0 to 3 additional heteroatoms and substituents in the ring selected from the group consisting of (C1-C6)alkyl;

U represents-NR5-;

R5represents hydrogen;

and pharmaceutically acceptable salts of this compound;

where "heteroalkyl" means the radical (C1-C6)alkyl, substituted with one, two or three substituents, independently selected from-ORa, -NRbRcand-S(O)nRd(in which n is 0, 1 or 2); this assumes that heteroalkyl radical attached via a carbon atom included in this heteroalkyl radical, and Rarepresents hydrogen, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, Rbrepresents hydrogen, Rcrepresents hydrogen or-S(O)nR' (where n is 0, 1 or 2; and in which R' represents aryl); Rdrepresents hydrogen (provided that n is 0), (C1-C6)alkyl, (C3 -C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl;

"heteroaryl" means a monovalent monocyclic or bicyclic radical, containing from 5 to 12 atoms in the ring and containing at least one aromatic ring containing one, two or three heteroatoms selected from N, O or S, with the remaining atoms in the ring are With, it is assumed that the heteroaryl radical is attached via atom included in the aromatic ring and heteroaryl ring is optionally substituted independently with one to four substituents selected from (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, nitro, hydroxy, amino, mono-(C1-C6)alkylamino, di(C1-C6)alkylamino;

"heterocyclyl" means a saturated or unsaturated non-aromatic cyclic radical containing from 3 to 8 atoms in the ring, in which one or two atoms belonging to the ring are heteroatoms selected from O, NR (where R independently represents hydrogen, C1-C6)alkyl or any of the substituents listed below), or S(O)n(in which n is 0, 1 or 2), and the remaining atoms in the ring are C; one or two atoms may be neo is Astelin replaced by a carbonyl group, and the ring - heterocyclyl may be optionally substituted independently with one, two or three substituents selected from (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, aryl(C1-C6)alkyl, halogen, nitro, cyano, cyano(C1-C6)alkyl, (C1-C6)alkoxy, -(CR'R")n-COR (where n denotes an integer from 0 to 5, R' and R" independently represent hydrogen, R represents a (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl), -(CR'R")n-COOR (n means an integer from 0 to 5, R' and R" independently represent a(C1-C6)alkyl, and R is a (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl), -(CR'R")n-C(=Q)NRaRb(in which Q represents O or S, n means an integer from 0 to 5, R' and R" independently represent hydrogen or (C1-C6)alkyl, and Raand Rbindependently from each other, represent hydrogen, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl), or -(CR'R")n1-S(O)nRd(where n1 denotes an integer from 0 to 5, Rdmeans hydrogen (when the service is provided that n is 0), (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, amino, mono(C1-C6)alkylamino, di(C1-C6)alkylamino and n is 0, 1 or 2);

"aryl" means a monovalent monocyclic or bicyclic aromatic hydrocarbon radical containing from 6 to 10 atoms in the ring, which is optionally independently substituted by one to four substituents selected from (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, cyano, cyano(C1-C6)alkyl, hydroxy, (C1-C6)alkoxy, acylamino, halogen(C1-C6)alkyl, (C1-C6)heteroalkyl, COR (where R represents hydrogen, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl), -S(O)n-Rd(in which n is 0, 1 or 2, and when n is 0, Rdis a (C1-C6)alkyl, (C3-C7)cycloalkyl or (C3-C7)cycloalkyl(C1-C6)alkyl, and when n is 1 or 2, Rdis a (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl, amino, mono(C1-C6)alkylamino or the and(C 1-C6)alkylamino), -NS(O)2Rf(in which Rfmeans (C1-C6)alkyl),-NHCORe(in which Remeans amino, (C1-C6)alkylamino, di(C1-C6)alkylamino or (C1-C4)alkoxy), -(CR'R")n-COOR (where n denotes an integer from 0 to 5, R' and R" independently represent hydrogen or (C1-C6)alkyl, and R is a (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl), -(CR'R")n-CONRaRb(in which n means an integer from 0 to 5, R' and R" independently represent hydrogen or (C1-C6)alkyl, and Raand Rbindependently of one another represent hydrogen, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl);

"acyl" means a group-C(O)R'in which R' represents a (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl;

"heterothermy cycloalkyl" means a group (C3-C7)cycloalkyl, in which one, two or three hydrogen atoms are replaced by substituents, independently selected from the group consisting of cyano, cyanomethyl, hydroxy, hydroxymethyl, (C1-C6)alkoxy, acylamino, -SO nR (in which n is 0, 1 or 2 and when n is 0, R is a hydrogen or (C1-C6)alkyl, and when n is 1 or 2, R is a (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl, amino, mono-(C1-C6) alkylamino, di(C1-C6) alkylamino) or-NHSO2R, in which R represents -(C1-C6)alkyl.

2. The compound according to claim 1, according to which a represents a hydrogen, (C1-C10)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, (C1-C10)heteroalkyl, heterocyclyl, heterocyclyl(C1-C6)alkyl, heterothermy(C3-C7)cycloalkyl, aryl, aryl(C1-C4)alkyl, aryl(C1-C4)heteroalkyl, heteroaryl, heteroaryl(C1-C4)alkyl or heteroaryl(C1-C4)heteroalkyl;

where "aryl" means a monovalent monocyclic or bicyclic aromatic hydrocarbon radical containing from 6 to 10 atoms in the ring, which is optionally independently substituted by one to four substituents selected from (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, cyano, cyano(C1-C6)alkyl, hydroxy, (C1-C6)alkoxy, acylamino, halogen(C1-C6)alkyl, (C1-C6)heteroalkyl, COR (in this definition, R is hydrogen, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl), -S(O)n-Rd(in which n is 0, 1 or 2, and when n is 0, Rdis a (C1-C6)alkyl, (C3-C7)cycloalkyl or (C3-C7)cycloalkyl(C1-C6)alkyl, and when n is 1 or 2, Rdis a (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl, amino, mono(C1-C6)alkylamino or di(C1-C6)alkylamino), -(CR'R")n-COOR (where n denotes an integer from 0 to 5, R' and R" independently represent hydrogen or (C1-C6)alkyl, and R is a (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C6)alkyl), or -(CR'R")n-CONRaRb(in which n means an integer from 0 to 5, R' and R" independently represent hydrogen or (C1-C6)alkyl, and Raand Rbindependently of one another represent hydrogen, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7cycloalkyl(C 1-C6)alkyl);

"heteroalkyl" means (C1-C6)alkyl radical, substituted by one, two or three substituents, independently selected from-ORa, -NRbRcand-S(O)nRd(in which n is 0, 1 or 2); this assumes that heteroalkyl radical attached via a carbon atom included in this heteroalkyl radical, and Rarepresents hydrogen, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, Rbrepresents hydrogen, Rcrepresents hydrogen, Rdrepresents hydrogen (provided that n is 0), (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl;

"heterothermy cycloalkyl" means (C3-C7)cycloalkyl group in which one, two or three hydrogen atoms are replaced by substituents, independently selected from the group consisting of cyano, hydroxy, (C1-C6)alkoxy, acylamino, -SOnR (in which n is 0, 1 or 2, and when n is 0, R is a hydrogen or a (C1-C6) alkyl, and when n is 1 or 2, R is a (C1-C6) alkyl, (C3-C7) cycloalkyl, (C3-C7) cycloalkyl(C1-the 6) alkyl, amino, mono-(C1-C6) alkylamino, di(C1-C6) alkylamino).

3. The compound according to claim 1 or 2, according to which V denotes N, X is CH.

4. The compound according to claim 3, according to which Y represents O or S.

5. The compound according to claim 3, according to which R4means hydrogen.

6. The compound according to claim 3, whereby the fragment contains a nitrogen atom in position at a distance of two atoms from the atom through which the fragment is attached to the rest of the molecule.

7. The compound according to claim 3, whereby the fragment is substituted or unsubstituted imidazolyl, substituted or unsubstituted thiazolyl or substituted or unsubstituted triazolyl.

8. The compound according to claim 3, whereby the fragment represents a 1-Mei-5-yl, 5-Mei-1-yl, thiazol-5-yl, imidazol-1-yl or 4-methyl-1,2,4-triazole-3-yl.

9. The compound according to claim 3, whereby U represents-NH-.

10. The compound according to claim 3, according to which Z denotes N(R2)(R3).

11. The compound according to claim 3, according to which Z signifies NH2.

12. The compound according to claim 3, according to which Y represents S.

13. The compound according to claim 3, according to which R1means (C1-C10)alkyl, (C1-C10)heteroalkyl, heterocyclyl(C1-C6)alkyl or (C1-C6)alkylen-C(O)R11.

14. With the unity according to claim 3, in which the fragment And means (C1-C10)alkyl, (C3-C7)cycloalkyl, (C1-C10)heteroalkyl, heterocyclyl, heterocyclyl(C1-C6)alkyl, heterothermy (C3-C7)cycloalkyl, aryl, aryl(C1-C4)alkyl or heteroaryl.

15. The compound according to claim 1 or 2, according to which V denotes CH and X is N.

16. The connection 15 in which Y represents O or S; Z signifies NH2; U represents NH.

17. The connection indicated in paragraph 15, in which the fragment And means (C1-C10)alkyl, (C3-C7)cycloalkyl, (C1-C10)heteroalkyl, heterocyclyl, heterocyclyl(C1-C6)alkyl, heterothermy(C3-C7)cycloalkyl, aryl, aryl(C1-C4)alkyl or heteroaryl.

18. The connection indicated in paragraph 15, in which R1is a (C1-C10)alkyl, (C1-C10)heteroalkyl, heterocyclyl(C1-C6)alkyl or (C1-C6)alkylen-C(O)R11.

19. The connection 15, which fragment contains the nitrogen atom in position at a distance of two atoms from the atom through which the fragment is attached to the rest of the molecule.

20. The connection indicated in paragraph 15, in which the fragment is substituted or unsubstituted imidazolyl, substituted or unsubstituted thiazolyl or substituted or unsubstituted three what sollom.

21. The compound according to claim 2, which is a

2-(tetrahydropyran-4-ylmethyl)-(2-cyclopropylamino-6-(3-methyl-3H-imidazol-4-yl)pyrimidine-4-carbaldehyde)thiosemicarbazone; or

2-methyl-(2-tert-butylamino-6-(3-methyl-3H-imidazol-4-yl)pyrimidine-4-carbaldehyde)thiosemicarbazone; or

2-(tetrahydropyran-4-ylmethyl)-(2-(1-methanesulfonamido-4-ylamino)-6-(3-methyl-3H-imidazol-4-yl)pyrimidine-4-carbaldehyde) thiosemicarbazone; or

2-methyl-(2-cyclopropylamino-6-(3-methyl-3H-imidazol-4-yl)pyrimidine-4-carbaldehyde)thiosemicarbazone; or

2-methyl-(2-(2-TRANS-acetonitrile-cyclopropylamino)-6-(3-methyl-3H-imidazol-4-yl)pyrimidine-4-carbaldehyde)thiosemicarbazone; or

2-methyl-(2-(4-N-methylcarbamoyl)-6-(3-methyl-3H-imidazol-4-yl)-pyrimidine-4-carbaldehyde)thiosemicarbazone; or

2-methyl-(2-[3-(1-hydroxy-ethyl)-phenylamino]-6-(3-methyl-3H-imidazol-4-yl)-pyrimidine-4-carbaldehyde of thiosemicarbazone.

22. Composition, inhibiting the enzyme IKK-βcomprising a therapeutically effective amount of a compound according to any one of claims 1 to 20, or a salt of this compound, and a filler.

23. The compound according to any one of claims 1 to 21 or a salt of this compound intended for use as therapeutically active substances with inhibitory activity against the enzyme IKK-β.

24. Connection item 23, in which combinatii with a second therapeutic agent, selected from the group consisting of prednisone, dexamethasone, beclomethasone, methylprednisone, betamethasone, hydrocortisone, methotrexate, cyclosporine, rapamycin, tacrolimus, antihistamines drugs, TNF (tumor necrosis factor) antibodies, IL-1 (interleukin) antibodies, soluble TNF receptors, soluble IL-1 receptor antagonists to TNF or IL-1 receptors, non-steroidal anti-inflammatory agents, MOR-2 (cyclooxygenase) inhibitors, antidiabetic agents, and anticancer agents.

25. The compound of the formula:

in which one of V or X is N and the other means-CRaor both V and X mean-CRa(in which each of Raindependently represents hydrogen);

R4means hydrogen, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-alkyl;

fragment a represents hydrogen, (C1-C10)alkyl, halogen(C1-C6)alkyl, (C1-C10)heteroalkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, heterocyclyl, heterocyclyl(C1-C6)alkyl, heterothermy(C3-C7)cycloalkyl, aryl, aryl(C1-C4)alkyl, aryl(C1-C4)heteroalkyl, heteroaryl, heteroaryl(C1-C 4)alkyl, heteroaryl(C1-C4)heteroalkyl or RaRbNC(=X)-, in which Raand Rbindependently represent aryl, and X is S;

the fragment represents a substituted or unsubstituted five-membered aromatic ring containing at least one nitrogen atom and 0 to 3 additional heteroatoms and substituents of the ring are selected from the group consisting of (C1-C6)alkyl;

U represents-NR5-;

R5means hydrogen.

26. Connection A.25, according to which V denotes N, and X is CH; R4means hydrogen; fragment And means (C1-C10)alkyl, (C3-C7)cycloalkyl, (C1-C10)heteroalkyl, heterocyclyl, heterocyclyl(C1-C6)alkyl, heterothermy (C3-C7)cycloalkyl, aryl, aryl(C1-C4)alkyl or heteroaryl; fragment b is a substituted or unsubstituted imidazolyl, substituted or unsubstituted thiazolyl or substituted or unsubstituted triazolyl; U represents NH.



 

Same patents:

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to compounds of the general formula (I): wherein R1 means hydrogen atom or lower alkyl; R2 means lower alkyl, -(CH2)n-O-lower alkyl, -(C3-C6)-cycloalkyl or -(CH2)n-NR'2 wherein R' means hydrogen atom, lower alkyl or -(CH2)n-O-lower alkyl independently of one another for R'2; or R'2 in common with nitrogen atom can form pyrrolidine ring, and wherein n = 1, 2 or 3. Also, invention relates to a pharmaceutical composition possessing antagonistic activity with respect to A2 receptors and containing one or some compounds of the general formula (I) and its pharmaceutically acceptable excipients. Invention provides synthesis of compound of the general formula (I) possessing antagonistic activity with respect to A2 receptors.

EFFECT: valuable medicinal property of compounds and pharmaceutical composition.

11 cl, 19 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel polycyclic compounds of the formula (I): wherein radicals and symbols have values given in the invention claim. Compounds of the formula (I) possess properties of H3 receptors antagonist. Also, invention relates to a pharmaceutical composition containing compounds of the formula (I). Also, invention relates to a method for treatment of disease of group comprising difficulty in nasal breath, obesity, somnolence, narcolepsy, attention deficiency with hyperactivity, Alzheimer's disease and schizophrenia that involves using compounds of the formula (I) and, optionally, in combination of H receptor antagonist.

EFFECT: valuable medicinal properties of compound and pharmaceutical composition.

39 cl, 3 tbl, 31 ex

FIELD: organic chemistry, medicine, biochemistry, pharmacy.

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EFFECT: valuable medicinal and biochemical properties of compounds and pharmaceutical composition.

19 cl, 22 ex

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EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

10 cl, 1 tbl, 276 ex

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EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

16 cl, 100 ex

FIELD: organic chemistry, pharmacy.

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EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

8 cl, 6 tbl, 83 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of nicotine- or isonicotine-benzothiazole of general formulas (IA) and (IB) their pharmaceutically acceptable acid-additive salts and a medicinal agent based on thereof. In compounds of general formula (IA) and (IB) R1 means phenyl, piperidine-1-yl or morpholine; A means -O-; R means -(CH2)n-N(R'')-C(O)-lower alkyl, -(CH2)n-O-lower alkyl, -(CH2)n-O-(CH2)n-O-lower alkyl, lower alkyl, -(CH2)n-morpholinyl, -(CH2)n-phenyl, -(CH2)n-N(R''), -(CH2)n-pyridinyl, -(CH2)n-CF3, -(CH2)n-2-oxopyrrolidinyl or (C4-C6)-cycloalkyl; R'' mean(s) independently of one another hydrogen atom or lower alkyl; n= 1 or 2; A means -N(R')-; R means lower alkyl, (C4-C6)-cycloalkyl, -(CH2)n-O-lower alkyl, -(CH2)n-pyridinyl, -(CH2)n-piperidinyl, -(CH2)n-phenyl, -(CH2)n-N(R'')-C(O)-lower alkyl, -(CH2)n-morpholinyl or -(CH2)n-N(R'')2; R' and R'' mean independently of one another hydrogen atom or lower alkyl; n = 1 or 2; or A means -CH2-; R means -N(R'')-(CH2)m-O-lower alkyl, -N(R'')2, S-lower alkyl, or R means azethidinyl, pyrrolidinyl or piperidinyl that are substituted optionally with hydroxy-group or lower alkoxy-group; or R means morpholinyl, -N(R'')-(CH2)m-(C4-C6)-cycloalkyl, -N(R'')-(CH2)m-C(O)-O-lower alkyl, -O-(CH2)m-O-lower alkyl or alkoxy-group; R'' mean(s) independently of one another hydrogen atom or lower alkyl; m = 1, 2 or 3; or A means -S-; R means lower alkyl, or A-R mean in common piperazinyl substituted with alkyl, -C(O)-lower alkyl or oxo-group, or group A-R means piperidinyl substituted with lower alkoxy-group or hydroxy-group, or group A-R means morpholinyl substituted with lower alkyl, or group A-R means (C4-C6)-cycloalkyl, azethidine-1-yl optionally substituted with hydroxy-group or lower alkoxy-group, or group A-R means thiomorpholinyl-1,1-dioxo-group, tetrahydropyrane or 2-oxa-5-azabicyclo[2.2.1]hept-5-yl. Proposed compounds can be used in treatment of diseases mediated by adenosine A2A-receptors, for example, Alzheimer disease, some depressive states, toxicomania and Parkinson's disease.

EFFECT: valuable medicinal properties of compounds and agent.

37 cl, 10 sch, 109 ex

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to compound represented by the structural formula: or its pharmaceutically acceptable salt wherein Z represents -(CH2)n-; double dotted line represents a double bond; n = 0-2; R1 and R2 are chosen independently from the group comprising hydrogen atom (H), alkyl with 1-6 carbon atoms; R3 means H, hydroxy-, alkoxy-group with 1-6 carbon atoms, -C(O)OR17 or alkyl with 1-6 carbon atoms; Het means monocyclic heteroaromatic group consisting of 6 atoms and comprising 5 carbon atoms and one heteroatom chosen from nitrogen atom (N) and wherein Het is bound through ring carbon atom and wherein Het-group has one substitute W chosen independently from the group comprising bromine atom (Br), heterocycloalkyl representing group consisting of 4 carbon atoms and one heteroatom chosen from N; heterocycloalkyl representing group consisting of 4 carbon atoms and one heteroatom chosen from N substituted with OH-substituted alkyl with 1-6 carbon atoms or =O; R21 -aryl-NH-; -C(=NOR17)R18; R21-aryl; R41-heteroaryl representing group consisting of 5-6 atoms comprising 3-5 carbon atoms and 1-4 heteroatoms chosen independently from the group: N, S and O; R8 and R10 are chosen independently from group comprising R1; R9 means H; R11 is chosen from group comprising R1 and -CH2OBn wherein Bn means benzyl; B means -(CH2)n4CR12=CR12a(CH2)n5; n4 and n5 mean independently 0; R12 and R12a are chosen independently from group comprising H, alkyl with 1-6 carbon atoms; X means -O-; Y means =O; R15 is absent as far as double dotted line mean a simple bond; R16 means lower alkyl with 1-6 carbon atoms; R17 and R18 are chosen independently from group comprising H, alkyl with 1-6 carbon atoms; R21 means 1-3 substituted chosen independently from group comprising hydrogen atom, -CN, -CF3, halogen atom, alkyl with 1-6 carbon atoms and so on; R22 is chosen independently from group comprising hydrogen atom; R24-alkyl with 1-10 carbon atoms; R25-aryl and so on; R23 is chosen independently from group comprising hydrogen atom, R24-alkyl with 1-10 carbon atoms, R25-aryl and -CH2OBn; R24 means 1-3 substitutes chosen independently from group comprising hydrogen atom, halogen atom, -OH, alkoxy-group with 1-6 carbon atoms; R25 means hydrogen atom; R41 means 1-4 substitutes chosen independently from group comprising hydrogen atom, alkyl with 1-6 carbon atoms and so on. Also, invention relates to a pharmaceutical composition possessing the inhibitory activity with respect to receptors activated by protease and comprising the effective dose of derivative of nor-seco-chimbacine of the formula (I) and a pharmaceutically acceptable excipient. Also, invention relates to methods for inhibition of thrombin and cannabinoid receptors comprising administration in mammal derivative of nor-seco-chimbacine of the formula (I) in the effective dose as active substance. Invention provides derivatives of nor-seco-chimbacine as antagonists of thrombin receptors.

EFFECT: valuable medicinal and biological properties of compounds and pharmaceutical composition.

8 cl, 1 tbl, 18 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention elates to derivatives of benzothiazole of the general formula (I): wherein R means hydrogen atom, -(CH2)n-phenyl optionally substituted with a substitute chosen from the following group: halogen atom, (lower)-alkyl, (lower)-alkoxy-group, trifluoromethyl or -N(R')-C(O)-(lower)-alkyl, -(CH2)n-pyridinyl optionally substituted with (lower)-alkyl, -(CH2)n-(C3-C6)-cycloalkyl optionally substituted with hydroxy-group, -(CH2)n-benzo[1,3]dioxolyl, -(CR'2)-thiophenyl, -(CR'2)n-thiazolyl optionally substituted with (lower)-alkyl, -(CH2)n-C(O)-thiophenyl optionally substituted with halogen atom, -(CH2)-furanyl optionally substituted with (lower)-alkyl, -(CHR')n-benzofuran-1-yl, -(CH2)n-benzo[b]thiophenyl, -(CH2)n-N(R')-C(O)-phenyl optionally substituted with halogen atom or (lower)-alkoxy-group. -(CH2)n-C(O)-phenyl optionally substituted with (lower)-alkoxy-group, -(CH2)n-C(O)-2,3-dihydrobenzo[1,4]dioxine-6-yl, -(CH2)n-N(R')-C(O)-pyridinyl, -(CH2)n-tetrahydrofuranyl, -CH-biphenyl, -CH-(phenyl)pyridinyl, -(CH2)n-1-oxo-(CH2)n-CH-(phenyl)tetrahydropyranyl, -(CH2)n-1-oxo-1,2,3,4-tetrahydroquinoline-3-yl or -(CH2)n-S-[1,3,4]thiadiazol-2-yl optionally substituted with amino-group; R' means hydrogen atom or (lower)-alkyl and independently of one another in case R'2; n = 0, 1, 2, 3 or 4. Also, invention relates to a medicament possessing high affinity to adenosine A2A-receptors and high selectivity with respect to A1-receptors and comprising one or more derivatives of benzothiazole of the formula (I) and pharmaceutically acceptable excipients. Invention provides using derivatives of benzothiazole as ligands of adenosine receptors.

EFFECT: valuable medicinal properties of compounds and medicament.

13 cl, 2 tbl, 3 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel derivatives of 2-oxo-1-pyrrolidine of the formula (I) or their pharmaceutically acceptable salts wherein X means -CA1NR5R6 or -CA1-R8 wherein A1 and A2 mean independently oxygen atom; R1 means hydrogen atom (H), (C1-C20)-alkyl, (C6-C10)-aryl or -CH2-R1a wherein R1a means (C6-C10)-aryl; R3 means H, -NO2, nitrooxy-group, C≡N, azido-group, -COOH, amido-group, (C1-C20)-alkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl, (C6-C10)-aryl, thiazolyl, oxazolyl, furyl, thienyl, pyrrolyl, tetrazolyl, pyrimidinyl, triazolyl, pyridinyl, -COOR11, -COR11 wherein R11 means (C1-C12)-alkyl; R3a means H, (C1-C20)-alkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl or (C6-C10)-aryl; R5 and R6 are similar or different and each means independently H, (C1-C6)-alkyl, and R8 means -OH and wherein each alkyl can be substituted independently with from 1 to 5 substitutes chosen from halogen atom, isothiocyanate, -OH, -NO2, -CN, azido-group, (C3-C6)-cycloalkyl and (C6-C10)-aryl;, and wherein each (C6-C10)-aryl can be substituted independently with from 1 to 5 substitutes chosen from halogen atom, -NH2, -NO2, azido-group, (C1-C6)-alkoxy-group, (C1-C6)-alkyl and (C1-C6)-halogenalkyl, and wherein each alkenyl can be substituted independently with at least one substitute chosen from halogen atom and -OH, and under condition that at least one radical among R and R3a differs from H, and when compound represent a mixture of possible isomers then X means -CONR5R6; A2 means oxygen atom, and R1 means H, -CH3, -C2H5, -C3H7, and when each R1 and R3a means H and A2 means oxygen atom and X means -CONR5R6 then R3 differs from -COOH, -CH, -COOR11, amido-group, naphthyl, phenyl rings substituted with (C1-C6)-alkoxy-group or halogen atom in para-position in naphthyl or phenyl ring. Compounds of the formula (I) can be used in pharmaceutical compositions for treatment of epilepsy, epileptogenesis, convulsions, epileptic seizures, essential tremor and neuropathic pain.

EFFECT: improved method of synthesis, valuable medicinal properties of derivatives and pharmaceutical compositions.

27 cl, 3 tbl, 9 ex

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to compounds of the general formula (I): wherein R1 means hydrogen atom or lower alkyl; R2 means lower alkyl, -(CH2)n-O-lower alkyl, -(C3-C6)-cycloalkyl or -(CH2)n-NR'2 wherein R' means hydrogen atom, lower alkyl or -(CH2)n-O-lower alkyl independently of one another for R'2; or R'2 in common with nitrogen atom can form pyrrolidine ring, and wherein n = 1, 2 or 3. Also, invention relates to a pharmaceutical composition possessing antagonistic activity with respect to A2 receptors and containing one or some compounds of the general formula (I) and its pharmaceutically acceptable excipients. Invention provides synthesis of compound of the general formula (I) possessing antagonistic activity with respect to A2 receptors.

EFFECT: valuable medicinal property of compounds and pharmaceutical composition.

11 cl, 19 ex

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to an improved method for synthesis of 2-(3',5'-diamino-1',2',4'-triazol-1'-yl)-4-R1-5-R2-1,3-thiazoles of the general formula (I): , wherein R1 represents hydrogen atom (H), direct or branched (C1-C4)-alkyl or COO-(C1-C4)-alkyl or phenyl optionally substituted with one or some substitutes chosen from halogen atom; R2 represents H, direct or branched (C1-C4)-alkyl, COO-(C1-C4)-alkyl. Method for synthesis involves addition to aqueous solution of 4-R1-5-R2-1-hydrazino-1,3-thiazole hydrochloride of the formula (II): , wherein R1 and R2 have above given values of N-cyanoguanidine of the formula (III): in the mole ratio (II) : (III) = (1.10-1.20):100. Prepared mixture is heated at temperature 80-95°C followed by its neutralization, filtering off and recrystallization. Method provides preparing 2-(3',5'-diamino-1',2',4'-triazol-1'-yl)-4-R1-5-R2-1,3-thiazole from inexpensive and available raw and without using complex technological procedures. Synthesized compounds can be used in synthesis of medicinal and biologically active substances.

EFFECT: improved method of synthesis.

10 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivative compound of carboxylic acid represented by the formula (I): , wherein each X and Y represents independently (C1-C4)-alkylene; Z means -O-; each R1, R2, R3 and R4 means independently hydrogen atom or (C1-C8)-alkyl; R5 means (C2-C8)-alkenyl; A means -O- or -S-; D means D1, D2, D3, D4 or D5 wherein D1 means (C1-C8)-alkyl; D2 means compound of the formula: wherein ring 1 represents saturated 6-membered monoheteroaryl comprising one nitrogen atom and, optionally, another one heteroatom chosen from oxygen, sulfur and nitrogen atoms; D3 means compound of the formula: wherein ring 2 represents (1) completely saturated (C3-C10)-monocarboxylic aryl, or (2) optionally saturated 5-membered monoheteroaryl comprising 3 atoms chosen from nitrogen and sulfur atoms, or completely saturated 6-membered monoheteroaryl comprising 1 heteroatom representing oxygen atom; D4 means compound of the formula: ; D5 means compound of the formula: ; R6 represents (1) hydrogen atom, (2) (C1-C8)-alkyl, (3) -NR7R8 wherein R7 or R8 represent hydrogen atom or (C1-C8)-alkyl, or R7 and R8 taken in common with nitrogen atom to which they are added form saturated 5-6-membered monoheteroaryl comprising one nitrogen atom and, optionally, another one heteroatom representing oxygen atom; E means -CH or nitrogen atom; m means a whole number 1-3, or its nontoxic salt. Invention relates to a regulator activated by peroxisome proliferator receptor, agent used in prophylaxis and/or treatment of diseases associated with metabolism disorders, such as diabetes mellitus, obesity, syndrome X, hypercholesterolemia or hyperlipoproteinemia, hyperlipidemia, atherosclerosis, hypertension, diseases coursing with circulation disorder, overeating or heart ischemic disease, and to an agent that increases cholesterol level associated with HDL, reduces cholesterol level associated with LDL and/or VLDL, eliminates risk factor in development of diabetes mellitus and/or syndrome X and comprising a compound represented by the formula (I) or its nontoxic salt as an active component and a carrier, excipient or solvent optionally. Invention proposes derivative compounds of carboxylic acid possessing the modulating activity with respect to peroxisome proliferator receptor (PPAR).

EFFECT: valuable medicinal properties of compounds.

15 cl, 5 tbl, 48 ex

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to novel derivatives of 3-oxo-1-cyclobutene of the general formula (I): and their salts, solvates, hydrates and N-oxides wherein R1 represents group of the formula: Ar1L2Ar2Alk wherein Ar1 represents aromatic or heteroaromatic group; L2 represents a covalent bond or -O-, -NH- or -CONH-; Ar2 represents arylene or heteroarylene group; Alk represents chain -CH2CH(R) or -CH(CH2R)- wherein R represents -CO2H or -COOAlk7 wherein Alk7 represents (C1-C8)-alkyl, (C3-C8)-cycloalkyl, (C3-C8)-heterocycloalkyl group and others; X represents group -N(R2)- wherein R2 represents hydrogen atom or (C1-C6)-alkyl group; V represents oxygen atom; Rx, Ry and Rz represent atom or group -L1(Alk1)n(R3)v wherein L1 represents covalent bond or -O-, -S-, -Se-, -S(O)-, -NH- or -N(CH3)-; Alk1 represents aliphatic group; R3 represents hydrogen, halogen atom, group -OR3a, -SR3a and others wherein R3a represents hydrogen atom, (C1-C6)-alkyl and others; n = 0 or 1; v = 1, 2 or 3 under condition that if n = 0 and L1 represents covalent bond then v = 1; or Rz represents atom or group given above, and Rx and Ry taken together form spiro-bound cycloaliphatic or heterocycloaliphatic group. Compounds of the formula (I) possess inhibitory activity with respect to α4-integrin and can be used in medicine.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

26 cl, 216 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of piperidine of the general formula (I): or their pharmaceutically acceptable salts wherein rings A and B represent optionally substituted benzene rings; R1 represents alkyl, hydroxyl, thiol, carbonyl, sulfinyl, unsubstituted or substituted sulfonyl group and others; R2 represents hydrogen atom, hydroxyl, amino-group, alkyl, unsubstituted or substituted carbonyl group or halogen atom; Z represents oxygen atom or group -N(R3)- wherein R3 and R4 represent hydrogen atom or alkyl group under condition that N-acetyl-1-benzyloxycarbonyl-2-phenyl-4-piperidineamine is excluded. Compounds of the formula (I) or their salts possess antagonistic activity with respect to tachykinin NK1-receptors and can be used in medicine in treatment and prophylaxis of inflammatory, allergic diseases, pain, migraine, diseases of central nervous system, digestive organs and others.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition, improved method of treatment.

18 cl, 138 tbl, 527 ex

Benzothiazoles // 2293736

FIELD: organic chemistry, medicine, pharmacology.

SUBSTANCE: invention relates to compounds of the general formula (I): wherein R1 represents 3,6-dihydro-2H-pyran-4-yl, 5,6-dihydro-4H-pyran-3-yl, 5,6-dihydro-4H-pyran-2-yl, tetrahydropyran-2,3- or 4-yl, cyclohex-1-enyl, cyclohexyl, or it represents 1,2,3,6-tetrahydropyridin-4-yl or piperidin-4-yl that are optionally substituted with -C(O)CH3 or -C(O)OCH3 in position 1 at nitrogen atom (N); R2 represents lower alkyl, piperidin-1-yl substituted with hydroxy-group optionally, or it represents phenyl optionally substituted with -(CH2)n-N(R')-C(O)-(CH2)n-NR'2, -(CH2)n-halogen, lower alkyl or -(CH2)n-N(R')-(CH2)n-O-lower alkyl, or it represents morpholinyl or pyridinyl that is substituted optionally with halogen atom, -N(R')-(CH2)n-O-lower alkyl, lower alkyl, lower alkoxy-group, morpholinyl or -(CH)n-pyrrolidinyl; n = 0, 1 or 2; R' represents hydrogen atom or lower alkyl, and to their pharmaceutically acceptable acid-additive salts. Also, invention relates to a medicament possessing affinity to adenosine A2A-receptors and containing one or some compounds of the general formula (I) and pharmaceutically acceptable excipients.

EFFECT: valuable medicinal properties of compounds.

17 cl, 47 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention elates to derivatives of benzothiazole of the general formula (I): wherein R means hydrogen atom, -(CH2)n-phenyl optionally substituted with a substitute chosen from the following group: halogen atom, (lower)-alkyl, (lower)-alkoxy-group, trifluoromethyl or -N(R')-C(O)-(lower)-alkyl, -(CH2)n-pyridinyl optionally substituted with (lower)-alkyl, -(CH2)n-(C3-C6)-cycloalkyl optionally substituted with hydroxy-group, -(CH2)n-benzo[1,3]dioxolyl, -(CR'2)-thiophenyl, -(CR'2)n-thiazolyl optionally substituted with (lower)-alkyl, -(CH2)n-C(O)-thiophenyl optionally substituted with halogen atom, -(CH2)-furanyl optionally substituted with (lower)-alkyl, -(CHR')n-benzofuran-1-yl, -(CH2)n-benzo[b]thiophenyl, -(CH2)n-N(R')-C(O)-phenyl optionally substituted with halogen atom or (lower)-alkoxy-group. -(CH2)n-C(O)-phenyl optionally substituted with (lower)-alkoxy-group, -(CH2)n-C(O)-2,3-dihydrobenzo[1,4]dioxine-6-yl, -(CH2)n-N(R')-C(O)-pyridinyl, -(CH2)n-tetrahydrofuranyl, -CH-biphenyl, -CH-(phenyl)pyridinyl, -(CH2)n-1-oxo-(CH2)n-CH-(phenyl)tetrahydropyranyl, -(CH2)n-1-oxo-1,2,3,4-tetrahydroquinoline-3-yl or -(CH2)n-S-[1,3,4]thiadiazol-2-yl optionally substituted with amino-group; R' means hydrogen atom or (lower)-alkyl and independently of one another in case R'2; n = 0, 1, 2, 3 or 4. Also, invention relates to a medicament possessing high affinity to adenosine A2A-receptors and high selectivity with respect to A1-receptors and comprising one or more derivatives of benzothiazole of the formula (I) and pharmaceutically acceptable excipients. Invention provides using derivatives of benzothiazole as ligands of adenosine receptors.

EFFECT: valuable medicinal properties of compounds and medicament.

13 cl, 2 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: compound is represented by structural formula

or its pharmaceutically permissible salts, where R1 is the hydrogen atom (1), C1-8acyl(2), hydroxyl (3), halogen atom (5), C2-8acyl (3), C1-8-alcocsy (4), substituted with phenyl or C2-8acyl, substituted with NR2R3; R2R3 independently represent hydrogen atom (1) or C1-8acyl(2), X and Y each independently representing C (1), CH (2) or N (3). is (1) single or (2) double bond. is 5-7-member carbocyclic group or 5-7-member partially or fully saturated heterocyclic group defined in claim 1 of invention. A is one of A1 to A5 groups defined by claim 1 of the invention. The compounds show inhibiting properties relative to poly(ADP-ribose)polymerase are usable as prophylactic and/or curative drugs for treating ischemic diseases (in brain, spinal cord, heart, digestive tract, skeletal muscle, eye retina, e.t.c.), inflammatory diseases (intestinal inflammation, disseminated sclerosis, arthritis, e.t.c.), neurodegenerative disorders (extrapyramidal disorder, Alzheimer disease, muscle dystrophy, cerebrospinal canal stenosis in lumbar segment of the vertebral column, e.t.c.), diabetes, stroke, cerebral injury, hepatic insufficiency, hyperalgesia, e.t.c. The compounds are also of use in struggling against retroviruses (HIV and others), as sensitizing agents for treating cancer cases and immunodepressant agents.

EFFECT: enhanced effectiveness of treatment.

19 cl, 90 tbl

FIELD: organic chemistry, biochemistry, medicine, pharmacy.

SUBSTANCE: invention relates to compounds 2,6-di-tert.-butyl-4-{2-[2-(methylamino)ethyl]-1,3-thiazole-4-yl}phenol, 2,6-di-tert.-butyl-4-[4-(hydroxymethyl)-1,3-oxazole-2-yl]phenol, 4-methylphenyl-2-[4-(1,1-biphenyl-4-yl)-1H-imidazole-2-yl]ethylcarbamate and others or their pharmaceutically acceptable salts. Also, invention relates to using these compounds for preparing a medicinal agent possessing one of the following three activities: inhibition of monoamine oxidases activity, inhibition of lipids peroxidation and modulating activity with respect to sodium channels. Proposed derivatives of thiazole, oxazole or imidazole possess one of the following species of pharmacological activity: inhibition of monoamine oxidases activity, inhibition of lipids peroxidation and modulation of sodium channels.

EFFECT: valuable biochemical and biological properties of derivatives.

34 cl, 119 ex

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to new 2-arylimino-2,3-dihydrothiazole derivatives of formula described in claims having affinity and selectivity to somatostatin receptors and useful as drugs for treatment of pathological conditions or diseases mediated by one or more somatostatin receptors, such as acromegalia, chromophone adenoma, endocrine pancreatic tumor, argentaffinoma syndrome, gastrointestinal hemorrhage, etc.

EFFECT: new agent for treatment of pathological conditions or diseases mediated by somatostatin receptors.

6 cl, 2836 ex

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to alkylated (1H-benzimidazol-5-yl)-(-4-substituted phenyl)-amine derivatives, in particular compound of formula and pharmaceutically acceptable salts or solvates thereof, wherein R1, R2, and R9, are independently hydrogen, halogen, cyano, nitro, trifluoromethyl, difluoromethoxy, trifluorimethoxy, azido, etc.; R7 is optionally substituted C1-C10-alkyl, C3-C10-cycloalkyl, etc.; A is-OR3 or NR4R3; R8 is hydrogen, -Cl, -Br, -F, cyano, nitro, etc.; and meanings of the rest substituents are as defined in specification. Also disclosed is composition for MEK inhibition and uses of benzinidazole compounds.

EFFECT: new compounds with value biological properties.

32 cl, 56 ex

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