Substituted methyl-amines, serotonin 5-ht6 receptor antagonists, methods of production and use

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted methyl-amines of general formula 1, having serotonin 5-HT6 receptor antagonist properties. In formula 1 , W is naphthalene, indolysin or quinoline; R1 is hydrogen, fluorine, chlorine, methyl; R2 is hydrogen, fluorine, methyl, phenyl, thiophen-2-yl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 is methyl; or W is benzene, R3 assumes the value given above; R1 is 3-Cl, R2 is 3-piperazin-1-yl or 3-(4-methylpiperazin-1-yl); or R1 is hydrogen, R2 is phenyl or pyridyl; or R1 is hydrogen, fluorine, chlorine, methyl; R2 is 4-piperazin-1-yl or 4-(4-methylpiperazin-1-yl); or W is oxazole, R3 is optionally substituted methyl; R1 is chlorine or fluorine, R2 is methyl, or R1 is hydrogen, fluorine, chlorine, methyl; R2 is piperazin-1-yl, 4-methylpiperazin-1-yl, or R1 is chlorine, fluorine or methyl; R2 is furan-2-yl, or R1 is hydrogen, fluorine, chlorine, methyl; R2 is furan-2-yl, R3 is (tetrahydrofuran-2-yl)methyl, or R1 is hydrogen, fluorine, chlorine, methyl; R2 is thiophen-2-yl, R3 is 2-methoxyethyl, or R1 is chlorine or fluorine, R2 is thiophen-2-yl, R3 is methyl.

EFFECT: compounds can be used to treat central nervous system (CNS) diseases, such as psychiatric disorders, schizophrenia, anxiety disorders, as well as for improving mental capacity, for treating obesity or for studying the molecular mechanism of inhibiting serotonin 5-HT6 receptors.

15 cl, 27 dwg, 2 tbl, 25 ex

 

The text descriptions are given in facsimile form.

1. Substituted methyl-amines of General formula 1 may also be in crystalline form or in the form of pharmaceutically acceptable salts,

where W represents a naphthalene, endolysin or quinoline;
R1 represents hydrogen, fluorine, chlorine, methyl;
R2 represents hydrogen, fluorine, methyl, phenyl, thiophene-2-yl, furan-2-yl, pyridyl, piperazine-1-yl or 4-methylpiperazin-1-yl;
R3 represents methyl;
or
W represents a benzene, R3 has the above meaning;
R1 represents a 3-C1, R2 represents 3-piperazine-1-yl or 3-(4-methylpiperazin-1-yl);
or
R1 represents hydrogen,
R2 represents phenyl or pyridyl;
or
R1 presented yet a hydrogen, fluorine, chlorine, methyl;
R2 represents a 4-piperazine-1-yl or 4-(4-methylpiperazin-1-yl);
or
W represents oxazole,
R3 represents an optionally substituted methyl;
R1 represents a chlorine or fluorine,
R2 represents methyl,
or
R1 represents hydrogen, fluorine, chlorine, methyl;
R2 represents piperazine-1-yl, 4-methylpiperazin-1-Il,
or
R1 represents a chlorine, fluorine or methyl;
R2 represents furan-2-yl,
or
R1 represents hydrogen, fluorine, chlorine, methyl;
R2 represents furan-2-yl,
R3 represents (tetrahydrofuran-2-yl)methyl,
or
R1 represents hydrogen, fluorine, chlorine, methyl;
R2 represents thiophene-2-Il,
R3 represents a 2-methoxyethyl, or
R1 represents a chlorine or fluorine,
R2 represents thiophene-2-Il,
R3 represents methyl.

2. Compounds according to claim 1, in which W represents an optionally substituted 1,2-phenylene (1.1); 1,2-naphtaline (1.2.1, 1.2.2, 1.3); 1,2-indolizine (1.4.1, 1.4.2); 3,4-chinoline (1.5 and 1.7), 5,6-chinoline (1.6) or 4,5-oxazole (1.8),



where R1 and R2 have the above value for the corresponding value W.

3. Compounds according to claim 2, in which R1=H, 3-F or 3-C1.

4. Compounds according to claim 3, in which R2 represents hydrogen, methyl, piperazine-1-yl or 4-methylpiperazin-1-yl.

5. Compounds according to claim 1, including:
methyl-[3-piperazine-1-yl-6-(3-chlorophenylsulfonyl)phenyl]-amine 1.1(2),
methyl-[3-(4-methyl-piperazine-1-yl)-6-(3-chlorophenylsulfonyl)phenyl]-amine 1.1(5),

methyl-(4-piperazine-1-yl-6-phenylsulfonyl)-amine 1.1(7),
methyl-[4-piperazine-1-yl-6-(3-chlorophenylsulfonyl)phenyl]-amine 1.1(8),
methyl-[4-piperazine-1-yl-6-(3-perpenicular)phenyl]-amine 1.1(9),
methyl-[4-(4-methylpiperazin-1-yl)-6-phenylsulfonyl)-amine 1.1(10),
methyl-[4-(4-methylpiperazin-1-yl)-6-(3-chlorophenylsulfonyl)phenyl]-amine 1.1(11),
methyl-[4-(4-methylpiperazin-1-yl)-6-(3-perpenicular)phenyl]-amine 1.1(12),

N-methyl-N-[4-(phenylsulfonyl)-1,1'-biphenyl-3-yl]amine 1.1(13),
methyl-(5-pyridin-3-yl-2-phenylsulfonyl)-amine 1.1(14),

methyl-(4-piperazine-1-yl-2-phenolsulfonephthalein-1-yl)-amine 1.2.1(1),
methyl-[4-piperazine-1-yl-2-(3-chlorophenylsulfonyl)naphthalene-1-yl]-amine 1.2.1(2),
methyl-[4-piperazine-1-yl-2-(3-perpenicular)naphthalene-1-yl)-amine 1.2.1(3),
methyl-[4-(4-methylpiperazin-1-yl)-2-phenolsulfonephthalein-1-yl)-amine 1.2.1(),
methyl-[4-(4-methylpiperazin-1-yl)-2-(3-chlorophenylsulfonyl)naphthalene-1-yl)-amine 1.2.1(5),
methyl-[4-(4-methylpiperazin-1-yl)-2-(3-perpenicular)naphthalene-1-yl]-amine 1.2.1(6),

methyl-(5-piperazine-1-yl-2-phenolsulfonephthalein-1-yl)-amine 1.2.2(1),
methyl-[5-piperazine-1-yl-2-(3-chlorophenylsulfonyl)naphthalene-1-yl]-amine 1.2.2(2),
methyl-[5-piperazine-1-yl-2-(3-perpenicular)naphthalene-1-yl]-amine 1.2.2(3),
methyl-[5-(4-methylpiperazin-1-yl)-2-phenolsulfonephthalein-1-yl]-amine 1.2.2(4),
methyl-[5-(4-methylpiperazin-1-yl)-2-(3-chlorophenylsulfonyl)naphthalene-1-yl]-amine 1.2.2(5),
methyl-[5-(4-methylpiperazin-1-yl)-2-(3-perpenicular)naphthalene-1-yl]-amine 1.2.2(6),

methyl-(4-piperazine-1-yl-1-phenolsulfonephthalein-2-yl)-amine 1.3(1),
methyl-[4-piperazine-1-yl-1-(1-chlorophenylsulfonyl)naphthalene-2-yl]-amine 1.3(2),
methyl-[4-piperazine-1-yl-1-(1-perpenicular)naphthalene-2-yl]-amine 1.3(3),
methyl-[4-(4-methylpiperazin-1-yl)-1-phenolsulfonephthalein-2-yl]-amine 1.3(4),
methyl-[4-(4-methylpiperazin-1-yl)-1-(3-chlorophenylsulfonyl)naphthalene-2-yl]-amine 1.3(5),
methyl-[4-(4-methylpiperazin-1-yl)-1-(3-perpenicular)naphthalene-2-yl]-amine 1.3(6),

methyl-(1-phenolsulfonephthalein-2-yl)-amine 1.4.1(1),
methyl-[1-(3-chlorophenylsulfonyl)indolizine-2-yl]-amine 1.4.1(2),
methyl-[1-(3-perpenicular)indolizine-2-yl]-amine 1.4.1(3),
methyl-(3-methyl-1-finals lonelydaisy-2-yl)-amine 1.4.1(4),
methyl-[3-methyl-1-(3-chlorophenylsulfonyl)indolizine-2-yl]-amine 1.4.1(5),
methyl-[3-methyl-1-(3-perpenicular)indolizine-2-yl]-amine 1.4.1(6),
methyl-(3-piperazine-1-yl-1-phenolsulfonephthalein-2-yl)-amine 1.4.1(7),
methyl-[3-piperazine-1-yl-1-(3-chlorophenylsulfonyl)indolizine-2-yl]-amine 1.4.1(8),
methyl-[3-piperazine-1-yl-1-(3-perpenicular)indolizine-2-yl]-amine 1.4.1(9),
methyl-[3-(4-methylpiperazin-1-yl)-1-phenolsulfonephthalein-2-yl]-amine 1.4.1(10),
methyl-[3-(4-methylpiperazin-1-yl)-1-(3-chlorophenylsulfonyl-2-yl]-amine 1.4.1(11),
methyl-[3-(4-methylpiperazin-1-yl)-1-(3-fortuneloungeonlinecasino-2-yl]-amine 1.4.1(12),

methyl-(5-methyl-1-phenolsulfonephthalein-2-yl)-amine 1.4.2(1),
methyl-[5-methyl-1-(3-chlorophenylsulfonyl)indolizine-2-yl]-amine 1.4.2(2),
methyl-[5-methyl-1-(3-perpenicular)indolizine-2-yl]-amine 1.4.2(3),
methyl-(5-piperazine-1-yl-1-phenolsulfonephthalein-2-yl)-amine 1.4.2(4),
methyl-[5-piperazine-1-yl-1-(3-chlorophenylsulfonyl)indolizine-2-yl]-amine 1.4.2(5),
methyl-[5-piperazine-1-yl-1-(3-perpenicular)indolizine-2-yl]-amine 1.4.2(6),
methyl-[5-(4-methylpiperazin-1-yl)-1-phenolsulfonephthalein-2-yl]-amine 1.4.2(7),
methyl-[5-(4-methylpiperazin-1-yl)-1-(3-chlorophenylsulfonyl)indolizine-2-yl]-amine 1.4.2(8),
methyl-[5-(4-methylpiperazin-1-yl)-1-(3-perpenicular)indolizine-2-yl]-amine 1.4.2(9),

methyl-(8-piperazine-1-yl-3-phenylsulfonyl the Olin-4-yl)-amine 1.5(1),
methyl-[8-piperazine-1-yl-3-(3-chlorophenylsulfonyl)quinoline-4-yl]-amine 1.5(2),
methyl-[8-piperazine-1-yl-3-(3-perpenicular)quinoline-4-yl]-amine 1.5(3),
methyl-8[8-(4-methylpiperazin-1-yl)-3-phenylsulfonyl-4-yl]-amine 1.5(4),
methyl-[8-(4-methylpiperazin-1-yl)-3-(3-chlorophenylsulfonyl)quinoline-4-yl]-amine 1.5(5),
methyl-[8-(4-methylpiperazin-1-yl)-3-(3-perpenicular)quinoline-4-yl]-amine 1.5(6),

methyl-(8-piperazine-1-yl-5-phenylsulfonyl-6-yl)-amine 1.6(1),
methyl-[8-piperazine-1-yl-5-(3-chlorophenylsulfonyl)quinoline-6-yl]-amine 1.6(2),
methyl-[8-piperazine-1-yl-5-(3-perpenicular)quinoline-6-yl)-amine 1.6(3),
methyl-[8-(4-methylpiperazin-1-yl)-5-phenylsulfonyl-6-yl]-amine 1.6(4),
methyl-[8-(4-methylpiperazin-1-yl)-5-(3-chlorophenylsulfonyl)quinoline-6-yl]-amine 1.6(5),
methyl-[8-(4-methylpiperazin-1-yl)-5-(3-perpenicular)quinoline-6-yl]-amine 1.6(6),

methyl-(8-piperazine-1-yl-4-phenylsulfonyl-3-yl)-amine 1.7(1),
methyl-[8-piperazine-1-yl-4-(3-chlorophenylsulfonyl)quinoline-3-yl]-amine 1.7(2),
methyl-[8-piperazine-1-yl-4-(3-perpenicular)quinoline-3-yl]-amine 1.7(3),
methyl-[8-methylpiperazin-1-yl)-4-phenylsulfonyl-3-yl]-amine 1.7(4),
methyl-[8-(4-methylpiperazin-1-yl)-4-(3-chlorophenylsulfonyl)quinoline-3-yl]-amine 1.7(5),
methyl-[8-(4-methylpiperazin-1-yl)-4-(3-perpenicular)quinoline-3-yl]-amine 1.7(6),

IU the Il-[2-methyl-4-(3-chlorophenylsulfonyl)oxazol-5-yl]-amine 1.8(2),
methyl-[2-methyl-4-(3-perpenicular)oxazol-5-yl]-amine 1.8(3),
methyl-(2-piperazine-1-yl-4-phenylsulfonylacetate-5-yl)-amine 1.8(4),
methyl-[2-piperazine-1-yl-4-(3-chlorophenylsulfonyl)oxazol-5-yl]-amine 1.8(5),
methyl-[2-piperazine-1-yl-4-(3-perpenicular)oxazol-5-yl]-amine 1.8(6),
methyl-[2-(4-methylpiperazin-1-yl)-4-phenylsulfonylacetate-5-yl]-amine 1.8(7),
methyl-[2-(4-methylpiperazin-1-yl)-4-(3-chlorophenylsulfonyl)oxazol-5-yl]-amine 1.8(8),
methyl-[2-(4-methylpiperazin-1-yl)-4-(3-perpenicular)oxazol-5-yl]-amine 1.8(9),

6. Antagonist of serotonin 5-HT6receptors represents a substituted methyl-amine of General formula 1 may also be in crystalline form or in pharmaceutically acceptable salt according to any one of claims 1 to 5.

7. Active ingredient of pharmaceutical compositions and medicines, representing at least one antagonist of serotonin 5-HT6receptors item 6.

8. Pharmaceutical composition for prevention and treatment of diseases of the Central nervous system, the pathogenesis of which is associated with 5-HT6receptors, including cognitive disorders and neurodegenerative diseases, containing the active ingredient according to claim 7 in a pharmaceutically effective amount.

9. The pharmaceutical composition of claim 8 in the form of tablets, capsules, or injections, placed in pharmaceutically pickup is acceptable package.

10. The pharmaceutical composition of claim 8 or 9 for the prevention and treatment of mental disorders and schizophrenia.

11. The pharmaceutical composition of claim 8 or 9 for the prevention and treatment of anxiety disorders.

12. The pharmaceutical composition of claim 8 or 9 to improve mental abilities.

13. The pharmaceutical composition of claim 8 or 9 for the prevention and treatment of obesity.

14. Method for the prevention and treatment of diseases of the Central nervous system, the pathogenesis of which is associated with 5-HT6receptors, which consists in the introduction to the patient an active component according to claim 7, or pharmaceutical composition according to any one of PP-13.

15. Substituted methyl-amines of General formula 1 according to any one of claims 1 to 5 for studying the molecular mechanism of inhibition of serotonin 5-HT6the receptors.



 

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13 cl, 12 dwg, 459 ex

Antiviral compound // 2441010

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17 cl, 8 dwg, 255 ex

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10 cl, 25 ex

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13 cl, 18 ex, 2 tbl

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indexRR1R2НННIbClННIcClОСН3ОСН3IdСН3ННIeНОСН3Н

, the corresponding 4-[2-(2-nitrophenyl)-1H-indol-3-yl]-but-3-en-2-ones II are boiled in acetic acid in the presence of twenty-fold molar excess of carbonyl iron for 5 minutes.

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1 cl, 4 ex, 2 tbl

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10 cl, ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel diarylamine-containing compounds of formula (I) or formula (4b), pharmaceutically acceptable salts thereof, which have c-kit inhibiting properties. In formulae (I) and (4b), each R1 independently denotes H, -C(O)OH and -L1-C1-6alkyl, where L1 denotes -O- or -C(O)O-, or any two neighbouring R1 groups can together form a 5-6-member heterocyclic ring containing a nitrogen atom or an oxygen atom as a heteroatom, a 6-member heterocyclic ring with one or two nitrogen atom s as heteroatoms, optionally substituted with a C1-4alkyl, and R5 denotes hydrogen or C1-C6alkyl; values of radicals Ar and Q are given in the claim. The invention also relates to a pharmaceutical composition containing said compounds, and a method of treating diseases whose development is promoted by c-kit receptor activity.

EFFECT: more effective use of the compounds.

17 cl, 3 tbl, 9 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to novel antibacterial chinolin derivatives of formula (1a), their stereochemically isomeric forms, N-oxides and pharmaceutically acceptable salts and solvates , where p equals 1; q equals 0, 1, 2, 3 or 4; R1 represents hydrogen, halogen, aryl or Het; R2 represents hydrogen or alkyloxy; R3 represents arylalkyl; each R4 and R5 independently represent hydrogen or alkyl; R7 represents hydrogen, alkyl or aryl; where aryl is selected from phenyl or naphtyl and is optionally substituted with 1, 2 or 3 substituents selected from hydroxy, halogen, cyano, nitro, amino, mono- or dialkylamino, alkyl, C2-6alkenyl, optionally substituted with phenyl, halogenalkyl, alkyloxy, halogenalkyloxy, carboxyl, alkyloxycarbonyl, aminocarbonyl, morpholinyl or mono- or dialkylaminocarbonyl; where Het is selected from furanyl, thienyl, pyridinyl, benzofuranyl, optionally substituted with 1, 2 or 3 substituents selected from halogen, hydroxyl, alkyl or alkyloxy.

EFFECT: compounds can be used for creation of preparations on their base for treatment of bacterial infection

21 cl, 4 ex, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to compounds of formula (IC-2), to their pharmaceutically acceptable salts, N- oxides or solvates. In formula (IC-2) Z represents carbomoyl group, which can be replaced with C1-4 alkyl or hydroxy; R1 represents C1-8 alkyl or C1-8 alkoxy; R4 and R4-1 each independently represent hydrogen atom or C1-8 alkyl; m represents integer number from 1 to 5, when m equals 2 or larger number, all R1 can have same or different values. Invention also relates to compounds, representing 1-({6-[(2-methoxy-4-propylbenzyl)oxy]-1-methyl-3,4-dihydro-2-napthlenyl}methyl)-3-azetidinecarbonic acid, 1-({6-[(4-isobutyl-2-methoxybenzyl)oxy]-1-methyl-3,4-dihydro-2-naphthalinyl}methyl)-3- azetidinecarbonic acid and other, given in formula of claimed invention.

EFFECT: obtaining pharmaceutical composition, which has agonistic activity with respect to EDG-1, EDG-6 and/or EDG-8, containing as active component invention compound, to method of prevention and/or treatment of disease, conditioned by EDG-1, EDG-6 and/or EDG-8 invention compounds, to method of prevention and/or treatment of disseminated sclerosis and method of immune reaction suppression and/or induction of lymphopenia, to application of invention compounds for obtaining medication for prevention and/or treatment of disease, conditioned by EDG-1, EDG-6 and/or EDG-8, to application of compounds for obtaining medication for prevention and/or treatment of disseminated sclerosis, to application of compounds for obtaining immunodepresant and/or medication inducing lymphopenia and to crystal forms of some individual compounds.

17 cl, 10 dwg, 5 tbl, 251 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel derivatives of 2,6-substituted-4-monosubstituted aminopyrimidines of formula (I) or pharmaceutically acceptable salts thereof, which have prostaglandin D2 receptor antagonist properties. In formula R1 is 2,4-dichlorophenyl or 4-trifluoromethoxyphenyl, and when R1 is 2,4-dichlorophenyl, R2 is 3-carboxypyrrolidinyl, 3,5-di-(1-hydroxy-1-methylethyl)phenyl, 3-aminopiperdin-1-yl, 4-aminopiperidin-1-yl, 4-acetamidepiperidin-1-yl, 1-methyl-2-carboxy-2,3-dihydro-1H-indol-5-yl, 3-(1-tert-butylsulphonylaminocarbonyl-1-methylethyl)phenyl, 3-(1-dimethylaminosulphonylaminocarbonyl-1-methylethyl)phenyl, 3-(1-thiomorpholin-4-ylcarbonyl-1-methylethyl)phenyl, 3-(1-aminocarbonyl-1-methylethyl)phenyl, 3-(1-dimethylaminocarbonyl-1-methylethyl)phenyl, 3-carboxymethylpiperidin-1-yl, 3-methylsulphonylaminocarbonylpiperidin-1-yl, 3-ethylsulphonylaminocarbonylpiperidin-1-yl, 3-tert-butylsulphonylaminocarbonylpiperidin-1-yl, 3-trifluoromethylsulphonylaminocarbonylpiperidin-1-yl, 3-[(1H-tetrazol-5-yl)aminocarbonyl]piperidin-1-yl, 3-aminocarbonylpiperidin-1-yl, 3-dimethylaminocarbonylpiperidin-1-yl, 3-dimethylaminosulphonylaminocarbonylpiperidin-1-yl or 2-carboxy-2,3-dihydrobenzofuran-5-yl, and when R1 is 4-trifluoromethoxyphenyl, R2 is 3-(1-methyl-1-carboxyethyl)piperidinyl, 3-carboxypiperidinyl, 3-methylsulphonylaminocarbonylpiperidin-1-yl, 5-carboxythiophen-2-yl. The invention also relates to a pharmaceutical composition containing the said compounds.

EFFECT: high efficiency of using said compounds.

3 cl, 1 tbl, 13 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel benzimidazole derivatives of formula

and pharmaceutically acceptable salts and esters thereof, where R1 denotes C1-10alkyl, lower alkoxy group-lower alkyl, lower alkoxy group-carbonyl-lower alkyl, C3-6cycloalkyl, C3-6cycloalkyl-lower alkyl, phenyl, phenyl-lower alkyl, di(phenyl)-lower alkyl, heterocyclyl, such as piperidinyl, tetrahydropyranyl, 2-oxo-pyrrolidinyl-lower alkyl, where the cycloalkyl, phenyl or heterocyclyl group is optionally substituted with 1-2 substitutes independently selected from a group comprising lower alkyl, lower alkoxy group, lower alkoxy group-carbonyl, morpholinyl, formylamino group and halogen; R2 denotes hydrogen or lower alkyl; R3 denotes lower alkyl, C3-6cycloalkyl, partially unsaturated cyclohexyl, phenyl, phenyl-lower alkyl, pyridinyl, benzodioxolyl, tetrahydropyranyl, where the phenyl group is optionally substituted with 1-2 substitutes independently selected from a group comprising a halogen, lower alkyl, lower alkoxy group, fluoro-lower alkyl, fluoro-lower alkoxy group, N(lower alkyl)2; R4 denotes: a) heteroaryl which is an aromatic 5-6-member monocyclic ring or a 9-10-member bicyclic ring containing 1 or 2 heteroatoms selected from nitrogen, oxygen and/or sulphur, which is optionally substituted with 1-2 substitutes independently selected from a group comprising lower alkyl, phenyl, lower alkoxy group, -N(lower alkyl)2, oxo group, NH2, halogen, cyano group and morpholinyl; b) unsubstituted naphthyl, naphthyl or phenyl, which are substituted with 1-3 substitutes independently selected from a group comprising halogen, hydroxy group, NH2, CN, hydroxy-lower alkyl, lower alkoxy group, lower alkyl-carbonyl, lower alkoxy group-carbonyl, sulphamoyl, di-lower alkyl-sulphamoyl, lower alkyl-sulphonyl, thiophenyl, pyrazolyl, thiadiazolyl, imidazolyl, triazolyl, tetrazolyl, 2-oxopyrrolidinyl, lower alkyl, fluoro-lower alkyl, fluoro-lower alkoxy group, N(lower alkyl)2, carbamoyl, lower alkenyl, benzoyl, phenoxy group and phenyl which is optionally substituted with 1-2 substitutes independently selected from halogen and fluoro-lower alkyl; or c) if R3 denotes cycloalkyl and R1 denotes cycloalkyl, then R4 can also denote phenyl; R5, R6, R7 and R8 independently denote H, halogen, lower alkoxy group or lower alkyl, or R6 and R7, which are bonded to each other, form a 6-member aromatic carbocyclic ring together with carbon atoms to which they are bonded; provided that the compound of formula (I) is not selected from a group comprising butylamide 2-[2-(2-chlorophenyl)benzoimidazol-1-yl]-4-methylpentanoic acid and 2-(2-benzo[1,3]dioxol-5-ylbenzoimidazol-1-yl)-N-benzyl-butyric acid amide. The invention also relates to a pharmaceutical composition based on the formula I compound.

EFFECT: novel benzimidazole derivatives which are useful as farnesoid X receptor antagonists are obtained.

30 cl, 379 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula , where R1 is a 3-7-member carbocyclic ring and n is a number ranging from 1 to 8, and the rest of the radicals are described in the claim.

EFFECT: possibility of using such compounds and compositions in therapy as metabotropic glutamate receptor modulators.

33 cl, 367 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to chemical-pharmaceutical industry. Pharmaceutical compositions including, at least, one compound of formula where -X- represents, for instance, group of formula and Y represents, for instance, group of formula or its pharmaceutically acceptable salts, esters or amides, or pro-drugs and pharmaceutically acceptable carrier, which is acceptable in therapy, can be applied for modulation in vitro and in vivo processes of binding, mediated by binding of E-, P- or L- selectin.

EFFECT: obtaining novel floroglucin derivatives.

9 cl, 10 ex, 3 tbl

FIELD: chemistry.

SUBSTANCE: in formula (I) Cy1 is a 6-member heterocyclyl containing N as a heteroatom, a 5,6-member monocyclic or 9,10-member bicyclic heteroaryl containing 1-3 heteroatoms selected from N, S and O, phenyl or phenyl condensed with a 5-member heterocycle containing O as a heteroatom, each optionally having 1-3 identical or different substituting Cy1 groups which are: (C1-C6)-acyl, cyano, carboxy, hydroxy, (C1-C6)alkylsulphonyl, (C3-C6)-cycloalkyl, a 6-member heterocyclyl containing 1-2 heteroatoms selected from O and N, phenyl, a 5-member heteroaryl containing 1-3 heteroatoms selected from N, S and O, Y1Y2N-, Y1Y2NC(=O)-, Y1Y2NSO2-, (C1-C6)-alkyl-SO2-N(R5)-C(=O)-, R6-C(=O)-N(R5)-, R7-NH-C(=O)-NH-; (C1-C6)-alkoxycarbonyl; (C1-C6)-alkyl, which optionally contains 1-3 identical or different substitutes which are halogen, carboxy, cyano, hydroxy, Y1Y2N-, Y1Y2N-C(=O)-, R6-C(=O)-N(R5)-, R8-SO2-N(R5)-C(=O)-, 5-member heterocyclyl, containing N as a heteroatom, 5-member heteroaryl containing 1-3 heteroatoms selected from N and O; or (C1-C6)-alkoxycarbonyl; as well as (C1-C6)-alkoxy which optionally have 1-3 identical or different substitutes which are carboxy, (C1-C6)-alkoxycarbonyl, cyano, 3-member heterocyclyl containing O as a heteroatom, or 5-member heteroaryl containing 1-3 heteroatoms selected from N and O; where phenyl or heteroaryl fragments in the substituting Cy1 groups optionally and independently have substitutes represented by hydroxy, (C1-C6)-alkyl, (C1-C6)-alkoxy, carboxy, (C1-C6)-alkoxycarbonyl or R8-SO2-N(R5)-C(=O)-; and where cycloalkyl fragments in the substituting Cy1 groups which optionally and independently have substitutes represented by (C1-C6)-alkoxy, carboxy; Cy2 is a 9-member cycloalkenyl, phenyl, 5,6-member monocyclic or 9,10-member bicyclic heteroaryl containing 1-3 heteratoms selected from N, S and O, or phenyl condensed with a 5,6-member heterocycle containing 1-2 heteroatoms selected from N and O, each independently and optionally having 1-3 identical or different substitutes represented by (C1-C6)-alkoxy, (C1-C3)-alkyl, hydroxy, halogen, halogen-(C1-C6)-alkoxy, nitro, Y1Y2N-; L1 is an alkylene with a straight or branched chain containing 1-6 carbon atoms, optionally substituted carboxy; or L1 is -CH2-(C1-C5)halogenalkylene; L2 is a bond, -O- or -CH2-O-. Other values of radicals are given in the formula of invention.

EFFECT: novel compounds have prostaglandin D2 receptor antagonist properties, can be used in treating primarily allergic disorders such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma, food allergy and other diseases.

39 cl, 1 tbl, 99 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel pyrrole derivatives of the formula I: , where R1 and R2 independently denote Ph; mono- or disubstituted in different positions of the ring Ph, where substitute denotes -OCH3; C5-heteroaryl with one heteroatom selected from O or S; R2 denotes H, NO2, NH2, C(O)NH2; R4 denotes H, a straight or branched C1-C6-alkyl; n equals the number of methylene groups and is between 1 and 8 inclusively; X denotes O, S, NH; Y NH, -CH2-; Z denotes O, S; W denotes -OH, hydroxylamine, hydrazine, alkylhydrazine.

EFFECT: compounds can inhibit histone deacetylase, which enables their use in cancer treatment.

10 cl, 9 dwg, 18 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new cyclopenta[b]benzofuranyl derivatives of formula wherein substitutes R1, R2, R3, R4, R5, R6 and R7 and n are specified in the patent clam. These compounds exhibit properties of NF-kB-activity and/or AP-1 inhibitor/modulator. Also, the inventive subject matter are methods for preparing intermediate compounds thereof, a pharmaceutical composition containing them, administration thereof for prevention and/or treatment of inflammatory and autoimmune diseases, neurodegenerative diseases and hyperproliferative diseases caused by NF-kB- and/or AP-1-activity, and a method for prevention and/or treatment of said diseases.

EFFECT: preparation of new cyclopenta[b]benzofuranyl derivatives.

21 cl, 3 tbl, 151 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to compound described by formula where R1 represents a monocyclic nitrogen-containing heterocyclic group optionally condensed with heterocycle with the monocyclic nitrogen-containing heterocyclic group optionally condensed with heterocycle, optionally having 1 to 5 substitutes chosen from a group consisting of (1) halogen atom, (2) cyano, (3) hydroxy, (4) C1-6 alkoxy optionally having 1 to 3 halogen atoms, (5) amino, (6) mono- C1-6 alkylamino, (7) C1-6 alkoxycarbonyl and (8) C1-6 alkyl optionally having 1 to 3 halogen atoms, R2 represents (i) C6-14 aryl group optionally substituted by 1 to 5 substitutes chosen of a group consisting of (1) halogen atom, (2) cyano, (3) C1-6 alkoxy optionally having 1 to 3 halogen atoms, (4) C1-6 alkylthio optionally having 1 to 3 halogen atoms, (5) C1-6alkylcarbonyl, (6) C1-6 alkylsulphonyl, (7) C1-6 alkylthionyl, (8) C3-7 cycloalkyl, (9) C1-6 alkyl group optionally having 1 to 3 halogen atoms, and (10) C1-6 alkyl group substituted by 1 to 3 hydroxy, (ii) a thienyl group optionally substituted by 1 to 4 substitutes chosen from a group consisting of (1) cyano and (2) C1-6 alkyl group optionally having 1 to 3 halogen atoms, (iii) a pyridyl group optionally substituted by 1 to 4 substitutes chosen from a group consisting of (1) halogen atom, (2) 5-10-members aromatic heterocyclic group containing carbon atom, and 1 or 2 presentations of 1-4 heteroatoms chosen from nitrogen atom, sulphur atom and oxygen atom, and (3) C1-6 alkyl group optionally having 1 to 3 halogen atoms, or (iv) a bipyridyl group optionally substituted by 1 to 3 halogen atoms, each R3 and R4 represents hydrogen atom, or one of R3 and R4 represents hydrogen atom, and another represent a lower alkyl group, halogen atom or a cyanogroup, and R5 represents an alkyl group, or to its salt. Also, the invention refers to a pharmaceutical composition showing an acid secretion inhibitory effect enabled by the compound of formula I, to a method for treatment or prevention, besides, to application of the compound of formula I for preparing a pharmaceutical composition for treatment or prevention of a number of diseases presented in the patent claim.

EFFECT: preparation of the new compounds showing the acid secretion inhibitory effect and exhibiting antiulcerant action.

20 cl, 92 ex, 24 tbl

FIELD: chemistry.

SUBSTANCE: present invention refers to new compounds of formula I-9 where q is represented by 1; R11 is represented by C3-8-alkyl; C3-8-cycloalkyl or C3-8-cycloalkyl-C1-3-alkyl; A is represented by phenyl substituted by one or more substituting groups independently chosen from R12; and R12 is represented by -(CH2)-NR13R14; R13 is represented by C1-6-alkylcarbanil; and R14 is represented by hydrogen; and to the pharmaceutically acceptable salts of such compounds and to the pharmaceutical compositions based on such compounds. It has been revealed that the compounds of formula I-9 are histamine NZ-receptor antagonists and thus that they can be used in treatment of diseases connected with expression of such receptors.

EFFECT: compounds of formula I-9 can be used in treatment of diseases connected with expression of histamine NZ-receptors.

6 cl, 216 ex

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