NOVEL AMINE DERIVATIVE OR SALT THEREOF Russian patent published in 2018 - IPC C07D209/08 C07D213/80 C07D215/38 C07D217/24 C07D401/06 A61K31/4035 A61K31/4184 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, specifically a heterocyclic compound of formula (1), where G¹, G² and G³ are CH or a nitrogen atom, where at most 2 of G¹, G² and G³ represent a nitrogen atom; R¹ is a chlorine atom, a bromine atom, C_1-3alkyl group, a trifluoromethyl group, a C_3-6cycloalkyl group, a phenyl group or a C₁alkoxy group; R² is -COOR⁵ (where R⁵ represents a hydrogen atom) or -C(O)N(R⁶)SO₂R⁷ (where R⁶ represents a hydrogen atom and R⁷ is C₁alkyl group); R³ is hydrogen atom; and R⁴ is an optionally substituted naphthyl group; an optionally substituted fluorenyl group; optionally substituted with 1 to 2 indolyl groups; a substituted indazolyl group; a substituted tetrahydroquinolyl group; a substituted isoquinolyl group; a substituted dihydroquinazolinyl group; or a substituted dihydrobenzothiazolyl group; an optionally substituted tetrahydrocarbazolyl group; provided that (1) if R⁴ is an optionally substituted condensed naphthyl group, G³ represents a nitrogen atom; and (2) if G¹ is CH, G² is CH, G³ is CH, R¹ is a chlorine atom, C_1-3alkyl group or a trifluoromethyl group, R² is -COOH, and R³ represents a hydrogen atom, then R⁴ represents a group represented by general formulae (2-1)–(2-4), (where X^1aa, X^1ba, X^1ca are the same and are CR^9a (where R^9a represents a hydrogen atom); X^1e represents a nitrogen atom; X^1da is a CR^9a (where R^9a represents a hydrogen atom) or a nitrogen atom; X² is CR¹⁰ (where R¹⁰ represents a hydrogen atom, C₁alkyl group substituted with 1 hydroxyl group) or a nitrogen atom; X³ is a CR¹¹ (where R¹¹ represents a hydrogen atom, a phenyl-C₁alkyl group, a benzoyl group) or a nitrogen atom; X⁴ represents CH₂, CH₂-CH₂ or C=O; X⁵ is CH₂ or C=O; X⁶ represents CH₂, CH₂-CH₂, C=O, NR¹² (where R¹² represents a hydrogen atom, C₁alkyl group), an oxygen atom or a sulphur atom; and R^8a is C₄alkyl group, C₃cycloalkyl group, C_3-6cycloalkyl-C₁alkyl group, an optionally substituted phenyl group, optionally substituted with 1 phenyl-C₁alkyl group, a benzoyl group, a heterocyclic group (selected from pyridinyl, thiazolyl, pyrazinyl, quinolinyl, methylthiopyrimidinyl, methylpyridazinyl) or heterocyclyl-C₁alkyl group (wherein the heterocyclic group is selected from quinolinyl, thiazolyl, pyridinyl); wherein said substituents are disclosed in the claims. Invention also relates to a pharmaceutical composition, a keratin proliferation and TNFα production inhibitor and a compound based on the compound of formula (1). (1) (2-1) (2-2) (2-3) (2-4).

EFFECT: novel heterocyclic compound having a TNFα inhibitory activity is obtained.

1 cl, 3 tbl, 650 ex