4-ALKYNYL IMIDAZOLE DERIVATIVE AND MEDICINE COMPRISING SAME AS ACTIVE INGREDIENT Russian patent published in 2018 - IPC C07D233/90 C07D401/06 C07D401/12 C07D403/12 C07D413/12 A61K31/4164 A61K31/4174 A61K31/4178 A61K31/4245 A61K31/4439 A61P17/06 A61P19/00 A61P25/04 A61P29/00 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a 4-alkynyl imidazole derivative represented by general formula (1) or a pharmaceutically acceptable salt thereof. In formula (1), ring A is C₄-C₈cycloalkyl, phenyl optionally substituted with C₁-C₄alkyl group or 6-membered heteroaryl containing one nitrogen atom as a ring atom; ring B is phenyl or 6-membered heteroaryl containing one nitrogen atom as a ring atom; m is an integer having any value from 0 to 1; n is an integer having any value from 1 to 3; R¹ is a C₁-C₄ alkyl group, a halogen atom, C₃-C₈cycloalkyl or C₁-C₄ haloalkyl group; R² and R³, each independently represent a hydrogen atom, a halogen atom or C₁-C₄ alkyl group, or taken together with the carbon atom with which R² and R³ are adjacent, can form C₃-C₆ carbon ring; R⁴ and R⁵, each independently represent a hydrogen atom or C_1-C₄ alkyl group, or taken together with the carbon atom with which R⁴ and R⁵ are adjacent, can form C_3-C₆ carbon ring, and R⁶ and R⁷, each independently represent a hydrogen atom, C_1-C₄ alkyl group, C_1-C₄ alkoxy group, a halogen atom, C_1-C₄ haloalkyl group or C₁-C₄ haloalkoxy group; X is -OR⁸, or a halogen atom; R⁸ is a hydrogen atom or C₁-C₄ alkyl group; Y is a single bond or an oxygen atom; and E is -CO₂H, -CO₂P, which is an alkyl ester or bioisostere of a carboxyl group selected from tetrazolyl or oxadiazolonyl. Invention also relates to a pharmaceutical agent having an antagonistic action against EP4 and an antagonist of an EP4 receptor. (1).

EFFECT: technical result: novel compounds of general formula (1) having an antagonistic effect on EP4, which are useful as pharmaceutical agents for the treatment of diseases associated with the EP4 receptor.

20 cl, 23 tbl, 24 ex