CONDENSED HETEROCYCLIC DERIVATIVE, THERAPEUTIC COMPOSITION WHICH CONTAINS IT AND ITS APPLICATION IN MEDICINE Russian patent published in 2011 - IPC C07D495/04 C07D487/04 A61K31/519 A61K31/55 A61P15/00 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to condensed heterocyclic derivative, represented by formula (I): where ring A represents 5-member monocyclic heteroaryl, containing 1 or 2 heteroatoms, selected from N or S; R^A represents lower alkyl group, optionally substituted with hydroxyl group, COW¹, COOW¹ or CONW²W³, in which W¹-W³ independently represent a hydrogen atom or lower alkyl group; m represents integer 0 or 2; ring B represents benzene ring or thiophene ring; R^B represents halogen atom, cyano group, lower alkyl group or OW⁴, in which W⁴ represents a hydrogen atom or lower alkyl group; n represents integer 0-2; E¹ represents an oxygen atom; E² represents an oxygen atom; U represents a single bond or lower alkelene group; X represents group, represented by Y, -CO-Y, -SO₂-Y, -S-L-Y, -O-L-Y, -CO-L-Y, -SO-L-Y, -SO₂-L-Y, -S-Z or -O-Z, in which L represents a lower alkylene group optionally substituted with halogen or hydroxy group; Y represents group, represented by Z or -NW⁷W⁸, where W⁷ and W⁸ independently represent a hydrogen atom, lower alkyl group or Z on condition that W⁷ and W⁸ are not simultaneously hydrogen atoms, or W⁷ and W⁸ can bind together with adjacent nitrogen atom with formation of cyclic amino group; Z represents cycloalkyl group, optionally condensed with phenyl and optionally substituted with phenyl group, optionally substituted with halogen or alkoxy group; 6-8-member heterocycoalkyl group, which has 1 heteroatom, selected from nitrogen atom or oxygen atom, optionally condensed with phenyl and optionally substituted with phenyl; phenyl group optionally substituted with a substituent, selected from group, consisting of a halogen atom, cyano group, alkyl group, optionally substituted with halogen atom, hydroxy group or alkoxy group, alkoxy group, optionally substituted with halogen atom, hydroxy group, alkoxy group, alkoxy-carbonyl-oxy group or acyloxy group, alkylthio group, carboxy group and alkoxy-carbonyl group; pyridyl; or its pharmaceutically acceptable salt. Invention also relates to pharmaceutical composition possessing antagonistic activity with respect to gonatotropin-releasing hormone, based on the claimed compound.

EFFECT: obtained are novel compounds and based on them pharmaceutical composition, which can be applied in medicine for prevention or treatment of a disease depending on sex hormones, which is selected from group, consisting of benign prostatic hypertrophy, hysteromyoma, endometriosis, premature puberty, prostate cancer, ovarian cancer and breast cancer.

29 cl, 112 tbl, 428 ex