4-PHENYL-5-OXO-1, 4, 5, 6, 7, 8-HEXAHYDROCHINOLINE DERIVATIVES AS MEDICATIONS FOR TREATMENT OF INFERTILITY Russian patent published in 2010 - IPC C07D215/20 C07D401/12 C07D405/12 C07D417/12 A61K31/47 A61K31/4709 A61P5/24 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel derivatives of 4-phenyl-5-oxo-1,4,5,6,7,8-hexahydrochinoline, represented by formula , where R¹ represents (1-6C)alkyl; R² represents halogen, (1-4C)alcoxy; R³ represents OH, NO₂, CN, fluoridated with (1-4C)alkoxy, (1-4C)alkoxy(2-4C)alkoxy. hydroxy(2-4C)alkoxy, (1-4C)alkoxycarbonyl, R⁷, R⁸-amino, R⁹, R¹⁰-amino, R⁹, R¹⁰-aminocarbonyl, R⁹, R¹⁰-aminosulfonyl or phenyl(1-4C)alkoxy, where phenyl ring in composition phenyl(1-4C)alkoxy is optionally substituted with one or several substituents, selected from (1-4C)alkoxy; R⁴ represents R¹¹-phenyl or R¹¹-(4-5C)heteroaryl, which represents heteroaromatic group, containing 4-5 carbon atoms and at least one heteroatom, selected from N and S, where phenyl or heteroaryl group is optionally additionally substituted with one or several substituents, selected from nitro, (1-4C)alkyl, (1-4C)alkoxy; R⁷ represents H, (1-4C)alkyl; R⁸ represents (1-4C)alkylsulfonyl, (1-4C)alkylcarbonyl, (1-4C)alkoxycarbonyl, (1-4C)alkoxy(1-4C)alkylcarbonyl, furylcarbonyl; phenyl(1-4C)alkylcarbonyl, where phenyl ring is optionally substituted with one or several substituents, selected from (1-4C)alkoxy; R⁹ and R¹⁰ are not necessarily selected from H, (1-6C)alkyl and (1-4C)alkoxy(2-4C)alkyl; or R⁹ and R¹⁰ can be bound together with formation of morpholinyl ring; R¹¹ represents H, R¹², R¹³-amino, R¹⁴, R¹⁵-aminocarbonyl or R¹⁴, R¹⁵-aminosulfonyl; R¹² represents H; R¹³ represents (1-4C)alkylsulfonyl, (1-4C)alkylcarbonyl, (1-4C)alkoxycarbonyl or pyperazinyl(1-4C)alkylcarbonyl; R¹⁴ and R¹⁵ are independently selected from H, (1-6C)alkyl, (1-4C)alkoxy(2-4C)alkyl and imidazolyl(1-4C)alkyl; X represents O or R¹⁶-N; Y represents CH₂ or C(O);Z represents CN; R¹⁶ represents H, (1-4C)alkyl, (1-4C)alkylcarbonyl; or their pharmaceutically acceptable salts. Invention also relates to pharmaceutical composition, as well as to application of 4-phenyl-5-oxo-1,4,5,6,7,8-hexahydrochinoline derivatives by any of i.i. 1-10.

EFFECT: obtaining novel biologically active compounds, which possess agonistic activity with respect to FSH receptor.

13 cl, 43 ex