ACYLAMINO-SUBSTITUTED DERIVATIVES OF CONDENSED CYCLOPENTACARBOXYLIC ACIDS AND THEIR APPLICATION AS PHARMACEUTICALS Russian patent published in 2014 - IPC C07C235/54 C07C235/84 C07C323/62 C07C323/19 C07D213/64 C07D277/56 C07D333/32 C07D333/80 A61K31/4402 A61K31/38 A61K31/16 A61P9/00 A61P29/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compound of formula (I) , where ring A is cycloalkane ring with number of members from 3 to 7, benzene ring or monocyclic 5-member or 6-member aromatic heterocyclic ring, containing 1 heteromember of ring, selected from the group, containing N and S, and benzene and heterocyclic rings can optionally have one or two similar or different substituents, selected from the group, containing halogen, HO-, R¹-O-, H₂N-C(O)- and NC-; Y is selected from the group, containing S, C(R¹²)=C(R¹³) and C(R¹⁵)=N; Z is selected from the group, containing C(R¹⁶); R¹, R³⁰, R³³, R³⁵, R⁵⁴ and R⁵⁵ independently on each other group R¹, R³⁰, R³³, R³⁵, R⁵⁴ and R⁵⁵ are selected from the group, containing (C₁-C₆)-alkyl, (C₂-C₆)-alkenyl, (C₃-C₇)-cycloalkyl and (C₃-C₇)-cycloalkyl-(C₁-C₄)-alkyl-, and all of them can optionally have one or more similar or different substituents R⁷⁰; R³ and R⁵ represent hydrogen; R⁴ and R⁶ are selected independently on each other, from the group, containing hydrogen and , (C₁-C₄)-alkyl; R¹², R¹³, R¹⁵ and R¹⁶ are selected independently on each other, from the group, containing hydrogen, halogen and O₂N-; R²⁰ is selected from the group, containing hydrogen and (C₁-C₄)-alkyl; one of the groups R²¹ and R²² is group of formula II: R²⁴-R²³-, and the other of groups R²¹ and R²² is selected from the group, containing hydrogen, halogen, R³⁰, HO-, R³⁰-O-, R³⁰-S(O)_m-, H₂N-, R³⁰-NH-, R³⁰-N(R³⁰)-, R³⁰-C(O)- and NC-; R²³ is chain, containing from 1 to 5 chain members of which 0 or 1 chain member is heteromember of chain, selected from the group, containing N(R²⁵), O, S, with other chain members being similar or different groups C(R²⁶)(R²⁶), where two adjacent groups can be bound to each other by double bond; R²⁴ is selected from the group, containing hydrogen, R³¹, R³¹-O-, R³¹-NH-, R³¹-N(R³¹)-, R³¹-C(O)-NH-, HO-C(O)- and monocyclic, bicyclic or tricyclic ring with number of members from 5 to 10, which is saturated or non-saturated and contains 0, 1, 2 or 3 similar or different ring heteromembers, selected from the group, containing N, N(R³²), O, S, and ring can optionally have on ring carbon atoms one or 2-3 similar or different substituents, selected from the group, containing halogen, R³³, R³³-O-, R³³-S(O)_m-, R³³-C(O)-NH-, R³³-S(O)₂-NH-, R³³-C(O)-, HO-C(O)-, H₂N-C(O)-, R³³-NH-C(O)-, R³³-N(R³³)-S(O)²-, NC-, oxo, phenyl and Het; on condition that total number of C, N, O and S atoms, present in two groups R²³ and R²⁴, constitutes not less than 5; R²⁵ is selected from the group, containing hydrogen and (C₁-C₄)-alkyl; R²⁶, independently on each other group R²⁶, is selected from the group, containing hydrogen, fluorine, (C₁-C₄)-alkyl and HO-, or two groups R²⁶, together with included into them chain members, form monocyclic ring with number of members 4, which is saturated and contains 1 ring heteromember, selected from the group, containing O; R³¹ is selected from the group, containing (C₁-C₆)-alkyl, which can optionally have one substituent R⁷⁰; R³² is selected independently on each other, from the group, containing hydrogen, R³⁵ and phenyl; R⁵⁰ is selected from the group, containing R⁵¹-O- and R⁵²-N(R⁵³)-; R⁵¹ is selected from the group, containing hydrogen and R⁵⁴; R⁵² is selected from the group, containing hydrogen; R⁵³ is selected from the group, containing hydrogen; R⁷⁰ is selected from the group, containing HO-, R⁷¹-O-, H₂N-, R⁷¹-NH-, R⁷¹-N(R⁷¹)-, R⁷¹-C(O)-NH-, HO-C(O)-, H₂N-C(O)- and phenyl; R⁷¹, independently on each other group R⁷¹, is selected from the group, containing (C₁-C₄)-alkyl; Het, independently on each other group Het, is monocyclic heterocyclic ring with number of members 5, which contains 1 or 2 similar or different ring heteromembers, selected from the group, containing N and S, and ring is saturated or non-saturated and optionally substituted with one or more similar or different substituents, selected from the group, containing (C₁-C₄)-alkyl; m, independently on each other number m, is integer number, selected from the group, containing 0, 1 and 2; phenyl, independently on each other phenyl group, can optionally have one or more similar or different substituents, selected from the group, containing halogen and (C₁-C₄)-alkyl.

EFFECT: invention also relates to method of obtaining compound of formula (I) and its application for manufacturing pharmaceutical for inhibiting receptor Edg-2.

17 cl, 14 tbl, 362 ex