PRODRUGS OF CONJUGATED BICYCLIC C5aR ANTAGONISTS Russian patent published in 2023 - IPC C07D471/04 C07D487/04 A61K31/4162 A61K31/506 A61K31/675 C07F9/6561 C07K5/06 C07K5/08 A61P1/00 A61P3/00 A61P7/00 A61P9/00 A61P11/00 A61P13/00 A61P17/00 A61P19/02 A61P21/04 A61P25/00 A61P27/02 A61P29/00 A61P35/00 A61P37/06 

FIELD: pharmaceutical chemistry.

SUBSTANCE: group of inventions includes compounds of formulas (IB), (IC), (IIA) or (IIB) or their pharmaceutically acceptable salts, a pharmaceutical composition and a treatment method based on them. In formulas (IB), (IC), (IIA) or (IIB), cycle term a is C(R^2c), cycle term b is C(R^2d) and cycle term e is C(R^2e); X¹ is selected from the group consisting of bond and C_1-8 alkylene; R¹ is selected from the following: a) a 6-membered heteroaryl containing as ring(s) vertices 1-4 heteroatoms selected from N, O and S; b) C_6-10 aryl; the -X¹-R¹ group is unsubstituted or substituted with 1-5 R^x substituents; R^2a and R^2e are each independent C_1-6 alkyl; R^2b, R^2c and R^2d each independently represents a hydrogen atom; each R³ is C_1-4 alkyl; R⁴ is -NHC(O)NHP¹; each R⁵ is halogen; R^5' is a hydrogen atom; R⁶ is selected from the group consisting of C_1-6 alkoxy and halo; R⁷ is P¹ ; and R⁸ is -CH₂OP¹; each P¹ is a prodrug component; each R^x is independently selected from the group consisting of halo, CN, C_1-4 alkyl, C_1-4 alkoxy, C_1-4 haloalkyl, C_1-4 haloalkoxy, C_1-4 hydroxyalkyl, C_2-4 alkenyl, C_3-6 cycloalkyl, CO₂-C_1-4 alkyl and CONH₂; subscript m is 0, 1, 2, 3, or 4; and subscript n is 0, 1, 2, or 3; where P¹ is selected from the groups indicated in the claims.

EFFECT: technical result: compounds of formulas (IB), (IC), (IIA) or (IIB) with inhibitory activity against C5aR.

14 cl, 2 dwg, 1 tbl, 65 ex