5-5 CONDENSED RINGS AS C5a INHIBITORS Russian patent published in 2022 - IPC C07D487/04 A61K31/4162 A61K31/4439 A61P37/02 

FIELD: organic chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, namely to a heterocyclic compound of the formula (I) or its pharmaceutically acceptable salt, where a cycle element A¹ is selected from a group consisting of N and CH; a cycle elements A² is selected from a group consisting of N, CH, and C(R⁴); each of cycle elements A³, A⁴, A⁵, and A⁶ is independently selected from a group consisting of CH and C(R⁴); each of dotted lines is independently a simple or double bond; R¹ is selected from a group consisting of -C_1-8alkylene-heteroaryl, -C₁ alkylene-C₆ aryl, C_1-8 alkyl, -C(O)-C_1-8 alkyl, -C(O)-C₆ aryl, -C(O)-heteroaryl, -C(O)-C_3-6 cycloalkyl, -C(O)NR^1aR^1b, SO₂-C₆ aryl, -C(O)-C₁ alkylene-O-C₆ aryl, -C(O)-C_1-3 alkylene-C_3-6 cycloalkyl, and -CO₂R^1a; the heteroaryl group is a 5-6-element aromatic ring containing 1-2 heteroatoms as cycle elements, selected from N and O; where R^1a and R^1b each independently is selected from a group consisting of a hydrogen atom and C_1-8 alkyl; where R¹ is optionally substituted with 1-2 substitutes R⁵; R^2a and R^2e each is C_1-6 alkyl; R^2b, R^2c, and R^2d each is a hydrogen atom; each R³ is C_1-6 alkyl; each R⁴ is independently selected from a group consisting of C_1-6 alkyl, C_1-6 alkoxy group, C_1-6 hydroxyalkyl, halogen, cyano group, and -CO₂R^4a; each R^4a is a hydrogen atom; each R⁵ is independently selected from a group consisting of C_1-8 alkyl, C_1-8 haloalkyl, C_1-8 hydroxyalkyl, C_3-6 cycloalkyl, halogen, OH, -NR^5aR^5b, -NR^5aC(O)₂R^5b, and CO₂R^5a; where each R^5a and R^5b is independently selected from a group consisting of a hydrogen atom and C_1-8 alkyl; and subscript n is 0, 1, or 2. The invention also relates to a pharmaceutical composition based on a compound of the formula (I) or its pharmaceutically acceptable salt and to a method for the treatment of the specified diseases with a compound of the formula (I), or its salt, or a composition based on it.

EFFECT: C5a receptor modulators are obtained, useful in the treatment of diseases with pathological activation of C5a.

28 cl, 3 tbl, 13 ex