6-5 CONDENSED RINGS AS C5a INHIBITORS Russian patent published in 2022 - IPC C07D487/04 C07D471/04 C07D519/00 A61K31/437 A61K31/497 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 A⁰ is NH; each of cycle elements A¹ and A³ is independently selected from a group consisting of N, CH, and C(R⁴); each of cycle elements A², A⁵, and A⁶ is independently selected from a group consisting of N, CH, and C(R⁴); cycle element A⁴ is selected from a group consisting of N, CH, and C(R⁴); and no more than two of A³, A⁴, A⁵, and A⁶ are N; each of dotted bonds is independently a simple or double bond; R¹ is selected from a group consisting of heteroaryl, phenyl, -C_1-8alkylene-phenyl, C_3-8 cycloalkyl, tetrahydropyranyl, C_1-8 alkyl, -C(O)NR^1aR^1b, and -CO₂R^1a; where the heteroaryl group is a 5-6-element aromatic ring containing 1-3 heteroatoms as cycle elements, selected from N and S; where R^1a and R^1b each independently is selected from a group consisting of a hydrogen atom, C_1-8 alkyl, C_6-10 aryl, and -C_1-6 alkylene-C_6-10 aryl; where R¹ is optionally substituted with 1-3 substitutes R⁵; R^2a and R^2e each independently is selected from a group consisting of C_1-6 alkyl, C_1-6 alkoxy group, and halogen atom; R^2b, R^2c, and R^2d each is a hydrogen atom; subscript n is 0 or 2, and two R³ groups, when present, are combined to form an oxogroup (=O); each R⁴ is independently selected from a group consisting of C_1-6 alkyl, C_1-6 alkoxy group, C_1-6 hydroxyalkyl, halogen, -NR^4aR^4b, -CONR^4aR^4b, and -CO₂R^4a; each R^4a and R^4b is independently selected from a group consisting of a hydrogen atom and C_1-4 alkyl; each R⁵ is independently selected from a group consisting of C_1-8 alkyl, C_1-8 alkoxy group, C_1-8 haloalkyl, C_1-8 haloalkoxy group, C_1-8 hydroxyalkyl, C_3-6 cycloalkyl, halogen, C_2-8 alkenyl, -CONR^5aR^5b, -NR^5aR^5b, -C_1-8 alkylene-NR_5aR_5b, and CO₂R^5a; where each R^5a and R^5b is a hydrogen atom or, when they are attached to the same nitrogen atom, R^5a and R^5b are combined with a nitrogen atom to form a 5-element ring containing 0 additional heteroatoms as cycle elements. 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, 78 ex