SPIROCYCLIC COMPOUNDS Russian patent published in 2021 - IPC C07D471/10 C07D487/10 A61K31/4439 A61K31/444 A61K31/4545 A61K31/496 A61K31/506 A61K31/5377 A61P35/00 

FIELD: pharmacology.

SUBSTANCE: invention relates to a compound of Formula (I) or its pharmacologically acceptable salt, wherein R1 is selected from a group consisting of hydrogen, unsubstituted or substituted monocyclic C_3-8 cycloalkyl, unsubstituted or substituted phenyl,unsubstituted or substituted 5-6-membered monocyclic heterocycle, unsubstituted or substituted 5-6-membered monocyclic heterocyclyl, cyano, unsubstituted C_1-6 haloalkyl, mono-C_1-6 alkyl-substituted amino group, and di-C1-6 alkyl-substituted amino group; Y¹ represents C и R^2a represents hydrogen, Y² represents C and R^2b represents hydrogen; Y³ hydrogen C and R^2c represents hydrogen; each R^3a, each R^3b, R^3c, R^3d, each R^3e, each R^3f, R^3g, R^3h, R³ⁱ and R^3j represents hydrogen; each R^4a and each R^4b independently represents hydrogen or deuterium; each R^5a, R^5b, R^5c, R^5e, R^5f, R^5g and R^5h represents hydrogen; R⁶ represents an unsubstituted or substituted 5-6-membered monocyclic heteroaryl; A¹ is selected from a group consisting of an unsubstituted bridged C_5–10 cycloalkyl, an unsubstituted or substituted phenyl, and an unsubstituted or substituted 6-membered monocyclic heteroaryl; X¹ represents hydrogen or O provided that if X¹ represents hydrogen, then -------is a single bond, and if X1 is an O, then ------- is a double bond; X² represents О or S; Y⁴ represents C(Y^1a), C or N, Y^1a is selected from a group consisting of hydrogen and halogen; -------- is a single or double bond; and if Y⁴ represents C(Y^1a) and -------- is a single bond, then R^5d is selected from a group consisting of hydrogen, and if Y⁴ represents C and -------- is a double bond, then R^5d is missing; and if Y⁴ represents N, then -------- is a single bond, and R^5d is selected from a group consisting of hydrogen; m is 1 or 2; n is 0 or 1and p is 1; the values of other radicals are indicated in the claim. The invention also relates to individual compounds, to methods of alleviating or treating cancer, mediated ERK1 and/or ERK2, to a method of inhibiting replication of malignancy or tumor, to a method of inhibiting the activity of ERK1 and/or ERK2, the use of an effective amount of a compound of the invention in the manufacture of medicines.

EFFECT: new compounds of Formula (I) have been obtained that have inhibitory activity against ERK1 and/or ERK2 and that can be used in the treatment of cancer.

(I)

45 cl, 5 tbl, 62 ex