HETEROCYCLIC ANALOGUES OF PYRIMIDINES AS JAK INHIBITORS Russian patent published in 2015 - IPC C07D403/12 C07D491/10 A61K31/506 A61P29/00 A61P35/00 A61P37/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of structural formula which possesses JAK kinase inhibitory activity. In formula (I), R represents H; F; Cl; CH₃ or CF₃; cycle A represents a 5-merous aromatic heterocycle, wherein Z¹, Z² and Z³ are independently specified in a group consisting of C(R¹); N and N(R¹), provided at least one of Z¹, Z², Z³ represents N or N(R¹); each of R¹ independently represents H, C(O)R²; T¹; C_1-6alkyl; wherein C_1-6alkyl is independently substituted by one or more R³, which are identical or different; R² is specified in T¹; R⁴, R^4a are independently specified in a group consisting of H; T¹; C_1-6alkyl; wherein C_1-6alkyl is optionally substituted by one or more R⁵, which are identical or different; Y⁰ represents (CR^Y3R^Y4)_n; n means 0 or 1; one of the groups R^Y1; R^Y2; R^Y3; R^Y4 represents R^Y0, and others are specified in a group consisting of H and CH₃; X¹ represents C(R^6a) or N; X² means C(R^6b) or N; X³ means CH; X⁴ means C(R^6c); X⁵ means C(R^6d). The T¹, R³, R⁵, R^Y5, R^Y5a, R^6a, R^6b, R^6c, R^6d, R^Y0, T^Y1 radical values are presented in the patent claim.

EFFECT: invention refers to the pharmaceutical composition containing the above compounds, to the compound applicable in the method of treating or preventing an immunological, inflammatory, autoimmune or allergic disorder or disease related to graft rejection, and to the method of treating, controlling, delaying the onset or preventing JAK-related diseases or disorders.

37 cl, 9 tbl