PYRROLOTRIAZINE DERIVATIVES AS KINASE INHIBITOR Russian patent published in 2020 - IPC C07D487/04 C07D519/00 A61K31/53 

Abstract RU 2726632 C1

FIELD: chemistry.

SUBSTANCE: present invention relates to a compound of chemical formula 1, having inhibitory activity on janus-kinase (JAK3) and Bruton tyrosine kinase (BTK), or a pharmaceutically acceptable salt thereof. In one embodiment, in chemical formula 1, X is O; A is a ring selected from a group consisting of benzothiazole, isothiazole, isoxazole, pyrazole, pyrrole, thiazole, thiophene and 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine; R1 denotes hydrogen; C1-4 alkyl, unsubstituted or substituted with one substitute selected from a group consisting of C1-4 alkoxy and N(C1-4 alkyl)2; C1-4 alkoxy; C1-4 haloalkyl; C3-6 cycloalkyl; N(C1-4 alkyl)2; pyrazolyl unsubstituted or substituted with one or two C1-4 alkyl groups; or , where Y1 is NH, N(C1-4 alkyl) or O; Y2 is CH or N; L is a bond, C1-4 alkylene or CO; R2 denotes hydrogen, C1-4 alkyl or halogen, and R3 is C1-4 alkyl substituted with halogen; C2-4 alkenyl unsubstituted or substituted with halogen; or C2-4 alkynyl. In another embodiment in chemical formula 1 X is O; A is a ring selected from the group consisting of benzene and pyridine; R1 denotes hydrogen; C1-4 alkyl, unsubstituted or substituted with one substitute selected from a group consisting of C1-4 alkoxy and N (C1-4 alkyl)2 ; C1-4 alkoxy; C1-4 haloalkyl; C3-6 cycloalkyl; N(C1-4 alkyl)2; pyrazolyl unsubstituted or substituted with one or two C1-4 alkyl groups; or , where Y1 is NH, N (C1-4 alkyl) or O; Y2 is CH or N; L is a bond, C1-4 alkylene or CO; R2 is halogen, and R3 is C1-4 alkyl substituted with halogen; C2-4 alkenyl unsubstituted or substituted with halogen; or C2-4 alkynyl. Present invention also refers to a pharmaceutical composition containing said compounds or their pharmaceutically acceptable salts.

[chemical formula 1].

EFFECT: pharmaceutical composition can be used for preventing or treating an inflammatory disease, an autoimmune disease, a proliferative disease, a hyperproliferative disease, an immuno-mediated disease, cancer or tumour.

9 cl, 1 tbl, 50 ex

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RU 2 726 632 C1

Authors

Kim, In Woo

Yoo, Ja Kyung

Kim, Ji Duck

Jun, Sun Ah

Lee, Jun Hee

Dates

2020-07-15Published

2018-03-19Filed