SUBSTITUTED PYRROLO [2,3-D] PYRIDAZIN-4-ONES AND PYRAZOLO [3,4-D] PYRIDAZIN-4-ONES AS PROTEINKINASE INHIBITORS Russian patent published in 2021 - IPC C07D487/04 A61K31/5025 A61P35/00 

Abstract RU 2749038 C2

FIELD: pharmaceutical compounds.

SUBSTANCE: invention relates to a compound of Formula (II) or a pharmaceutically acceptable salt thereof, which can find use as inhibitors of Bruton's tyrosine kinase (BTK). In Formula (II), ring Q1 is selected from aryl and heteroaryl, where aryl and heteroaryl are each unsubstituted or substituted with at least one substituent independently selected from RX, where aryl is phenyl or naphthyl, where heteroaryl is a 5-6 membered aromatic, monocyclic ring containing from 1 to 2 heteroatoms selected from N, with the remaining ring atoms being carbon; ring Q2 is selected from heterocyclyl, where heterocyclyl is a single aliphatic ring with 4-6 ring atoms containing 1 to 2 heteroatoms selected from N; L is selected from -O-, -N(RA1)C(O)- and -C(O)N(RA1)-; W is -C(O)-; Y is selected from N and CR6; R1 is hydrogen; each R2 is hydrogen; R3 is hydrogen; R5 is selected from hydrogen and C1-10 alkyl; R4 is selected from hydrogen, C1-10 alkyl, heterocyclyl or heterocyclyl-C1-4 alkyl, where heterocyclyl is unsubstituted or substituted by at least one substituent independently selected from RX, where heterocyclyl is a single aliphatic ring with 4-5 ring atoms containing 1 heteroatom selected from N; or R3 and R4, taken together, form a bond; R6 is hydrogen; each RA1 is hydrogen; each RX is independently selected from hydrogen, C1-10 alkyl, halogen, CN and NO2; n is 0; p is 0. The invention also relates to a pharmaceutical composition for inhibiting the kinase activity of Bruton's tyrosine kinase (BTK), containing an effective amount of the said compound and at least one pharmaceutically acceptable carrier, and to a method of treating, ameliorating or preventing a condition that responds to BTK inhibition, comprising administering to a subject in need of such treatment, an effective amount of the said compound.

EFFECT: invention can be used for treatment of an inflammatory and/or autoimmune condition.

34 cl, 2 tbl, 117 ex

(II)

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RU 2 749 038 C2

Authors

Chzhao, Sindun

Chzhan, Vejpen

Chen, Chzhifan

Chen, Lin

Van, Syanlun

Li, Chzhifu

Tan, Zhuj

Yan, Litszyun

Tan, Khaokhan

Lyu, Bin

Ran, Kaj

Tszou, Tszunyao

Lin, Min

Sun, Tszin

Van, Vejbo

Dates

2021-06-03Published

2017-06-20Filed