THIENODIAZEPINE DERIVATIVES AND THEIR USE Russian patent published in 2023 - IPC C07D495/14 C07D519/00 C07D243/06 A61K31/55 A61P35/00 

Abstract RU 2795005 C2

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a compound of formula (I) or (II), its stereoisomer or a pharmaceutically acceptable salt having BRD4 inhibition activity, a pharmaceutical composition based on them and their use in the manufacture of a medicament for the treatment or prevention of a disease associated with BRD4. In the general formula (I) or (II) T is selected from the group consisting of C and N; R1 is C1-3 alkyl; R2, R3 and R4 are individually and independently selected from the group consisting of H, F, Cl, Br and C1-6 alkyl; R5 is H; R6 is separately and independently selected from the group consisting of H, F, Cl, Br, OH, NH2, C1-6 alkyl and C1-6 heteroalkyl, which is not necessarily substituted with a 1R group; ring A is selected from the group consisting of C3-7 cycloalkyl, 5-12 membered heterocycloalkyl and 5-6 membered heteroaryl; ring B is a 4-7 membered heterocycloalkyl; n is selected from the group consisting of 0, 1, 2; R is individually and independently selected from the group consisting of NH2 and C1-6 alkyl.

EFFECT: development of compounds with significant inhibitory activity against BRD4 bromodomain.

20 cl, 4 tbl, 37 ex

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RU 2 795 005 C2

Authors

Shen, Chunli

U, Chende

Lyu, Yun

Gun, Chzhen

Li, Tszyan

Chen, Shukhuej

Dates

2023-04-27Published

2018-09-06Filed