CYANOTHIENOTRIAZOLODIAZEPINES AND METHODS FOR THEIR USE Russian patent published in 2021 - IPC C07D495/14 A61K31/55 A61K31/551 A61P3/10 A61P9/00 A61P15/16 A61P19/02 A61P35/00 

Abstract RU 2750164 C2

FIELD: organic chemistry.

SUBSTANCE: present invention relates to the compound of Formula (I):

(I),

or its pharmacologically acceptable salts, a stereoisomer, or a tautomer, wherein radicals R1, R2, RA1, RA2, RC, RB, C, X1 are defined in the claim. A pharmaceutical composition is also proposed, a set for use in the treatment of a disease associated with a bromodomain-containing protein and/or with a bromodomain, methods for treating diseases associated with aberrant bromodomain activity, a method for male contraception, methods for inhibiting the activity of a bromodomain in a biological sample, methods for inhibiting binding of a bromodomain-containing protein to an acetyl-lysine residue of a second protein in a subject, methods for inhibiting gene expression, methods for inducing apoptosis, methods for inducing G1 blocking in a cell.

EFFECT: obtaining new organic compounds, which may be agents that have ability to bind bromodomain-containing proteins, and may be suitable for treatment of diseases associated with the activity of bromodomain-containing proteins.

78 cl, 1 dwg, 5 tbl, 2 ex

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RU 2 750 164 C2

Authors

Bradner Dzhejms I.

Tsi Tszyun

Tanaka Minoru

Bakli Dennis

Dates

2021-06-22Published

2016-09-09Filed