ALPHA- AND BETA-UNSATURATED AMIDE COMPOUND-A BENZOTRIAZOLE DERIVATIVE USED AS A TGF-ΒRI INHIBITOR Russian patent published in 2020 - IPC C07D471/04 A61K31/4439 A61K31/444 A61P35/00 

Abstract RU 2737737 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein in formula (I) R1 is selected from hydrogen, amino or from a group consisting of C1-3 alkyl and C3-6 cycloalkyl, and said group is optionally substituted with 1 R; R2 is selected from a group consisting of C1-3 alkyl, C3-6 cycloalkyl and phenyl, and said group is optionally substituted with 1 R; R3 denotes hydrogen; optionally, R2 and R3 are bonded to form 5-member ring; each of R4 and R5 is independently selected from hydrogen, halogen or is C1-3 alkyl; L is selected from a single bond, -CH2-; R is selected from CN, OH, or C1-6 alkyl, optionally substituted with 1, 2 or 3 R'; R' is F. Invention also relates to individual compounds, to pharmaceutical compositions, to the use of the compound, to the use of the pharmaceutical composition, to a pharmaceutical combination.

EFFECT: technical result is obtaining novel compounds of formula (I), having the properties of a TGF-βRI inhibitor.

19 cl, 7 tbl, 3 dwg

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RU 2 737 737 C2

Authors

Sun, Fej

Vu, Lifan

Din, Charlz Z.

Khu, Guopin

Li, Tszyan

Chen, Shukhuej

Lu, Tszyanyuj

Dates

2020-12-02Published

2017-06-08Filed