PYRAZOLO[1,5-A]PYRAZIN-4-YL DERIVATIVES AS JAK-INHIBITORS Russian patent published in 2020 - IPC C07D487/04 A61K31/4985 A61P37/02 A61P29/00 A61P25/28 

Abstract RU 2718902 C2

FIELD: chemistry; pharmaceutics.

SUBSTANCE: invention relates to a compound having structure (I), or a pharmaceutically acceptable salt thereof, where A, A' and A'' are independently O, C = O, CR' or NR'', where R' and R'' can independently be H, amino, -NR7COR6, -CONR7R8, C1-C6 alkyl or hydroxy(C1-C6 alkyl)-, and R'' can be present or absent and is present where valence rules enable, and where not more than one of A, A' and A'' is O; R0 and R independently represent H or C1-C6 alkyl; R1 is H; R2 is selected from a group consisting of H, C1-C6 alkyl-, C1-C6 alkoxy-, phenyl(C1-C6 alkyl)-, pyrazole, -COR6 and -(CH2)n-W, where W is cyano, hydroxy, C3-C8 cycloalkyl and -SO2-R9, where R9 is C1-C6 alkyl; where each of said alkyl and cycloalkyl can be unsubstituted or substituted with halogen; X is CR3 or N, where R3 can be H or C1-C6 alkyl; R4 and R5 independently represent H, amino, C1-C6 alkyl or hydroxy(C1-C6 alkyl)-; R6, R7 and R8 each independently represent H, C1-C6 alkyl or C3-C8 cycloalkyl and n equals 0, 1, 2 or 3.

EFFECT: pyrazolo[1,5-a]pyrazin-4-yl derivatives have inhibitory action on janus kinase (JAK).

24 cl, 2 tbl, 37 ex

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RU 2 718 902 C2

Authors

Brown, Matthew Frank

Dermenci, Alpay

Fensome, Andrew

Gerstenberger, Brian Stephen

Hayward, Matthew Merrill

Owen, Dafydd Rhys

Wright, Stephen Wayne

Xing, Li Huang

Yang, Xiaojing

Dates

2020-04-15Published

2017-02-10Filed