SUBSTITUTED PYRAZOLE[1,5-a]PYRIMIDINE-7-AMINE DERIVATIVE, COMPOSITION AND PHARMACEUTICAL USE THEREOF Russian patent published in 2024 - IPC C07D487/04 A61K31/519 A61P35/00 

Abstract RU 2824118 C1

FIELD: medicine; pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical technology, namely to a pyrazolo [1,5-a]pyrimidine-7-amine derivative of formula (III-a) or (III-b), its pharmaceutically acceptable salt or its stereoisomer, where R1a is hydrogen, C1-6 alkyl or deuterated C1-6 alkyl; n is 1, 2, 3 or 4; t is equal to 1, 2 or 3; each of R11 and R12 independently represent hydrogen; R2 is hydrogen, C1-6 alkyl or halogen; R3 is hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkoxy or halogen, where C1-6 alkyl is unsubstituted or substituted with 1, 2 or 3 substitutes selected from C1-3 alkoxy; R4 is hydrogen, -C(O)(C1-3 alkyl), -(C=N)-C1-3 alkyl or -(C=N)-NRa0Rb0; R5 is hydrogen; Ra is hydrogen, C1-6 alkyl, C3-6 cycloalkyl, cyano or halogen, where C1-6 alkyl is unsubstituted or substituted with 1, 2 or 3 substitutes selected from halogen; Rb is hydrogen; (R0)m means that hydrogen atoms in the ring are substituted with m groups R0, where m is 0; each of Ra0 and Rb0 independently represents hydrogen. Invention also relates to use of a compound of formula (III-a) or (III-b), or a pharmaceutically acceptable salt thereof, or a stereoisomer in preparing a drug for treating or preventing a disease associated with CDK9 activity.

EFFECT: obtaining compounds having inhibitory activity on CDK9 for treating CDK9-mediated diseases.

15 cl, 5 tbl, 96 ex

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RU 2 824 118 C1

Authors

Zhao, Zhiming

Wu, Shenghua

Hua, Mojia

Hao, Shenglei

Wang, Lulu

Liu, Yang

Dates

2024-08-06Published

2022-01-21Filed