MACROCYCLE CONTAINING AMINOPYRAZOLE AND PYRIMIDINE, AND ITS PHARMACEUTICAL COMPOSITION AND USE Russian patent published in 2022 - IPC C07D498/22 C07D471/22 A61K31/519 A61P35/04 

Abstract RU 2779497 C2

FIELD: medicine.

SUBSTANCE: present invention relates to a macrocycle of the formula (I) or to its pharmaceutically acceptable salt, to a pharmaceutical composition containing them, and to their use in the inhibition of activity of tropomyosin-receptor kinase A (hereinafter – TrkA-kinase) and in the treatment of diseases mediated by TrkA-kinase.

, where X is selected from a group containing of a bond, -O-, -S-, and -NR4-; Y is selected from a group consisting of and , where “*” is an end of the group Y, attached to an aminopyrazolopyrimidine ring, and R1-R5, m, n, Cy have values specified in the claims.

EFFECT: development of a new effective inhibitor of TrkA-kinase activity.

26 cl, 2 tbl, 37 ex

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RU 2 779 497 C2

Authors

Dai Liguang

Duan Xiaowei

Yang Yanqing

Liu Xijie

Li Hongjuan

Zhao Na

Sun Yinghui

Kong Fansheng

Zhang Jiuqing

Zhu Yizhong

Yang Ling

Liu Fei

Dates

2022-09-08Published

2018-08-23Filed