AMINOPYRAZOLOPYRIMIDINE COMPOUND USED AS INHIBITOR OF TYROSINE KINASE RECEPTOR OF NEUROTROPHIC FACTOR Russian patent published in 2022 - IPC C07D487/04 A61K31/519 A61K31/5377 A61P35/00 

Abstract RU 2764523 C2

FIELD: organic chemistry; pharmacology.

SUBSTANCE: group of inventions relates to the field of organic chemistry and pharmacology, namely to a compound that can inhibit the activity of Trk kinase. The compound is represented by the formula I or its pharmaceutically acceptable salt, where R1, R4 and R7 are hydrogen; R2 is selected from a group consisting of hydrogen, C1-6alkyl, -C(=O)R9, -C(=O)NHR9 and -S(=O)2R9, where C1-6alkyl is not substituted or substituted with one substituent independently selected from a group consisting of 6-element aliphatic heterocyclyl and optionally substituted phenyl; R3 is selected from a group consisting of hydrogen, halogen, cyano, -C(=O)R10, -C(=O)NR10R11, -C(=S)NR10R11, phenyl and 5-element aromatic heterocyclyl, where phenyl and 5-element aromatic heterocyclyl, each independently, are not substituted or substituted with one substituent independently selected from a group consisting of C1-6alkyl, C1-6alkoxycarbonyl, morpholinyl and optionally substituted pyrrolidinyl carbonyl; R5 and R6 are independently selected from a group consisting of hydrogen, halogen and hydroxy, or R5 and R6 together form oxo; R8 is phenyl that is not substituted or substituted with one or two substituents independently selected from halogen; R9 is selected from a group consisting of C1-6alkyl and phenyl, where phenyl is not substituted or substituted with one substituent independently selected from C1-6alkyl; R10 and R11 are independently selected from a group consisting of hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, 3-6-element cycloalkyl and phenyl, where C1-6alkyl, C1-6alkoxy, 3-6-element cycloalkyl and phenyl, each independently, are not substituted or substituted with one, two or three substituents independently selected from a group consisting of halogen, hydroxy, C1-4alkyl and hydroxy(C1- 6alkyl) group, 2,2-dimethyl-1,3-dioxolan-4-yl and N,N-di(C1-4alkyl)amino; or R10 and R11, together with N, to which they are attached, form 5-element aliphatic heterocycle that is not substituted or substituted with one substituent selected from hydroxy, where “optionally substituted” means that the group can be not substituted or substituted with one substituent independently selected from hydroxy or C1-6alkoxy, and the specified “aliphatic heterocycle” or “aromatic heterocycle” contain 1-2 heteroatoms independently selected from sulfur, oxygen and/or nitrogen. The group of inventions also relates to specific compounds, a pharmaceutical composition based on it, their use in the preparation of a drug and a method for the treatment of a disease mediated by Trk.

EFFECT: providing the effective treatment or prevention of a disease mediated by the tyrosine kinase receptor Trk.

39 cl, 4 tbl, 52 ex

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RU 2 764 523 C2

Authors

Zhu Li

Hu Yuandong

Wu Wei

Dai Liguang

Duan Xiaowei

Yang Yanqing

Sun Yinghui

Han Yongxin

Peng Yong

Kong Fansheng

Luo Hong

Yang Ling

Xu Hongjiang

Guo Meng

Wang Shanchun

Zhong Zhaobai

Dates

2022-01-18Published

2017-10-27Filed