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Certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor
专利权人:
HUTCHISON MEDIPHARMA LIMITED
发明人:
SU WEI-GUO,DAI GUANGXIU,JIA HONG
申请号:
NZ60112810
公开号:
NZ601128A
申请日:
2010.12.30
申请国别(地区):
NZ
年份:
2014
代理人:
摘要:
Disclosed are 1-(heteroarylalkyl)-6-(heteroaryl)-1H-[1,2,3]triazolo[4,5-b]pyrazine derivatives as represented by the general formual (1), and/or at least one pharmaceutically acceptable salt thereof, wherein: X is N Y is absent R1 is an optionally substituted fused bicyclic heteroaryl ring selected from pyrazolo[1,5-a]pyridine, imidazo[1,2-a]pyridine, imidazo[1,2-a]pyrazine, 1H-thieno[3,2-c]pyrazole, 1H-pyrrolo[2,3-b]pyridine, thieno[3,2-c]pyridine, imidazo[1,5a]pyridine, pyrido[3,2-d][1,3]thiazole, pyrazolo[3,4-b]pyridine, thieno[2,3-b]pyridine, [1,2,4]triazolo[1,5-a]pyridine, pyrazolo[1,5-a]pyrimidine, imidazo[1,2-b]pyridazine and 1H-pyrrolo[3,2-b]pyridine R2 and R3 are independently selected from hydrogen, and alkyl, or R2 and R3, together with the carbon to which they are attached, form a ring chosen from 3- to 7-membered cycloalkyl and 3- to 7-membered heterocycle R4 is selected from halo, alkyl, cycloalkyl, heterocycle, aryl and heteroaryl, each of which except for halo is optionally substituted R5 is selected from hydrogen, halo, hydroxy, amino, trifluoromethyl, difluoromethyl, alkyl, alkenyl, and alkynyl and wherein the remaining substituents are as defined herein. Representative compounds include those such as 1-(1-(imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine. Further disclosed is a composition comprising at least one compound as defined above, and/or at least one pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable carrier for the treatment of cancer (and particularly for the treatment of lung cancer, stomach cancer, colorectal cancer, esophageal cancer, hepatocellular cancer, breast cancer, kidney cancer and ovarian cancer).
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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