GRECO, MICHAEL NICHOLAS,格雷科 迈克尔 尼古拉斯,格雷科 邁克爾 尼古拉斯,COSTANZO, MICHAEL JOHN,科斯坦佐 迈克尔 约翰,科斯坦佐 邁克爾 約翰,PENG, JIRONG,彭 继荣,彭 繼榮,ZHANG, DON,张 东,張 東
申请号：
TW108103389
公开号：
TW201940166A
申请日:
2019.01.29
申请国别(地区):
TW
年份:
2019
代理人:
摘要：
2-Aminopyrimidine-substituted 2H-indazole compounds of formula (I), where R1is hydrogen, and their prodrugs, where R1is a metabolizable group under physiological conditions, as cyclin-dependent kinase (CDK) and cell-proliferation inhibitors, and therapeutic uses and methods of preparation thereof, are disclosed. These compounds, and pharmaceutically acceptable salts, solvates, prodrugs, and pharmaceutical compositions thereof, are useful for treating diseases and disorders associated with activity of cyclin-dependent kinases, in particular CDK4/6, including but not limited to various cancers and inflammation-related diseases or conditions.本發明揭示式(I)之經2-胺基嘧啶取代之2H-吲唑化合物(其中R1係氫)及其前藥(其中R1係在生理條件下可代謝之基團)，其作為週期蛋白依賴性激酶(CDK)及細胞增殖抑制劑，及其治療用途及製備方法。該等化合物及其醫藥上可接受之鹽、溶劑合物、前藥及醫藥組合物可用於治療與週期蛋白依賴性激酶、特定而言CDK4/6之活性相關之疾病及病症，包括(但不限於)各種癌症及發炎有關之疾病或病狀。
