BETANCORT, JUAN MANUEL,贝坦科特胡安曼努尔,貝坦科特胡安曼努爾,STAFFORD, JEFFREY ALAN,史塔福德杰佛瑞艾伦,史塔福德傑佛瑞艾倫,STANSFIELD, RYAN,史丹斯菲尔德莱恩,史丹斯菲爾德萊恩,VEAL, JAMES MARVIN,维尔詹姆士马文,維爾詹姆士馬文
申请号：
TW105112168
公开号：
TW201642860A
申请日:
2016.04.19
申请国别(地区):
TW
年份:
2016
代理人:
摘要：
Described herein is the bromodomain inhibitor 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one, including crystalline forms, amorphous forms, solvates, and hydrates thereof, as well as pharmaceutical compositions that include this bromodomain inhibitor. In some embodiments the pharmaceutical composition comprises 4-[2-(cyclopropylmethoxy)-5-methyl sulfonylphenyl]-2-methylisoquinolin-1-one that has been processed by micronization or spray dried dispersion. In some embodiments, the pharmaceutical composition further comprises at least one polymer. In some embodiments, the pharmaceutical compositions comprises a solid polymer matrix comprising 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one and at least one polymer. Pharmaceutical compositions comprising 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one are useful for the treatment of cancer or neoplastic disease.本文描述布羅莫結構域抑制劑4-[2-(環丙基甲氧基)-5-甲基磺醯基苯基]-2-甲基異喹啉-1-酮，包括其結晶形式、非結晶形式、溶劑化物及水合物，以及包括此布羅莫結構域抑制劑之醫藥組成物。在一些實施例中，醫藥組成物包含藉由微粉化或噴霧乾燥分散液來處理之4-[2-(環丙基甲氧基)-5-甲基磺醯基苯基]-2-甲基異喹啉-1-酮。在一些實施例中，醫藥組成物進一步包含至少一種聚合物。在一些實施例中，醫藥組成物包含固體聚合物基質，該固體聚合物基質包含4-[2-(環丙基甲氧基)-5-甲基磺醯基苯基]-2-甲基異喹啉-1-酮及至少一種聚合物。包含4-[2-(環丙基甲氧基)-5-甲基磺醯基苯基]-2-甲基異喹啉-1-酮之醫藥組成物可用於治療癌症或腫瘤疾病。
