原肌球蛋白相關激酶(TRK)抑制劑之醫藥調配物农业专利-农业学术服务平台

发明人:: LIEBERMAN, HARVEY,利伯曼　哈威,YANG, DONGLAI,杨　东来,楊　東來,PHILBROOK, C. MICHAEL,菲尔布鲁克　希麦可,菲爾布魯克　希麥可,SANTOS, MICHAEL,桑托斯　麦可,桑托斯　麥可,HO, CHRIS,何　裕会,何　裕會,利伯曼哈威,杨东来,楊東來,菲尔布鲁克希麦可,菲爾布魯克希麥可,桑托斯麦可,桑托斯麥可,何裕会,何裕會

摘要：: Pharmaceutical formulations with a tropomyosin-related kinase inhibitor (“Trk inhibitor”) are disclosed. The pharmaceutical formulations comprise 3-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)-6-(1-methyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridin-2-amine in microcrystalline suspension formulations in its monohydrate form, which shows improved characteristics over the anhydrate form, and in extended release formulations. The extended release pharmaceutical formulations comprise 3-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)-6-(1-methyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridin-2-amine-loaded microspheres.本申請公開了具有原肌球蛋白相關激酶抑制劑(「“Trk抑制劑”」)的醫藥調配物。所述醫藥調配物包含在微晶懸浮液調配物中的呈其單水合物形式的及在延長釋放調配物中的3-(3-甲氧基-4-((4-甲氧基苄基)氧基)苄基)-6-(1-甲基-1H-吡唑-4-基)-3H-咪唑并[4,5-b]吡啶-2-胺，所述單水合物形式顯示出相對於無水物形式而言改善的特徵。所述延長釋放醫藥調配物包含載有3-(3-甲氧基-4-((4-甲氧基苄基)氧基)苄基)-6-(1-甲基-1H-吡唑-4-基)-3H-咪唑并[4,5-b]吡啶-2-胺的微球。