申请人:Mitsubishi Kasei Corporation
公开号:US05422359A1
公开(公告)日:1995-06-06
Alpha-aminoketone derivatives of the present invention strongly inhibit thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L and calpain or the like and have excellent properties in absorbance on oral administration, tissue distribution and cell membrane permeability. The alpha-aminoketone derivatives can thus be used as therapeutic agents for treating muscular dystrophy, amyotrophy, cardiac infarction, stroke, Alzheimer's disease, disturbance of consciousness or dyskinesia caused upon brain trauma, multiple sclerosis, peripheral nervous neuropathy, cataract, inflammation, allergosis, fulminant hepatitis, osteoporosis, hypercalcemia, breast carcinoma, prostatic carcinoma or prostatomegaly. They may also be used as therapeutic agents for suppressing growth of cancer cells, preventing metastasis of cancer or suppressing aggregation of plaques.
本发明的α-
氨基酮衍
生物强烈抑制半胱
氨酸
蛋白酶,如
木瓜蛋白酶、B型卡
特普西因、H型卡
特普西因、L型卡
特普西因和
钙蛋白酶等,并具有在口服时的良好吸收性、组织分布和细胞膜通透性等优良性质。因此,α-
氨基酮衍
生物可用作治疗肌萎缩症、肌萎缩、心肌梗塞、中风、阿尔茨海默病、脑外伤引起的意识障碍或运动障碍、多发性硬化症、周围神经病变、白内障、炎症、过敏反应、急性肝炎、骨质疏松症、高
钙血症、乳腺癌、前列腺癌或前列腺增生的治疗剂。它们还可以用作抑制癌细胞生长、预防癌转移或抑制斑块聚集的治疗剂。