申请人:Mitsubishi Chemical Corporation
公开号:EP0603769A1
公开(公告)日:1994-06-29
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. It 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-氨基酮衍生物可强烈抑制硫醇蛋白酶,如木瓜蛋白酶、酪蛋白酶 B、酪蛋白酶 H、酪蛋白酶 L 和钙蛋白酶或类似物,并在口服吸收、组织分布和细胞膜渗透性方面具有优异的特性。因此,α-氨基酮衍生物可用作治疗剂,用于治疗肌肉萎缩症、肌萎缩症、心肌梗塞、中风、老年痴呆症、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、白内障、炎症、过敏症、暴发性肝炎、骨质疏松症、高钙血症、乳腺癌、前列腺癌或前列腺肥大。它还可用作抑制癌细胞生长、防止癌症转移或抑制斑块聚集的治疗剂。