Aminoketone derivatives according to the present invention strongly inhibits thiol protease such as calpain, papain, cathepsin B, cathepsin H, cathepsin L or the like and has excellent properties concerning absorbance on oral administration, tissue distribution and cell membrane permeability. The aminoketone derivatives can thus be used as therapeutic agents for treating muscular dystrophy, cataract, cardiac infarction, stroke, Alzheimer's disease, amyotrophy, osteoporosis and hypercalcemia and so on. It may also be used as therapeutic agents for preventing metastasis of cancer. In addition, the present derivatives are also applicable as the intermediates upon preparation of ketone derivatives, which has the inhibitory activity against thiol protease.
根据本发明的
氨基酮衍
生物可强烈抑制
硫醇
蛋白酶,如
钙蛋白酶、
木瓜蛋白酶、
酪蛋白酶 B、
酪蛋白酶 H、
酪蛋白酶 L 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,
氨基酮衍
生物可用作治疗剂,用于治疗肌肉萎缩症、白内障、心肌梗塞、中风、老年痴呆症、肌萎缩症、骨质疏松症和高
钙血症等。它还可用作预防癌症转移的治疗剂。此外,本衍
生物还可作为制备酮衍
生物的中间体,对
硫醇
蛋白酶具有抑制活性。