| 摘要 |
<p>PURPOSE:To obtain a thiolprotease inhibitor containing a 2-alkynylmalonic acid derivative and useful for treating osteoporosis and hypercalcemia. CONSTITUTION:This inhibitor contains a compound of the formula (R is H, an aryl, an aralkyl, a cycloalkyl, a lower alkyl, etc.; R<1> is H or a carboxyl- protecting group; R<2> is hydroxy, a lower alkoxy, etc.) or its salt as an active ingredient. The compound of the formula has excellent cathepsin L-inhibiting activity and cathepsin B inhibiting activity and is useful for preventing and treating muscular dystrophy, inflammation, renal hypertension, cataract, cardiac infarction, viral diseases, malignant tumor, allergic diseases and especially useful as a treating agent for osteoporosis and hypercalcemia, due to inhibition of collagen-decomposing ability.</p> |
