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.; R1 is H or a carboxyl- protecting group; R2 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.
SATO TOSHIO
KATSUNUMA NOBUHIKO
SATO TOSHIO
Next Patent: carbon dioxide electrolyzer