申请人:Takeda Chemical Industries, Ltd.
公开号:EP0655447A1
公开(公告)日:1995-05-31
A compound of the general formula:
wherein R¹ represents a carboxyl group which may optionally be esterified or amidated; R² represents a cyclic group which may optionally be substituted or a polar group; n is an integer of 0 to 6; R³ represents hydrogen or a hydrocarbon residue which may optionally be substituted; R⁴ represents (1) a hydrocarbon residue which is substituted by an optionally protected amino group or (2) an alkenyl group; or R³ and R⁴ may be combined with the adjacent nitrogen atom to form a heterocyclic group containing at least two hetero atoms, or a salt thereof.
The compound or a salt thereof of the present invention inhibits thiol proteases such as cathepsin L and B and serves well as a prophylactic/therapeutic agent for bone diseases such as osteoporosis.
通式如下的化合物
其中 R¹ 代表可选择酯化或酰胺化的羧基;R² 代表可选择被取代的环状基团或极性基团;n 为 0 至 6 的整数;R³ 代表氢或可选择被取代的烃残基;R⁴代表(1)被任选保护的氨基取代的烃残基或(2)烯基;或 R³ 和 R⁴ 可与相邻的氮原子结合形成至少含有两个杂原子的杂环基团或其盐。
本发明的化合物或其盐可抑制硫醇蛋白酶,如 cathepsin L 和 B,可作为骨质疏松症等骨病的预防/治疗药物。