公开(公告)号：US5556853A

公开(公告)日：1996-09-17

申请号：US330833

申请日：1994-10-27

申请人： Shigetoshi Tsubotani ,  Takizawa Masayuki ,  Shirasaki Mikio ,  Yukio Fujisawa

发明人： Shigetoshi Tsubotani ,  Takizawa Masayuki ,  Shirasaki Mikio ,  Yukio Fujisawa

IPC分类号： A61K31/335 ,  C07D303/48 ,  C07D405/12 ,  A61K31/535 ,  C07D413/12

CPC分类号： C07D405/12 ,  A61K31/335 ,  C07D303/48

摘要： A compound of the general formula: ##STR1## wherein R.sup.1 represents a carboxyl group which may optionally be esterified or amidated; R.sup.2 represents a cyclic group which may optionally be substituted or a polar group; n is an integer of 0 to 6; R.sup.3 represents hydrogen or a hydrocarbon residue which may optionally be substituted; R.sup.4 represents (1) a hydrocarbon residue which is substituted by an optionally protected amino group or (2) an alkenyl group; or R.sup.3 and R.sup.4 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.

摘要翻译： 一种通式如下的化合物：其中R 1表示可任意被酯化或酰胺化的羧基; R 2表示可任选被取代的环状基团或极性基团; n为0〜6的整数。 R 3表示氢或可任选被取代的烃残基; R4表示（1）被任选保护的氨基取代的烃残基或（2）烯基; 或者R 3和R 4可以与相邻的氮原子结合形成含有至少两个杂原子的杂环基或其盐。 本发明的化合物或其盐抑制硫蛋白酶如组织蛋白酶L和B，并且作为骨疾病如骨质疏松症的预防/治疗剂起作用。