公开(公告)号：EP1307203A1

公开(公告)日：2003-05-07

申请号：EP01916412.8

申请日：2001-03-07

申请人： SMITHKLINE BEECHAM CORPORATION

发明人： CUMMINGS, Maxwell, D. ,  MARQUIS Robert, W., Jr. ,  RU, Yu ,  THOMPSON, Scott, K. ,  VEBER, Daniel, F. ,  YAMASHITA, Dennis, S.

IPC分类号： A61K31/55 ,  A61P19/08 ,  A61P19/10 ,  C07D401/00 ,  C07D403/00 ,  C07D413/00

CPC分类号： C07C271/12 ,  C07C271/14 ,  C07D223/04 ,  C07D223/08 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D491/04 ,  C07D495/04

摘要： The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.

摘要翻译： 本发明提供C1-6烷基-4-氨基 - 氮杂环庚烷-3-酮蛋白酶抑制剂及其抑制蛋白酶（包括组织蛋白酶K）的药学上可接受的盐，水合物和溶剂合物，这类化合物的药物组合物，这类化合物的新中间体和方法 用于治疗过度骨丢失或软骨或基质降解（包括骨质疏松症）的疾病; 牙龈疾病，包括牙龈炎和牙周炎; 关节炎，更具体地说，骨关节炎和类风湿性关节炎; 佩吉特氏病; 恶性肿瘤高钙血症; 和代谢性骨病; 和寄生虫疾病，包括疟疾，通过向有需要的患者施用一种或多种本发明化合物。