申请人:SMITHKLINE BEECHAM CORP
公开号:WO2000038687A1
公开(公告)日:2000-07-06
The present invention provides 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, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
本发明提供了4-氨基-氮杂丙烷-3-酮蛋白酶抑制剂及其药学上可接受的盐、水合物和溶剂化物,其能够抑制蛋白酶,包括卡他普西蛋白酶K,还提供了这些化合物的制药组合物、这些化合物的新中间体以及用于治疗过度骨质流失或软骨或基质降解等疾病的方法,包括骨质疏松症;牙龈疾病,包括牙龈炎和牙周炎;关节炎,更具体地说是骨关节炎和类风湿性关节炎;帕吉特病;恶性高钙血症;以及代谢性骨病,通过向需要的患者施用本发明化合物来抑制骨质流失或过度软骨或基质降解。