281219-31-6Relevant articles and documents
Protease inhibitors
-
, (2008/06/13)
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.
Azepanone-based inhibitors of human and rat cathepsin K
Marquis,Ru,LoCastro,Zeng,Yamashita,Oh,Erhard,Davis,Tomaszek,Tew,Salyers,Proksch,Ward,Smith,Levy,Cummings,Curtis Haltiwanger,Trescher,Wang,Hemling,Quinn,Cheng,Lin,Smith,Janson,Zhao,McQueney,D'Alessio,Lee,Marzulli,Dodds,Blake,Hwang,James,Gress,Bradley,Lark,Gowen,Veber
, p. 1380 - 1395 (2007/10/03)
The synthesis, in vitro activities, and pharmacokinetics of a series of azepanone-based inhibitors of the cysteine protease cathepsin K (EC 3.4.22.38) are described. These compounds show improved configurational stability of the C-4 diastereomeric center