Protease inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 419/02 (2006.01) A61K 31/55 (2006.01) C07D 223/08 (2006.01) C07D 223/12 (2006.01) C07D 401/02 (2006.01) C07D 401/10 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/02 (2006.01) C07D 403/12 (2006.01) C07D 405/02 (2006.01) C07D 405/12 (2006.01) C07D 405/14 (2006.01) C07D 409/02 (2006.01) C07D 409/12 (2006.01) C07D 409/14 (2006.01) C07D 411/02 (2006.01) C07D 413/02 (2006.01) C07D 413/14 (2006.01) C07D 417/02 (2006.01) C07D 417/12 (2006.01) C07D 417/14 (2006.01) C07D 471/04 (2006.01) C07D 49

Patent

CA 2356671

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.

L'invention concerne des inhibiteurs de protéases 4-amino-azepan-3-ones, des solvates, des hydrates et des sels de ceux-ci, acceptables au plan pharmaceutique, qui inhibent les protéases dont la cathépsine K, des compositions pharmaceutiques comprenant lesdits composés, des nouveaux intermédiaires desdits composés et des méthodes de traitement de maladies se manifestant par une perte osseuse excessive ou une dégradation du cartilage ou de la matrice, dont l'ostéoporose; l'arthrite, notamment l'arthrose et la polyarthrite rhumatoïde; la maladie osseuse de Paget; l'hypocalcémie maligne; et la maladie métabolique des os. Lesdites méthodes consistent à inhiber ladite perte osseuse ou la dégradation excessive du cartilage ou de la matrice, par l'administration à un patient en ayant besoin d'un composé de l'invention.

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