Protease inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 417/14 (2006.01) A61K 31/55 (2006.01) C07D 223/12 (2006.01) C07D 401/02 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/02 (2006.01) C07D 403/14 (2006.01) C07D 405/02 (2006.01) C07D 405/14 (2006.01) C07D 409/02 (2006.01) C07D 409/14 (2006.01) C07D 413/02 (2006.01) C07D 413/14 (2006.01) C07D 415/00 (2006.01) C07D 417/00 (2006.01) C07D 417/02 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2412353

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 à base de 4-amino-azépan-3-one et des sels, hydrates et solvates pharmaceutiquement acceptables de ceux-ci, qui inhibent des protéases, y compris la cathepsine K ; des compositions pharmaceutiques renfermant ces composés, de nouveaux produits intermédiaires contenant ces composés et des méthodes de traitement de maladies impliquant une perte osseuse excessive ou une dégradation matricielle ou cartilagineuse, y compris l'ostéoporose ; des affections des gencives, y compris la gingivite et la parodontite; l'arthrite, plus spécifiquement, l'ostéoarthrite et la polyarthite rhumatoïde ; la maladie de Paget ; une hypercalcémie de tumeur maligne ; et des maladies osseuses métaboliques. Ces méthodes de traitement comprennent une inhibition de la perte osseuse ou d'une dégradation cartilagineuse ou matricielle par l'administration, à un patient nécessitant un tel traitement, d'un composé de l'invention.

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