Protease inhibitors

Details Protease inhibitors Protease inhibitors

C - Chemistry, Metallurgy

07

D

C07D 495/04 (2006.01) A61K 31/55 (2006.01) A61K 31/64 (2006.01) A61P 19/00 (2006.01) C07D 405/14 (2006.01) C07D 409/04 (2006.01) C07D 409/14 (2006.01)

Patent

CA 2436850

The present invention provides C3-C6 1-amino-1-acyl cycloalkane-substituted 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 la C¿3?-¿6? 1-amino-1-acyle cycloalcane-substitué 4-amino-azepan-3-one protéase, et des sels, hydrates et solvates pharmaceutiquement acceptables de ceux-ci, qui inhibent les protéases, notamment la cathépsine K; des compositions pharmaceutiques desdits composés; ainsi que des nouveaux produits intermédiaires desdits composés. L'invention concerne également des méthodes de traitement de maladies entraînant une perte osseuse ou une dégradation de cartilage ou de matrice excessives, notamment l'ostéoporose; de maladies gingivales, notamment la gingivite et la parodontite; de l'arthrite, plus particulièrement l'arthrose et la polyarthrite rhumatoïde, de la maladie de Paget, de l'hypercalcémie maligne, et de maladies osseuses métaboliques, qui consistent à inhiber ladite perte osseuse ou ladite dégradation de cartilage et de matrice excessives par administration à un patient nécessitant ce traitement d'un composé de l'invention.

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