Smithkline Beecham Corporation

Hye-Ja Oh

Daniel F Veber

Timothy Francis Gallagher

Scott Kevin Thompson

Dennis Shinji Yamashita

Stacie Marie Halbert

Renee Louise DesJarlais

Thomas Joseph Carr

Jack Hwekwo Yen

Dennis Alan Holt

Mark A Levy

The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions 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.

Protease inhibitors

The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions 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 and bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Invented are 17.beta.-substituted acyl-4-aza analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates and processes used in preparing these compounds.

17.alpha. and 17.beta. substituted acyl 4 aza steroids

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Exton, PA, United States of America

Hye-Ja Oh