Carbohydrazide protease inhibitors
AssigneeSmithKline Beecham Corporation
InventorsStacie Marie Halbert, Scott Kevin Thompson
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Abstract
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, inducing osteoporosis; gingival disease including gingivitis and periodontists; 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.
Claims13
A compound according to Formula IV:
- wherein:
- R21 and R26 are independently C5-6alkyl;
- C2-6alkenyl;
- C3-11cycloalkyl;
- T-C3- 6alkyl;
- V-C1-6alkyl;
- T-C2-6alkenyl;
- or
- T-(CH2)nCH(T)(CH2)N;
- optionally substituted by one or
- two halogens, SR20, OR20, NR20R27 or C1-4alkyl;
- R27 is R28CO, or R28OCO;
- R28 is C1-6alkyl;
- C3-11cycloalkyl;
- Ar;
- Het;
- T-C1-6alkyl;
- or
- T-(CH2)nCH(T)(CH2)n;
- optionally substituted by one or two halogens,
- SR20,OR20, NR20R73,or C1-6alkyl;
- R20, R22, R23, R24, R25, and R73 are independently H, C1-4alkyl, Ar-C0-6alkyl, or
- Het-C0-6alkyl;
- R58 and R59 are independently H, C1-6alkyl, Ar-C0-6alkyl, or Het-C0-6alkyl;
- T is Ar, or Het;
- V is C3-7cycloalkyl;
- n is 1 to 6:
- Ar is phenyl or naphthyl, optionally substituted by one or more of
- Ph-C0-6alkyl, Het-C0-6alkyl, C1-6alkoxy, Ph-C0-6alkoxy,
- Het-C0-6alkoxy, OH, (CH2)1-6NR58R59, or
- O(CH2)1-6NR58R59;
- or a pharmaceutically acceptable salt, hydrate or solvate thereof.
Dependencies are inferred from the claim text.