Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2011-08-30
2011-08-30
Chu, Yong (Department: 1626)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C514S230500, C514S312000, C514S254080, C514S338000, C514S403000, C514S374000, C514S359000, C514S406000, C514S367000, C514S381000, C514S382000, C514S397000, C548S453000, C548S253000, C548S311700, C548S159000, C548S154000, C548S364400, C548S261000, C548S235000, C548S362500, C546S276700, C546S158000, C544S353000, C544S373000, C544S105000, C340S593000
Reexamination Certificate
active
08008290
ABSTRACT:
A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof,wherein:R3is selected from cyclopentyl and cyclohexyl;R9is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group.Compounds of formula (I) exhibit surprisingly high dual efficacies for human cathepsin S and K and are useful for the treatment of rheumatoid arthritis, osteoarthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, cardiovascular diseases which exhibit significant damage and remodeling of extracellular matrix (ECM) and chronic pain.
REFERENCES:
patent: WO 02057270 (2002-07-01), None
patent: WO 2008/007127 (2008-01-01), None
Hackh's Chemical Dictionary, 5th ed. McGraw-Hill, Inc., 1987.
Byrn et al. Solid-State Chemistry of Drugs, 2d, Chapter 11 Hydrates and Solvates, 233-247 (1999).
Morissette et al. Adv. Drug Delivery Rev. 56:274 (2004).
Rouhi, Chem. & Eng. News, Feb. 24, 2003, 81(8), 32-35.
International Preliminary Report on Patentability PCT/GB2009/000672 (Parent), May 24, 2010.
Flinn Nicholas S.
Quibell Martin
Watts John P.
Amura Therapeutics Limited
Barker Michael
Chu Yong
Edwards Angell Palmer & & Dodge LLP
Williams Kathleen
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