Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases.
Type:
Grant
Filed:
September 27, 2002
Date of Patent:
August 30, 2005
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Younes Bekkali, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R. R. Young, Eugene R. Hickey, Weimin Liu, Usha R. Patel
Abstract: Compounds according to the following formula (I): wherein the variables Q and R1 to R6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F, L and B; pharmaceutical compositions containing such compounds, and method of treating diseases and pathological conditions exacerbated by these cysteine proteases such as, but not limited to rheumatoid arthritis, multiple sclerosis and other autoimmune diseases, osteoporosis, asthma, Alzheimer's disease, atherosclerosis and endometriosis.
Type:
Grant
Filed:
March 27, 2003
Date of Patent:
April 12, 2005
Assignee:
Boehringer Ingelheim Pharmaceuticals Inc.
Inventors:
Thomas A. Gilmore, Eugene Richard Hickey, Weimin Liu, Peter Allen Nemoto, Denice M. Spero
Abstract: Disclosed are compounds of formula (I): wherein R1, R2, W and X of formula (I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
Type:
Grant
Filed:
August 1, 2003
Date of Patent:
March 29, 2005
Assignee:
Boehringer Ingelheim Pharmaceuticals Inc.
Inventors:
Pier Francesco Cirillo, Abdelhakim Hammach, Victor Kamhi, Neil Moss, Paul S. Riska, Christopher Pargellis
Abstract: The invention provides a method for determining whether a compound inhibits acetohydroxyacid synthase. The invention further provides a method for determining whether a plant is resistant to an acetohydroxyacid synthase inhibiting compound.