E.i. Dupont De Nemours and Company

Bristol-myers Squibb Compnay

Bristol-myers Squibb Pharma Company

The Dupont Merck Pharmaceutical Company

James M Trzaskos

Ronald L Magolda

Carl P Decicco

Timothy C Burn

Micky Daniel Tortorella

Robert A Copeland

Ruiqin Liu

Michael A Pratta

Elizabeth C Arner

Fude Yang

Kimberly A Solomon

Soo Sung Ko

Paul R Johnson

Simon H Stam

James L Gaylor

George A Boswell

Peter John Gillies

Jeffrey T Billheimer

Indawati De Lucca

Spencer Drummond, Jr

The invention is directed to the family of aggrecan degrading metallo proteases (ADMPs) that exhibit the ability to cleave the aggrecan core protein between amino acid residues Glu-Ala. The invention encompasses the nucleic acids encoding such enzymes, processes for production of recombinant ADMPs, compositions containing such enzymes, and the use of these enzymes in various assays and for the development of novel inhibitors for use as therapies for diseases involving aggrecanase-mediated degradation of cartilage or other aggrecanase-associated diseases.

Antibodies to aggrecan-degrading metalloprotease and diagnostic methods using same

The invention is directed to the family of aggrecan degrading metallo proteases (ADMPs) that exhibit the ability to cleave the aggrecan core protein between amino acid residues Glu -Ala . The invention encompasses the nucleic acids encoding such enzymes, processes for production of recombinant ADMPs, compositions containing such enzymes, and the use of these enzymes in various assays and for the development of novel inhibitors for use as therapies for diseases involving aggrecanase-mediated degradation of cartilage or other aggrecanase-associated diseases.

Aggrecan degrading metallo proteases

Nucleic acids encoding aggrecan degrading metallo proteases

Antihypercholesterolemic bis-trifluoromethyl-substituted imidazolines

The present invention relates to novel substituted 15-oxa-, 15-thia-, and 15-aza- dihydrolanosterols, to pharmaceutical compositions containing such compounds, and to methods of using these compounds to suppress the activity of 3-hydroxy-3- methylglutaryl coenzyme A reductase (HMGR), an enzyme which is important in cholesterol biosynthesis. The overall effect of these heterocyclic lanosterol analogs is to decrease cholesterol formation, thereby resulting in lower serum cholesterol levels in mammals, and impaired ergosterol synthesis in fungi.

Heterocyclic steroid compounds

Lanosterols substituted in the 14 and/or 15 position(s) which are active in inhibiting lanosta-8,24-dien-3.beta.-ol 14.alpha.-methyl-demethylase activity, suppressing 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR) activity, decreasing cholesterol synthesis and reducing serum cholesterol levels are disclosed.

Steroid derivatives useful as hypocholesterolemics

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Boothwyn, PA, United States of America

James M Trzaskos