Merck + Co., Inc.

Jeffrey P Bergman

Richard L Tolman

Soumya P Sahoo

Ranjit C Desai

Victoria K Lombardo

Conrad Santini

Wei Han

Christopher J Dinsmore

Hiroo Koyama

Julia K Boueres

Dominick F Gratale

Edward J Metzger

Theresa M Williams

Bruce E Witzel

Donald W Graham

Gary H Rasmusson

Alan D Adams

Derek J Von Langen

Gregory D Berger

Joel Peter Berger

David E Moller

Mark D Leibowitz

Jonthan R Young

Substituted 5-aryl-2,4-thiazolidinediones and oxazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR &agr; and/or &ggr; mediated diseases, disorders and conditions.

Arylthiazolidinedione derivatives

Arylthiazolidinedione and aryloxazolidinedione derivatives

Substituted 5-aryl-2,4-thiazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR &agr;, &dgr; and/or &ggr; mediated diseases, disorders and conditions.

Arylthiazolidinedione derivitives

Substituted 5-aryl-2,4-thiazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR .alpha., .delta. and/or .gamma. mediated diseases, disorders and conditions.

The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Inhibitors of farnesyl-protein transferase

The instant invention is concerned with acetylphenols which are useful as antiobesity and antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering or modulating triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility or for treating atherosclerosis are also disclosed.

Antidiabetic agents

17-amino substituted 4-azasteroid 5.alpha.-reductase inhibitors

Compounds of the formula I ##STR1## wherein R.sub.1 hydrogen or methyl; R.sub.2 is methyl; R.sub.3 hydrogen, Alk-R.sub.4, X-Alk, C.sub.1-6 -X-Alk, XCO-Alk, CN, CO-Alk, CO-Ar, CO-O-Alk, CO-NH-Alk, CO-NH-Ar, CO-NH-Het and CO-N(Alk).sub.2 ; Alk is C.sub.1-12 straight or branched alkyl; Ar is phenyl, Het is piperidinyl, piperizinyl, pyrrolidinyl, pyrrolyl, furanyl or thienyl and X is O, N or S. Such compounds are useful in the treatment of pathologic conditions that benefit from blockade of isozymes of 5.alpha.-reductase.

7-substituted-.delta.4-6-azasteroid derivatives as 5.alpha.-reductase

Growing community of inventors

Tenafly, NJ, United States of America

Jeffrey P Bergman