Smithkline Beecham Corporation

Smithkline Beckman Corporation

Dimitri E Gaitanopoulos

Joseph Weinstock

Jack Dale Leber

Mei Li

Robert Gene Franz

Bruce Mico

This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.

Fatty acid synthase inhibitors

Macrophage scavenger receptor antagonists are provided. Methods of treating cardiovascular disease comprising administration of the present compounds are also provided. The present compounds inhibit lipid accumulation within macrophage-derived foam cells.

Macrophage scavenger receptor antagonists

Angiotensin II receptor antagonists having tile formula: ##STR1## or a pharmaceutically acceptable salt thereof which are useful in regulating hypertension and in the treatment of congestive heart failure, renal failure, and glaucoma, pharmaceutical compositions including these antagonists, and methods of using these compounds to produce angiotensin II receptor antagonism in mammals. These antagonists function as prodrugs in vivo.

Imidazolyl-alkenoic acids

Prodrug carbamate derivatives of fenoldopam which provide fenoldopam plasma levels of similar magnitude and over a much longer period of time than the parent compound. An absence of a high initial peak effect associated with the parent compound is noted. A lead compound of the series is 6-chloro-7,8-diethylcarbamoyl-1-(4'-ethylcarbamoylphenyl)-2,3,4,5-tetrahyd ro-1H-3-benzazepine. The R-enantiomers are the most biologically active and preferred compounds.

Carbamates of

Fenoldopam 4',8-bis-hydrogen sulfate and its salts are useful prodrugs to obtain extended dopaminergic activity. A useful species is the monoammonium salt.

Fenoldopam 4',8-bis-hydrogen sulfate and dopaminergic use thereof

3-Carboxy-2-(.omega.-carboxyalkanoyl)-2-azabicyclo-[2.2.1]heptenes have been demonstrated to improve kidney function. 3-Carboxy-2-azabicyclo[2.2.1]heptane and its esters are important new chemical intermediates.

Growing community of inventors

Eaglesville, PA, United States of America

Dimitri E Gaitanopoulos