Merck + Co., Inc.

Shu S Yang

Michael N Chang

Yuan-Ching P Chiang

Donald W Graham

John C Chabala

James V Heck

Kathryn L Thompson

Richard L Tolman

Tesfaye Biftu

Tsung-Ying Shen

Bruce E Witzel

Conrad P Dorn

Gary H Rasmusson

Thomas R Beattie

Howard Jones

Philippe L Durette

Timothy Francis Gallagher

Raman Kumar Bakshi

David Penman Jacobus

Narindar N Girotra

San-Bao Hwang

Michael D Lewis

Narindar M Girotra

Ester derivatives of 4-aza-steroids

17-Ethers and thioethers of 4-aza-steroids

Novel 1,3-Diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediated by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.

1,3-diaryl cyclopentanes and derivatives thereof as PAF antagonists

This application relates to compounds of formula (I), which are useful as antihypercholesterolemic agents. ##STR1##

Beta-lactams as antihypercholesterolemics

Novel 1,3-diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediate by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.

Compounds of formula (I), which are useful as antihypercholesterolemic agents, are disclosed. ##STR1##

Beta-lactams as anticholesterolemic agents

This invention relates to acetylenic cyclic carbonates that are useful in the treatment of fungal diseases and hypercholesterolemic conditions.

Acetylenic cyclic carbonates

The compounds of the following general structural formula (I) ##STR1## are 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) synthase inhibitors and useful as antihypercholesterolemic agents for the treatment of disease in which the inhibition of cholesterol biosynthesis would be useful, such as arteriosclerosis, hyperlipidemia and familial hypercholesterolemia.

Antihypercholesterolemic .beta.-lactones

The compounds of the following structural formula (I) ##STR1## ar 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) synthase inhibitors and useful as antihypercholesterolemic agents for the treatment of disease in which the inhibition of cholesterol biosynthesis would be useful, such as arteriosclerosis, hyperlipidemia and familial hypercholesterolemia.

The compounds of the following structural formula (I) ##STR1## are 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) synthase inhibitors and useful as antihypercholesterolemic agents for the treatmet of disease in which the inhibition of cholesterol biosynthesis would be useful, such as arteriosclerosis, hyperlipidemia and familial hypercholesterolemia.

Antihypercholesterolemic beta-lactones

Indene derivatives have been found to have potent and specific PAF (Platelet-Activating-Factor) antagonistic activities and are thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, and adult respiratory distress syndrome.

Indene derivatives and their use as PAF-antagonists

Phosphatidyl inositol analogs are found to be effective phospholipase C inhibitors and thereby potent anti-inflammatory and analgesic agents. These phosphatidyl inositol analogs are prepared by condensation of a protected inositol with a substituted phosphonic or phosphorous acid followed by removal of protecting groups.

Phosphatidyl inositol analogs useful as anti-inflammatory/analgesic

Sulfonyl or carbonyl derivatives of inositols are found to be effective phospholipase C inhibitors and thereby potent anti-inflammatory and analgesic agents. These inositol derivatives are prepared by condensation of a protected inositol with a substituted sulfonic or carboxylic acid derivative followed by removal of protecting groups.

Sulfonyl or carbonyl inositol derivatives useful as

Novel cholecalciferol and dihydrotachysterol.sub.3 derivatives produced against metabolic conversions at the 25-position, their preparation, pharmaceutical compositions, methods of treating steroid-induced osteoporosis, senile osteoporosis and secondary hyperparathyroidism, especially that induced by an insufficient amount of calcium in relationship to the amount of phosphate, novel intermediates and their preparation are disclosed.

Blocked cholecalciferol and dihydrotachysterol 3 derivatives

Certain novel peptide carbazates, their preparation, pharmaceutical compositions and novel methods of treating pancreatitis.

Growing community of inventors

Bridgewater, NJ, United States of America

Shu S Yang