Merck + Co., Inc.

Yuan-Ching P Chiang

Michael N Chang

Shu S Yang

James V Heck

John C Chabala

Donald W Graham

Sander G Mills

Tesfaye Biftu

Malcolm MacCoss

Kathryn L Thompson

Shrenik K Shah

Paul E Finke

Albert J Robichaud

Michael D Lewis

Robert M Burk

William H Parsons

Conrad P Dorn

Jeffrey John Hale

Charles G Caldwell

Mitree M Ponpipom

Robert L Bugianesi

John J Acton, Iii

Hiroo Koyama

Conrad Santini

Narindar N Girotra

Gregory D Berger

Laura C Meurer

Claude Dufresne

Chan-Hwa Kuo

James D Bergstrom

Daniel J Miller

Robert W Marquis, Jr

Lori L Whiting

Sandra P Plevyak

Narindar M Girotra

Patrick T Dunn

Disclosed are spiro-substituted azacycles of formula I are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma. In particular compounds of formula I are shown to be neurokinin antagonists.

Spiro-substituted azacycles as neurokinin antagonists

The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, m, n and the dashed lines are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.

Phenyl spiroethercycloalkyl tachykinin receptor antagonists

Disclosed are substituted aryl piperazines of Formula I ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis. In particular compounds of Formula I are shown to be neurokinin antagonists.

Substituted aryl piperazines as neurokinin antagonists

Cholesterol lowering compounds

Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents and as inhibitors of squalene synthase.

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.

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

Triyne cyclic carbonates

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## 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

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Piscataway, NJ, United States of America

Yuan-Ching P Chiang