Merck + Co., Inc.

Smithkline Beecham Corporation

Nps Pharmaceuticals, Inc.

Versicor, Inc.

Nbs Pharmaceuticals, Inc.

Robert L Smith

Edward J Cragoe, Jr

Gerald E Stokker

Ta-Jyh Lee

William F Hoffman

John B Bicking

Ta J Lee

Mark G Bock

Alvin K Willard

Samuel L Graham

S Jane deSolms

George D Hartman

Neville J Anthony

Clarence S Rooney

Wasyl Halczenko

Otto D Hensens

Manuel F Balandrin

Edward S Inamine

Edward M Scolnick

Linda D Artman

David R Houck

Albert A Deana, Deceased

Otto W Woltersdorf, Jr

James Francis Callahan

Donald E Kuhla

Pradip Kumar Bhatnagar

Bradford C Van Wagenen

Maria Amparo Lago

Joelle Lorraine Burgess

Robert M Barmore

Eric G Del Mar

Derek Sheehan

Linda Sue Southall

Thomas The Nguyen

Edward J Gragoe, Jr

Raul Rolando Calvo

William M Bryan

Gnanasambandam Kumaravel

Preparations and extracts of valerian, as well as isovaleramide, isovaleric acid, and certain structurally related compounds, exhibit clinically significant pharmacological properties that implicate a treatment for a variety of pathological conditions, including spasticity and convulsions, which are ameliorated by effecting a modulation of CNS activity. The compositions in question generally are non-cytotoxic and do not elicit weakness or sedative activity at doses that are effective for the symptomatic treatment of such pathological conditions.

Treating a variety of pathological conditions, including spasticity and convulsions, by effecting a modulation of CNS activity with isovaleramide, isovaleric acid, or a related compound

Preparations and extracts of valerian, as well as isovaleramide, isovaleric acid, and certain structurally related compounds exhibit clinically significant pharmacological properties which implicate a treatment for a variety of pathological conditions, including spasticity and convulsions, which are ameliorated by effecting a modulation of CNS activity. The compositions in question generally are non-cytotoxic and do not elicit weakness or sedative activity at doses that are effective for the symptomatic treatment of such pathological conditions.

Novel arylalkylamino compounds exhibiting calcilytic properties are provided.

Calcilytic compounds

The subject invention features substituted N-heteroaromatic compounds, libraries of substituted N-heteroaromatic compounds, and methods of synthesis thereof. For example, the present invention provides methods for synthesizing substituted N-heteroaromatic compounds, and is particularly amenable to the generation of libraries of substituted N- heteroaromatic compounds by combinatorial chemistry. The methods of the invention generally feature the reaction of O-linked heteroaromatic N-oxides with nucleophiles to produce substituted N-heteroaromatic compounds.

Synthesis of substituted N-heteroaromatic compounds and methods of use

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 present invention is directed to farnesyl pyrophosphate analogs 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.

Farnesyl pyrophosphate analogs

Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formula (II): ##STR1##

HMG-CoA reductase inhibitors

Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as anti-hypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1##

Novel HMG-CoA reductase inhibitors

Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1## and pharmaceutically acceptable salts of the compounds (II) in which Z is hydrogen are disclosed.

Antihypercholesterolemic compounds

Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1##

Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) or (II): ##STR1## wherein: n is 1 to 5;

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Lansdale, PA, United States of America

Robert L Smith