G.d. Searle & Company

Pharmacia Corporation

Other

Monsanto Company

Pfizer Corporation

Warner-lambert Company

G.d. Searle LLC

C. D. Searle & Co.

Reitz, David B.

Pulwer, Mitchell J.

Miller, William H.

David B Reitz

Robert E Manning

Jinglin J Li

Horng-Chih Huang

Len F Lee

William L Neumann

Melvin L Rueppel

Samuel J Tremont

Wei Huang

John Joseph Parlow

Darin E Jones

Brenda Case

Michael J Hayes

Shyamal C Banerjee

Raymond E Miller

Ching-Cheng Wang

John Jeffrey Talley

Thomas Dale Penning

Paul Waddell Collins

Stephen R Bertenshaw

Roland S Rogers

Michael S South

John Isidro Trujillo

Scott A Long

Richard John Lindmark

Qingping Zeng

Matthew William Mahoney

Gary W Franklin

Carrie Kusturin

Rhonda Wood

Donald W Hansen, Jr

Barnett S Pitzele

Timothy J Hagen

E Ann Hallinan

Monica B Norton

Sofya Tsymbalov

Philippe R Bovy

Robert Alan Chrusciel

William H Miller

Mitchell J Pulwer

Joe T Collins

Victor Snieckus

Danny J Garland

Andrew James Carpenter

Jinglin (James T) Li

Rondald K Webber

Tom Dice

Rick Fenton

Michael J South

Horng-Chi Huang

Joseph Gerace Rico

Susan Landis Hockerman

Karen B Peterson

James J Li

Marvin Jay Meyers

Ricky L Fenton

Xiangyang Chen

Graciela B Arhancet

Thomas A Dice

Karen H Peterson

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R, R, R, R, R, R, R, R, R, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.

Pyrazoline compounds

Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney. Conjugates of particular interest are glutamyl derivatives of biphenylmethyl 1H-substituted-1,2,4-triazole compounds, of which N-acetylglutamic acid, 5-[[4'-[(3,5-dibutyl-1H-1,2,4-triazol-1-yl)methyl][1,1&#x2032;-biphenyl]-2-yl]]carbonylhydrazide, (shown below) is an example: 

Renal-selective biphenylalkyl 1H-substituted-1,2,4-triazole angiotensin II antagonists for treatment of hypertension

The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

Substituted polycyclic aryl and heteroarpyl pyrazinones useful for selective inhibition of the coagulation cascade

A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I:wherein Y is selected from O, S and NR; wherein Ris selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein Rand Rare independently aryl or heteroaryl; and wherein Rand Rare optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.

3,4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents

Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade

A process for preparing enantiomerically enriched tetrahydrobenzothipeine oxides comprises cyclizing an enantiomerically enriched aryl-3-propanalsulfoxide wherein the sulfur atom of the aryl-3-propanalsulfoxide is a chiral center.

Method of preparing enantiomerically-enriched tetrahydrobenzothiepine oxides

A class of 1-phenyl imidazol-2-one biphenylmethyl compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formulawherein each of R, Rand Ris independently selected from hydrido, alkyl, alkoxy, cyano, halo, hydroxy, carboxyl, alkoxycarbonyl, formyl and acetyl; alkylcarbonyl and haloalkylcarbonyl; with the proviso that at least one of R, Rand Rmust be a substituent other than hydrido, and with the further proviso that when each of Rand Ris hydrido, then Rcannot be chloro; wherein Ris hydrido; wherein Ris alkyl; and wherein Ris tetrazolyl; or a stereoisomer or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.

1-phenyl imidazol-2-one biphenylmethyl compounds for treatment of circulatory disorders

The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.

Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade

Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.

Benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake

Substituted biphenyl compounds for the treatment of inflammation

3,4-diaryl thiopenes and analogs thereof having use as antiinflammatory agents

3.4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents

Growing community of inventors

Chesterfield, MO, United States of America

David B Reitz