Bristol-myers Squibb Compnay

Bristol-myers Squibb Pharma Company

Other

Universitéde Montreal

Dietmar A Seiffert

Richard Eric Olson

Lorin Andrew Thompson

Robert Zaczek

Thomas J Mitchell

Jinglan Zhou

Mimi Lifen Quan

R Michael Lawrence

Edward H Ruediger

Alain Martel

Karyn O'Neil

Shoshana L Posy

Jon J Hangeland

Daniel H Deon

Jacques Banville

Michael Matthew Miller

Timothy C Burn

Marc Gagnon

Gregory Franklin Hollis

Cailan Wang

Jeffrey T Billheimer

Pancras C Wong

Julia Guy

Ira B Dicker

Robert M Knabb

François Tremblay

Leah A Breth

Jeannine M Hollis

Henry J George

Jennifer E Kochie

Jean-François Lavallée

The present invention provides imidazothiadiazole compounds of Formula (I) wherein A, B, D, R, R, R, R, X, Xand s are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments. 

Imidazothiadiazole derivatives as protease activated receptor 4 (PAR4) inhibitors for treating platelet aggregation

The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein the variables A, B, L, L, X, X, X, X, R, R, R, R, Rand Rare as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Tetrahydroquinoline derivatives useful as serine protease inhibitors

This invention relates to a novel method of screening for inhibitors of beta-amyloid production, and thereby identifying such inhibitors as therapeutics for neurological and other disorders involving APP processing and beta-amyloid production. This invention also relates to identifying macromolecules involved in APP processing and beta-amyloid production. Furthermore, inhibitors identified by the screening method of the present invention are useful in the treatment of neurological disorders, such as Alzheimer's disease, which involve elevated levels of A&#x3b2; peptides.

Use of small molecule radioligands to discover inhibitors of amyloid-beta peptide production and for diagnostic imaging

The present invention is directed generally to methods and composition for monitoring the processing of epitope-tagged beta-APP. More specifically, the present invention relates to the use of such methods and composition for monitoring responses of cells expressing such epitope-tagged beta-APP or fragments thereof or cell free systems containing the epitope-tagged polypeptides to therapy of diseases associated with an altered metabolism of the beta amyloid precursor protein (APP), and for screening and evaluation of potential drugs for the treatment of these disorders, including Alzheimer's disease (AD).

Epitope-tagged beta-amyloid precursor protein and DNA encoding the same

A method of using radiolabelled and/or radiopharmaceutical small molecule inhibitors of beta-amyloid peptide production for the diagnosis of neurological and other disorders involving APP processing and beta-amyloid production. Radiolabelled small molecule inhibitors identified by the methods of the present invention would be useful in the diagnosis of neurological disorders, such as Alzheimer's disease, which involve elevated levels of A&#x3b2; peptides.

This invention relates to a novel method of screening for inhibitors of beta-amyloid production, and thereby identifying such inhibitors as therapeutics for neurological and other disorders involving APP processing and beta-amyloid production. This invention also relates to identifying macromolecules involved in APP processing and beta-amyloid production. Furthermore, inhibitors identified by the screening method of the present invention are useful in the treatment of neurological disorders, such as Alzheimer's disease, which involve elevated levels of A&bgr; peptides.

Detection of patients at risk for developing integrin antagonist/agonist mediated disease states

Method for screening compounds to identify beta-amyloid production modulators

Use of small molecule radioligands to discover inhibitors of amyloid-beta peptide production

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Boothwyn, PA, United States of America

Dietmar A Seiffert