Bristol-myers Squibb Compnay

Bristol-myers Squibb

Andrew K Dilger

Kumar Balashanmuga Pabbisetty

William R Ewing

Donald J P Pinto

Wu Yang

Leon M Smith, Ii

James R Corte

Michael J Orwat

Yufeng Wang

Tianan Fang

Yeheng Zhu

Indawati De Lucca

Ruth Richmond Wexler

Scott A Shaw

Peter W Glunz

Nicholas Ronald Wurtz

Ellen K Kick

Paul Joseph Gilligan

Manoranjan Panda

Vladimir Ladziata

Sutjano Jusuf

Meriah Neissel Valente

Benjamin P Vokits

Andrew Quoc Viet

Indawati DeLucca

Donald Jp Pinto

Leon M Smith

Ginger Chao Rakestraw

Joanne M Smallheer

Stanley Richard Krystek, Jr

Charles G Clark

Aaron Yamniuk

Steven Sheriff

Lumelle A Schneeweis

Jason Robert Pinckney

Christina Terragni

Joseph M Luettgen

Yongmi An

Kevin Kish

Leon M Smith Ii

Donald JP Pinto

Leon M Ii Smith

Donald JP Pinto Pinto

The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Pyrimidinones as factor XIA inhibitors

The present invention provides novel antigen binding peptides, such as an antibody or antibody fragment, that specifically bind to selective FXIa inhibitors and/or dual inhibitors of FXIa, and plasma kallikrein. The present invention further relates to methods of reducing the antithrombotic effect of FXIa inhibitors by administering to a subject a pharmaceutically effective dose of the antigen binding peptides provided herein. In addition, the present invention provides detection reagents and methods for detecting the level of the inhibitors of FXIa in a biological sample.

Antibodies and antigen binding peptides for factor XIa inhibitors and uses thereof

The present invention provides compounds of Formula (1): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

The present invention provides compounds of Formula (I); wherein the substituents are each as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, and may be useful for the treatment and/or prophylaxis of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases. 

Triazolopyridine inhibitors of myeloperoxidase and/or EPX

The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

Spiroheptane salicylamides and related compounds as inhibitors of ROCK

The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same. 

Spirolactams as inhibitors of ROCK

The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same. 

Factor XIa macrocycle inhibitors bearing a non-aromatic P2' group

The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same. 

Spiroheptane salicylamides and related compounds as inhibitors of rock

Pyrimidinones as factor XIa inhibitors

The present invention provides compounds of Formula (I): wherein A, Y and Rare each as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments. 

Triazolopyridine inhibitors of myeloperoxidase

Factor XIa macrocyclic inhibitors bearing alkyl or cycloalkyl P2' moieties

The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Macrocyclic factor XIa inhibitors bearing heterocyclic groups

The present invention provides compounds of Formula (V):  or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Dihydropyridone P1 as factor XIa inhibitors

The present invention provides compounds of Formula (I): wherein A and Rare each as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments. 

Triazolopyridine and triazolopyrimidine inhibitors of myeloperoxidase

Macrocycles with aromatic P2' groups as factor xia inhibitors

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Ewing, NJ, United States of America

Andrew K Dilger