Bristol-myers Squibb Compnay

Anurag S Srivastava

Douglas G Batt

Soo Sung Ko

Robert J Cherney

Scott Hunter Watterson

Qingjie Liu

Qing Shi

Myra Beaudoin Bertrand

Joseph Anthony Tino

Michael G Yang

Percy H Carter

Charles Malcolm Langevine

John V Duncia

Daniel S Gardner

George V Delucca

Michael A Galella

David Marcoux

Lyndon A M Cornelius

Jagabandhu Das

T G Murali Dhar

Michael A Poss

Jingwu Duan

John T Hynes

Rajeev S Bhide

Zili Xiao

Khehyong Ngu

Zheming Ruan

Lan-Ying Qin

Robert V Moquin

James Neels

George V De Lucca

Carolyn A Weigelt

Tg Murali Dhar

Soo S Koo

Lyndon AM Cornelius

Charles M Langevine

The present invention provides compounds of Formula (I) useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders, wherein each of Ring A, L, Q, R1, R2, R3, R4, R7, and R8 along with other variables are as defined herein. 

Indole and azaindole inhibitors of pad enzymes

Disclosed are compounds of Formula (I) wherein: the two dotted lines represent either two single or two double bonds; Q is: Ris F, Cl, &#x2014;CN, or &#x2014;CH; Ris Cl or &#x2014;CH; Ris &#x2014;C(CH)OH or &#x2014;CHCHOH; Ris H or &#x2014;CH; each Ris independently F, Cl, &#x2014;CH, and/or &#x2014;OCH; and n is zero, 1, or 2. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

Substituted tetrahydrocarbazole and carbazole carboxamide compounds

Disclosed are compounds of Formula (I) or a salt thereof; wherein: X is N or CH; Qis: (i) Cl, Br, I, &#x2014;CN, &#x2014;CH, or &#x2014;CF; (ii) a 5-membered heteroaryl selected from pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, oxadiazolyl, and thiadiazolyl; (iii) a 6?membered heteroaryl selected from pyridinyl, pyridazinyl, and pyrimidinyl; or (iv) a bicyclic heteroaryl selected from indolyl, pyrrolopyridinyl, pyrazolopyridinyl and benzo[d]oxazolyl; wherein each of said 5-membered, 6-membered, and bicyclic heteroaryl is substituted with zero to 1 Rand zero to 1 R; and R, R, R, R, R, R, R, and Rare defined herein. Also disclosed are methods of using such compounds as modulators of PI3K, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases. 

Bicyclic heteroaryl amine compounds

There are described ROR&#x3b3; modulators of the formula (I), and formula (II) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR&#x3b3; activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR&#x3b3; activity, for example, autoimmune and/or inflammatory disorders.

Tricyclic sulfones as ROR&#x3b3; modulators

Disclosed are compounds of Formula (I); and salts thereof, wherein: Formula (II); Q is: Ris &#x2014;C(CH)2OH, &#x2014;NHC(=0)C(CH), &#x2014;N(CH3)2, or &#x2014;CHR; Ris CI or &#x2014;CH; Ris H, F, or &#x2014;CH; Ris H or &#x2014;CH; Ris H, F, CI, or &#x2014;OCH3 Ris H or F; and Rd is &#x2014;OH, &#x2014;OCH3, &#x2014;NHC(=0)CH3, or fORMULA (III), Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease. 

Carbazole carboxamide compounds

Disclosed are compounds of Formula (I): (I) or stereoisomers, salts, or prodrugs thereof, wherein: (i) R1 and R2 are independently C-Calkyl, or (ii) Rand Rtogether with the carbon atom to which they are attached, form a cyclic group; and Q is H, Calkyl, phenyl or 5- to 6-membered heteroaryl substituted with zero to 3 substituents, and G is defined herein. Also disclosed are method of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. There compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and chronic inflammatory disease. 

Substituted 3-phenyl-1,2,4-Oxadiazole compounds

The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the treatment of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.

Cyclic derivatives as modulators of chemokine receptor activity

This invention relates generally to modulators of chemokine receptor activity having unexpected combination of desirable pharmacological properties. Pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and prevention of inflammatory, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases, particularly diabetes, Crohn's disease, atherosclerosis, and multiple sclerosis, along with methods of preparing compounds and intermediates therefor. Metabolites of active compounds are also provided herein, pharmaceutical compositions and use thereof are also provided.

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Belle Mead, NJ, United States of America

Anurag S Srivastava