Bristol-myers Squibb Compnay

Syngene International Limited

Qing Shi

Douglas G Batt

Qingjie Liu

Joseph Anthony Tino

Anurag S Srivastava

Scott Hunter Watterson

George V Delucca

David Marcoux

Myra Beaudoin Bertrand

Soo Sung Ko

Robert J Cherney

Andrew J Tebben

Charles Malcolm Langevine

Lyndon A M Cornelius

Michael A Galella

T G Murali Dhar

Michael A Poss

Jingwu Duan

Rajeev S Bhide

Zheming Ruan

Lan-Ying Qin

George V De Lucca

Chunjian Liu

Hua Gong

William P Gallagher

James Neels

Jason J Zhu

Carolyn A Weigelt

Carlos A Guerrero

Candice Lee Joe

John Ryan Coombs

Sanjeewa Rupasinghe

Srinivas Kalidindi

Sathasivam Shunmugaraj

Moorthy Kandasamy

Siva Sankar Bondigela

Rajappa Vaidyanathan

Shankar Tulsidas Tendulkar

Sankar Kuppusamy

Francisco González-Bobes

Lyndon AM Cornelius

Charles M Langevine

TG Murali Dhar

The invention generally relates to a process for preparing compounds, including Compound of Formula (I), useful as key intermediates in the preparation of compounds having ROR&#x3b3;t antagonist properties. 

Synthetic process

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

Disclosed are compounds of Formula (I); or a salt thereof; wherein Qi is (i) Cl, Br, I, &#x2014;CN, &#x2014;CH, or &#x2014;CF; or (ii) pyrazole, triazole, or pyridinyl, each substituted with R; Qis pyridinyl, indazolyl, isoquinolinyl, or benzo[d]imidazolyl substituted with Rand R; and 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. 

Heteroaryl substituted pyrrolotriazine amine compounds as PI3K inhibitors

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 nicotinamide compounds of Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. Also disclosed are methods of using such compounds in the treatment of at least one Btk associated condition, such as, for example, inflammatory disease, and pharmaceutical compositions comprising such compounds. 

Nicotinamide compounds useful as kinase modulators

Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.

Carbazole carboxamide compounds useful as kinase inhibitors

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Princeton, NJ, United States of America

Qing Shi