Bristol-myers Squibb Compnay

Syngene International Limited

David Marcoux

T G Murali Dhar

Hai-Yun Xiao

Alaric J Dyckman

Michael G Yang

Zili Xiao

John L Gilmore

Robert J Cherney

Qing Shi

Douglas G Batt

Jingwu Duan

Lyndon A M Cornelius

Michael A Poss

Joseph Anthony Tino

Rajeev S Bhide

Qingjie Liu

Zheming Ruan

Anurag S Srivastava

Lan-Ying Qin

Myra Beaudoin Bertrand

Carolyn A Weigelt

Scott Hunter Watterson

Yeheng Zhu

Hua Gong

William P Gallagher

James Neels

Jason J Zhu

Tg Murali Dhar

Carlos A Guerrero

Candice Lee Joe

Shankar Tulsidas Tendulkar

Francisco González-Bobes

Sankar Kuppusamy

Rajappa Vaidyanathan

Siva Sankar Bondigela

Moorthy Kandasamy

Sathasivam Shunmugaraj

Srinivas Kalidindi

Sanjeewa Rupasinghe

John Ryan Coombs

Lyndon AM Cornelius

TG Murali Dhar

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein Ris &#x2014;OH or &#x2014;OP(O)(OH), and X, X, X, R, R, R, R, and Rare defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P, 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 bicyclic compounds

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

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), Formula (II), Formula (III), and Formula (IV) or salts thereof, wherein Ris &#x2014;OH or &#x2014;OP(O)(OH); and Ris defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P, 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 tricyclic heterocyclic compounds

There are described ROR&#x3b3; modulators of the formula (I), 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 gamma modulators

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

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Pennington, NJ, United States of America

David Marcoux