Bristol-myers Squibb Compnay

Cerep Sa

Other

Exelixis, Inc.

T G Murali Dhar

Hai-Yun Xiao

Edwin J Iwanowicz

Alaric J Dyckman

Jingwu Duan

John L Gilmore

Bin Jiang

Zili Xiao

Michael G Yang

Zhonghui Lu

Robert J Cherney

Scott Hunter Watterson

Bingwei Vera Yang

Eric Nicolai

Katerina Leftheris

William John Pitts

Stephen T Wrobleski

John T Hynes

David S Weinstein

James Edward Sheppeck

Jagabandhu Das

Douglas G Batt

John V Duncia

Joseph Anthony Tino

Chunjian Liu

Daniel S Gardner

Ping Chen

Gregory S Bisacchi

James M Lin

Qingjie Liu

Deqiang Niu

Wei Xu

Michael A Poss

Joseph B Santella

Dharmpal S Dodd

Wayne D Vaccaro

Joel C Barrish

Soo Sung Ko

Percy H Carter

Rajeev S Bhide

Yong Wang

Elena S Koltun

Ramesh Kumar Sistla

Yufen Zhao

Lynne Canne Bannen

Zulan Pi

Jianmin Wang

Jack Z Gougoutas

Yeheng Zhu

Arthur M P Doweyko

David Marcoux

Michele Launay

Dominique Potin

Henry H Gu

Magali Jeannine Blandine Maillet

Hua Gong

Arun Kumar Gupta

Carolyn A Weigelt

Ananta Karmakar

Lyndon A M Cornelius

Lidia M Doweyko

Timothy F Herpin

Shuqun Lin

Weiwei Guo

Qing Shi

Lan-Ying Qin

Myra Beaudoin Bertrand

Arthur M Doweyko

David R Tortolani

Chenkou Wei

Boris M Seletsky

Manoranjan Panda

Khehyong Ngu

Tram N Huynh

Venkatram Reddy Paidi

Toomas Mitt

Marta Dabros

Srinivasan Thangathirupathy

Julio Hernan Cuervo

Zheming Ruan

Charles Malcolm Langevine

Xiao Zhu

Anurag S Srivastava

Kumaravel Selvakumar

Sunghoon Ma

Mary F Malley

Yu Fan

Ling Li

E Scott Priestley

Byung Gyu Kim

Jianqing Li

Daniel Richard Roberts

Joon Won Jeong

Douglas D McLeod

Alyssa H Antropow

Albert J DelMonte

Eric J Chan

Robert E Waltermire

Ning Li

Edwin J Iwan Wicz

wherein and X-Xand R-R, along with other variables are as defined herein. The disclosure generally relates to substituted heterocyclic compounds of Formula (Ia), which are inhibitors of PAD4, method for preparing these compounds, pharmaceutical compositions comprising these compounds and use of these compounds in the treatment of a disease or a disorder associated with PAD4 enzyme activity.

Heterocyclic PAD4 inhibitors

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

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.

ROR &#x3b3; modulators

Disclosed are compounds of Formula (I): (I) or a salt thereof, wherein: X is CH or N; Y is CH or N; Ris &#x2014;OH or &#x2014;OP(O)(OH); L is &#x2014;CR&#x2550;N&#x2014;O&#x2014;CRR&#x2014; or CRR&#x2014;O&#x2014;N&#x2550;CR; Lis a bond, &#x2014;C(O)&#x2014;, or S(O)&#x2014;; and R, R, R, m, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P1, 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. 

Oxime ether compounds

There are described RORmodulators 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 RORactivity 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 RORactivity, for example, autoimmune and/or inflammatory disorders. 

Tricyclic sulfones as RORmodulators

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; Gamma 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; Gamma activity, for example, autoimmune and/or inflammatory disorders. 

Heterocyclic sulfones as ROR gamma modulators

Disclosed are compounds of Formula (I) or a salt thereof, wherein: A is CRor N; B is CRor N; D is CRor N; Lis &#x2014;(CRR)&#x2014;; Lis &#x2014;(CRR)&#x2014;; and X, Z, R, R, R, R, R, and Rare define herein. Also disclosed are methods of using such compounds as modulators of TNF&#x3b1;, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases. 

Heterocyclic compounds useful as modulators of TNF alpha

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 is described a ROR&#x3b3; modulator of the formula (I), or stereoisomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof. Also provided are pharmaceutical compositions comprising the same. The compound of the invention may be 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 sulfone compound as a ROR gamma modulator

Tricyclic sulfones as ROR gamma modulators

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Newtown, PA, United States of America

T G Murali Dhar