Bristol-Myers Squibb Compnay

Bristol-Myers Squibb Pharma Company

The Dupont Merck Pharmaceutical Company

Dupont Pharmaceuticals Company

Bristol-Myers Squibb Pharmaceutical Company

Robert J Cherney

Percy H Carter

John V Duncia

Daniel S Gardner

T G Murali Dhar

Anurag S Srivastava

Douglas G Batt

Michael G Yang

Jingwu Duan

Soo Sung Ko

David Marcoux

Steven P Seitz

Lyndon A M Cornelius

Joseph Anthony Tino

Joseph B Santella

Qingjie Liu

Qing Shi

Lan-Ying Qin

Michael A Poss

Michael J Orwat

Scott Hunter Watterson

Hai-Yun Xiao

Carl P Decicco

Rajeev S Bhide

Zhongyu Wang

Zheming Ruan

Robert F Kaltenbach

Irina Cipora Jacobson

Gregory James Pacofsky

Arthur D Patten

Emeka A Akamike

Percy Carter

Deqiang Niu

Jagabandhu Das

Jun Li

Alaric J Dyckman

John T Hynes

Ramesh Kumar Sistla

Matthew Ernst Voss

Zili Xiao

William F DeGrado

Jung-Hui Sun

Khehyong Ngu

Manoranjan Panda

Boris M Seletsky

Venkatram Reddy Paidi

Ronald L Magolda

Hua Gong

Srinivasan Thangathirupathy

Victor W Rosso

Julio Hernan Cuervo

Xiao Zhu

Charles Malcolm Langevine

Kumaravel Selvakumar

Lihua Chen

Yanlei Zhang

James Neels

Myra Beaudoin Bertrand

Gregory D Brown

Jianqing Li

Carolyn A Weigelt

Tg Murali Dhar

Xiaohua He

Siva Josyula Prasad

Robert Frank Kaltenbach, Iii

Carl Peter DeCicco

Alyssa H Antropow

Bryan W King

Vijaya Kumar Cm

Mallikarjun Reddy Sura

Tirupathi Rao Alajangi

Krishna Mahadevu

Piyush Agarwal

Ooha Morampudi

Audrey Graham Ross

Paul E Gormisky

Zhengdong Zhu

Guobin Miao

Jalathi S Nair

Arul Mozhi Subbiah Karuppiah

Chu-Bio Xue

Elizabeth Arner

David Nelson

Lyndon AM Cornelius

TG Murali Dhar

Charles M Langevine

Anurag Srivastava

Jale Muslehiddinoglu

Martin G Eastgate

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

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

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

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) 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

Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X, X, X, W, Q, Q, and Gare 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.

Tricyclic heterocyclic compounds

The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.

N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-A][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, a dual modulator of chemokine receptor activity, crystalline forms and processes

Disclosed are compounds of Formula (I) or stereoisomers, salts, or prodrugs thereof, wherein: Q is, or Ris phenyl substituted with zero to 3 substituents; and R, R, R, R, R, and G 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. 

Mandelamide heterocyclic compounds

The present application describes the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed.

Piperidinyl compound as a modulator of chemokine receptor activity

Disclosed are compounds of Formula (I) or stereoisomers, salts, or prodrugs thereof, wherein: W is CHor O; Q is Formula (II), Formula (III) or Formula (IV); and R, R, R, R, n, and G are 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. 

Heterocyclic compounds as S1P1 agonists for the treatment of autoimmune and vascular diseases

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Newtown, PA, United States of America

Robert J Cherney