Bristol-myers Squibb Compnay

Bristol-myers Squibb Pharma Company

Other

Bristol-myers Squibb Pharma Corporation

John V Duncia

Joseph B Santella

Daniel S Gardner

Dean A Wacker

Soo Sung Ko

George V DeLucca

John T Hynes

Percy H Carter

Satheesh Kesavan Nair

Hong Wu

Venkatram Reddy Paidi

Robert J Cherney

Ramesh Kumar Sistla

Michael G Yang

Natesan Murugesan

Sreekantha Ratna Kumar

Ui Tae Kim

Douglas G Batt

William John Pitts

Rajeev S Bhide

Changsheng Zheng

Wenqing Yao

T G Murali Dhar

Paul Steven Watson

Kandhasamy Sarkunam

John E Macor

Dharmpal S Dodd

David S Weinstein

Zili Xiao

George V Delucca

Cullen L Cavallaro

Deqiang Niu

Joseph Anthony Tino

Steven H Spergel

Rulin Zhao

Jayakumar Sankara Warrier

Boguslaw Mudryk

Khehyong Ngu

Anurag S Srivastava

Xiao Zhu

Weiwei Guo

Tg Murali Dhar

Rui-Qin Liu

Cheryl McArdle Clark

Subba Rao Polimera

Boris M Seletsky

Manoranjan Panda

Zhongyu Wang

Srinivasan Thangathirupathy

Julio Hernan Cuervo

Lyndon A M Cornelius

Kumaravel Selvakumar

Gregory D Brown

Michael E Randazzo

Alyssa H Antropow

Jeffrey G Varnes

Audrey Graham Ross

Paul E Gormisky

Zhengdong Zhu

Ooha Morampudi

Guobin Miao

Jalathi S Nair

Arul Mozhi Subbiah Karuppiah

Piramanayagam Arunachalam

Joseph B Santella Iii

Durgarao Kantheti

Vijaya Kumar Cm

Mallikarjun Reddy Sura

Tirupathi Rao Alajangi

Krishna Mahadevu

Piyush Agarwal

Lyndon AM Cornelius

TG Murali Dhar

Natessan Murugesan

Boguslaw M Mudryk

Christopher Annunziato

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.

Substituted thienopyrroles as PAD4 inhibitors

Compounds of formula (I) or a stereoisomer or pharmaceutically-acceptable salt thereof, are useful in the modulation of IL-12, IL-23 and/or IFN&#x3b1;, by acting on Tyk-2 to cause signal transduction inhibition. 

Substituted imidazo[1,2-b]pyridazines as interleukin-23 and interferon-&#x3b1; modulators

Disclosed are compounds of Formula (I) Formula (I) or salts thereof, wherein HET is a heteroaryl selected from oxazolyl, pyrazolyl, imidazo[1,2-b]pyridazin-3-yl, and pyrazolo[1,5-a]pyrimidin-3-yl, wherein said heteroaryl is attached to the pyridinyl group in the compound of Formula (I) by a carbon ring atom in the heteroaryl and wherein said heteroaryl is substituted with zero to 2 R; and R, R, and Rare define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer. 

Heteroaryl substituted aminopyridine compounds

Compounds having the following formula: or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein Ris a monocyclic heteroaryl group, and R, R, R, Rand Rare as defined herein, are useful as kinase modulators, including IRAK-4 inhibition.

Heteroaryl substituted pyridyl compounds useful as kinase modulators

Disclosed are compounds of Formula (I) or salts thereof, wherein HET is a heteroaryl selected from pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3 d]pyrimidinyl, pyrazolo[3,4 b]pyridinyl, pyrazolo[3,4 d]pyrimidinyl, imidazolo[4,5 b]pyridinyl, and imidazolo[4,5 d]pyrimidinyl, wherein said heteroaryl is attached to the pyridinyl group in the compound of Formula (I) by a nitrogen ring atom in said heteroaryl and wherein said heteroaryl is substituted with zero to 2 R; A is pyrazolyl, imidazolyl, triazolyl, isoxazolyl, oxadiazolyl or dihydroisoxazolyl, each substituted with zero or 1 R; and R, R, and Rare define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer. 

Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where all substituents are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFN&#x3b1;, by acting on Tyk-2 to cause signal transduction inhibition.

Phosphine oxide alkyl amide substituted heteroaryl compounds as modulators of IL-12, IL-23 and/or IFN alpha responses

Disclosed are compounds of Formula (I) or salts thereof, wherein: HET is a heteroaryl selected from imidazo[1,2-b]pyridazinyl and pyrazolo[1,5-a]pyrimidinyl, wherein said heteroaryl is attached to the pyridinyl group in the compound of Formula (I) by a carbon ring atom in the heteroaryl and wherein said heteroaryl is substituted with zero to 2 Rb; A is pyrazolyl, imidazolyl, or triazolyl, each substituted with zero or 1 Ra; and R3, Ra, and Rb are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer. 

Compounds having the following formula (I) or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein Ris a monocyclic heteroaryl group, and R, R, R, Rand Rare as defined herein, are useful as kinase modulators, including IRAK-4 inhibition. 

Compounds having the following formula (I) or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein Ris a bicyclic heterocycle, and R, R, R, Rand Rare as defined herein, that are useful as kinase modulators, including IRAK-4 modulation. 

Bicyclic heterocycle substituted pyridyl compounds useful as kinase modulators

The present application describes modulators of chemokine receptor activity 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 transplant rejection using modulators of formula (I) are disclosed.

Spirocyclic compounds as modulators of chemokine receptor activity

Disclosed are compounds of Formula (I) or salts thereof, wherein: HET is a heteroaryl selected from pyrazolyl, indolyl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-d]pyrimidinyl, pyrazolo[3,4-b]pyridinyl, pyrazolo[3,4-d]pyrimidinyl, 2,3-dihydro-1H-pyrrolo[2,3-b]pyridinyl, imidazo[4,5-b]pyridinyl, and purinyl, wherein said heteroaryl is substituted with Rand R; and Rand Rare define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases.

Heteroaryl substituted nicotinamide compounds

The present application describes modulators of chemokine receptor activity 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 transplant rejection using modulators of formula (I) are disclosed. 

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

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Newtown, PA, United States of America

John V Duncia