Bristol-myers Squibb Compnay

Bristol-myers Squibb Pharma Company

The Dupont Merck Pharmaceutical Company

Other

Dupont Pharmaceuticals Company

Bristol-myers Squibb Pharma Corporation

Joseph B Santella

Daniel S Gardner

Dean A Wacker

Soo Sung Ko

John T Hynes

George V DeLucca

Satheesh Kesavan Nair

Hong Wu

Venkatram Reddy Paidi

Natesan Murugesan

Percy H Carter

Sreekantha Ratna Kumar

Ramesh Kumar Sistla

William John Pitts

Rajeev S Bhide

Wenqing Yao

Robert J Cherney

John J Duncia

Paul Steven Watson

John E Macor

Richard Eric Olson

Mimi Lifen Quan

William Henry Miller

T G Murali Dhar

John V Duncia

Kandhasamy Sarkunam

George V Delucca

Cullen L Cavallaro

Ryan M Moslin

Patricia C Weber

Khehyong Ngu

Ui Tae Kim

Dharmpal S Dodd

David S Weinstein

Changsheng Zheng

Tg Murali Dhar

Rui-Qin Liu

Carol L Ensinger

Mary K VanAtten

Cheryl McArdle Clark

Subba Rao Polimera

Douglas G Batt

John Wityak

Stephen T Wrobleski

John S Tokarski

Jayakumar Sankara Warrier

Zhongyu Wang

Charles Malcolm Langevine

Xiao Zhu

Lyndon A M Cornelius

Yanlei Zhang

Gregory James Pacofsky

Eugene Cruz Amparo

Jeffrey G Varnes

Christopher Annunziato

Daniel S Gardner, Iv

Sylwia Stachura

John J V Duncia

Piramanayagam Arunachalam

Durgarao Kantheti

Lyndon AM Cornelius

Charles M Langevine

TG Murali Dhar

Natessan Murugesan

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

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

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. 

Imidazopyridazine compounds useful 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 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. 

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

Compounds having the following formula (I): or a stereoisomer or pharmaceutically-acceptable salt thereof, where R, R, R, R, and Rare 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. 

Alkyl amide-substituted pyrimidine compounds useful in the modulation of IL-12, IL-23 and/or IFN&#x3b1;

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 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

Piperidinyl derivative as a modulator of chemokine receptor activity

The present application describes modulators of MIP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. 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 atherosclerosis using the modulators are disclosed. 

Piperidine derivatives as modulators of chemokine receptor activity

The present application describes modulators of MIP-1&#x3b1; of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R, R, R, R, Rand R, are as defined herein. 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 atherosclerosis using the modulators of formula (I) are disclosed. 

Piperidinyl derivatives as modulators of chemokine receptor activity

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Springfield, PA, United States of America

Joseph B Santella