Bristol-myers Squibb Compnay

Bristol-myers Squibb Pharma Company

Other

Bristol-myers Squibb Pharma Corporation

Daniel S Gardner

John V Duncia

Joseph B Santella

John T Hynes

Percy H Carter

Venkatram Reddy Paidi

Robert J Cherney

Satheesh Kesavan Nair

Hong Wu

Dean A Wacker

Ramesh Kumar Sistla

Natesan Murugesan

Soo Sung Ko

Sreekantha Ratna Kumar

Douglas G Batt

William John Pitts

Michael G Yang

Rajeev S Bhide

T G Murali Dhar

Kandhasamy Sarkunam

Anurag S Srivastava

John E Macor

Dharmpal S Dodd

George V DeLucca

Cullen L Cavallaro

Deqiang Niu

Joseph Anthony Tino

David S Weinstein

George V Delucca

Khehyong Ngu

Xiao Zhu

Weiwei Guo

Rui-Qin Liu

Subba Rao Polimera

Boris M Seletsky

Manoranjan Panda

Ryan M Moslin

Zhongyu Wang

Julio Hernan Cuervo

Srinivasan Thangathirupathy

Charles Malcolm Langevine

Kumaravel Selvakumar

Yanlei Zhang

Gregory D Brown

Tg Murali Dhar

Alyssa H Antropow

Piramanayagam Arunachalam

Durgarao Kantheti

Vijaya Kumar Cm

Mallikarjun Reddy Sura

Tirupathi Rao Alajangi

Krishna Mahadevu

Piyush Agarwal

Ooha Morampudi

Sylwia Stachura

Audrey Graham Ross

Paul E Gormisky

Zhengdong Zhu

Guobin Miao

Jalathi S Nair

Arul Mozhi Subbiah Karuppiah

Joseph B Santella Iii

Christopher Annunziato

Charles M Langevine

Natessan Murugesan

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

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

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

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

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Furlong, PA, United States of America

Daniel S Gardner