公开(公告)号：US08633226B2

公开(公告)日：2014-01-21

申请号：US13628180

申请日：2012-09-27

Applicant: Bristol-Myers Squibb Company

Inventor： Joseph B. Santella

IPC: A61K31/445 ,  C07D211/00

CPC classification number: C07D211/52

Abstract: 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.

Abstract translation: 本申请描述了式（I）化合物或其立体异构体或其药学上可接受的盐。 此外，公开了使用本发明的化合物治疗和预防炎症性疾病如哮喘和过敏性疾病以及自身免疫病态如类风湿性关节炎和关节病的方法。

公开(公告)号：US20220402950A1

公开(公告)日：2022-12-22

申请号：US17265844

申请日：2019-08-07

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Daniel S. Gardner ,  John V. Duncia ,  Joseph B. Santella ,  Khehyong Ngu ,  Christopher Annunziato

IPC: C07F9/6561 ,  C07D471/08 ,  C07D401/14 ,  A61K45/06

Abstract: The present invention provides compounds of Formula (I): useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.

公开(公告)号：US20220380372A1

公开(公告)日：2022-12-01

申请号：US17634615

申请日：2020-08-12

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： John Hynes ,  Hong Wu ,  Venkatram Reddy Paidi ,  Subba Rao Polimera ,  Satheesh Kesavan Nair ,  Joseph B. Santella

IPC: C07D487/04 ,  C07D519/00

Abstract: Disclosed are compounds of Formula (I) or a salt or prodrug thereof, wherein: X is C or N; Y is C or N; Z is CR4 or N; provided that when: (i) X is N, then Y is C; and (ii) X is C, then Y is N and Z is N; and wherein R1, R2, R3, and R4 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.

公开(公告)号：US20220064180A1

公开(公告)日：2022-03-03

申请号：US17265833

申请日：2019-08-07

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Daniel S. Gardner ,  John V. Duncia ,  Joseph B. Santella

IPC: C07D495/04 ,  A61K45/06 ,  C07D519/00

Abstract: The present invention provides compounds of formula (I) useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.

公开(公告)号：US10544133B2

公开(公告)日：2020-01-28

申请号：US16009389

申请日：2018-06-15

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Rajeev S. Bhide ,  John V. Duncia ,  John Hynes ,  Satheesh Kesavan Nair ,  William J. Pitts ,  Sreekantha Ratna Kumar ,  Daniel S. Gardner ,  Natesan Murugesan ,  Venkatram Reddy Paidi ,  Joseph B. Santella ,  Ramesh Kumar Sistla ,  Hong Wu

IPC: C07D407/14 ,  C07D401/14 ,  C07D401/12 ,  C07D417/14 ,  C07D213/74 ,  C07D405/12 ,  C07D405/14

Abstract: Compounds having the following formula: or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein R2 is a monocyclic heteroaryl group, and R1, R3, R4, R5 and R6 are as defined herein, are useful as kinase modulators, including IRAK-4 inhibition.

公开(公告)号：US20190292191A1

公开(公告)日：2019-09-26

申请号：US16314574

申请日：2016-06-23

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： John V. Duncia ,  Daniel S. Gardner ,  John Hynes ,  John E. Macor ,  Natesan Murugesan ,  Joseph B. Santella ,  Hong Wu ,  Durgarao Kantheti ,  Satheesh Kesavan Nair ,  Venkatram Reddy Paidi ,  Sreekantha Ratna Kumar ,  Kandhasamy Sarkunam ,  Ramesh Kumar Sistla ,  Subba Rao Polimera

IPC: C07D487/04 ,  C07D471/04 ,  C07D413/04 ,  C07D401/14

Abstract: 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 Rb; and R1, R3, 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.

公开(公告)号：US10202390B2

公开(公告)日：2019-02-12

申请号：US15738435

申请日：2016-06-23

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： John V. Duncia ,  Daniel S. Gardner ,  John Hynes ,  John E. Macor ,  Satheesh Kesavan Nair ,  Venkatram Reddy Paidi ,  Joseph B. Santella ,  Kandhasamy Sarkunam ,  Ramesh Kumar Sistla ,  Subba Rao Polimera ,  Hong Wu

IPC: C07D487/04

Abstract: 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.

公开(公告)号：US20180325899A1

公开(公告)日：2018-11-15

申请号：US15776094

申请日：2016-11-17

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： David S. Weinstein ,  Ryan M. Moslin ,  Yanlei Zhang ,  Daniel S. Gardner ,  Joseph B. Santella ,  Charles M. Langevine ,  Sylwia Stachura

IPC: A61K31/5025 ,  A61K31/53 ,  A61K31/5377 ,  A61P29/00 ,  A61P37/02

CPC classification number: A61K31/5025 ,  A61K31/53 ,  A61K31/5377 ,  A61P29/00 ,  A61P37/02 ,  C07D487/04

Abstract: Compounds of formula I or a stereoisomer or pharmaceutically-acceptable salt thereof, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.

公开(公告)号：US20150299139A1

公开(公告)日：2015-10-22

申请号：US14441213

申请日：2013-11-07

Applicant: Bristol-Myers Squibb Company

Inventor： Joseph B. Santella ,  Ryan M. Moslin ,  David S. Weinstein ,  Stephen T. Wrobleski ,  John S. Tokarski

IPC: C07D239/48

CPC classification number: C07D239/48 ,  C07D239/95

Abstract: Compounds having the following formula (I): or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα by acting on Tyk-2 to cause signal transduction inhibition.

Abstract translation: 具有下式（I）的化合物或其立体异构体或药学上可接受的盐，其中R 1，R 2，R 3，R 4和R 5如本文所定义，可用于调节IL-12，IL-23和/ 或通过作用于Tyk-2引起信号转导抑制的IFNα。

公开(公告)号：US20180186799A1

公开(公告)日：2018-07-05

申请号：US15738362

申请日：2016-06-23

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Daniel S. GARDNER ,  Joseph B. Santella ,  Venkatram Reddy Paidi ,  Hong Wu ,  John V. Duncia ,  Satheesh Kesavan Nair ,  John Hynes ,  Xiao Zhu

IPC: C07D487/04 ,  C07D471/04

CPC classification number: C07D487/04 ,  C07D471/04

Abstract: 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 Rb; A is pyrazolyl, imidazolyl, triazolyl, isoxazolyl, oxadiazolyl or dihydroisoxazolyl, 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.