公开(公告)号：US10273237B2

公开(公告)日：2019-04-30

申请号：US15102991

申请日：2014-12-10

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Chunjian Liu ,  James Lin ,  Ryan M. Moslin ,  David S. Weinstein ,  John S. Tokarski

IPC: C07D487/04 ,  C07D487/14 ,  C07D498/14

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.

公开(公告)号：US20170209426A1

公开(公告)日：2017-07-27

申请号：US15480787

申请日：2017-04-06

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ryan M. Moslin ,  David S. Weinstein ,  Stephen T. Wrobleski ,  Yanlei Zhang ,  John S. Tokarski ,  Michael E. Mertzman ,  Chunjian Liu

IPC: A61K31/455 ,  A61K31/506

CPC classification number: A61K31/455 ,  A61K31/44 ,  A61K31/444 ,  A61K31/506 ,  C07B59/002 ,  C07B2200/05 ,  C07D213/56 ,  C07D213/82 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

Abstract: Compounds having the following formula I: or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein 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.

公开(公告)号：US12291522B2

公开(公告)日：2025-05-06

申请号：US17927426

申请日：2021-05-27

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Chunjian Liu ,  Wei Wang ,  Bruce A. Ellsworth ,  James Aaron Balog ,  Alicia Regueiro-Ren

IPC: C07H19/056 ,  C07D405/14 ,  C07H17/02

Abstract: The present disclosure relates to compounds of Formula (I), which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions.

公开(公告)号：US20230167092A1

公开(公告)日：2023-06-01

申请号：US17997288

申请日：2021-04-27

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Chunjian Liu ,  James Lin ,  David S. Weinstein

IPC: C07D403/12 ,  C07D473/00 ,  C07D401/12 ,  C07D405/14 ,  C07D403/14 ,  C07D401/14 ,  C07D487/04 ,  C07D413/14

CPC classification number: C07D403/12 ,  C07D473/00 ,  C07D401/12 ,  C07D405/14 ,  C07D403/14 ,  C07D401/14 ,  C07D487/04 ,  C07D413/14 ,  C07B2200/05

Abstract: There are disclosed compounds of the following formula I or a stereoisomer or pharmaceutically-acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFN?, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating inflammatory and autoimmune diseases or disorders.

公开(公告)号：US20220144818A1

公开(公告)日：2022-05-12

申请号：US17601942

申请日：2020-04-08

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Chunjian Liu ,  Jianxin Feng ,  Pratik Devasthale ,  Natesan Murugesan ,  Bruce A. Ellsworth ,  Alicia Regueiro-Ren ,  Susheel Jethanand Nara ,  Prasada Rao Jalagam ,  Manoranjan Panda

IPC: C07D417/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14

Abstract: The present disclosure relates to compounds of Formula (I) or (II), which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions.

公开(公告)号：US11286252B2

公开(公告)日：2022-03-29

申请号：US16760810

申请日：2018-10-31

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Jianxin Feng ,  Chunjian Liu ,  Yanting Huang

IPC: C07D413/14 ,  C07D261/08 ,  C07D413/04 ,  C07D413/12 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

Abstract: The present invention provides compounds of Formula (I), or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

公开(公告)号：US09987266B2

公开(公告)日：2018-06-05

申请号：US15480787

申请日：2017-04-06

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ryan M. Moslin ,  David S. Weinstein ,  Stephen T. Wrobleski ,  Yanlei Zhang ,  John S. Tokarski ,  Michael E. Mertzman ,  Chunjian Liu

IPC: A61K31/455 ,  A61K31/506

CPC classification number: A61K31/455 ,  A61K31/44 ,  A61K31/444 ,  A61K31/506 ,  C07B59/002 ,  C07B2200/05 ,  C07D213/56 ,  C07D213/82 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

Abstract: Compounds having the following formula I: or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein 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.

公开(公告)号：US09663467B2

公开(公告)日：2017-05-30

申请号：US15034915

申请日：2014-01-16

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ryan M. Moslin ,  David S. Weinstein ,  Stephen T. Wrobleski ,  Yanlei Zhang ,  John S. Tokarski ,  Michael E. Mertzman ,  Chunjian Liu

IPC: C07D213/56 ,  C07D405/12 ,  C07D401/12 ,  C07D213/82 ,  C07D413/12 ,  C07D417/12 ,  C07B59/00

CPC classification number: A61K31/455 ,  A61K31/44 ,  A61K31/444 ,  A61K31/506 ,  C07B59/002 ,  C07B2200/05 ,  C07D213/56 ,  C07D213/82 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

Abstract: Compounds having the following formula (I): or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein 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.

公开(公告)号：US20170022192A1

公开(公告)日：2017-01-26

申请号：US15289437

申请日：2016-10-10

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ryan M. Moslin ,  David S. Weinstein ,  Stephen T. Wrobleski ,  John S. Tokarski ,  Amit Kumar ,  Douglas G. Batt ,  Shuqun Lin ,  Chunjian Liu ,  Steven H. Spergel ,  Yanlei Zhang ,  Qingjie Liu

IPC: C07D417/14 ,  C07B59/00 ,  C07D403/12 ,  C07D413/14 ,  C07D403/14 ,  C07D401/14 ,  C07D417/12 ,  C07D413/12 ,  C07D401/12 ,  C07D237/24

CPC classification number: C07D417/14 ,  C07B59/002 ,  C07B2200/05 ,  C07D237/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

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: 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IFNα，通过作用于Tyk-2 引起信号转导抑制。

公开(公告)号：US20150299183A1

公开(公告)日：2015-10-22

申请号：US14441183

申请日：2013-11-07

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ryan M. Moslin ,  David S. Weinstein ,  Stephen T. Wrobleski ,  John S, Tokarski ,  Amit Kumar ,  Douglas G. Batt ,  Shuqun Lin ,  Chunjian Liu ,  Steven H. Spergel ,  Yanlei Zhang

IPC: C07D417/14 ,  C07D403/12 ,  C07D401/14 ,  C07D401/12

CPC classification number: C07D417/14 ,  C07B59/002 ,  C07B2200/05 ,  C07D237/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

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IFNα ，通过作用于Tyk-2引起信号转导抑制。