公开(公告)号：US12269819B2

公开(公告)日：2025-04-08

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: C07H17/02 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

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：US20220356180A1

公开(公告)日：2022-11-10

申请号：US17244938

申请日：2021-04-29

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

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：US20220185800A1

公开(公告)日：2022-06-16

申请号：US17439845

申请日：2020-03-25

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Chunjian Liu ,  David S. Yoon ,  Wei Wang ,  Jianxin Feng ,  Bruce A. Ellsworth ,  Alicia Regueiro-Ren

IPC: C07D405/14 ,  C07D417/14

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：US20210179599A1

公开(公告)日：2021-06-17

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

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：US20230312565A1

公开(公告)日：2023-10-05

申请号：US18042069

申请日：2021-08-18

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Chunjian Liu ,  Alicia Regueiro-Ren

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: The present invention relates to 1H-pyrrolo[3,2-c]pyridine and 1H-pyrrolo[2,3-c]pyridine derivatives of formula (I) or a salt thereof. The present compounds are inhibitors of TLR9 and useful in treating preventing, or slowing fibrotic diseases, such as e.g. liver fibrosis, renal fibrosis, biliary fibrosis or pancreatic fibrosis, nonalcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD), chronic kidney disease, diabetic kidney disease, primary sclerosing cholangitis (PSC) or primary biliary cirrhosis (PBC), or idiopathic pulmonary fibrosis (IPF).

公开(公告)号：US20230295122A1

公开(公告)日：2023-09-21

申请号：US18041719

申请日：2021-08-18

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： David S. Yoon ,  Alicia Regueiro-Ren ,  Michael Mandler ,  Shoshana L. Posy ,  Chunjian Liu

IPC: C07D401/14 ,  C07D451/04 ,  C07D471/04 ,  C07D405/14 ,  C07D417/14 ,  C07D413/14 ,  C07D235/18 ,  C07D519/00 ,  C07D405/12 ,  C07D401/10 ,  C07D487/10 ,  C07D487/04 ,  C07D403/10 ,  C07D401/12 ,  C07D451/02

CPC classification number: C07D401/14 ,  C07D451/04 ,  C07D471/04 ,  C07D405/14 ,  C07D417/14 ,  C07D413/14 ,  C07D235/18 ,  C07D519/00 ,  C07D405/12 ,  C07D401/10 ,  C07D487/10 ,  C07D487/04 ,  C07D403/10 ,  C07D401/12 ,  C07D451/02

Abstract: The present invention relates to 1H-benzo[d]imidazole derivatives of formula (I) or a salt thereof. The present compounds are inhibitors of TLR9 and useful in treating preventing, or slowing fibrotic diseases, such as e.g. liver fibrosis, renal fibrosis, biliary fibrosis or pancreatic fibrosis, non-alcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD), chronic kidney disease, diabetic kidney disease, primary sclerosing cholangitis (PSC) or primary biliary cirrhosis (PBC), or idiopathic pulmonary fibrosis (IPF).

公开(公告)号：US20200283430A1

公开(公告)日：2020-09-10

申请号：US16759660

申请日：2018-10-31

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Joseph E. Carpenter ,  Matthias Broekema ,  Jianxin Feng ,  Chunjian Liu ,  Wei Wang ,  Ying Wang

IPC: C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D487/04 ,  C07D471/04 ,  C07D519/00

Abstract: The present invention provides compounds of Formula (I): 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 famesoid 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：US20190152948A1

公开(公告)日：2019-05-23

申请号：US16195951

申请日：2018-11-20

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Chunjian Liu ,  Michael G. Yang ,  Zili Xiao ,  Ling Chen ,  Ryan M. Moslin ,  John S. Tokarski ,  David S. Weinstein

IPC: C07D401/14 ,  C07D401/12 ,  C07D413/14 ,  C07D417/14 ,  C07D405/14 ,  C07F9/6558 ,  C07D471/04

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：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.