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：US20210380578A1

公开(公告)日：2021-12-09

申请号：US16759782

申请日：2018-10-31

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Joseph E. Carpenter ,  Jianxin Feng ,  Ji Jiang ,  Soong-Hoon Kim ,  Ying Wang ,  Gang Wu

IPC: C07D417/14 ,  C07D413/14 ,  C07D413/06 ,  C07D471/08 ,  C07D487/04 ,  C07D401/14 ,  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：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：US11370785B2

公开(公告)日：2022-06-28

申请号：US16759782

申请日：2018-10-31

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Joseph E. Carpenter ,  Jianxin Feng ,  Ji Jiang ,  Soong-Hoon Kim ,  Ying Wang ,  Gang Wu

IPC: C07D417/14 ,  C07D401/14 ,  C07D413/06 ,  C07D413/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  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：US11168079B2

公开(公告)日：2021-11-09

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: C07D401/14 ,  A61K31/4545 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  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：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.