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：US11970511B2

公开(公告)日：2024-04-30

申请号：US17251964

申请日：2019-06-13

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Richard A. Hartz ,  Li Xu ,  David S. Yoon ,  Alicia Regueiro-Ren ,  Prasada Rao Jalagam ,  Manoranjan Panda ,  Satheesh Kesavan Nair

IPC: C07H17/04 ,  A61P13/12

CPC classification number: C07H17/04 ,  A61P13/12

Abstract: The present disclosure relates to compounds of Formula (1), which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods making and using such compounds and compositions.

公开(公告)号：US10336684B2

公开(公告)日：2019-07-02

申请号：US16033645

申请日：2018-07-12

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Peter T. W. Cheng ,  David S. Yoon

IPC: C07C229/42 ,  C07C59/72 ,  C07D205/04 ,  C07C62/34 ,  C07C59/68 ,  C07C59/64 ,  C07D213/65 ,  C07D211/46 ,  C07D211/42 ,  C07D211/14 ,  C07D207/12 ,  C07D223/08 ,  A61K31/192 ,  A61K31/196 ,  A61K31/397 ,  A61K31/402 ,  A61K31/44 ,  A61K31/451 ,  A61K31/55

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.

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：US20190127358A1

公开(公告)日：2019-05-02

申请号：US16175895

申请日：2018-10-31

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： David S. Yoon ,  Rushith Kumar Anumula ,  Srinivas Cheruku ,  Yanting Huang ,  Elizabeth Anne Jurica ,  Wei Meng ,  Susheel Jethanand Nara ,  Rishikesh Narayan ,  Ramesh Kumar Sistla ,  Ximao Wu ,  Guohua Zhao

IPC: C07D413/14 ,  C07D413/04 ,  A61P35/00 ,  A61P29/00 ,  A61P13/12 ,  A61P1/16 ,  A61P1/18

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：US20240067638A1

公开(公告)日：2024-02-29

申请号：US18042036

申请日：2021-08-18

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： David S. Yoon ,  Alicia Regueiro-Ren ,  Andrew P. Degnan ,  Gang WU

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: The present invention relates to imidazo[1,2-a]pyridine and [1,2,4]triazolo[1, 5-a]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：US20210323991A1

公开(公告)日：2021-10-21

申请号：US17251964

申请日：2019-06-13

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Richard A. Hartz ,  Li Xu ,  David S. Yoon ,  Alicia Regueiro-Ren ,  Prasada Rao Jalagam ,  Manoranjan Panda ,  Satheesh Kesavan Nair

IPC: C07H17/04 ,  A61P13/12

Abstract: The present disclosure relates to compounds of Formula (1), which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods making and using such compounds and compositions.

公开(公告)号：US20220009913A1

公开(公告)日：2022-01-13

申请号：US17299325

申请日：2019-12-04

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Jacob Swidorski ,  Brett R. Beno ,  David S. Yoon ,  Alicia Regueiro-Ren

IPC: C07D405/14

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：US10730863B2

公开(公告)日：2020-08-04

申请号：US16175895

申请日：2018-10-31

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： David S. Yoon ,  Rushith Kumar Anumula ,  Srinivas Cheruku ,  Yanting Huang ,  Elizabeth Anne Jurica ,  Wei Meng ,  Susheel Jethanand Nara ,  Rishikesh Narayan ,  Ramesh Kumar Sistla ,  Ximao Wu ,  Guohua Zhao

IPC: C07D413/14 ,  C07D413/04 ,  A61P35/00 ,  A61P29/00 ,  A61P13/12 ,  A61P1/16 ,  A61P1/18 ,  C07D261/08 ,  A61K31/428 ,  C07D417/14 ,  A61K31/4245 ,  C07D471/04 ,  A61K31/429 ,  A61K31/422 ,  C07D417/12

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：US20180319737A1

公开(公告)日：2018-11-08

申请号：US16033645

申请日：2018-07-12

Applicant: Bristol-Myers Squibb Company

Inventor： PETER T. W. CHENG ,  David S. Yoon

IPC: C07C229/42 ,  C07D223/08 ,  A61K31/451 ,  A61K31/397 ,  A61K31/402 ,  A61K31/44 ,  A61K31/55 ,  C07C59/72 ,  A61K31/192 ,  A61K31/196 ,  C07C62/34 ,  C07C59/68 ,  C07C59/64 ,  C07D213/65 ,  C07D211/46 ,  C07D211/42 ,  C07D211/14 ,  C07D207/12 ,  C07D205/04

CPC classification number: C07C229/42 ,  A61K31/192 ,  A61K31/196 ,  A61K31/397 ,  A61K31/402 ,  A61K31/44 ,  A61K31/451 ,  A61K31/55 ,  C07C59/64 ,  C07C59/68 ,  C07C59/72 ,  C07C62/34 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/18 ,  C07D205/04 ,  C07D207/12 ,  C07D211/14 ,  C07D211/42 ,  C07D211/46 ,  C07D213/65 ,  C07D223/08

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.