公开(公告)号：US20220213026A1

公开(公告)日：2022-07-07

申请号：US17431091

申请日：2020-02-14

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Dean A. Wacker ,  Susheel Jethanand Nara ,  Srinivas Cheruku ,  Kandhasamy Sarkunam ,  Firoz Ali Jaipuri ,  Soodamani Thangavel ,  Rishikesh Narayan ,  Subba Reddy Bandreddy ,  Srinivas Jogi ,  Pavan Kalyan Kathi

IPC: C07C233/61 ,  C07D295/04 ,  C07D207/06 ,  C07D205/04 ,  C07D309/04 ,  C07D405/14 ,  C07D271/06 ,  C07D277/64 ,  C07D413/04 ,  C07D405/04

Abstract: Disclosed are compounds of Formula (I) or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, wherein Q is a 5-membered heterocyclyl or 5-membered heteroaryl having 1 to 4 heteroatoms independently selected from N, O, and S, substituted with zero to 4 R1; and A, X1, X2, X3, X4, Z1, Z2, R1, R2, R3a, R3b, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); 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：US12030835B2

公开(公告)日：2024-07-09

申请号：US17431091

申请日：2020-02-14

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Dean A. Wacker ,  Susheel Jethanand Nara ,  Srinivas Cheruku ,  Kandhasamy Sarkunam ,  Firoz Ali Jaipuri ,  Soodamani Thangavel ,  Rishikesh Narayan ,  Subba Reddy Bandreddy ,  Srinivas Jogi ,  Pavan Kalyan Kathi

IPC: C07C233/61 ,  C07D205/04 ,  C07D207/06 ,  C07D271/06 ,  C07D277/64 ,  C07D295/04 ,  C07D309/04 ,  C07D405/04 ,  C07D405/14 ,  C07D413/04

CPC classification number: C07C233/61 ,  C07D205/04 ,  C07D207/06 ,  C07D271/06 ,  C07D277/64 ,  C07D295/04 ,  C07D309/04 ,  C07D405/04 ,  C07D405/14 ,  C07D413/04

Abstract: Disclosed are compounds of Formula (I) or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, wherein Q is a 5-membered heterocyclyl or 5-membered heteroaryl having 1 to 4 heteroatoms independently selected from N, O, and S, substituted with zero to 4 R1; and A, X1, X2, X3, X4, Z1, Z2, R1, R2, R3a, R3b, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); 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：US20220162201A1

公开(公告)日：2022-05-26

申请号：US17431006

申请日：2020-02-14

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Dean A. Wacker ,  Susheel Jethanand Nara ,  Srinivas Cheruku ,  Kandhasamy Sarkunam ,  Firoz Ali Jaipuri ,  Rishikesh Narayan ,  Subba Reddy Bandreddy ,  Srinivas Jogi

IPC: C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D403/12 ,  C07D217/06 ,  C07D271/06 ,  C07D417/14

Abstract: Disclosed are compounds of Formula (I): or a stereoisomer, a tautomer, or a salt or solvate thereof, wherein Q is C2-6 alkenyl or C2-6 alkynyl, each substituted with zero to 2 R1; and the other variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. Also disclosed are 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：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：US12227496B2

公开(公告)日：2025-02-18

申请号：US17431006

申请日：2020-02-14

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Dean A. Wacker ,  Susheel Jethanand Nara ,  Srinivas Cheruku ,  Kandhasamy Sarkunam ,  Firoz Ali Jaipuri ,  Rishikesh Narayan ,  Subba Reddy Bandreddy ,  Srinivas Jogi

IPC: C07D413/12 ,  C07D217/06 ,  C07D271/06 ,  C07D403/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: Disclosed are compounds of Formula (I): or a stereoisomer, a tautomer, or a salt or solvate thereof, wherein Q is C2-6 alkenyl or C2-6 alkynyl, each substituted with zero to 2 R1; and the other variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. Also disclosed are 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：US20220081430A1

公开(公告)日：2022-03-17

申请号：US17430903

申请日：2020-02-14

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Dean A. Wacker ,  Susheel Jethanand Nara ,  Srinivas Cheruku ,  Kandhasamy Sarkunam ,  Firoz Ali Jaipuri ,  Soodamani Thangavel ,  Rishikesh Narayan ,  Srinivas Jogi ,  Pavan Kalyan Kathi

IPC: C07D413/12 ,  C07D401/12 ,  C07D271/06 ,  C07D213/26 ,  C07D417/12

Abstract: Disclosed are compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, when Q is: (i) halo, cyano, hydroxyl, NRxRx, C(O)OH, C(O)NH2, C1-6 alkyl substiuted with zero to 6 R1a, or P(O)R1cR1c, or (ii) L R1; and A, X1, X2, X3, X4, Z1, Z2, R1, R1a, R1c, R2, R3a, R3b, Rx, L, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); 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：US20210261535A1

公开(公告)日：2021-08-26

申请号：US16789551

申请日：2020-02-13

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Dean A. Wacker ,  Susheel Jethanand Nara ,  Srinivas Cheruku ,  Kandhasamy Sarkunam ,  Firoz Ali Jaipuri ,  Soodamani Thangavel ,  Rishikesh Narayan ,  Subba Reddy Bandreddy ,  Srinivas Jogi ,  Pavan Kalyan Kathi

IPC: C07D413/12 ,  C07D271/06 ,  A61P11/00

Abstract: Disclosed are compounds of Formula (I): or a stereoisomer, a tautomer, or a salt or solvate thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. Also disclosed are 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：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.