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：US11254663B2

公开(公告)日：2022-02-22

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 ,  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：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：US10959986B2

公开(公告)日：2021-03-30

申请号：US16555634

申请日：2019-08-29

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： James Aaron Balog ,  Steven P. Seitz ,  Susheel Jethanand Nara ,  Saumya Roy ,  Srinivasan Thangathirupathy ,  Soodamani Thangavel ,  Ramesh Kumar Sistla

IPC: A61K31/415 ,  A61K31/5377 ,  C07D231/12 ,  C07D401/12 ,  C07D403/12 ,  C07D261/08 ,  C07D277/22 ,  C07D285/08 ,  C07D211/60 ,  C07D317/50 ,  C07D307/36 ,  C07D333/54 ,  C07D231/56 ,  C07D221/22 ,  C07D471/04 ,  C07D487/04 ,  A61K31/17 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/42 ,  A61K31/426 ,  A61K31/433 ,  A61K31/357 ,  A61K31/341 ,  A61K31/381 ,  C07C275/42

Abstract: There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the disclosure.

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：US20200069695A1

公开(公告)日：2020-03-05

申请号：US16555431

申请日：2019-08-29

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： James Aaron Balog ,  Steven P. Seitz ,  Susheel Jethanand Nara ,  Saumya Roy ,  Srinivasan Thangathirupathy ,  Soodamani Thangavel ,  Srinivas Cheruku

IPC: A61K31/5377 ,  C07C275/42 ,  A61K31/17 ,  C07D277/64 ,  A61K31/428 ,  C07C211/54 ,  A61K31/136 ,  C07D239/47 ,  A61K31/505 ,  A61K31/275 ,  C07D241/18 ,  A61K31/4965 ,  C07D239/42 ,  A61K31/5375 ,  C07D295/03 ,  C07D413/12

Abstract: There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the disclosure.

公开(公告)号：US20160332985A1

公开(公告)日：2016-11-17

申请号：US15112294

申请日：2015-01-23

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Richard A. Hartz ,  Vijay T. Ahuja ,  John E. Macor ,  Joanne J. Bronson ,  Bireshwar Dasgupta ,  Carolyn Diane Dzierba ,  Susheel Jethanand Nara ,  Maheswaran Sivasamban Karatholuvhu

IPC: C07D401/04 ,  C07D401/14 ,  C07D215/12 ,  C07D413/04 ,  C07D471/04

CPC classification number: C07D401/04 ,  C07D215/12 ,  C07D215/18 ,  C07D401/14 ,  C07D413/04 ,  C07D471/04

Abstract: The present disclosure is generally directed to compounds of formula (I) which can inhibit AAKI (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAKI.

公开(公告)号：US20160016967A1

公开(公告)日：2016-01-21

申请号：US14767952

申请日：2014-02-06

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Vivekananda M. Vrudhula ,  Carolyn Diane Dzierba ,  Joanne J. Bronson ,  John E. Macor ,  Susheel Jethanand Nara ,  Ramkumar Rajamani ,  Maheswaran Sivasamban Karatholuvhu

IPC: C07D491/052

CPC classification number: C07D491/052

Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.

Abstract translation: 本公开一般涉及可以抑制AAK1（衔接子相关激酶1），包含这些化合物的组合物和抑制AAK1的方法的化合物。

公开(公告)号：US08901305B2

公开(公告)日：2014-12-02

申请号：US13946344

申请日：2013-07-19

Applicant: Bristol-Myers Squibb Company

Inventor： Vivekananda M. Vrudhula ,  Senliang Pan ,  Ramkumar Rajamani ,  Susheel Jethanand Nara ,  Maheswaran Sivasamban Karatholuvhu ,  Tarun Kumar Maishal ,  Jonathan L. Ditta ,  Carolyn Diane Dzierba ,  Joanne J. Bronson ,  John E. Macor

IPC: A61K31/44 ,  C07D471/00 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.

Abstract translation: 本公开一般涉及可抑制AAK1（衔接子相关激酶1），包含这些化合物的组合物和抑制AAK1的方法的化合物。