公开(公告)号：US10167254B2

公开(公告)日：2019-01-01

申请号：US15584818

申请日：2017-05-02

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： James Aaron Balog ,  Emily Charlotte Cherney ,  Weiwei Guo ,  Audris Huang ,  Jay A. Markwalder ,  Steven P. Seitz ,  Weifang Shan ,  David K. Williams ,  Natesan Murugesan ,  Susheel Jethanand Nara ,  Saumya Roy ,  Soodamani Thangavel ,  Ramesh Kumar Sistla ,  Srinivas Cheruku ,  Srinivasan Thangathirupathy ,  Yadagiri Kanyaboina ,  Nagalakshmi Pulicharla

IPC: A61K31/17 ,  C07C275/40 ,  A61K31/196 ,  A61K31/277 ,  A61K31/351 ,  A61K31/382 ,  A61K31/397 ,  A61K31/428 ,  A61K31/437 ,  A61K31/445 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/538 ,  A61K39/395 ,  C07C229/42 ,  C07C255/58 ,  C07D205/04 ,  C07D211/14 ,  C07D239/47 ,  C07D265/36 ,  C07D277/64 ,  C07D295/155 ,  C07D309/04 ,  C07D335/02 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D309/14 ,  C07D407/12 ,  C07D487/08 ,  C07D265/30 ,  C07D207/08 ,  C07D211/08 ,  C07D307/22 ,  C07C255/57 ,  C07C235/38 ,  C07C235/56 ,  C07C233/81 ,  C07C275/42 ,  C07D207/12 ,  C07D239/34 ,  C07D317/46 ,  C07D413/14 ,  C07D471/08 ,  C07C275/30 ,  A61K45/06

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 invention.

公开(公告)号：US20180346440A1

公开(公告)日：2018-12-06

申请号：US15763280

申请日：2016-09-29

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Joanne J. Bronson ,  Ling Chen ,  Jonathan L. Ditta ,  Carolyn Diane Dzierba ,  Prasada Rao Jalagam ,  Guanglin Luo ,  John E. Macor ,  Tarun Kumar Maishal ,  Susheel Jethanand Nara ,  Ramkumar Rajamani ,  Ramesh Kumar Sistla ,  Soodamani Thangavel

IPC: C07D401/04 ,  C07D413/14 ,  A61P25/16 ,  A61P25/28 ,  A61P25/18 ,  A61P25/02

Abstract: The present disclosure is directed to biaryl compounds of formula (I) which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds and their use for treating e.g. pain, Alzheimer's disease, Parkinson's disease and schizophrenia.

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：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：US20200069646A1

公开(公告)日：2020-03-05

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 ,  C07C275/42 ,  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 ,  A61K31/5377

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：US10544120B2

公开(公告)日：2020-01-28

申请号：US15763280

申请日：2016-09-29

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Joanne J. Bronson ,  Ling Chen ,  Jonathan L. Ditta ,  Carolyn Diane Dzierba ,  Prasada Rao Jalagam ,  Guanglin Luo ,  John E. Macor ,  Tarun Kumar Maishal ,  Susheel Jethanand Nara ,  Ramkumar Rajamani ,  Ramesh Kumar Sistla ,  Soodamani Thangavel

IPC: C07D401/04 ,  C07D413/14 ,  A61P25/16 ,  A61P25/28 ,  A61P25/18 ,  A61P25/02

Abstract: The present disclosure is directed to biaryl compounds of formula (I) which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds and their use for treating e.g. pain, Alzheimer's disease, Parkinson's disease and schizophrenia.

公开(公告)号：US10174044B2

公开(公告)日：2019-01-08

申请号：US15563697

申请日：2016-04-04

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Susheel Jethanand Nara ,  Carolyn Diane Dzierba ,  John E. Macor ,  Joanne J. Bronson ,  Rajamani Ramkumar ,  Tarun Kumar Maishal ,  Maheswaran Sivasamban Karatholuvhu ,  Soodamani Thangavel ,  Kamalraj Thiyagarajan

IPC: A61K31/436 ,  C07D491/052 ,  C07D471/04 ,  C07D491/04 ,  A61P25/28 ,  A61P25/02 ,  A61P25/04 ,  A61P25/18 ,  A61P25/16 ,  C07B59/00

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.