公开(公告)号：US12145927B2

公开(公告)日：2024-11-19

申请号：US17261968

申请日：2019-07-22

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： James Aaron Balog ,  Steven P. Seitz ,  Jay A. Markwalder ,  David K. Williams ,  Weifang Shan ,  Susheel Jethanand Nara ,  Saumya Roy ,  Srinivas Cheruku ,  Nagalakshmi Pulicharla

IPC: C07D405/14 ,  C07D307/79 ,  C07D313/08 ,  C07D405/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  C07K16/28

Abstract: The present invention provides compounds of formula (I) wherein all of the variables are as defined herein. These compounds are inhibitors of indoleamine 2,3-dioxygenase (IDO), which may be used as medicaments for the treatment of proliferative disorders, such as cancer, viral infections and/or autoimmune diseases.

公开(公告)号：US11713312B2

公开(公告)日：2023-08-01

申请号：US17544490

申请日：2021-12-07

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

CPC classification number: C07D413/12 ,  A61P11/00 ,  C07D271/06

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：US10253027B2

公开(公告)日：2019-04-09

申请号：US14902868

申请日：2014-07-01

Applicant: Bristol-Myers Squibb Company

Inventor： Richard A. Hartz ,  Vijay T. Ahuja ,  Joanne J. Bronson ,  Carolyn Diane Dzierba ,  John E. Macor ,  Susheel Jethanand Nara ,  Ramkumar Rajamani

IPC: C07D487/04 ,  C07D409/10 ,  C07D233/61 ,  C07D401/12 ,  C07D401/10 ,  C07D263/32 ,  C07D213/56 ,  C07D285/12 ,  C07D277/30 ,  C07D213/73 ,  C07D213/65 ,  C07D249/08 ,  C07D233/54 ,  C07D249/06 ,  C07D237/08 ,  C07D213/72 ,  C07D213/16 ,  C07D285/08 ,  C07D231/12 ,  C07D213/62 ,  C07D277/20 ,  C07D213/61 ,  C07D263/30 ,  C07D413/12 ,  C07D417/12

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.

公开(公告)号：US20180141956A1

公开(公告)日：2018-05-24

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

CPC classification number: C07D491/052 ,  A61P25/02 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  C07B59/002 ,  C07B2200/05 ,  C07D471/04 ,  C07D491/04

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.

公开(公告)号：US09932320B2

公开(公告)日：2018-04-03

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: C07D401/14 ,  C07D401/04 ,  C07D215/12 ,  C07D215/18 ,  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：US20180079712A1

公开(公告)日：2018-03-22

申请号：US15564146

申请日：2016-04-01

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: C07C229/42 ,  C07C275/42 ,  C07D295/155 ,  C07D239/47 ,  C07D277/64 ,  C07D335/02 ,  C07D409/12 ,  C07D309/14 ,  C07D405/12 ,  C07D211/14 ,  C07D401/12 ,  C07D317/46 ,  C07D239/34 ,  C07D413/12 ,  C07D265/30 ,  C07C233/81 ,  C07D405/14 ,  C07D207/12 ,  C07D487/08 ,  C07D487/04 ,  C07D471/08 ,  C07D265/36 ,  C07D413/14

Abstract: There are disclosed compounds of formula (I) 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：US09708337B2

公开(公告)日：2017-07-18

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 ,  A61K31/436

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.

公开(公告)号：US20160289171A1

公开(公告)日：2016-10-06

申请号：US15088211

申请日：2016-04-01

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: C07C229/42 ,  A61K31/196 ,  C07D239/47 ,  A61K31/505 ,  C07C255/58 ,  A61K31/277 ,  C07C275/40 ,  A61K31/17 ,  C07D295/155 ,  A61K31/5375 ,  C07D277/64 ,  A61K31/428 ,  C07D335/02 ,  A61K31/382 ,  C07D409/12 ,  A61K31/506 ,  C07D309/04 ,  A61K31/351 ,  C07D405/12 ,  C07D211/14 ,  A61K31/445 ,  C07D401/12 ,  C07D413/12 ,  A61K31/5377 ,  C07D405/14 ,  C07D417/12 ,  C07D487/04 ,  A61K31/519 ,  A61K31/501 ,  C07D471/04 ,  A61K31/437 ,  C07D205/04 ,  A61K31/397 ,  A61K31/538 ,  C07D265/36 ,  A61K39/395

CPC classification number: C07C275/40 ,  A61K31/17 ,  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 ,  A61K39/3955 ,  A61K39/39558 ,  A61K45/06 ,  C07C229/42 ,  C07C233/81 ,  C07C235/38 ,  C07C235/56 ,  C07C255/57 ,  C07C255/58 ,  C07C275/30 ,  C07C275/42 ,  C07D205/04 ,  C07D207/08 ,  C07D207/12 ,  C07D211/08 ,  C07D211/14 ,  C07D239/34 ,  C07D239/47 ,  C07D265/30 ,  C07D265/36 ,  C07D277/64 ,  C07D295/155 ,  C07D307/22 ,  C07D309/04 ,  C07D309/14 ,  C07D317/46 ,  C07D335/02 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08

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.

Abstract translation: 公开了调节或抑制吲哚胺2,3-双加氧酶（IDO）的酶活性的化合物，含有所述化合物的药物组合物和治疗增殖性疾病如癌症，病毒感染和/或炎症性疾病的方法，其利用 发明。

公开(公告)号：US20140179725A1

公开(公告)日：2014-06-26

申请号：US14188141

申请日：2014-02-24

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: C07D491/20 ,  C07D491/052

CPC classification number: C12N9/99 ,  C07D491/04 ,  C07D491/052 ,  C07D491/20

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。

公开(公告)号：US20230212158A1

公开(公告)日：2023-07-06

申请号：US17998261

申请日：2021-05-10

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Prasada Rao Jalagam ,  Susheel Jethanand Nara ,  Manoranjan Panda ,  Murugesan Natesan ,  Pratik Devasthale

IPC: C07D405/14 ,  C07D405/04 ,  C07D487/08

CPC classification number: C07D405/14 ,  C07D405/04 ,  C07D487/08

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. (Formula (I))