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：US11253525B2

公开(公告)日：2022-02-22

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: A61P35/00 ,  A61K31/17 ,  A61K31/44 ,  A61K31/50 ,  A61K31/136 ,  A61K31/275 ,  A61K31/351 ,  A61K31/428 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/5375 ,  A61K31/5377 ,  C07C211/54 ,  C07C229/42 ,  C07C255/58 ,  C07C275/42 ,  C07D213/90 ,  C07D237/22 ,  C07D239/42 ,  C07D239/47 ,  C07D241/18 ,  C07D265/30 ,  C07D277/64 ,  C07D295/03 ,  C07D407/12 ,  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：US10399932B2

公开(公告)日：2019-09-03

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: C07D309/14 ,  C07D405/12 ,  C07D413/12 ,  C07D335/02 ,  C07D211/10 ,  C07D265/30 ,  C07D409/12 ,  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 ,  A61K39/395 ,  C07C229/42 ,  C07C255/58 ,  C07D205/04 ,  C07D211/14 ,  C07D239/47 ,  C07D265/36 ,  C07D277/64 ,  C07D295/155 ,  C07D309/04 ,  C07D401/12 ,  C07D405/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D407/12 ,  C07D487/08 ,  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 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：US10246469B2

公开(公告)日：2019-04-02

申请号：US15763281

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 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D237/08 ,  C07D239/26 ,  C07D213/34 ,  A61K31/50 ,  A61K31/51 ,  A61K31/505 ,  A61K31/506 ,  A61K31/44 ,  A61K31/4427 ,  A61P25/28 ,  C07D513/04 ,  A61P25/18 ,  A61P25/16 ,  C07D213/74

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：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：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：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：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：US12059420B2

公开(公告)日：2024-08-13

申请号：US17261954

申请日：2019-07-22

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： James Aaron Balog ,  Jay A. Markwalder ,  Weifang Shan ,  David K. Williams ,  Susheel Jethanand Nara ,  Saumya Roy ,  Soodamani Thangavel ,  Srinivas Cheruku ,  Ramesh Kumar Sistla

IPC: A61K31/506 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/519 ,  A61K31/5377 ,  A61K39/395 ,  C07D213/74 ,  C07D213/75 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D487/04

CPC classification number: A61K31/506 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/519 ,  A61K31/5377 ,  A61K39/3955 ,  C07D213/74 ,  C07D213/75 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D487/04

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：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.