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公开(公告)号:US09771320B2
公开(公告)日:2017-09-26
申请号:US15109741
申请日:2015-01-05
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: Jingwu Duan , T. G. Murali Dhar , Bin Jiang , Zhonghui Lu , Ananta Karmakar , Arun Kumar Gupta , Carolyn A. Weigelt
IPC: C07C317/14 , C07D213/81 , C07D401/04 , C07D237/08 , C07C317/20 , C07C317/30 , C07C317/46 , C07D471/04 , C07D213/30 , C07D213/56 , C07D309/04 , C07D309/14 , C07D317/44 , C07D231/12 , C07D239/38 , C07D241/12 , C07D471/10 , C07D257/04 , C07D261/08 , C07D263/32 , C07D271/06 , C07D211/36 , C07D295/16 , C07D295/20 , C07D303/06 , C07D305/14 , C07D205/04 , C07D211/62 , C07D213/40 , C07D213/75 , C07D295/155 , C07D295/108 , C07D319/20 , C07D285/06 , C07D295/18 , C07D295/22 , C07D303/34 , C07C317/22 , C07C317/44 , C07C317/32 , C07C317/50 , C07D213/85 , C07D295/185
CPC classification number: C07C317/14 , C07C317/20 , C07C317/22 , C07C317/30 , C07C317/32 , C07C317/44 , C07C317/46 , C07C317/50 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07D205/04 , C07D211/36 , C07D211/62 , C07D213/30 , C07D213/40 , C07D213/56 , C07D213/75 , C07D213/81 , C07D213/85 , C07D231/12 , C07D237/08 , C07D239/38 , C07D241/12 , C07D257/04 , C07D261/08 , C07D263/32 , C07D271/06 , C07D285/06 , C07D295/108 , C07D295/155 , C07D295/18 , C07D295/185 , C07D295/20 , C07D295/22 , C07D303/06 , C07D303/34 , C07D305/14 , C07D309/04 , C07D309/14 , C07D317/44 , C07D319/20 , C07D401/04 , C07D471/04 , C07D471/10
Abstract: Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.
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公开(公告)号:US20200347071A1
公开(公告)日:2020-11-05
申请号:US16963886
申请日:2019-01-24
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: Scott Hunter Watterson , Murugaiah Andappan Murugaiah Subbaiah , Carolyn Diane Dzierba , Hua Gong , Jason M. Guernon , Junqing Guo , Amy C. Hart , Guanglin Luo , John E. Macor , William J. Pitts , Jianliang Shi , Brian Lee Venables , Carolyn A. Weigelt , Yong-Jin Wu , Zhizhen Barbara Zheng , Sing-Yuen Sit , Jie Chen
IPC: C07D487/04
Abstract: The disclosure relates to compounds of formula I which are useful as kinase modulators including RIPK 1 modulation. The disclosure also provides methods of making and using the compounds for example in treatments related to necrosis or inflammation as well as other indications.
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公开(公告)号:US09708253B2
公开(公告)日:2017-07-18
申请号:US15109733
申请日:2015-01-05
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: Jingwu Duan , T. G. Murali Dhar , Bin Jiang , Ananta Karmakar , Arun Kumar Gupta , Zhonghui Lu , Carolyn A. Weigelt
IPC: C07C317/20 , C07C317/24 , C07C317/30 , C07D205/04 , C07D207/27 , C07D211/46 , C07D211/78 , C07D213/30 , C07D231/12 , C07D213/81 , C07D213/82 , C07D309/08 , C07D231/14 , C07D231/56 , C07D401/04 , C07D403/04 , C07D237/08 , C07D237/20 , C07D237/24 , C07D405/04 , C07D239/28 , C07C317/46 , C07D241/24 , C07D249/04 , C07D471/04 , C07D207/277 , C07D277/60 , C07D295/096 , C07D211/48 , C07D211/62 , C07D295/185 , C07D213/56 , C07D213/71 , C07D213/75 , C07D309/04 , C07D335/02 , C07D401/06 , C07D401/12 , C07D295/205 , C07D213/40 , C07D231/54 , C07D237/22 , C07D249/06 , C07D277/82 , C07D295/16 , C07D295/195
CPC classification number: C07C317/20 , C07C317/24 , C07C317/30 , C07C317/46 , C07C2601/02 , C07C2601/14 , C07D205/04 , C07D207/27 , C07D207/277 , C07D211/46 , C07D211/48 , C07D211/62 , C07D211/78 , C07D213/30 , C07D213/40 , C07D213/56 , C07D213/71 , C07D213/75 , C07D213/81 , C07D213/82 , C07D231/12 , C07D231/14 , C07D231/54 , C07D231/56 , C07D237/08 , C07D237/20 , C07D237/22 , C07D237/24 , C07D239/28 , C07D241/24 , C07D249/04 , C07D249/06 , C07D277/60 , C07D277/82 , C07D295/096 , C07D295/16 , C07D295/185 , C07D295/195 , C07D295/205 , C07D309/04 , C07D309/08 , C07D335/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D405/04 , C07D471/04
Abstract: Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.
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公开(公告)号:US11618753B2
公开(公告)日:2023-04-04
申请号:US16963886
申请日:2019-01-24
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: Scott Hunter Watterson , Murugaiah Andappan Murugaiah Subbaiah , Carolyn Diane Dzierba , Hua Gong , Jason M. Guernon , Junqing Guo , Amy C. Hart , Guanglin Luo , John E. Macor , William J. Pitts , Jianliang Shi , Brian Lee Venables , Carolyn A. Weigelt , Yong-Jin Wu , Zhizhen Barbara Zheng , Sing-Yuen Sit , Jie Chen
IPC: A61K31/53 , C07D253/08 , C07D487/04
Abstract: The disclosure relates to compounds of formula I which are useful as kinase modulators including RIPK 1 modulation. The disclosure also provides methods of making and using the compounds for example in treatments related to necrosis or inflammation as well as other indications.
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公开(公告)号:US10435369B2
公开(公告)日:2019-10-08
申请号:US15806554
申请日:2017-11-08
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: David Marcoux , Myra Beaudoin Bertrand , T. G. Murali Dhar , Michael G. Yang , Zili Xiao , Hai-Yun Xiao , Yeheng Zhu , Carolyn A. Weigelt , Douglas G. Batt
IPC: C07C317/12 , C07C317/44 , A61K31/10 , C07D211/48 , A61P37/00 , C07D205/04 , C07D205/08 , C07D207/10 , C07D207/16 , C07D207/277 , C07D211/96 , C07D213/40 , C07D213/75 , C07D231/08 , C07D241/08 , C07D257/04 , C07D295/195 , C07D307/22 , C07D309/10 , C07D333/48 , C07D335/02 , C07D471/04 , C07D471/10 , C07D213/81 , C07D215/36 , C07D231/06 , C07D231/18 , C07D233/64 , C07D233/76 , C07D233/78 , C07D233/90 , C07D401/04 , C07D401/12 , C07D405/04 , C07C317/20 , C07C317/24 , C07C317/30 , C07D405/12 , C07D249/12 , C07D261/18 , C07D263/20 , C07D207/09 , C07D207/28 , C07D285/06 , C07D211/62 , C07D295/16 , C07D211/78 , C07D213/56 , C07D305/08 , C07F9/09
Abstract: There are described RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.
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公开(公告)号:US20180127368A1
公开(公告)日:2018-05-10
申请号:US15806554
申请日:2017-11-08
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: David Marcoux , Myra Beaudoin Bertrand , T.G. Murali Dhar , Michael G. Yang , Zili Xiao , Hai-Yun Xiao , Yeheng Zhu , Carolyn A. Weigelt , Douglas G Batt
IPC: C07D211/48 , C07D213/40 , C07D295/195 , C07D213/75 , C07D333/48 , C07C317/44 , C07D335/02 , C07D471/04 , C07D307/22 , C07D241/08 , C07D207/10 , C07D207/16 , C07D231/08 , C07D309/10 , C07D211/96 , C07D471/10 , C07D205/04 , C07D207/277 , C07D257/04 , C07D205/08 , A61P37/00
CPC classification number: C07D211/48 , A61P37/00 , C07B2200/05 , C07B2200/07 , C07C317/20 , C07C317/24 , C07C317/30 , C07C317/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/38 , C07C2602/44 , C07C2602/50 , C07C2603/08 , C07C2603/12 , C07C2603/16 , C07C2603/90 , C07D205/04 , C07D205/08 , C07D207/09 , C07D207/10 , C07D207/16 , C07D207/277 , C07D207/28 , C07D211/62 , C07D211/78 , C07D211/96 , C07D213/40 , C07D213/56 , C07D213/75 , C07D213/81 , C07D215/36 , C07D231/06 , C07D231/08 , C07D231/18 , C07D233/64 , C07D233/76 , C07D233/78 , C07D233/90 , C07D241/08 , C07D249/12 , C07D257/04 , C07D261/18 , C07D263/20 , C07D285/06 , C07D295/16 , C07D295/195 , C07D305/08 , C07D307/22 , C07D309/10 , C07D333/48 , C07D335/02 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D471/04 , C07D471/10 , C07F9/091
Abstract: There are described RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.
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公开(公告)号:US20180002358A1
公开(公告)日:2018-01-04
申请号:US15701818
申请日:2017-09-12
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: Jingwu Duan , T.G. Murali Dhar , David Marcoux , Qing Shi , Douglas G. Batt , Qingjie Liu , Robert J. Cherney , Lyndon A.M. Cornelius , Anurag S. Srivastava , Myra Beaudoin Bertrand , Carolyn A. Weigelt
IPC: C07F9/6574 , C07D209/30 , C07D493/08 , C07D491/107 , C07D491/052 , C07D471/04 , C07D417/14 , C07D417/12 , C07D417/06 , C07D417/04 , C07D413/12 , C07D413/10 , C07D413/06 , C07D409/06 , C07D409/04 , C07D405/06 , C07D403/12 , C07D403/06 , C07D401/12 , C07D401/06 , C07D221/10 , C07D215/36 , C07D209/70 , C07D209/60 , C07D495/04 , C07D495/08
CPC classification number: C07F9/65742 , C07D209/30 , C07D209/60 , C07D209/70 , C07D215/36 , C07D221/10 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D409/04 , C07D409/06 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/052 , C07D491/107 , C07D493/08 , C07D495/04 , C07D495/08
Abstract: There are described RORγ modulators of the formula (I), and formula (II) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.
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公开(公告)号:US09815859B2
公开(公告)日:2017-11-14
申请号:US15148209
申请日:2016-05-06
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: Jingwu Duan , T. G. Murali Dhar , David Marcoux , Qing Shi , Douglas G. Batt , Qingjie Liu , Robert J. Cherney , Lyndon A. M. Cornelius , Anurag S. Srivastava , Myra Beaudoin Bertrand , Carolyn A. Weigelt
IPC: A61K31/437 , C07F9/6574 , C07D215/36 , C07D409/04 , C07D417/04 , C07D209/30 , C07D209/60 , C07D209/70 , C07D221/10 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D409/06 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/052 , C07D491/107 , C07D493/08 , C07D495/04 , C07D495/08
CPC classification number: C07F9/65742 , C07D209/30 , C07D209/60 , C07D209/70 , C07D215/36 , C07D221/10 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D409/04 , C07D409/06 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/052 , C07D491/107 , C07D493/08 , C07D495/04 , C07D495/08
Abstract: There are described RORγ modulators of the formula (I), and formula (II) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.
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公开(公告)号:US20160326195A1
公开(公告)日:2016-11-10
申请号:US15148209
申请日:2016-05-06
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: Jingwu Duan , T.G. Murali Dhar , David Marcoux , Qing Shi , Douglas G. Batt , Qingjie Liu , Robert J. Cherney , Lyndon A.M. Cornelius , Anurag S. Srivastava , Myra Beaudoin Bertrand , Carolyn A. Weigelt
IPC: C07F9/6574 , C07D221/10 , C07D401/06 , C07D209/70 , C07D409/06 , C07D491/052 , C07D401/12 , C07D403/06 , C07D417/06 , C07D493/08 , C07D405/06 , C07D413/10 , C07D413/06 , C07D471/04 , C07D417/14 , C07D495/04 , C07D495/08 , C07D417/12 , C07D413/12 , C07D403/12 , C07D491/107 , C07D209/60
CPC classification number: C07F9/65742 , C07D209/30 , C07D209/60 , C07D209/70 , C07D215/36 , C07D221/10 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D409/04 , C07D409/06 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/052 , C07D491/107 , C07D493/08 , C07D495/04 , C07D495/08
Abstract: There are described RORγ modulators of the formula (I), and formula (II) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.
Abstract translation: 或其立体异构体,互变异构体,其药学上可接受的盐,溶剂合物或前药,其中所有取代基均在本文中定义。 还提供了包含其的药物组合物。 这样的化合物和组合物可用于调节细胞中RORγ活性的方法和用于治疗受试者治疗受益于RORγ活性(例如自身免疫和/或炎症性疾病)的疾病或病症的受试者的方法。
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