公开(公告)号：US20220331296A1

公开(公告)日：2022-10-20

申请号：US17527833

申请日：2021-11-16

申请人： Incyte Corporation ,  Incyte Holdings Corporation

发明人： Andrew P. Combs ,  Eddy W. Yue ,  Richard B. Sparks ,  Wenyu Zhu ,  Jiacheng Zhou ,  Qiyan Lin ,  Lingkai Weng ,  Tai-Yuen Yue ,  Pingli Liu

IPC分类号： A61K31/4245 ,  C07D271/08 ,  A61K39/395 ,  C07D413/12 ,  C07D413/04

摘要： The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.

公开(公告)号：US20190167692A1

公开(公告)日：2019-06-06

申请号：US16269871

申请日：2019-02-07

申请人： Incyte Corporation ,  Incyte Holdings Corporation

发明人： Lingkai Weng ,  Lei Qiao ,  Jiacheng Zhou ,  Pingli Liu ,  Yongchun Pan

IPC分类号： A61K31/53 ,  C07D487/04 ,  C07D253/07 ,  C07D401/10

摘要： The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.

公开(公告)号：US09873688B2

公开(公告)日：2018-01-23

申请号：US15093486

申请日：2016-04-07

申请人： Incyte Corporation ,  Incyte Holdings Corporation

发明人： Ming Tao ,  William Frietze ,  David J. Meloni ,  Lingkai Weng ,  Jiacheng Zhou ,  Yongchun Pan

IPC分类号： C07D413/04 ,  C07D271/08 ,  C07D271/07 ,  C07C307/06 ,  C07D271/04

CPC分类号： C07D413/04 ,  C07C307/06 ,  C07D271/04 ,  C07D271/08

摘要： The present application is directed to processes and intermediates for making 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful in the treatment of cancer and other disorders.

公开(公告)号：US20220024934A1

公开(公告)日：2022-01-27

申请号：US17365888

申请日：2021-07-01

申请人： Incyte Corporation

发明人： Lei Qiao ,  Lingkai Weng ,  Chongsheng Eric Shi ,  David Meloni ,  Qiyan Lin ,  Michael Xia ,  Vaqar Sharief ,  William Frietze ,  Zhongjiang Jia ,  Yongchun Pan ,  Pingli Liu ,  Tai-Yuen Yue ,  Jiacheng Zhou

IPC分类号： C07D487/04

摘要： The present application provides processes for preparing (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, which is useful as an inhibitor phosphoinositide 3-kinase-delta (PI3Kδ), as well as a salt form and intermediates related thereto.

公开(公告)号：US20210030722A1

公开(公告)日：2021-02-04

申请号：US16849610

申请日：2020-04-15

申请人： Incyte Corporation ,  Incyte Holdings Corporation

发明人： Andrew P. Combs ,  Eddy W. Yue ,  Richard B. Sparks ,  Wenyu Zhu ,  Jiacheng Zhou ,  Qiyan Lin ,  Lingkai Weng ,  Tai-Yuen Yue ,  Pingli Liu

IPC分类号： A61K31/4245 ,  C07D271/08 ,  A61K39/395 ,  C07D413/12 ,  C07D413/04

摘要： The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.

公开(公告)号：US20170258800A1

公开(公告)日：2017-09-14

申请号：US15355630

申请日：2016-11-18

申请人： Incyte Corporation ,  Incyte Holdings Corporation

发明人： Lingkai Weng ,  Lei Qiao ,  Jiacheng Zhou ,  Pingli Liu ,  Yongchun Pan

IPC分类号： A61K31/53 ,  C07D401/10 ,  C07D487/04 ,  C07D253/07

CPC分类号： A61K31/53 ,  C07D253/07 ,  C07D401/10 ,  C07D487/04

摘要： The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.

公开(公告)号：US20160257689A1

公开(公告)日：2016-09-08

申请号：US15054474

申请日：2016-02-26

申请人： Incyte Corporation

发明人： Lei Qiao ,  Lingkai Weng ,  ChongShen Eric Shi ,  David Meloni ,  Qiyan Lin ,  Michael Xia ,  Vaqar Sharief ,  William Frietze ,  Zhongjiang Jia ,  Yongchun Pan ,  Pingli Liu ,  Tai-Yuen Yue ,  Jiacheng Zhou

IPC分类号： C07D487/04

CPC分类号： C07D487/04 ,  C07B2200/13

摘要： The present application provides processes for preparing (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, which is useful as an inhibitor phosphoinositide 3-kinase-delta (PI3Kδ), as well as a salt form and intermediates related thereto.

摘要翻译： 本申请提供了制备（R）-4-（3 - （（S）-1-（4-氨基-3-甲基-1H-吡唑并[3,4-d]嘧啶-1-基）乙基） -5-氯-2-乙氧基-6-氟苯基）吡咯烷-2-酮，其可用作抑制剂磷酸肌醇3-激酶-δ（PI3Kδ），以及与其相关的盐形式和中间体。

公开(公告)号：US20160221996A1

公开(公告)日：2016-08-04

申请号：US15093486

申请日：2016-04-07

申请人： Incyte Corporation ,  Incyte Holdings Corporation

发明人： Ming Tao ,  William Frietze ,  David J. Meloni ,  Lingkai Weng ,  Jiacheng Zhou ,  Yongchun Pan

IPC分类号： C07D413/04

CPC分类号： C07D413/04 ,  C07C307/06 ,  C07D271/04 ,  C07D271/08

摘要： The present application is directed to processes and intermediates for making 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful in the treatment of cancer and other disorders.

公开(公告)号：US20240173303A1

公开(公告)日：2024-05-30

申请号：US18213019

申请日：2023-06-22

申请人： Incyte Corporation ,  Incyte Holdings Corporation

发明人： Andrew P. Combs ,  Eddy W. Yue ,  Richard B. Sparks ,  Wenyu Zhu ,  Jiacheng Zhou ,  Qiyan Lin ,  Lingkai Weng ,  Tai-Yuen Yue ,  Pingli Liu

IPC分类号： A61K31/4245 ,  A61K39/395 ,  C07D271/08 ,  C07D413/04 ,  C07D413/12

CPC分类号： A61K31/4245 ,  A61K39/3955 ,  C07D271/08 ,  C07D413/04 ,  C07D413/12

摘要： The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.

公开(公告)号：US11452726B2

公开(公告)日：2022-09-27

申请号：US17014414

申请日：2020-09-08

申请人： Incyte Corporation ,  Incyte Holdings Corporation

发明人： Lingkai Weng ,  Lei Qiao ,  Jiacheng Zhou ,  Pingli Liu ,  Yongchun Pan

IPC分类号： C07D253/07 ,  A61K31/53 ,  C07D401/10 ,  C07D487/04

摘要： The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.