公开(公告)号：US11787784B2

公开(公告)日：2023-10-17

申请号：US17358991

申请日：2021-06-25

申请人： Incyte Corporation

发明人： Zhongjiang Jia ,  William Frietze

IPC分类号： C07D403/14 ,  C07D403/12

CPC分类号： C07D403/14 ,  C07D403/12 ,  C07B2200/13

摘要： The present invention relates to salt forms of the hematopoietic progenitor kinase 1 (HPK1) inhibitors N-(2-((2S,4S)-4-Amino-2-(hydroxymethyl)pyrrolidin-1-yl)-5-fluorophenyl)-2-(2-fluoro-6-methoxyphenyl)pyrimidine-4-carboxamide and N-(2-((2S,4S)-4-Amino-2-(hydroxymethyl)pyrrolidin-1-yl)-4-(4-cyanopyridin-3-yl)phenyl)-2-(2-fluoro-6-methoxyphenyl)pyrimidine-4-carboxamide, including methods of preparation thereof, where the compounds are useful in the treatment of HPK1 mediated diseases such as cancer.

公开(公告)号：US20210079016A1

公开(公告)日：2021-03-18

申请号：US16952915

申请日：2020-11-19

申请人： Incyte Corporation

发明人： Shili Chen ,  William Frietze ,  Zhongjiang Jia ,  Pingli Liu ,  Jiacheng Zhou

IPC分类号： C07D498/04 ,  C07D413/04

摘要： The present invention relates to an amorphous solid form of (4S)-7-(3,5-dimethylisoxazol-4-yl)-4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one, and processes for its preparation, which is an inhibitor of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and is useful in the treatment of various diseases such as cancer.

公开(公告)号：US10858372B2

公开(公告)日：2020-12-08

申请号：US16425193

申请日：2019-05-29

申请人： Incyte Corporation

发明人： Shili Chen ,  William Frietze ,  Zhongjiang Jia ,  Pingli Liu ,  Jiacheng Zhou

IPC分类号： C07D498/04 ,  C07D413/04 ,  A61K31/535

摘要： The present invention relates to an amorphous solid form of (4S)-7-(3,5-dimethylisoxazol-4-yl)-4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one, and processes for its preparation, which is an inhibitor of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and is useful in the treatment of various diseases such as cancer.

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：US20170121347A1

公开(公告)日：2017-05-04

申请号：US15337202

申请日：2016-10-28

申请人： Incyte Corporation

发明人： Shili Chen ,  William Frietze ,  Zhongjiang Jia ,  Pingli Liu ,  Jiacheng Zhou

IPC分类号： C07D498/04 ,  C07D413/04

CPC分类号： C07D498/04 ,  A61K31/535 ,  C07D413/04

摘要： The present invention relates to an amorphous solid form of (4S)-7-(3,5-dimethylisoxazol-4-yl)-4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one, and processes for its preparation, which is an inhibitor of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and is useful in the treatment of various diseases such as cancer.

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：US20230219976A1

公开(公告)日：2023-07-13

申请号：US18104045

申请日：2023-01-31

申请人： Incyte Corporation

发明人： Shili Chen ,  William Frietze ,  Zhongjiang Jia ,  Pingli Liu ,  Jiacheng Zhou

IPC分类号： C07D498/04 ,  C07D413/04 ,  A61K31/535

CPC分类号： C07D498/04 ,  C07D413/04 ,  A61K31/535

摘要： The present invention relates to an amorphous solid form of (4S)-7-(3,5-dimethylisoxazol-4-yl)-4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one, and processes for its preparation, which is an inhibitor of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and is useful in the treatment of various diseases such as cancer.

公开(公告)号：US20190300545A1

公开(公告)日：2019-10-03

申请号：US16425193

申请日：2019-05-29

申请人： Incyte Corporation

发明人： Shili Chen ,  William Frietze ,  Zhongjiang Jia ,  Pingli Liu ,  Jiacheng Zhou

IPC分类号： C07D498/04 ,  C07D413/04

摘要： The present invention relates to an amorphous solid form of (4S)-7-(3,5-dimethylisoxazol-4-yl)-4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one, and processes for its preparation, which is an inhibitor of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and is useful in the treatment of various diseases such as cancer.

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.