公开(公告)号：US20230111912A1

公开(公告)日：2023-04-13

申请号：US17981887

申请日：2022-11-07

申请人： Incyte Corporation

发明人： Zhongjiang Jia ,  Ganfeng Cao ,  Qiyan Lin ,  Yongchun Pan ,  Lei Qiao ,  Vaqar Sharief ,  Chongsheng Eric Shi ,  Michael Xia ,  Changsheng Zheng ,  Jiacheng Zhou ,  Qun Li

IPC分类号： C07D401/14 ,  C07F7/18 ,  C07D401/12 ,  A61K31/4545

摘要： The present invention relates to salt forms of the Pim kinase inhibitor N-{(7R)-4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, including methods of preparation thereof, and intermediates in the preparation thereof, where the compound is useful in the treatment of Pim kinase-related diseases such as cancer.

公开(公告)号：US11505540B2

公开(公告)日：2022-11-22

申请号：US17147877

申请日：2021-01-13

申请人： Incyte Corporation

发明人： Zhongjiang Jia ,  Ganfeng Cao ,  Qiyan Lin ,  Yongchun Pan ,  Lei Qiao ,  Vaqar Sharief ,  Chongsheng Eric Shi ,  Michael Xia ,  Changsheng Zheng ,  Qun Li

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07F7/18 ,  A61K31/4545

摘要： The present invention relates to salt forms of the Pim kinase inhibitor N-{(7R)-4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, including methods of preparation thereof, and intermediates in the preparation thereof, where the compound is useful in the treatment of Pim kinase-related diseases such as cancer.

公开(公告)号：US12043614B2

公开(公告)日：2024-07-23

申请号：US17981887

申请日：2022-11-07

申请人： Incyte Corporation

发明人： Zhongjiang Jia ,  Ganfeng Cao ,  Qiyan Lin ,  Yongchun Pan ,  Lei Qiao ,  Vaqar Sharief ,  Chongsheng Eric Shi ,  Michael Xia ,  Changsheng Zheng ,  Jiacheng Zhou ,  Qun Li

IPC分类号： C07D401/14 ,  A61K31/4545 ,  C07D401/12 ,  C07F7/18

CPC分类号： C07D401/14 ,  A61K31/4545 ,  C07D401/12 ,  C07F7/1804 ,  C07B2200/13

摘要： The present invention relates to salt forms of the Pim kinase inhibitor N-{(7R)-4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, including methods of preparation thereof, and intermediates in the preparation thereof, where the compound is useful in the treatment of Pim kinase-related 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：US20190055237A1

公开(公告)日：2019-02-21

申请号：US15989414

申请日：2018-05-25

申请人： Incyte Corporation

发明人： Yongchun Pan ,  Chongsheng Eric Shi ,  Ming Tao ,  Wayne Han ,  Michael Xia ,  Dengjin Wang ,  Zhongjiang Jia ,  Jiacheng Zhou ,  Qun Li

IPC分类号： C07D471/04

摘要： The present disclosure relates to solid forms of N-{[2′-(2,6-difluoro-3,5-dimethoxyphenyl)-3′-oxo-2′,3′-dihydro-1′H-spiro[cyclopropane-1,4′-[2,7]naphthyridin]-6′-yl]methyl}acrylamide, methods of preparation thereof, and intermediates in the preparation thereof, which are useful in the treatment of the FGFR-associated or mediated diseases such as cancer.

公开(公告)号：US12024522B2

公开(公告)日：2024-07-02

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 ,  Jianji Wang

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.

公开(公告)号：US20230406852A1

公开(公告)日：2023-12-21

申请号：US18240805

申请日：2023-08-31

申请人： Incyte Corporation

发明人： Jiacheng Zhou ,  Shili Chen ,  Zhongjiang Jia ,  Yi Li ,  Qiyan Lin ,  Pingli Liu ,  Yongchun Pan ,  Timothy Martin ,  Bo Shen ,  Chongsheng Eric Shi ,  Naijing Su ,  Yongzhong Wu ,  Michael Xia

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： The present invention relates to processes of preparing PD-1/PD-L1 inhibitor (R)-1-((7-cyano-2-(3′-(3-(((R)-3-hydroxypyrrolidin-1-yl)methyl)-1,7-naphthyridin-8-ylamino)-2,2′-dimethylbiphenyl-3-yl)benzo[d]oxazol-5-yl)methyl)pyrrolidine-3-carboxylic acid, or salts thereof, related synthetic intermediates, and salts of the intermediates, where the PD-1/PD-L1 inhibitor is useful in the treatment of various diseases including infectious diseases and cancer.

公开(公告)号：US11780836B2

公开(公告)日：2023-10-10

申请号：US17520060

申请日：2021-11-05

申请人： Incyte Corporation

发明人： Jiacheng Zhou ,  Shili Chen ,  Zhongjiang Jia ,  Yi Li ,  Qiyan Lin ,  Pingli Liu ,  Yongchun Pan ,  Timothy Martin ,  Bo Shen ,  Chongsheng Eric Shi ,  Naijing Su ,  Yongzhong Wu ,  Michael Xia

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： The present invention relates to processes of preparing PD-1/PD-L1 inhibitor (R)-1-((7-cyano-2-(3′-(3-(((R)-3-hydroxypyrrolidin-1-yl)methyl)-1,7-naphthyridin-8-ylamino)-2,2′-dimethylbiphenyl-3-yl)benzo[d]oxazol-5-yl)methyl)pyrrolidine-3-carboxylic acid, or salts thereof, related synthetic intermediates, and salts of the intermediates, where the PD-1/PD-L1 inhibitor is useful in the treatment of various diseases including infectious diseases and cancer.

公开(公告)号：US11472801B2

公开(公告)日：2022-10-18

申请号：US16783839

申请日：2020-02-06

申请人： Incyte Corporation

发明人： Yongchun Pan ,  Chongsheng Eric Shi ,  Ming Tao ,  Wayne Han ,  Michael Xia ,  Dengjin Wang ,  Zhongjiang Jia ,  Jiacheng Zhou ,  Qun Li

IPC分类号： C07D471/04

摘要： The present disclosure relates to solid forms of N-{[2′-(2,6-difluoro-3,5-dimethoxyphenyl)-3′-oxo-2′,3′-dihydro-1′H-spiro[cyclopropane-1,4′-[2,7]naphthyridin]-6′-yl]methyl}acrylamide, methods of preparation thereof, and intermediates in the preparation thereof, which are useful in the treatment of the FGFR-associated or mediated diseases such as cancer.

公开(公告)号：US20220144830A1

公开(公告)日：2022-05-12

申请号：US17520060

申请日：2021-11-05

申请人： Incyte Corporation

发明人： Jiacheng Zhou ,  Shili Chen ,  Zhongjiang Jia ,  Yi Li ,  Qiyan Lin ,  Pingli Liu ,  Yongchun Pan ,  Timothy Martin ,  Bo Shen ,  Chongsheng Eric Shi ,  Naijing Su ,  Yongzhong Wu ,  Michael Xia

IPC分类号： C07D471/04

摘要： The present invention relates to processes of preparing PD-1/PD-L1 inhibitor (R)-1-((7-cyano-2-(3′-(3-(((R)-3-hydroxypyrrolidin-1-yl)methyl)-1,7-naphthyridin-8-ylamino)-2,2′-dimethylbiphenyl-3-yl)benzo[d]oxazol-5-yl)methyl)pyrrolidine-3-carboxylic acid, or salts thereof, related synthetic intermediates, and salts of the intermediates, where the PD-1/PD-L1 inhibitor is useful in the treatment of various diseases including infectious diseases and cancer.