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：US11753406B2

公开(公告)日：2023-09-12

申请号：US16987557

申请日：2020-08-07

申请人： Incyte Corporation

发明人： Zhongjiang Jia ,  Pingli Liu ,  David J. Meloni ,  Yongchun Pan ,  Yongzhong Wu ,  Jiacheng Zhou ,  Qun Li

IPC分类号： C07D471/04 ,  A61K9/00

CPC分类号： C07D471/04 ,  A61K9/0053 ,  C07B2200/13

摘要： The present invention relates to salt forms of the 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, including methods of preparation thereof, where the compound is useful in the treatment of various diseases including infectious diseases and cancer.

公开(公告)号：US11512064B2

公开(公告)日：2022-11-29

申请号：US17200082

申请日：2021-03-12

申请人： Incyte Corporation

发明人： Zhongjiang Jia ,  Wayne Han ,  Yongchun Pan ,  Timothy Martin ,  Jiacheng Zhou ,  Qun Li

IPC分类号： C07D401/04 ,  A61K9/00

摘要： The present invention relates to processes and intermediates for preparing 3-(cyanomethyl)-3-(4-{[(1R,2S)-2-phenylcyclopropyl]amino}piperidin-1-yl)azetidine-1-sulfonamide, and salts and solid forms thereof, which selectively modulate demethylase. Particular embodiments contemplate compounds and disease indications amenable to treatment by modulation of lysine specific demethylase-1 (LSD1).

公开(公告)号：US11001571B2

公开(公告)日：2021-05-11

申请号：US16555620

申请日：2019-08-29

申请人： Incyte Corporation

发明人： Yun-Long Li ,  Jincong Zhuo ,  Ding-Quan Qian ,  Song Mei ,  Ganfeng Cao ,  Yongchun Pan ,  Qun Li ,  Zhongjiang Jia

IPC分类号： C07D403/14 ,  A61P37/06

摘要： The present invention provides compounds of Formula I: or pharmaceutically acceptable salts thereof, as well as their compositions and methods of use, that inhibit the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.

公开(公告)号：US20200071289A1

公开(公告)日：2020-03-05

申请号：US16555907

申请日：2019-08-29

申请人： Incyte Corporation

发明人： Zhongjiang Jia ,  Wayne Han ,  Yongchun Pan ,  Timothy Martin ,  Jiacheng Zhou ,  Qun Li

IPC分类号： C07D401/04 ,  A61K9/00

摘要： The present invention relates to processes and intermediates for preparing 3-(cyanomethyl)-3-(4-{[(1R,2S)-2-phenylcyclopropyl]amino}piperidin-1-yl)azetidine-1-sulfonamide, and salts and solid forms thereof, which selectively modulate demethylase. Particular embodiments contemplate compounds and disease indications amenable to treatment by modulation of lysine specific demethylase-1 (LSD1).

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：US20180170907A1

公开(公告)日：2018-06-21

申请号：US15825306

申请日：2017-11-29

申请人： Incyte Corporation

发明人： Zhongjiang Jia ,  Qun Li

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

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

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：US20140343030A1

公开(公告)日：2014-11-20

申请号：US14279929

申请日：2014-05-16

申请人： Incyte Corporation

发明人： Yun-Long Li ,  Jincong Zhuo ,  Ding-Quan Qian ,  Song Mei ,  Ganfeng Cao ,  Yongchun Pan ,  Qun Li ,  Zhongjiang Jia

IPC分类号： C07D403/14

CPC分类号： C07D403/14

摘要： The present invention provides compounds of Formula I: or pharmaceutically acceptable salts thereof, as well as their compositions and methods of use, that inhibit the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.

摘要翻译： 本发明提供式I化合物或其药学上可接受的盐，以及它们的组合物和使用方法，其抑制Janus激酶（JAK）的活性，并且可用于治疗与JAK的活性有关的疾病，包括 ，例如炎症性疾病，自身免疫性疾病，癌症和其它疾病。

公开(公告)号：US20240132523A1

公开(公告)日：2024-04-25

申请号：US18516438

申请日：2023-11-21

申请人： Incyte Corporation

发明人： Zhongjiang Jia ,  Shili Chen ,  Yi Li ,  Timothy Martin ,  Bo Shen ,  Naijing Su ,  Jiacheng Zhou ,  Qun Li

IPC分类号： C07D519/00 ,  A61K9/00 ,  C07C61/135 ,  C07C211/56

CPC分类号： C07D519/00 ,  A61K9/0053 ,  C07C61/135 ,  C07C211/56 ,  C07B2200/13

摘要： This application relates to solid forms and salt forms of the PD-1/PD-L1 inhibitor 4,4′-(((((2,2′-dichloro-[1,1′-biphenyl]-3,3′-diyl)bis(azanediyl))bis(carbonyl))bis(1-methyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridine-2,5-diyl))bis(ethane-2,1-diyl))bis(bicyclo[2.2.1]heptane-1-carboxylic acid), including processes of preparation thereof, where the solid forms and salt forms are useful in the treatment of various diseases including infectious diseases and cancer.

公开(公告)号：US11866451B2

公开(公告)日：2024-01-09

申请号：US17094396

申请日：2020-11-10

申请人： Incyte Corporation

发明人： Zhongjiang Jia ,  Shili Chen ,  Yi Li ,  Timothy Martin ,  Bo Shen ,  Naijing Su ,  Jiacheng Zhou ,  Qun Li

IPC分类号： C07D519/00 ,  A61K9/00 ,  C07C61/135 ,  C07C211/56

CPC分类号： C07D519/00 ,  A61K9/0053 ,  C07C61/135 ,  C07C211/56 ,  C07B2200/13

摘要： This application relates to solid forms and salt forms of the PD-1/PD-L1 inhibitor 4,4′-(((((2,2′-dichloro-[1,1′-biphenyl]-3,3′-diyl)bis(azanediyl))bis(carbonyl))bis(1-methyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridine-2,5-diyl))bis(ethane-2,1-diyl))bis(bicyclo[2.2.1]heptane-1-carboxylic acid), including processes of preparation thereof, where the solid forms and salt forms are useful in the treatment of various diseases including infectious diseases and cancer.