公开(公告)号：US20210107901A1

公开(公告)日：2021-04-15

申请号：US17067203

申请日：2020-10-09

申请人： Incyte Corporation

发明人： Yingda Ye ,  Zhenwu Li ,  Ding-Quan Qian ,  Sarah Winterton ,  Kaijiong Xiao ,  Liangxing Wu ,  Wenqing Yao ,  Joshua Hummel ,  Meizhong Xu ,  Min Ye ,  Yingnan Chen ,  Margaret Favata ,  Yvonne Lo

IPC分类号： C07D471/04 ,  C07D519/00 ,  C07D487/04

摘要： The present application provides bicyclic amines that are inhibitors of cyclin-dependent kinase 2 (CDK2), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.

公开(公告)号：US10947230B2

公开(公告)日：2021-03-16

申请号：US16566509

申请日：2019-09-10

申请人： Incyte Corporation ,  Incyte Holdings Corporation

发明人： Yaping Sun ,  Wenqing Yao ,  Liangxing Wu ,  Meizhong Xu ,  Ding-Quan Qian ,  Fenglei Zhang

IPC分类号： C07D471/04 ,  A61P35/00 ,  A61K31/4375

摘要： The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

公开(公告)号：US10806785B2

公开(公告)日：2020-10-20

申请号：US15851497

申请日：2017-12-21

申请人： Incyte Corporation

发明人： Liang Lu ,  Wenyu Zhu ,  Ding-Quan Qian ,  Kaijiong Xiao

IPC分类号： A61K39/39 ,  A61P37/00 ,  A61P37/04 ,  A61P35/00 ,  A61K45/06 ,  C07D213/81 ,  C07D263/57 ,  C07D413/06 ,  C07D413/14 ,  C07D471/04 ,  C07D519/00 ,  G01N33/50 ,  A61K39/00

摘要： Compositions and methods for inducing PD-L1 internalization are disclosed. The methods include reducing the amount of cell surface PD-L1 by contacting a cell expressing PD-L1 with a compound that binds to cell surface PD-L1 and induces PD-L1 internalization. Compounds that induce PD-L1 internalization can be used to enhance, stimulate and/or increase an immune response and treat a PD-1-related disease or condition.

公开(公告)号：US20200317680A1

公开(公告)日：2020-10-08

申请号：US16909686

申请日：2020-06-23

申请人： Incyte Corporation ,  Incyte Holdings Corporation

发明人： Jincong Zhuo ,  Meizhong Xu ,  Chunhong He ,  Colin Zhang ,  Ding-Quan Qian ,  David M. Burns ,  Yun-Long Li ,  Brian Metcalf ,  Wenqing Yao

IPC分类号： C07D487/04 ,  A61K31/53 ,  A61K31/4709 ,  C07D403/06 ,  A61P35/00

摘要： The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.

公开(公告)号：US20190241560A1

公开(公告)日：2019-08-08

申请号：US16239051

申请日：2019-01-03

申请人： Incyte Corporation

发明人： Liang Lu ,  Liangxing Wu ,  Ding-Quan Qian ,  Wenqing Yao

IPC分类号： C07D471/04

摘要： The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR4 enzyme and are useful in the treatment of FGFR4-associated diseases such as cancer.

公开(公告)号：US20190211014A1

公开(公告)日：2019-07-11

申请号：US16195026

申请日：2018-11-19

申请人： Incyte Corporation

发明人： Liangxing Wu ,  Joel R. Courter ,  Chunhong He ,  Ding-Quan Qian ,  Bo Shen ,  Xiaozhao Wang ,  Wenqing Yao ,  Fenglei Zhang

IPC分类号： C07D471/10 ,  C07D211/32 ,  C07D401/12 ,  C07D401/06 ,  C07D211/58 ,  C07D205/04 ,  A61K31/506 ,  A61K31/497 ,  A61K31/454 ,  A61K31/445 ,  A61K31/4523 ,  A61K31/435 ,  A61K31/4468 ,  A61K31/397 ,  A61K45/06 ,  C07D211/16 ,  C07D211/14 ,  C07D211/34

摘要： The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

公开(公告)号：US20180282340A1

公开(公告)日：2018-10-04

申请号：US15925996

申请日：2018-03-20

申请人： Incyte Corporation ,  Incyte Holdings Corporation

发明人： Jincong Zhuo ,  Meizhong Xu ,  Chunhong He ,  Colin Zhang ,  Ding-Quan Qian ,  David M. Burns ,  Yun-Long Li ,  Brian Metcalf ,  Wenqing Yao

IPC分类号： C07D487/04 ,  A61K31/53 ,  A61K31/4709 ,  C07D403/06

摘要： The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.

公开(公告)号：US20180177870A1

公开(公告)日：2018-06-28

申请号：US15851497

申请日：2017-12-21

申请人： Incyte Corporation

发明人： Phillip C. Liu ,  Alla Volgina ,  Richard Wynn ,  Nina Zolotarjova ,  Liangxing Wu ,  Kaijiong Xiao ,  Song Mei ,  Liang Lu ,  Wenyu Zhu ,  Yingda Ye ,  Haisheng Wang ,  Ding-Quan Qian ,  Wenqing Yao

IPC分类号： A61K39/39 ,  A61K45/06 ,  G01N33/50 ,  C07D471/04 ,  C07D213/81 ,  C07D519/00 ,  C07D413/06 ,  C07D263/57 ,  C07D413/14 ,  A61P35/00 ,  A61P37/04

摘要： Compositions and methods for inducing PD-L1 internalization are disclosed. The methods include reducing the amount of cell surface PD-L1 by contacting a cell expressing PD-L1 with a compound that binds to cell surface PD-L1 and induces PD-L1 internalization. Compounds that induce PD-L1 internalization can be used to enhance, stimulate and/or increase an immune response and treat a PD-1-related disease or condition.

公开(公告)号：US09957229B2

公开(公告)日：2018-05-01

申请号：US15602693

申请日：2017-05-23

申请人： Incyte Corporation ,  Incyte Holdings Corporation

发明人： Wenqing Yao ,  Jincong Zhuo ,  Meizhong Xu ,  Colin Zhang ,  Brian W. Metcalf ,  Chunhong He ,  Ding-Quan Qian

IPC分类号： C07D471/10 ,  C07D207/06 ,  A61K31/407 ,  C07D491/107 ,  C07D513/10 ,  C07D498/20 ,  C07D495/04 ,  C07D493/10 ,  C07D491/20 ,  C07D491/10 ,  C07D487/10 ,  C07D487/08 ,  C07D487/04 ,  C07D471/04 ,  C07D417/04 ,  C07D413/14 ,  C07D413/10 ,  C07D405/14 ,  C07D405/04 ,  C07D403/04 ,  C07D401/14 ,  C07D401/10 ,  C07D401/06 ,  C07D401/04 ,  C07D333/34 ,  C07D295/185 ,  C07D221/20 ,  C07D217/26 ,  C07D217/06 ,  C07D213/38 ,  C07D211/70 ,  C07D211/66 ,  C07D211/64 ,  C07D211/58 ,  C07D211/52 ,  C07D211/48 ,  C07D211/46 ,  C07D211/34 ,  C07D211/22 ,  C07D211/18 ,  C07D211/16 ,  C07D209/70 ,  C07D209/62 ,  C07D209/52 ,  C07D209/44 ,  C07D209/42 ,  C07D209/08 ,  C07D207/27 ,  C07D207/16 ,  C07D207/14 ,  C07D207/12 ,  C07D207/10 ,  C07D207/08 ,  A61K31/4439

CPC分类号： C07D207/06 ,  A61K31/407 ,  A61K31/4439 ,  C07D207/08 ,  C07D207/10 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D207/27 ,  C07D209/08 ,  C07D209/42 ,  C07D209/44 ,  C07D209/52 ,  C07D209/62 ,  C07D209/70 ,  C07D211/16 ,  C07D211/18 ,  C07D211/22 ,  C07D211/34 ,  C07D211/46 ,  C07D211/48 ,  C07D211/52 ,  C07D211/58 ,  C07D211/64 ,  C07D211/66 ,  C07D211/70 ,  C07D213/38 ,  C07D217/06 ,  C07D217/26 ,  C07D221/20 ,  C07D295/185 ,  C07D333/34 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/10 ,  C07D491/107 ,  C07D491/20 ,  C07D493/10 ,  C07D495/04 ,  C07D498/20 ,  C07D513/10

摘要： The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

公开(公告)号：US20170166564A1

公开(公告)日：2017-06-15

申请号：US15358371

申请日：2016-11-22

申请人： Incyte Corporation ,  Incyte Holdings Corporation

发明人： Yaping Sun ,  Liang Lu ,  Wenqing Yao ,  Jincong Zhuo ,  Liangxing Wu ,  Meizhong Xu ,  Ding-Quan Qian ,  Chunhong He ,  Fenglei Zhang

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.