公开(公告)号：US20220227736A1

公开(公告)日：2022-07-21

申请号：US17705079

申请日：2022-03-25

申请人： Incyte Corporation

发明人： Richard B. Sparks ,  Stacey Shepard ,  Andrew P. Combs ,  Andrew W. Buesking ,  Lixin Shao ,  Haisheng Wang ,  Nikoo Falahatpisheh

IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D491/107 ,  C07D487/10 ,  C07D487/08 ,  C07D403/14

摘要： The present disclosure provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that modulate the activity of phosphoinositide 3-kinases-gamma (PI3Kγ) and are useful in the treatment of diseases related to the activity of PI3Kγ including, for example, autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.

公开(公告)号：US20200002341A1

公开(公告)日：2020-01-02

申请号：US16436195

申请日：2019-06-10

申请人： Incyte Holdings Corporation ,  Incyte Corporation

发明人： Jiacheng Zhou ,  James D. Rodgers ,  Haisheng Wang

IPC分类号： C07D487/04 ,  C07F7/18 ,  C07F7/10 ,  C07F5/02 ,  C07F7/08

摘要： The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.

公开(公告)号：US20150175604A1

公开(公告)日：2015-06-25

申请号：US14575284

申请日：2014-12-18

申请人： Incyte Corporation

发明人： James D. Rodgers ,  Stacey Shepard ,  Haisheng Wang ,  Lixin Shao

IPC分类号： C07D471/14

CPC分类号： C07D471/14 ,  A61K31/437

摘要： The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.

公开(公告)号：US20130296299A1

公开(公告)日：2013-11-07

申请号：US13889618

申请日：2013-05-08

申请人： Incyte Corporation

发明人： James D. Rodgers ,  Haisheng Wang ,  Andrew P. Combs ,  Richard B. Sparks

IPC分类号： C07D471/04

CPC分类号： C07D471/04 ,  C07D487/04

摘要： The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.

公开(公告)号：US11952367B2

公开(公告)日：2024-04-09

申请号：US17705079

申请日：2022-03-25

申请人： Incyte Corporation

发明人： Richard B. Sparks ,  Stacey Shepard ,  Andrew P. Combs ,  Andrew W. Buesking ,  Lixin Shao ,  Haisheng Wang ,  Nikoo Falahatpisheh

IPC分类号： C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107

CPC分类号： C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107

摘要： The present disclosure provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that modulate the activity of phosphoinositide 3-kinases-gamma (PI3Kγ) and are useful in the treatment of diseases related to the activity of PI3Kγ including, for example, autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.

公开(公告)号：US20220169649A1

公开(公告)日：2022-06-02

申请号：US17365789

申请日：2021-07-01

申请人： Incyte Corporation

发明人： Yanran Ai ,  Onur Atasoylu ,  Yu Bai ,  Joseph Barbosa ,  David M. Burns ,  Daniel Levy ,  Brent Douty ,  Hao Feng ,  Leah C. Konkol ,  Cheng-Tsung Lai ,  Xun Liu ,  Song Mei ,  Jun Pan ,  Haisheng Wang ,  Liangxing Wu ,  Wenqing Yao ,  Eddy W. Yue

IPC分类号： C07D471/14 ,  C07D519/00

摘要： The present application provides tricyclic urea compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer.

公开(公告)号：US10442803B2

公开(公告)日：2019-10-15

申请号：US15688313

申请日：2017-08-28

申请人： Incyte Corporation

发明人： James D. Rodgers ,  Stacey Shepard ,  Haisheng Wang ,  Lixin Shao

IPC分类号： C07D471/14 ,  A61K31/437

摘要： The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.

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：US09334274B2

公开(公告)日：2016-05-10

申请号：US14250843

申请日：2014-04-11

申请人： Incyte Corporation ,  Incyte Holdings Corporation

发明人： James D Rodgers ,  Stacey Shepard ,  Argyrios G Arvanitis ,  Haisheng Wang ,  Louis Storace ,  Beverly Folmer ,  Wenyu Zhu ,  Joseph Glenn ,  Lixin Shao

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D487/04 ,  C07D519/00 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

摘要： The present invention relates to N-(hetero)aryl-pyrrolidine derivatives of Formula I: which are JAK inhibitors, such as selective JAK1 inhibitors, useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.

摘要翻译： 本发明涉及式I的N-（杂）芳基 - 吡咯烷衍生物：其是JAK抑制剂，例如选择性JAK1抑制剂，其可用于治疗JAK相关疾病，包括例如炎性和自身免疫性疾病，以及 作为癌症。

公开(公告)号：US09309246B2

公开(公告)日：2016-04-12

申请号：US14575284

申请日：2014-12-18

申请人： Incyte Corporation

发明人： James D. Rodgers ,  Stacey Shepard ,  Haisheng Wang ,  Lixin Shao

IPC分类号： C07D471/14

CPC分类号： C07D471/14 ,  A61K31/437

摘要： The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.

摘要翻译： 本发明涉及作为BET蛋白如BRD2，BRD4，BRD4和BRD-t的抑制剂的三环杂环，可用于治疗诸如癌症的疾病。