公开(公告)号：US20220288078A1

公开(公告)日：2022-09-15

申请号：US17536925

申请日：2021-11-29

Applicant: Incyte Holdings Corporation ,  Incyte Corporation

Inventor： Hui-Yin Li ,  James D. Rodgers

IPC: A61K31/519 ,  A61P17/12 ,  A61P17/06 ,  A61P17/08 ,  C07D487/04 ,  A61K9/00 ,  A61K9/20

Abstract: The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.

公开(公告)号：US11331320B2

公开(公告)日：2022-05-17

申请号：US16821624

申请日：2020-03-17

Applicant: Incyte Corporation ,  Incyte Holdings Corporation

Inventor： James D. Rodgers ,  Stacey Shepard

IPC: A61K31/519 ,  A61P29/00 ,  A61P35/04 ,  C07D471/04 ,  C07D487/04 ,  C07D417/04 ,  A61K31/573 ,  A61K45/06 ,  A61P17/04 ,  A61K9/00 ,  A61K9/20 ,  C07B59/00

Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines 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, skin disorders, myeloid proliferative disorders, cancer, and other 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

Applicant: Incyte Holdings Corporation ,  Incyte Corporation

Inventor： Jiacheng Zhou ,  James D. Rodgers ,  Haisheng Wang

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

Abstract: 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：US20170071947A1

公开(公告)日：2017-03-16

申请号：US15356957

申请日：2016-11-21

Applicant: Incyte Corporation ,  Incyte Holdings Corporation

Inventor： James D. Rodgers ,  Stacey Shepard

IPC: A61K31/519 ,  A61K31/573 ,  A61K9/00

CPC classification number: A61K31/519 ,  A61K9/0014 ,  A61K9/0053 ,  A61K9/20 ,  A61K31/573 ,  A61K45/06 ,  C07B59/002 ,  C07B2200/05 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines 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, skin disorders, myeloid proliferative disorders, cancer, and other diseases.

Abstract translation: 本发明提供调节Janus激酶活性的杂芳基取代的吡咯并[2,3-b]吡啶和杂芳基取代的吡咯并[2,3-b]嘧啶，可用于治疗与Janus激酶活性有关的疾病， 例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。

公开(公告)号：US20160346286A1

公开(公告)日：2016-12-01

申请号：US15233652

申请日：2016-08-10

Applicant: Incyte Corporation ,  Incyte Holdings Corporation

Inventor： James D. Rodgers ,  Stacey Shepard

IPC: A61K31/519 ,  A61K9/20 ,  A61K9/00 ,  A61K45/06 ,  A61K31/573

CPC classification number: A61K31/519 ,  A61K9/0014 ,  A61K9/0053 ,  A61K9/20 ,  A61K31/573 ,  A61K45/06 ,  C07B59/002 ,  C07B2200/05 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines 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, skin disorders, myeloid proliferative disorders, cancer, and other diseases.

公开(公告)号：US20160046650A1

公开(公告)日：2016-02-18

申请号：US14923105

申请日：2015-10-26

Applicant: INCYTE CORPORATION ,  INCYTE HOLDINGS CORPORATION

Inventor： Andrew P. Combs ,  Richard B. Sparks ,  Thomas P. Maduskuie, JR. ,  James D. Rodgers

IPC: C07D498/06 ,  C07D519/00

CPC classification number: C07D498/06 ,  C07D471/06 ,  C07D498/16 ,  C07D519/00

Abstract: 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：US09206187B2

公开(公告)日：2015-12-08

申请号：US14020505

申请日：2013-09-06

Applicant: Incyte Corporation ,  Incyte Holdings Corporation

Inventor： James D. Rodgers ,  Stacey Shepard ,  Jordan S. Fridman ,  Krishna Vaddi

IPC: A61K31/519 ,  C07D487/04 ,  C07D471/04 ,  A61K45/06 ,  A61K31/437

CPC classification number: A61K31/519 ,  A61K9/0014 ,  A61K9/0053 ,  A61K9/20 ,  A61K31/573 ,  A61K45/06 ,  C07B59/002 ,  C07B2200/05 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines 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, skin disorders, myeloid proliferative disorders, cancer, and other diseases.

Abstract translation: 本发明提供调节Janus激酶活性的杂芳基取代的吡咯并[2,3-b]吡啶和杂芳基取代的吡咯并[2,3-b]嘧啶，可用于治疗与Janus激酶活性有关的疾病， 例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。

公开(公告)号：US11744832B2

公开(公告)日：2023-09-05

申请号：US17689510

申请日：2022-03-08

Applicant: Incyte Corporation ,  Incyte Holdings Corporation

Inventor： James D. Rodgers ,  Stacey Shepard

IPC: A61K31/519 ,  A61K45/06 ,  C07B59/00 ,  A61K9/00 ,  A61K9/20 ,  A61P37/00 ,  A61P35/04 ,  A61P17/04 ,  A61P29/00 ,  C07D471/04 ,  C07D487/04 ,  C07D417/04 ,  A61K31/573

CPC classification number: A61K31/519 ,  A61K9/0014 ,  A61K9/0053 ,  A61K9/20 ,  A61K31/573 ,  A61K45/06 ,  A61P17/04 ,  A61P29/00 ,  A61P35/04 ,  A61P37/00 ,  C07B59/002 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07B2200/05

Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines 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, skin disorders, myeloid proliferative disorders, cancer, and other diseases.

公开(公告)号：US10975085B2

公开(公告)日：2021-04-13

申请号：US16436195

申请日：2019-06-10

Applicant: Incyte Holdings Corporation ,  Incyte Corporation

Inventor： Jiacheng Zhou ,  James D. Rodgers ,  Haisheng Wang

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

Abstract: The present invention is related to processes for preparing a composition comprising (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile, and related synthetic intermediate compounds. This compound is useful as an inhibitor 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：US10919912B2

公开(公告)日：2021-02-16

申请号：US16585568

申请日：2019-09-27

Applicant: Incyte Corporation ,  Incyte Holdings Corporation

Inventor： Andrew P. Combs ,  Richard B. Sparks ,  Thomas P. Maduskuie, Jr. ,  James D. Rodgers

IPC: C07D498/04 ,  C07D498/06 ,  C07D498/16 ,  C07D471/06 ,  A61P35/00 ,  C07D519/00

Abstract: The present invention relates to tricyclic heterocycles of Formula (I): 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.