公开(公告)号：WO2015081246A1

公开(公告)日：2015-06-04

申请号：PCT/US2014/067691

申请日：2014-11-26

Applicant: INCYTE CORPORATION

Inventor： YUE, Eddy W. ,  COMBS, Andrew P.

IPC: C07D471/04 ,  A61K31/437 ,  A61P9/00 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00

CPC classification number: C07D471/04

Abstract: The present invention relates to bicyclic 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.

Abstract translation: 本发明涉及双环杂环，其为BET蛋白如BRD2，BRD3，BRD4和BRD-t的抑制剂，并且可用于治疗诸如癌症的疾病。

公开(公告)号：WO2015081189A1

公开(公告)日：2015-06-04

申请号：PCT/US2014/067598

申请日：2014-11-26

Applicant: INCYTE CORPORATION ,  BUESKING, Andrew W.

Inventor： BUESKING, Andrew W. ,  YUE, Eddy W. ,  COMBS, Andrew P.

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00

CPC classification number: A61K31/437 ,  A61K31/4545 ,  C07D471/04

Abstract: The present invention relates to bicyclic 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：WO2014143768A1

公开(公告)日：2014-09-18

申请号：PCT/US2014/027872

申请日：2014-03-14

Applicant: INCYTE CORPORATION

Inventor： COMBS, Andrew P. ,  SPARKS, Richard B. ,  MADUSKUIE, Thomas P. Jr. ,  RODGERS, James D.

IPC: C07D471/06 ,  C07D498/06 ,  A61K31/5383 ,  A61K31/437 ,  A61P35/00 ,  A61P29/00 ,  A61P31/00

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.

Abstract translation: 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。

公开(公告)号：WO2012125629A1

公开(公告)日：2012-09-20

申请号：PCT/US2012/028915

申请日：2012-03-13

Applicant: INCYTE CORPORATION ,  COMBS, Andrew P.

Inventor： COMBS, Andrew P.

IPC: C07D403/12 ,  C07D513/04 ,  A61K31/517 ,  A61K31/429 ,  A61P29/00 ,  A61P37/00

CPC classification number: C07D513/04 ,  A61K31/498 ,  A61K31/519 ,  C07D401/12 ,  C07D403/12

Abstract: The present invention provides substituted diamino-pyrimidine and substituted diamino-pyridine derivatives of Formula I; wherein X, Y, R 1 , R 2 , and Ar are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.

Abstract translation: 本发明提供取代的二氨基 - 嘧啶和式I的取代的二氨基 - 吡啶衍生物; 其中X，Y，R 1，R 2和Ar如本文所定义，其调节磷酸肌醇3-激酶（PI3K）的活性，并且可用于治疗与PI3Ks的活性相关的疾病，包括例如炎症性疾病，免疫 基于疾病，癌症和其他疾病。

公开(公告)号：WO2020102216A1

公开(公告)日：2020-05-22

申请号：PCT/US2019/060955

申请日：2019-11-12

Applicant: INCYTE CORPORATION

Inventor： SHEPARD, Stacey ,  COMBS, Andrew P.

IPC: C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  A61P25/00 ,  A61P9/00 ,  A61P25/28 ,  A61P35/00 ,  A61P37/00 ,  A61K31/501

Abstract: This application relates to compounds of Formula (IIu) as well as specific compounds thereof wherein a pyrazole or triazole is present instead of the imidazole drawn above and pharmaceutically acceptable salts thereof, which are inhibitors of PI3K-y which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.

公开(公告)号：WO2017120194A1

公开(公告)日：2017-07-13

申请号：PCT/US2017/012135

申请日：2017-01-04

Applicant: INCYTE CORPORATION

Inventor： SPARKS, Richard B. ,  SHEPARD, Stacey ,  COMBS, Andrew P. ,  BUESKING, Andrew W. ,  SHAO, Lixin ,  WANG, Haisheng ,  FALAHATPISHEH, Nikoo

IPC: C07D401/14 ,  C07D403/14 ,  A61K31/506 ,  A61P35/00

CPC classification number: C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107

Abstract: 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.

Abstract translation: 本公开提供了调节磷酸肌醇3激酶-γ（PI3Kγ）活性并用于治疗与下列药物活性有关的疾病的式I化合物或其药学上可接受的盐： 包括例如自身免疫疾病，癌症，心血管疾病和神经退行性疾病的PI3Kγ。

公开(公告)号：WO2015081203A1

公开(公告)日：2015-06-04

申请号：PCT/US2014/067629

申请日：2014-11-26

Applicant: INCYTE CORPORATION ,  DOUTY, Brent

Inventor： DOUTY, Brent ,  YUE, Eddy W. ,  COMBS, Andrew P.

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00

CPC classification number: A61K31/538 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/498 ,  A61K31/519 ,  A61K31/5377 ,  C07D471/04

Abstract: The present invention relates to bicyclic 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.

Abstract translation: 本发明涉及作为BET蛋白如BRD2，BRD4，BRD4和BRD-t的抑制剂的双环杂环，并且可用于治疗诸如癌症的疾病。

公开(公告)号：WO2012087881A1

公开(公告)日：2012-06-28

申请号：PCT/US2011/065743

申请日：2011-12-19

Applicant: INCYTE CORPORATION ,  LI, Yun-Long ,  COMBS, Andrew P. ,  YUE, Eddy W. ,  MADUSKUIE JR., Thomas P. ,  SPARKS, Richard B.

Inventor： LI, Yun-Long ,  COMBS, Andrew P. ,  YUE, Eddy W. ,  MADUSKUIE JR., Thomas P. ,  SPARKS, Richard B.

IPC: C07D473/32 ,  A61K31/52 ,  A61P35/00

CPC classification number: C07D473/34 ,  A61K31/52 ,  A61K31/5377 ,  A61K45/06 ,  C07D473/32

Abstract: The present invention provides N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines derivatives that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.

Abstract translation: 本发明提供了调节磷酸肌醇3-激酶（PI3K）活性的N-（1-（取代苯基）乙基）-9H-嘌呤-6-胺衍生物，可用于治疗与 PI3Ks包括例如炎症性疾病，基于免疫的疾病，癌症和其它疾病。

公开(公告)号：WO2007075598A2

公开(公告)日：2007-07-05

申请号：PCT/US2006/048290

申请日：2006-12-19

Applicant: INCYTE CORPORATION ,  COMBS, Andrew P. ,  TAKVORIAN, Amy ,  ZHU, Wenyu ,  SPARKS, Richard B.

Inventor： COMBS, Andrew P. ,  TAKVORIAN, Amy ,  ZHU, Wenyu ,  SPARKS, Richard B.

CPC classification number: A61K31/541 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D271/08 ,  C07D285/06 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12

Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as pharmaceutical compositions thereof and methods of use thereof relating to the treatment of cancer and other diseases.

Abstract translation: 本发明涉及作为吲哚胺2,3-双加氧酶（IDO）的调节剂的N-羟基脒基化合物，以及其药物组合物及其涉及治疗癌症的使用方法和 其他疾病。

公开(公告)号：WO2019226213A3

公开(公告)日：2019-11-28

申请号：PCT/US2019/021186

申请日：2019-03-07

Applicant: INCYTE CORPORATION

Inventor： SHEPARD, Stacey ,  COMBS, Andrew P. ,  FALAHATPISHEH, Nikoo ,  SHAO, Lixin

IPC: C07D241/20 ,  C07D241/28 ,  C07D403/04 ,  C07D403/08 ,  C07D403/14 ,  C07D405/12 ,  C07D413/14 ,  C07D413/04 ,  C07D417/04 ,  A61P35/00 ,  A61K31/497

Abstract: This application relates to compounds of Formula (I): (I) or pharmaceutically acceptable salts thereof, which are inhibitors of PI3K-γ which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.