公开(公告)号：WO2012135009A1

公开(公告)日：2012-10-04

申请号：PCT/US2012/030310

申请日：2012-03-23

Applicant: INCYTE CORPORATION ,  COMBS, Andrew P. ,  LI, Yun-Long ,  YUE, Eddy W.

Inventor： COMBS, Andrew P. ,  LI, Yun-Long ,  YUE, Eddy W.

IPC: C07D401/12 ,  C07D239/48 ,  A61P19/00

CPC classification number: C07D239/48 ,  A61K31/505 ,  C07C53/18 ,  C07D401/12 ,  C07D403/12

Abstract: The present invention provides pyrimidine-4,6-diamine derivatives of Formula (I): wherein the variables 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: 本发明提供式（I）的嘧啶-4,6-二胺衍生物：其中本文所定义的变量调节磷酸肌醇3-激酶（PI3K）的活性，并且可用于治疗与 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：WO2011075643A1

公开(公告)日：2011-06-23

申请号：PCT/US2010/061023

申请日：2010-12-17

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

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

IPC: C07D519/00 ,  A61K31/52 ,  A61P19/02 ,  A61P29/00

CPC classification number: C07D519/00

Abstract: The present invention provides fused derivatives of Formula (I) that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PBKs including, for example, inflammatory disorders, immune- based disorders, cancer, and other diseases.

Abstract translation: 本发明提供调节磷酸肌醇3-激酶（PI3K）的活性的式（I）的融合衍生物，并且可用于治疗与PBK的活性相关的疾病，包括例如炎症性疾病，基于免疫的疾病， 癌症等疾病。

公开(公告)号：WO2011075630A1

公开(公告)日：2011-06-23

申请号：PCT/US2010/060980

申请日：2010-12-17

Applicant: INCYTE CORPORATION ,  LI, Yun-Long ,  COMBS, Andrew, P. ,  YUE, Eddy, W. ,  LI, Hui-Yin

Inventor： LI, Yun-Long ,  COMBS, Andrew, P. ,  YUE, Eddy, W. ,  LI, Hui-Yin

IPC: C07D473/16 ,  C07D473/34 ,  A61K31/52 ,  A61P29/00 ,  A61P35/00

CPC classification number: C07D473/34 ,  C07D473/16

Abstract: The present invention provides fused aryl and heteroaryl derivatives of Formula I 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: 本发明提供调节磷酸肌醇3-激酶（PI3K）的活性的式I的稠合芳基和杂芳基衍生物，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，基于免疫的疾病 ，癌症等疾病。

公开(公告)号：WO2010005958A3

公开(公告)日：2010-06-24

申请号：PCT/US2009049794

申请日：2009-07-07

Applicant: INCYTE CORP ,  COMBS ANDREW P ,  YUE EDDY W ,  SPARKS RICHARD B ,  ZHU WENYU ,  ZHOU JIACHENG ,  LIN QIYAN ,  WENG LINGKAI ,  YUE TAI-YUEN ,  LIU PINGLI

Inventor： COMBS ANDREW P ,  YUE EDDY W ,  SPARKS RICHARD B ,  ZHU WENYU ,  ZHOU JIACHENG ,  LIN QIYAN ,  WENG LINGKAI ,  YUE TAI-YUEN ,  LIU PINGLI

IPC: C07D271/08 ,  A61K31/4245 ,  A61P1/00 ,  A61P11/00 ,  A61P17/00 ,  A61P19/00 ,  A61P25/00 ,  A61P27/00 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00

CPC classification number: A61K31/4245 ,  A61K39/0011 ,  A61K39/3955 ,  C07D271/08 ,  C07D413/04 ,  C07D413/12

Abstract: The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives. The present invention provides, inter alia, IDO inhibitors of Formula I: or a pharmaceutically acceptable salt thereof, wherein: R1 is NH2 or CH3; R2 is C1, Br, CF3, CH3, or CN; R3 is H or F; and n is 1 or 2.

Abstract translation: 本发明涉及1,2,5-恶二唑衍生物及其组合物，其为吲哚胺2,3-双加氧酶的抑制剂，可用于治疗癌症和其它疾病，以及其用于治疗癌症和其它疾病的方法和中间体 制备这样的1,2,5-恶二唑衍生物。 本发明尤其提供式I的IDO抑制剂：或其药学上可接受的盐，其中：R 1是NH 2或CH 3; R2是C1，Br，CF3，CH3或CN; R3为H或F; n为1或2。

公开(公告)号：WO2008036642A3

公开(公告)日：2008-08-07

申请号：PCT/US2007078745

申请日：2007-09-18

Applicant: INCYTE CORP ,  COMBS ANDREW P ,  GLASS BRIAN M ,  SPARKS RICHARD B ,  YUE EDDY WAI

Inventor： COMBS ANDREW P ,  GLASS BRIAN M ,  SPARKS RICHARD B ,  YUE EDDY WAI

IPC: C07D413/04 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/426 ,  A61P11/06 ,  A61P25/00 ,  A61P31/18 ,  A61P35/00 ,  A61P37/00 ,  C07D261/18 ,  C07D261/20 ,  C07D277/56 ,  C07D417/04

CPC classification number: C07D413/04 ,  C07D261/18 ,  C07D261/20 ,  C07D277/56 ,  C07D417/04

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

Abstract translation: 本发明涉及作为吲哚胺2,3-双加氧酶（IDO）调节剂的N-羟基脒基化合物，以及其组合物和药物方法。

公开(公告)号：WO2008036653A3

公开(公告)日：2008-03-27

申请号：PCT/US2007/078759

申请日：2007-09-18

Applicant: INCYTE CORPORATION ,  COMBS, Andrew P. ,  GLASS, Brian M. ,  SPARKS, Richard B. ,  YUE, Eddy Wai

Inventor： COMBS, Andrew P. ,  GLASS, Brian M. ,  SPARKS, Richard B. ,  YUE, Eddy Wai

IPC: C07D261/18 ,  C07D261/20 ,  C07D333/70 ,  C07D307/68 ,  A61K31/415 ,  A61K31/34 ,  A61K31/381 ,  A61P35/00 ,  A61P29/00 ,  A61P25/00 ,  A61P31/12

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

公开(公告)号：WO2008036653A2

公开(公告)日：2008-03-27

申请号：PCT/US2007078759

申请日：2007-09-18

Applicant: INCYTE CORP ,  COMBS ANDREW P ,  GLASS BRIAN M ,  SPARKS RICHARD B ,  YUE EDDY WAI

Inventor： COMBS ANDREW P ,  GLASS BRIAN M ,  SPARKS RICHARD B ,  YUE EDDY WAI

IPC: C07D261/18 ,  A61K31/34 ,  A61K31/381 ,  A61K31/415 ,  A61P25/00 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  C07D261/20 ,  C07D307/68 ,  C07D333/70

CPC classification number: C07D261/18 ,  C07D261/20 ,  C07D307/68 ,  C07D333/70

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

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-羟基脒基化合物及其组合物和药物方法。

公开(公告)号：WO2008036652A2

公开(公告)日：2008-03-27

申请号：PCT/US2007/078758

申请日：2007-09-18

Applicant: INCYTE CORPORATION ,  COMBS, Andrew P. ,  YUE, Eddy Wai

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

CPC classification number: C07D263/32 ,  C07D261/08 ,  C07D263/34 ,  C07D271/08 ,  C07D277/28 ,  C07D285/06 ,  C07D307/52 ,  C07D333/20

Abstract: The present invention is directed to amidino heterocyclic compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.

Abstract translation: 本发明涉及作为吲哚胺2,3-双加氧酶（IDO）的调节剂的脒基杂环化合物，以及其组合物和药物方法。

公开(公告)号：WO2008036643A2

公开(公告)日：2008-03-27

申请号：PCT/US2007/078746

申请日：2007-09-18

Applicant: INCYTE CORPORATION ,  COMBS, Andrew P.

Inventor： COMBS, Andrew P.

CPC classification number: C07D241/20 ,  C07C259/18 ,  C07D213/78 ,  C07D237/24 ,  C07D241/26 ,  C07D241/28

Abstract: The present invention is directed to amidino heterocyclic compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as to pharmaceutical compositions comprising such compounds and to pharmaceutical methods of treatment comprising administration of such compounds and pharmaceutical compositions.

Abstract translation: 本发明涉及作为吲哚胺2,3-双加氧酶（IDO）的调节剂的脒基杂环化合物，以及包含这些化合物的药物组合物和包括施用这些化合物和药物组合物的药物治疗方法。

公开(公告)号：WO2008036642A2

公开(公告)日：2008-03-27

申请号：PCT/US2007/078745

申请日：2007-09-18

Applicant: INCYTE CORPORATION ,  COMBS, Andrew, P. ,  GLASS, Brian, M. ,  SPARKS, Richard, B. ,  YUE, Eddy Wai

Inventor： COMBS, Andrew, P. ,  GLASS, Brian, M. ,  SPARKS, Richard, B. ,  YUE, Eddy Wai

IPC: C07D413/04 ,  C07D261/20 ,  C07D261/18 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/426 ,  A61P11/06 ,  A61P25/00 ,  A61P37/00 ,  A61P31/18 ,  A61P35/00 ,  C07D417/04 ,  C07D277/56

CPC classification number: C07D413/04 ,  C07D261/18 ,  C07D261/20 ,  C07D277/56 ,  C07D417/04

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

Abstract translation: 本发明涉及作为吲哚胺2,3-双加氧酶（IDO）调节剂的N-羟基脒基化合物，以及其组合物和药物方法。