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1. 发明申请

WO2011075630A1 SUBSTITUTED FUSED ARYL AND HETEROARYL DERIVATIVES AS PI3K INHIBITORS 审中-公开
标题翻译：作为PI3K抑制剂的取代的芳香族和异构体衍生物
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
申请人： INCYTE CORPORATION , LI, Yun-Long , COMBS, Andrew, P. , YUE, Eddy, W. , LI, Hui-Yin
发明人： LI, Yun-Long , COMBS, Andrew, P. , YUE, Eddy, W. , LI, Hui-Yin
IPC分类号： C07D473/16 , C07D473/34 , A61K31/52 , A61P29/00 , A61P35/00
CPC分类号： C07D473/34 , C07D473/16
摘要： 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.
摘要翻译：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。

2. 发明申请

WO2013033569A1 HETEROCYCLYLAMINES AS PI3K INHIBITORS 审中-公开
标题翻译：杂环化合物作为PI3K抑制剂
公开(公告)号：WO2013033569A1
公开(公告)日：2013-03-07
申请号：PCT/US2012/053398
申请日：2012-08-31
申请人： INCYTE CORPORATION , LI, Yun-Long , YAO, Wenqing , COMBS, Andrew, P. , YUE, Eddy, W. , MEI, Song , ZHU, Wenyu , GLENN, Joseph , MADUSKUIE, Thomas, P., Jr. , SPARKS, Richard, B. , DOUTY, Brent
发明人： LI, Yun-Long , YAO, Wenqing , COMBS, Andrew, P. , YUE, Eddy, W. , MEI, Song , ZHU, Wenyu , GLENN, Joseph , MADUSKUIE, Thomas, P., Jr. , SPARKS, Richard, B. , DOUTY, Brent
IPC分类号： C07D471/04 , C07D487/04 , A61K31/519 , A61P35/00 , A61P29/00 , A61P27/00 , A61P19/00 , A61P1/00 , A61P17/00
CPC分类号： A61K31/519 , C07D471/04 , C07D487/04 , C07D519/00
摘要： The present invention provides heterocyclylamine 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.
摘要翻译：本发明提供式（I）的杂环基胺衍生物：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，癌症和其它疾病。

3. 发明申请

WO2012087881A1 N-(1-(SUBSTITUTED-PHENYL)ETHYL)-9H-PURIN-6-AMINES AS PI3K INHIBITORS 审中-公开
标题翻译：作为PI3K抑制剂的N-（1-（取代苯基）乙基）-9H-嘌呤-6-胺
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
申请人： INCYTE CORPORATION , LI, Yun-Long , COMBS, Andrew P. , YUE, Eddy W. , MADUSKUIE JR., Thomas P. , SPARKS, Richard B.
发明人： LI, Yun-Long , COMBS, Andrew P. , YUE, Eddy W. , MADUSKUIE JR., Thomas P. , SPARKS, Richard B.
IPC分类号： C07D473/32 , A61K31/52 , A61P35/00
CPC分类号： C07D473/34 , A61K31/52 , A61K31/5377 , A61K45/06 , C07D473/32
摘要： 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.
摘要翻译：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。

4. 发明申请

WO2012135009A1 PYRIMIDINE-4,6-DIAMINE DERIVATIVES AS PI3K INHIBITORS 审中-公开
标题翻译：作为PI3K抑制剂的吡哩啶-4,6-二胺衍生物
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
申请人： INCYTE CORPORATION , COMBS, Andrew P. , LI, Yun-Long , YUE, Eddy W.
发明人： COMBS, Andrew P. , LI, Yun-Long , YUE, Eddy W.
IPC分类号： C07D401/12 , C07D239/48 , A61P19/00
CPC分类号： C07D239/48 , A61K31/505 , C07C53/18 , C07D401/12 , C07D403/12
摘要： 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.
摘要翻译：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。

5. 发明申请

WO2011075643A1 SUBSTITUTED HETEROARYL FUSED DERIVATIVES AS PI3K INHIBITORS 审中-公开
标题翻译：作为PI3K抑制剂的替代异氟醚融合衍生物
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
申请人： INCYTE CORPORATION , COMBS, Andrew P. , LI, Yun-Long , YUE, Eddy W. , SPARKS, Richard B.
发明人： COMBS, Andrew P. , LI, Yun-Long , YUE, Eddy W. , SPARKS, Richard B.
IPC分类号： C07D519/00 , A61K31/52 , A61P19/02 , A61P29/00
CPC分类号： C07D519/00
摘要： 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.
摘要翻译：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。

6. 发明申请

WO2011163195A1 FUSED PYRROLE DERIVATIVES AS PI3K INHIBITORS 审中-公开
标题翻译：作为PI3K抑制剂的FUSED PYRORO衍生物
公开(公告)号：WO2011163195A1
公开(公告)日：2011-12-29
申请号：PCT/US2011/041202
申请日：2011-06-21
申请人： INCYTE CORPORATION , LI, Yun-Long , COMBS, Andrew P.
发明人： LI, Yun-Long , COMBS, Andrew P.
IPC分类号： C07D473/34 , C07D519/00 , A61K31/52 , A61P35/00
CPC分类号： C07D473/34 , A61K31/52 , C07D519/00
摘要： The present invention provides fused pyrrole derivatives of Formula (I) wherein V, W, X, Y, L, Q, Ar, Z, R 1 and R 6 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.
摘要翻译：本发明提供式（I）的稠合吡咯衍生物，其中V，W，X，Y，L，Q，Ar，Z，R 1和R 6在本文中定义，其调节磷酸肌醇3-激酶（PI3K）的活性，可用于治疗与PI3Ks的活性相关的疾病，包括例如炎性疾病，基于免疫的疾病，癌症和其它疾病。

7. 发明申请

WO2011008487A1 PYRIMIDINONES AS PI3K INHIBITORS 审中-公开
标题翻译： PYRIMIDINONES作为PI3K抑制剂
公开(公告)号：WO2011008487A1
公开(公告)日：2011-01-20
申请号：PCT/US2010/040150
申请日：2010-06-28
申请人： INCYTE CORPORATION , LI, Yun-Long , METCALF, Brian, W. , COMBS, Andrew, P.
发明人： LI, Yun-Long , METCALF, Brian, W. , COMBS, Andrew, P.
IPC分类号： C07D473/34 , C07D513/04 , A61K31/52 , A61P29/00 , A61P37/00
CPC分类号： C07D519/00 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention provides pyrimidinones 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.
摘要翻译：本发明提供了调节磷酸肌醇3-激酶（PI3K）的活性的嘧啶酮，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，癌症和其它疾病。

8. 发明申请

WO2011028685A1 HETEROCYCLIC DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-D]PYRIMIDINES AS JANUS KINASE INHIBITORS 审中-公开
标题翻译：吡唑并[4-y]吡咯烷[2,3-D]嘧啶的杂环衍生物作为JANUS KINASE INHIBITORS
公开(公告)号：WO2011028685A1
公开(公告)日：2011-03-10
申请号：PCT/US2010/047252
申请日：2010-08-31
申请人： INCYTE CORPORATION , RODGERS, James, D. , LI, Yun-Long , SHEPARD, Stacey , WANG, Haisheng
发明人： RODGERS, James, D. , LI, Yun-Long , SHEPARD, Stacey , WANG, Haisheng
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： The present invention provides heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3 djpyrimidines of Formula Ia or a pharmaceutically acceptable salt thereof; wherein: A is H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-I4 cycloalkyl, C 2-13 heterocycloalkyl, C 6-14 aryl, C 1-14 heteroaryl, C 3-14 cycloalkyl-C 1-4 alkyl, C 2-13 heterocycloalkyl-C 1-4 alkyl, C 6-14 aryl-C 1-4 alkyl, or C 14 heteroaryl-C 14 alkyl, wherein said C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-14 cycloalkyl, C 2-13 heterocycloalkyl, C 6-14 aryl, C 1-14 heteroaryl, C 3-14 cycloalkyl-C 1-4 alkyl, C 2-13 heterocycloalkyl-C 1-4 alkyl, C 6-14 aryl-C 1-4 alkyl, and C 1-14 heteroaryl-C 1-4 alkyl are each optionally substituted with I, 2, 3, 4, 5, or 6 independently selected R 8 substituents; L is absent, C(=O), C(=O)NH, S(=O), or S(O) 2 ; X is CH or N; Y is H, cyano, halo, C 1-4 alkyl, or C 1-4 haloalkyl; Z is CR 7 or N; R 1 , R 2 , and R 3 are each independently H, hydroxyl, halo, C 1-3 alkyl, or C 1-3 haloalkyl; R 4 and R 5 are each independently H, C 1-3 alkyl, or C 1-3 haloalkyl; or R 4 and R 5 together with the carbon atom to which they are attached can form a 3-, 4-, 5-, 6- υr 7-membered cycloalkyl ring; as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example inflammatory disorders, autoimmune disorders, cancer, and other diseases.
摘要翻译：本发明提供式Ia的吡唑-4-基 - 吡咯并[2,3-d]嘧啶的杂环衍生物或其药学上可接受的盐; 其中：A是H，C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-14环烷基，C 2-3-13杂环烷基，C 6-14芳基，C 1-14杂芳基，C 3-14环烷基-C 1-4烷基 C 2-4烷基-C 1-4烷基，C 6-14芳基-C 1-4烷基或C 14杂芳基-C 14烷基，其中所述C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-14环烷基， C2-13杂环烷基，C6-14芳基，C1-14杂芳基，C3-14环烷基C1-4烷基，C2-13杂环烷基-C1-4烷基，C6-14芳基C1-4烷基和C1-14杂芳基 -C 1-4烷基各自任选被1个，2个，3个，4个，5个或6个独立选择的R8取代基取代; L不存在，C（= O），C（= O）NH，S（= O）或S（O）2; X是CH或N; Y是H，氰基，卤素，C 1-4烷基或C 1-4卤代烷基; Z为CR7或N; R 1，R 2和R 3各自独立地为H，羟基，卤素，C 1-3烷基或C 1-3卤代烷基; R 4和R 5各自独立地为H，C 1-3烷基或C 1-3卤代烷基; 或R 4和R 5与它们所连接的碳原子一起可以形成3-，4-，5-，6-7R元环烷基环; 以及它们的组合物和使用方法，其调节Janus激酶（JAK）的活性，并且可用于治疗与JAK的活性相关的疾病，包括例如炎症性疾病，自身免疫性疾病，癌症和其他疾病。

9. 发明申请

WO2010135621A1 3-[4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL]OCTANE- OR HEPTANE-NITRILE AS JAK INHIBITORS 审中-公开
标题翻译： 3- [4-（7H-吡咯烷并[2,3-D]嘧啶-4-基] -1H-吡唑并[1-y]]异喹啉酮或其衍生物作为JAK抑制剂
公开(公告)号：WO2010135621A1
公开(公告)日：2010-11-25
申请号：PCT/US2010/035728
申请日：2010-05-21
申请人： INCYTE CORPORATION , LI, Yun-Long , RODGERS, James D.
发明人： LI, Yun-Long , RODGERS, James D.
IPC分类号： A61K31/519 , C07D487/04 , A61P35/00 , A61P17/00 , A61P27/02 , A61P29/00
CPC分类号： A61K31/519 , C07D487/04
摘要： The present invention relates to the Janus kinase (JAK) inhibitors 3-[4-(7H-pyrrolo[2,3- d]pyrimidin-4-yl)-1H-pyrazol-l-yl]octanenitrile or 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-y1)-1H- pyrazol-l-yl]heptanenitrile, as well as its compositions and methods of use, which is useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, skin disorders, cancer, and other diseases.
摘要翻译：本发明涉及Janus激酶（JAK）抑制剂3- [4-（7H-吡咯并[2,3-d]嘧啶-4-基）-1H-吡唑-1-基]辛腈或3- [4- （7H-吡咯并[2,3-d]嘧啶-4-基）-1H-吡唑-1-基]庚腈，以及其组合物和使用方法，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，皮肤病症，癌症和其它疾病。

10. 发明申请

WO2007103719A3 MODULATORS OF 11-β HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME 审中-公开
公开(公告)号：WO2007103719A3
公开(公告)日：2007-09-13
申请号：PCT/US2007/063055
申请日：2007-03-01
申请人： INCYTE CORPORATION , ZHUO, Jincong , LI, Yun-Long , XU, Meizhong , HE, Chunhong , YAO, Wenqing
发明人： ZHUO, Jincong , LI, Yun-Long , XU, Meizhong , HE, Chunhong , YAO, Wenqing
IPC分类号： C07D213/64 , C07D233/78 , C07D401/04 , C07D471/10 , C07D493/10 , C07D498/10 , A61K31/4523 , A61K31/4525 , A61K31/453 , A61K31/454 , A61P3/00 , C07C321/26 , C07C233/65 , C07C317/14 , C07D207/26
摘要： The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1 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.

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