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1. 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。

2. 发明申请

WO2004002410A2 2,4-DISUBSTITUTED-PYRIDINE N-OXIDES USEFUL AS HIV REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译： 2,4-取代的吡啶类N-氧化物作为HIV逆转录酶抑制剂有用
公开(公告)号：WO2004002410A2
公开(公告)日：2004-01-08
申请号：PCT/US2003/019917
申请日：2003-06-25
申请人： BRISTOL-MYERS SQUIBB COMPANY , RODGERS, James, D. , WANG, Haisheng
发明人： RODGERS, James, D. , WANG, Haisheng
IPC分类号： A61K
CPC分类号： C07D213/89 , A61K31/44
摘要： The present invention relates to 2,4-disubstituted pyridine-N-oxide compounds of formula (I) or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
摘要翻译：本发明涉及可用作HIV逆转录酶抑制剂的式（I）的2,4-二取代吡啶-N-氧化物化合物或其立体异构形式，立体异构混合物或其药学上可接受的盐形式，以及药物组合物和包含其的诊断试剂盒，及其用于治疗病毒感染的方法或作为测定标准品或试剂。

3. 发明申请

WO2012068440A1 HETEROCYCLIC-SUBSTITUTED PYRROLOPYRIDINES AND PYRROLOPYRIMIDINES AS JAK INHIBITORS 审中-公开
标题翻译：作为JAK抑制剂的杂环取代的吡咯烷酮和吡咯烷酮
公开(公告)号：WO2012068440A1
公开(公告)日：2012-05-24
申请号：PCT/US2011/061351
申请日：2011-11-18
申请人： INCYTE CORPORATION , RODGERS, James, D. , ZHU, Wenyu , GLENN, Joseph
发明人： RODGERS, James, D. , ZHU, Wenyu , GLENN, Joseph
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines of Formula I: wherein X, Y, Z, L, A, R 5 , n, m, and r are defined above, 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I的杂环取代的吡咯并吡啶和吡咯并嘧啶：其中X，Y，Z，L，A，R 5，n，m和r如上所定义，以及它们的组合物和使用方法， Janus激酶（JAKs）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，癌症和其它疾病。

4. 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。

5. 发明申请

WO2010083283A2 PROCESSES FOR PREPARING JAK INHIBITORS AND RELATED INTERMEDIATE COMPOUNDS 审中-公开
标题翻译：制备JAK抑制剂及相关中间体化合物的方法
公开(公告)号：WO2010083283A2
公开(公告)日：2010-07-22
申请号：PCT/US2010/021003
申请日：2010-01-14
申请人： INCYTE CORPORATION , ZHOU, Jiacheng , LIU, Pingli , LIN, Qiyan , METCALF, Brian, W. , MELONI, David , PAN, Yongchun , XIA, Michael , LI, Mei , YUE, Tai-Yuen , RODGERS, James, D. , WANG, Haisheng
发明人： ZHOU, Jiacheng , LIU, Pingli , LIN, Qiyan , METCALF, Brian, W. , MELONI, David , PAN, Yongchun , XIA, Michael , LI, Mei , YUE, Tai-Yuen , RODGERS, James, D. , WANG, Haisheng
IPC分类号： C07D231/16 , C07D487/04 , C07F5/04 , C07F7/08
CPC分类号： C07D487/04 , C07F5/025 , C07F7/083 , C07F7/10 , C07F7/1892 , Y02P20/55
摘要： The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3- d i]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.
摘要翻译：本发明涉及制备式III的手性取代的吡唑并吡咯并[2,3-d]嘧啶的方法和相关的合成中间体化合物。手性取代的吡唑并吡咯并[2,3-d]嘧啶可用作Janus Kinase家族蛋白酪氨酸激酶（JAKs）的抑制剂，用于治疗炎性疾病，骨髓增生性疾病和其他疾病。

6. 发明申请

WO2008157208A2 SALTS OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE 审中-公开
标题翻译：甘油激酶抑制剂（R）-3-（4-（7H-吡咯烷并[2,3-d]嘧啶-4-基）-1H-吡唑-1-基）-3-环戊基丙烯酸的盐
公开(公告)号：WO2008157208A2
公开(公告)日：2008-12-24
申请号：PCT/US2008/066662
申请日：2008-06-12
申请人： INCYTE CORPORATION , RODGERS, James, D. , LI, Hui-Yin
发明人： LI, Hui-Yin
CPC分类号： A61K31/519 , A61K9/0053 , A61K9/20 , C07B2200/07 , C07B2200/13 , C07D487/04
摘要： 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.
摘要翻译：本发明提供（R）-3-（4-（7H-吡咯并[2,3-d]嘧啶-4-基）-1H-吡唑-1-基）-3-环戊基丙腈的盐形式，其可用于 Janus激酶活性的调节，并且可用于治疗与Janus激酶活性相关的疾病，包括例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。

7. 发明申请

WO2013026025A1 CYCLOHEXYL AZETIDINE DERIVATIVES AS JAK INHIBITORS 审中-公开
标题翻译：作为JAK抑制剂的CYCLOHEXYL AZETIDINE DERIVATIVES
公开(公告)号：WO2013026025A1
公开(公告)日：2013-02-21
申请号：PCT/US2012/051439
申请日：2012-08-17
申请人： INCYTE CORPORATION , RODGERS, James D. , ARVANITIS, Argyrios G.
发明人： RODGERS, James D. , ARVANITIS, Argyrios G.
IPC分类号： C07D473/04 , A61K31/519 , A61P29/00 , A61P35/00 , A61P37/02
CPC分类号： C07D473/04 , C07D487/04
摘要： The present invention provides cyclohexyl azetidine derivatives of formula (I), as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
摘要翻译：本发明提供式（I）的环己基氮杂环丁烷衍生物及其组合物和使用方法，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，癌症和其它疾病。

8. 发明申请

WO2011103423A1 CYCLOBUTANE AND METHYLCYCLOBUTANE DERIVATIVES AS JANUS KINASE INHIBITORS 审中-公开
标题翻译：作为JANUS KINASE抑制剂的CYCLOBUTANE AND METHYLCYCLOBUTANE DERIVATIVES
公开(公告)号：WO2011103423A1
公开(公告)日：2011-08-25
申请号：PCT/US2011/025433
申请日：2011-02-18
申请人： INCYTE CORPORATION , LI, Yun-long , RODGERS, James, D.
发明人： LI, Yun-long , RODGERS, James, D.
IPC分类号： C07D487/04 , A61K31/519 , A61P17/00 , A61P27/00 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： C07D487/04
摘要： The present invention relates to cyclobutane and methylcyclobutane derivatives, as well as their salts, compositions, and methods of use, which are Janus kinase (JAK) inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer and myeloproliferative disorders.
摘要翻译：本发明涉及环丁烷和甲基环丁烷衍生物，以及它们的盐，组合物和使用方法，其是可用于治疗JAK相关疾病的Janus激酶（JAK）抑制剂，包括例如炎性和自身免疫性疾病，以及癌症和骨髓增生性疾病。

9. 发明申请

WO2010083283A3 PROCESSES FOR PREPARING JAK INHIBITORS AND RELATED INTERMEDIATE COMPOUNDS 审中-公开
标题翻译：制备JAK抑制剂和相关中间体化合物的过程
公开(公告)号：WO2010083283A3
公开(公告)日：2010-10-14
申请号：PCT/US2010021003
申请日：2010-01-14
申请人： INCYTE CORP , ZHOU JIACHENG , LIU PINGLI , LIN QIYAN , METCALF BRIAN W , MELONI DAVID , PAN YONGCHUN , XIA MICHAEL , LI MEI , YUE TAI-YUEN , RODGERS JAMES D , WANG HAISHENG
发明人： ZHOU JIACHENG , LIU PINGLI , LIN QIYAN , METCALF BRIAN W , MELONI DAVID , PAN YONGCHUN , XIA MICHAEL , LI MEI , YUE TAI-YUEN , RODGERS JAMES D , WANG HAISHENG
IPC分类号： C07D231/16 , C07D487/04 , C07F5/04 , C07F7/08
CPC分类号： C07D487/04 , C07F5/025 , C07F7/083 , C07F7/10 , C07F7/1892 , Y02P20/55
摘要： The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-di]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.
摘要翻译：本发明涉及制备式III的手性取代的吡唑基吡咯并[2,3-d]嘧啶和相关合成中间体化合物的方法。手性取代的吡唑基吡咯并[2,3-d]嘧啶可用作蛋白酪氨酸激酶（JAK）的Janus激酶家族的抑制剂，用于治疗炎性疾病，骨髓增殖性疾病和其他疾病。

10. 发明申请

WO2008157207A3 METABOLITES OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-LH-PYRAZOL-L-YL)-3- CYCLOPENTYLPROPANENITRILE 审中-公开
公开(公告)号：WO2008157207A3
公开(公告)日：2008-12-24
申请号：PCT/US2008/066658
申请日：2008-06-12
申请人： INCYTE CORPORATION , RODGERS, James D. , ARVANITIS, Argyrios G. , SHI, Jack Guoen
发明人： RODGERS, James D. , ARVANITIS, Argyrios G. , SHI, Jack Guoen
IPC分类号： C07D487/04 , A61K31/519
摘要： The present invention provides active metablites of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile 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.

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