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1. 发明申请

WO2007117494A1 DEAZAPURINES USEFUL AS INHIBITORS OF JANUS KINASES 审中-公开
标题翻译： DEAZAPURINES有用作JANK KINASES的抑制剂
公开(公告)号：WO2007117494A1
公开(公告)日：2007-10-18
申请号：PCT/US2007/008367
申请日：2007-04-05
申请人： VERTEX PHARMACEUTICALS INCORPORATED , LEDEBOER, Mark , MESSERSMITH, David , MALTAIS, Francois , GAO, Huai , WANG, Tiansheng , CAO, Jingrong , DUFFY, John , MARTINEZ-BOTELLA, Gabriel , FORSTER, Cornelia , MARONE, Valerie , WANNAMAKER, Marion , SALITURO, Francesco , PIERCE, Albert , FARMER, Luc
发明人： LEDEBOER, Mark , MESSERSMITH, David , MALTAIS, Francois , GAO, Huai , WANG, Tiansheng , CAO, Jingrong , DUFFY, John , MARTINEZ-BOTELLA, Gabriel , FORSTER, Cornelia , MARONE, Valerie , WANNAMAKER, Marion , SALITURO, Francesco , PIERCE, Albert , FARMER, Luc
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of formula (I): useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要翻译：本发明涉及式（I）化合物：可用作蛋白激酶抑制剂，特别是JAK家族激酶的抑制剂。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。

2. 发明申请

WO2009085913A1 PYRAZOLO [1,5-a] PYRIMIDINES USEFUL AS JAK2 INHIBITORS 审中-公开
标题翻译：吡唑并[1,5-a]吡嗪类作为JAK2抑制剂有用
公开(公告)号：WO2009085913A1
公开(公告)日：2009-07-09
申请号：PCT/US2008/087362
申请日：2008-12-18
申请人： VERTEX PHARMACEUTICALS INCORPORATED , LEDEBOER, Mark , STEWART, Michelle , MESSERSMITH, David , DUFFY, John , MARTINEZ-BOTELLA, Gabriel , COME, Jon , GAO, Huai , SALITURO, Francesco , MARONE, Valerie , PIERCE, Albert
发明人： LEDEBOER, Mark , STEWART, Michelle , MESSERSMITH, David , DUFFY, John , MARTINEZ-BOTELLA, Gabriel , COME, Jon , GAO, Huai , SALITURO, Francesco , MARONE, Valerie , PIERCE, Albert
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of formula (I) useful as selective inhibitors of JAK2 kinase. The invention also provides pharmaceutical acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various diseases, conditions or disorders. The invention also provides processes for preparing the compounds of the invention.
摘要翻译：本发明涉及可用作JAK2激酶选择性抑制剂的式（I）化合物。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。本发明还提供了制备本发明化合物的方法。

3. 发明申请

WO2008116139A2 COMPOUNDS USEFUL AS INHIBITORS OF JANUS KINASES 审中-公开
标题翻译：化合物作为JANK KINASES的抑制剂有用
公开(公告)号：WO2008116139A2
公开(公告)日：2008-09-25
申请号：PCT/US2008/057797
申请日：2008-03-21
申请人： VERTEX PHARMACEUTICALS INCORPORATED , WANNAMAKER, Marion , SALITURO, Francesco , PIERCE, Albert , ARONOV, Alexander , MARTINEZ-BOTELLA, Gabriel , WANG, Jian , FARMER, Luc , LEDEBOER, Mark , WANG, Tiansheng , BETHIEL, Randy , LEDFORD, Brian , PORTER, Emilie
发明人： WANNAMAKER, Marion , SALITURO, Francesco , PIERCE, Albert , ARONOV, Alexander , MARTINEZ-BOTELLA, Gabriel , WANG, Jian , FARMER, Luc , LEDEBOER, Mark , WANG, Tiansheng , BETHIEL, Randy , LEDFORD, Brian , PORTER, Emilie
CPC分类号： C07D401/14 , C07D213/74 , C07D239/42 , C07D401/04 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂，特别是JAK家族激酶的化合物。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。

4. 发明申请

WO2007041130A2 DEAZAPURINES USEFUL AS INHIBITORS OF JANUS KINASES 审中-公开
标题翻译： DEAZAPURINES有用作JANK KINASES的抑制剂
公开(公告)号：WO2007041130A2
公开(公告)日：2007-04-12
申请号：PCT/US2006/037593
申请日：2006-09-28
申请人： VERTEX PHARMACEUTICALS INCORPORATED , SALITURO, Francesco , FARMER, Luc , WANG, Tiansheng , WANG, Jian , BETHIEL, Randy , WANNAMAKER, Marion , MARTINEZ-BOTELLA, Gabriel , DUFFY, John , ARONOV, Alexander , LAUFFER, David , PIERCE, Albert
发明人： SALITURO, Francesco , FARMER, Luc , WANG, Tiansheng , WANG, Jian , BETHIEL, Randy , WANNAMAKER, Marion , MARTINEZ-BOTELLA, Gabriel , DUFFY, John , ARONOV, Alexander , LAUFFER, David , PIERCE, Albert
IPC分类号： C07D487/04 , C07D519/00 , A61K31/495 , A61P29/00
CPC分类号： C07D487/04
摘要： The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂，特别是JAK家族激酶的化合物。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。

5. 发明申请

WO2007084557A2 AZAINDOLES USEFUL AS INHIBITORS OF JANUS KINASES 审中-公开
标题翻译：阿拉伯糖作为JANK KINASES的抑制剂有用
公开(公告)号：WO2007084557A2
公开(公告)日：2007-07-26
申请号：PCT/US2007/001225
申请日：2007-01-17
申请人： VERTEX PHARMACEUTICALS INCORPORATED , FARMER, Luc , MARTINEZ-BOTELLA, Gabriel , PIERCE, Albert , SALITURO, Francesco , WANG, Jian , WANNAMKER, Marion , WANG, Tiansheng
发明人： FARMER, Luc , MARTINEZ-BOTELLA, Gabriel , PIERCE, Albert , SALITURO, Francesco , WANG, Jian , WANNAMKER, Marion , WANG, Tiansheng
IPC分类号： C07D471/04 , A61K31/506 , A61K31/53 , A61P29/00 , C07D495/10 , A61K31/517 , A61P25/00 , A61P37/00
CPC分类号： A61K31/506 , A61K31/517 , A61K31/53 , A61K31/5377 , A61K45/06 , C07D471/04 , C07D495/10 , C07D519/00 , C12N9/12 , C12Y207/10002
摘要： The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂，特别是JAK家族激酶的化合物。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。

6. 发明申请

WO2002085909A1 9-DEAZAGUANINE DERIVATIVES AS INHIBITORS OF GSK-3 审中-公开
标题翻译：作为GSK-3的抑制剂的9-二氮杂萘衍生物
公开(公告)号：WO2002085909A1
公开(公告)日：2002-10-31
申请号：PCT/US2002/012395
申请日：2002-04-19
申请人： VERTEX PHARMACEUTICALS INCORPORATED , CAO, Jingrong , CHOQUETTE, Debbie , DAVIES, Robert , FORSTER, Cornelia , LAUFFER, David , PIERCE, Albert , TOMLINSON, Ronald , WANNAMAKER, Marion , METZ, Natalie
发明人： CAO, Jingrong , CHOQUETTE, Debbie , DAVIES, Robert , FORSTER, Cornelia , LAUFFER, David , PIERCE, Albert , TOMLINSON, Ronald , WANNAMAKER, Marion , METZ, Natalie
IPC分类号： C07D487/14
CPC分类号： C07D471/14 , C07D487/04 , C07D487/14 , C07D491/04 , C07D495/04 , C07D513/04 , C07D513/14
摘要： The present invention provides compounds of formula I:or a pharmaceutically acceptable derivative thereof, wherein X is oxygen or sulfur; Y is -S-, -O- or -NR 1 -; and R 2 , R 3 , and R 4 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of GSK-3 mammalian protein kinase. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatement and prevention of various disorders, such as diabetes and Alzheimer's disease.
摘要翻译：本发明提供式I化合物或其药学上可接受的衍生物，其中X是氧或硫; Y是-S-，-O-或-NR1-; R2，R3和R4如说明书所述。这些化合物是蛋白激酶的抑制剂，特别是GSK-3哺乳动物蛋白激酶的抑制剂。本发明还提供包含本发明抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病如糖尿病和阿尔茨海默氏病的方法。

7. 发明申请

WO2008112651A3 AMINOPYRIMIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES 审中-公开
公开(公告)号：WO2008112651A3
公开(公告)日：2008-09-18
申请号：PCT/US2008/056433
申请日：2008-03-10
申请人： VERTEX PHARMACEUTICALS INCORPORATED , PIERCE, Albert , COME, Jon , COURT, John , GAO, Huai , HENKEL, Gregory , LIU, Michael , NEUBERGER, Timothy
发明人： PIERCE, Albert , COME, Jon , COURT, John , GAO, Huai , HENKEL, Gregory , LIU, Michael , NEUBERGER, Timothy
IPC分类号： C07D471/04 , A61K31/506 , A61P3/10 , A61P9/00 , A61P25/00
摘要： The present invention relates to compounds (I) useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.

8. 发明申请

WO2002102800A1 5-(2-AMINOPYRIMIDIN-4-YL) BENZISOXAZOLES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的5-（2-氨基吡啶-4-YL）苯唑沙因
公开(公告)号：WO2002102800A1
公开(公告)日：2002-12-27
申请号：PCT/US2002/019186
申请日：2002-06-14
申请人： VERTEX PHARMACEUTICALS INCORPORATED , MOON, Young, Choon , GREEN, Jeremy , DAVIES, Robert , CHOQUETTE, Deb , PIERCE, Albert , LEDEBOER, Mark
发明人： MOON, Young, Choon , GREEN, Jeremy , DAVIES, Robert , CHOQUETTE, Deb , PIERCE, Albert , LEDEBOER, Mark
IPC分类号： C07D413/04
CPC分类号： C07D413/04 , C07D413/14
摘要： Described herein are benzisoxazole compounds of formula I or a pharmaceutically acceptable derivative or prodrug thereof, wherein A-B is N-O or O-N; Ar is an optionally substituted C 5-10 aryl group; R 1 is hydrogen or an optionally substituted group selected from C1-I0 aliphatic, C 5-10 aryl, C 6-12 aralkyl, C 3-10 heterocyclyl, or C 4-12 heterocyclylalkyl; and T, n, R 2 and R 3 are as described in the specification. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK-3 and JAK mammalian protein kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various -, protein kinase mediated disorders.
摘要翻译：本文描述的是式I的苯并异恶唑化合物或其药学上可接受的衍生物或前药，其中A-B是N-O或O-N; Ar是任选取代的C 5-10芳基; R 1是氢或选自C 1-10脂族，C 5-10芳基，C 6-12芳烷基，C 3-10杂环基或C 4-12杂环基烷基的任选取代的基团; 和T，n，R 2和R 3如说明书中所述。这些化合物是蛋白激酶的抑制剂，特别是GSK-3和JAK哺乳动物蛋白激酶的抑制剂。本发明还提供包含本发明化合物的药学上可接受的组合物以及利用这些化合物和组合物治疗各种蛋白激酶介导的病症的方法。

9. 发明申请

WO2009076593A1 MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR 审中-公开
标题翻译： CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR的调节剂
公开(公告)号：WO2009076593A1
公开(公告)日：2009-06-18
申请号：PCT/US2008/086562
申请日：2008-12-12
申请人： VERTEX PHARMACEUTICALS INCORPORATED , BINCH, Hayley , GROOTENHUIS, Peter, D.J. , PIERCE, Albert , FANNING, Lev, T.D.
发明人： BINCH, Hayley , GROOTENHUIS, Peter, D.J. , PIERCE, Albert , FANNING, Lev, T.D.
IPC分类号： C07D487/04 , A61K31/517 , A61K31/519 , A61P1/18 , A61P3/06 , A61P25/16 , A61P25/28
CPC分类号： C07D487/04 , A61K31/519 , A61K45/06
摘要： The present invention relates to modulators of ATP-Binding Cassette ("ABC") transporters or fragments thereof of formula (I), including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators.
摘要翻译：本发明涉及式（I）的ATP-结合盒（“ABC”）转运蛋白或其片段的调节剂，包括囊性纤维化跨膜电导调节剂，其组合物及其方法。本发明还涉及使用这种CFTR调节剂治疗疾病的方法。

10. 发明申请

WO2003011287A1 PYRAZOLON DERIVATIVES AS INHIBITORS OF GSK-3 审中-公开
标题翻译：作为GSK-3的抑制剂的吡唑啉衍生物
公开(公告)号：WO2003011287A1
公开(公告)日：2003-02-13
申请号：PCT/US2002/024726
申请日：2002-08-02
申请人： VERTEX PHARMACEUTICALS INCORPORATED , GREEN, Jeremy , ARNOST, Michael, J. , PIERCE, Albert
发明人： GREEN, Jeremy , ARNOST, Michael, J. , PIERCE, Albert
IPC分类号： A61K31/415
CPC分类号： C07D401/12 , C07D231/20 , C07D231/46 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to compounds of formula (I) that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula (I) or pharmaceutical compositions comprising compounds of formula (I) to inhibit GSK-3 activity. The invention further provides methods of utilizing these compounds and pharmaceutical compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. The invention also relates to methods for inhibiting Aurora-2 activity and for treating or preventing Aurora-2-mediated diseases using compounds of formula (I) or pharmaceutical compositions comprising compounds of formula (I). The invention also relates to methods for inhibiting cyclin-dependent kinase-2 activity and for treating or preventing inhibiting cyclin-dependent kinase-2-mediated diseases using compounds of formula (I) or pharmaceutical compositions comprising compounds of formula (I).
摘要翻译：本发明涉及可用作GSK-3抑制剂的式（I）化合物。本发明还涉及使用式（I）化合物或包含式（I）化合物的药物组合物抑制GSK-3活性的方法。本发明还提供了利用这些化合物和药物组合物治疗和预防各种疾病如糖尿病和阿尔茨海默病的方法。本发明还涉及使用式（I）化合物或包含式（I）化合物的药物组合物来抑制Aurora-2活性和治疗或预防Aurora-2介导的疾病的方法。本发明还涉及使用式（I）化合物或包含式（I）化合物的药物组合物来抑制细胞周期蛋白依赖性激酶-2活性和治疗或预防抑制细胞周期蛋白依赖性激酶2介导的疾病的方法。

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