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1.发明公开SYNERGISTIC MODULATION OF FLT3 KINASE USING A FLT3 INHIBITOR AND A FARNESYL TRANSFERASE INHIBITOR 审中-公开FLT3激酶协同使用调制FLT3抑制剂和FARNESYLTRANSFERASEHEMMER
公开(公告)号：EP1898912A1
公开(公告)日：2008-03-19
申请号：EP06784682.4
申请日：2006-06-07
IPC分类号： A61K31/4427 , A61P35/00 , A61K31/00
CPC分类号： A61K45/06 , A61K31/4427 , A61K31/454 , A61K2300/00
摘要： The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from compounds of Formula (I'). Included within the present invention is both prophylactic and therapeutic methods for treating a subject at risk of (or susceptible to) developing a cell proliferative disorder or a disorder related to FLT3.
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2.发明公开SYNERGISTIC MODULATION OF FLT3 KINASE USING ALKYLQUINOLINES AND ALKYLQUINAZOLINES 审中-公开烷基喹啉和烷基喹唑啉对FLT3激酶的协同调节
公开(公告)号：EP1893214A1
公开(公告)日：2008-03-05
申请号：EP06772423.7
申请日：2006-06-07
IPC分类号： A61K31/517 , A61P35/00 , A61K31/4709 , A61K31/00
CPC分类号： A61K31/4709 , A61K31/00 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , A61K2300/00
摘要： The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from alkylquinoline and alkylquinazoline compounds of Formula (I'): where R1, R2, R3, Z, G, Q and X are as defined herein. Included within the present invention is both prophylactic and therapeutic methods for treating a subject at risk of (or susceptible to) developing a cell proliferative disorder or a disorder related to FLT3.
摘要翻译： 本发明涉及在细胞或受试者中抑制FLT3酪氨酸激酶活性或表达或降低FLT3激酶活性或表达的方法，所述方法包括施用法尼基转移酶抑制剂和FLT3激酶抑制剂，所述FLT3激酶抑制剂选自下式的烷基喹啉和烷基喹唑啉化合物： I'）：其中R 1，R 2，R 3，Z，G，Q和X如本文所定义。 包括在本发明内的是用于治疗处于患有（或易患）发展细胞增殖性病症或与FLT3相关的病症的个体的预防和治疗方法。
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3.发明授权4-AZETIDINYL-1-HETEROARYL-CYCLOHEXANOL ANTAGONISTS OF CCR2 有权4-氮杂环丁烷基-1- HETEROARYLCYCLOHEXANOLE作为拮抗剂的CCR2
公开(公告)号：EP2376475B1
公开(公告)日：2015-09-02
申请号：EP09768584.6
申请日：2009-12-09
发明人： ZHANG, Xuqing , HUFNAGEL, Heather, Rae , HOU, Cuifen , JOHNSON, Dana, L. , SUI, Zhihua , FEGELY, Barry , BRESLIN, David
IPC分类号： C07D401/08 , C07D403/08 , C07D407/14 , C07D409/08 , C07D413/08 , C07D417/08 , C07D417/14 , A61K31/422 , A61K31/4178 , A61K31/4427 , A61K31/506 , A61P7/12
CPC分类号： C07D401/08 , C07D403/08 , C07D407/14 , C07D409/08 , C07D413/08 , C07D417/08 , C07D417/14
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4.发明授权
公开(公告)号：EP1506175B1
公开(公告)日：2009-04-01
申请号：EP03728909.7
申请日：2003-05-13
发明人： HO, Chih, Yung , BRUNMARK, Bengt, Anders , EMANUEL, Stuart , GALEMMO JR., Robert, A. , JOHNSON, Dana, L. , LUDOVICI, Donald, W. , MAHAROOF, Umar , MEI, Jay, M. , SECHLER, Jan, L. , STROBEL, Eric, D. , TUMAN, Robert, W. , YEN, Hwa, Kwo
IPC分类号： C07D231/54 , C07D231/56 , C07D401/12 , C07D413/12 , A61K31/416 , A61P35/04
CPC分类号： C07F9/65038 , C07D231/54 , C07D231/56 , C07D233/64 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D491/04 , C07D495/04
摘要： The invention is directed to N-substituted tricyclic 3-AMINOPYRAZOLE derivatives, which are useful as inhibitors of platelet-derived growth factor receptor (PDGF-R) kinase, and methods for the preparation of said derivatives. The present invention is further directed to pharmaceutical compositions comprising the compounds of the presentinvention and to methods for treating conditions such as tumors and other cell proliferative disorders.
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公开(公告)号：EP1951234A2
公开(公告)日：2008-08-06
申请号：EP06846103.7
申请日：2006-10-17
发明人： BALLENTINE, Shelley, K. , BAUMANN, Christian, Andrew , CHEN, Jingsheng , ILLIG, Carl, R. , MEEGALLA, Saneth K. , RUDOLPH, M. Jonathan , TUMAN, Robert, W. , WALL, Mark, J. , WILSON, Kenneth , JOHNSON, Dana, L.
IPC分类号： A61K31/4439 , A61K31/454 , A61K31/497 , A61K31/5355 , A61P35/00
CPC分类号： A61K31/4439 , A61K31/454 , A61K31/497 , A61K31/5355 , Y10S514/908
摘要： A method of reducing or inhibiting kinase activity of FLT3 in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 using a compound of the present invention (I), or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.
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公开(公告)号：EP1893598A1
公开(公告)日：2008-03-05
申请号：EP06772652.1
申请日：2006-06-07
发明人： BAINDUR, Nand , GAUL, Michael David , KREUTTER, Kevin, Douglas , XU, Guozhang , TUMAN, Robert, W. , JOHNSON, Dana, L. , BAUMANN, Christian, Andrew , KIM, Alexander, J.
IPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , A61K31/517 , A61P35/00
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula I: wherein R1, R2, R3, B, Z, G, Q and X are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of FLT3 and/or c kit and/or TrkB, the use of such compounds to reduce or inhibit kinase activity of FLT3 and/or c kit and/or TrkB in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 and/or c kit and/or TrkB . The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
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