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公开(公告)号：EP1899319A2
公开(公告)日：2008-03-19
申请号：EP06772478.1
申请日：2006-06-07
发明人： BAINDUR, Nand , GAUL, Michael, David , KREUTTER, Kevin, Douglas , BAUMANN, Christian, Andrew , XU, Guozhang , KIM, Alexander, J. , ZHAO, Bao-Ping
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04
摘要： The invention is directed to aminoquinoline and aminoquinazoline compounds of Formula I: where R1, R2, R3, B, Z, Q, p, q and X are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of FLT3 and/or TrkB, the use of such compounds to reduce or inhibit kinase activity of FLT3 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 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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2.发明公开SYNERGISTIC MODULATION OF FLT3 KINASE USING THIENOPYRIMIDINE AND THIENOPYRIDINE KINASE MODULATORS 审中-公开与噻吩并嘧啶和噻吩并吡啶激酶抑制剂FLT3激酶协同调制
公开(公告)号：EP1893215A1
公开(公告)日：2008-03-05
申请号：EP06772424.5
申请日：2006-06-07
IPC分类号： A61K31/519 , A61K31/517 , A61K31/506 , A61P35/00 , A61K31/4709 , A61K31/00
CPC分类号： A61K31/506 , A61K31/00 , A61K31/4709 , A61K31/4743 , A61K31/517 , A61K31/519 , 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 thienopyrimidine and thienopyridine compounds Formula I' and Formula II': where R1, R3, B, Z, Q, p, 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.
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3.发明公开SYNERGISTIC MODULATION OF FLT3 KINASE USING AMINOQUINOLINE AND AMINOQUINAZOLINE KINASE MODULATORS 审中-公开与喹啉和喹唑啉激酶调节FLT3激酶协同调制
公开(公告)号：EP1893206A2
公开(公告)日：2008-03-05
申请号：EP06772443.5
申请日：2006-06-07
IPC分类号： A61K31/4709 , A61K31/517 , A61P35/00
CPC分类号： A61K31/4709 , A61K31/517 , 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 aminoquinoline and aminoquinazoline compounds of Formula (I’) : where R1, R2, R3, B, Z, Q, p, 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.
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4.发明公开SYNERGISTIC MODULATION OF FLT3 KINASE USING AMINOPYRIMIDINES KINASE MODULATORS AND A FARNESYL TRANSFERASE INHIBITOR 审中-公开FLT3激酶MT氨基嘧啶激酶调节剂的协同调制和法尼基转移酶抑制剂
公开(公告)号：EP1901745A2
公开(公告)日：2008-03-26
申请号：EP06772631.5
申请日：2006-06-07
IPC分类号： A61K31/4709
CPC分类号： A61K31/4709 , A61K9/0019 , A61K9/2018 , A61K31/506 , 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 aminopyrimidine compounds of Formula I': where R3, B, Z, r and R1 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.
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5.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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6.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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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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