公开(公告)号：US20070004660A1

公开(公告)日：2007-01-04

申请号：US11422395

申请日：2006-06-06

申请人： Christian Baumann ,  Michael Gaul ,  Dana Johnson ,  Robert Tuman

发明人： Christian Baumann ,  Michael Gaul ,  Dana Johnson ,  Robert Tuman

IPC分类号： A61K48/00 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/517 ,  A61K31/496

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： 本发明涉及抑制FLT3酪氨酸激酶活性或在细胞或受试者中表达或降低FLT3激酶活性或表达的方法，其包括施用法呢基转移酶抑制剂和FLT3激酶抑制剂，其选自烷基喹啉和式I的烷基喹唑啉化合物 '：其中R 1，R 2，R 3，Z，G，Q和X如本文所定义。 本发明包括预防和治疗方法，用于治疗患有（或易于）发展为与FLT3相关的细胞增殖性疾病或紊乱的风险的受试者。

公开(公告)号：US20060281772A1

公开(公告)日：2006-12-14

申请号：US11422349

申请日：2006-06-06

申请人： Nand Baindur ,  Michael Gaul ,  Kevin Kreutter ,  Christian Baumann ,  Alexander Kim ,  Guozhang Xu ,  Robert Tuman ,  Dana Johnson

发明人： Nand Baindur ,  Michael Gaul ,  Kevin Kreutter ,  Christian Baumann ,  Alexander Kim ,  Guozhang Xu ,  Robert Tuman ,  Dana Johnson

IPC分类号： A61K31/517 ,  A61K31/4709 ,  C07D403/04 ,  C07D401/04

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.

摘要翻译： 本发明涉及式I的烷基喹啉和烷基喹唑啉化合物：其中R 1，R 2，R 3，B，Z，G， Q和X如本文所定义，使用这些化合物如蛋白酪氨酸激酶调节剂，特别是FLT3和/或c-kit和/或TrkB的抑制剂，使用这些化合物来降低或抑制FLT3和/或 c-kit和/或TrkB，以及这些化合物在受试者中用于预防或治疗细胞增殖性疾病和/或与FLT3和/或c-kit和/或TrkB相关的疾病的用途。 本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

公开(公告)号：US20060281788A1

公开(公告)日：2006-12-14

申请号：US11422413

申请日：2006-06-06

申请人： Christian Baumann ,  Michael Gaul ,  Dana Johnson ,  Robert Tuman

发明人： Christian Baumann ,  Michael Gaul ,  Dana Johnson ,  Robert Tuman

IPC分类号： A61K31/454 ,  A61K48/00

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.

公开(公告)号：US20070149572A1

公开(公告)日：2007-06-28

申请号：US11550077

申请日：2006-10-17

申请人： Shelley Ballentine ,  Christian Baumann ,  Jinsheng Chen ,  Carl Illig ,  Sanath Meegalla ,  M. Rudolph ,  Robert Tuman ,  Mark Wall ,  Kenneth Wilson ,  Dana Johnson

发明人： Shelley Ballentine ,  Christian Baumann ,  Jinsheng Chen ,  Carl Illig ,  Sanath Meegalla ,  M. Rudolph ,  Robert Tuman ,  Mark Wall ,  Kenneth Wilson ,  Dana Johnson

IPC分类号： A61K31/454

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 ompound of the present invention: 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.

摘要翻译： 一种减少或抑制细胞或受试者中FLT3的激酶活性的方法，以及使用本发明的方法使用这些化合物在受试者中预防或治疗细胞增殖性疾病和/或与FLT3相关的病症：或 其溶剂合物，水合物，互变异构体或其药学上可接受的盐。 本发明还涉及治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

公开(公告)号：US20060281769A1

公开(公告)日：2006-12-14

申请号：US11422400

申请日：2006-06-06

申请人： Christian Baumann ,  Michael Gaul

发明人： Christian Baumann ,  Michael Gaul

IPC分类号： A61K48/00 ,  A61K31/519 ,  A61K31/4743

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.

摘要翻译： 本发明涉及抑制FLT3酪氨酸激酶活性或在细胞或受试者中表达或降低FLT3激酶活性或表达的方法，其包括施用法呢基转移酶抑制剂和选自噻吩并嘧啶和噻吩并吡啶化合物的FLT3激酶抑制剂，式I' 和式II'：其中R 1，R 3，B，Z，Q，p，q和X如本文所定义。 本发明包括预防和治疗方法，用于治疗患有（或易于）发展为与FLT3相关的细胞增殖性疾病或紊乱的风险的受试者。

公开(公告)号：US20060281764A1

公开(公告)日：2006-12-14

申请号：US11422362

申请日：2006-06-06

申请人： Michael Gaul ,  Guozhang Xu ,  Christian Baumann

发明人： Michael Gaul ,  Guozhang Xu ,  Christian Baumann

IPC分类号： C07D403/04 ,  A61K31/506

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

摘要： The invention is directed to aminopyrimidine compounds of Formula I: where R3, B, Z, Q, p, q and R1 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.

摘要翻译： 本发明涉及式I的氨基嘧啶化合物：其中R 3，B，Z，Q，p，q和R 1'如本文所定义，使用这样的 作为蛋白质酪氨酸激酶调节剂的化合物，特别是FLT3和/或c-kit和/或TrkB的抑制剂，使用这些化合物来降低或抑制细胞中FLT3和/或c-kit和/或TrkB的激酶活性 受试者以及这些化合物在受试者中预防或治疗细胞增殖性疾病和/或与FLT3和/或c-kit和/或TrkB相关的疾病的用途。 本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

公开(公告)号：US20060281771A1

公开(公告)日：2006-12-14

申请号：US11422379

申请日：2006-06-06

申请人： Christian Baumann ,  Michael Gaul

发明人： Christian Baumann ,  Michael Gaul

IPC分类号： A61K48/00 ,  A61K31/517 ,  A61K31/4709

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.

摘要翻译： 本发明涉及抑制FLT3酪氨酸激酶活性或在细胞或受试者中表达或降低FLT3激酶活性或表达的方法，包括施用法呢基转移酶抑制剂和FLT3激酶抑制剂，其选自式I的氨基喹啉和氨基喹唑啉化合物 '：其中R 1，R 2，R 3，B，Z，Q，p，q和X如本文所定义。 本发明包括预防和治疗方法，用于治疗患有（或易于）发展为与FLT3相关的细胞增殖性疾病或紊乱的风险的受试者。

公开(公告)号：US20060281755A1

公开(公告)日：2006-12-14

申请号：US11422405

申请日：2006-06-06

申请人： Christian Baumann ,  Michael Gaul

发明人： Christian Baumann ,  Michael Gaul

IPC分类号： A61K48/00 ,  A61K31/506

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.

摘要翻译： 本发明涉及一种抑制FLT3酪氨酸激酶活性或在细胞或受试者中表达或降低FLT3激酶活性或表达的方法，包括施用法呢基转移酶抑制剂和选自式I'的氨基嘧啶化合物的FLT3激酶抑制剂： 其中R 3，B，Z，r和R 1'如本文所定义。 本发明包括预防和治疗方法，用于治疗患有（或易于）发展为与FLT3相关的细胞增殖性疾病或紊乱的风险的受试者。

公开(公告)号：US20060281768A1

公开(公告)日：2006-12-14

申请号：US11422359

申请日：2006-06-06

申请人： Michael Gaul ,  Kevin Kreutter ,  Christian Baumann

发明人： Michael Gaul ,  Kevin Kreutter ,  Christian Baumann

IPC分类号： A61K31/519 ,  A61K31/4743 ,  C07D498/02

CPC分类号： C07D495/04

摘要： The invention is directed to thienopyrimidines and thienopyridines compounds of Formula I and Formula II: where R1, 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, the use of such compounds to reduce or inhibit 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. 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.

摘要翻译： 本发明涉及式I和式II的噻吩并嘧啶和噻吩并吡啶化合物：其中R 1，R 3，B，Z，Q，p，q和X分别为 本文定义的蛋白酪氨酸激酶调节剂，特别是FLT3抑制剂的这种化合物在细胞或受试者中使用这些化合物来降低或抑制FLT3的激酶活性，以及​​使用这些化合物预防或治疗 受试者与FLT3相关的细胞增殖性疾病和/或障碍。 本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

公开(公告)号：US20070021435A1

公开(公告)日：2007-01-25

申请号：US11422366

申请日：2006-06-06

申请人： Michael Gaul ,  Guozhang Xu ,  Christian Baumann

发明人： Michael Gaul ,  Guozhang Xu ,  Christian Baumann

IPC分类号： A61K31/506 ,  C07D403/14

CPC分类号： C07D239/48 ,  C07D401/12 ,  C07D403/04

摘要： The invention is directed to aminopyrimidine compounds of Formula I: where R3, B, Z, r and R1 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.

摘要翻译： 本发明涉及式I的氨基嘧啶化合物：其中R 3，B，Z，r和R 1如本文所定义，使用这些化合物作为蛋白质酪氨酸 激酶调节剂，特别是FLT3和/或c-kit和/或TrkB的抑制剂，使用这些化合物降低或抑制细胞或受试者中FLT3和/或c-kit和/或TrkB的激酶活性，以及 使用这样的化合物来预防或治疗受试者细胞增殖性病症和/或与FLT3和/或c-kit和/或TrkB相关的病症。 本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。