公开(公告)号：US08030305B2

公开(公告)日：2011-10-04

申请号：US11612020

申请日：2006-12-18

申请人： Tianbao Lu ,  Richard Alexander ,  Richard W. Connors ,  Maxwell D. Cummings ,  Robert A. Galemmo ,  Heather Rae Hufnagel ,  Dana L. Johnson ,  Ehab Khalil ,  Kristi A. Leonard ,  Thomas P. Markotan ,  Anna C. Maroney ,  Jan L. Sechler ,  Jeremy M. Travins ,  Robert W. Tuman

发明人： Tianbao Lu ,  Richard Alexander ,  Richard W. Connors ,  Maxwell D. Cummings ,  Robert A. Galemmo ,  Heather Rae Hufnagel ,  Dana L. Johnson ,  Ehab Khalil ,  Kristi A. Leonard ,  Thomas P. Markotan ,  Anna C. Maroney ,  Jan L. Sechler ,  Jeremy M. Travins ,  Robert W. Tuman

IPC分类号： C07D487/04 ,  A61K31/5025 ,  A61P35/00

CPC分类号： C07D487/04 ,  C07D519/00

摘要： The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. 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的三唑并哒嗪化合物：其中R 1，R 5，R 6，R 7，R 8和A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c-Met的抑制剂，以及使用 的这样的化合物以减少或抑制细胞或受试者中c-Met的激酶活性，并调节细胞或受试者中的c-Met表达，以及这些化合物在受试者中用于预防或治疗细胞增殖性病症和 /或与c-Met有关的障碍。 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：US20090098181A1

公开(公告)日：2009-04-16

申请号：US12187524

申请日：2008-08-07

申请人： Tianbao Lu ,  Richard Alexander ,  Richard W. Connors ,  Maxwell D. Cummings ,  Robert A. Galemmo ,  Heather Rae Hufnagel ,  Dana L. Johnson ,  Ehab Khalil ,  Kristi A. Leonard ,  Thomas P. Markotan ,  Anna C. Maroney ,  Jan L. Sechler ,  Jeremy M. Travins ,  Robert W. Tuman

发明人： Tianbao Lu ,  Richard Alexander ,  Richard W. Connors ,  Maxwell D. Cummings ,  Robert A. Galemmo ,  Heather Rae Hufnagel ,  Dana L. Johnson ,  Ehab Khalil ,  Kristi A. Leonard ,  Thomas P. Markotan ,  Anna C. Maroney ,  Jan L. Sechler ,  Jeremy M. Travins ,  Robert W. Tuman

IPC分类号： A61F2/04 ,  C07D487/04 ,  A61K31/5025 ,  C12N9/99 ,  A61K31/541

CPC分类号： C07D487/04 ,  C07D519/00

摘要： The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. 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的三唑并哒嗪化合物：其中R 1，R 5，R 6，R 7，R 8和A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c-Met的抑制剂，以及使用 的这样的化合物以减少或抑制细胞或受试者中c-Met的激酶活性，并调节细胞或受试者中的c-Met表达，以及这些化合物在受试者中预防或治疗细胞增殖性病症和 /或与c-Met有关的障碍。 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：US08173654B2

公开(公告)日：2012-05-08

申请号：US12187524

申请日：2008-08-07

申请人： Tianbao Lu ,  Richard Alexander ,  Richard W. Connors ,  Maxwell D. Cummings ,  Robert A. Galemmo ,  Heather Rae Hufnagel ,  Dana L. Johnson ,  Ehab Khalil ,  Kristi A. Leonard ,  Thomas P. Markotan ,  Anna C. Maroney ,  Jan L. Sechler ,  Jeremy M. Travins ,  Robert W. Tuman

发明人： Tianbao Lu ,  Richard Alexander ,  Richard W. Connors ,  Maxwell D. Cummings ,  Robert A. Galemmo ,  Heather Rae Hufnagel ,  Dana L. Johnson ,  Ehab Khalil ,  Kristi A. Leonard ,  Thomas P. Markotan ,  Anna C. Maroney ,  Jan L. Sechler ,  Jeremy M. Travins ,  Robert W. Tuman

IPC分类号： A61K31/4985 ,  C07D487/04 ,  A61P3/10 ,  A61P17/06 ,  A61P25/18 ,  A61P19/02 ,  A61P9/10 ,  A61P9/00 ,  A61P35/00

CPC分类号： C07D487/04 ,  C07D519/00

摘要： The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. 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的三唑并哒嗪化合物：其中R 1，R 5，R 6，R 7，R 8和A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c-Met的抑制剂，以及使用 的这样的化合物以减少或抑制细胞或受试者中c-Met的激酶活性，并调节细胞或受试者中的c-Met表达，以及这些化合物在受试者中预防或治疗细胞增殖性病症和 /或与c-Met有关的障碍。 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：US07662824B2

公开(公告)日：2010-02-16

申请号：US11377077

申请日：2006-03-16

申请人： Kristi Leonard ,  Tianbao Lu ,  Robert W. Tuman ,  Dana L. Johnson ,  Anna C. Maroney ,  Jan L. Sechler ,  Richard W. Connors ,  Richard S. Alexander ,  Maxwell D. Cummings ,  Robert A. Galemmo ,  Thomas P. Markotan

发明人： Kristi Leonard ,  Tianbao Lu ,  Robert W. Tuman ,  Dana L. Johnson ,  Anna C. Maroney ,  Jan L. Sechler ,  Richard W. Connors ,  Richard S. Alexander ,  Maxwell D. Cummings ,  Robert A. Galemmo ,  Thomas P. Markotan

IPC分类号： A61K31/496 ,  A61K31/404 ,  C07D405/14 ,  C07D405/12 ,  C07D407/14

CPC分类号： C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12

摘要： The invention is directed to acylhydrazones compounds of Formula I: where R1, R2 and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. 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的酰腙化合物：其中R 1，R 2和A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c-Met的抑制剂，以及使用这些化合物来减少或抑制 c-Met在细胞或受试者中的激酶活性和调节细胞或受试者中的c-Met表达，以及这些化合物用于预防或治疗受试者的细胞增殖性病症和/或与c- 遇见 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。