公开(公告)号：US20070142305A1

公开(公告)日：2007-06-21

申请号：US11657912

申请日：2007-01-25

申请人： Chih Ho ,  Bengt Brunmark ,  Stuart Emanuel ,  Robert Galemmo ,  Dana Johnson ,  Donald Ludovici ,  Umar Maharoof ,  Jay Mei ,  Jan Sechler ,  Eric Strobel ,  Robert Tuman ,  Hwa Yen

发明人： Chih Ho ,  Bengt Brunmark ,  Stuart Emanuel ,  Robert Galemmo ,  Dana Johnson ,  Donald Ludovici ,  Umar Maharoof ,  Jay Mei ,  Jan Sechler ,  Eric Strobel ,  Robert Tuman ,  Hwa Yen

IPC分类号： A61K31/7052 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/4162 ,  C07D413/02 ,  C07D403/02

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 present invention and to methods for treating conditions such as tumors and other cell. proliferative disorders.

摘要翻译： 本发明涉及可用作血小板衍生生长因子受体（PDGF-R）激酶抑制剂的N-取代三环3-氨基吡唑衍生物，以及制备所述衍生物的方法。 本发明还涉及包含本发明化合物的药物组合物和用于治疗诸如肿瘤和其它细胞的病症的方法。 增生性疾病

公开(公告)号：US20070203136A1

公开(公告)日：2007-08-30

申请号：US11612020

申请日：2006-12-18

申请人： Tianbao Lu ,  Richard Alexander ,  Richard Connors ,  Maxwell Cummings ,  Robert Galemmo ,  Heather Rae Hufnagel ,  Dana Johnson ,  Ehab Khalil ,  Kristi Leonard ,  Thomas Markotan ,  Anna Maroney ,  Jan Sechler ,  Jeremy Travins ,  Robert Tuman

发明人： Tianbao Lu ,  Richard Alexander ,  Richard Connors ,  Maxwell Cummings ,  Robert Galemmo ,  Heather Rae Hufnagel ,  Dana Johnson ,  Ehab Khalil ,  Kristi Leonard ,  Thomas Markotan ,  Anna Maroney ,  Jan Sechler ,  Jeremy Travins ,  Robert Tuman

IPC分类号： A61K31/503 ,  A61K31/5377 ,  C07D487/04

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，以及这些化合物用于降低或抑制激酶活性的用途 c-Met在细胞或受试者中的调节，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疾病和/或与c-Met有关的障碍的用途。 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：US20070066610A1

公开(公告)日：2007-03-22

申请号：US11377077

申请日：2006-03-16

申请人： Kristi Leonard ,  Tianbao Lu ,  Robert Tuman ,  Dana Johnson ,  Anna Maroney ,  Jan Sechler ,  Richard Connors ,  Richard Alexander ,  Maxwell Cummings ,  Robert Galemmo ,  Thomas Markotan

发明人： Kristi Leonard ,  Tianbao Lu ,  Robert Tuman ,  Dana Johnson ,  Anna Maroney ,  Jan Sechler ,  Richard Connors ,  Richard Alexander ,  Maxwell Cummings ,  Robert Galemmo ,  Thomas Markotan

IPC分类号： A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  A61K31/404 ,  C07D413/14 ,  C07D405/14

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的抑制剂以及这些化合物在细胞或受试者中降低或抑制c-Met的激酶活性并调节细胞或受试者中的c-Met表达的用途，以及这些化合物用于预防或 在受试者中治疗与c-Met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：US20050130910A1

公开(公告)日：2005-06-16

申请号：US10986500

申请日：2004-11-10

申请人： Chih Ho ,  Robert Galemmo ,  Dana Johnson ,  Jay Mei ,  Stanley Belkowski ,  Richard Connors

发明人： Chih Ho ,  Robert Galemmo ,  Dana Johnson ,  Jay Mei ,  Stanley Belkowski ,  Richard Connors

IPC分类号： A61K31/4162 ,  A61K31/422 ,  A61K31/427 ,  A61K31/7056 ,  C07D231/54 ,  C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D413/02 ,  C07D417/02 ,  C07D495/04 ,  C07H17/00 ,  G01N33/543 ,  G01N33/574

CPC分类号： C07D403/12 ,  C04B35/632 ,  C07D231/54 ,  C07D231/56 ,  C07D401/12 ,  C07D495/04 ,  G01N33/574 ,  G01N2333/71 ,  G01N2500/00

摘要： The present invention relates to immobilized N-substituted tricyclic 3-aminopyrazole compounds of Formula 1 as tools for the identification of bimolecular targets in cells of therapeutic significance, profiling the selectivity of compounds, prediction of possible related toxicities and exploration of mechanisms of action in biological systems for therapeutic indications related to compounds. These agents can be used to identify biomolecules with the potential to interact with the immobilized reagent. The identified biomolecule may be then be used as a therapeutic target, serve as a marker of drug action, or alternatively describe an untoward or toxic potential of the immobilized agent.

摘要翻译： 本发明涉及式1的固定化N-取代三环3-氨基吡唑化合物，作为用于鉴定细胞中双分子靶标的具有治疗意义的工具，分析化合物的选择性，预测可能的相关毒性和探索生物学作用机制 与化合物相关的治疗适应症系统。 这些试剂可用于鉴定具有与固定化试剂相互作用的潜力的生物分子。 所鉴定的生物分子然后可以用作治疗靶，用作药物作用的标记，或者替代地描述固定化剂的不利或有毒的潜力。