公开(公告)号：US20110112110A1

公开(公告)日：2011-05-12

申请号：US12935795

申请日：2009-03-30

申请人： Carlo Gambacorti Passerini ,  Rosalind Helen Gunby ,  Alfonso Zambon ,  Leonardo Scapozza ,  Shaheen Ahmed ,  Peter G. Goekjian ,  David Gueyrard ,  Florence Popowycz ,  Cerric Schneider

发明人： Carlo Gambacorti Passerini ,  Rosalind Helen Gunby ,  Alfonso Zambon ,  Leonardo Scapozza ,  Shaheen Ahmed ,  Peter G. Goekjian ,  David Gueyrard ,  Florence Popowycz ,  Cerric Schneider

IPC分类号： A61K31/496 ,  C07D403/10 ,  A61K31/4178 ,  C07D417/14 ,  C07D405/14 ,  A61K31/444 ,  A61K31/4439 ,  C07D417/10 ,  A61K31/433 ,  A61P35/00

CPC分类号： C07D233/88 ,  C07D277/40 ,  C07D277/46 ,  C07D307/68

摘要： Inhibitors of the oncogenic tyrosine kinase ALK and of the Bcr-Abl mutant T315I Bcr-Abl, pharmaceutical compositions containing the same and their use for the treatment of hyper-proliferative diseases.

摘要翻译： 致癌性酪氨酸激酶ALK和Bcr-Abl突变体T315I Bcr-Abl的抑制剂，含有它们的药物组合物及其用于治疗高增殖性疾病的用途。

公开(公告)号：US20110053946A1

公开(公告)日：2011-03-03

申请号：US12988619

申请日：2009-04-27

申请人： Ion Niculescu-Duvaz ,  Alfonso Zambon ,  Dan Niculescu-Duvaz ,  Steven Whittaker ,  Richard Marais ,  Caroline Joy Springer

发明人： Ion Niculescu-Duvaz ,  Alfonso Zambon ,  Dan Niculescu-Duvaz ,  Steven Whittaker ,  Richard Marais ,  Caroline Joy Springer

IPC分类号： A61K31/4985 ,  C07D401/12 ,  A61K31/4709 ,  C12N5/00 ,  A61P35/00 ,  C07D471/04 ,  A61K31/437

CPC分类号： C07D471/04

摘要： The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain aryl-quinolyl compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.

摘要翻译： 本发明一般涉及用于治疗增殖性疾病，癌症等的治疗化合物领域，更具体地涉及本文所述的某些芳基 - 喹啉基化合物，其特别地抑制RAF（例如，B-RAF）活性 。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制RAF（例如BRAF）活性，抑制受体酪氨酸激酶（RTK）活性抑制 细胞增殖，以及通过抑制RAF，RTK等改善增殖性疾病如癌症（例如结肠直肠癌，黑素瘤）等疾病和病症的治疗。

公开(公告)号：US20100298320A1

公开(公告)日：2010-11-25

申请号：US12808249

申请日：2008-12-19

申请人： Caroline Joy Springer ,  Dan Niculescu-Duvaz ,  Ion Niculescu-Duvaz ,  Richard Marais ,  Bartholomeus Marinus Josephus Marie Suijkerbuijk ,  Alfonso Zambon ,  Arnaud Nourry ,  Delphine Menard

发明人： Caroline Joy Springer ,  Dan Niculescu-Duvaz ,  Ion Niculescu-Duvaz ,  Richard Marais ,  Bartholomeus Marinus Josephus Marie Suijkerbuijk ,  Alfonso Zambon ,  Arnaud Nourry ,  Delphine Menard

IPC分类号： A61K31/5377 ,  C12N5/02 ,  A61K31/4985 ,  A61P35/04 ,  C07D471/04

CPC分类号： C07D471/04 ,  A61K31/4985

摘要： The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.

摘要翻译： 本发明一般涉及用于治疗增殖性疾病，癌症等的治疗化合物领域，更具体地涉及本文所述的某些吡啶并[2,3-b]吡嗪-8-取代的化合物，其特别地， 抑制RAF（例如，B-RAF）活性。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制RAF（例如BRAF）活性，抑制受体酪氨酸激酶（RTK）活性抑制 细胞增殖，以及通过抑制RAF，RTK等改善增殖性疾病如癌症（例如结肠直肠癌，黑素瘤）等疾病和病症的治疗。

公开(公告)号：US08815896B2

公开(公告)日：2014-08-26

申请号：US13520613

申请日：2011-01-27

申请人： Caroline Springer ,  Ion Niculescu-Duvaz ,  Richard Marais ,  Dan Niculescu-Duvaz ,  Alfonso Zambon ,  Delphine Menard

发明人： Caroline Springer ,  Ion Niculescu-Duvaz ,  Richard Marais ,  Dan Niculescu-Duvaz ,  Alfonso Zambon ,  Delphine Menard

IPC分类号： C07D401/02 ,  A61K31/4353

CPC分类号： A61K31/437 ,  A61K31/4353 ,  C07D401/02 ,  C07D471/04

摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (I) (for convenience, collectively referred to herein as “IP compounds”), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterized by (e.g., driven by) mutant RAS (“mutant RAS cancer”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer.

摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及下列通式（I）的某些化合物（为了方便起见，统称为“IP化合物”），其特别可用于治疗 癌症，例如以突变RAS（“突变RAS癌症”）为特征的癌症。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在治疗癌症中的用途，例如突变RAS癌症。

公开(公告)号：US20120283288A1

公开(公告)日：2012-11-08

申请号：US13520613

申请日：2011-01-27

申请人： Caroline Springer ,  Ion Niculescu-Duvaz ,  Richard Marais ,  Dan Niculescu-Duvaz ,  Alfonso Zambon ,  Delphine Menard

发明人： Caroline Springer ,  Ion Niculescu-Duvaz ,  Richard Marais ,  Dan Niculescu-Duvaz ,  Alfonso Zambon ,  Delphine Menard

IPC分类号： A61K31/437 ,  A61P35/00 ,  A61P35/02 ,  C07D471/04

CPC分类号： A61K31/437 ,  A61K31/4353 ,  C07D401/02 ,  C07D471/04

摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (I) (for convenience, collectively referred to herein as “IP compounds”), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterised by (e.g., driven by) mutant RAS (“mutant RAS cancer”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer.

摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及下列通式（I）的某些化合物（为了方便起见，本文统称为IP化合物），其尤其可用于治疗癌症 ，例如以突变RAS（突变RAS癌症）为特征的癌症（例如驱动的）。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在治疗癌症中的用途，例如突变RAS癌症。

公开(公告)号：US08198279B2

公开(公告)日：2012-06-12

申请号：US12808249

申请日：2008-12-19

申请人： Caroline Joy Springer ,  Dan Niculescu-Duvaz ,  Ion Niculescu-Duvaz ,  Richard Marais ,  Bartholomeus Marinus Josephus Marie Suijkerbuijk ,  Alfonso Zambon ,  Arnaud Nourry ,  Delphine Menard

发明人： Caroline Joy Springer ,  Dan Niculescu-Duvaz ,  Ion Niculescu-Duvaz ,  Richard Marais ,  Bartholomeus Marinus Josephus Marie Suijkerbuijk ,  Alfonso Zambon ,  Arnaud Nourry ,  Delphine Menard

IPC分类号： A61K31/4985 ,  C07D471/14

CPC分类号： C07D471/04 ,  A61K31/4985

摘要： The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B—RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.

摘要翻译： 本发明一般涉及用于治疗增殖性疾病，癌症等的治疗化合物领域，更具体地涉及本文所述的某些吡啶并[2,3-b]吡嗪-8-取代的化合物，其特别地， 抑制RAF（例如，B-RAF）活性。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制RAF（例如BRAF）活性，抑制受体酪氨酸激酶（RTK）活性抑制 细胞增殖，以及通过抑制RAF，RTK等改善增殖性疾病如癌症（例如结肠直肠癌，黑素瘤）等疾病和病症的治疗。

公开(公告)号：US08546387B2

公开(公告)日：2013-10-01

申请号：US13459120

申请日：2012-04-28

申请人： Caroline Joy Springer ,  Dan Niculescu-Duvaz ,  Ion Niculescu-Duvaz ,  Richard Marais ,  Bartholomeus Marinus Josephus Marie Suijkerbuijk ,  Alfonso Zambon ,  Arnaud Nourry ,  Delphine Menard

发明人： Caroline Joy Springer ,  Dan Niculescu-Duvaz ,  Ion Niculescu-Duvaz ,  Richard Marais ,  Bartholomeus Marinus Josephus Marie Suijkerbuijk ,  Alfonso Zambon ,  Arnaud Nourry ,  Delphine Menard

IPC分类号： A61K31/4985 ,  A61K31/5377 ,  C07D471/14 ,  C07D413/14

CPC分类号： C07D471/04 ,  A61K31/4985

摘要： The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.

摘要翻译： 本发明一般涉及用于治疗增殖性疾病，癌症等的治疗化合物领域，更具体地涉及本文所述的某些吡啶并[2,3-b]吡嗪-8-取代的化合物，其特别地， 抑制RAF（例如，B-RAF）活性。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制RAF（例如BRAF）活性，抑制受体酪氨酸激酶（RTK）活性抑制 细胞增殖，以及通过抑制RAF，RTK等改善增殖性疾病如癌症（例如结肠直肠癌，黑素瘤）等疾病和病症的治疗。

公开(公告)号：US08383816B2

公开(公告)日：2013-02-26

申请号：US12988619

申请日：2009-04-27

申请人： Ion Niculescu-Duvaz ,  Alfonso Zambon ,  Dan Niculescu-Duvaz ,  Steven Whittaker ,  Richard Marais ,  Caroline Joy Springer

发明人： Ion Niculescu-Duvaz ,  Alfonso Zambon ,  Dan Niculescu-Duvaz ,  Steven Whittaker ,  Richard Marais ,  Caroline Joy Springer

IPC分类号： C07D513/02

CPC分类号： C07D471/04

摘要： The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain aryl-quinolyl compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.

摘要翻译： 本发明一般涉及用于治疗增殖性疾病，癌症等的治疗化合物领域，更具体地涉及本文所述的某些芳基 - 喹啉基化合物，其特别地抑制RAF（例如，B-RAF）活性 。 本发明还涉及包含这种化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制RAF（例如BRAF）活性，抑制受体酪氨酸激酶（RTK）活性抑制 细胞增殖，以及通过抑制RAF，RTK等改善增殖性疾病如癌症（例如结肠直肠癌，黑素瘤）等疾病和病症的治疗。

公开(公告)号：US20120238568A1

公开(公告)日：2012-09-20

申请号：US13459120

申请日：2012-04-28

申请人： Caroline Joy Springer ,  Dan Niculescu-Duvaz ,  Ion Niculescu-Duvaz ,  Richard Marais ,  Bartholomeus Marinus Josephus Marie Suijkerbuijk ,  Alfonso Zambon ,  Arnaud Nourry ,  Delphine Menard

发明人： Caroline Joy Springer ,  Dan Niculescu-Duvaz ,  Ion Niculescu-Duvaz ,  Richard Marais ,  Bartholomeus Marinus Josephus Marie Suijkerbuijk ,  Alfonso Zambon ,  Arnaud Nourry ,  Delphine Menard

IPC分类号： C07D471/04 ,  A61P35/00 ,  A61K31/5377 ,  A61K31/4985 ,  C12N5/07

CPC分类号： C07D471/04 ,  A61K31/4985

摘要： The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.

摘要翻译： 本发明一般涉及用于治疗增殖性疾病，癌症等的治疗化合物领域，更具体地涉及本文所述的某些吡啶并[2,3-b]吡嗪-8-取代的化合物，其特别地， 抑制RAF（例如，B-RAF）活性。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制RAF（例如BRAF）活性，抑制受体酪氨酸激酶（RTK）活性抑制 细胞增殖，以及通过抑制RAF，RTK等改善增殖性疾病如癌症（例如结肠直肠癌，黑素瘤）等疾病和病症的治疗。