公开(公告)号：EP2190845A2

公开(公告)日：2010-06-02

申请号：EP08827808.0

申请日：2008-08-21

申请人： ArQule, Inc.

发明人： ASHWELL, Mark, A. ,  TANDON, Manish ,  NAMDEW, Nivedita, D. ,  LAPIERRE, Jean, Marc ,  LIU, Yanbin ,  WU, Hui

IPC分类号： C07D471/06 ,  C07D487/06 ,  C07D513/04 ,  A61K31/429 ,  A61P35/00

CPC分类号： C07D513/04 ,  C07D471/06 ,  C07D487/06

摘要： The present invention provides hydroxamic acid compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the hydroxamic acid compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of the present invention.

公开(公告)号：EP2723741B8

公开(公告)日：2016-09-21

申请号：EP12802947.7

申请日：2012-06-21

申请人： ArQule, Inc.

发明人： ASHWELL, Mark, A. ,  BRASSARD, Chris ,  FILIKOV, Anton ,  HILL, Jason ,  KOERNER, Steffi ,  LAPIERRE, Jean-Marc ,  LIU, Yanbin ,  NAMDEV, Nivedita ,  NICEWONGER, Robert ,  PALMA, Rocio ,  TANDON, Manish ,  VENSEL, David ,  MATSUDA, Akihisa ,  IIMURA, Shin ,  YOSHIDA, Kenichi ,  YAMAZAKI, Takanori ,  KITAMURA, Takahiro ,  ISOYAMA, Takeshi

IPC分类号： C07D471/04 ,  C07D401/04 ,  C07D413/14 ,  A61K31/4745 ,  A61P35/00

CPC分类号： C07D471/04 ,  C07D451/02 ,  C07D491/08 ,  C07D498/08

公开(公告)号：EP2379506B1

公开(公告)日：2015-09-02

申请号：EP09793690.0

申请日：2009-12-30

申请人： ArQule, Inc.

发明人： ALI, Syed, M. ,  ASHWELL, Mark ,  TANDON, Manish ,  YANG, Rui-yang ,  LIU, Yanbin ,  VENSEL, David ,  EATHIRAJ, Sudharshan ,  PALMA, Rocio ,  LAPIERRE, Jean-marc ,  WESTLUND, Neil ,  WU, Hui ,  NAMDEV, Nivedita ,  KELLEHER, Eugene

IPC分类号： C07D221/10 ,  C07D401/12 ,  C07D471/10 ,  A61K31/55 ,  A61P35/00

CPC分类号： C07D239/70 ,  C07D221/10 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D471/10

公开(公告)号：EP2519522B1

公开(公告)日：2014-09-24

申请号：EP10841702.3

申请日：2010-12-29

申请人： ArQule, Inc.

发明人： ASHWELL, Mark, A. ,  BRASSARD, Chris ,  FILIKOV, Anton ,  HILL, Jason ,  KOERNER, Steffi ,  LAPIERRE, Jean-Marc ,  LIU, Yanbin ,  NAMDEV, Nivedita ,  NICEWONGER, Robert ,  PALMA, Rocio ,  TANDON, Manish ,  VENSEL, David ,  MATSUDA, Akihisa ,  IIMURA, Shin ,  YAMAMOTO, Yuko

IPC分类号： C07D471/04 ,  C07D401/04 ,  C07D401/14 ,  A61K31/437 ,  A61P35/00

CPC分类号： C07D471/04

公开(公告)号：EP2414360A1

公开(公告)日：2012-02-08

申请号：EP10711972.9

申请日：2010-03-31

申请人： ArQule, Inc.

发明人： TANDON, Manish ,  LIU, Yanbin ,  NAMDEV, Nivedita ,  ASHWELL, Mark, A. ,  PALMA, Rocio

IPC分类号： C07D471/22 ,  A61K31/519 ,  A61P35/00 ,  C07D471/14

CPC分类号： C07D471/22 ,  C07D471/14

摘要： The present invention relates to substituted dipyrido-pyrimido-diazepine compounds of formula (I), substituted benzo-pyrido-pyrimido-diazepine compounds of formula (I) and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted dipyrido-pyrimido-diazepine compounds, substituted benzo-pyrido-pyrimido- diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

摘要翻译： 本发明涉及式（I）的取代的二吡啶并 - 嘧啶并二氮杂化合物，式（I）的取代的苯并吡啶并 - 嘧啶并二氮杂化合物和合成这些化合物的方法。 本发明还涉及含有取代的二吡啶并嘧啶二氮杂化合物，取代的苯并吡啶并嘧啶二氮杂化合物和治疗细胞增殖性疾病如癌症的方法的药物组合物，通过将这些化合物和药物组合物给予有需要的受试者 。

公开(公告)号：EP1877097A2

公开(公告)日：2008-01-16

申请号：EP05785192.5

申请日：2005-08-11

申请人： ARQULE, INC.

发明人： ASHWELL, Mark ,  TANDON, Manish ,  LAPIERRE, Jean-Marc ,  LIU, Yanbin

IPC分类号： A61K47/48 ,  C07D311/92 ,  A61P35/00

CPC分类号： B82Y5/00 ,  A61K31/785 ,  A61K47/54 ,  A61K47/542 ,  A61K47/64 ,  A61K47/665

摘要： The present invention relates to quinone prodrug compositions and therapeutic methods using such prodrug compositions. Preferably, the quinone compounds of the invention are napthoquinone compounds such as β-lapachone or β-lapachone analogs. The quinone prodrug compositions of the invention exhibit improved solubility, stability, bioavailability, and pharmacokinetic properties, as well as improved plasma half-life in vivo.

公开(公告)号：EP1877097B1

公开(公告)日：2012-06-20

申请号：EP05785192.5

申请日：2005-08-11

申请人： ARQULE, INC.

发明人： ASHWELL, Mark ,  TANDON, Manish ,  LAPIERRE, Jean-Marc ,  LIU, Yanbin

IPC分类号： A61K47/48 ,  C07D311/92 ,  A61P35/00

CPC分类号： B82Y5/00 ,  A61K31/785 ,  A61K47/54 ,  A61K47/542 ,  A61K47/64 ,  A61K47/665

摘要： The present invention relates to quinone prodrug compositions and therapeutic methods using such prodrug compositions. Preferably, the quinone compounds of the invention are napthoquinone compounds such as β-lapachone or β-lapachone analogs. The quinone prodrug compositions of the invention exhibit improved solubility, stability, bioavailability, and pharmacokinetic properties, as well as improved plasma half-life in vivo.

公开(公告)号：EP2361254A1

公开(公告)日：2011-08-31

申请号：EP09768464.1

申请日：2009-12-04

申请人： ArQule, Inc.

发明人： LAPIERRE, Jean-marc ,  LIU, Yanbin ,  TANDON, Manish ,  ASHWELL, Mark, A.

IPC分类号： C07D498/04 ,  C07D513/04 ,  A61K31/429 ,  A61K31/424 ,  A61P35/00

CPC分类号： C07D498/04 ,  C07D513/04

摘要： The present invention provides imidazooxazole and imidazothiazole compounds and their syntheses. The compounds of the present invention are capable of inhibiting the activity of RAF kinase, such as B-RAF
V600E . The compounds are useful for the treatment of cell proliferative disorders such as cancer.

公开(公告)号：EP2013218A2

公开(公告)日：2009-01-14

申请号：EP07755575.3

申请日：2007-04-16

申请人： ARQULE, INC.

发明人： LAPIERRE, Jean-Marc ,  NAMDEV, Nivedita D. ,  ASHWELL, Mark A. ,  FRANCE, Dennis S. ,  WU, Hui ,  HUTCHINS, Patrick M. ,  TANDON, Manish ,  LIU, Yanbin ,  LINK, Jeff S. ,  ALI, Syed M. ,  BRASSARD, Chris J. ,  NICEWONGER, Robb B. ,  FILIKOV, Anton ,  CARAZZA, Rebecca J.

IPC分类号： C07D498/04 ,  C07D513/04 ,  A61K31/429 ,  A61K31/4188 ,  A61K31/35

CPC分类号： C07D513/04

摘要： The present invention provides imidazooxazole and imidazothiazole compounds and their synthesis. The compounds of the present invention are capable of inhibiting the activity of RAF kinase, such as B-RAFV600E. The compounds are useful for the treatment of cell proliferative disorders such as cancer.

公开(公告)号：EP2723741B1

公开(公告)日：2016-04-27

申请号：EP12802947.7

申请日：2012-06-21

申请人： ArQule, Inc.

发明人： ASHWELL, Mark, A. ,  BRASSARD, Chris ,  FILIKOV, Anton ,  HILL, Jason ,  KOERNER, Steffi ,  LAPIERRE, Jean-Marc ,  LIU, Yanbin ,  NAMDEV, Nivedita ,  NICEWONGER, Robert ,  PALMA, Rocio ,  TANDON, Manish ,  VENSEL, David ,  MATSUDA, Akihisa ,  IIMURA, Shin ,  YOSHIDA, Kenichi ,  YAMAZAKI, Takanori ,  KITAMURA, Takahiro ,  ISOYAMA, Takeshi

IPC分类号： C07D471/04 ,  C07D401/04 ,  C07D413/14 ,  A61K31/4745 ,  A61P35/00

CPC分类号： C07D471/04 ,  C07D451/02 ,  C07D491/08 ,  C07D498/08