公开(公告)号：EP1904504B1

公开(公告)日：2014-03-19

申请号：EP06842339.1

申请日：2006-05-19

申请人： MethylGene Inc.

发明人： SAAVEDRA, Oscar, Mario ,  CLARIDGE, Stephen, William ,  ZHAN, Lijie ,  RAEPPEL, Franck ,  VAISBURG, Arkadii ,  RAEPPEL, Stephane ,  DEZIEL, Robert ,  MANNION, Michael ,  ZHOU, Nancy, Z. ,  ISAKOVIC, Ljubomir

IPC分类号： C07D495/04 ,  C07D487/04 ,  A61K31/4365 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/437 ,  A61K31/444 ,  A61K31/496 ,  A61K31/55 ,  A61P35/00 ,  C07D498/04

CPC分类号： C07D495/04 ,  A61K31/519 ,  A61K31/522

公开(公告)号：EP2183254A1

公开(公告)日：2010-05-12

申请号：EP08800252.2

申请日：2008-08-28

申请人： MethylGene Inc.

发明人： CLARIDGE, Stephen William ,  ISAKOVIC, Ljubomir ,  MANNION, Michael ,  RAEPPEL, Stéphane ,  SAAVEDRA, Oscar Mario ,  GAUDETTE, Frédéric ,  ZHAN, Lijie ,  ZHOU, Nancy Z. ,  RAEPPEL, Franck ,  DÉZIEL, Robert ,  VAISBURG, Arkadii ,  UNO, Tetsuyuki

IPC分类号： C07D495/04 ,  A61K31/00 ,  A61K31/4365 ,  A61P27/02 ,  A61P35/00 ,  A61P9/00

CPC分类号： C07D495/04

摘要： The invention relates to compounds of Formula (I) and their use for inhibiting protein tyrosine kinase activity In Formula (I), the group M is thieno[3,2,b]pyridinyl as shown, and the group D is a ring or ring system, and the groups Z, Ar, and G are as defined herein The invention relates particularly to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signalling, for example, the inhibition of VEGF receptor signalling and HGF receptor signalling The invention also provides compositions and methods for treating cell proliferative diseases and conditions, such as cancer, and for treating ophthalmic diseases, including age-related macular degeneration (AMD) and diabetic retinopathy (DR).

公开(公告)号：EP1957498A2

公开(公告)日：2008-08-20

申请号：EP06851548.5

申请日：2006-05-19

申请人： MethylGene Inc.

发明人： SAAVEDRA, Oscar, Mario ,  CLARIDGE, Stephen, William ,  ZHAN, Lijie ,  RAEPPEL, Franck ,  VAISBURG, Arkadii ,  RAEPPEL, Stephane ,  DEZIEL, Robert ,  MANNION, Michael ,  ZHOU, Nancy ,  GAUDETTE, Frederic ,  ISAKOVIC, Ljubomir ,  WAHHAB, Amal ,  GRANGER, Marie-Claude ,  BERNSTEIN, Naomy

IPC分类号： C07D495/04

CPC分类号： C07D495/04

摘要： The invention relates to compounds of formula A, and their use for inhibiting the VEGF receptor KDR and the HGF receptor c-met Pn preferred structures of formula A, A
1 is S, A
2 =A
3 =CH, Z is O, S, S(O)
0-2 or NR
5 , Ar is phenyl, and G includes a nitrogen linker to Ar The groups D, G, and R
5 are as defined herein The invention also provides compositions and methods for treating cell proliferative diseases and conditions Examples of the diseases include breast cancer, lung cancer, colon cancer, rectal cancer, bladder cancer, leukemia and renal

摘要翻译： 本发明涉及式A化合物及其用于抑制式A的VEGF受体KDR和HGF受体c-met P n优选结构的用途，A 1是S，A 2 = A 3 = CH，Z是O，S ，S（O）0-2或NR 5，Ar为苯基，并且G包括与Ar连接的氮连接基团D，G和R 5如本文所定义。本发明还提供了用于治疗细胞增殖性疾病的组合物和方法，和 病症的例子包括乳腺癌，肺癌，结肠癌，直肠癌，膀胱癌，白血病和肾

公开(公告)号：EP2183255A1

公开(公告)日：2010-05-12

申请号：EP08800257.1

申请日：2008-08-29

申请人： MethylGene Inc.

发明人： RAEPPEL, Franck ,  ISAKOVIC, Ljubomir ,  CLARIDGE, Stephen William ,  MANNION, Michael ,  ZHAN, Lijie ,  GRANGER, Marie-Claude ,  VAISBURG, Arkadii ,  NANTEL, Miguel

IPC分类号： C07D495/04 ,  A61K31/4365

CPC分类号： C07D495/04 ,  C07D213/38 ,  C07D213/51 ,  C07D213/61

摘要： The invention relates to processes and intermediates for manufacturing fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, and to processes and intermediates for preparing intermediates that are useful in the manufacture of fused heterocyclic-type kinase inhibitor compounds, particularly at an industrial level The processes are aimed at ultimately forming compounds of the formula (A) where M is thieno[3,2,b]pyridinyl as shown, the group D is a ring or ring system, preferably pyridine, and the group Z, Ar, and G are as defined herein Such compounds can act to inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signalling, for example, the inhibition of VEGF receptor signalling and HGF receptor signalling.

公开(公告)号：EP1844062A2

公开(公告)日：2007-10-17

申请号：EP06718809.4

申请日：2006-01-18

申请人： Methylgene, Inc.

发明人： WAHHAB, Amal ,  BESTERMAN, Jeffrey, M. ,  DELORME, Daniel ,  ISAKOVIC, Ljubomir ,  LLEWELLYN, David ,  RAHIL, Jubrail ,  SAAVEDRA, Oscar ,  DEZIEL, Robert

IPC分类号： C07H19/16 ,  A61P35/02 ,  A61K31/7076

CPC分类号： C07H19/16

摘要： The invention relates to the inhibition of DNA methyltransferase isoforms DNMT1 and DNMT3b2. The invention provides compounds and methods for inhibiting DNMT1 and DNMT3b2.

公开(公告)号：EP2183254B1

公开(公告)日：2017-06-21

申请号：EP08800252.2

申请日：2008-08-28

申请人： MethylGene Inc.

发明人： CLARIDGE, Stephen William ,  ISAKOVIC, Ljubomir ,  MANNION, Michael ,  RAEPPEL, Stéphane ,  SAAVEDRA, Oscar Mario ,  GAUDETTE, Frédéric ,  ZHAN, Lijie ,  ZHOU, Nancy Z. ,  RAEPPEL, Franck ,  DÉZIEL, Robert ,  VAISBURG, Arkadii ,  UNO, Tetsuyuki

IPC分类号： C07D495/04 ,  A61K31/00 ,  A61K31/4365 ,  A61P27/02 ,  A61P35/00 ,  A61P9/00

CPC分类号： C07D495/04

公开(公告)号：EP1957498B1

公开(公告)日：2017-02-15

申请号：EP06851548.5

申请日：2006-05-19

申请人： MethylGene Inc.

发明人： SAAVEDRA, Oscar, Mario ,  CLARIDGE, Stephen, William ,  ZHAN, Lijie ,  RAEPPEL, Franck ,  VAISBURG, Arkadii ,  RAEPPEL, Stéphane ,  DEZIEL, Robert ,  MANNION, Michael ,  ZHOU, Nancy ,  GAUDETTE, Frederic ,  ISAKOVIC, Ljubomir ,  WAHHAB, Amal ,  GRANGER, Marie-Claude ,  BERNSTEIN, Naomy

IPC分类号： C07D495/04 ,  A61K31/4365 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61P35/00

CPC分类号： C07D495/04

公开(公告)号：EP2262815A1

公开(公告)日：2010-12-22

申请号：EP09716596.3

申请日：2009-02-27

申请人： MethylGene Inc.

发明人： MANNION, Michael ,  RAEPPEL, Stéphane ,  CLARIDGE, Stephen William ,  GAUDETTE, Frédéric ,  ZHAN, Lijie ,  ISAKOVIC, Ljubomir ,  SAAVEDRA, Oscar Mario ,  UNO, Tetsuyuki ,  KISHIDA, Masashi ,  VAISBURG, Arkadii

IPC分类号： C07D495/04 ,  A61K31/4365

CPC分类号： C07D495/04 ,  C07F9/6561

摘要： This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and opthalmological diseases, disorders and conditions.

摘要翻译： 本发明涉及抑制蛋白酪氨酸激酶活性的化合物。 特别地，本发明涉及抑制生长因子受体的蛋白质酪氨酸激酶活性的化合物，导致抑制受体信号传导，例如抑制VEGF受体信号传导。 本发明还提供了用于治疗细胞增殖性疾病和病症以及眼科疾病，病症和病症的化合物，组合物和方法。

公开(公告)号：EP1904504A2

公开(公告)日：2008-04-02

申请号：EP06842339.1

申请日：2006-05-19

申请人： Methylgene, Inc.

发明人： SAAVEDRA, Oscar, Mario ,  CLARIDGE, Stephen, William ,  ZHAN, Lijie ,  RAEPPEL, Franck ,  VAISBURG, Arkadii ,  RAEPPEL, Stephane ,  DEZIEL, Robert ,  MANNION, Michael ,  ZHOU, Nancy, Z. ,  ISAKOVIC, Ljubomir

IPC分类号： C07D495/04 ,  A61P35/00 ,  A61K31/4365 ,  C07D487/04

CPC分类号： C07D495/04 ,  A61K31/519 ,  A61K31/522

摘要： The invention relates to the inhibition of vascular endothelial growth factor (VEGF) receptor signaling and hepatocyte growth factor (HGF) receptor signaling The invention provides compound A and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions. Formula (A).

公开(公告)号：EP1735319A1

公开(公告)日：2006-12-27

申请号：EP05714678.9

申请日：2005-03-29

申请人： Methylgene, Inc.

发明人： DELORME, Daniel ,  VAISBURG, Arkadii ,  MORADEI, Oscar ,  LEIT, Silvana ,  RAEPPEL, Stephane ,  FRECHETTE, Sylvie ,  BOUCHAIN, Giliane ,  ZHOU, Zhihong ,  PAQUIN, Isabelle ,  GAUDETTE, Frederic ,  ISAKOVIC, Ljubomir

IPC分类号： C07D495/04

CPC分类号： C07C311/21 ,  C07C237/40 ,  C07C311/39 ,  C07D209/08 ,  C07D209/14 ,  C07D209/16 ,  C07D213/22 ,  C07D213/38 ,  C07D213/74 ,  C07D231/38 ,  C07D235/16 ,  C07D237/20 ,  C07D239/26 ,  C07D239/42 ,  C07D239/48 ,  C07D263/58 ,  C07D271/06 ,  C07D277/74 ,  C07D277/82 ,  C07D295/088 ,  C07D295/135 ,  C07D295/185 ,  C07D307/85 ,  C07D333/38 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D409/04 ,  C07D417/04 ,  C07D417/12 ,  C07D495/04

摘要： The invention relates to a series of compounds useful for inhibiting histone deacetylase (HDAC) enzymatic activity. The invention also provides a method for inhibiting histone descetylase in a cell using said compounds as well as a method for treating cell proliferative diseases and conditions using said HDAC inhibitors. Further, the invention provides pharmaceutical compositions comprising the HDAC inhibiting compounds and a pharmaceutically acceptable carrier.