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公开(公告)号：EP1551795A1
公开(公告)日：2005-07-13
申请号：EP03757608.9
申请日：2003-10-16
申请人： Methylgene, Inc.
发明人： RAEPPEL, Stephane , GAUDETTE, Frederic , PAQUIN, Isabelle , VAISBURG, Arkadii , DELORME, Daniel
IPC分类号： C07C235/84
CPC分类号： C07C311/19 , C07C233/80 , C07C235/84 , C07C237/40 , C07C2601/02 , C07C2601/08 , C07D209/16 , C07D209/44 , C07D211/22 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/50 , C07D213/74 , C07D239/47 , C07D249/14 , C07D277/82 , C07D295/155 , C07D295/185 , C07D317/66 , C07D401/12
摘要： The invention provides compoods and methods for treating cell proliferative- diseases. The invention provides new inhibitors of histone deacetylase enzymatic activity, compositions of the compounds comprising the inhibitors and a pharmaceutically acceptable carrier, excipient, or diluent, and methods of using the compounds to inhibit cellular proliferation in vitro and therapeutically.
摘要翻译： 本发明提供了治疗细胞增殖性疾病的综合症和方法。 本发明提供组蛋白脱乙酰酶酶活性的新抑制剂，包含抑制剂和药学上可接受的载体，赋形剂或稀释剂的化合物的组合物，以及在体外和治疗上使用该化合物抑制细胞增殖的方法。
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公开(公告)号：EP2049200B1
公开(公告)日：2015-04-29
申请号：EP07870696.7
申请日：2007-05-21
申请人： MethylGene Inc.
发明人： DININNO, Frank , HAMMOND, Milton L. , DYKSTRA, Kevin , KIM, Seongkon , TAN, Qiang , YOUNG, Katherine , HERMES, Jeffrey Donald , CHEN, Helen , RAEPPEL, Stephane , MANNION, Michael , GAUDETTE, Frederic , VAISBURG, Arkadii , RAHL, Jubrail , GEORGOPAPADAKOU, Nafsika , ZHOU, Nancy Z.
IPC分类号： A61P31/04 , C07F9/6539 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561 , A61K31/67 , A61K31/675
CPC分类号： C07F9/655354 , C07F9/65395 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561
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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
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公开(公告)号：EP2024376A1
公开(公告)日：2009-02-18
申请号：EP07795059.0
申请日：2007-05-21
发明人： DININNO, Frank , HAMMOND, Milton, L. , DYKSTRA, Kevin , KIM, Seongkon , TAN, Qiang , YOUNG, Katherine , HERMES, Jeffrey, Donald , RAEPPEL, Stephane , MANNION, Michael , ZHOU, Nancy, Z. , GAUDETTE, Frederic , VAISBURG, Arkadii , RAHIL, Jubrail , GEORGOPAPADAKOU, Nafsika
IPC分类号： C07F9/6539 , C07F9/655 , C07F9/6553 , C07F9/6558 , A61K31/662 , A61P31/04
CPC分类号： C07F9/655354 , C07F9/6539 , C07F9/65517 , C07F9/655345 , C07F9/65586
摘要： This invention provides novel β-lactamase inhibitors of the aryl-and heteroaryl-sulfonamidomethylphosphonate monoester class. The compounds inhibit three classes of β-lactamases and synergize the antibacterial effects of β-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the β-lactam antibiotics as a result of the presence of the β-lactamases. Formula (I) or a pro-drug or pharmaceutically acceptable salt thereof, wherein: W represents: Formula (II).
摘要翻译： 本发明提供了芳基 - 和杂芳基 - 磺酰胺甲基膦酸酯单酯类的新型β-内酰胺酶抑制剂。 由于β-内酰胺酶的存在，这些化合物抑制三类β-内酰胺酶并且协同β-内酰胺类抗生素（例如亚胺培南和头孢他啶）对通常对β-内酰胺类抗生素耐药的微生物的抗菌作用 。 式（I）或其前药或药学上可接受的盐，其中：W表示：式（II）。
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公开(公告)号：EP2049200A2
公开(公告)日：2009-04-22
申请号：EP07870696.7
申请日：2007-05-21
申请人： MethylGene Inc.
发明人： DININNO, Frank , HAMMOND, Milton L. , DYKSTRA, Kevin , KIM, Seongkon , TAN, Qiang , YOUNG, Katherine , HERMES, Jeffrey Donald , CHEN, Helen , RAEPPEL, Stephane , MANNION, Michael , GAUDETTE, Frederic , VAISBURG, Arkadii , RAHIL, Jubrail , GEORGOPAPADAKOU, Nafsika , ZHOU, Nancy Z.
IPC分类号： A61P31/04 , C07F9/6539 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561 , A61K31/67 , A61K31/675
CPC分类号： C07F9/655354 , C07F9/65395 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561
摘要： This invention provides novel β-lactamase inhibitors of the aryl-and heteroarylsulfonarnidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of β-lactamases and synergize the antibacterial effects of β-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the β-lactam antibiotics as a result of the presence of the β-lactamases. Formula (I) or pharmaceutically acceptable salt thereof.
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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
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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).
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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.
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公开(公告)号：EP1429765A2
公开(公告)日：2004-06-23
申请号：EP02763627.3
申请日：2002-09-12
申请人： Methylgene, Inc.
发明人： DELORME, Daniel , WOO, Soon, Hyung , VAISBURG, Arkadii , MORADEL, Oscar , LEIT, Silvana , RAEPPEL, Stephane , FRECHETTE, Sylvie , BOUCHAIN, Giliane
IPC分类号： A61K31/44 , A61K31/506 , A61K31/16 , A61K31/472 , A61K31/47 , A61K31/428 , A61K31/41 , C07D213/74 , C07D401/12 , C07D405/12 , C07D213/82 , C07C237/20 , C07D215/38 , C07D215/36 , C07D239/42 , C07D239/52 , C07D217/04 , C07D277/82 , C07D277/42 , C07D257/04 , A61P35/00
CPC分类号： C07D213/30 , C07C15/18 , C07C233/44 , C07C233/80 , C07C235/38 , C07C235/42 , C07C235/56 , C07C235/84 , C07C237/20 , C07C237/22 , C07C237/40 , C07C237/42 , C07C255/58 , C07C255/59 , C07C275/34 , C07C275/36 , C07C311/42 , C07C323/32 , C07C323/36 , C07C323/44 , C07C323/60 , C07C381/00 , C07C2601/14 , C07C2602/08 , C07C2603/18 , C07D213/74 , C07D231/12 , C07D233/56 , C07D233/64 , C07D239/91 , C07D249/08 , C07D251/18 , C07D251/52 , C07D251/54 , C07D263/14 , C07D263/24 , C07D265/36 , C07D271/06 , C07D277/42 , C07D277/74 , C07D277/82 , C07D295/155 , C07D307/12 , C07D307/28 , C07D311/56 , C07D311/58 , C07D333/36 , C07D333/38 , C07D401/12 , C07D403/04 , C07D409/12 , C07D473/40 , C07D487/04 , C07D495/04 , C07D513/04 , C07F7/0812 , C07F7/0818
摘要： The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
摘要翻译： 本发明涉及抑制组蛋白脱乙酰酶。 本发明提供了抑制组蛋白脱乙酰酶酶活性的化合物和方法。 本发明还提供了治疗细胞增殖性疾病和病症的组合物和方法。
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