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公开(公告)号：EP1896040B1
公开(公告)日：2012-08-01
申请号：EP06786161.7
申请日：2006-06-29
IPC分类号： C07F9/6506 , A61K31/675 , A61P35/00
CPC分类号： A61K31/675 , A61K31/337 , A61K31/513 , A61K31/7068 , A61K33/24 , C07F9/65062 , C07F9/65065 , C07F9/65397
摘要： Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
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公开(公告)号：EP1951679B1
公开(公告)日：2015-02-18
申请号：EP06801197.2
申请日：2006-08-10
发明人： YING, Weiwen , DU, Zhenjian , FOLEY, Kevin
IPC分类号： C07D233/70 , C07D403/04 , C07D233/84 , C07D233/88 , A61K31/4168 , A61P35/00
CPC分类号： A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/428 , A61K31/4709 , A61K31/52 , A61K31/5377 , A61K31/675 , C07D233/70 , C07D233/84 , C07D233/88 , C07D403/02 , C07D403/04 , C07D403/10 , C07F9/65065
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3.发明公开SYNTHESIS OF 1-ALKYL-2-AMINO-IMIDAZOL-5-CARBOXYLIC ACID ESTER VIA CALPHA-SUBSTITUTED N-ALKYL-GLYCINE ESTER DERIVATIVES 审中-公开合成缬氨酸2-烷基-2-氨基咪唑烷-5-碳酸钠ÜberCAL HA TE TE TE ATE ATE ATE ATE ATE ATE ATE ATE ATE ATE
公开(公告)号：EP3055295A1
公开(公告)日：2016-08-17
申请号：EP14789990.0
申请日：2014-10-10
申请人： Merck Patent GmbH
发明人： JASPER, Christian , HAHN, Helmut Dieter , BREUNING, Marcel André , KRATTIGER, Philipp , DEBOR, Michaela
IPC分类号： C07D317/12 , C07F9/22
CPC分类号： C07F9/65065 , C07D317/12 , C07D317/30 , C07F9/222
摘要： The invention provides an efficient and high yielding process for preparing TH-302, comprising at least one step wherein a dioxolane intermediate is generated in an aqueous layer, resulting in a synthesis that is amenable to scale up conditions.
摘要翻译： 本发明提供了一种制备TH-302的有效和高产率的方法，其包括至少一个步骤，其中在水层中产生二氧戊环中间体，导致可扩展条件的合成。
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公开(公告)号：EP2727926A4
公开(公告)日：2015-03-04
申请号：EP12804846
申请日：2012-06-27
发明人： MACHINAGA NOBUO , CHIBA JUN , HASHIMOTO RYUJI , OTOYO MAMORU , INOUE RYOTAKU
IPC分类号： C07F9/09 , A61K31/661 , A61P1/04 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P27/14 , A61P29/00 , A61P37/02 , A61P37/06 , A61P37/08
CPC分类号： C07F9/65062 , C07F7/1844 , C07F7/1856 , C07F9/572 , C07F9/65065 , C07F9/65583
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公开(公告)号：EP2336141A3
公开(公告)日：2011-09-14
申请号：EP11157963.7
申请日：2006-06-29
IPC分类号： C07F9/6506 , A61K31/675 , A61P35/00
CPC分类号： A61K31/675 , A61K31/337 , A61K31/513 , A61K31/7068 , A61K33/24 , C07F9/65062 , C07F9/65065 , C07F9/65397
摘要： Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more other anti-neoplastic agents.
摘要翻译： 当单独给药或与一种或多种其他抗肿瘤剂组合使用时，氨基磷酸酯烷化剂前药可用于治疗癌症。
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公开(公告)号：EP1951679A1
公开(公告)日：2008-08-06
申请号：EP06801197.2
申请日：2006-08-10
发明人： YING, Weiwen , DU, Zhenjian , FOLEY, Kevin
IPC分类号： C07D233/70 , C07D403/04 , C07D233/84 , C07D233/88 , A61K31/4168 , A61P35/00
CPC分类号： A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/428 , A61K31/4709 , A61K31/52 , A61K31/5377 , A61K31/675 , C07D233/70 , C07D233/84 , C07D233/88 , C07D403/02 , C07D403/04 , C07D403/10 , C07F9/65065
摘要： Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Formula (I) Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14- membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.
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公开(公告)号：EP1896040A2
公开(公告)日：2008-03-12
申请号：EP06786161.7
申请日：2006-06-29
IPC分类号： A61K31/685
CPC分类号： A61K31/675 , A61K31/337 , A61K31/513 , A61K31/7068 , A61K33/24 , C07F9/65062 , C07F9/65065 , C07F9/65397
摘要： Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
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公开(公告)号：EP2336141B1
公开(公告)日：2016-03-30
申请号：EP11157963.7
申请日：2006-06-29
IPC分类号： C07F9/6506 , A61K31/675 , A61P35/00 , C07F9/6539 , A61K31/337 , A61K31/513 , A61K31/7068 , A61K33/24
CPC分类号： A61K31/675 , A61K31/337 , A61K31/513 , A61K31/7068 , A61K33/24 , C07F9/65062 , C07F9/65065 , C07F9/65397
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公开(公告)号：EP2727926A1
公开(公告)日：2014-05-07
申请号：EP12804846.9
申请日：2012-06-27
IPC分类号： C07F9/09 , A61K31/661 , A61P1/04 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P27/14 , A61P29/00 , A61P37/02 , A61P37/06 , A61P37/08
CPC分类号： C07F9/65062 , C07F7/1844 , C07F7/1856 , C07F9/572 , C07F9/65065 , C07F9/65583
摘要： To provide a novel compound that has S1P lyase inhibitory ability and induces a reduction in the number of lymphocytes, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the compound or pharmaceutically acceptable salt thereof as an active ingredient. A compound represented by the general formula (I):
or a pharmaceutically acceptable salt thereof.摘要翻译： 提供具有S1P裂解酶抑制能力并诱导淋巴细胞数目减少的新型化合物或其药学上可接受的盐，以及含有该化合物或其药学上可接受的盐作为有效成分的药物组合物。 由通式（I）表示的化合物或其药学上可接受的盐。
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公开(公告)号：EP2336141A2
公开(公告)日：2011-06-22
申请号：EP11157963.7
申请日：2006-06-29
IPC分类号： C07F9/6506 , A61K31/675 , A61P35/00
CPC分类号： A61K31/675 , A61K31/337 , A61K31/513 , A61K31/7068 , A61K33/24 , C07F9/65062 , C07F9/65065 , C07F9/65397
摘要： Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more other anti-neoplastic agents.
摘要翻译： 当单独施用或与一种或多种其它抗肿瘤剂组合时，氨基磷酸烷基酯前体药物可用于治疗癌症。
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