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公开(公告)号：EP1420780A2
公开(公告)日：2004-05-26
申请号：EP02767418.3
申请日：2002-08-22
申请人： Novartis AG , Novartis Pharma GmbH
发明人： NICOLAOU, Kyriacos, Costa , NAMOTO, Kenji , RITZEN, Andreas , ULVEN, Trond , SHOJI, Mutsuru , ALTMANN, Karl-Heinz
IPC分类号： A61K31/365 , C07D313/00 , C07D417/06 , C07D407/04 , A61P35/02
CPC分类号： C07D495/08 , C07D313/00 , C07D405/06 , C07D405/12 , C07D417/06 , C07D417/12
摘要： The invention relates to cis- and trans-12, 13-cyclopropyl and 12, 13-cyclobutyl epothilones of formula (I) to (IV), wherein Ar is a radical represented by the following structure:, and the other radicals and symbols have the meanings as defined herein; to their chemical synthesis and biological evaluation; their use in the treatment of neoplastic diseases and to pharmaceutical preparations containing such compounds. The compounds described herein are potent tubulin polymerization promoters and cytotoxic agents.
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公开(公告)号：EP1546152B1
公开(公告)日：2007-12-19
申请号：EP03747872.4
申请日：2003-08-01
IPC分类号： C07D493/04 , C07D417/06 , C07D405/06 , C07D407/06 , A61K31/427 , A61K31/4427 , A61P35/00 , A61P17/06
CPC分类号： C07D405/06 , C07D407/06 , C07D417/06 , C07D493/04
摘要： This invention relates Epothilone derivatives of formula (I), wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives , for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumour.
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公开(公告)号：EP1546152A1
公开(公告)日：2005-06-29
申请号：EP03747872.4
申请日：2003-08-01
IPC分类号： C07D493/04 , C07D417/06 , C07D405/06 , C07D407/06 , A61K31/427 , A61K31/4427 , A61P35/00 , A61P17/06
CPC分类号： C07D405/06 , C07D407/06 , C07D417/06 , C07D493/04
摘要： This invention relates Epothilone derivatives of formula (I), wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives , for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumour.
摘要翻译： 本发明涉及式（I）的埃坡霉素衍生物，其中符号和取代基如说明书中所定义，涉及其制备方法，涉及包含此类衍生物的药物组合物以及涉及此类衍生物在制备药物组合物中的用途 用于治疗增殖性疾病，例如肿瘤。
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公开(公告)号：EP1420780B1
公开(公告)日：2008-10-01
申请号：EP02767418.3
申请日：2002-08-22
申请人： Novartis AG , Novartis Pharma GmbH
发明人： NICOLAOU, Kyriacos, Costa , NAMOTO, Kenji , RITZEN, Andreas , ULVEN, Trond , SHOJI, Mutsuru , ALTMANN, Karl-Heinz
IPC分类号： A61K31/365 , C07D313/00 , C07D417/06 , C07D407/04 , A61P35/02
CPC分类号： C07D495/08 , C07D313/00 , C07D405/06 , C07D405/12 , C07D417/06 , C07D417/12
摘要： The invention relates to cis- and trans-12, 13-cyclopropyl and 12, 13-cyclobutyl epothilones of formula (I) to (IV), wherein Ar is a radical represented by the following structure:, and the other radicals and symbols have the meanings as defined herein; to their chemical synthesis and biological evaluation; their use in the treatment of neoplastic diseases and to pharmaceutical preparations containing such compounds. The compounds described herein are potent tubulin polymerization promoters and cytotoxic agents.
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