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1.发明公开DERIVES D'ACIDE HYDROXY-BISPHOSPHONIQUE COMME VECTEUR CIBLANT LE TISSU OSSEUX 有权羟基二膦酸衍生物比骨组织LOOKING VECTORS
公开(公告)号：EP2240501A1
公开(公告)日：2010-10-20
申请号：EP09700113.5
申请日：2009-01-05
申请人： Université de Nantes , Chu Nantes , INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM) , Centre National de la Recherche Scientifique (CNRS)
发明人： EGOROV, Maxim , FORTUN, Yannick , HEYMANN, Dominique , LEBRETON, Jacques , MATHE, Monique , PADRINES, Marc , REDINI, Françoise
IPC分类号： C07F9/38 , A61K31/663 , A61P35/00 , A61P19/10 , A61P3/14
CPC分类号： C07F9/3873 , C07F9/5728
摘要： The present invention relates to hydroxy-bisphosphonic acid derivatives corresponding to general formula (I): in which: - n and m denote, independently of one another, an integer ranging from 1 to 4, - X denotes an oxygen atom or an N-R3 group, - R1 and R3 denote, independently of one another, a linear or branched C1 to C6 alkyl group, and - R2 denotes a residue of a molecule of therapeutic or diagnostic interest, or pharmaceutically acceptable salts of said derivatives, and also the method for the preparation thereof and the therapeutic or diagnostic use thereof.
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2.发明授权DERIVES D'ACIDE HYDROXY-BISPHOSPHONIQUE COMME VECTEUR CIBLANT LE TISSU OSSEUX 有权羟基二膦酸衍生物比骨组织LOOKING VECTORS
公开(公告)号：EP2240501B1
公开(公告)日：2015-10-14
申请号：EP09700113.5
申请日：2009-01-05
申请人： Université de Nantes , CHU Nantes , INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM) , Centre National de la Recherche Scientifique (CNRS)
发明人： EGOROV, Maxim , FORTUN, Yannick , HEYMANN, Dominique , LEBRETON, Jacques , MATHE, Monique , PADRINES, Marc , REDINI, Françoise
IPC分类号： C07F9/38 , A61K31/663 , A61P35/00 , A61P19/10 , A61P3/14
CPC分类号： C07F9/3873 , C07F9/5728
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公开(公告)号：EP2240500B1
公开(公告)日：2014-10-01
申请号：EP09700083.0
申请日：2009-01-05
申请人： Université de Nantes , CHU Nantes , INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM) , Centre National de la Recherche Scientifique (CNRS)
发明人： EGOROV, Maxim , FORTUN, Yannick , HEYMANN, Dominique , LEBRETON, Jacques , MATHE, Monique , PADRINES, Marc , REDINI, Françoise
IPC分类号： C07F9/38
CPC分类号： C07F9/386 , C07F9/3873 , C07F9/5728
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公开(公告)号：EP2240500A1
公开(公告)日：2010-10-20
申请号：EP09700083.0
申请日：2009-01-05
申请人： Université de Nantes , Chu Nantes , INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM) , Centre National de la Recherche Scientifique (CNRS)
发明人： EGOROV, Maxim , FORTUN, Yannick , HEYMANN, Dominique , LEBRETON, Jacques , MATHE, Monique , PADRINES, Marc , REDINI, Françoise
IPC分类号： C07F9/38
CPC分类号： C07F9/386 , C07F9/3873 , C07F9/5728
摘要： The present invention relates to a method for preparing a hydroxy-bisphosphonic acid derivative or a salt thereof, from the corresponding carboxylic acid, comprising the following steps: - activation of the carboxylic acid function in the form of the boronate derivative thereof through the action of a borane, then - reaction with tris(trimethylsilyl)phosphite, under Arbuzov conditions - treatment with an alcohol, chosen in particular from an aliphatic alcohol or trifluoromethanol, and - separation of the hydroxy-bisphosphonic acid derivative formed, from the reaction medium.
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