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公开(公告)号：EP1896492A2
公开(公告)日：2008-03-12
申请号：EP06733954.9
申请日：2006-01-26
CPC分类号： C07F15/0093
摘要： Disclosed herein are novel platinum-based complexes possessing one nitrile substituent group (mononitrile) covalently-bonded to the platinum, one or more nitrogen donor ligands capable of forming hydrogen bonds with the bases in DNA or RNA and leaving groups (i.e., L1 and L2 )which can be hydrolyzed in vivo to active species, which can then form coordinate adducts with DNA or RNA at the Guanine or Adenine bases thereof. Also disclosed herein are the reaction schemes for the synthesis of said platinum complexes, as well as methods of treatment of various types of cancer by the administration of a pharmaceutically-effective dose of said novel platinum complexes.
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公开(公告)号：EP1896491A2
公开(公告)日：2008-03-12
申请号：EP06719723.6
申请日：2006-01-26
发明人： XIAO, Zejun , KOCHAT, Harry , HAUSHEER, Frederick
IPC分类号： C07F15/00 , A61K31/555
CPC分类号： C07F15/0093
摘要： Disclosed herein are novel platinum-based analogs with a single substituted azole ligand: RN=NR7, wherein the RN=NR7 functional group is covalently bonded to the platinum through nitrogen of NR7. The analogs also have nitrogen donor ligands capable of forming hydrogen bonds with the bases in DNA or RNA, and one or more leaving groups which can be displaced by water, hydroxide ions or other nucleophiles, which is thought to form active species in vivo, and then, form cross-linked complexes between nucleic acid strands, principally between purines in DNA (or RNA), i.e., at the Guanine or Adenine bases, thereof. These platinum analogs may also be more easily transported into tumor cells, due to their increased lipophilicity and are likely to be useful as anti¬ neoplastic agents, and in modulating or interfering with the synthesis or replication or transcription of DNA or translation or function of RNA in vitro or in vivo, as they are potentially capable of forming a platinum coordinate complex with an intact or nascent DNA or RNA and thereby interfering with cellular synthesis, transcription or replication of nucleic acid polynucleotides.
摘要翻译： 本文公开了具有单个取代的吡咯配体的新型铂基类似物：RN = NR7，其中RN = NR7官能团通过NR7的氮共价键合至铂。 类似物还具有能够与DNA或RNA中的碱基形成氢键的氮供体配体和可以被水，氢氧根离子或其他亲核试剂取代的一个或多个离去基团，其被认为在体内形成活性物质，并且 然后在核酸链之间形成交联复合物，主要是在DNA（或RNA）中的嘌呤，即在其鸟嘌呤或腺嘌呤碱基之间。 由于其亲脂性增加，这些铂类似物也可以更容易地转运到肿瘤细胞中，并且可能用作抗肿瘤剂，并且调节或干扰DNA的合成或复制或转录或RNA的翻译或功能 因为它们可能能够与完整或新生的DNA或RNA形成铂配位络合物，从而干扰核酸多核苷酸的细胞合成，转录或复制。
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公开(公告)号：EP1896490B1
公开(公告)日：2013-03-06
申请号：EP06719722.8
申请日：2006-01-26
IPC分类号： C07F15/00
CPC分类号： C07F15/0093
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公开(公告)号：EP1896491B1
公开(公告)日：2010-11-17
申请号：EP06719723.6
申请日：2006-01-26
发明人： XIAO, Zejun , KOCHAT, Harry , HAUSHEER, Frederick
IPC分类号： C07D237/30 , C07D237/32 , C07D249/18 , C07D257/04 , A61P35/00 , A61K31/7135
CPC分类号： C07F15/0093
摘要： Disclosed herein are novel platinum-based analogs with a single substituted azole ligand: RN=NR7, wherein the RN=NR7 functional group is covalently bonded to the platinum through nitrogen of NR7. The analogs also have nitrogen donor ligands capable of forming hydrogen bonds with the bases in DNA or RNA, and one or more leaving groups which can be displaced by water, hydroxide ions or other nucleophiles, which is thought to form active species in vivo, and then, form cross-linked complexes between nucleic acid strands, principally between purines in DNA (or RNA), i.e., at the Guanine or Adenine bases, thereof. These platinum analogs may also be more easily transported into tumor cells, due to their increased lipophilicity and are likely to be useful as anti¬ neoplastic agents, and in modulating or interfering with the synthesis or replication or transcription of DNA or translation or function of RNA in vitro or in vivo, as they are potentially capable of forming a platinum coordinate complex with an intact or nascent DNA or RNA and thereby interfering with cellular synthesis, transcription or replication of nucleic acid polynucleotides.
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公开(公告)号：EP1896490A1
公开(公告)日：2008-03-12
申请号：EP06719722.8
申请日：2006-01-26
IPC分类号： C07F15/00
CPC分类号： C07F15/0093
摘要： Disclosed herein are novel platinum-based analogs with a single substituted imine ligand: R7RC=NR8, wherein the R7RC=NR8 functional group is covalently bonded to the platinum through nitrogen. The analogs also have nitrogen donor ligands capable of forming hydrogen bonds with the bases in DNA or RNA, and one or more leaving groups which can be displaced by water, hydroxide ions or other nucleophiles, which is thought to form active species in vivo, and then, form cross-linked complexes between nucleic acid strands, principally between purines in DNA (or RNA), i.e., at the Guanine or Adenine bases, thereof. These platinum analogs may also be more easily transported into tumor cells, due to their increased lipophilicity and are likely to be useful as anti-neoplastic agents, and in modulating or interfering with the synthesis or replication or transcription of DNA or translation or function of RNA in vitro or in vivo, as they are potentially capable of forming a platinum coordinate complex with a intact or nascent DNA or RNA and thereby interfering with cellular synthesis, transcription or replication of nucleic acid polynucleotides.
摘要翻译： 本文公开了具有单个取代的亚胺配体的新型铂基类似物：R7RC = NR8，其中R7RC = NR8官能团通过氮共价键合至铂。 类似物还具有能够与DNA或RNA中的碱基形成氢键的氮供体配体和可以被水，氢氧根离子或其他亲核试剂取代的一个或多个离去基团，其被认为在体内形成活性物质，并且 然后在核酸链之间形成交联复合物，主要是在DNA（或RNA）中的嘌呤，即在其鸟嘌呤或腺嘌呤碱基之间。 这些铂类似物由于它们的亲脂性增加也可以更容易地转运到肿瘤细胞中，并且可能用作抗肿瘤剂，并且调节或干扰DNA的合成或复制或转录或RNA的翻译或功能 因为它们可能与完整或新生的DNA或RNA形成铂配位络合物，从而干扰核酸多核苷酸的细胞合成，转录或复制。
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