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1. 发明申请

US20070004697A1 Monoimine ligand platinum analogs 有权
标题翻译：单配体铂类似物
公开(公告)号：US20070004697A1
公开(公告)日：2007-01-04
申请号：US11340806
申请日：2006-01-26
申请人： Frederick Hausheer , Zejun Xiao , Harry Kochat
发明人： Frederick Hausheer , Zejun Xiao , Harry Kochat
IPC分类号： A61K31/555 , C07F15/00 , A61K31/282
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：本文公开了具有单取代亚胺配体的新型铂基类似物：R 7 RC-NR 8，其中R 7 R RC-NR 官能团通过氮共价键合到铂上。类似物还具有能够与DNA或RNA中的碱形成氢键的氮供体配体，以及被认为在体内形成活性物质的水，氢氧根离子或其它亲核试剂置换的一个或多个离去基团，以及然后，在核酸链之间形成交联的复合物，主要在DNA（或RNA）中的嘌呤之间，即在鸟嘌呤或腺嘌呤碱基上。这些铂类似物也可以更容易地转运到肿瘤细胞中，这是因为它们的亲脂性增加并且可能被用作抗肿瘤剂，并且在调节或干扰DNA的合成或复制或转录或RNA的翻译或功能在体外或体内，因为它们潜在地能够与完整或新生的DNA或RNA形成铂配位复合物，从而干扰核酸多核苷酸的细胞合成，转录或复制。

2. 发明申请

US20070004696A1 Monoazole ligand platinum analogs 失效
标题翻译：单唑配体铂类似物
公开(公告)号：US20070004696A1
公开(公告)日：2007-01-04
申请号：US11340805
申请日：2006-01-26
申请人： Zejun Xiao , Harry Kochat , Frederick Hausheer
发明人： Zejun Xiao , Harry Kochat , Frederick Hausheer
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：本文公开了具有单取代的唑配体的新型铂基类似物：RN-NR 7，其中RN-NR 7官能团通过氮共价键合到铂上的NR 7。类似物还具有能够与DNA或RNA中的碱形成氢键的氮供体配体，以及被认为在体内形成活性物质的水，氢氧根离子或其它亲核试剂置换的一个或多个离去基团，以及然后，在核酸链之间形成交联的复合物，主要在DNA（或RNA）中的嘌呤之间，即在鸟嘌呤或腺嘌呤碱基上。这些铂类似物也可以更容易地转运到肿瘤细胞中，这是因为它们的亲脂性增加并且可能被用作抗肿瘤剂，并且在调节或干扰DNA的合成或复制或转录或RNA的翻译或功能在体外或体内，因为它们潜在地能够与完整或新生的DNA或RNA形成铂配位复合物，从而干扰核酸多核苷酸的细胞合成，转录或复制。

3. 发明授权

US07268244B2 Monoimine ligand platinum analogs 有权
公开(公告)号：US07268244B2
公开(公告)日：2007-09-11
申请号：US11340806
申请日：2006-01-26
申请人： Frederick H. Hausheer , Zejun Xiao , Harry Kochat
发明人： Frederick H. Hausheer , Zejun Xiao , Harry Kochat
IPC分类号： C07F15/00 , A61K31/28
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.

4. 发明授权

US07759488B2 Monoazole ligand platinum analogs 失效
标题翻译：单唑配体铂类似物
公开(公告)号：US07759488B2
公开(公告)日：2010-07-20
申请号：US11340805
申请日：2006-01-26
申请人： Zejun Xiao , Harry Kochat , Frederick H. Hausheer
发明人： Zejun Xiao , Harry Kochat , Frederick H. Hausheer
IPC分类号： C07F15/00 , A61K31/555 , A61P31/00 , A61P35/00
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：本文公开了具有单取代的唑配体的新型铂基类似物：RN = NR7，其中RN = NR7官能团通过NR7的氮与铂共价结合。类似物还具有能够与DNA或RNA中的碱形成氢键的氮供体配体，以及被认为在体内形成活性物质的水，氢氧根离子或其它亲核试剂置换的一个或多个离去基团，以及然后，在核酸链之间形成交联的复合物，主要在DNA（或RNA）中的嘌呤之间，即在鸟嘌呤或腺嘌呤碱基上。这些铂类似物也可以更容易地转运到肿瘤细胞中，这是因为它们的亲脂性增加并且可能被用作抗肿瘤剂，并且在调节或干扰DNA的合成或复制或转录或RNA的翻译或功能在体外或体内，因为它们潜在地能够与完整或新生的DNA或RNA形成铂配位复合物，从而干扰核酸多核苷酸的细胞合成，转录或复制。

5. 发明申请

US20070173485A1 Platinum complexes with mononitrile-containing ligands 失效
标题翻译：铂配合物与含有单腈的配体
公开(公告)号：US20070173485A1
公开(公告)日：2007-07-26
申请号：US11405141
申请日：2006-04-17
申请人： Zejun Xiao , Frederick Hausheer , Pavankumar Petluru
发明人： Zejun Xiao , Frederick Hausheer , Pavankumar Petluru
IPC分类号： A61K31/282 , A61K31/555 , C07F15/00
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 iii 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.
摘要翻译：本文公开了具有与铂共价连接的一个腈取代基（单腈）的新型铂基络合物，能够与DNA或RNA中的碱形成氢键的离子基团（即L

6. 发明申请

US20070004798A1 Platinum complexes with mononitrile-containing ligands 失效
公开(公告)号：US20070004798A1
公开(公告)日：2007-01-04
申请号：US11340048
申请日：2006-01-26
申请人： Zejun Xiao , Frederick Hausheer , Pavankumar Petluru
发明人： Zejun Xiao , Frederick Hausheer , Pavankumar Petluru
IPC分类号： A61K31/282 , C07F15/00
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.

7. 发明授权

US07238823B2 Platinum complexes with mononitrile-containing ligands 失效
标题翻译：铂配合物与含有单腈的配体
公开(公告)号：US07238823B2
公开(公告)日：2007-07-03
申请号：US11340048
申请日：2006-01-26
申请人： Zejun Xiao , Frederick H. Hausheer , Pavankumar Petluru
发明人： Zejun Xiao , Frederick H. Hausheer , Pavankumar Petluru
IPC分类号： C07F15/00 , A61K31/28
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.
摘要翻译：本文公开了具有与铂共价连接的一个腈取代基（单腈）的新型铂基络合物，能够与DNA或RNA中的碱形成氢键的离子基团（即L

8. 发明授权

US07569606B2 Platinum complexes with mononitrile-containing ligands 失效
标题翻译：铂配合物与含有单腈的配体
公开(公告)号：US07569606B2
公开(公告)日：2009-08-04
申请号：US11405141
申请日：2006-04-17
申请人： Zejun Xiao , Frederick H. Hausheer , Pavankumar Petluru
发明人： Zejun Xiao , Frederick H. Hausheer , Pavankumar Petluru
IPC分类号： A61K31/28 , C07F15/00
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 iii 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.
摘要翻译：本文公开了具有与铂共价连接的一个腈取代基（单腈）的新型铂基络合物，能够与DNA或RNA中的碱形成氢键的离子基团（即L1和L2）的一个或多个氮供体配体），其可以体内水解成活性物质，其然后可以在鸟嘌呤或腺嘌呤碱基上与DNA或RNA形成配位加合物。本文还公开了用于合成所述铂络合物的反应方案，以及通过施用药学有效剂量的所述新型铂络合物治疗各种类型的癌症的方法。

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