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1. 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

2. 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.

3. 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。

4. 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。

5. 发明授权

US07687497B2 C10-substituted camptothecin analogs 有权
标题翻译： C10取代的喜树碱类似物
公开(公告)号：US07687497B2
公开(公告)日：2010-03-30
申请号：US11974756
申请日：2007-10-16
申请人： Kesavaram Narkunan , Xinghai Chen , Harry Kochat , Frederick Hausheer
发明人： Kesavaram Narkunan , Xinghai Chen , Harry Kochat , Frederick Hausheer
IPC分类号： A61K31/4375 , A61K31/5377 , A61P35/00 , C07F7/10
CPC分类号： C07F7/0812 , A61K31/4375 , A61K31/5377
摘要： The novel C10-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW
摘要翻译：本发明的新颖的C10修饰的喜树碱类似物及其药学上可接受的盐：（i）具有有效的抗肿瘤活性（即纳米摩尔或亚纳摩尔浓度），用于在体外抑制人和动物肿瘤细胞的生长; （ii）是拓扑异构酶I的有效抑制; （iii）对MDR / MRP耐药性不敏感; （iv）不需要代谢药物活化：（v）缺乏A环或B环的葡糖醛酸化; （vi）降低与血浆蛋白质的药物结合亲和力; （vii）维持内酯稳定性; （viii）维持药物效力; 和（ix）具有低分子量（例如MW <600）。

6. 发明申请

US20070135519A1 Chemoprotective methods and compositions 失效
标题翻译：化学保护方法和组合物
公开(公告)号：US20070135519A1
公开(公告)日：2007-06-14
申请号：US11638193
申请日：2006-12-13
申请人： Frederick Hausheer
发明人： Frederick Hausheer
IPC分类号： A61K31/255 , A61K31/185
CPC分类号： A61K31/185 , A61K31/255
摘要： Compositions and methods for reducing, preventing, mitigating, and/or delaying the onset of, attenuating the severity of, and/or hastening the resolution of, for example, one or more chemotherapy-associated toxicities in a subject receiving one or more chemotherapeutic agents.
摘要翻译：用于减少，预防，减轻和/或延缓接受一种或多种化学治疗剂的受试者中例如一种或多种化疗相关毒性的分解的减轻，和/或促进其分解的组合物和方法。

7. 发明授权

US07777060B2 Platinum analogs with bis-nitrile-containing ligands 有权
标题翻译：含双腈配体的铂类似物
公开(公告)号：US07777060B2
公开(公告)日：2010-08-17
申请号：US11978818
申请日：2007-10-30
申请人： Xinghai Chen , Pavankumar N. V. Petluru , Qiuli Huang , Kesavaram Narkunan , Frederick Hausheer
发明人： Xinghai Chen , Pavankumar N. V. Petluru , Qiuli Huang , Kesavaram Narkunan , Frederick Hausheer
IPC分类号： C07F15/00 , A61K31/282 , A61P35/00
CPC分类号： C07F15/0093
摘要： Disclosed herein are novel platinum-based analogs possessing two nitrile substituent groups (bis-nitrile) covalently-bonded to the platinum. Also disclosed herein are the reaction schemes for the synthesis of said platinum complexes, as well as quantitative in vitro IC50 data.
摘要翻译：本文公开了具有共价键合到铂上的两个腈取代基（双腈）的新型铂基类似物。本文还公开了用于合成所述铂络合物的反应方案以及体外定量IC50数据。

8. 发明申请

US20090099224A1 C7- substituted camptothecin analogs 有权
标题翻译： C7-取代的喜树碱类似物
公开(公告)号：US20090099224A1
公开(公告)日：2009-04-16
申请号：US11974754
申请日：2007-10-16
申请人： Kesavaram Narkunan , Xinghai Chen , Harry Kochat , Frederick Hausheer
发明人： Kesavaram Narkunan , Xinghai Chen , Harry Kochat , Frederick Hausheer
IPC分类号： A61K31/4375 , A61P35/00 , C07F7/10
CPC分类号： C07F7/0812 , A61K31/4375
摘要： The novel C7-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW
摘要翻译：本发明的新颖的C7-改性的喜树碱类似物及其药学上可接受的盐：（i）具有用于在体外抑制人和动物肿瘤细胞生长的有效抗肿瘤活性（即纳摩尔或亚纳摩尔浓度）（ii）是拓扑异构酶I的有效抑制; （iii）对MDR / MRP耐药性不敏感; （iv）不需要代谢药物活化：（v）缺乏A环或B环的葡糖醛酸化; （vi）降低与血浆蛋白质的药物结合亲和力; （vii）维持内酯稳定性; （viii）维持药物效力; 和（ix）具有低分子量（例如MW <600）。

9. 发明申请

US20060094692A1 Pharmaceutical formulations of camptothecins and process for making same 审中-公开
标题翻译：喜树碱的药物制剂及其制备方法
公开(公告)号：US20060094692A1
公开(公告)日：2006-05-04
申请号：US10976203
申请日：2004-10-28
申请人： Frederick Hausheer , Jianyan Wang , Harry Kochat
发明人： Frederick Hausheer , Jianyan Wang , Harry Kochat
IPC分类号： A61K31/695 , A61K31/4745
CPC分类号： A61K31/4745 , A61K9/0019 , A61K31/695 , A61K47/10 , A61K47/12 , A61K47/16 , A61K47/26 , A61K47/34
摘要： This invention relates to pharmaceutically elegant formulations of highly lipophilic camptothecin derivatives.
摘要翻译：本发明涉及高亲脂性喜树碱衍生物的药学上优雅的制剂。

10. 发明申请

US20060063742A1 Method of treatment for or protection against lymphedema 审中-公开
标题翻译：治疗或防止淋巴水肿的方法
公开(公告)号：US20060063742A1
公开(公告)日：2006-03-23
申请号：US10945754
申请日：2004-09-21
申请人： Frederick Hausheer
发明人： Frederick Hausheer
IPC分类号： A61K31/66 , A61K31/185
CPC分类号： A61K31/185 , A61K31/66
摘要： A method of reducing the risks of lymphedema, particularly secondary lymphedema associated with surgery or radiotherapy is disclosed. The method of this invention includes administering effective amounts of specific sulfur-containing drug agents according to Formula I herein to a patient at risk of developing lymphedema.
摘要翻译：公开了减少淋巴水肿风险的方法，特别是与手术或放射疗法相关的继发淋巴水肿。本发明的方法包括向具有发展淋巴水肿风险的患者施用有效量的本发明式I的特定含硫药物。

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