-
公开(公告)号：US20080194680A1
公开(公告)日：2008-08-14
申请号：US11978818
申请日：2007-10-30
IPC分类号： A61K31/282 , C07F15/00 , 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。
-
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。
-
公开(公告)号：US07687497B2
公开(公告)日：2010-03-30
申请号：US11974756
申请日：2007-10-16
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）。
-
公开(公告)号：US20090099224A1
公开(公告)日：2009-04-16
申请号：US11974754
申请日：2007-10-16
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）。
-
公开(公告)号：US07687496B2
公开(公告)日：2010-03-30
申请号：US11974754
申请日：2007-10-16
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）在体外具有抑制人和动物肿瘤细胞生长的有效的抗肿瘤活性（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）。
-
公开(公告)号：US20090099166A1
公开(公告)日：2009-04-16
申请号：US11974756
申请日：2007-10-16
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）。
-
7.发明申请Compounds and methods for reducing undesired toxicity of chemotherapeutic agents 审中-公开用于减少化学治疗剂不期望的毒性的化合物和方法公开(公告)号：US20050256055A1
公开(公告)日：2005-11-17
申请号：US10843930
申请日：2004-05-12
申请人： Frederick Hausheer , Harry Kochat , Qiuli Huang
发明人： Frederick Hausheer , Harry Kochat , Qiuli Huang
摘要： Novel compositions and formulations are disclosed that have use as toxicity-reducing agents for various chemotherapeutic agents and as treatment for certain diseases and conditions. The compositions of matter are amino acid and peptide heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium.
摘要翻译： 公开了作为各种化学治疗剂的毒性还原剂和某些疾病和病症治疗的新型组合物和制剂。 物质的组成是2-巯基乙磺酸钠的氨基酸和肽杂合二硫化物。
-
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 。
-
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。
-
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。
-
-
-
-
-
-
-
-
-
搜索结果
15 条记录 (耗时 0.03 秒)
