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公开(公告)号：US5677286A
公开(公告)日：1997-10-14
申请号：US429941
申请日：1995-04-27
申请人： Brian K. Shull , Clarke Slemon , Masato Koreeda
发明人： Brian K. Shull , Clarke Slemon , Masato Koreeda
摘要： The present invention relates to chemotherapeutic agents, and more particularly, to novel analogs of camptothecin. The camptothecin analogs display increased solubility through the hydrophilicity of added non-ionic sugar substituents. In accordance with the present invention, a member from the class of novel camptothecin analogs is to be delivered in vivo as a chemotherapeutic agent to fight cancer growth in the body.
摘要翻译： 本发明涉及化学治疗剂，更具体地涉及喜树碱的新型类似物。 喜树碱类似物通过添加的非离子糖取代基的亲水性显示增加的溶解度。 根据本发明，来自新兴喜树碱类似物类的成员将作为化学治疗剂在体内递送以抵抗体内的癌症生长。
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公开(公告)号：US6093805A
公开(公告)日：2000-07-25
申请号：US915699
申请日：1997-08-21
CPC分类号： C07H15/18 , C07H15/256 , C07H17/04 , C07J17/005 , C07J9/00 , C07J9/005
摘要： Novel glycosides, especially steroidal and non-steroidal glycosides are provided. The steroidal and non-steroidal glycosides preferably are prepared from aglycons which possess valuable properties such as pharmacological properties. The glycosides are prepared from useful aglycons and possess useful properties which are the same as those of their respective unglycosylated aglycons. The glycosides are provided in acylated and deacylated form. The acylated glycosides after hydrolysis of the acyl groups possess enhanced water solubility properties, as illustrated in the case where the aglycon is acetominophen.
摘要翻译： 提供新的糖苷，特别是甾体和非甾体糖苷。 甾体和非甾体糖苷优选由具有有价值性质如药理学性质的糖苷配制剂制备。 糖苷由有用的糖苷配制而成，具有与它们各自的未糖基化糖苷基相同的有用性质。 糖苷以酰化和脱酰基形式提供。 酰基水解后的酰化糖苷具有增强的水溶性，如糖苷配基是乙酰氨基酚的情况所示。
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公开(公告)号：US5693767A
公开(公告)日：1997-12-02
申请号：US251869
申请日：1994-06-01
CPC分类号： C07H15/18 , C07H15/256 , C07H17/04 , C07J17/005 , C07J9/00 , C07J9/005
摘要： Novel glycosides, especially steroidal and non-steroidal glycosides are provided. The steroidal and non-steroidal glycosides preferably are prepared from aglycons which possess valuable properties such as pharmacological properties. The glycosides are prepared from useful aglycons and possess useful properties which are the same as those of their respective unglycosylated aglycons. The glycosides are provided in acylated and deacylated form. The acylated glycosides after hydrolysis of the acyl groups possess enhanced water solubility properties, as illustrated in the case where the aglycon is acetominophen.
摘要翻译： 提供新的糖苷，特别是甾体和非甾体糖苷。 甾体和非甾体糖苷优选由具有有价值性质如药理学性质的糖苷配制剂制备。 糖苷由有用的糖苷配制而成，具有与它们各自的未糖基化糖苷基相同的有用性质。 糖苷以酰化和脱酰基形式提供。 酰基水解后的酰化糖苷具有增强的水溶性，如糖苷配基是乙酰氨基酚的情况所示。
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公开(公告)号：US5932709A
公开(公告)日：1999-08-03
申请号：US876824
申请日：1997-06-16
申请人： Brian Keith Shull , Clarke Slemon , Masato Koreeda
发明人： Brian Keith Shull , Clarke Slemon , Masato Koreeda
摘要： The present invention relates to chemotherapeutic agents, and more particularly, to novel analogs of camptothecin. The camptothecin analogs display increased solubility through the hydrophilicity of added non-ionic sugar substituents. In accordance with the present invention, a member from the class of novel camptothecin analogs is to be delivered in vivo as a chemotherapeutic agent to fight cancer growth in the body.
摘要翻译： 本发明涉及化学治疗剂，更具体地涉及喜树碱的新型类似物。 喜树碱类似物通过添加的非离子糖取代基的亲水性显示增加的溶解度。 根据本发明，来自新兴喜树碱类似物类的成员将作为化学治疗剂在体内递送以抵抗体内的癌症生长。
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公开(公告)号：US5453500A
公开(公告)日：1995-09-26
申请号：US249492
申请日：1994-05-26
申请人： Masato Koreeda , Brian K. Shull , Wu Yang
发明人： Masato Koreeda , Brian K. Shull , Wu Yang
IPC分类号： C07H15/26 , C07D327/06 , A61K7/035 , A61K31/715 , C07D343/00
CPC分类号： C07H15/26
摘要： Novel water-soluble mono and disaccharides of 1,2-dithiins, as well as methods for their synthesis and the synthesis of 3,6-bis(hydroxymethyl)-1,2-dithiin, are provided. The water-soluble compounds have useful medicinal applications, e.g., as an antifungal agent or antibacterial agent in a pharmaceutically acceptable carrier.
摘要翻译： 提供了1,2-二噻吩的新型水溶性单二糖和二糖，以及它们的合成方法和3,6-双（羟甲基）-1,2-二噻吩的合成。 水溶性化合物具有有用的医学应用，例如在药学上可接受的载体中作为抗真菌剂或抗菌剂。
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公开(公告)号：US6103884A
公开(公告)日：2000-08-15
申请号：US623335
申请日：1996-03-27
摘要： Novel analogs of fusidic acid are described with one or more carbohydrate units attached. Certain glycosylated analogs of fusidic acid have enhanced solubility properties in diluents or excipient of choice as compared to unmodified fusidic acid. Certain glycosylated analogs may be employed as chemotherapeutic agents and particular analogs may be useful for fighting anti-microbial infections.
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公开(公告)号：US06462182B1
公开(公告)日：2002-10-08
申请号：US09616658
申请日：2000-07-14
IPC分类号： C07H1500
摘要： Novel analogs of fusidic acid are described with one or more carbohydrate units attached. Certain glycosylated analogs of fusidic acid have enhanced solubility properties in diluents or excipient of choice as compared to unmodified fusidic acid. Certain glycosylated analogs may be employed as chemotherapeutic agents and particular analogs may be useful for fighting anti-microbial infections.
摘要翻译： 描述了连接一个或多个碳水化合物单元的夫西地酸的新型类似物。 与未修饰的夫西地酸相比，夫西地酸的某些糖基化类似物具有增强的稀释剂或赋形剂的溶解性。 某些糖基化类似物可用作化学治疗剂，特定的类似物可用于抗菌抗感染。
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公开(公告)号：US06720307B2
公开(公告)日：2004-04-13
申请号：US10189242
申请日：2002-07-02
IPC分类号： A61K3170
摘要： Novel analogs of fusidic acid are described with one or more carbohydrate units attached. Certain glycosylated analogs of fusidic acid have enhanced solubility properties in diluents or excipient of choice as compared to unmodified fusidic acid. Certain glycosylated analogs may be employed as chemotherapeutic agents and particular analogs may be useful for fighting anti-microbial infections.
摘要翻译： 描述了连接一个或多个碳水化合物单元的夫西地酸的新型类似物。 与未修饰的夫西地酸相比，夫西地酸的某些糖基化类似物具有增强的稀释剂或赋形剂的溶解性。 某些糖基化类似物可用作化学治疗剂，特定的类似物可用于抗菌感染。
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公开(公告)号：US5668168A
公开(公告)日：1997-09-16
申请号：US470102
申请日：1995-06-06
申请人： Thien V. Truong , Donald E. Bierer , Jeffrey M. Dener , Richard Hector , Michael S. Tempesta , Bernard Loev , Wu Yang , Masato Koreeda
发明人： Thien V. Truong , Donald E. Bierer , Jeffrey M. Dener , Richard Hector , Michael S. Tempesta , Bernard Loev , Wu Yang , Masato Koreeda
IPC分类号： A61K9/12 , A61K31/38 , A61K31/385 , A61P31/04 , A61P31/10 , C07C323/14 , C07C323/16 , C07D339/04 , C07D339/08 , C07C321/06
CPC分类号： C07C323/14 , A61K31/385 , C07D339/04 , C07D339/08
摘要： This invention pertains to a novel group of 1,2-dithiin compounds useful as antiinfective agents, and a novel synthetic process to produce the same. The compounds are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans or Aspergillus fumigatus.
摘要翻译： 本发明涉及可用作抗感染剂的新型1,2-二硫素化合物组合物及其制备方法。 这些化合物特别有效地治疗真菌感染，特别是由白色念珠菌，新型隐球菌或烟曲霉引起的真菌感染。
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公开(公告)号：US5556875A
公开(公告)日：1996-09-17
申请号：US110917
申请日：1995-08-24
申请人： Thien V. Truong , Donald E. Bierer , Jeffrey M. Dener , Richard Hector , Michael S. Tempesta , Bernard Loev , Wu Yang , Masato Koreeda
发明人： Thien V. Truong , Donald E. Bierer , Jeffrey M. Dener , Richard Hector , Michael S. Tempesta , Bernard Loev , Wu Yang , Masato Koreeda
IPC分类号： A61K9/12 , A61K31/38 , A61K31/385 , A61P31/04 , A61P31/10 , C07C323/14 , C07C323/16 , C07D339/04 , C07D339/08
CPC分类号： C07C323/14 , A61K31/385 , C07D339/04 , C07D339/08
摘要： This invention pertains to a novel group of 1,2-dithiin compounds useful as antiinfective agents, and a novel synthetic process to produce the same. The compounds are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans or Aspergillus fumigatus.
摘要翻译： 本发明涉及可用作抗感染剂的新型1,2-二硫素化合物组合物及其制备方法。 这些化合物特别有效地治疗真菌感染，特别是由白色念珠菌，新型隐球菌或烟曲霉引起的真菌感染。
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