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1. 发明申请

WO2010080817A2 CARBOHYDRATE-CYCLOPAMINE CONJUGATES AS ANTICANCER AGENTS 审中-公开
标题翻译：碳水化合物 - 环糊精作为反应剂代谢物
公开(公告)号：WO2010080817A2
公开(公告)日：2010-07-15
申请号：PCT/US2010/020240
申请日：2010-01-06
申请人： UTAH STATE UNIVERSITY , CHANG, Cheng Wei T. , GARROSSIAN, Massoud
发明人： CHANG, Cheng Wei T. , GARROSSIAN, Massoud
IPC分类号： C07D491/107 , C07D403/04 , A61K31/4355 , A61P35/00 , A61K31/7028
CPC分类号： C07D491/107
摘要： Various anticancer compounds are disclosed, including a series of carbohydrate-cyclopamine conjugates. These compounds include pyranose, furanose, and mannitol conjugates, linked through a 1,2,3-triazine ring to the nitrogen of cyclopamine. Methods for preparing these compounds, pharmaceutical compositions containing these compounds, and their use as anticancer agents are also disclosed.
摘要翻译：公开了各种抗癌化合物，包括一系列碳水化合物 - 环巴胺共轭物。这些化合物包括通过1,2,3-三嗪环与环巴胺的氮连接的吡喃糖，呋喃糖和甘露糖醇缀合物。还公开了制备这些化合物的方法，含有这些化合物的药物组合物及其作为抗癌剂的用途。

2. 发明申请

WO2009152202A3 NEW AMINOGLYCOSIDES: SYNTHESIS AND USE AS ANTIFUNGALS 审中-公开
标题翻译：新型氨基酸：合成和用作抗菌剂
公开(公告)号：WO2009152202A3
公开(公告)日：2010-04-01
申请号：PCT/US2009046827
申请日：2009-06-10
申请人： CHANG CHENG-WEI T , EVANS C KENT , TAKEMOTO JON Y , UNIV UTAH STATE
发明人： CHANG CHENG-WEI T , EVANS C KENT , TAKEMOTO JON Y
IPC分类号： A01N43/16 , A01P1/00
CPC分类号： A01N43/16 , C07H15/234
摘要： The present invention relates to a novel aminoglycoside analog with the chemical formula 6-O-(6-Deoxy-4-O-n-octyl-a-D-glucopyranosyl)neamine, which exhibits improved antimicrobial and biocidal properties. The compound of the present invention is an analogue of kanamycin B. Also provided are methods of synthesizing and methods of using the compound of the present invention. The compound of the present invention is useful in treating or preventing fungal disease.
摘要翻译：本发明涉及具有化学式6-O-（6-脱氧-4-O-辛基-α-D-吡喃葡萄糖基）奈胺的新型氨基糖苷类似物，其具有改善的抗微生物性和杀生物性。本发明的化合物是卡那霉素B的类似物。还提供了合成方法和使用本发明化合物的方法。本发明的化合物可用于治疗或预防真菌性疾病。

3. 发明申请

WO2010030808A2 NOVEL ANTIBIOTICS AGAINST RESISTANT BACTERIA 审中-公开
标题翻译：抗抗生素的新型抗生素
公开(公告)号：WO2010030808A2
公开(公告)日：2010-03-18
申请号：PCT/US2009056552
申请日：2009-09-10
申请人： CHANG CHENG-WEI T , UNIV UTAH STATE
发明人： CHANG CHENG-WEI T
IPC分类号： A61K31/7036 , A61K31/702 , A61P31/04
CPC分类号： A61K31/702 , A61K31/7036 , C07H15/232 , Y02P20/55
摘要： The present invention is in the technical field of antimicrobials. More particularly, the present invention is in the technical field of aminoglycoside antimicrobials. In one aspect the present invention provides novel methods of synthesizing new classes of antimicrobial aminoglycosides. In a second aspect the present invention also provides two novel aminoglycosides useful as antimicrobials. The present invention relates to novel antibacterial aminoglycoside derivatives that exhibit improved antimicrobial properties. One advantage of the present invention is a facile synthetic protocol for the production of neomycin B derivatives with various modifications at the 5" position, which enables the direct modification of commercially available aminoglycosides using carbamate type protecting groups. Also provided are methods of using the compound of the present invention. The compounds of the present invention are useful in treating or preventing bacterial infection and may be especially useful in the treatment of infections with MRSA and VRE.
摘要翻译：本发明在抗菌药物的技术领域。更具体地说，本发明在氨基糖苷类抗菌药物的技术领域。一方面，本发明提供了合成新类型的抗微生物氨基糖苷类的新方法。在第二方面，本发明还提供了两种用作抗微生物剂的新型氨基糖苷类。本发明涉及具有改善的抗微生物性质的新型抗菌氨基糖苷衍生物。本发明的一个优点是用于生产在5“位上具有各种修饰的新霉素B衍生物的简便的合成方案，其能够使用氨基甲酸酯型保护基团直接修饰市售的氨基糖苷类，还提供了使用化合物本发明的化合物可用于治疗或预防细菌感染，并且可特别用于治疗MRSA和VRE的感染。

4. 发明申请

WO2010080817A3 CARBOHYDRATE-CYCLOPAMINE CONJUGATES AS ANTICANCER AGENTS 审中-公开
标题翻译：碳水化合物 - 环丙胺缀合物作为抗癌剂
公开(公告)号：WO2010080817A3
公开(公告)日：2010-11-25
申请号：PCT/US2010020240
申请日：2010-01-06
申请人： UNIV UTAH STATE , CHANG CHENG WEI T , GARROSSIAN MASSOUD
发明人： CHANG CHENG WEI T , GARROSSIAN MASSOUD
IPC分类号： C07D491/107 , A61K31/4355 , A61K31/7028 , A61P35/00 , C07D403/04
CPC分类号： C07D491/107
摘要： Various anticancer compounds are disclosed, including a series of carbohydrate-cyclopamine conjugates. These compounds include pyranose, furanose, and mannitol conjugates, linked through a 1,2,3-triazine ring to the nitrogen of cyclopamine. Methods for preparing these compounds, pharmaceutical compositions containing these compounds, and their use as anticancer agents are also disclosed.
摘要翻译：公开了各种抗癌化合物，包括一系列碳水化合物 - 环巴胺缀合物。这些化合物包括吡喃糖，呋喃糖和甘露醇结合物，通过1,2,3-三嗪环连接到环巴胺的氮上。还公开了制备这些化合物的方法，含有这些化合物的药物组合物以及它们作为抗癌剂的用途。

5. 发明申请

WO2010030808A3 NOVEL ANTIBIOTICS AGAINST RESISTANT BACTERIA 审中-公开
公开(公告)号：WO2010030808A3
公开(公告)日：2010-03-18
申请号：PCT/US2009/056552
申请日：2009-09-10
申请人： CHANG, Cheng-Wei, T. , UTAH STATE UNIVERSITY
发明人： CHANG, Cheng-Wei, T.
IPC分类号： A61K31/7036 , A61P31/04 , A61K31/702
摘要： The present invention is in the technical field of antimicrobials. More particularly, the present invention is in the technical field of aminoglycoside antimicrobials. In one aspect the present invention provides novel methods of synthesizing new classes of antimicrobial aminoglycosides. In a second aspect the present invention also provides two novel aminoglycosides useful as antimicrobials. The present invention relates to novel antibacterial aminoglycoside derivatives that exhibit improved antimicrobial properties. One advantage of the present invention is a facile synthetic protocol for the production of neomycin B derivatives with various modifications at the 5" position, which enables the direct modification of commercially available aminoglycosides using carbamate type protecting groups. Also provided are methods of using the compound of the present invention. The compounds of the present invention are useful in treating or preventing bacterial infection and may be especially useful in the treatment of infections with MRSA and VRE.

6. 发明申请

WO2009152202A2 NEW AMINOGLYCOSIDES: SYNTHESIS AND USE AS ANTIFUNGALS 审中-公开
标题翻译：新型氨基酸：合成和用作抗菌剂
公开(公告)号：WO2009152202A2
公开(公告)日：2009-12-17
申请号：PCT/US2009/046827
申请日：2009-06-10
申请人： CHANG, Cheng-wei, T. , EVANS, C., Kent , TAKEMOTO, Jon, Y. , UTAH STATE UNIVERSITY
发明人： CHANG, Cheng-wei, T. , EVANS, C., Kent , TAKEMOTO, Jon, Y.
IPC分类号： A01N43/16 , A01P1/00
CPC分类号： A01N43/16 , C07H15/234
摘要： The present invention relates to a novel aminoglycoside analog with the chemical formula 6- O -(6-Deoxy-4- O - n -octyl-α-D-glucopyranosyl)neamine, which exhibits improved antimicrobial and biocidal properties. The compound of the present invention is an analogue of kanamycin B. Also provided are methods of synthesizing and methods of using the compound of the present invention. The compound of the present invention is useful in treating or preventing fungal disease.
摘要翻译：本发明涉及具有化学式6-O-（6-脱氧-4-O-辛基-α-D-吡喃葡萄糖基）奈胺的新型氨基糖苷类似物，其具有改善的抗微生物性和杀生物性。本发明的化合物是卡那霉素B的类似物。还提供了合成方法和使用本发明化合物的方法。本发明的化合物可用于治疗或预防真菌性疾病。

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