专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明专利

IL237309D0 Benzocyclooctyne compounds and uses thereof 未知
公开(公告)号：IL237309D0
公开(公告)日：2015-04-30
申请号：IL23730915
申请日：2015-02-19
申请人： ACADEMIA SINICA , CHI HUEY WONG , JIM MIN FANG , JIUN JIE SHIE
IPC分类号： C07D20060101

2. 发明申请

US20100113397A1 SYNTHESIS OF OSELTAMIVIR CONTAINING PHOSPHONATE CONGENERS WITH ANTI-INFLUENZA ACTIVITY 有权
标题翻译：含有抗感染活性的含有磷酸肌酸钠的奥沙利铂的合成
公开(公告)号：US20100113397A1
公开(公告)日：2010-05-06
申请号：US12201955
申请日：2008-08-29
申请人： Chi-Huey Wong , Jim-Min Fang , Jiun-Jie Shie , Yih-Shyun Edmond Cheng , Jia-Tsrong Jan
发明人： Chi-Huey Wong , Jim-Min Fang , Jiun-Jie Shie , Yih-Shyun Edmond Cheng , Jia-Tsrong Jan
IPC分类号： A61K31/66 , A61P31/16 , C07F9/02
CPC分类号： A61K31/70 , A61K31/7076
摘要： Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to known neuraminidase inhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novel phosphonate compounds, via D-xylose. Another efficient and flexible synthesis of Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was also achieved in 11 steps and >20% overall yields from the readily available fermentation product (1S-cis)-3-bromo-3,5-cyclohexadiene-1,2-diol. Most of the reaction intermediates were obtained as crystals without tedious purification procedures. The key transformations include an initial regio- and stereoselective bromoamidation of a bromoarene cis-dihydrodiol, as well as the final palladium-catalyzed carbonylation and phosphonylation.
摘要翻译：描述了新的膦酸酯化合物。该化合物具有作为抗H1N1和H5N1病毒野生型和H274Y突变体的神经氨酸酶抑制剂的活性。本公开还提供了通过D-木糖对已知的神经氨酸酶抑制剂奥司他韦和抗流感药物Tamiflu以及新的膦酸酯化合物的对映选择性合成途径。 Tamiflu和高效神经氨酸酶抑制剂Tamiphosphor的另一种有效和灵活的合成还通过11个步骤实现，并且来自容易获得的发酵产物（1S-顺式）-3-溴-3,5-环己二烯-1的总收率> 20％ 2-二醇。大多数反应中间体是以晶体形式获得，而不需要繁琐的纯化程序。关键转化包括溴芳烃顺式 - 二氢二醇的初始区域和立体选择性溴酰胺化，以及最终的钯催化羰基化和膦酰化反应。

3. 发明授权

US09403855B2 Zanamivir phosphonate congeners with anti-influenza activity and determining oseltamivir susceptibility of influenza viruses 有权
标题翻译：具有抗流感活性的Zanamivir膦酸酯同系物并测定流感病毒的奥司他韦敏感性
公开(公告)号：US09403855B2
公开(公告)日：2016-08-02
申请号：US13697794
申请日：2011-05-10
申请人： Chi-Huey Wong , Jim-Min Fang , Yih-Shyun Edmund Cheng , Jiun-Jie Shie
发明人： Chi-Huey Wong , Jim-Min Fang , Yih-Shyun Edmund Cheng , Jiun-Jie Shie
IPC分类号： C07D309/28 , C07F9/655 , G01N33/569 , A61K31/665 , A61K31/683
CPC分类号： G01N33/56983 , A61K31/665 , A61K31/683 , C07F9/6552 , G01N2333/11
摘要： Methods and compositions for detection of drug resistant pathogens and treatment against infections thereof are provided. Methods for detection of oseltamivir-resistant influenza viruses by competitive binding assays utilizing non-oseltamivir influenza virus neuraminidase inhibitors and oseltamivir carboxylate are provided. Influenza virus neuraminidase inhibitors coupled to sensors and useful for employment in the methods of the invention are disclosed. Novel phosphonate compounds active as neuraminidase inhibitors against wild-type and oseltamivir-resistant influenza strains of H1N1, H5N1 and H3N2 viruses are disclosed. An enantioselective synthetic route to preparation of these phosphonate compounds via sialic acid is provided.
摘要翻译：提供了用于检测耐药性病原体的方法和组合物以及对其感染的治疗。提供了通过使用非奥司他韦流感病毒神经氨酸酶抑制剂和奥司他韦羧酸酯的竞争性结合测定法检测奥司他韦抗性流感病毒的方法。公开了耦合到传感器并且可用于本发明方法中的流感病毒神经氨酸酶抑制剂。公开了作为抗H1N1，H5N1和H3N2病毒的野生型和奥司他韦抗性流感病毒株的神经氨酸酶抑制剂活性的新型膦酸酯化合物。提供了通过唾液酸制备这些膦酸酯化合物的对映选择性合成途径。

4. 发明申请

US20130225532A1 ZANAMIVIR PHOSPHONATE CONGENERS WITH ANTI-INFLUENZA ACTIVITY AND DETERMINING OSELTAMIVIR SUSCEPTIBILITY OF INFLUENZA VIRUSES 有权
标题翻译：具有抗流感病毒活性的ZAMAMIVIR磷酸盐浓缩物，并确定了OSELTAMIVIR流感病毒的易感性
公开(公告)号：US20130225532A1
公开(公告)日：2013-08-29
申请号：US13697794
申请日：2011-05-10
申请人： Chi-Huey Wong , Jim-Min Fang , Yih-Shyun Edmund Cheng , Jiun-Jie Shie
发明人： Chi-Huey Wong , Jim-Min Fang , Yih-Shyun Edmund Cheng , Jiun-Jie Shie
IPC分类号： C07F9/655
CPC分类号： G01N33/56983 , A61K31/665 , A61K31/683 , C07F9/6552 , G01N2333/11
摘要： Methods and compositions for detection of drug resistant pathogens and treatment against infections thereof are provided. Methods for detection of oseltamivir-resistant influenza viruses by competitive binding assays utilizing non-oseltamivir influenza virus neuraminidase inhibitors and oseltamivir carboxylate are provided. Influenza virus neuraminidase inhibitors coupled to sensors and useful for employment in the methods of the invention are disclosed. Novel phosphonate compounds active as neuraminidase inhibitors against wild-type and oseltamivir-resistant influenza strains of H1N1, H5N1 and H3N2 viruses are disclosed. An enantioselective synthetic route to preparation of these phosphonate compounds via sialic acid is provided.
摘要翻译：提供了用于检测耐药性病原体的方法和组合物以及对其感染的治疗。提供了通过使用非奥司他韦流感病毒神经氨酸酶抑制剂和奥司他韦羧酸酯的竞争性结合测定法检测奥司他韦抗性流感病毒的方法。公开了耦合到传感器并且可用于本发明方法中的流感病毒神经氨酸酶抑制剂。公开了作为抗H1N1，H5N1和H3N2病毒的野生型和奥司他韦抗性流感病毒株的神经氨酸酶抑制剂活性的新型膦酸酯化合物。提供了通过唾液酸制备这些膦酸酯化合物的对映选择性合成途径。

5. 发明授权

US07888337B2 Synthesis of oseltamivir containing phosphonate congeners with anti-influenza activity 有权
标题翻译：含有具有抗流感活性的膦酸酯同系物的奥司他韦的合成
公开(公告)号：US07888337B2
公开(公告)日：2011-02-15
申请号：US12201955
申请日：2008-08-29
申请人： Chi-Huey Wong , Jim-Min Fang , Jiun-Jie Shie , Yih-Shyun Edmond Cheng , Jia-Tsrong Jan
发明人： Chi-Huey Wong , Jim-Min Fang , Jiun-Jie Shie , Yih-Shyun Edmond Cheng , Jia-Tsrong Jan
IPC分类号： A61K31/66
CPC分类号： A61K31/70 , A61K31/7076
摘要： Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to known neuraminidase inhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novel phosphonate compounds, via D-xylose. Another efficient and flexible synthesis of Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was also achieved in 11 steps and >20% overall yields from the readily available fermentation product (1S-cis)-3-bromo-3,5 -cyclohexadiene-1,2-diol. Most of the reaction intermediates were obtained as crystals without tedious purification procedures. The key transformations include an initial regio- and stereoselective bromoamidation of a bromoarene cis-dihydrodiol, as well as the final palladium-catalyzed carbonylation and phosphonylation.
摘要翻译：描述了新的膦酸酯化合物。该化合物具有作为抗H1N1和H5N1病毒野生型和H274Y突变体的神经氨酸酶抑制剂的活性。本公开还提供了通过D-木糖对已知的神经氨酸酶抑制剂奥司他韦和抗流感药物Tamiflu以及新的膦酸酯化合物的对映选择性合成途径。 Tamiflu和高效神经氨酸酶抑制剂Tamiphosphor的另一种有效和灵活的合成还通过11个步骤实现，并且来自容易获得的发酵产物（1S-顺式）-3-溴-3,5-环己二烯-1的总收率> 20％ 2-二醇。大多数反应中间体是以晶体形式获得，而不需要繁琐的纯化程序。关键转化包括溴芳烃顺式 - 二氢二醇的初始区域和立体选择性溴酰胺化，以及最终的钯催化羰基化和膦酰化反应。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式