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201. 发明申请

US20120270824A1 MANNOSE DERIVATIVES AS ANTAGONISTS OF BACTERIAL ADHESION 审中-公开
标题翻译： MANNOSE衍生物作为细菌粘附的拮抗剂
公开(公告)号：US20120270824A1
公开(公告)日：2012-10-25
申请号：US13515353
申请日：2010-12-13
申请人： Beat Ernst , Janno Herold
发明人： Beat Ernst , Janno Herold
IPC分类号： A61K31/7034 , C07H15/26 , A61P31/04 , C07H15/207
CPC分类号： C07H15/26 , C07H15/18 , C07H15/203 , C07H15/207
摘要： Compounds of the formula (I) wherein n is 0, 1 or 2, R1 is aryl, heteroaryl or heterocyclyl, and R2 and R3 are hydrogen or a substituent as described in the specification, are useful for the prevention and treatment of bacterial infections, in particular of urinary infections caused by E. coli.
摘要翻译：式（I）的化合物，其中n为0,1或2，R 1为芳基，杂芳基或杂环基，R 2和R 3为氢或本说明书所述的取代基，可用于预防和治疗细菌感染，特别是由大肠杆菌引起的尿路感染。

202. 发明申请

US20120003260A1 Solid-Phase and Solution-Phase Synthesis of Glycosylphosphatidylinositol Glycans 审中-公开
标题翻译：固相和溶液相合成糖基磷脂酰肌醇甘氨酸
公开(公告)号：US20120003260A1
公开(公告)日：2012-01-05
申请号：US13109562
申请日：2011-05-17
申请人： Peter H. Seeberger , Michael C. Hewitt , Daniel Snyder
发明人： Peter H. Seeberger , Michael C. Hewitt , Daniel Snyder
IPC分类号： A61K39/385 , A61P37/04 , A61P33/02 , C07H15/207 , C07K17/10
CPC分类号： C08B37/006 , C07H15/203 , C07H15/207
摘要： One aspect of the present invention relates to solution-phase approaches to GPI synthesis. Another aspect of the present invention relates to key building blocks, and syntheses thereof, useful for GPI assembly. Yet another aspect of the invention relates to an automated method for the synthesis of GPIs and fragments thereof.
摘要翻译：本发明的一个方面涉及GPI合成的溶液相方法。本发明的另一方面涉及可用于GPI组装的关键构造块及其合成。本发明的另一方面涉及用于合成GPI及其片段的自动化方法。

203. 发明申请

US20110251148A1 GLYCOMIMETIC COMPOUNDS AND METHODS TO INHIBIT INFECTION BY HIV 审中-公开
标题翻译：糖尿病感染化合物及其抑制方法
公开(公告)号：US20110251148A1
公开(公告)日：2011-10-13
申请号：US13081068
申请日：2011-04-06
申请人： John L. MAGNANI , Arun K. Sarkar
发明人： John L. MAGNANI , Arun K. Sarkar
IPC分类号： A61K31/7056 , A61P31/18 , C07H15/00
CPC分类号： C07H15/207 , A61K47/55 , C07H15/26
摘要： Compounds, compositions and methods are provided for use to inhibit infection by human immunodeficiency virus (HIV). More specifically, the present invention relates to glycomimetic compounds that inhibit HIV infection, and uses thereof.
摘要翻译：提供化合物，组合物和方法用于抑制人免疫缺陷病毒（HIV）的感染。更具体地，本发明涉及抑制HIV感染的糖模拟化合物及其用途。

204. 发明申请

US20110245196A1 NOVEL SULFATED OLIGOSACCHARIDE DERIVATIVES 有权
标题翻译：新型硫化寡糖衍生物
公开(公告)号：US20110245196A1
公开(公告)日：2011-10-06
申请号：US12738552
申请日：2008-10-16
申请人： Vito Ferro , Karoli Tomislav , Liu Ligong , Handley Paul Newton , Johnstone Kenneth David , Norbert Wimmer , Hammond Edward Timothy
发明人： Vito Ferro , Karoli Tomislav , Liu Ligong , Handley Paul Newton , Johnstone Kenneth David , Norbert Wimmer , Hammond Edward Timothy
IPC分类号： A61K31/7016 , C07H13/02 , C07H13/00 , C07J31/00 , A61K31/7024 , A61K31/702 , A61P35/04 , A61P35/00 , A61P29/00 , A61P7/02 , A61P9/00 , A61P31/00 , A61P3/06
CPC分类号： C07J43/003 , C07H3/04 , C07H3/06 , C07H5/02 , C07H5/04 , C07H5/06 , C07H11/00 , C07H15/04 , C07H15/207 , C07H15/24 , C07H15/26 , C07H17/02 , C07J17/005 , C07J31/006 , C07J41/0088 , C07J41/0094
摘要： The invention relates to novel compounds that have utility as inhibitors of heparan sulfate-binding proteins; compositions comprising the compounds, and use of the compounds and compositions thereof for the antiangiogenic, antimetastatic, anti-inflammatory, antimicrobial, anticoagulant and/or antithrombotic treatment of a mammalian subject.
摘要翻译：本发明涉及可用作硫酸乙酰肝素结合蛋白的抑制剂的新型化合物; 包含该化合物的组合物，以及该化合物及其组合物用于哺乳动物受试者的抗血管生成，抗转移，抗炎，抗微血管和/或抗血栓形成治疗的用途。

205. 发明授权

US07375213B2 Methods of producing C-aryl glucoside SGLT2 inhibitors 有权
标题翻译：生产C-芳基葡萄糖苷SGLT2抑制剂的方法
公开(公告)号：US07375213B2
公开(公告)日：2008-05-20
申请号：US10745075
申请日：2003-12-23
申请人： Prashant P. Deshpande , Bruce A. Ellsworth , Janak Singh , Theodor W. Denzel , Chiajen Lai , Gerard Crispino , Michael E. Randazzo , Jack Z. Gougoutas
发明人： Prashant P. Deshpande , Bruce A. Ellsworth , Janak Singh , Theodor W. Denzel , Chiajen Lai , Gerard Crispino , Michael E. Randazzo , Jack Z. Gougoutas
IPC分类号： C07H15/203 , C07H15/20 , C07H1/00
CPC分类号： C07H23/00 , C07H5/04 , C07H5/06 , C07H7/00 , C07H15/207
摘要： Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.
摘要翻译：生产用于治疗糖尿病和相关疾病的C-芳基葡萄糖苷SGLT2抑制剂的方法。及其中间体。 C-芳基葡糖苷可以与形成氨基酸复合物的试剂络合。

206. 发明授权

US07348309B2 Glycorandomization and production of novel vancomycin analogs 有权
标题翻译：新型万古霉素类似物的糖配合和生产
公开(公告)号：US07348309B2
公开(公告)日：2008-03-25
申请号：US10670073
申请日：2003-09-24
申请人： Jon Thorson
发明人： Jon Thorson
IPC分类号： A61K38/16
CPC分类号： C07H1/00 , C07H15/207 , C07H15/22 , C07H17/08
摘要： The present invention provides combinatorial methods for rapidly generating a diverse library of glycorandomized structures, comprising incubating one or more aglycons and a pool of NDP-sugars in the presence of a glycosyltransferase. The glycosyltransferase may be one that is associated with or involved in production of natural secondary metabolites, or one which is putatively associated with or involved in production of natural secondary metabolites. The glycosyltransferase may show significant flexibility with respect to its NDP-sugar donors and/or its aglycons. NDP-sugar donors may be commercially available, or may be produced by utilizing mutant or wild type nucleotidyltransferases significant flexibility with respect to their substrates.
摘要翻译：本发明提供用于快速产生多糖文库结构的组合方法，其包括在糖基转移酶存在下孵育一种或多种糖苷和一组NDP-糖。糖基转移酶可以是与天然次生代谢产物相关或参与生产天然次生代谢产物，或与天然次生代谢产物相关或参与生产天然次生代谢产物相关或相关的糖基转移酶。糖基转移酶对于其NDP-糖供体和/或其糖苷酸可显示出显着的灵活性。 NDP-糖供体可以是可商购的，或者可以通过利用相对于其底物具有显着柔性的突变体或野生型核苷酸转移酶来产生。

207. 发明申请

US20070238866A1 METHODS OF PRODUCING C-ARYL GLUCOSIDE SGLT2 INHIBITORS 有权
标题翻译：生产C-ARYL GLUCOSIDE SGLT2抑制剂的方法
公开(公告)号：US20070238866A1
公开(公告)日：2007-10-11
申请号：US11764839
申请日：2007-06-19
申请人： Prashant Deshpande , Bruce Ellsworth , Janak Singh , Theodor Denzel , Chiajen Lai , Gerard Crispino , Michael Randazzo , Jack Gougoutas
发明人： Prashant Deshpande , Bruce Ellsworth , Janak Singh , Theodor Denzel , Chiajen Lai , Gerard Crispino , Michael Randazzo , Jack Gougoutas
IPC分类号： C07H15/20 , A61K31/70
CPC分类号： C07H23/00 , C07H5/04 , C07H5/06 , C07H7/00 , C07H15/207
摘要： Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.
摘要翻译：生产用于治疗糖尿病和相关疾病的C-芳基葡萄糖苷SGLT2抑制剂的方法。及其中间体。 C-芳基葡糖苷可以与形成氨基酸复合物的试剂络合。

208. 发明申请

US20070207986A1 Inositol pyrophosphates, and methods of use thereof 失效
标题翻译：肌醇焦磷酸盐及其使用方法
公开(公告)号：US20070207986A1
公开(公告)日：2007-09-06
申请号：US11600685
申请日：2006-11-16
申请人： Yves Nicolau , Jean-Marie Lehn , Konstantina Fylaktakidou , Ruth Greferath
发明人： Yves Nicolau , Jean-Marie Lehn , Konstantina Fylaktakidou , Ruth Greferath
IPC分类号： A61K31/6615 , G01N33/72
CPC分类号： A61K31/6615 , A61K31/66 , A61K31/70 , A61K31/715 , A61K35/18 , C07F9/117 , C07F9/65746 , C07H15/207 , C12N5/0641
摘要： The present invention comprises compounds, compositions thereof, and methods capable of delivering modified inositol hexaphosphate (IHP) comprising an internal pyrophosphate ring to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.
摘要翻译：本发明包括化合物，其组合物和能够将包含内部焦磷酸盐环的修饰的肌醇六磷酸（IHP）递送至哺乳动物细胞的细胞质的方法。在某些实施方案中，本发明涉及通过将IHP递送至红细胞的细胞质来增强哺乳动物红细胞传递氧的能力的化合物，其组合物和方法。

209. 发明申请

US20060089330A1 Solid-phase and solution-phase synthesis of glycosylphosphatidylinositol glycans 有权
标题翻译：糖基磷脂酰肌醇聚糖的固相和溶液相合成
公开(公告)号：US20060089330A1
公开(公告)日：2006-04-27
申请号：US10520963
申请日：2003-07-10
申请人： Peter Seeberger , Michael Hewitt
发明人： Peter Seeberger , Michael Hewitt
IPC分类号： C08B37/00 , A61K31/715
CPC分类号： C08B37/006 , C07H15/203 , C07H15/207
摘要： One aspect of the present invention relates to solution-phase approaches to GPI synthesis. Another aspect of the present invention relates to key building blocks, and syntheses thereof, useful for GPI assembly. Yet another aspect of the invention relates to an automated method for the synthesis of GPIs and fragments thereof.
摘要翻译：本发明的一个方面涉及GPI合成的溶液相方法。本发明的另一方面涉及可用于GPI组装的关键构造块及其合成。本发明的另一方面涉及用于合成GPI及其片段的自动化方法。

210. 发明授权

US06884604B2 Glycorandomization and the production of novel erythronolide and coumarin analogs 有权
标题翻译： Glycoronomide和香豆素类似物的生物学研究
公开(公告)号：US06884604B2
公开(公告)日：2005-04-26
申请号：US10109672
申请日：2002-04-01
申请人： Jon S. Thorson
发明人： Jon S. Thorson
IPC分类号： C07H1/00 , C07H15/203 , C07H17/08 , C12N15/54 , C12P19/18 , C12P19/30
CPC分类号： C07H15/207 , C07H1/00 , C07H15/22 , C07H17/08
摘要： The present invention provides combinatorial methods for rapidly generating a diverse library of glycorandomized structures, comprising incubating one or more aglycons and a pool of NDP-sugars in the presence of a glycosyltransferase. The glycosyltransferase may be one that is associated with or involved in production of natural secondary metabolites, or one which is putatively associated with or involved in production of natural secondary metabolites. The glycosyltransferase may show significant flexibility with respect to its NDP-sugar donors and/or its aglycons. NDP-sugar donors may be commercially available, or may be produced by utilizing mutant or wild type nucleotidyltransferases significant flexibility with respect to their substrates.
摘要翻译：本发明提供了用于快速产生多糖文库结构的组合方法，包括在糖基转移酶存在下孵育一种或多种糖苷和一组NDP-糖。糖基转移酶可以是与天然次生代谢产物相关或参与生产天然次生代谢产物，或与天然次生代谢产物相关或参与生产天然次生代谢产物相关或相关的糖基转移酶。糖基转移酶对于其NDP-糖供体和/或其糖苷酸可显示出显着的灵活性。 NDP-糖供体可以是可商购的，或者可以通过利用相对于其底物具有显着柔性的突变体或野生型核苷酸转移酶来产生。

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