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151. 发明授权

US09078908B2 Inositol pyrophosphates, and methods of use thereof 有权
公开(公告)号：US09078908B2
公开(公告)日：2015-07-14
申请号：US13923023
申请日：2013-06-20
申请人： NormOxys, Inc.
发明人： Yves Claude Nicolau , Jean-Marie Lehn , Konstantina C. Fylaktakidou , Ruth Greferath
IPC分类号： A61K31/66 , A61K31/70 , A61K35/18 , C07F9/117 , A61K31/6615 , A61K31/715 , C07F9/6574 , C07H15/207 , C12N5/078
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 hexaphospahte (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.

152. 发明申请

US20140200190A1 NOVEL GALACTOSIDE INHIBITORS OF GALECTINS 审中-公开
标题翻译： GALECTINS的新型糖皮质激素抑制剂
公开(公告)号：US20140200190A1
公开(公告)日：2014-07-17
申请号：US14215771
申请日：2014-03-17
申请人： Galecto Biotech AB
发明人： Hakon LEFFLER , Ulf J. NILSSON , Henrik VON WACHENFELDT
IPC分类号： C07H15/207
CPC分类号： C07H15/207 , C07H15/22 , C07H19/056
摘要： Compounds having an effect as i.a. galectin inhibitors, to the use of said compounds as a medicament, as well as for the manufacture of a medicament for treatment of disorders relating to the binding of galectin to receptors in a mammal, wherein the galectin is preferably a galectin-3. The novel compounds are defined by the general formula:
摘要翻译：化合物具有如i.a. 半乳凝素抑制剂，所述化合物用作药物，以及用于制备用于治疗与半乳凝素与哺乳动物中的受体结合相关的病症的药物，其中半乳凝素优选为半乳凝素-3。新化合物由以下通式定义：

153. 发明申请

US20140073594A1 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：US20140073594A1
公开(公告)日：2014-03-13
申请号：US14080926
申请日：2013-11-15
申请人： GlycoMimetics, Inc.
发明人： John L. Magnani , Arun K. Sarkar
IPC分类号： C07H15/207
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。

154. 发明授权

US08618269B2 Glycorandomization and production of novel novobiocin analogs 有权
标题翻译：新型新生霉素类似物的糖配合和生产
公开(公告)号：US08618269B2
公开(公告)日：2013-12-31
申请号：US13448811
申请日：2012-04-17
申请人： Jon Thorson
发明人： Jon Thorson
IPC分类号： C07H17/08 , C07G11/00 , C07H15/00 , C07H17/00 , A01N43/04 , A61K31/70
CPC分类号： C07H1/00 , C07H15/207 , C07H15/22 , C07H17/08
摘要： The present invention provides glycorandomized structures and 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化结构化文库的多糖结构和组合方法，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。

155. 发明申请

US20130274210A1 DENDRIMERS WITH A SACCHARIDE ENDING FOR ANTI-INFLAMMATORY PURPOSES 审中-公开
标题翻译：具有抗炎炎症目的的杀菌剂
公开(公告)号：US20130274210A1
公开(公告)日：2013-10-17
申请号：US13819872
申请日：2011-08-31
申请人： Jacques Prandi , Germain Puzo , Cédric-Olivier Turrin , Emilyne Blattes , Alain Vercellone , Jérôme Nigou , Jean-Pierre Majoral , Anne-Marie Caminade
发明人： Jacques Prandi , Germain Puzo , Cédric-Olivier Turrin , Emilyne Blattes , Alain Vercellone , Jérôme Nigou , Jean-Pierre Majoral , Anne-Marie Caminade
IPC分类号： C07H15/207
CPC分类号： C07H15/207 , C07H15/04 , C07H15/18 , C08G79/04 , C08G83/003
摘要： The present invention relates to dendrimers with a monosaccharide, oligosaccharide or polysaccharide terminal group, to their preparation method and their therapeutic uses, notably anti-inflammatory uses.
摘要翻译：本发明涉及具有单糖，寡糖或多糖末端基团的树枝状大分子，其制备方法及其治疗用途，特别是抗炎用途。

156. 发明申请

US20130157968A1 COSMETIC COMPOSITION 有权
标题翻译：化妆品组合物
公开(公告)号：US20130157968A1
公开(公告)日：2013-06-20
申请号：US13639997
申请日：2011-04-14
申请人： Charlotte Simmler , Virginie Leplanquais , Emmanuelle Noblesse , Patrice Andre , Annelise Lobstein
发明人： Charlotte Simmler , Virginie Leplanquais , Emmanuelle Noblesse , Patrice Andre , Annelise Lobstein
IPC分类号： A61K8/60 , C07H1/08 , A61Q19/08 , C07H15/207
CPC分类号： A61K8/602 , A61K8/498 , A61K31/7034 , A61Q19/08 , C07H1/08 , C07H15/203 , C07H15/207
摘要： The invention relates to novel eucomic acid (2-(4-hydroxybenzyl)malic acid) derivatives or plant extracts comprising such derivatives, and also to cosmetic or dermatological compositions containing these compounds or these extracts, and to cosmetic care methods using said compositions. Exemplary compounds are represented by formula (I) below: in which, with the proviso that R1, R2 and R3 are not simultaneously a hydrogen atom, R1 and R3 each independently represent a hydrogen atom or a saturated or unsaturated, preferably C1-C12, hydrocarbon-based chain comprising an aromatic group, preferably a phenyl, said aromatic group being preferably substituted with a group comprising a sugar, preferably a monosaccharide or disaccharide, said chain optionally also comprising one or more heteroatoms preferably chosen from O, S and N, and R2 represents a hydrogen atom or a sugar, preferably a monosaccharide or disaccharide, said sugar being optionally substituted, in particular with a residue comprising a saturated or unsaturated, preferably C1-C12, hydrocarbon-based chain itself comprising an aromatic group, preferably a phenyl, said hydrocarbon-based chain optionally also comprising one or more heteroatoms preferably chosen from O, S and N.
摘要翻译：本发明涉及包含这些衍生物的新型的泛酸（2-（4-羟基苄基）苹果酸）衍生物或植物提取物，以及含有这些化合物或这些提取物的化妆品或皮肤病学组合物以及使用所述组合物的化妆品护理方法。示例性化合物由下式（I）表示：其中，条件是R1，R2和R3不同时为氢原子，R1和R3各自独立地表示氢原子或饱和或不饱和的，优选C1-C12，优选苯基的所述芳族基团优选被包含糖，优选单糖或二糖的基团取代，所述链任选地还包含一个或多个优选选自O，S和N的杂原子，并且R 2表示氢原子或糖，优选单糖或二糖，所述糖任选被取代，特别是与包含饱和或不饱和的，优选C 1 -C 12的基于烃的链本身包含芳族基团的残基，优选为苯基，所述烃基链任选还包含一个或多个优选选自O，S和N的杂原子。

157. 发明申请

US20120309701A1 COMPOUNDS AND METHODS FOR TREATING BACTERIAL INFECTIONS 有权
标题翻译：化合物和治疗细菌感染的方法
公开(公告)号：US20120309701A1
公开(公告)日：2012-12-06
申请号：US13453991
申请日：2012-04-23
申请人： James W. Janetka , Zhenfu Han , Scott Hultgren , Jerome S. Pinkner , Corinne Cusumano
发明人： James W. Janetka , Zhenfu Han , Scott Hultgren , Jerome S. Pinkner , Corinne Cusumano
IPC分类号： A61K31/7034 , C07H19/056 , A61K31/7056 , C07H15/22 , A61P13/02 , A61K31/7048 , A61K31/7042 , A61K31/706 , A61P31/04 , C07H15/207 , A61K31/7036
CPC分类号： C07H15/20 , A01N43/10 , A01N43/16 , A01N43/38 , A01N43/42 , A01N43/52 , A01N43/54 , A01N43/76 , A01N43/78 , A01N47/36 , A01N55/08 , A61K31/505 , A61K31/7034 , A61K31/7042 , A61K31/7048 , A61K31/7056 , A61K31/706 , C07D309/10 , C07H15/203 , C07H15/207 , C07H15/22 , C07H15/26 , C07H19/056
摘要： The present invention encompasses compounds and methods for treating urinary tract infections.
摘要翻译：本发明包括用于治疗尿路感染的化合物和方法。

158. 发明申请

US20120264924A1 Glycorandomization and Production of Novel Novobiocin Analogs 有权
标题翻译：新型新生霉素类似物的糖配合和生产
公开(公告)号：US20120264924A1
公开(公告)日：2012-10-18
申请号：US13448811
申请日：2012-04-17
申请人： Jon Thorson
发明人： Jon Thorson
IPC分类号： C07H15/22
CPC分类号： C07H1/00 , C07H15/207 , C07H15/22 , C07H17/08
摘要： The present invention provides glycorandomized structures and 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化结构化文库的多糖结构和组合方法，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。

159. 发明申请

US20110172176A1 CRYSTAL STRUCTURES OF SGLT2 INHIBITORS AND PROCESSES FOR PREPARING SAME 有权
标题翻译： SGLT2抑制剂的晶体结构及其制备方法
公开(公告)号：US20110172176A1
公开(公告)日：2011-07-14
申请号：US13049712
申请日：2011-03-16
申请人： Jack Z. Gougoutas , Hildegard Lobinger , Srividya Ramakrishnan , Prashant P. Deshpande , Jeffrey T. Bien , Chiajen Lai , Chenchi Wang , Peter Riebel , John Anthony Grosso , Alexandra A. Nirschl , Janak Singh , John D. DiMarco
发明人： Jack Z. Gougoutas , Hildegard Lobinger , Srividya Ramakrishnan , Prashant P. Deshpande , Jeffrey T. Bien , Chiajen Lai , Chenchi Wang , Peter Riebel , John Anthony Grosso , Alexandra A. Nirschl , Janak Singh , John D. DiMarco
IPC分类号： A61K31/7034 , C07H15/207 , C07H1/00 , A61P3/04 , A61P3/10 , A61P17/02 , A61P3/06 , A61P9/10 , A61P9/12
CPC分类号： C07H15/207 , A61K31/7034 , A61K45/06 , A61P3/10 , C07H7/04
摘要： The present invention relates to physical crystal structures of a compound of the formula I: wherein R1, R2, R2a, R3 and R4 are as defined herein, especially pharmaceutical compositions containing structures of compound I or II, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
摘要翻译：本发明涉及式I化合物的物理结晶结构：其中R1，R2，R2a，R3和R4如本文所定义，特别是含有化合物I或II结构的药物组合物，其制备方法，制备方法以及使用这种结构治疗糖尿病等疾病的方法。

160. 发明授权

US07932379B2 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：US07932379B2
公开(公告)日：2011-04-26
申请号：US11764839
申请日：2007-06-19
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： 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。

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