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21. 发明申请

US20160176909A1 REGIOSELECTIVE SILYL EXCHANGE OF PER-SILYLATED OLIGOSACCHARIDES 审中-公开
标题翻译：过氧化硅酸钠的间苯二酚交换
公开(公告)号：US20160176909A1
公开(公告)日：2016-06-23
申请号：US14975537
申请日：2015-12-18
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： Jacquelyn Gervay-Hague , Matthew Schombs
IPC分类号： C07H13/04 , C07H3/06 , C07H23/00
CPC分类号： C07H13/04 , C07H3/06 , C07H23/00 , Y02P20/55
摘要： The present invention provides novel, regioselectively-acylated oligosaccharide compounds and methods for preparing them. In another aspect, the. invention provides a method for preparing a selectively-acylated oligosaccharide. The method includes forming a reaction mixture containing a protected oligosaccharide and an acylating agent. The protected oligosaccharide includes at least three hydroxyl moieties and each hydroxyl moiety is protected with a silyl protecting group. The reaction mixture is formed under conditions sufficient to selectively replace at least one silyl protecting group with a —C(0)-C1_6 alkyl group, and the selectively-acylated oligosaccharide comprises at least one —C(0)-C1_6 alkyl group and at least one silyl protecting group.
摘要翻译：本发明提供新的区域选择性酰化寡糖化合物及其制备方法。在另一方面，本发明提供了制备选择性酰化寡糖的方法。该方法包括形成含有受保护的寡糖和酰化剂的反应混合物。受保护的寡糖包括至少三个羟基部分，并且每个羟基部分被甲硅烷基保护基团保护。反应混合物在足以选择性地用-C（O）-C 1-6烷基选择性取代至少一个甲硅烷基保护基的条件下形成，并且选择性酰化的寡糖包含至少一个-C（O）-C 1-6烷基，并且在至少一个甲硅烷基保护基。

22. 发明授权

US09284274B2 Chemical derivatives of jasmonate, pharmaceutical compositions and methods of use thereof 有权
标题翻译：茉莉酸的化学衍生物，药物组合物及其使用方法
公开(公告)号：US09284274B2
公开(公告)日：2016-03-15
申请号：US13831766
申请日：2013-03-15
申请人： RAMOT AT TEL-AVIV UNIVERSITY LTD. , SEPAL PHARMA LTD.
发明人： Yoel Kashman , Eliezer Flescher , Max Herzberg
IPC分类号： A01N43/42 , A61K31/47 , C07D215/12 , C07D215/14 , C07D215/24 , C07H13/04 , C07D215/32
CPC分类号： C07D215/24 , C07D215/32 , C07H13/04
摘要： The present invention relates to novel jasmonate derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for prevention and treatment of cancers.
摘要翻译：本发明涉及新颖的茉莉酸衍生物，其制备方法，包括这些化合物的药物组合物，以及使用这些化合物和组合物，特别是作为预防和治疗癌症的化学治疗剂的方法。

23. 发明申请

US20160021879A1 SYNTHETIC LIPOAMINO ACID GLUCOSAMINE DERIVATIVES FOR IMPROVEMENT OF PLANT GROWTH AND YIELD 审中-公开
标题翻译：用于改善植物生长和产量的合成LIPOAMINO酸型葡萄糖胺衍生物
公开(公告)号：US20160021879A1
公开(公告)日：2016-01-28
申请号：US14773585
申请日：2014-03-12
申请人： E.I. DU PONT DE NEMOURS AND COMPANY
发明人： Zheng-Zheng Huang , Subramaniam Sabesan , Zuohong Yin
IPC分类号： A01N43/16 , C07H15/04
CPC分类号： A01N43/16 , C07H13/04 , C07H13/06 , C07H15/04
摘要： The invention provides compounds, formulations and methods for improving plant emergence, growth and yield. More specifically, the present invention relates to compositions comprising the synthetic lipoamino acid glucosamine compounds of Formula I. These compounds may be applied to plant propagating materials, including seeds and other regenerable plant parts, including cuttings, bulbs, rhizomes and tubers. They may also be applied to foliage, or soil either prior to or following planting of plant propagating materials. Such applications may be made alone or in combination with fungicides, insecticides, nematicides and other agricultural agents used to improve plant growth and crop yield. The compounds of Formula I can improve the agronomic performance of a variety of crops including barley, canola, corn, potato, soybean and wheat.
摘要翻译：本发明提供用于改善植物出苗，生长和产量的化合物，制剂和方法。更具体地，本发明涉及包含式I的合成脂氨基葡糖胺化合物的组合物。这些化合物可以应用于植物繁殖材料，包括种子和其它可再生植物部分，包括扦插，鳞茎，根茎和块茎。它们也可以在种植植物繁殖材料之前或之后施用于叶子或土壤。这样的应用可以单独使用或与杀真菌剂，杀虫剂，杀线虫剂和用于改善植物生长和作物产量的其它农药联合使用。式I的化合物可以改善各种作物（包括大麦，卡诺拉，玉米，马铃薯，大豆和小麦）的农艺性能。

24. 发明申请

US20150368295A1 METHOD FOR PRODUCING PYRAZOLES, NOVEL PYRAZOLES AND APPLICATIONS THEREOF 有权
标题翻译：生产吡咯，新型吡咯并及其应用的方法
公开(公告)号：US20150368295A1
公开(公告)日：2015-12-24
申请号：US14766048
申请日：2014-02-07
申请人： COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES
发明人： Frederic TARAN , Manon CHAUMONTET , Sergii KOLODYCH , Evelia RASOLOFONJATOVO ANDOVOLA
IPC分类号： C07K5/08 , C07H19/06 , C07D401/04 , C07D409/04 , C07D231/12 , C07H13/04
CPC分类号： C07K5/08 , C07D231/12 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/04 , C07H1/00 , C07H13/04 , C07H15/26 , C07H19/06 , C07H19/073
摘要： A method for preparing a pyrazole of formula (I) in which R,R′ and R″ have different meanings, characterised in that it involves reacting a sydnone of formula (II) in which R and R′ have the meanings already indicated, with an alkyne of formula (III) in which R″ has the meaning already indicated, in the presence of copper, to obtain a pyrazole compound of formula (I) that is then isolated and salified if desired.
摘要翻译：制备式（I）的吡唑的方法，其中R，R'和R“具有不同的含义，其特征在于其包括将其中R和R'具有已经表示的含义的式（II）的硅藻土与在铜的存在下，R“具有已经表示的含义的式（III）的炔，得到式（I）的吡唑化合物，如果需要，则其分离和成盐。

25. 发明申请

US20150329555A1 SUBSTITUTED-6,8-DIOXABICYCLO[3.2.1]OCTANE-2,3-DIOL COMPOUNDS AS TARGETING AGENTS OF ASGPR 审中-公开
标题翻译：取代的6,8-二氧杂环戊烯[3.2.1]作为ASGPR的靶向剂的OCT-2,3-DIOL化合物
公开(公告)号：US20150329555A1
公开(公告)日：2015-11-19
申请号：US14714484
申请日：2015-05-18
申请人： Pfizer Inc.
发明人： Spiros Liras , Vincent Mascitti , Benjamin Thuma
IPC分类号： C07D493/08 , C07D309/14
CPC分类号： A61K31/706 , A61K31/7008 , A61K31/7056 , A61K38/465 , A61K47/64 , C07D309/14 , C07D493/08 , C07H13/04 , C07H15/08 , C07H15/12 , C07H15/26 , C07K5/06078 , C12Y301/00 , Y02A50/463
摘要： Compounds of Formula (A) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by pharmaceutical compositions and the uses thereof as asialoglycoprotein receptor (ASGPR) targeting agents.
摘要翻译：本文描述了式（A）的化合物及其用于治疗由药物组合物介导的疾病，病症和/或病症及其作为唾液酸糖蛋白受体（ASGPR）靶向剂的用途的用途。

26. 发明申请

US20150307915A1 DETECTION OF OLIGOSACCHARIDES 有权
标题翻译：检测寡糖
公开(公告)号：US20150307915A1
公开(公告)日：2015-10-29
申请号：US14706794
申请日：2015-05-07
申请人： BIOMARIN PHARMACEUTICAL INC.
发明人： Brett E. CRAWFORD , Jillian R. BROWN , Charles A. GLASS
IPC分类号： C12Q1/527 , C07H7/033 , C07H11/00
CPC分类号： C12Q1/527 , A61K31/702 , C07H3/04 , C07H3/06 , C07H5/06 , C07H7/033 , C07H11/00 , C07H13/04 , G01N33/66 , G01N2333/988 , G01N2400/40 , G01N2800/042 , G01N2800/52 , G01N2800/7071
摘要： Provided herein are processes for detecting oligosaccharides in a biological sample. In specific instances, the biological sample is provided from an individual suffering from a disorder associated with abnormal glycosaminoglycan accumulation.
摘要翻译：本文提供了检测生物样品中寡糖的方法。在具体情况下，生物样品由患有与异常糖胺聚糖累积相关的病症的个体提供。

27. 发明授权

US09163051B2 Crystal of spiroketal derivatives and process for preparation of spiroketal derivatives 有权
标题翻译：螺缩酮衍生物的晶体和螺甲醇衍生物的制备方法
公开(公告)号：US09163051B2
公开(公告)日：2015-10-20
申请号：US14034880
申请日：2013-09-24
申请人： Chugai Seiyaku Kabushiki Kaisha
发明人： Masatoshi Murakata , Takuma Ikeda , Nobuaki Kimura , Akira Kawase , Masahiro Nagase , Keisuke Yamamoto , Noriyuki Takata , Shinichi Yoshizaki , Koji Takano
IPC分类号： C07D313/00 , C07D315/00 , C07H19/01 , C07D493/10 , C07H7/04 , C07H13/04 , C07H23/00
CPC分类号： C07H19/01 , C07D493/10 , C07H1/00 , C07H7/04 , C07H13/04 , C07H23/00
摘要： The present invention provides a process for preparing a spiroketal derivative, via an intermediate represented by Formula (VI): wherein variable groups and numbers are as defined in the specification, which can be produced from dihalobenzene derivatives in one pot reaction.
摘要翻译：本发明提供了通过式（VI）表示的中间体制备螺缩酮衍生物的方法：其中可变基团和数目如说明书中所定义，其可以在一锅反应中由二卤代苯衍生物制备。

28. 发明申请

US20150259371A1 METHODS AND COMPOUNDS FOR INHIBITING GLYCOSYLTRANSFERASES 审中-公开
标题翻译：抑制谷氨酰转肽酶的方法和化合物
公开(公告)号：US20150259371A1
公开(公告)日：2015-09-17
申请号：US13696248
申请日：2011-05-06
申请人： David Jaro Vocadlo , Tracey Maureen Gloster , Lehua Deng , Wesley Franklin Zandberg
发明人： David Jaro Vocadlo , Tracey Maureen Gloster , Lehua Deng , Wesley Franklin Zandberg
IPC分类号： C07H15/203 , C07H15/04
CPC分类号： C07H15/203 , A61K31/382 , A61K31/70 , A61K31/7008 , A61K31/7024 , A61K31/7034 , A61K31/7072 , C07H13/04 , C07H15/04 , C07H19/10
摘要： The invention provides, in part, compounds that are capable of inhibiting a glycosyltransferase, such as a uridine diphospho-N-acetylglucosamine:polypeptide β N-acetylglucosaminyltransferase, an N-acetylgalactosaminyltransferase, a fucosyltransferase, a xylotransferase or a sialyltransferase. The invention also provides methods for using the compounds.
摘要翻译：本发明部分提供能够抑制糖基转移酶的化合物，例如尿苷二磷酸-N-乙酰葡糖胺：多肽＆bgr; N-乙酰葡糖胺基转移酶，N-乙酰半乳糖胺基转移酶，岩藻糖基转移酶，木糖转移酶或唾液酸转移酶。本发明还提供了使用该化合物的方法。

29. 发明申请

US20150252400A1 GLYCOCONJUGATE SYNTHESIS 有权
标题翻译：甘氨酸合成
公开(公告)号：US20150252400A1
公开(公告)日：2015-09-10
申请号：US14430930
申请日：2013-09-25
申请人： GLYCOM A/S
发明人： Pauline Peltier-Pain , Gyula Dekany , Christophe Pain , Pierre Chassagne , Nicolas Fierfort , Dóra Molnàr-Gàbor
IPC分类号： C12P19/44 , C07H15/08 , C07H13/04
CPC分类号： C12P19/44 , C07H13/04 , C07H15/04 , C07H15/08 , C07H15/26 , C12P19/18
摘要： The invention relates to a method for producing a glycoconjugate comprising an oligosaccharide part covalently linked to a non-sugar moiety selected from the group consisting of amino acids, peptides, proteins, lipids, longer alkyl groups, polyethylene glycols, α,β-unsaturated amido group and polyvinyl alcohols, using a genetically modified cell.
摘要翻译：本发明涉及一种制备糖缀合物的方法，其包含与非糖部分共价连接的寡糖部分，所述寡糖部分选自氨基酸，肽，蛋白质，脂质，较长的烷基，聚乙二醇，α，β-不饱和酰胺基和聚乙烯醇，使用转基因细胞。

30. 发明授权

US09073959B2 Process for the production of sucrose-6-ester 有权
标题翻译：蔗糖-6-酯的制备方法
公开(公告)号：US09073959B2
公开(公告)日：2015-07-07
申请号：US12901820
申请日：2010-10-11
申请人： Edward Micinski , David Coleman
发明人： Edward Micinski , David Coleman
IPC分类号： C07H13/04 , C07H13/06 , C07H13/08 , C07F7/22
CPC分类号： C07H13/04 , C07F7/2224 , C07H13/06 , C07H13/08
摘要： A process for the production of sucrose-6-ester is disclosed. The process includes, in order, the steps of: (a) providing a first reaction mixture including sucrose, a reaction vehicle, and an organotin-based acylation promoter; (b) removing water from the first reaction mixture to afford a second reaction mixture that is substantially free from water; and (c) adding a carboxylic acid anhydride to the second reaction mixture to afford a third reaction mixture, thereby producing a sucrose-6-ester; wherein: during step (b), the removing of water includes distillation of water with the reaction vehicle using an apparatus supplying a heat flux of from 500 to 25,000 BTU/hrft2 (1577 to 78865 W/m2) selected from the group consisting of wiped film evaporators, agitated thin film evaporators, falling film evaporators and rising film evaporators.
摘要翻译：公开了生产蔗糖-6-酯的方法。该方法按顺序包括以下步骤：（a）提供包含蔗糖，反应载体和基于有机锡的酰化促进剂的第一反应混合物; （b）从第一反应混合物中除去水，得到基本上不含水的第二反应混合物; 和（c）向第二反应混合物中加入羧酸酐，得到第三反应混合物，由此生产蔗糖-6-酯; 其中：在步骤（b）中，除去水包括使用提供500至25,000BTU / hrft2（1577至78865W / m 2）的热通量的装置与反应车辆蒸馏水，所述热通量选自擦拭薄膜蒸发器，搅拌薄膜蒸发器，降膜蒸发器和上升膜蒸发器。

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