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1. 发明授权

US10556024B2 18F labeling of proteins using sortases 有权
公开(公告)号：US10556024B2
公开(公告)日：2020-02-11
申请号：US15035924
申请日：2014-11-13
申请人： Whitehead Institute for Biomedical Research , The General Hospital Corporation
发明人： Mohammad Rashidian , Hidde L. Ploegh , Ralph Weissleder , Edmund J. Keliher
IPC分类号： A61K51/00 , A61K51/10 , C07H5/02 , C07K16/28 , C12N9/50 , G01N33/60
摘要： The present invention, in some aspects, provides methods, reagents, compositions, and kits for the radiolabeling of proteins, for example, of proteins useful for positron emission tomography (PET) or single-photon emission computed tomography (SPECT) (e.g., for diagnostic and therapeutic applications), using sortase-mediated transpeptidation reactions. Some aspects of this invention provide methods for the conjugation of an agent, for example, a radioactive agent or molecule to diagnostic or therapeutic peptides or proteins. Compositions comprising sortagged, radiolabeled proteins as well as reagents for generating radiolalebed proteins are also provided. Kits comprising reagents useful for the generation of radiolabeled proteins are provided, as are precursor proteins that comprise a sortase recognition motif.

2. 发明授权

US10342858B2 Glycan conjugates and methods of use thereof 有权
公开(公告)号：US10342858B2
公开(公告)日：2019-07-09
申请号：US14832993
申请日：2015-08-21
申请人： Academia Sinica
发明人： Chi-Huey Wong , Chung-Yi Wu
IPC分类号： C07H5/02 , C07H5/04 , C07H5/06 , A61K39/00 , C07H15/04 , C07H15/26 , C07K16/30 , C07K16/44 , C08B37/00 , A61K31/715 , A61K31/7028
摘要： The present disclosure is directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA3/SSEA4/GloboH associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globo-series glycosphingolipid synthesis. The present disclosure relates to methods and compositions which can modulate the globo-series glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globo-series glycosphingolipid SSEA3/SSEA4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globo-series synthetic pathway. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions.

3. 发明授权

US10081651B2 Chlorination of sucrose-6-esters 有权
公开(公告)号：US10081651B2
公开(公告)日：2018-09-25
申请号：US15502372
申请日：2015-06-16
申请人： Tate & Lyle Technology Limited
发明人： Thomas Eilers , Halil Aktas
IPC分类号： C07H5/02 , C07H13/04
CPC分类号： C07H5/02 , C07H13/04
摘要： There is provided a method for the chlorination of a sucrose-6-acylate to produce a 4,1′,6′-trichloro-4,1′,6′-trideoxy-galactosucrose-6-acylate, wherein said method comprises the following steps (i) to (v): (i) providing a first component comprising sucrose-6-acylate; (ii) providing a second component comprising a chlorinating agent; (iii) combining said first component and said second component to afford a mixture; (iv) heating said mixture for a heating period in order to provide chlorination of sucrose-6-acylate at the 4, 1′ and 6′ positions thereof; (v) quenching said mixture to produce a 4,1′,6′-trichloro-4,1′,6′-trideoxy-galactosucrose-6-acylate; wherein at least one of said first component and said second component comprises a reaction vehicle, and said reaction vehicle comprises a tertiary amide; and wherein said mixture comprises a cosolvent during a least a portion of the heating period of step (iv), wherein said cosolvent comprises dimethylacetamide (DMAc).

4. 发明申请

US20180008949A1 Piercing Device 审中-公开
公开(公告)号：US20180008949A1
公开(公告)日：2018-01-11
申请号：US15546924
申请日：2016-03-10
申请人： GE Healthcare Limited
发明人： Xavier Franci , Philippe Dumont , Steve Lignon , Audrey Marie Lange , Nicolas Verbrugge
IPC分类号： B01J19/00 , A61K51/04 , B01J19/18 , C07H5/02
CPC分类号： B01J19/004 , A61K51/0491 , B01J19/0093 , B01J19/18 , B01J2219/00799 , B01J2219/00833 , B01J2219/00862 , B01J2219/00867 , B01J2219/00894 , B01J2219/00916 , B01J2219/00918 , B01J2219/00927 , B01J2219/00952 , C07B2200/05 , C07H5/02
摘要： The present invention provides a system for the production of a radiopharmaceutical including a radiosynthesis apparatus and a disposable cassette. The system of the invention includes a device that enables a position on the cassette to be freed for inclusion of an additional reagent vial. With the system of the invention a broader range of radiochemical syntheses can be envisaged using the cassette.

5. 发明申请

US20170326255A1 SUCROSE ESTER BASED CATIONIC GENE VECTOR AND PREPARATION METHOD THEREOF 审中-公开
公开(公告)号：US20170326255A1
公开(公告)日：2017-11-16
申请号：US15546942
申请日：2015-06-25
申请人： DALIAN NATIONALITIES UNIVERSITY
发明人： Shubiao ZHANG , Defu ZHI , Shaohui CUI , Yinan ZHAO , Quan ZHOU
IPC分类号： A61K48/00 , A61K9/127 , C12N15/88 , A61K47/26 , A61K9/107 , C07H5/02 , A61K47/28 , C07J17/00 , C12N15/113
CPC分类号： A61K48/0033 , A61K9/1075 , A61K9/127 , A61K9/1272 , A61K47/26 , A61K47/28 , C07H1/00 , C07H5/02 , C07H13/06 , C07J17/005 , C12N15/111 , C12N15/113 , C12N15/88 , C12N2310/14 , C12N2320/32
摘要： The invention provides a class of sucrose ester based cationic lipids and preparation method thereof. The vector prepared using the cationic lipid can be used to deliver nucleic acid. The sucrose ester based cationic lipid is prepared by using a chemical synthesis method in the invention, wherein the synthesis method is simple, and has a relatively high product yield. A composition, including suspension, emulsion, micelle and liposome and the like, can be prepared by mixing the sucrose ester based cationic lipid compound of the invention with a co-lipid. Sucrose ester based cationic lipid complex can be prepared by using the said composition and nucleic acid, which has advantages such as simple preparation, low toxicity and high transfection efficiency, and is a novel and highly efficient gene vector.

6. 发明申请

US20150367005A1 METHOD OF SYNTHESIZING FLUORINE-18 LABELED RADIOPHARMACEUTICALS IN ETHANOL AND WATER 审中-公开
标题翻译：在乙醇和水中合成荧光素-18标记的放射性物质的方法
公开(公告)号：US20150367005A1
公开(公告)日：2015-12-24
申请号：US14744627
申请日：2015-06-19
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN
发明人： Peter J. H. Scott , Megan N. Stewart , Brian Hockley
IPC分类号： A61K51/04 , C07H5/02 , C07C309/73 , C07B59/00
CPC分类号： A61K51/0491 , C07B59/00 , C07B2200/05 , C07C209/68 , C07C213/08 , C07C253/30 , C07C303/30 , C07D233/91 , C07D405/04 , C07D451/00 , C07H5/02 , C07J1/007 , C07C255/42 , C07C309/73 , C07C215/40
摘要： A method of preparing fluorine-18 labeled radiopharmaceuticals (18F-radiopharmaceuticals) is disclosed. More particularly, the present invention relates to a method of preparing an 18F-radiopharmaceutical by reacting a salt containing fluorine-18 (18F) with an alkyl halide or an alkyl sulfonate in the presence of water and ethanol to obtain a high yield of the 18F-radiopharmaceutical. The synthetic method eliminates the use of toxic and/or environmentally-unfriendly organic solvents.
摘要翻译：公开了制备氟-18标记的放射性药物（18F-放射性药物）的方法。更具体地说，本发明涉及通过在水和乙醇的存在下使含有氟-18（18F）的盐与烷基卤化物或烷基磺酸盐反应来制备18 F放射性药物的方法，以获得高产率的18F 放射性药物。合成方法消除了使用有毒和/或不利于环境的有机溶剂。

7. 发明申请

US20150232392A1 METHOD FOR SYNTHESIZING RADIOPHARMACEUTICALS USING A CARTRIDGE 有权
标题翻译：使用盒子合成放射线辐射的方法
公开(公告)号：US20150232392A1
公开(公告)日：2015-08-20
申请号：US14401790
申请日：2013-05-24
申请人： Futurechem Co., LTD.
发明人： Dae Yoon Chi , Byoung Se Lee , Jae Hak Lee , So Young Chu , Woon Jung Jung
IPC分类号： C07B59/00 , A61K51/04 , C07H19/06 , C07C213/08 , C07J1/00 , C07D233/91 , C07D417/04 , C07H5/02 , C07D451/02
CPC分类号： C07B59/007 , A61K51/0453 , A61K51/0455 , A61K51/0491 , A61K51/0493 , A61K51/082 , C07B59/00 , C07B59/001 , C07B59/002 , C07B59/004 , C07B59/005 , C07B2200/05 , C07C213/08 , C07D233/91 , C07D417/04 , C07D451/02 , C07H5/02 , C07H19/06 , C07J1/00 , C07J1/007 , C07J71/0089
摘要： The present invention relates to a method for synthesizing a radiopharmaceutical using a cartridge, which makes it possible to carry out several steps of reaction required for synthesizing a radiopharmaceutical in the cartridge filled with a polymer. A method for synthesizing a radiopharmaceutical according to the present invention enables each step's reaction to be carried out with the solution confined in the cartridge so as not to flow out, thus being simplified compared to the conventional methods for synthesizing radiopharmaceuticals, and expediting the synthesis thereof.
摘要翻译：本发明涉及一种使用药筒合成放射性药物的方法，其使得可以在填充有聚合物的药筒中进行合成放射性药物所需的几个反应步骤。根据本发明的合成放射性药物的方法能够使限制在药筒中的溶液进行每个步骤的反应，从而不会流出，因此与用于合成放射性药物的常规方法相比，简化了其加速合成。

8. 发明授权

US08981079B2 Purification of tertiary formamide contaminated with tertiary acetamide 有权
标题翻译：用叔乙酰胺污染的叔甲酰胺的纯化
公开(公告)号：US08981079B2
公开(公告)日：2015-03-17
申请号：US13378531
申请日：2010-06-18
申请人： James Edwin Wiley, Jr. , Mohamad R. Jaber
发明人： James Edwin Wiley, Jr. , Mohamad R. Jaber
IPC分类号： C07H5/02 , C07C233/03 , C07C231/24 , C07H1/06
CPC分类号： C07C231/24 , C07H1/06 , C07H5/02 , C07C233/03
摘要： A chlorinating agent such as a chloroiminium species is used to remove or neutralize tertiary acetamide present as a contaminant in a tertiary formamide solvent. Tertiary formamide solvent purified or treated in this manner can be used as a reaction vehicle for the chlorination of sucrose-6-acylates, thereby improving the yields of the desired sucralose-6-acylate (an intermediate in the production of sucralose).
摘要翻译：使用氯化剂如氯亚胺鎓物质来除去或中和作为叔甲酰胺溶剂中的污染物存在的叔乙酰胺。以这种方式纯化或处理的叔甲酰胺溶剂可用作蔗糖-6-酰化物氯化反应载体，从而提高所需三氯半乳蔗糖-6-酰化物（三氯蔗糖生产中的中间体）的产率。

9. 发明授权

US08927706B2 Based-assisted formation of tin-sucrose adducts 有权
标题翻译：基于辅助的锡 - 蔗糖加合物的形成
公开(公告)号：US08927706B2
公开(公告)日：2015-01-06
申请号：US13262102
申请日：2010-03-10
申请人： Thomas Kennedy Hutton , Peter Jay Seaberg , Christopher C. Kerwood
发明人： Thomas Kennedy Hutton , Peter Jay Seaberg , Christopher C. Kerwood
IPC分类号： C07H1/00 , C07H3/04 , C07H5/02 , A23L1/236 , C07H13/04 , C07H23/00
CPC分类号： C07H1/00 , A23L27/30 , C07H3/04 , C07H5/02 , C07H13/04 , C07H23/00
摘要： A method of forming a sucrose-6-ester includes in sequence the steps of: a) contacting sucrose with a organotin-based acylation promoter in a solvent in the presence of a base selected from amines and basic alkali metal salts; b) removing water to form a tin-sucrose adduct; and c) contacting the tin-sucrose adduct with an acylating agent to form the sucrose-6-ester. The sucrose-6-ester may then be converted to sucralose.
摘要翻译：形成蔗糖-6-酯的方法包括以下步骤：a）在选自胺和碱金属碱的碱的存在下，在溶剂中使蔗糖与有机锡基酰化促进剂接触; b）除去水以形成锡 - 蔗糖加合物; 和c）使锡 - 蔗糖加合物与酰化剂接触以形成蔗糖-6-酯。然后将蔗糖-6-酯转化成三氯蔗糖。

10. 发明授权

US08536326B2 Method for preparing sucralose with high yield 有权
标题翻译：高产量制备三氯蔗糖的方法
公开(公告)号：US08536326B2
公开(公告)日：2013-09-17
申请号：US13008920
申请日：2011-01-19
申请人： Hengbo Liang , Zhengyou Wang , Li Rao
发明人： Hengbo Liang , Zhengyou Wang , Li Rao
IPC分类号： C13K13/00 , C07H5/02
CPC分类号： C07H5/02 , A23L27/37
摘要： A method for preparing sucralose with high yield, comprising the following preparation steps: First, negative effects of other impurities on reaction are reduced by first preparing a pure Vilsmeier chlorinating reagent. Second, side reactions are prevented by adding composite catalyst to increase selectivity of chlorination reaction. Third, by extracting less polar impurities using less polar solvent when sucralose-6-ester is undergoing deesterification, products are qualified at the very first time so that refining steps are avoided. Accordingly, product loss is reduced and product yield is increased. By using the present invention to prepare sucralose, product yield could be increased to more than 40%.
摘要翻译：一种以高产率制备三氯蔗糖的方法，包括以下制备步骤：首先，首先制备纯Vilsmeier氯化试剂，降低其他杂质对反应的负面影响。其次，通过添加复合催化剂以提高氯化反应的选择性来防止副反应。第三，当三氯半乳蔗糖-6-酯进行脱酯化时，通过使用极性较小的溶剂萃取较少的极性杂质，产品在第一次合格，从而避免了精制步骤。因此，产品损失降低，产品产量增加。通过使用本发明制备三氯半乳蔗糖，可以将产率提高至40％以上。

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