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71. 发明申请

US20200289393A1 Oral Care Compositions Containing Deoxy Sugar Antimetabolites 审中-公开
公开(公告)号：US20200289393A1
公开(公告)日：2020-09-17
申请号：US16884958
申请日：2020-05-27
申请人： Colgate-Palmolive Company , The Forsyth Institute
发明人： Lyndsay SCHAEFFER-KORBYLO , Jorge FRIAS-LOPEZ
IPC分类号： A61K8/60 , A61Q11/00 , A61K8/69 , C07H5/06 , C07H5/02 , C07H3/08
摘要： Described herein are oral care compositions comprising a deoxy sugar antimetabolite and methods of inhibiting microbial biofilm formation and/or degrading a microbial biofilm in a subject.

72. 发明申请

US20190309005A1 LIQUID-LIQUID EXTRACTION OF DMF 审中-公开
公开(公告)号：US20190309005A1
公开(公告)日：2019-10-10
申请号：US16450256
申请日：2019-06-24
申请人： Tate & Lyle Technology Limited
发明人： David DENTEL , Thomas EILERS , Edward MICINSKI
IPC分类号： C07H5/02 , C07H13/04 , C07H1/06 , B01D11/04 , C07H1/00
摘要： The present invention relates to 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 includes steps of: (i) combining the sucrose-6-acylate with a chlorinating agent in a reaction vehicle comprising a tertiary amide to afford a mixture; (ii) heating said mixture for a heating period in order to provide chlorination of sucrose-6-acylate at the 4, 1′ and 6′ positions thereof; and (iii) quenching the product stream of (ii) to produce a 4,1′,6′-trichloro-4,1′,6′-trideoxy-galactosucrose-6-acylate; wherein before said quenching, a portion of said tertiary amide is removed by extraction into a solvent in which said tertiary amide is at least partially soluble.

73. 发明申请

US20190276487A1 DEVICE AND CASSETTE FOR PERFORMING A PLURALITY OF SYNTHESIS PROCESSES OF PREPARING A RADIOPHARMACEUTICAL IN SERIES 审中-公开
公开(公告)号：US20190276487A1
公开(公告)日：2019-09-12
申请号：US16424677
申请日：2019-05-29
申请人： OUT AND OUT CHEMISTRY S.P.R.L.
发明人： Vincent Luc Antoine Tadino , Guillaume André René Villeret
IPC分类号： C07H5/02 , C07C229/36 , C07D207/46 , C07D233/91 , C07C39/40 , B01J41/00 , C07C215/40 , B01J19/24 , C07B59/00 , C01D3/02 , C07H19/06 , C07C53/18
摘要： A cassette for performing a plurality of synthesis processes of preparing a radiopharmaceutical in series in a synthesizer, includes: at least one manifold provided with a plurality of valves connectable to and operable by the synthesizer; an anion-exchanger comprising an anionic exchange material; an eluent container comprising an eluent; and a recondition container comprising a reconditioning agent.

74. 发明授权

US10370398B2 Liquid-liquid extraction of DMF 有权
公开(公告)号：US10370398B2
公开(公告)日：2019-08-06
申请号：US15628141
申请日：2017-06-20
申请人： Tate & Lyle Technology Limited
发明人： David Dentel , Thomas Eilers , Edward Micinski
IPC分类号： C07H5/02 , C07H1/06 , B01D11/04 , C07H1/00 , C07H13/04
摘要： The present invention relates to 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 includes steps of: (i) combining the sucrose-6-acylate with a chlorinating agent in a reaction vehicle comprising a tertiary amide to afford a mixture; (ii) heating said mixture for a heating period in order to provide chlorination of sucrose-6-acylate at the 4, 1′ and 6′ positions thereof; and (iii) quenching the product stream of (ii) to produce a 4,1′,6′-trichloro-4,1′,6′-trideoxy-galactosucrose-6-acylate; wherein before said quenching, a portion of said tertiary amide is removed by extraction into a solvent in which said tertiary amide is at least partially soluble.

75. 发明授权

US10023601B2 Hydrolysis resistant sialic acid derivatives and methods for their use 有权
公开(公告)号：US10023601B2
公开(公告)日：2018-07-17
申请号：US15119622
申请日：2015-02-18
申请人： The University of British Columbia
发明人： Stephen G. Withers , Thomas J. Morley , Lars Baumann
IPC分类号： C07H13/02 , C12P21/00 , C07K1/107 , C07H5/02 , C08H1/00
摘要： This invention provides compound having a structure of Formulas: Furthermore, methods and uses of such compounds for covalently bonding to a sugar acceptor, to form modified protein therapeutics having reduced enzymatic hydrolysis, improved biological stability or an improved pharmacokinetic property.

76. 发明申请

US20170320901A1 Fluoride Trapping Arrangement 审中-公开
公开(公告)号：US20170320901A1
公开(公告)日：2017-11-09
申请号：US15526139
申请日：2015-11-12
申请人： GE Healthcare Limited
发明人： Xavier Franci , Steve Lignon , Audrey Marie Lange , Nicolas Verbrugge
IPC分类号： C07H5/02 , B01D15/42 , B01J47/022 , B01J41/20 , A61K51/04 , B01J41/09 , B01D15/36 , B01D15/18 , B01D15/14 , C07H1/06 , B01J41/04
CPC分类号： C07H5/02 , A61K51/0497 , B01D15/14 , B01D15/1885 , B01D15/363 , B01D15/424 , B01J41/04 , B01J41/09 , B01J41/20 , B01J47/022 , C07B59/00 , C07B2200/05 , C07H1/06
摘要： The present invention provides a new chemical process, a new cassette configuration, and new software for the automated production of multiple batches of an [18F]labelled compound on a single cassette. The invention allows one synthesizer in one hot cell to produce sequentially a plurality of batches of [18F]-labelled PET tracer in the same day. In particular, the present invention provides a novel arrangement useful for the trapping of [18F]fluoride and recovery of [18O]water.

77. 发明授权

US09550704B2 Method for synthesizing radiopharmaceuticals using a cartridge 有权
标题翻译：使用药筒合成放射性药物的方法
公开(公告)号：US09550704B2
公开(公告)日：2017-01-24
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： A61K51/04 , A61K51/08 , C07B59/00 , C07H5/02 , C07H19/06 , C07D451/02 , C07J1/00 , C07D233/91 , C07D417/04 , C07C213/08
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。

78. 发明授权

US09481705B2 Modular radiochemistry synthesis system 有权
公开(公告)号：US09481705B2
公开(公告)日：2016-11-01
申请号：US14941164
申请日：2015-11-13
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： Nagichettiar Satyamurthy , Jorge R. Barrio , Bernard Amarasekera , R. Michael Van Dam , Sebastian Olma , Dirk Williams , Mark Eddings , Clifton Kwang-Fu Shen
IPC分类号： C07H19/16 , B01J19/00 , B01J19/12 , C07B59/00 , C07C201/06 , C07D207/46 , C07H5/02 , C07H19/06
CPC分类号： C07H19/16 , B01J19/004 , B01J19/126 , B01J2219/00049 , B01J2219/24 , C07B59/001 , C07B59/002 , C07B59/005 , C07B2200/05 , C07C201/06 , C07D207/46 , C07H5/02 , C07H19/06 , Y10T436/115831 , Y10T436/12
摘要： A modular chemical production system includes multiple modules for performing a chemical reaction, particularly of radiochemical compounds, from a remote location. One embodiment comprises a reaction vessel including a moveable heat source with the position thereof relative to the reaction vessel being controllable from a remote position. Alternatively the heat source may be fixed in location and the reaction vial is moveable into and out of the heat source. The reaction vessel has one or more sealing plugs, the positioning of which in relationship to the reaction vessel is controllable from a remote position. Also the one or more reaction vessel sealing plugs can include one or more conduits there through for delivery of reactants, gases at atmospheric or an elevated pressure, inert gases, drawing a vacuum and removal of reaction end products to and from the reaction vial, the reaction vial with sealing plug in position being operable at elevated pressures. The modular chemical production system is assembled from modules which can each include operating condition sensors and controllers configured for monitoring and controlling the individual modules and the assembled system from a remote position. Other modules include, but are not limited to a Reagent Storage and Delivery Module, a Cartridge Purification Module, a Microwave Reaction Module, an External QC/Analysis/Purification Interface Module, an Aliquotting Module, an F-18 Drying Module, a Concentration Module, a Radiation Counting Module, and a Capillary Reactor Module.

79. 发明授权

US09296774B2 Halogenated dideoxy sugar derivates, preparation method and application thereof 有权
标题翻译：卤代二脱氧糖衍生物及其制备方法及应用
公开(公告)号：US09296774B2
公开(公告)日：2016-03-29
申请号：US13540609
申请日：2012-07-02
申请人： Hua Mao
发明人： Hua Mao
IPC分类号： A01N43/04 , A61K31/70 , A01N43/16 , A61K31/35 , C07H5/04 , C07H5/06 , C08B37/00 , C07H11/04 , C07H5/02 , C07D493/04
CPC分类号： C07H11/04 , C07D493/04 , C07H5/02
摘要： A halogenated dideoxy sugar derivative, having the following general structure I wherein X is halogen, R1 and R2 are H or Br; R3 and R4 are OH or OAc. The compounds 1-14 of the current invention has strong inhibition effect on human nasopharyngeal cancer CNE-2Z cells, human lung cancer A549 cells. human colon cancer HT-29 cells, human liver cancer Bel-7402 cells, human rectum cancer cells HCE 8693, human stomach cancer BGC-803 cells, human esophagus cancer CaEs-17 cells, human breast cancer cells MCF-7, human ovarian cancer cells A2780, pancreatic cancer cells PC-3, human bladder cells EJ, human brain glia cells TG-905, human leukemia cells K562, human melanoma M 14 cells and human anaplastic thyroid carcinoma TA-K cells. They can be used to prepare anti-tumor medicament and have significant clinic value.
摘要翻译：具有以下一般结构I的卤代双脱氧糖衍生物，其中X是卤素，R 1和R 2是H或Br; R3和R4是OH或OAc。本发明化合物1-14对人鼻咽癌CNE-2Z细胞，人肺癌A549细胞具有强烈的抑制作用。人结肠癌HT-29细胞，人肝癌Bel-7402细胞，人直肠癌细胞HCE 8693，人胃癌BGC-803细胞，人食管癌CaEs-17细胞，人乳腺癌细胞MCF-7，人卵巢癌细胞A2780，胰腺癌细胞PC-3，人膀胱细胞EJ，人脑胶质细胞TG-905，人白血病细胞K562，人黑素瘤M14细胞和人间变性甲状腺癌TA-K细胞。它们可用于制备抗肿瘤药物，具有显着的临床价值。

80. 发明授权

US09073802B2 Method for producing 18F-labeled compound and high molecular compound to be used in the method 有权
标题翻译：方法中使用的18F标记化合物和高分子化合物的制备方法
公开(公告)号：US09073802B2
公开(公告)日：2015-07-07
申请号：US13578569
申请日：2011-02-08
申请人： Takashi Takahashi , Hiroshi Tanaka , Tsutomu Nakada
发明人： Takashi Takahashi , Hiroshi Tanaka , Tsutomu Nakada
IPC分类号： C07H5/02 , C08F236/20 , A61K51/04 , C07B59/00 , C07H15/26
CPC分类号： C07B59/00 , A61K51/0491 , C07H15/26 , C08F236/20
摘要： The present invention aims at solving the problems of conventional methods for producing an 18F-labeled compound, that is, the problem of purification of a compound in a liquid phase synthesis method and the problem of an insufficient yield due to the reduction of reactivity in a solid phase synthesis method. There is provided a method for producing an 18F-labeled compound including: allowing a high molecular compound containing a residue of a precursor compound to be labeled and a residue of a phase transfer catalyst in the molecule thereof to react with 18F−; and removing the 18F-labeled compound from the high molecular compound.
摘要翻译：本发明旨在解决用于制备18F标记化合物的常规方法的问题，即液相合成法中化合物的纯化问题以及由于反应性降低引起的产率不足的问题固相合成法。提供了一种制备18 F标记化合物的方法，包括：使含有前体化合物残基的高分子化合物被标记，分子中的相转移催化剂残基与18F-反应; 并从高分子化合物中除去18F标记的化合物。

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