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81. 发明申请

US20150133650A1 DEVICE AND METHOD FOR THE PRODUCTION OF RADIOCHEMICAL COMPOUNDS 有权
标题翻译：用于生产放射化学化合物的装置和方法
公开(公告)号：US20150133650A1
公开(公告)日：2015-05-14
申请号：US14592283
申请日：2015-01-08
申请人： ABX ADVANCED BIOCHEMICAL COMPOUNDS GMBH , GESIM-GESELLSCHAFT FUER SILIZIUM-MIKROSYSTEME MBH
发明人： Marco MUELLER , Steffen HOWITZ
IPC分类号： C07B59/00 , C07H5/02 , B01J19/00
CPC分类号： C07B59/005 , B01J19/004 , B01J19/0046 , B01J19/0093 , B01J2219/00038 , B01J2219/0004 , B01J2219/00094 , B01J2219/00132 , B01J2219/00141 , B01J2219/00283 , B01J2219/00333 , B01J2219/00364 , B01J2219/00585 , B01J2219/00599 , B01J2219/00704 , B01J2219/0072 , B01J2219/00731 , B01J2219/00788 , B01J2219/0081 , B01J2219/00882 , B01J2219/00889 , B01J2219/00916 , B01J2219/00941 , C07B59/00 , C07B2200/05 , C07H5/02
摘要： The invention relates to a device for the preparation of radiochemical compounds. It is provided that the device comprises at least a reaction module, a dosing module, and a storage module, wherein the reaction module has at least one reaction vessel having a closable opening through which substances needed for the preparation of a predetermined radiochemical compound can be introduced into the reaction vessel of the reaction module and through which the prepared radiochemical compound can be removed from the reaction vessel of the reaction module; the dosing module has at least one pipetting head which can be moved relative to the storage module and the reaction module and in x, y, and z directions and also has at least one dosing unit; and at least one reservoir for one of the substances needed for the preparation of the respective radiochemical compound is formed in the storage module.
摘要翻译：本发明涉及一种用于制备放射化学化合物的装置。该装置至少包括反应模块，计量模块和存储模块，其中反应模块具有至少一个反应容器，该反应容器具有可闭合的开口，制备预定的放射化学化合物所需的物质可以通过该封闭开口引入反应模块的反应容器中，通过该反应模块可以从反应模块的反应容器中除去所制备的放射化学化合物; 所述计量模块具有至少一个移液头，其可相对于所述储存模块和所述反应模块以及x，y和z方向移动，并且还具有至少一个计量单元; 并且在储存模块中形成用于制备各放射化学化合物所需的物质之一的至少一个贮存器。

82. 发明授权

US08957033B2 Inhibitor of sodium-dependent glucose transport protein and preparation method therefor and use thereof 有权
标题翻译：钠依赖性葡萄糖转运蛋白的抑制剂及其制备方法及用途
公开(公告)号：US08957033B2
公开(公告)日：2015-02-17
申请号：US14114197
申请日：2012-02-20
申请人： Michael Wang
发明人： Michael Wang
IPC分类号： A61K31/70 , C07H1/00 , C07H5/02 , C07D309/10 , A61K9/00 , A61K9/16 , A61K9/20 , A61K31/351 , A61K45/06 , C07H7/04
CPC分类号： A61K31/70 , A61K9/0019 , A61K9/1623 , A61K9/1635 , A61K9/1652 , A61K9/2018 , A61K9/2027 , A61K9/2059 , A61K31/351 , A61K45/06 , C07D309/10 , C07H7/04 , A61K2300/00
摘要： Disclosed is a compound of formula I, or a pharmaceutically acceptable salt, solvate, polymorph, enantiomer or racemic mixture thereof, wherein R1 and R2 are each independently hydrogen, —OH, alkyl, —CF3, —OCHF2, —OCF3 or halogen; R3 is cycloalkyl, —OCH2CF3, —OCH2CHF2, —OCH2CH2F or —OCH2CH3; R4 is hydrogen, —OH, —O aryl, —OCH2 aryl, alkyl, cycloalkyl, —CF3, —OCHF2, —OCF3, —OCH2CF3, —OCH2CHF2, —OCH2CH2F or halogen; A is —CX1X2, wherein X1 and X2 are each independently H, F and Cl, and when both X1 and X2 are H, R3 is not —OCH2CH3. The compound has an activity of inhibitors of sodium-dependent glucose transport protein. Also disclosed is a method for preparing the compound, a pharmaceutical composition comprising the compound, use of the compound and pharmaceutical composition thereof in preparing medicaments of SGLT2 inhibitors and treating related diseases.
摘要翻译：公开了式I化合物或其药学上可接受的盐，溶剂化物，多晶型物，对映体或外消旋混合物，其中R 1和R 2各自独立地为氢，-OH，烷基，-CF 3，-OCHF 2，-OCF 3或卤素; R 3是环烷基，-OCH 2 CF 3，-OCH 2 CHF 2，-OCH 2 CH 2 F或-OCH 2 CH 3; R4是氢，-OH，-O芳基，-OCH2芳基，烷基，环烷基，-CF3，-OCHF2，-OCF3，-OCH2CF3，-OCH2CHF2，-OCH2CH2F或卤素; A是-CX1X2，其中X1和X2各自独立地为H，F和Cl，并且当X1和X2都是H时，R3不是-OCH2CH3。该化合物具有钠依赖性葡萄糖转运蛋白抑制剂的活性。还公开了制备该化合物的方法，包含该化合物的药物组合物，该化合物的用途及其药物组合物在制备SGLT2抑制剂的药物和治疗相关疾病中的用途。

83. 发明授权

US08912320B2 Process for removing dimethylamine 有权
标题翻译：去除二甲胺的方法
公开(公告)号：US08912320B2
公开(公告)日：2014-12-16
申请号：US13262147
申请日：2010-03-24
申请人： John Kerr , Robert Jansen , Anthony Baiada , Duane Leinhos , James Edwin Wiley
发明人： John Kerr , Robert Jansen , Anthony Baiada , Duane Leinhos , James Edwin Wiley
IPC分类号： C07C209/86 , C07H1/06 , C07H5/02
CPC分类号： C07H5/02
摘要： A process for removing dimethylamine (DMA) before and/or during and/or after deacylation in a reaction vessel of a feed stream comprising a sucralose-6-acylate resulting from the chlorination of a sucrose-6-acylate in the presence of dimethyl formamide (DMF), wherein the deacylation is conducted at a first set of conditions of temperature, pH and pressure, the process comprising: (a) providing a side stream loop from and to the reaction vessel; (b) adjusting the conditions of one or more of temperature, pH, and pressure in the loop, and setting the flow rate through the loop, to remove DMA while minimising carbohydrate degradation.
摘要翻译：在二甲基甲酰胺存在下，在包含由蔗糖-6-酰化物氯化得到的三氯半氯蔗糖-6-酰化物的进料流的反应容器中脱酰基之前和/或之前和/或之后除去二甲胺（DMA）的方法（DMF），其中所述脱酰基在温度，pH和压力的第一组条件下进行，所述方法包括：（a）从反应容器提供侧流回路; （b）调节循环中的一个或多个温度，pH和压力的条件，并设定流过循环的流速，以除去DMA同时使碳水化合物降解最小化。

84. 发明申请

US20140316130A1 USE OF MICROFABRICATED DEVICES 有权
标题翻译：微型装置的使用
公开(公告)号：US20140316130A1
公开(公告)日：2014-10-23
申请号：US14253049
申请日：2014-04-15
申请人： HAMMERSMITH IMANET LIMITED
发明人： FRANK BRADY , SAJINDER KAUR LUTHRA , JAMES MILLAR GILLIES , NICHOLAS TOBY JEFFREY
IPC分类号： C07H5/02 , C07D401/04 , C07D223/16 , C07C211/48 , C07C229/36
CPC分类号： C07H5/02 , B01J19/0093 , B01J2219/00783 , B01J2219/00889 , B01J2219/00905 , B01J2219/00952 , B01L3/5027 , B01L3/502715 , C07B59/00 , C07B59/001 , C07B59/002 , C07B59/005 , C07C211/48 , C07C229/36 , C07D223/16 , C07D401/04
摘要： This invention relates to the miniaturisation of radiosyntheses onto microfabricated devices, and in particular to use of microfabricated devices for radiosynthesis, isolation, and analysis of radiotracers for use in Positron Emission Tomography (PET).
摘要翻译：本发明涉及在微加工装置上放射合成的小型化，特别是涉及使用微加工装置进行放射性合成，分离和分析用于正电子发射断层扫描（PET）的放射性示踪剂。

85. 发明授权

US08785403B2 Glucopyranoside compound 有权
标题翻译：吡喃葡萄糖苷化合物
公开(公告)号：US08785403B2
公开(公告)日：2014-07-22
申请号：US13494602
申请日：2012-06-12
申请人： Sumihiro Nomura , Eiji Kawanishi , Kiichiro Ueta
发明人： Sumihiro Nomura , Eiji Kawanishi , Kiichiro Ueta
IPC分类号： C07H5/02 , A01N43/04 , A61K31/70
CPC分类号： C07H19/056 , A61K31/7042 , A61K31/7056 , A61K38/24 , A61K38/28 , A61K45/06 , C07H7/04 , C07H7/06 , C07H19/04 , C07H19/044 , C07H19/048 , A61K2300/00
摘要： A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); or a pharmaceutically acceptable salt thereof, or a prodrug thereof.
摘要翻译：下式的化合物：其中环A和环B是：（1）环A是任选取代的不饱和单环杂环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环，或任选取代的苯环，（2）环A是任选取代的苯环，环B是任选取代的不饱和单环杂环或任选取代的不饱和稠环杂双环，或（3）环A是任选取代的不饱和稠合杂双环环和环B独立地是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的苯环; X是碳原子或氮原子; Y为 - （CH 2）n - （n为1或2）; 或其药学上可接受的盐，或其前药。

86. 发明授权

US08497367B2 Sucralose purification process 有权
标题翻译：三氯蔗糖纯化工艺
公开(公告)号：US08497367B2
公开(公告)日：2013-07-30
申请号：US12413955
申请日：2009-03-30
申请人： Robert Jansen , Gordon Walker , John Kerr , Anthony Baiada
发明人： Robert Jansen , Gordon Walker , John Kerr , Anthony Baiada
IPC分类号： C07H5/02
CPC分类号： C07H5/02
摘要： A process for the extraction of sucralose from an aqueous solution containing at least sucralose, other chlorinated saccharides, sodium chloride and dimethylammonium chloride into an organic solvent for sucralose by contacting said organic solvent with said solution to extract sucralose into the organic solvent. The ratio of sodium chloride to dimethylammonium chloride in the aqueous solution is increased prior to or during contact so as to increase the partition coefficient of sucralose into said organic solvent.
摘要翻译：通过使所述有机溶剂与所述溶液接触将三氯半乳蔗糖，其它氯化糖，氯化钠和二甲基氯化铵的水溶液提取到三氯半乳蔗糖的有机溶剂中以将三氯蔗糖萃取到有机溶剂中的方法。在接触之前或接触期间，水溶液中氯化钠与二甲基氯化铵的比例增加，从而增加三氯蔗糖分配成所述有机溶剂的分配系数。

87. 发明授权

US08476424B2 Removal of acids from tertiary amide solvents 失效
标题翻译：从叔酰胺溶剂中除去酸
公开(公告)号：US08476424B2
公开(公告)日：2013-07-02
申请号：US12403762
申请日：2009-03-13
申请人： John Kerr , Robert Jansen , Christian J. Isaac , James Edwin Wiley, Jr. , Duane A. Leinhos
发明人： John Kerr , Robert Jansen , Christian J. Isaac , James Edwin Wiley, Jr. , Duane A. Leinhos
IPC分类号： C07H1/06 , C07H5/02
CPC分类号： C07C231/24 , B01D11/0426 , B01D11/0446 , B01D11/0476 , B01D11/0492 , C07H1/06 , C07H5/02 , C07H13/04 , C07C233/03
摘要： A method of removing a carboxylic acid from a liquid that contains a tertiary amide solvent includes a step of contacting the liquid with an extraction medium comprising an amine. The amine is immiscible with both water and the tertiary amide solvent, and the contacting step forms a de-acidified phase containing the tertiary amide solvent and a phase containing the extraction medium and the carboxylic acid. Both the liquid that contains the tertiary amide solvent and the de-acidified phase may also contain a sucrose-6-acylate.
摘要翻译：从含有叔酰胺溶剂的液体中除去羧酸的方法包括使液体与包含胺的萃取介质接触的步骤。胺与水和叔酰胺溶剂不混溶，接触步骤形成含有叔酰胺溶剂的脱酸相和含有萃取介质和羧酸的相。含有叔酰胺溶剂和脱酸相的液体也可以含有蔗糖-6-酰化物。

88. 发明申请

US20120276108A1 MONOSACCHARIDE-BASED COMPOUNDS FOR THE TREATMENT OF PROLIFERATIVE AND INFLAMMATORY DERMATOLOGICAL DISEASES 审中-公开
标题翻译：用于治疗增殖和炎症性皮肤病的基于单体化合物的化合物
公开(公告)号：US20120276108A1
公开(公告)日：2012-11-01
申请号：US13347968
申请日：2012-01-11
申请人： Waldemar Priebe
发明人： Waldemar Priebe
IPC分类号： A61K31/7024 , A61K31/7028 , C07H13/04 , C07H5/02 , C07D335/02 , A61K31/382 , C07H5/06 , A61K31/7008 , A61K31/70 , C07H13/06 , C07H7/02 , C07H99/00 , C07H5/10 , C07H9/04 , A61P17/00 , A61P17/06 , A61P17/08 , A61P17/10 , A61P29/00 , A61P17/02 , A61P35/00 , A61P37/06 , A61P31/04 , A61K39/395 , A61K31/7004 , C07H15/04
CPC分类号： C07H3/02 , A61K31/7004 , A61K31/7008 , A61K45/06 , C07H5/02 , C07H5/06 , C07H7/02 , C07H9/04 , C07H13/06 , C07H15/02 , A61K2300/00
摘要： The present invention relates to compounds and methods which may be useful as inhibitors of glycolysis, inhibitors of protein glycosylation, anti-virals, and down-regulators of insulin receptor and IGF-1 receptor for the treatment or prevention of inflammatory dermatological diseases or proliferative dermatological diseases.
摘要翻译：本发明涉及可用作糖酵解抑制剂，蛋白质糖基化抑制剂，抗病毒剂和胰岛素受体和IGF-1受体下调体的化合物和方法，用于治疗或预防炎性皮肤病学或增殖性皮肤病学疾病

89. 发明申请

US20120087943A1 AGENT FOR PREVENTING ADVERSE SIDE EFFECTS OF CARCINOSTATIC AGENT 有权
标题翻译：防止药物代谢不良副作用的药剂
公开(公告)号：US20120087943A1
公开(公告)日：2012-04-12
申请号：US13377887
申请日：2010-02-22
申请人： Masahide Ikeguchi , Manabu Yamamoto , Takayuki Kimura , Yasunari Miki
发明人： Masahide Ikeguchi , Manabu Yamamoto , Takayuki Kimura , Yasunari Miki
IPC分类号： A61K36/03 , A61P39/00 , A61K31/737 , C07H5/02 , A01H13/00
CPC分类号： A61K31/737 , A61K36/03
摘要： The present invention provides a side effect inhibitor of drug therapy for colorectal cancer using 5-fluorouracil, comprising fucoidan or a fucoidan-containing material; a method for inhibiting side effects of drug therapy for colorectal cancer using 5-fluorouracil, which comprises administering fucoidan or a fucoidan-containing material to a colorectal cancer patient; and use of fucoidan or a fucoidan-containing material for the production of a side effect inhibitor of drug therapy for colorectal cancer using 5-fluorouracil.
摘要翻译：本发明提供使用5-氟尿嘧啶，包含岩藻依聚糖或含岩藻依聚糖的材料的结肠直肠癌药物治疗的副作用抑制剂; 一种使用5-氟尿嘧啶抑制药物治疗结直肠癌副作用的方法，其包括对结肠直肠癌患者施用岩藻依聚糖或含岩藻依聚糖的材料; 以及使用含有岩藻依聚糖的岩藻多糖或含有岩藻依聚糖的材料用于使用5-氟尿嘧啶生产结肠直肠癌药物治疗副作用抑制剂。

90. 发明授权

US08101746B2 Granular sucralose, and method of making it 有权
标题翻译：颗粒三氯蔗糖及其制备方法
公开(公告)号：US08101746B2
公开(公告)日：2012-01-24
申请号：US11886494
申请日：2006-03-20
申请人： Warren L. Nehmer , Roy O. Elmore , William R. Skelding , Alexandria L. Bailey
发明人： Warren L. Nehmer , Roy O. Elmore , William R. Skelding , Alexandria L. Bailey
IPC分类号： C13K13/00 , C07H5/02 , C07H1/00
CPC分类号： A23L27/37 , A23P10/22 , A23V2002/00 , A23V2250/264 , A23V2200/22 , A23V2200/224 , A23V2200/254
摘要： Granular sucralose-containing particles are produced by the methods of the invention, which involve coating sucralose from solution to form granules with this coated sucralose on an outer region thereof. The granules may incorporate agglomerated sucralose particles, with the solution-coated sucralose adding mass and generally resulting in a granule having a relatively smoothed and rounded. The granules have good flow properties, are low dusting, and resist caking. Methods of making the granules involve spraying an aqueous sucralose solution onto a fluidized bed of sucralose particles, followed by drying to form the granules.
摘要翻译：通过本发明的方法制备含粒状的三氯蔗糖的颗粒，其包括从溶液中涂覆三氯半乳蔗糖以在其外部区域上与该涂覆的三氯半乳蔗糖形成颗粒。颗粒可以包含附聚的三氯半乳蔗糖颗粒，溶液涂覆的三氯蔗糖加入物质，并且通常导致具有相对平滑和圆润的颗粒。颗粒具有良好的流动性，低粉尘和抗结块。制造颗粒的方法包括将三氯蔗糖水溶液喷洒到三氯半乳蔗糖颗粒的流化床上，然后干燥以形成颗粒。

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