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11. 发明申请

US20120264932A1 DIGITAL MICROFLUIDIC PLATFORM FOR RADIOCHEMISTRY 有权
标题翻译：用于放射化学的数字微流平台
公开(公告)号：US20120264932A1
公开(公告)日：2012-10-18
申请号：US13500785
申请日：2010-10-15
申请人： R. Michael Van Dam , Chang-Jin Kim , Supin Chen , Huijiang Ding , Gaurav Jitendra Shah , Pei Yuin Keng
发明人： R. Michael Van Dam , Chang-Jin Kim , Supin Chen , Huijiang Ding , Gaurav Jitendra Shah , Pei Yuin Keng
IPC分类号： B01J19/08 , C07H5/02 , C07C205/12
CPC分类号： C07B39/00 , B01J19/0093 , B01J2219/00783 , B01J2219/00853 , B01J2219/00873 , B01L3/502784 , B01L2300/1827 , B01L2400/0427 , B01L2400/0487 , C07B59/001 , C07B59/002 , C07B59/005 , C07B2200/05 , C07C201/12 , C07C227/16 , C07D473/18 , C07H1/00
摘要： Disclosed herein are methods of performing microchemical reactions and electro- wetting-on-dielectric devices (EWOD devices) for use in performing those reactions. These devices and method are particularly suited for preparing radiochemical compounds, particularly compounds containing 18F.
摘要翻译：本文公开了用于执行这些反应的微量化学反应和电润湿介电装置（EWOD装置）的方法。这些装置和方法特别适用于制备放射化学化合物，特别是含有18F的化合物。

12. 发明授权

US08258291B2 Process for the preparation of sucralose by the chlorination of sugar with triphosgene (BTC) 失效
标题翻译：用三光气（BTC）氯化糖制备三氯蔗糖的方法
公开(公告)号：US08258291B2
公开(公告)日：2012-09-04
申请号：US11552789
申请日：2006-10-25
申请人： David Losan Ho , Wan Zhenghao
发明人： David Losan Ho , Wan Zhenghao
IPC分类号： C07H1/00 , C07H5/02
CPC分类号： C07H1/00 , C07H5/02
摘要： In one embodiment of the invention a method to prepare sucralose-6 -acylate through chlorinating sucrose-6-acylate by BTC in the process of sucralose preparation is disclosed. In this embodiment a Vilsmeier reagent is firstly prepared below 0° C. by dissolving BTC in DMF or in component solvent, containing DMF, toluene, dichloroethane, chloroform and carbon tetrachloride. Consequently, sucrose-6-ester was chlorinated by Vilsmeier reagent. BTC can also be dissolved in one or several organic solvent such as toluene, dichloroethane, chloroform and carbon tetrachloride, and added to a DMF solution of sucrose-6-acylate for chlorination. Sucralose was prepared through de-esterifying the obtained sucralose 6-ester using sodium methoxide/methanol or sodium ethoxide/ethanol.
摘要翻译：在本发明的一个实施方案中，公开了在三氯蔗糖制备过程中通过BTC氯化蔗糖-6-酰化物制备三氯蔗糖-6-乙酸酯的方法。在本实施例中，首先通过将BTC溶解在DMF或含有DMF，甲苯，二氯乙烷，氯仿和四氯化碳的组分溶剂中，在0℃以下制备Vilsmeier试剂。因此，蔗糖-6-酯被Vilsmeier试剂氯化。 BTC也可以溶解在一种或几种有机溶剂如甲苯，二氯乙烷，氯仿和四氯化碳中，并加入蔗糖-6-酰化物的DMF溶液进行氯化。通过使用甲醇钠/甲醇或乙醇钠/乙醇使得到的三氯蔗糖6-酯脱酯化来制备三氯蔗糖。

13. 发明申请

US20110288287A1 Halogen Substituted Saccharide, Method for Producing Same, Reaction Composition of Same and Device for Producing Same 审中-公开
标题翻译：卤素取代的糖，其生产方法，其反应组合物及其制备装置
公开(公告)号：US20110288287A1
公开(公告)日：2011-11-24
申请号：US13142897
申请日：2009-12-25
申请人： Masahiro Sato , Hajime Kawanami , Fujio Mizukami
发明人： Masahiro Sato , Hajime Kawanami , Fujio Mizukami
IPC分类号： C07H5/02 , B01J19/00
CPC分类号： C07H5/02 , A61K51/0491 , B01J19/0093 , B01J2219/00788 , B01J2219/00891 , C07B63/00 , C07H1/00 , Y02P20/544
摘要： The present invention provides: a method for synthesizing a halogen-substituted saccharide from a leaving group-substituted saccharide in a short-time and continuously; a reaction composition; and a device for synthesis of same, i.e., the method being for synthesizing a halogen-substituted saccharide from a leaving group-substituted saccharide by a halogen-substituted saccharide synthesis reaction using a subcritical fluid or a supercritical fluid as the reaction solvent; the reaction composition of the same being an aqueous solution of halogen-substituted saccharide; and the device for synthesis being a device for producing the same, the method being for producing a halogen-substituted saccharide with a subcritical fluid or a supercritical fluid at a temperature of 100 to 400° C. and a pressure of 0.1 to 40 MPa or a mixed solvent of aprotic organic solvent or inorganic solvent mixed therein as the reaction solvent, under catalyst-free condition, by introducing the leaving group-substituted saccharide and the reaction solvent into a circulating-type high-temperature and high-pressure device to produce selectively a halogen-substituted saccharide while reducing the amount of energy consumption and the amount of waste, at high yield, high selectivity, high speed and continuously.
摘要翻译：本发明提供一种短时间连续地从离去基取代的糖中合成卤素取代的糖类的方法，反应组合物; 以及其合成装置，即通过使用亚临界流体或超临界流体作为反应溶剂的卤素取代的糖合成反应从离去基团取代的糖合成卤素取代的糖的方法; 其反应组合物为卤素取代的糖的水溶液; 并且该合成装置是用于制备该装置的方法，该方法用于在100至400℃的温度和0.1至40MPa的压力下用亚临界流体或超临界流体制备卤素取代的糖，或作为反应溶剂混合的非质子有机溶剂或无机溶剂的混合溶剂，在无催化剂条件下，通过将离去基取代的糖和反应溶剂引入循环型高温高压装置中来生产选择性地卤素取代的糖，同时以高产率，高选择性，高速度和连续地降低能量消耗量和废物量。

14. 发明授权

US07879807B2 Tetrasubstituted glucopyranosylated benzene derivatives, medicaments containing such compounds, their use and process for their manufacture 有权
标题翻译：四取代的吡喃葡萄糖基化苯衍生物，含有此类化合物的药物，其用途及其制备方法
公开(公告)号：US07879807B2
公开(公告)日：2011-02-01
申请号：US12527774
申请日：2008-02-20
申请人： Frank Himmelsbach , Matthias Eckhardt , Peter Eickelmann , Leo Thomas
发明人： Frank Himmelsbach , Matthias Eckhardt , Peter Eickelmann , Leo Thomas
IPC分类号： A01N43/04 , A61K31/70 , C07H1/00 , C07H5/02
CPC分类号： C07H7/04
摘要： Tetrasubstituted glucopyranosylated benzene derivatives of general formula (I) as defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.
摘要翻译：包括互变异构体，其立体异构体，其混合物及其盐的如权利要求1所定义的通式（I）的四取代吡喃葡糖基化苯衍生物。根据本发明的化合物适用于治疗代谢性疾病。

15. 发明授权

US07858587B2 Glucopyranosyl-substituted difluorobenzyl-benzene derivates, medicaments containing such compounds, their use and process for their manufacture 有权
标题翻译：吡喃葡萄糖基取代的二氟苄基苯衍生物，含有这些化合物的药物，它们的用途和制造方法
公开(公告)号：US07858587B2
公开(公告)日：2010-12-28
申请号：US12441968
申请日：2007-09-20
申请人： Matthias Eckhardt , Frank Himmelsbach , Peter Eickelmann , Leo Thomas
发明人： Matthias Eckhardt , Frank Himmelsbach , Peter Eickelmann , Leo Thomas
IPC分类号： A01N43/04 , A61K31/70 , C07H1/00 , C07H5/02
CPC分类号： C07H7/04 , C07D309/10
摘要： Glucopyranosyl-substituted difluorobenzyl-benzene derivatives of general formula (I) as defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.
摘要翻译：包括互变异构体，其立体异构体，其混合物及其盐的如权利要求1所定义的通式（I）的吡喃葡糖基取代的二氟苄基 - 苯衍生物。根据本发明的化合物适用于治疗代谢性疾病。

16. 发明申请

US20100285570A1 FLUORIDE PROCESSING METHOD 有权
标题翻译：氟处理方法
公开(公告)号：US20100285570A1
公开(公告)日：2010-11-11
申请号：US12810893
申请日：2008-12-22
申请人： Alexander Jackson , Rajiv Bhalla
发明人： Alexander Jackson , Rajiv Bhalla
IPC分类号： C07H5/02 , C07D487/22 , C09K3/00 , B01J19/00 , C07K2/00 , C07H21/00 , C07K16/00 , C12N1/00 , C12N1/20 , C12N7/00
CPC分类号： C07D487/08 , B01J19/0093 , B01J2219/00781 , C01B9/08 , C07B59/002
摘要： The invention relates to methods for processing [18F]-fluoride target water using a solid-support bound Cryptand of formula (I) and to apparatus for performing such methods. The resultant [18F]-fluoride is useful for preparation of radiopharmaceuticals by nucleophilic fluorination, specifically for use in Positron Emission Tomography (PET).
摘要翻译：本发明涉及使用式（I）的固体支持结合的地埋剂对[18 F] - 氟化物靶水进行处理的方法和用于进行这些方法的装置。所得的[18 F] - 氟化物可用于通过亲核氟化制备放射性药物，特别用于正电子发射断层扫描（PET）。

17. 发明申请

US20090324513A1 Process for Producing Chlorinated Sucrose 审中-公开
标题翻译：生产氯化蔗糖的方法
公开(公告)号：US20090324513A1
公开(公告)日：2009-12-31
申请号：US10593158
申请日：2004-05-20
申请人： Rakesh Ratnam , Shrikant Kulkarni , Suneet Aurora
发明人： Rakesh Ratnam , Shrikant Kulkarni , Suneet Aurora
IPC分类号： C07H5/02 , C13K13/00 , A61K8/72 , A61Q11/00 , B32B1/00 , A23G4/06 , A23G3/36 , A23L2/60 , A23L1/236
CPC分类号： C07H1/06 , C07H5/02 , Y10T428/2982
摘要： Present invention relates to disclosure of application of some innovative techniques useful for substantially improving process efficiency of production of chlorinated sucrose including their intermediates and derivatives. Application of mild methods of drying has been made for recovery of chlorinated sucrose or their intermediates and derivatives, in substantially pure form or with other solid chemical impurities, obtained at various stages in the process of production of chlorinated sucrose. Mild methods of drying included agitated thin film drying, spray drying, freeze drying and super critical extraction. Use of alkoxides has been introduced for deacylation instead of alkali hydroxides or alkaline earth hydroxides. Deacylation has been shown to be effective both, either before or after drying of the reaction mixture. Extraction and purification of desired products i.e. of chlorinated sucrose or its intermediates or derivatives, from dried solid mixtures could be achieved by using appropriate extraction method, including but not limited to solvent extraction and super critical extraction. Further purification of such extracts can be done by crystallization or direct drying under mild conditions.
摘要翻译：本发明涉及一些创新技术的应用的公开，这些创新技术可用于显着提高包括其中间体和衍生物在内的氯化蔗糖生产的工艺效率。在氯代蔗糖生产过程中的不同阶段获得的氯代蔗糖或其中间体和衍生物的应用是以基本上纯的形式或其他固体化学杂质进行的。温和的干燥方法包括搅拌薄膜干燥，喷雾干燥，冷冻干燥和超临界萃取。已经引入了使用烷氧化物来代替碱金属氢氧化物或碱土金属氢氧化物脱醇。在反应混合物干燥之前或之后，已经显示脱酰基化有效。从干燥的固体混合物中提取和纯化所需产物即氯化蔗糖或其中间体或衍生物可以通过使用适当的提取方法来实现，包括但不限于溶剂萃取和超临界萃取。这种提取物的进一步纯化可以通过在温和条件下结晶或直接干燥来进行。

18. 发明申请

US20050203290A1 Crystalline form of sucralose, and method for producing it 审中-公开
标题翻译：三氯半乳蔗糖的结晶形式及其生产方法
公开(公告)号：US20050203290A1
公开(公告)日：2005-09-15
申请号：US11128501
申请日：2005-05-13
申请人： Steven Catani , Carolyn Merkel , Nicholas Vernon
发明人： Steven Catani , Carolyn Merkel , Nicholas Vernon
IPC分类号： C07H1/06 , C07H5/02 , C07H3/00
CPC分类号： C07H5/02 , C07H1/06
摘要： A crystalline form of sucralose, and a method of making it. The method involves continuously crystallizing sucralose from an aqueous solution by a process providing continuous removal and recirculation of the vessel contents, and providing a long residence time for sucralose in the system. The crystals thus formed are of a relatively low length/diameter ratio, have an unsymmetrical shape, and exhibit good stability. The larger crystals in particular are tapered as compared to the rod-like larger crystals in prior art product.
摘要翻译：三氯半乳蔗糖的结晶形式及其制备方法。该方法包括通过提供容器内容物的连续去除和再循环的方法从水溶液中连续结晶三氯蔗糖，并为三氯蔗糖在系统中提供长的停留时间。由此形成的晶体具有相对低的长度/直径比，具有不对称的形状，并表现出良好的稳定性。与现有技术产品中的棒状较大晶体相比，较大的晶体特别是锥形。

19. 发明授权

US06939858B2 Malto-oligosaccharide derivatives and use thereof 失效
标题翻译：麦芽寡糖衍生物及其用途
公开(公告)号：US06939858B2
公开(公告)日：2005-09-06
申请号：US10297408
申请日：2001-06-01
申请人： Riichiro Uchida , Ayako Nasu
发明人： Riichiro Uchida , Ayako Nasu
IPC分类号： A61K31/706 , A61P3/10 , A61P43/00 , C07H3/06 , C07H5/02 , A61K31/70 , C07H17/00
CPC分类号： C07H5/02 , A61K31/706 , C07H3/06
摘要： The present invention provides a substance which strongly inhibits human α-amylase and is effective for the prevention and treatment of hyperglycemia, for example, diabetes and the diseases caused thereby, and an α-amylase inhibitor and a prophylactic or therapeutic agent for hyperglycemia containing the said substance as active principle.Maltoligosaccharide derivatives represented by the following formula: (wherein n is an integer of 0 to 2; m is an integer of 0 to 2; and X represents a hydrogen atom or a hydrophobic group) or their hydrates or physiologically acceptable salts are provided, and they are contained as active principle to prepare an α-amylase inhibitor and a prophylactic or therapeutic agent for hyperglycemia such as diabetes.
摘要翻译：本发明提供了强烈抑制人α-淀粉酶并有效预防和治疗高血糖的物质，例如糖尿病及由此引起的疾病，以及α-淀粉酶抑制剂和含有高糖血症的高血糖症的预防或治疗剂说物质为活性原则。由下式表示的低分子量寡糖衍生物（其中，n为0〜2的整数，m为0〜2的整数，X为氢原子或疏水基）或其水合物或生理上可接受的盐，作为制备α-淀粉酶抑制剂和糖尿病等高血糖症的预防或治疗剂，含有它们作为活性成分。

20. 发明授权

US6013790A Heavily fluorinated sugar analogs 失效
标题翻译：重油糖类似物
公开(公告)号：US6013790A
公开(公告)日：2000-01-11
申请号：US937672
申请日：1997-09-25
申请人： Stephen G. Dimagno
发明人： Stephen G. Dimagno
IPC分类号： C07H5/02 , C07H19/06 , C07H19/16 , C07H19/00
CPC分类号： C07H5/02 , C07H19/06 , C07H19/16
摘要： Heavily fluorinated sugar analogs of formula ##STR1## wherein R.sub.1 is selected from alkyl, alkenyl, aryl, CH.sub.2 OH, --CH.sub.2 --O-alkyl, --CH.sub.2 --O-aryl, --CH.sub.2 OPO.sub.3 H, --CH.sub.2 --O-carbohydrate, --CH.sub.2 --NH-peptide, or --CH.sub.2 --O-peptide;wherein R.sub.2 is selected from hydroxy, --O-carbohydrate, --NH-peptide, ##STR2## wherein R.sub.3 is selected from H, halogen, lower alkyl, lower alkenyl, lower haloalkyl, lower haloalkenyl, amino, mono- or di-lower alkylamino;wherein R.sub.4 is selected from amino, hydroxy, alkoxy, or halogen; andwherein R.sub.5 is H or amino. The compounds of formula (I) are useful as antiviral and antineoplastic agents and the compounds of formula (II) are useful as plant growth inhibitors and herbicides. Also disclosed is a method for preparing the heavily fluorinated sugars of the present invention which utilizes inexpensive starting materials which incorporate the desired number of fluorine moieties and a new reagent, benzyloxymethylzinc bromide, for introducing the 5'-hydroxymethyl moiety. The synthetic method of the present invention is advantageous in that it does not require late stage fluorination step.
摘要翻译：其中R1选自烷基，烯基，芳基，CH2OH，-CH2-O-烷基，-CH2-O-芳基，-CH2OPO3H，-CH2-O-碳水化合物，-CH2-NH-肽，或-CH 2 -O-肽; 其中R2选自羟基，-O-碳水化合物，-NH-肽，其中R 3选自H，卤素，低级烷基，低级烯基，低级卤代烷基，低级卤代烯基，氨基，单 - 或二 - 低级烷基氨基; 其中R 4选自氨基，羟基，烷氧基或卤素; 并且其中R5是H或氨基。式（I）化合物可用作抗病毒和抗肿瘤剂，式（II）化合物可用作植物生长抑制剂和除草剂。还公开了一种制备本发明的重质氟化糖的方法，该方法利用掺有所需数目的氟部分的廉价起始原料和用于引入5'-羟甲基部分的新试剂苄氧基甲基溴化锌。本发明的合成方法的优点在于不需要后期氟化步骤。

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