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41. 发明授权

US08802842B2 Method for the preparation of a crystalline form 有权
标题翻译：制备结晶形式的方法
公开(公告)号：US08802842B2
公开(公告)日：2014-08-12
申请号：US12892310
申请日：2010-09-28
申请人： Dirk Weber , Svenja Renner , Tobias Fiedler , Simone Orlich
发明人： Dirk Weber , Svenja Renner , Tobias Fiedler , Simone Orlich
IPC分类号： C07H1/06 , C07H1/08 , C07H15/203 , C07H5/02 , A01N43/04 , A61K31/70
CPC分类号： C07H15/203
摘要： The invention relates to a method for the preparation for a crystalline form of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene. In addition the invention relates to a crystalline form obtainable by this method, to a pharmaceutical composition and to the use thereof for preparing medicaments.
摘要翻译：本发明涉及一种制备1-氯-4-（（R） - D-吡喃葡萄糖-1-基）-2- [4 - （（S） - 四氢呋喃-3-基氧基） - 苄基] - 苯。此外，本发明涉及通过该方法获得的结晶形式，涉及药物组合物及其用于制备药物的用途。

42. 发明申请

US20140187768A1 CHLORINATION OF CARBOHYDRATES AND CARBOHYDRATE DERIVATIVES 审中-公开
标题翻译：碳酸氢盐和碳酸氢盐衍生物的氯化
公开(公告)号：US20140187768A1
公开(公告)日：2014-07-03
申请号：US14198182
申请日：2014-03-05
申请人： Lexington Pharmaceuticals Laboratories, LLC
发明人： William Randal ERICKSON , Stephen Craig FIELDS
IPC分类号： C07H1/00 , C07H5/02
CPC分类号： C07H1/00 , C07H5/02 , C07H13/04
摘要： Disclosed is a method for chlorinating a carbohydrate or a derivative thereof to produce a polychlorinated carbohydrate or a derivative thereof, such as sucralose, the method involves (i) reacting the carbohydrate or derivative thereof with a chlorinating agent to obtain a reaction mixture comprising said polychlorinated carbohydrate or derivative thereof and at least one under-chlorinated carbohydrate or derivative thereof, (ii) returning the at least one under-chlorinated carbohydrate or derivative thereof to a chlorinating step and further chlorinating the at least one under-chlorinated carbohydrate or derivative thereof to obtain the desired polychlorinated carbohydrate or derivative thereof; and (iii) optionally repeating steps (i) and (ii) “n” times where n≧1. The polychlorinated carbohydrate or a derivative thereof is obtained in high yields.
摘要翻译：公开了一种用于氯化碳水化合物或其衍生物以产生多氯代碳水化合物或其衍生物如三氯蔗糖的方法，该方法包括（i）使碳水化合物或其衍生物与氯化剂反应以获得包含所述多氯代碳水化合物或其衍生物和至少一种氯化不足的碳水化合物或其衍生物，（ii）将至少一种下氯化碳水化合物或其衍生物返回到氯化步骤中，并进一步将至少一种下氯化碳水化合物或其衍生物氯化为获得所需的多氯代碳水化合物或其衍生物; 和（iii）任选地重复步骤（i）和（ii）n≥1的“n”倍。以高产率获得多氯代碳水化合物或其衍生物。

43. 发明申请

US20130005956A1 Synthesis of 18F-labeled Tracers in Hydrous Organic Solvents 有权
标题翻译：有机溶剂中18F标记的Tracers的合成
公开(公告)号：US20130005956A1
公开(公告)日：2013-01-03
申请号：US13634708
申请日：2011-04-08
申请人： Umesh Gangadharmath , Joseph Walsh , Hartmuth Kolb
发明人： Umesh Gangadharmath , Joseph Walsh , Hartmuth Kolb
IPC分类号： C07B59/00 , C09K3/00 , C07H5/02 , C07D417/12 , C07D403/06 , C07H19/06
CPC分类号： B01D15/363 , A61K51/04 , A61K51/0448 , A61K51/0453 , A61K51/0455 , A61K51/0459 , A61K51/047 , A61K51/0491
摘要： A method for synthesizing an 18F-labeled probe. The method includes a step of eluting an amount of 18F with a first solvent which includes a predetermined amount of water and at least one organic solvent. In this step, the 18F elutes as an 18F solution. The method also includes a step of using the 18F solution to perform 18F-labeling in the presence of at least one labeling reagent and at least one phase transfer catalyst so as to generate the 18F-labeled probe. In the method, there is no step of drying the 18F starting from a time when the eluting step is performed and ending at a time when the 18F-labeling step is performed.
摘要翻译：合成18F标记的探针的方法。该方法包括用包含预定量的水和至少一种有机溶剂的第一溶剂洗脱一定量的18F的步骤。在这一步中，18F洗脱为18F溶液。该方法还包括使用18F溶液在存在至少一种标记试剂和至少一种相转移催化剂的情况下进行18F标记以产生18F标记的探针的步骤。在该方法中，从执行洗脱步骤的时间开始并且在进行18F标记步骤的时刻结束时，没有干燥18F的步骤。

44. 发明申请

US20120121734A1 COMPOSITIONS CONTAINING SUCRALOSE AND APPLICATION THEREOF 审中-公开
标题翻译：含有磺化物及其应用的组合物
公开(公告)号：US20120121734A1
公开(公告)日：2012-05-17
申请号：US13354229
申请日：2012-01-19
申请人： Maki Inoue , Kazumi Iwai , Naoto Ojima , Takuya Kawai , Mitsumi Kawamoto , Shunsuke Kuribi , Miho Sakaguchi , Chie Sasaki , Kazuhito Shizu , Mariko Shiguryou , Kazutaka Hirao , Miki Fujii , Yoshito Morita , Nobuharu Yasunami , Junko Yoshifuji
发明人： Maki Inoue , Kazumi Iwai , Naoto Ojima , Takuya Kawai , Mitsumi Kawamoto , Shunsuke Kuribi , Miho Sakaguchi , Chie Sasaki , Kazuhito Shizu , Mariko Shiguryou , Kazutaka Hirao , Miki Fujii , Yoshito Morita , Nobuharu Yasunami , Junko Yoshifuji
IPC分类号： A23L1/236 , A61K36/756 , A61K36/718 , A61K36/54 , A61K36/258 , A61K36/233 , A61K36/51 , A61K36/708 , A61K36/8888 , A61K36/25 , C07H5/02 , A61K36/515
CPC分类号： A21D2/08 , A23C11/10 , A23G3/48 , A23J3/04 , A23J3/08 , A23J3/16 , A23J3/18 , A23L13/20 , A23L17/00 , A23L19/00 , A23L33/15
摘要： Novel utilization of sucralose which is a high intense sweetener. Compositions containing sucralose including: sweetening compositions having excellent sweetness qualities based on the characteristics of sucralose; foods with a masked unpleasant smell and unpleasant taste; performance food compositions (viscous food compositions, gel food compositions, emulsified food compositions); foods with improved flavors; preservatives and foods with improved quality of taste; and flavor compositions with improved flavors. Novel utilization of sucralose as a sweetener improver, a masking agent for unpleasant smell/unpleasant taste, a flavor improver, a function improver (viscosity, gelling properties, emulsification properties), a taste characteristic improver, and a flavor improver/enhancer.
摘要翻译：作为高浓度甜味剂的三氯半乳蔗糖的新颖利用。包含三氯半乳蔗糖的组合物包括：基于三氯蔗糖特征的具有优异甜味品质的甜味组合物; 具有掩盖的令人不快的气味和不愉快的味道的食物; 性能食品组合物（粘性食品组合物，凝胶食品组合物，乳化食品组合物）; 口味改善的食物防腐剂和食品质量提高; 和具有改善风味的风味组合物。三氯蔗糖作为甜味剂改良剂，令人不快的气味/不愉快味道的掩蔽剂，风味改良剂，功能改进剂（粘度，胶凝性，乳化性），味觉特征改进剂和风味改良剂/增强剂的新颖利用。

45. 发明申请

US20100322858A1 Radiohaloimatinibs and Methods of Their Synthesis and Use in PET Imaging of Cancers 审中-公开
标题翻译：他们合成和应用于PET成像的放射性卤代西他滨及其方法
公开(公告)号：US20100322858A1
公开(公告)日：2010-12-23
申请号：US12438045
申请日：2007-08-22
申请人： William Bornmann , Mian Alauddin , Juri Gelovani , Pradip Ghosh , Liwei Guo , Dongmei Han , David Maxwell , Uday Mukhopadhyay , Zhenghong Peng , Aleksandr Shavrin , Yunming Ying
发明人： William Bornmann , Mian Alauddin , Juri Gelovani , Pradip Ghosh , Liwei Guo , Dongmei Han , David Maxwell , Uday Mukhopadhyay , Zhenghong Peng , Aleksandr Shavrin , Yunming Ying
IPC分类号： A61K49/04 , C07H5/02
CPC分类号： A61K51/0491
摘要： We disclose methods of synthesizing radiohalidated organic compounds and their use in positron emission tomography (PET) imaging of cancer cells.
摘要翻译：我们公开了合成放射性有机化合物的方法及其在癌细胞正电子发射断层扫描（PET）成像中的应用。

46. 发明申请

US20100290988A1 FLUORINATED FRUCTOSE DERIVATIVES FOR PET IMAGING 有权
标题翻译：用于PET成像的氟化果胶衍生物
公开(公告)号：US20100290988A1
公开(公告)日：2010-11-18
申请号：US12467052
申请日：2009-05-15
申请人： Chris CHEESEMAN , Frederick WEST , Tina GRANT , Brendan TRAYNER , John MERCER , Andrei MANOLESCU
发明人： Chris CHEESEMAN , Frederick WEST , Tina GRANT , Brendan TRAYNER , John MERCER , Andrei MANOLESCU
IPC分类号： A61K51/04 , C07H5/02
CPC分类号： A61K51/0491 , C07B59/002 , C07H1/00 , C07H5/02 , C07H15/04 , C07H23/00
摘要： The present invention is directed to fructose-based radiopharmaceuticals, pharmaceutical compositions comprising same, precursors and methods for preparing same, and methods of using same for diagnostic imaging of cancer cells and non-imaging tracer studies.
摘要翻译：本发明涉及基于果糖的放射性药物，包含其的药物组合物，其前体及其制备方法，以及其用于癌细胞诊断成像和非成像示踪剂研究的方法。

47. 发明申请

US20100184969A1 Process to Prepare Sucralose 审中-公开
标题翻译：制备三氯蔗糖的方法
公开(公告)号：US20100184969A1
公开(公告)日：2010-07-22
申请号：US12084214
申请日：2006-11-07
申请人： Mangesh Rajadhyaksha , Ajit Shirwaiker
发明人： Mangesh Rajadhyaksha , Ajit Shirwaiker
IPC分类号： C07H5/02
CPC分类号： C07H1/00 , C07H1/06 , C07H5/02
摘要： The present invention relates to a process to prepare sucralose. More particularly the said process relates to the production of sucralose, chemically known as, 6-Dichloro-1,6-dideoxy-β-D-fructofuranosyl-4-chloro-4-deoxy-alpha-D-galactopyranoside of formula (1)
摘要翻译：本发明涉及一种制备三氯蔗糖的方法。更具体地说，所述方法涉及化学上称为式（1）的6-二氯-1,6-二脱氧-β-呋喃果糖基-4-氯-4-脱氧-α-D-吡喃半乳糖苷的三氯半乳蔗糖的生产）

48. 发明申请

US20090281294A1 PROCESS FOR PRODUCTION OF COMPOUND LABELED WITH RADIOACTIVE FLUORINE 审中-公开
标题翻译：生产符合放射性荧光的化合物的方法
公开(公告)号：US20090281294A1
公开(公告)日：2009-11-12
申请号：US12086147
申请日：2006-11-30
申请人： Keiichi Hirano , Daisaku Nakamura
发明人： Keiichi Hirano , Daisaku Nakamura
IPC分类号： C07H5/02
CPC分类号： C07B59/00 , A61K51/0491 , C07H5/02 , C07H13/06
摘要： A process for the production of [18F]-TAFDG can produce [18F]-TAFDG in a high radiofluorination yield. A process for the production of an organic compound labeled with radioactive fluorine includes the steps of preparing a reaction solution containing [18F]fluoride ions, a phase transfer catalyst, potassium ions, 1,3,4,6-tetra-O-acetyl-2-O-trifluoromethanesulfonyl-β-D-mannopyranose as a labeling precursor compound and a solvent, and giving a reaction condition to the reaction solution to obtain 1,3,4,6-tetra-O-acetyl-2-[18F]fluoro-2-deoxyglucose, in which the solvent contains water.
摘要翻译：制备[18F] -TAFDG的方法可以以高放射性氟化产率产生[18 F] -TAFDG。制备用放射性氟标记的有机化合物的方法包括以下步骤：制备含有[18 F]氟离子的反应溶液，相转移催化剂，钾离子，1,3,4,6-四-O-乙酰基 - 2-O-三氟甲磺酰基-β-D-吡喃甘露糖作为标记前体化合物和溶剂，并向反应溶液提供反应条件，得到1,3,4,6-四-O-乙酰基-2- [18 F] 氟-2-脱氧葡萄糖，其中溶剂含有水。

49. 发明授权

US06933382B2 Process for the synthesis of 2-deoxy-D-glucose 失效
标题翻译：合成2-脱氧-D-葡萄糖的方法
公开(公告)号：US06933382B2
公开(公告)日：2005-08-23
申请号：US10392396
申请日：2003-03-20
申请人： Hari Babu Mereyala , Mamidyala Sreeman Kumar
发明人： Hari Babu Mereyala , Mamidyala Sreeman Kumar
IPC分类号： C07H1/00 , C07H5/02 , C12P19/02 , C13K1/00
CPC分类号： C07H5/02
摘要： The present invention provides a process for the synthesis of 2-deoxy-D-glucose comprising haloalkoxylation of R-D-Glucal wherein R is selected from H and 3, 4, 6-tri-O-benzyl, to obtain alkyl 2-deoxy-2-halo-R-α/β-D-gluco/mannopyranoside, converting alkyl 2-deoxy-2-halo-R-α/β-D-gluco/mannopyranoside by reduction to alkyl 2-deoxy-α/β-D-glucopyranoside, hydrolysing alkyl 2-deoxy-α/β-D-glucopyranoside to 2-deoxy-D-glucose.
摘要翻译：本发明提供了一种合成2-脱氧-D-葡萄糖的方法，其包括RD-葡萄糖的卤代烷氧基化，其中R选自H和3,4,6-三-O-苄基，得到烷基2-脱氧-2 α-卤代-β-D-吡喃葡萄糖苷/甘露聚糖苷，通过还原为2-脱氧-α-β-D-吡喃葡萄糖苷烷基，将2-脱氧-2-卤代-β-D-吡喃葡萄糖苷/ 吡喃葡萄糖苷，水解的2-脱氧-α-β-D-吡喃葡萄糖苷到2-脱氧-D-葡萄糖。

50. 发明授权

US06890581B2 Methods for buffer stabilized aqueous deacylation 有权
标题翻译：缓冲液水解脱酰基的方法
公开(公告)号：US06890581B2
公开(公告)日：2005-05-10
申请号：US10116758
申请日：2002-04-05
申请人： Nicholas M. Vernon , Edward Micinski , Steven J. Catani , Juan L. Navia
发明人： Nicholas M. Vernon , Edward Micinski , Steven J. Catani , Juan L. Navia
IPC分类号： A23L2/60 , A23L27/30 , C07H1/00 , C07H1/06 , C07H5/02 , A23G3/00
CPC分类号： C07H5/02 , A23L2/60 , A23L27/37 , C07H1/06
摘要： The present invention relates to novel methods for stabilizing aqueous deacylation, via use of buffers in the production of sucralose. The present invention provides a process for producing sucralose from an acyl-sucralose compound whereby the acyl-sucralose compound is deacylated in the presence of a buffering agent, which stabilizes the pH of the feed mixture and decreases the accumulation of undesired anhydro compounds. Further, the present invention provides a process whereby the acyl-sucralose compound is deacylated directly either prior to or after removal of the tertiary amide reaction vehicle from the neutralized chlorination feed mixture. An aqueous solution of sucralose including salts and other compounds is produced, from which sucralose is recovered by extraction and purified by crystallization.
摘要翻译：本发明涉及通过在制备三氯蔗糖中使用缓冲液来稳定水解性脱酰基的新方法。本发明提供了由酰基 - 三氯蔗糖化合物制备三氯半乳蔗糖的方法，其中酰基 - 三氯蔗糖化合物在缓冲剂存在下脱酰基化，其稳定了进料混合物的pH并降低了不期望的脱水化合物的积累。此外，本发明提供了一种方法，其中酰基 - 三氯蔗糖化合物在从中和的氯化进料混合物中除去叔酰胺反应介质之前或之后直接脱酰基化。产生包括盐和其它化合物的三氯半乳蔗糖水溶液，通过萃取回收三氯蔗糖并通过结晶纯化。

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