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41. 发明申请

WO2017205269A1 HALOALKYL FUCOSE-CONTAINING SELECTIN ANTAGONISTS 审中-公开
标题翻译： HALOALKYL含果糖选择性拮抗剂
公开(公告)号：WO2017205269A1
公开(公告)日：2017-11-30
申请号：PCT/US2017/033793
申请日：2017-05-22
申请人： GLYCOMIMETICS, INC.
发明人： ERNST, Beat , VARGA, Norbert , SMIESKO, Martin , WAGNER, Beatrice , PETERSON, John M. , MAGNANI, John L.
IPC分类号： C07H15/22 , C07H15/26 , A61K31/70 , A61K31/7028 , A61P35/00 , A61P43/00
摘要： Compounds of Formula (I), compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed. For example, haloalkyl fucose-containing E-selectin antagonists and compositions comprising at least one such agent are described.
摘要翻译：通过抑制E-选择素与E-选择素的结合来治疗和/或预防至少一种疾病，病症和/或病症的式（I）化合物，组合物和方法配体。例如，描述了含卤代烷基岩藻糖的E-选择素拮抗剂和包含至少一种此类试剂的组合物。

42. 发明申请

WO2015084846A1 HIGH TEMPERATURE SELECTION OF NUCLEOTIDE-SUPPORTED CARBOHYDRATE VACCINES AND RESULTING GLYCOSYLATED OLIGONUCLEOTIDES 审中-公开
标题翻译：高温选择核糖体支持的碳酸氢盐疫苗和结果糖苷化寡核苷酸
公开(公告)号：WO2015084846A1
公开(公告)日：2015-06-11
申请号：PCT/US2014/068158
申请日：2014-12-02
申请人： BRANDEIS UNIVERSITY
发明人： KRAUSS, Isaac, J.
IPC分类号： C07H15/22 , C07H21/04 , C12N15/10
CPC分类号： C07H21/04 , Y02A50/57
摘要： The invention relates to an oligonucleotide including one or more modified nucleoside bases having the structure — B— L— A wherein for each of the modified nucleosides A is independently a monosaccharide or oligosaccharide, L is a linker molecule, and B is independently a pyrimidine or pyridine base linked to the sugar-phosphate backbone of the oligonucleotide; and wherein the oligonucleotide binds specifically to a carbohydrate-binding monoclonal antibody with an affinity of less than 100 nM. Immunogenic conjugates that include the oligonucleotide, and pharmaceutical compositions that include the oligonucleotide or the immunogenic conjugate are also disclosed. Various method of using the oligonucleotides, immunogenic conjugates, and pharmaceutical compositions are disclosed, including inducing an immune response, inhibiting viral or bacterial infection, treating a cancerous condition, and detecting a neutralizing antibody. A method is also disclosed for selecting the oligonucleotides using an alternative Selection of Modified Aptamers (SELMA).
摘要翻译：本发明涉及包含一个或多个具有以下结构的修饰的核苷碱基的寡核苷酸：其中对于每个修饰的核苷A，独立地是单糖或寡糖，L是连接分子，B独立地是嘧啶或与寡核苷酸的糖 - 磷酸骨架连接的吡啶碱基; 并且其中寡核苷酸以小于100nM的亲和力特异性结合与碳水化合物结合的单克隆抗体。还公开了包含寡核苷酸的免疫原性缀合物和包含寡核苷酸或免疫原性缀合物的药物组合物。公开了使用寡核苷酸，免疫原性缀合物和药物组合物的各种方法，包括诱导免疫应答，抑制病毒或细菌感染，治疗癌症和检测中和抗体。还公开了使用修饰的选择性选择（SELMA）来选择寡核苷酸的方法。

43. 发明申请

WO2015000132A1 表阿霉素的制备方法及其中间体审中-公开
公开(公告)号：WO2015000132A1
公开(公告)日：2015-01-08
申请号：PCT/CN2013/078672
申请日：2013-07-02
申请人：浙江海正药业股份有限公司
发明人：严伟 , 童万增 , 王建平 , 杨伟强 , 钱宏冠
IPC分类号： C07H15/22
CPC分类号： C07H15/252
摘要：本发明提供了一种制备表阿霉素的方法及与谅方法相适应的中间体。所述制备方法可包括：使叔丁基二甲基氯硅梡与N-三氟乙酰基阿霉素反应获得化合物1 N-三氟乙酰基-14-O-叔丁基二甲基硅基阿霉素；氧化化合物1获得化合物2 4'-酮-N-三氟乙酰基-14-O-叔丁基二甲基硅基阿霉素；还原化合物2获得化合物3 N-三氟乙酰基-14-O-叔丁基二甲基硅基表阿霉素；以及随后由化合物3经脱保护和水解反应制备获得表阿霉素。本发明的方法不仅成本低、反应步骤少、收率和产物纯度高，而且还避免了传统方法经由溴化反应时产生的严重污染。

44. 发明申请

WO2012012339A2 GLYCOSYLATED ACETAMINOPHEN PRO-DRUG ANALOGS 审中-公开
标题翻译：甘氨酸乙酰胺类药物类似物
公开(公告)号：WO2012012339A2
公开(公告)日：2012-01-26
申请号：PCT/US2011/044383
申请日：2011-07-18
申请人： NUTEK PHARMA LTD. , SHULL, Brian , BALDWIN, John , GOPALASWAMY, Ramesh , HAROON, Zishan
发明人： SHULL, Brian , BALDWIN, John , GOPALASWAMY, Ramesh , HAROON, Zishan
IPC分类号： A61K31/7036 , C07H15/22 , A61P25/04
CPC分类号： C07H15/203
摘要： The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug analogs of the analgesic acetaminophen. This invention relates to a method for the production of a broad group of glycosides of acetaminophen derivatives.
摘要翻译：本发明涉及用于合成，制备和使用止痛对乙酰氨基酚的前药类似物的方法和组合物。本发明涉及一种生产广泛的对乙酰氨基酚衍生物糖苷的方法。

45. 发明申请

WO2010126435A1 NOVEL GALACTOSIDE INHIBITORS OF GALECTINS 审中-公开
标题翻译：新型糖皮质激素抑制剂
公开(公告)号：WO2010126435A1
公开(公告)日：2010-11-04
申请号：PCT/SE2010/050458
申请日：2010-04-26
申请人： FORSKARPATENT I SYD AB , LEFFLER, Hakon , NILSSON, Ulf J. , VON WACHENFELDT, Henrik
发明人： LEFFLER, Hakon , NILSSON, Ulf J. , VON WACHENFELDT, Henrik
IPC分类号： C07H15/22 , A61K31/7028 , A61K31/7056 , A61P19/02 , A61P29/00 , A61P35/00 , C07H19/056 , C07H5/06
CPC分类号： C07H15/207 , C07H15/22 , C07H19/056
摘要： The present invention relates to novel compounds having an effect as i.a. galectin inhibitors, to the use of said compounds as a medicament as well as for the manufacture of a medicament for treatment of disorders relating to the binding of galectin to receptors in a mammal, where in said galectin is preferably a galectin-3. The novel compounds are defined by the general formula: (I)
摘要翻译：本发明涉及具有如下效果的新化合物。半乳凝素抑制剂，所述化合物作为药物的用途以及制备用于治疗与半乳凝素与哺乳动物中的受体结合有关的病症的药物，其中所述半乳凝素优选为半乳凝素-3。新化合物由以下通式定义：（I）

46. 发明申请

WO01089532A1 PREPARATION OF FAGOPYRITOLS AND USES THEREFOR 审中-公开
标题翻译：吡咯啉的制备及其用途
公开(公告)号：WO01089532A1
公开(公告)日：2001-11-29
申请号：PCT/US2001/016683
申请日：2001-05-22
IPC分类号： A61K31/70 , A61K31/7034 , A61K36/70 , A61P3/10 , C07H1/08 , C07H15/207 , C07H3/04 , C07H3/06 , C07H15/22
CPC分类号： C07H15/207 , A61K31/70 , C07H1/08 , Y10S514/866 , A61K2300/00
摘要： The present invention describes isolated Fagopyritol A1, isolated Fagopyritol A3, and isolated Fagopyritol B3. Compositions which include two or more of Fagopyritol A1, Fagopyritol A2, Fagopyritol A3, Fagopyritol B1, Fagopyritol B2, Fagopyritol B3, and D- chiro -inositol, at least one of which is an isolated Fagopyritol A1, isolated Fagopyritol A3, or isolated Fagopyritol B3, are also disclosed. Methods for preparing substantially pure Fagopyritol A1, Fagopyritol A3, Fagopyritol B3, or mixtures thereof from buckwheat are also described. The fagopyritols can be used to prepare pharmaceutical compositions, the administration of which can be used to treat diabetes.
摘要翻译：本发明描述了分离的Fagopyritol A1，分离的Fagopyritol A3和分离的Fagopyritol B3。组合物，其包含Fagopyritol A1，Fagopyritol A2，Fagopyritol A3，Fagopyritol B1，Fagopyritol B2，Fagopyritol B3，以及D- <！ - SIPO - >醇，其中至少一种是分离的Fagopyritol A1，分离的Fagopyritol A3或分离的Fagopyritol B3也被公开。还描述了从荞麦制备基本上纯的Fagopyritol A1，Fagopyritol A3，Fagopyritol B3或其混合物的方法。吡咯并吡喃可用于制备药物组合物，其施用可用于治疗糖尿病。

47. 发明申请

WO99007720A2 A PROCESS FOR THE PURIFICATION OF ACARBOSE 审中-公开
标题翻译：一种治疗丙肝的方法
公开(公告)号：WO99007720A2
公开(公告)日：1999-02-18
申请号：PCT/IB1998/001188
申请日：1998-08-03
IPC分类号： C07H15/203 , A61K31/7028 , A61K31/7034 , A61P3/10 , C07H15/22 , C07H15/00
CPC分类号： C07H15/22
摘要： The present invention discloses a process for the purification of acarbose comprising loading a prepurified acarbose solution on a chromatography column packed with a non-aromatic strong acid cation exchanger which is hydrophilic and has high mass transfer and subsequent elution.
摘要翻译：本发明公开了一种用于净化阿卡波糖的方法，其包括将填充有亲水性且具有高质量转移和随后洗脱的非芳香族强酸阳离子交换剂的色谱柱上的预纯化的阿卡波糖溶液加载。

48. 发明申请

WO9534571A3 DRUG SALTS 审中-公开
标题翻译：药物销售
公开(公告)号：WO9534571A3
公开(公告)日：1996-05-02
申请号：PCT/EP9502254
申请日：1995-06-09
申请人： DUMEX LTD AS , DYRSTING HJARNE , KOCH TORBEN , PETERSEN KIM VOULUND
发明人： DYRSTING HJARNE , KOCH TORBEN , PETERSEN KIM VOULUND
IPC分类号： A61K31/66 , A61K31/70 , A61K31/715 , A61K38/12 , A61K38/14 , A61K45/06 , C07C237/26 , C07F9/117 , C07H5/10 , C07H11/00 , C07H11/04 , C07H15/22 , C07H15/232 , C07H15/234 , C07H15/236 , C07H15/238 , C07H17/08 , C08B37/02 , A61K47/48
CPC分类号： C07H17/08 , A61K31/66 , A61K31/70 , A61K31/715 , A61K38/12 , A61K38/14 , A61K45/06 , C07C237/26 , C07F9/117 , C07H5/10 , C07H11/00 , C07H11/04 , C07H15/22 , C07H15/232 , C07H15/234 , C07H15/236 , C07H15/238 , C08B37/0021
摘要： It has been found that sugar acid salts represent beneficial controlled release forms for basic organic drug compounds. Examples of appropriate salts include mono, di, oligo and polysaccharide poly-O-sulphonic acid salts of antibiotics such as tetracyclins.

49. 发明申请

WO9015810A3 IMPROVED PROCESS FOR PREPARING ISEPAMICIN 审中-公开
标题翻译：制备异丙孕酮的改进方法
公开(公告)号：WO9015810A3
公开(公告)日：1991-04-04
申请号：PCT/US9003328
申请日：1990-06-19
申请人： SCHERING CORP
发明人： TANN CHOU-HONG , THIRUVENGADAM TIRUVETTIPURAM K , CHIU JOHN SZE-HUNG , COLON CESAR , GREEN MICHAEL D
IPC分类号： C07D277/74 , C07B43/06 , C07C233/47 , C07C237/10 , C07H13/04 , C07H15/12 , C07H15/22 , C07H15/236 , C07H15/26
CPC分类号： C07H15/236 , C07H15/26 , Y02P20/55
摘要： An improved process for converting gentamicin B to isepamicin comprising forming 3,6'-di-N-formylgentamicin B, acylating the 1-amino group with an N-protected (S)-isoserine compound and removing all the blocking groups under conditions which result in high yields of isepamicin. A novel formylating agent, 2-formylmercaptobenzothiazole, and intermediate compounds are also disclosed.

50. 发明申请

WO1984001386A1 NEW AMINE GLUCOCYDE DERIVATIVES, PREPARATION AND UTILIZATION METHOD 审中-公开
标题翻译：新型氨基葡糖苷衍生物，制备和利用方法
公开(公告)号：WO1984001386A1
公开(公告)日：1984-04-12
申请号：PCT/CH1983000107
申请日：1983-09-23
申请人： SANDOZ AG
发明人： SANDOZ AG , LOIBNER, Hans , STREICHER, Wolfgang , STÜTZ, Peter
IPC分类号： C07H15/22
CPC分类号： C07H15/224 , C07H15/234
摘要： New amine glucoside derivatives having the formula (I), wherein R1 is hydrogen or a group having the formula (II, IIa, IIb, IIc), R2 is OH or NH2, R3 is hydrogen or OH, R4 is hydrogen or OH, R5 is an amino, methyl amino, dimethylamino group or, when R2 is the amino group, a hydroxyl group and R6 is hydrogen or a methyl group, and their acid addition salts; method for producing bonds having the formula (I) and their acid addition salts, as well as a utilization thereof.

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