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31. 发明公开

EP0673947A1 PSICOFURANOSE AND PSICOPYRANOSE DERIVATIVES 失效
标题翻译： PSICOFURANOSE和PSICOPYRANOSE衍生物
公开(公告)号：EP0673947A1
公开(公告)日：1995-09-27
申请号：EP94902104.2
申请日：1993-12-10
申请人： Sankyo Company Limited
发明人： TERASHIMA, Shiro , KATOH, Tadashi 9-1, Minamidai 1-chome , MATSUMOTO, Miyoko
IPC分类号： C07H7/027 , C07H9/04 , C07H15/04 , C07H15/18
CPC分类号： C07H19/04 , C07H7/027 , C07H19/01 , Y02P20/55
摘要： D-psicofuranose and D-psicopyranose derivatives represented by general formulae (I) and (II), useful as the key intermediates in a novel process for producing hydantocidin; wherein R¹ through R⁸ may be the same or different from one another and each represents hydrogen or a hydroxyl-protecting group; and X represents optionally protected hydroxymethyl, carboxyl, carbamoyl or allophanoyl.
摘要翻译：由通式（I）和（II）表示的D-吡喃阿拉伯糖和D-吡吡喃糖衍生物，其可用作生产嗜水菌素新的方法中的关键中间体; 其中R 1至R 6可以相同或不同，各自代表氢或羟基保护基; X代表任选保护的羟甲基，羧基，氨基甲酰基或异戊酰基。

32. 发明公开

EP0232202A3 Process for the oxidation of di-, tri-, oligo- and polysaccharides into polyhydroxycarboxylic acids, the catalyst used and the products so obtained 失效
标题翻译：将DI，TRI，OLIGO和多糖氧化成聚羟基羧酸的方法，使用的催化剂和所得产品
公开(公告)号：EP0232202A3
公开(公告)日：1988-03-09
申请号：EP87400201
申请日：1987-01-29
申请人： Roquette Frères
发明人： Fuertes, Patrick , Fleche, Guy
IPC分类号： C07H07/027 , C07C51/31 , C08B31/18 , C08B15/02
CPC分类号： C08B31/18 , C04B24/06 , C04B24/38 , C04B2103/22 , C04B2103/302 , C07C51/313 , C07H7/027 , C08B15/02 , C07C59/105

33. 发明公开

EP0000243A1 Process for preparing 3,5:4,6- protected derivatives of L- or D- gulonic acid, their use in preparing 2- keto-L- or D- gulonic acid or their esters or L- or D- ascorbic acid, and certain novel 2-nitrato-gulonate intermediates 失效
标题翻译：一种用于3,5-制备方法：4,6-保护的L-或D-古洛糖酸，其为2-的制备中使用的衍生物酮 - L-或D-古洛糖酸或其酯或抗坏血酸和L-或D-新2 -Nitrato古洛糖酸甲酯作为中间体。
公开(公告)号：EP0000243A1
公开(公告)日：1979-01-10
申请号：EP78300017.7
申请日：1978-06-05
申请人： PFIZER INC.
发明人： Crawford, Thomas Charles
IPC分类号： C07D307/62 , C07H7/02 , C07H9/04 , C07D493/04
CPC分类号： C07D493/04 , C07D307/62 , C07H7/027 , C07H9/04
摘要： The invention relates to a process in which a 3,5:4,6-protected derivative of L- or D-glulonic acid is prepared by contacting L- or D-gulono-1,4-lactone with an aldehvde dialkyl acetal, or with an aldehyde and an alcohol, in the presence of an acid having a pKa of less than 3. This protected derivative may be oxidised and hydrolysed to 2-keto-L- or D-gulonic acid or ester thereof, which in turn may be hydrolysed to L- or D-ascorbic acid. L-ascorbic acid is of course Vitamin C. The invention also relates to the novel intermediates produced by the above processes.
摘要翻译：本发明涉及在一个3.5的方法：L-或D-glulonic酸的4,6-保护的衍生物是通过contecting L-或D-古洛糖酸-1,4-内酯与醛二烷基缩醛，或制备与醛和醇，在具有小于3的pKa的酸的存在下进行该保护的衍生物可被氧化和水解成2-酮基L-或D-古洛糖酸或其酯，其又可以是水解以L-或D-抗坏血酸。 L-抗坏血酸是当然维生素C.本发明的因此涉及通过上述方法制备的新的中间体。

34. 发明公开

EP0000092A1 Method of preparing ascorbic acid and intermediates specially adapted for use therein 失效
标题翻译：一种生产抗坏血酸和特别适用于本方法中的中间体的过程。
公开(公告)号：EP0000092A1
公开(公告)日：1978-12-20
申请号：EP78300014.4
申请日：1978-06-02
申请人： PFIZER INC.
发明人： Crawford, Thomas Charles
IPC分类号： C07D307/62 , C07D493/04
CPC分类号： C07D307/33 , C07D307/62 , C07D407/04 , C07D493/04 , C07F7/1852 , C07F7/1856 , C07H7/027 , Y02P20/55
摘要： The invention relates to a process for preparing ascorbic acid in which (a) gulono-, galactono-, idono- or talono-1,4- lactone is reacted with at least one hydroxyl-protecting reagent so as to protected the free hydroxyl groups in the 5-, 6-and either the 2- or 3- positions, or, reacting gulono- or idono-1,4-lactone with at least one hydroxyl-protecting reagent so as to protect the free hydroxyl groups in the 3-, 5- and optionally the 6- positions (b) oxidizing the free hydroxyl group at the 2- or 3- position to oxidize it to an oxo group and (c) hydrolyzing the compound formed in (b) to ascorbic acid. Certain novel intermediates useful in the above process are also covered.
摘要翻译：本发明涉及一种用于在其中制备抗坏血酸（a）中古洛糖酸，galactono-，idono-或talono -1,4-内酯进行反应与至少一种羟基保护试剂，以便在受保护的游离羟基的5-，6-和无论是2-或3-位，或起反应古洛糖酸或idono -1,4-内酯与至少一种羟基保护试剂，以保护游离羟基在3-， 5-和6-位置上的任选的（b）在2-或3-位的氧化的游离羟基基团将其氧化以氧代基和（c）水解（b）中，以抗坏血酸所形成的化合物。因此在上述方法中有用的某些新的中间体都包括在内。

35. 发明公开

EP2706871A1 NUTRITIONAL PRODUCTS COMPRISING HUMAN MILK OLIGOSACCHARIDES AND METHODS FOR MANUFACTURE THEREOF 有权转让
标题翻译：与寡糖来自人乳的及其制造方法FOOD PRODUCTS
公开(公告)号：EP2706871A1
公开(公告)日：2014-03-19
申请号：EP12719746.5
申请日：2012-05-10
申请人： Nestec S.A.
发明人： BRASSART, Dominique , DEKANY, Gyula , ERDMANN, Peter , SCHWARZ, Andrea , SPRENGER, Norbert
IPC分类号： A23L1/29 , C07H3/06 , C07H15/04
CPC分类号： A23L5/00 , A23L7/00 , A23L29/30 , A23L33/00 , A23L33/125 , A23L33/40 , A23V2002/00 , C07H5/06 , C07H7/027 , C07H15/18 , A23V2250/28
摘要： A method for the manufacture of a mixture of human milk oligosaccharides is disclosed. The method involves the catalytic hydrogenolysis of compounds of the general formula 1 and 2. Nutritional substances including the manufactured HMOs are also disclosed.

36. 发明公开

EP2173759A4 OLIGOSIALIC ACID DERIVATIVES, METHODS OF MANUFACTURE, AND IMMUNOLOGICAL USES 审中-公开
标题翻译： OLIGOSIALINSÄÚREDERIVATE，工艺及其使用和它们的免疫学
公开(公告)号：EP2173759A4
公开(公告)日：2014-01-29
申请号：EP08796099
申请日：2008-07-03
申请人： CHILDRENS HOSP & RES CT OAK
发明人： MOE GREGORY R , HAGEN BRENT T
IPC分类号： C07H5/06 , A61K31/7008 , C07H19/00 , C07K2/00 , C07K9/00 , C07K14/00 , C07K16/00 , C07K16/30 , G01N33/574
CPC分类号： A61K39/0258 , A61K39/0011 , A61K39/095 , A61K2039/55505 , A61K2039/55544 , A61K2039/585 , A61K2039/6037 , C07H1/00 , C07H7/027 , C07H13/04 , C07K16/1217 , C07K16/1282 , C08B37/0006 , G01N33/57484 , G01N2333/22 , G01N2333/245 , G01N2400/02
摘要： The invention relates to methods of producing, and compositions comprising, an isolated alpha (2→8) or (2→9) oligosialic acid derivative bearing a non-reducing end enriched for one or more de-N-acetyl residues and resistant to degradation by exoneuraminidase. A representative production method involves: (i) treating an alpha (2→8) or (2→9) oligosialic acid precursor having a reducing end and a non-reducing end with sodium borohydride under conditions for de-N-acetylating the non-reducing end; and (ii) isolating alpha (2→8) or (2→9) oligosialic acid derivative having one or more de-N-acetylated residues and a non-reducing end that is resistant to degradation by exoneuraminidase. Isolated alpha (2→8) or (2→9) oligosialic acid derivatives that comprise a non-reducing end de-N-acetyl residue are provided, as well as antibodies specific for the derivatives, compositions comprising the derivatives, kits, and methods of use including protection against and detection of E. coli K1 and N. meningitidis bacterial infection, and in diagnosing and treating cancer.

37. 发明公开

EP2481746A1 Process for producing sugar chain asparagine derivative 审中-公开
标题翻译： Verfahren zur Herstellung von eines Zuckerketten-Asparaginderivats
公开(公告)号：EP2481746A1
公开(公告)日：2012-08-01
申请号：EP12162076.9
申请日：2002-06-19
申请人： Otsuka Chemical Co., Ltd. , Kajihara, Yasuhiro
发明人： Kajihara, Yasuhiro , Sasaki, Ken
IPC分类号： C07H13/10 , C07H15/12 , C07H5/06 , C07H7/027 , C12P13/04 , C12P19/04
CPC分类号： C07H13/10 , C07H5/06 , C07H7/027 , C07H15/12 , C12P13/04 , C12P19/04 , C12P19/28 , Y02P20/55
摘要： The present invention provides a process for preparing a sugar chain asparagine derivative. According to the process, various isolated sugar chain asparagine derivatives useful in the field of the development of pharmaceutical and the like can be conveniently obtained in a large amount as compared to that of the prior art. The present invention also provides a process for preparing a sugar chain asparagine and a process for preparing a sugar chain via a step for preparing a sugar chain asparagine derivative. The present invention further provides a novel sugar chain asparagine derivative, a sugar chain asparagine and a sugar chain.
摘要翻译：本发明提供了制备糖链天冬酰胺衍生物的方法。根据该方法，与现有技术相比，可以容易地获得用于药物开发领域的各种分离的糖链天冬酰胺衍生物。本发明还提供了制备糖链天冬酰胺的方法和通过制备糖链天冬酰胺衍生物的步骤制备糖链的方法。本发明还提供了一种新型糖链天冬酰胺衍生物，糖链天冬酰胺和糖链。

38. 发明授权

EP2013624B1 METHOD FOR THE IDENTIFICATION OF NEW LEADS FOR DRUG CANDIDATES 有权
标题翻译：方法确定新的候选药物先导化合物
公开(公告)号：EP2013624B1
公开(公告)日：2011-08-03
申请号：EP07733988.5
申请日：2007-03-14
申请人： Universität Basel
发明人： ERNST, Beat , CUTTING, Brian , SHELKE, Sachin V.
IPC分类号： G01N33/68 , C07H7/027 , C07H15/04 , G01R33/465
CPC分类号： G01N33/6845 , C07H7/027 , C07H15/04 , G01N24/088 , G01N2500/00 , G01R33/465
摘要： Disclosed is a method for producing new leads for drug candidates. The method employs a combinatorial approach for identifying high affinity ligands. The target may be unknown and/or may include one or more unknown binding sites. A method involving a combined screening and synthesis method for bi-site inhibitors is disclosed comprising: 1) determining if there is sufficient proximity between ligands binding to different sites of a target: e.g. by using spin-labelled ligands quenching can be measured with NMR if a first ligand and second allosteric ligand are in proximity 2) connecting both ligands having linkers, via in situ synthesis in the presence of the protein scaffold (e.g. target guided synthesis combined with fragment based self assembly). Click chemistry is a preferred embodiment here. Also disclosed are kits used in context of this method, leads discovered by the method and their use in drug development. Leads for drugs acting on myelin associated glycoprotein (MAG) have been identified and synthesised.

39. 发明授权

EP2084172B1 NEUE MIT BENZYLRESTEN SUBSTITUIERTE 1,4-BENZOTHIEPIN-1,1-DIOXIDDERIVATE, VERFAHREN ZU DEREN HERSTELLUNG, DIESE VERBINDUNGEN ENTHALTENDE ARZNEIMITTEL UND DEREN VERWENDUNG 有权
标题翻译： NEW用苄基取代的1,4-苯并硫-1,1-二氧化物的衍生物，用于生产药物含有它们及其用途
公开(公告)号：EP2084172B1
公开(公告)日：2010-12-22
申请号：EP07819434.7
申请日：2007-10-30
申请人： Sanofi-Aventis Deutschland GmbH
发明人： FRICK, Wendelin , GLOMBIK, Heiner , THEIS, Stefan , HEUER, Hubert , SCHAEFER, Hans-Ludwig , KRAMER, Werner
IPC分类号： C07H5/06 , A61K31/7028
CPC分类号： C07H5/06 , A61K31/38 , A61K31/7028 , A61K45/06 , C07D409/12 , C07H5/04 , C07H7/02 , C07H7/027 , C07H13/12 , C07H15/26 , A61K2300/00
摘要： The invention relates to the compounds of formula (I) and to the physiologically acceptable salts thereof. These compounds are suitable, for example, as hypolipidemics.

40. 发明公开

EP2119444A1 THERAPEUTIC AGENT FOR PAIN DISEASE 有权
标题翻译：治疗MITTEL GEGEN SCHMERZEN
公开(公告)号：EP2119444A1
公开(公告)日：2009-11-18
申请号：EP08704491.3
申请日：2008-02-06
申请人： Nippon Zoki Pharmaceutical Co., Ltd.
发明人： NAKAZAWA, Yoshitaka
IPC分类号： A61K31/7012 , A61P25/04 , C07H7/027
CPC分类号： A61K31/7012 , C07H7/027
摘要： Disclosed is an analgesic agent for a non-inflammatory pain disease, which comprises a sialic acid or a pharmaceutically acceptable salt thereof as an active ingredient. The sialic acid which is an active ingredient for the agent has an analgesic effect on a disease model animal of neurogenic pain which is an non-inflammatory pain. Therefore, the analgesic agent is useful as a pharmaceutical agent for the treatment of an non-inflammatory pain disease such as an neurogenic pain disease, e.g., trigeminal neuralgia, postherpetic neuralgia, entrapment neuropathy, complex regional pain syndrome, diabetic neuropathy, traumatic neuropathy, phantom limb pain, central pain after spinal cord injury or stroke, and neuropathy caused by pharmacotherapy or radiation therapy, or the like.
摘要翻译：公开了一种非炎症性疼痛疾病的止痛剂，其包含唾液酸或其药学上可接受的盐作为活性成分。作为药剂的活性成分的唾液酸对作为非炎症性疼痛的神经性疼痛的疾病模型动物具有镇痛作用。因此，止痛剂可用作治疗非炎症性疼痛疾病如神经性疼痛疾病，例如三叉神经痛，带状疱疹后神经痛，包埋神经病，复杂区域性疼痛综合征，糖尿病性神经病，外伤性神经病变，幻肢疼痛，脊髓损伤或中风后的中枢疼痛，以及由药物治疗或放射治疗引起的神经病变等。

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