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1. 发明授权

US06806363B1 Cobalamin conjugates useful as antitumor agents 有权
标题翻译：钴胺素共轭物可用作抗肿瘤剂
公开(公告)号：US06806363B1
公开(公告)日：2004-10-19
申请号：US09690197
申请日：2000-10-16
申请人： Douglas A. Collins , Henricus P. C. Hogenkamp
发明人： Douglas A. Collins , Henricus P. C. Hogenkamp
IPC分类号： C07H2300
CPC分类号： A61K41/0095
摘要： The invention provides cobalamin compounds linked to a neutron capture therapy target (e.g. Boron-10 or Gadolinium-157), and optionally linked to a detectable moiety, as well as pharmaceutical compositions comprising the compounds, and methods for using the compounds in medical diagnosis and therapy.
摘要翻译：本发明提供了与中子捕获治疗靶（例如硼-10或钆157）连接并且任选地连接到可检测部分的钴胺素化合物，以及包含该化合物的药物组合物，以及在医学诊断中使用该化合物的方法治疗。

2. 发明授权

US06262253B1 Vitamin B12 conjugates with gcsf, analogues thereof and pharmaceutical compositions 失效
标题翻译：具有gcsf的维生素B12缀合物，其类似物和药物组合物
公开(公告)号：US06262253B1
公开(公告)日：2001-07-17
申请号：US09244782
申请日：1999-02-05
申请人： Gregory John Russell-Jones , Steven William Westwood
发明人： Gregory John Russell-Jones , Steven William Westwood
IPC分类号： C07H2300
CPC分类号： C07K17/02 , A61K38/00 , A61K47/54 , A61K47/56 , A61K47/58 , C07K14/505 , C07K14/535
摘要： The invention describes complexes between VB12 analogues and either GCSF or EPO that retain both significant affinity for intrinsic factor (IF) in the VB12 portion of the complex and significant bioactivity of the GCSF or EPO portion of the complex. The invention also concerns a process for the synthesis of these complexes. This is achieved at least in part, by using a spacer compound, which is linked covalantly between the VB12 portion and the GCSF or EPO. The complexes preferably have the formula wherein V is vitamin B12 or a vitamin B12 analogue, or derivative, bonded to X either through a carboxylate group pendant to the corrin nucleus of VB12 or through the central cobalt atom or to a functional group introduced onto the VB12 molecule, X is selected from: —NHNH—, —NH—, —O—, —S—, —SS— or —CH2—, and A is an optionally substituted, saturated or unsaturated, branched or linear, C1-50 alkylene, cycloalkylene or aromatic group, optionally with one or more carbons within the linear chain being replaced with N, O or S, and wherein the optional substituents are selected from carbonyl, carboxy, hydroxy, amino and other groups, and Y is the covalent linkage between A and Z where Y is selected from —NHCO—, —CONH—, —CONHNHCO—, —N═N—, —N═CH—, —NHCH2—, —NHN═CH—, —NHNHCH2—, —SS—, —SCH2—, —CH2S—, —NHCRNH—, —COO—, —OCO—, and R is O, S or NH2, and Z is GCSF or EPO. The invention also describes reagents that can be used as probes for the detection of buried thiol groups of a protein or peptide, said reagent comprising a complex of either vitamin B12 (or an analogue thereof) or more generally of any instrumentally or visually detectable label, covalently linked to a diradical spacer, said spacer having a terminal reactive group capable of forming a disulphide bond with a free thiol in said protein or peptides.
摘要翻译：本发明描述了VB12类似物和GCSF或EPO之间的复合物，其在复合物的VB12部分中保留对内在因子（IF）的显着亲和力，并且复合物的GCSF或EPO部分具有显着的生物活性。本发明还涉及合成这些络合物的方法。这通过使用在VB12部分和GCSF或EPO之间共价连接的间隔体化合物至少部分地实现。络合物优选地具有通过从V12的金属核心或通过中心钴原子或通过引入到VB12分子上的官能团的羧酸基团而与X键合的维生素B12或维生素B12类似物或衍生物，X选自：-NHN - ， - NH - ， - O - ， - S - ， - S - 或-CH 2 - ，并且A是任选取代的饱和或不饱和支链或直链C1-50亚烷基，任选与线性链中的一个或多个碳原子被N，O或S取代的环亚烷基或芳基，其中任选的取代基选自羰基，羧基，羟基，氨基和其它基团，Y是 A和Z，其中Y选自-NHCO - ， - CONH - ， - CONHNHCO - ， - N = N-，-N = CH - ， - NHCH 2 - ， - NHN = CH - ， - NHNHCH 2 - ， - S - -SCH 2 - ， - CH 2 S - ， - NHCRNH-，-COO-， - OCO-，R是O，S或NH 2，Z是GCSF或EPO。本发明还描述了可用作检测蛋白质或肽的掩埋硫醇基团的探针的试剂，所述试剂包含维生素B12（或其类似物）或更通常的任何仪器上或视觉上可检测的标记物的复合物，共价连接到双基间隔物上，所述间隔物具有能与所述蛋白质或肽中的游离硫醇形成二硫键的末端反应基团。

3. 发明授权

US06265391B1 Method for preventing peripheral nerve damage 失效
标题翻译：防止周围神经损伤的方法
公开(公告)号：US06265391B1
公开(公告)日：2001-07-24
申请号：US09549756
申请日：2000-04-14
申请人： Victor D. Herbert
发明人： Victor D. Herbert
IPC分类号： C07H2300
CPC分类号： A61K31/714 , A61K2300/00
摘要： A vitamin B12 supplement composition comprising vitamin B12 with and/or without added folic acid that is essentially free of antioxidants, such as vitamin C, as well as iron is disclosed. Also disclosed are methods of using this vitamin composition to prevent brain and nervous system damage, such as peripheral nerve damage, as well as pernicious anemia, such as where such anemia is caused by a deficiency of vitamin B12 deficiency.
摘要翻译：公开了一种维生素B12补充剂组合物，其包含维生素B12和/或不含叶酸，其基本上不含抗氧化剂，例如维生素C，以及铁。还公开了使用这种维生素组合物来防止脑和神经系统损伤的方法，例如周围神经损伤，以及恶性贫血，例如由于缺乏维生素B12缺乏引起的贫血。

4. 发明授权

US06211356B1 Metallocene-phosphoramidite conjugates, process for their preparation and their use 失效
标题翻译：茂金属 - 亚磷酰胺共轭物，其制备方法及其用途
公开(公告)号：US06211356B1
公开(公告)日：2001-04-03
申请号：US09029954
申请日：1998-10-21
申请人： Manfred Wiessler , Dagmar Schütte
发明人： Manfred Wiessler , Dagmar Schütte
IPC分类号： C07H2300
CPC分类号： C07H19/10 , C07F17/00 , C07F17/02 , C07H21/00
摘要： The invention concerns metallocene-phosphoramidite conjugates comprising one or a plurality of metallocenes and one or a plurality of phosphoramidites. The invention further concerns a process for preparing the metallocene-phosphoramidite conjugates and their use.
摘要翻译：本发明涉及包含一种或多种金属茂和一种或多种亚磷酰胺的金属茂 - 亚磷酰胺缀合物。本发明还涉及一种制备茂金属 - 亚磷酰胺缀合物的方法及其应用。

5. 发明授权

US06514407B2 Chloro-, hydroxy- and alkoxysilane derivatives of polysaccharides or oligosaccharides, polymerizable and cross-linkable, their synthesis and their use as sources of novel support materials 失效
公开(公告)号：US06514407B2
公开(公告)日：2003-02-04
申请号：US09808190
申请日：2001-03-15
申请人： Raphael Duval
发明人： Raphael Duval
IPC分类号： C07H2300
CPC分类号： C07B57/00 , C08B15/05 , C08B37/00 , C08B37/0009 , C08B37/0012 , C08B37/0018 , C08B37/0021 , C08B37/0024 , C08B37/003 , C08B37/0054 , C08B37/0057 , Y02P20/544
摘要： There are described chloro-, hydroxy- and alkoxysilane derivatives of polysaccharides or oligosaccharides as novel compounds which are polymerizable and cross-linkable, and a method for obtaining them; novel support materials obtained from said derivatives and containing said silane derivatives of polysaccharides or oligosaccharides chemically grafted by a covalent bond with the support and polymerized and cross-linked in a three-dimensional network and a method for obtaining them; as well as the use of said material supports in separation or in preparation of enantiomers, through employment in gaseous, liquid or supercritical chromatography, by electrophoresis, electrochromatography or by percolation processes through membranes containing said support materials.

6. 发明授权

US06346616B1 Chloro-, hydroxy- and alkoxysilane derivatives of polysaccharides or oligosaccharides, polymerizable and cross-linkable, their synthesis and their use as sources of novel support materials 失效
标题翻译：可聚合和可交联的多糖或寡糖的氯代，羟基和烷氧基硅烷衍生物，它们的合成及其作为新型载体材料的来源
公开(公告)号：US06346616B1
公开(公告)日：2002-02-12
申请号：US09394868
申请日：1999-09-13
申请人： Raphaël Duval
发明人： Raphaël Duval
IPC分类号： C07H2300
CPC分类号： C07B57/00 , C08B15/05 , C08B37/00 , C08B37/0009 , C08B37/0012 , C08B37/0018 , C08B37/0021 , C08B37/0024 , C08B37/003 , C08B37/0054 , C08B37/0057 , Y02P20/544
摘要： There are described chloro-, hydroxy- and alkoxysilane derivatives of polysaccharides or oligosaccharides as novel compounds which are polymerizable and cross-linkable, and a method for obtaining them; novel support materials obtained from said derivatives and containing said silane derivatives of polysaccharides or oligosaccharides chemically grafted by a covalent bond with the support and polymerized and cross-linked in a three-dimensional network and a method for obtaining them; as well as the use of said material supports in separation or in preparation of enantiomers, through employment in gaseous, liquid or supercritical chromatography, by electrophoresis, electrochromatography or by percolation processes through membranes containing said support materials.
摘要翻译：描述了多糖或寡糖的氯代，羟基和烷氧基硅烷衍生物作为可聚合和可交联的新化合物及其获得方法; 从所述衍生物获得的新颖的载体材料，并含有通过与载体共价键化学接枝并在三维网络中聚合和交联的多糖或寡糖的所述硅烷衍生物及其获得方法; 以及通过使用气相，液体或超临界色谱法，通过电泳，电色谱法或通过含有所述载体材料的膜的渗滤方法在分离或制备对映异构体中使用所述材料载体。

7. 发明授权

US06211355B1 Radionuclide labeling of vitamin B12 and coenzymes thereof 有权
标题翻译：维生素B12及其辅酶的放射性核素标记
公开(公告)号：US06211355B1
公开(公告)日：2001-04-03
申请号：US09500780
申请日：2000-02-08
申请人： Douglas A. Collins , Henricus Petrus Hogenkamp
发明人： Douglas A. Collins , Henricus Petrus Hogenkamp
IPC分类号： C07H2300
CPC分类号： C07H23/00 , A61K41/0095 , A61K51/04 , A61K51/0497
摘要： A compound useful for in vivo imaging of organs and tumors is provided of formula: wherein is a cobalamin, is derived from a corrin carboxylic acid group of said cobalamin, Y is a linking group and X is a chelating group, optionally comprising a detectable radionuclide or a paramagnetic metal ion, and n is 1-3.
摘要翻译：用于器官和肿瘤的体内成像的化合物由下式提供：其中钴胺素衍生自所述钴胺素的corrin羧酸基团，Y是连接基团，X是螯合基团，任选地包含可检测的放射性核素或顺磁金属离子，n为1-3。

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