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1. 发明授权

US06590085B1 Derivatives of monosaccharides as cell adhesion inhibitors 失效
标题翻译：单糖衍生物作为细胞粘附抑制剂
公开(公告)号：US06590085B1
公开(公告)日：2003-07-08
申请号：US09276368
申请日：1999-03-25
申请人： Sudershan K Arora , Nawal Kishore , Jang Bahadur Gupta , Vishwas D Joshi
发明人： Sudershan K Arora , Nawal Kishore , Jang Bahadur Gupta , Vishwas D Joshi
IPC分类号： C07H1500
CPC分类号： C07H9/04
摘要： This invention relates generally to compounds and processes for synthesizing derivatives of 2-3-O-isopropylidene-&agr;-L-xylo-2-hexulofuranosonic acid. The compounds of this invention are useful, inter-alia, for the inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies, including inflammatory and autoimmune diseases, such as bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection and psoriasis. This invention also relates to pharmacological compositions containing derivatives of 2-3-O-isopropylidene-&agr;-L-xylo-2-hexulofuranosonic acid and the methods of treating such pathologies as listed above.
摘要翻译：本发明一般涉及用于合成2-3-O-异亚丙基-α-L-木糖-2-己二硼酸的衍生物的化合物和方法。本发明的化合物尤其用于抑制和预防细胞粘附和细胞粘附介导的病理学，包括炎性和自身免疫性疾病，例如支气管哮喘，类风湿性关节炎，I型糖尿病，多发性硬化，同种异体移植排斥和牛皮癣。本发明还涉及含有2-3-O-异亚丙基-α-L-木糖-2-己二酮酸的衍生物的药理学组合物和治疗上述病理学的方法。

2. 发明授权

US06479650B1 Fluorescent nucleoside analogs and combinatorial fluorophore arrays comprising same 有权
标题翻译：荧光核苷类似物和包含其的组合荧光团阵列
公开(公告)号：US06479650B1
公开(公告)日：2002-11-12
申请号：US09461636
申请日：1999-12-14
申请人： Eric T. Kool
发明人： Eric T. Kool
IPC分类号： C07H1500
CPC分类号： C07H21/00 , C07H7/06 , Y10S436/80 , Y10T436/143333
摘要： The present invention provides fluorescent nucleoside analogs which comprise a fluorescent cyclic compound joined to a carbon of a sugar molecule such as pentose, hexose, ribose or deoxyribose or analogs thereof in either an &agr; or &bgr; configuration. The subject compounds are useful as probes in the study of the structure and dynamics of nucleic acids and their complexes with proteins. In addition, the subject compounds are useful in any technique which uses labeled oligonucleotides for detection. Non-fluorescent spacer molecules in which a cyclohexane, cyclohexene, decalin, or benzene is joined to a carbon of a sugar moiety such as pentose, hexose, ribose or deoxyribose are also provided. Also provided are the 5′ dimethoxytrityl-3′-O-phosphoramidite derivatives, suitable for incorporation into oligonucleotides by automated synthesizers. Combinatorial fluorophore array (CFA) libraries comprising oligomers of the subject nucleoside analogs attached to one or more solid supports are also provided as are methods of selecting fluorophores from the CFA libraries. The present invention also provides oligonucleotide analogs comprising one or more of the subject nucleoside analogs in place of a DNA or RNA base.
摘要翻译：本发明提供荧光核苷类似物，其包含以α或β构型连接到糖分子如戊糖，己糖，核糖或脱氧核糖或其类似物的碳的荧光环化合物。主题化合物可用作研究核酸及其与蛋白质的配合物的结构和动力学的探针。此外，本发明化合物可用于使用标记的寡核苷酸进行检测的任何技术。还提供了其中环己烷，环己烯，十氢化萘或苯连接到糖部分的碳如戊糖，己糖，核糖或脱氧核糖的非荧光间隔分子。还提供了适用于通过自动合成仪并入寡核苷酸的5'二甲氧基三苯甲基-3'-O-亚磷酰胺衍生物。还提供了包含与一种或多种固体支持物连接的受试者核苷类似物的寡聚体的组合荧光团阵列（CFA）文库，其方法是从CFA文库中选择荧光团。本发明还提供了包含一种或多种目标核苷类似物代替DNA或RNA碱基的寡核苷酸类似物。

3. 发明授权

US06469148B1 Process for large scale preparation of sphingosines and ceramides 失效
标题翻译：用于大规模制备鞘氨醇和神经酰胺的方法
公开(公告)号：US06469148B1
公开(公告)日：2002-10-22
申请号：US09568387
申请日：2000-05-10
申请人： Elimelech Rochlin
发明人： Elimelech Rochlin
IPC分类号： C07H1500
CPC分类号： C07H9/04 , C07B2200/07 , C07C213/00 , C07C231/08 , C07C231/18 , C07H15/10 , C07C215/06 , C07C215/24 , C07C233/18
摘要： Synthetic methods for convenient large scale preparation of D-erythro sphingosines and ceramides of high isomeric purity are described.
摘要翻译：描述了方便大规模制备高异构纯度的D-赤型鞘氨醇和神经酰胺的合成方法。

4. 发明授权

US06316606B1 Polymeric compound comprising glycopolymer and a method for decomposing the same 失效
标题翻译：含聚合物的聚合物及其分解方法
公开(公告)号：US06316606B1
公开(公告)日：2001-11-13
申请号：US08878128
申请日：1997-06-18
申请人： Hiroyoshi Kishi , Toyoko Kobayashi , Kiyoshi Sakai , Norio Kaneko , Kazumi Tanaka , Chieko Mihara , Toshihiko Takeda , Yoshihiko Kikuchi
发明人： Hiroyoshi Kishi , Toyoko Kobayashi , Kiyoshi Sakai , Norio Kaneko , Kazumi Tanaka , Chieko Mihara , Toshihiko Takeda , Yoshihiko Kikuchi
IPC分类号： C07H1500
CPC分类号： C08G63/672 , C08B37/00 , C08G18/6484 , Y02P20/582
摘要： The present invention is an enzyme-decomposable polymer compound having recyclable decomposition products. The polymeric compound is a glycopolymer of a saccharide having only glucopyranose rings and a second component. In addition, the glycopolymer may contain molecular chains having at least one type of repeating unit, which chains are crosslinked by a saccharide having only glucopyranose rings.
摘要翻译：本发明是具有可回收分解产物的可分解酶的高分子化合物。高分子化合物是仅具有吡喃葡萄糖环的糖的糖聚合物和第二成分。此外，甘油聚合物可以含有具有至少一种类型的重复单元的分子链，该链由仅具有吡喃葡萄糖环的糖交联。

5. 发明授权

US06765089B1 Protecting and linking groups for organic synthesis on solid supports 失效
标题翻译：有机合成的保护和连接基团
公开(公告)号：US06765089B1
公开(公告)日：2004-07-20
申请号：US09509105
申请日：2000-03-20
申请人： Istvan Toth , Gyula Dekany , Barry Kellam
发明人： Istvan Toth , Gyula Dekany , Barry Kellam
IPC分类号： C07H1500
CPC分类号： C07H15/12 , C07D239/62
摘要： This invention relates to methods for synthesis of organic compounds, and in particular to compounds useful as protecting and linking groups for use in the synthesis of peptides, oligosaccharides, glycopeptides and glycolipids. The invention provides protecting and linking groups that are useful in both solid phase and solution synthesis, and are particularly applicable to combinatorial synthesis.
摘要翻译：本发明涉及有机化合物的合成方法，特别是涉及用于合成肽，寡糖，糖肽和糖脂的保护和连接基团的化合物。本发明提供了可用于固相和溶液合成的保护和连接基团，并且特别适用于组合合成。

6. 发明授权

US06423834B1 KDO aldolase and condensation reactions employed therewith 失效
标题翻译： KDO醛缩酶和与其一起使用的缩合反应
公开(公告)号：US06423834B1
公开(公告)日：2002-07-23
申请号：US09247164
申请日：1999-02-09
申请人： Chi-Huey Wong , Takeshi Sugai , Gwo-Jenn Shen
发明人： Chi-Huey Wong , Takeshi Sugai , Gwo-Jenn Shen
IPC分类号： C07H1500
CPC分类号： C12P19/02 , C07H7/027 , C12N9/88 , C12P7/58 , C12P9/00 , Y10S435/822
摘要： Aureobacterium barkerei strain KDO-37-2 (ATCC 49977) and KDO aldolase (EC 4.1.2.23) isolated therefrom are disclosed. The KDO aldolase is further disclosed to have a broad substrate specificity with respect to its reverse reaction, i.e. the condensation of aldoses with pyruvate to form a wide range of 2-keto-3-deoxy-onic acids, including 2-keto-3-deoxy-nonulosonic acid, 2-keto-3-deoxy-octulosonic acid, 2-keto-3-deoxy-heptulosonic acid, and 2-keto-3-deoxy-hexulosonic acid. In particular, 3-deoxy-D-manno-2-octulosonic acid (D-KDO), a vital component of lipopolysaccharides found in the bacterial outer membrane may be synthesized from D-arabinose and pyruvate in 67% yield. Additionally, protected forms of the KDO aldolase products, e.g. hexaacetyl 2-keto-3-deoxy-nonulosonic acid and pentaacetyl 2-keto-3-deoxy-octulosonic acid, may be decarboxylated to form the corresponding 2-deoxy-aldoses, e.g. 2-deoxy-octulose and 2-deoxy-heptulose respectively.
摘要翻译：公开了从其分离的巴氏杆菌菌株KDO-37-2（ATCC 49977）和KDO醛缩酶（EC 4.1.2.23）。进一步公开KDO醛缩酶相对于其逆反应具有广泛的底物特异性，即醛糖与丙酮酸的缩合形成宽范围的2-酮-3-脱氧ic酸，包括2-酮-3- 脱氧 - 非酮酸，2-酮-3-脱氧 - 八环酮酸，2-酮-3-脱氧 - 庚酮酸和2-酮-3-脱氧 - 己酸。特别地，在D-细菌外膜中发现的脂多糖的重要组分3-脱氧-D-壬烯-2-辛酮酸（D-KDO）可由D-阿拉伯糖和丙酮酸合成，产率67％。另外，保护形式的KDO醛缩酶产物，例如，六乙酰基2-酮-3-脱氧 - 非酮酸和五乙酰基2-酮-3-脱氧 - 八环酸可以脱羧以形成相应的2-脱氧醛糖，例如， 2-脱氧 - 八酮糖和2-脱氧 - 七氟醚。

7. 发明授权

US06403777B1 Metalloligands for cleaving nucleic acids 失效
标题翻译：用于切割核酸的金属配体
公开(公告)号：US06403777B1
公开(公告)日：2002-06-11
申请号：US09348225
申请日：1999-07-06
申请人： James A. Cowan
发明人： James A. Cowan
IPC分类号： C07H1500
CPC分类号： C07H23/00
摘要： Transition metal complexes, referred to hereinafter as “metalloligands”, that catalyze the degradation of DNA and the cleavage of RNA at select sites are provided. In one embodiment, the metalloligand has the following structure: wherein R1 is an amino group, i.e. an NH, or an alkylamino group comprising 1 or 2 carbon atoms; wherein R2 is selected from the group consisting of an amino group, a hydroxyl group, i.e., O(H), an alkylamino group comprising 1 or 2 carbon atoms; and an alkylhydroxyl group comprising 1 or 2 carbon atoms; wherein J is a ligand which comprises at least one carbon-containing five-membered or six-membered ring structure; and wherein M is a transition metal ion which is bound via coordinate bonds to R1 and R2. In another embodiment the metalloligand has the following structure: wherein R1′ and R1″ are the same or different and wherein R1′ and R1″ are an amino group or an alkylamino group comprising 1 or 2 carbon atoms; wherein R2′ and R2″ are the same or different and wherein R2′ and R2″ are selected from the group consisting of an amino group, a hydroxyl group, an alkylamino group comprising 1 or 2 carbon atoms, and an alkylhydroxyl group comprising one or two carbon atoms; wherein J′ and J″ are the same or different and wherein J′ and J″ are ligands which comprise at least one carbon-containing five-membered or six-membered ring structure; and wherein M is a transition metal ion which is bound via coordinate bonds to R1′, R1″, R2′ and R2″. Methods of cleaving nucleic acids using the metalloligands are also provided.
摘要翻译：提供了以下称为“金属配体”的过渡金属络合物，其催化DNA的降解和选择位点处的RNA的切割。在一个实施方案中，金属配体具有以下结构：其中R 1是氨基，即NH，或包含1或2个碳原子的烷基氨基; 其中R2选自氨基，羟基，即O（H），含有1或2个碳原子的烷基氨基; 和含有1或2个碳原子的烷基羟基; 其中J是包含至少一个含碳的五元或六元环结构的配体; 并且其中M是通过配位键与R 1和R 2结合的过渡金属离子。在另一个实施方案中，金属配体具有以下结构：其中R1'和R1“相同或不同，并且其中R1'和R1” 氨基或含有1或2个碳原子的烷基氨基; 其中R2'和R2“相同或不同，并且其中R2'和R2”选自氨基，羟基，包含1或2个碳原子的烷基氨基，和烷基羟基，包括一个或两个碳原子; 其中J'和J“相同或不同，并且其中J'和J”是包含至少一个含碳五元或六元环结构的配体; 并且其中M是通过配位键与R1'，R1“，R2'和R2”结合的过渡金属离子。还提供了使用金属配体切割核酸的方法。

8. 发明授权

US06350865B1 Process for the preparation of pentaacetyl-&bgr;-D-glucopyranose 失效
标题翻译：五乙酰基-β-D-吡喃葡萄糖的制备方法
公开(公告)号：US06350865B1
公开(公告)日：2002-02-26
申请号：US09506386
申请日：2000-02-18
申请人： Masahiro Tsuji , Hiroyuki Yamazaki
发明人： Masahiro Tsuji , Hiroyuki Yamazaki
IPC分类号： C07H1500
CPC分类号： C07H13/04 , C07H1/00
摘要： In a process for the preparation of pentaacetyl-&bgr;-D-glucopyranose by reacting D-glucose with acetic anhydride in the presence of sodium acetate catalyst, the improvement is provided wherein 5-10 mols of acetic anhydride are used per mol of D-glucose and the reaction is performed in an organic solvent. Pentaacetyl-&bgr;-D-glucopyranose is useful as intermediates for the synthesis of raw materials for industrial chemicals, medicines, cosmetics and the like.
摘要翻译：在乙酸钠催化剂存在下，通过D-葡萄糖与乙酸酐反应来制备五乙酰基-β-D-吡喃葡萄糖的方法中，提供了每摩尔D-葡萄糖使用5-10摩尔乙酸酐反应在有机溶剂中进行。五乙酰基-β-D-吡喃葡萄糖可用作合成工业化学品，药物，化妆品等原料的中间体。

9. 发明授权

US06737518B1 Process for preparation of 4,5-epoxymorphinan-6-oxyglucuronides 失效
标题翻译：制备4,5-环氧吗啡喃-6-氧基葡糖苷酸的方法
公开(公告)号：US06737518B1
公开(公告)日：2004-05-18
申请号：US09700035
申请日：2001-05-18
申请人： Arie L. Gutman , Genadi Nisnevitch , Lev Yudovitch , Igor Rokhman
发明人： Arie L. Gutman , Genadi Nisnevitch , Lev Yudovitch , Igor Rokhman
IPC分类号： C07H1500
CPC分类号： C07H17/08
摘要： Conjugation of 4,5-Epoxymorphinan-6-ols with Bromoglucuronides in the presence of Zinc containing compounds as activator under conditions capable of forming 4,5-Epoxymorphinan-6-oxyglucuronides is disclosed. This novel approach provides an efficient method for preparation of both anomers of 4,5-Epoxymorphinan-6-oxyglucuronides. The deprotected end products are useful as analgesic agents.
摘要翻译：公开了在能够形成4,5-环氧基吗啡喃-6-氧基葡糖苷酸的条件下，在含锌化合物作为活化剂的情况下，将4,5-环氧吗啡喃-6-ols与溴葡萄糖苷酸缀合。这种新方法提供了一种制备4,5-环氧吗啡喃-6-氧基葡糖苷酸的两种端基异构体的有效方法。去保护的最终产物可用作止痛剂。

10. 发明授权

US06686457B1 Material 有权
标题翻译：材料
公开(公告)号：US06686457B1
公开(公告)日：2004-02-03
申请号：US09722241
申请日：2000-11-27
申请人： Kurt Nilsson
发明人： Kurt Nilsson
IPC分类号： C07H1500
CPC分类号： B01J20/3219 , A61M1/3679 , A61M2202/0445 , A61M2202/206 , B01D15/00 , B01J20/3208 , B01J20/3212 , B01J20/3272 , B01J20/3274 , G01N33/80 , A61M2202/0057
摘要： Material characterized by that the material contains at least one biologically active saccharide which is covalently bound via at least one spacer to a crosslinked matrix.
摘要翻译：材料的特征在于该材料含有至少一种通过至少一个间隔物与交联基质共价结合的生物活性糖。

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