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71. 发明授权

US08124758B2 Process for the preparation of N-Acetyl-D-mannosamine monohydrate 有权
标题翻译： N-乙酰基-D-甘露糖胺一水合物的制备方法
公开(公告)号：US08124758B2
公开(公告)日：2012-02-28
申请号：US12227423
申请日：2007-05-18
申请人： Giovanni Cipolletti , Giancarlo Tamerlani , Ilaria Lombardi , Debora Bartalucci
发明人： Giovanni Cipolletti , Giancarlo Tamerlani , Ilaria Lombardi , Debora Bartalucci
IPC分类号： C07H1/06
CPC分类号： C07H1/00 , C07H13/04
摘要： A process is described for the preparation of N-Acetyl-D-mannosamine monohydrate of formula (I) a specific intermediate in the synthesis of N-Acetyl-neuraminic acid, that is an important starting product for the synthesis of various pharmaceutically active products.
摘要翻译：描述了用于制备式（I）的N-乙酰基-D-甘露糖胺一水合物的方法，其是合成N-乙酰神经氨酸的特定中间体，其是用于合成各种药学活性产物的重要起始产物。

72. 发明授权

US08088746B2 Bis-modified bicyclic nucleic acid analogs 有权
标题翻译：双改性双环核酸类似物
公开(公告)号：US08088746B2
公开(公告)日：2012-01-03
申请号：US12687429
申请日：2010-01-14
申请人： Punit P. Seth , Eric E. Swayze
发明人： Punit P. Seth , Eric E. Swayze
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： C07H21/00 , C07H7/02 , C07H9/04 , C07H13/04 , C07H15/18 , C07H17/02 , C07H19/04 , C07H19/06 , C07H19/16 , C07H23/00
摘要： The present disclosure describes bis-modified bicyclic nucleosides and oligomeric compounds that can be prepared comprising at least one of these bis-modified bicyclic nucleosides. More particularly, the bis-modified bicyclic nucleosides have at least one substituent group at the 5′-methylene and on the bridge methylene and can be chiral. These bis-modified bicyclic nucleosides are expected to be useful for enhancing one or more property of oligomeric compounds including for example enhancing nuclease resistance.
摘要翻译：本公开描述了可以制备的双改性双环核苷和寡聚化合物，其包含这些双改性双环核苷中的至少一种。更具体地，双改性双环核苷在5'-亚甲基和亚甲基桥上具有至少一个取代基，并且可以是手性的。预期这些双改性双环核苷可用于增强寡聚化合物的一种或多种性质，包括例如增强核酸酶抗性。

73. 发明申请

US20110206734A1 HYBRID SCFA-HYDROXYL-DERIVATIZED MONOSACCHARIDES, METHODS OF SYNTHESIS, AND METHODS OF TREATING DISORDERS 有权
标题翻译： HYBRID SCFA-羟基衍生的单糖，合成方法和治疗疾病的方法
公开(公告)号：US20110206734A1
公开(公告)日：2011-08-25
申请号：US12671994
申请日：2008-08-07
申请人： Kevin J. Yarema , Udayanath Aich , Christopher Thomas Campbell , Srinivasa-Gopalan Sampathkumar , Sean S. Choi , Michael Adam Meledeo , Christopher Weier
发明人： Kevin J. Yarema , Udayanath Aich , Christopher Thomas Campbell , Srinivasa-Gopalan Sampathkumar , Sean S. Choi , Michael Adam Meledeo , Christopher Weier
IPC分类号： A61K39/00 , C07H15/04 , A61K31/7028 , C07H13/04 , A61K31/7024 , A61P35/00 , C12N5/071
CPC分类号： A61K31/7008 , A61K31/7012 , A61K31/7028 , A61K45/06 , C07H5/06 , C07H7/027 , C07H13/04 , C07H15/04 , G01N33/5091
摘要： Described herein are fatty acid carbohydrate-hydroxyl-hybrid compounds and derivatives thereof, and methods of treating or preventing disease and disease symptoms using the compounds and compositions thereof.
摘要翻译：本文描述的是脂肪酸碳水化合物 - 羟基 - 杂合化合物及其衍生物，以及使用该化合物及其组合物治疗或预防疾病和疾病症状的方法。

74. 发明申请

US20110201801A1 SACCHARIDE STRUCTURES AND METHODS OF MAKING AND USING SUCH STRUCTURES 有权
标题翻译： SACCHARIDE结构和制造和使用这种结构的方法
公开(公告)号：US20110201801A1
公开(公告)日：2011-08-18
申请号：US12595235
申请日：2009-05-29
申请人： Sucharita Roy , Takashi Kei Kishimoto , Ganesh Venkataraman
发明人： Sucharita Roy , Takashi Kei Kishimoto , Ganesh Venkataraman
IPC分类号： C07H1/00
CPC分类号： C07H1/00 , C07H3/06 , C07H5/04 , C07H9/04 , C07H13/04 , C07H15/10 , C07H15/18 , C07H15/203 , C07H23/00 , C08B37/006 , Y02P20/55
摘要： Described are oligosaccharides having a protecting group at two, a plurality, a majority of, or each position in the oligosaccharide which is amenable to derivatization. Collections, libraries and methods of making and using such oligosaccharides are also described.
摘要翻译：描述了在寡糖中的两个，多个，大多数或每个位置具有可衍生化的保护基的寡糖。还描述了制备和使用这种寡糖的集合，文库和方法。

75. 发明授权

US07968751B2 Method of fluorination 失效
公开(公告)号：US07968751B2
公开(公告)日：2011-06-28
申请号：US12068481
申请日：2008-02-07
申请人： Shoji Hara , Tsuyoshi Fukuhara
发明人： Shoji Hara , Tsuyoshi Fukuhara
IPC分类号： C07C211/03 , C07C211/08
CPC分类号： C07D239/30 , C07B39/00 , C07B2200/09 , C07C17/093 , C07C17/16 , C07C17/18 , C07C29/64 , C07C51/60 , C07C67/307 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2601/20 , C07C2603/74 , C07H1/00 , C07H9/04 , C07H13/04 , C07H13/08 , C07H19/06 , C07C22/08 , C07C21/18 , C07C19/08 , C07C23/38 , C07C23/02 , C07C23/10 , C07C63/10 , C07C69/63 , C07C35/52 , C07C35/48
摘要： A method of fluorination comprising reacting monosaccharides, oligosaccharides, polysaccharides, composite saccharides formed by bonding of these saccharides with proteins and lipids and saccharides having polyalcohols, aldehydes, ketones and acids of the polyalcohols, and derivatives and condensates of these compounds with a fluorinating agent represented by general formula (I) thermally or under irradiation with microwave or an electromagnetic wave having a wavelength around the microwave region. In accordance with the method, the fluorination at a selected position can be conducted safely at a temperature in the range of 150 to 200° C. where the reaction is difficult in accordance with conventional methods. The above method comprising the irradiation with microwave or an electromagnetic wave having a wavelength around the microwave region can be applied to substrates other than saccharides. When a complex compound comprising HF and a base is reacted under irradiation with microwave, fluorination at a specific position which is difficult in accordance with conventional methods proceeds highly selectively, efficiently in a short time and safely.

76. 发明申请

US20110044901A1 NOVEL COMPOUNDS 有权
标题翻译：新型化合物
公开(公告)号：US20110044901A1
公开(公告)日：2011-02-24
申请号：US12596068
申请日：2007-11-14
申请人： Michael P. Seed , Michael Burnet , Hans Jurgen Gutchke
发明人： Michael P. Seed , Michael Burnet , Hans Jurgen Gutchke
IPC分类号： A61K49/00 , C07K9/00 , C07K14/00 , A61K38/14 , A61K31/7004 , C12N5/071 , G01N33/53 , A61P35/00 , A61P37/00 , A61P3/10 , A61P17/00 , A61P31/18 , A61P1/00 , A61P25/18 , A61P25/32
CPC分类号： C07K9/005 , C07H5/06 , C07H5/08 , C07H13/04 , C07H15/04
摘要： The present invention is directed to sulphated compounds comprising at least one glycosidic amine group, and polysaccharide, oligosaccharide, peptide and protein derivatives comprising such compounds, and mixtures thereof. The present invention is also directed to methods of synthesising such compounds. Such compounds may bind to a range of proteins, find application in methods of modifying, or testing for a modification in the level of a cytokine in vivo, ex vivo or in vitro, and find application in the treatment and/or prevention of inflammation, an inflammatory disorder, a proliferative disorder, an immune disorder, an angiogenesis-dependent disorder, a sensitivity disorder, an adverse endocrine reaction, a degenerative disorder, wound healing, depression, and other diseases and disorders.
摘要翻译：本发明涉及包含至少一种糖苷基的硫酸化合物，以及包含这些化合物的多糖，寡糖，肽和蛋白质衍生物及其混合物。本发明还涉及合成这些化合物的方法。这样的化合物可以结合一系列蛋白质，在体内，离体或体外在应用于修饰或测试细胞因子水平的修饰的方法中应用，并且可用于治疗和/或预防炎症，炎症性疾病，增殖性疾病，免疫疾病，血管发生依赖性病症，敏感性障碍，不良内分泌反应，退行性病症，伤口愈合，抑郁症和其它疾病和病症。

77. 发明申请

US20100240871A1 Galactose Alpha(1-3) Galactose Compositions 审中-公开
标题翻译：半乳糖α（1-3）半乳糖组合物
公开(公告)号：US20100240871A1
公开(公告)日：2010-09-23
申请号：US12604439
申请日：2009-10-23
申请人： T. Shantha Raju , Bernard J. Scallon
发明人： T. Shantha Raju , Bernard J. Scallon
IPC分类号： C07K16/00 , C12P21/00 , C07K14/00
CPC分类号： C07H3/06 , C07H13/04 , C07K16/00 , C07K2317/41 , C08B37/0036 , C08B37/006 , C12P21/005
摘要： An enzymatic method for synthesizing oligosaccharides comprising a terminal Gal-alpha(1,3)-Gal-beta(1-4)GlcNac is used to produce Fc-containing molecules with certain properties. The methods modify glycoproteins that interact with receptors or are processed in vivo and recognized as unique epitopes. In particular, the glycan groups on a therapeutic antibody capable of interaction with Fc-receptors are modified.
摘要翻译：用于合成包含末端Gal-α（1,3）-Gal-β（1-4）GlcNac的寡糖的酶法用于产生具有某些性质的含Fc分子。该方法修饰与受体相互作用或在体内加工并识别为独特表位的糖蛋白。特别地，能够与Fc受体相互作用的治疗性抗体上的聚糖基团被修饰。

78. 发明授权

US07763649B2 Carotenoid analogs or derivatives for controlling connexin 43 expression 有权
标题翻译：用于控制连接蛋白43表达的类胡萝卜素类似物或衍生物
公开(公告)号：US07763649B2
公开(公告)日：2010-07-27
申请号：US10793686
申请日：2004-03-04
申请人： Samuel Fournier Lockwood , Sean O'Malley , David G. Watumull , Laura M. Hix , Henry Jackson , Geoff Nadolski
发明人： Samuel Fournier Lockwood , Sean O'Malley , David G. Watumull , Laura M. Hix , Henry Jackson , Geoff Nadolski
IPC分类号： A61K31/34 , A61K31/35 , A61K31/335
CPC分类号： C07D207/16 , C07C403/24 , C07D265/30 , C07D307/58 , C07F9/117 , C07H13/04
摘要： A method of controlling (e.g., influencing or affecting) connexin 43 expression in a subject may include administering to the subject an effective amount of a pharmaceutically acceptable formulation. In some embodiments, controlling connexin 43 expression in a subject may effectively treat cardiac arrhythmia and/or cancerous and pre-cancerous cells in a subject. The pharmaceutically acceptable formulation may include a synthetic analog or derivative of a carotenoid. The subject may be administered a carotenoid analog or derivative, either alone or in combination with another carotenoid analog or derivative, or co-antioxidant formulation. The carotenoid analog may include a conjugated polyene with between 7 to 14 double bonds. The conjugated polyene may include an acyclic alkene including at least one substituent and/or a cyclic ring including at least one substituent. In some embodiments, a carotenoid analog or derivative may include at least one substituent.
摘要翻译：在受试者中控制（例如影响或影响）连接蛋白43表达的方法可包括向受试者施用有效量的药学上可接受的制剂。在一些实施方案中，控制受试者中连接蛋白43的表达可以有效地治疗受试者的心律失常和/或癌前和癌前细胞。药学上可接受的制剂可以包括类胡萝卜素的合成类似物或衍生物。受试者可以单独给予类胡萝卜素类似物或衍生物，或与另一种类胡萝卜素类似物或衍生物或共抗氧化剂制剂一起施用。类胡萝卜素类似物可以包括具有7至14个双键的共轭多烯。共轭多烯可以包括包含至少一个取代基的无环烯烃和/或包含至少一个取代基的环状环。在一些实施方案中，类胡萝卜素类似物或衍生物可包括至少一个取代基。

79. 发明申请

US20100184013A1 DETECTION OF OLIGOSACCHARIDES 有权
标题翻译：检测寡糖
公开(公告)号：US20100184013A1
公开(公告)日：2010-07-22
申请号：US12649094
申请日：2009-12-29
申请人： Brett E. CRAWFORD , Jillian R. BROWN , Charles A. GLASS
发明人： Brett E. CRAWFORD , Jillian R. BROWN , Charles A. GLASS
IPC分类号： C12Q1/00
CPC分类号： C12Q1/527 , A61K31/702 , C07H3/04 , C07H3/06 , C07H5/06 , C07H7/033 , C07H11/00 , C07H13/04 , G01N33/66 , G01N2333/988 , G01N2400/40 , G01N2800/042 , G01N2800/52 , G01N2800/7071
摘要： Provided herein are processes for detecting oligosaccharides in a biological sample. In specific instances, the biological sample is provided from an individual suffering from a disorder associated with abnormal glycosaminoglycan accumulation.
摘要翻译：本文提供了检测生物样品中寡糖的方法。在具体情况下，生物样品由患有与异常糖胺聚糖累积相关的病症的个体提供。

80. 发明授权

US07759070B2 Conserved inner core lipopolysaccharide epitopes as multi-species vaccine candidates 失效
标题翻译：保守的内核脂多糖表位作为多种疫苗候选物
公开(公告)号：US07759070B2
公开(公告)日：2010-07-20
申请号：US11569093
申请日：2005-05-16
申请人： Andrew D. Cox , James C. Richards
发明人： Andrew D. Cox , James C. Richards
IPC分类号： A61K8/73 , A61K31/715 , G01N33/53
CPC分类号： C12N1/36 , A61K31/739 , A61K39/0208 , A61K39/05 , A61K39/102 , A61K47/646 , A61K2039/505 , A61K2039/522 , A61K2039/552 , A61K2039/6081 , A61K2039/70 , C07H3/06 , C07H13/04 , C07K16/1242 , C08B37/0003 , C08B37/006 , C12P19/04 , C12P19/44 , C12R1/01
摘要： A conserved inner-core oligosaccharide epitope expressed on the lipopolysaccharide (LPS) of a range of disease causing pathogenic bacterial isolates, including Actinobacillus pleuropneumoniae (Ap), Mannheimia haemolytica (Mh) and Pasteurella multocida (Pm), is disclosed. Construction of a mutant bacterial strain exclusively expressing the conserved inner core OS epitope as a terminally exposed structure has allowed the identification, production and isolation of an inner core LPS which is common to all three organisms. Further provided are associated vaccines, antibodies raised against the conserved LPS inner core and glycoconjugates comprising the LPS inner core linked to an immunogenic carrier.
摘要翻译：公开了在致病细菌分离物的一系列疾病的脂多糖（LPS）上表达的保守的内核寡糖表位，包括放线杆菌胸膜肺炎放线芽孢杆菌（Ap），溶血性马氏解毒血症（Mh）和多杀巴斯德氏菌（Pm））。构建仅表达保守的内核OS表位作为末端暴露结构的突变细菌菌株允许鉴定，产生和分离所有三种生物共同的内核LPS。还提供了相关疫苗，针对保守的LPS内核产生的抗体和包含与免疫原性载体连接的LPS内核的糖缀合物。

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