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公开(公告)号：US09512158B2
公开(公告)日：2016-12-06
申请号：US13716570
申请日：2012-12-17
发明人： Mario R. Mautino , Nicholas N. Vahanian , Won-Bin Young , Gabriela Rossi , Charles J. Link , Firoz Jaipuri
CPC分类号： C07H5/04 , A61K31/70 , A61K39/0011 , A61K39/39 , A61K2039/55511 , C07H15/00 , C07H15/04
摘要： The invention relates to methods and compositions for causing the selective targeting and killing of tumor cells. The present invention describes prophylactic or therapeutic cancer vaccines based on purified TAA proteins or TAA-derived synthetic peptides altered by chemical, enzymatic or chemo-enzymatic methods to introduce αGal epitopes or αGal glycomimetic epitopes, in order to allow for enhanced opsonization of the antigen by natural anti-αGal antibodies to stimulate TAA capture and presentation, thereby inducing a humoral and cellular immune response to the TAA expressed by a tumor. The animal's immune system thus is stimulated to produce tumor specific cytotoxic cells and antibodies which will attack and kill tumor cells present in the animal.
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2.发明授权α-galactosylceramide derivatives, pharmaceutically acceptable salts thereof, preparation method and pharmaceutical composition for the immune adjuvant containing the same as an active ingredient 有权α-半乳糖神经酰胺衍生物，其药学上可接受的盐，含有其作为活性成分的免疫佐剂的制备方法和药物组合物公开(公告)号：US08883746B2
公开(公告)日：2014-11-11
申请号：US12521487
申请日：2007-12-27
申请人： Chang-Yuil Kang , SangHee Kim , Hyun-Jun Youn , Yoon-Sook Lee , Kyoo-A Lee , Taeho Lee , Dong Jae Baek , Minjae Cho
发明人： Chang-Yuil Kang , SangHee Kim , Hyun-Jun Youn , Yoon-Sook Lee , Kyoo-A Lee , Taeho Lee , Dong Jae Baek , Minjae Cho
IPC分类号： A61K31/7028 , A61K31/00 , C07H15/04 , C07H15/00
摘要： Disclosed are novel α-galactosylceramide derivatives, pharmaceutically acceptable salts thereof, preparation methods thereof, and pharmaceutical compositions for use in an immune adjuvant containing the same as an active ingredient. The derivatives, in which the amide moiety of α-GalCer is bioisosterically replaced with a triazole moiety, direct cytokine secretion toward IL-4 rather than IFN-γand thus can be used as a therapeutic for autoimmune diseases regulated by IL-4, such as type 1 diabetes and multiple sclerosis.
摘要翻译： 公开了新型α-半乳糖神经酰胺衍生物，其药学上可接受的盐，其制备方法和用于含有其作为活性成分的免疫佐剂的药物组合物。 其中α-GalCer的酰胺部分被三唑部分生物电离置换的衍生物直接导致IL-4的细胞因子分泌而不是IFN-γ，因此可用作IL-4调节的自身免疫性疾病的治疗剂，例如 1型糖尿病和多发性硬化症。
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公开(公告)号：US08853169B2
公开(公告)日：2014-10-07
申请号：US12037106
申请日：2008-02-26
CPC分类号： C07H15/00
摘要： The present invention relates to novel C-glycoside compounds of given absolute configuration, to a process for synthesizing them and to compositions containing them. The invention also relates to the cosmetic use of these C-glycoside compounds as agents to stimulate the synthesis of glycosaminoglycans containing a D-glucosamine and/or N-acetyl-D-glucosamine residue, advantageously hyaluronic acid, and/or of proteoglycans, advantageously proteoglycans containing hyaluronic acid, by fibroblasts and/or keratinocytes. The invention also relates to a cosmetic process for treating keratin materials using a composition containing at least one C-glycoside compound according to the invention.
摘要翻译： 本发明涉及给定绝对构型的新型C-糖苷化合物，其合成方法和含有它们的组合物。 本发明还涉及这些C-糖苷化合物的化妆品用途，有利地刺激含有D-葡糖胺和/或N-乙酰基-D-葡糖胺残基（有利地为透明质酸）和/或蛋白聚糖的糖胺聚糖的合成 含有透明质酸的蛋白聚糖，通过成纤维细胞和/或角质形成细胞。 本发明还涉及使用含有至少一种本发明的C-糖苷化合物的组合物来治疗角蛋白材料的美容方法。
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公开(公告)号：US20130237494A1
公开(公告)日：2013-09-12
申请号：US13814172
申请日：2011-08-03
申请人： Herbert Schott
发明人： Herbert Schott
IPC分类号： C07F9/6512 , A61K45/06 , A61K31/7068
CPC分类号： C07F9/6512 , A61K31/7068 , A61K45/06 , C07D239/54 , C07F9/65586 , C07H15/00 , C07H19/073 , C07H19/09
摘要： The present invention relates to novel bisphosphonate duplex drugs, methods for preparing said compound; pharmaceutical compositions containing the same; as well as the use of said compounds in human and veterinary medicine, and, in particular, for treating tumors, viral infections; or dental disorders.
摘要翻译： 本发明涉及新型二膦酸双倍体药物，制备所述化合物的方法; 含有该组合物的药物组合物; 以及所述化合物在人和兽医学中的用途，特别是用于治疗肿瘤，病毒感染; 或牙齿障碍。
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公开(公告)号：US08513394B2
公开(公告)日：2013-08-20
申请号：US11996084
申请日：2006-07-21
CPC分类号： C07H15/00 , A61K49/0032 , A61K49/0052 , C07H15/18 , C12Q1/34 , G01N21/6428 , G01N33/542 , G01N2333/924 , G01N2400/00
摘要： A fluorescent enzymatic substrate including a backbone saccharide nature having at least one saccharide unit. The saccharide unit includes a fluorophore F1 and an inhibitor I1 of the fluorescence of F1. The fluorophore F1 and the inhibitor I1, either directly or by the spacer arms B1 and B2, respectively, when at least one B1 and B2 is present, are grafted on the same saccharide unit of the backbone saccharide. One of th groups is F1 and I1 grafted in the anomeric position 1 of the saccharide unit.
摘要翻译： 包含具有至少一个糖单元的骨架糖性质的荧光酶底物。 糖单元包括荧光团F1和F1荧光的抑制剂I1。 当存在至少一个B1和B2时，分别将荧光团F1和抑制剂I1直接或间隔臂B1和B2分别接枝在骨架糖的同一个糖单元上。 第一组中的一个是F1和I1接枝在糖单元的异头位置1。
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公开(公告)号：US20130178613A1
公开(公告)日：2013-07-11
申请号：US13716569
申请日：2012-12-17
发明人： Mario R. MAUTINO , Nicholas N. Vahanian , Won-Bin Young , Gabriela Rossi , Charles J. Link , Firoz Jaipuri
IPC分类号： C07H5/04
CPC分类号： C07H5/04 , A61K31/70 , A61K39/0011 , A61K39/39 , A61K2039/55511 , C07H15/00 , C07H15/04
摘要： The invention relates to methods and compositions for causing the selective targeting and killing of tumor cells. The present invention describes prophylactic or therapeutic cancer vaccines based on purified TAA proteins or TAA-derived synthetic peptides altered by chemical, enzymatic or chemo-enzymatic methods to introduce αGal epitopes or αGal glycomimetic epitopes, in order to allow for enhanced opsonization of the antigen by natural anti-αGal antibodies to stimulate TAA capture and presentation, thereby inducing a humoral and cellular immune response to the TAA expressed by a tumor. The animal's immune system thus is stimulated to produce tumor specific cytotoxic cells and antibodies which will attack and kill tumor cells present in the animal.
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公开(公告)号：US20120258043A1
公开(公告)日：2012-10-11
申请号：US13456747
申请日：2012-04-26
申请人： Ramachandran RANGANATHAN , Kondareddiar RAMALINGAM , Radhakrishna PILLAI , Edmund R. MARINELLI , Rolf E. SWENSON
发明人： Ramachandran RANGANATHAN , Kondareddiar RAMALINGAM , Radhakrishna PILLAI , Edmund R. MARINELLI , Rolf E. SWENSON
IPC分类号： C07H15/203 , C07H23/00 , A61K49/00 , A61K31/7034 , A61K51/04 , A61P9/10 , A61P35/00 , A61P3/10 , A61P3/04 , A61P19/02 , A61P17/06 , A61P17/00 , C07K17/10 , A61P29/00
CPC分类号： C07H15/04 , A61K49/0002 , C07H7/02 , C07H15/00
摘要： Disclosed herein is a class of linkable tetrasaccharide compounds that includes the amino phenyl glycoside of sialyl Lewis X (SLeX) and related analogs. These compounds have conjugatable nucleophilic groups, making them useful in preparing multimeric SLeX compositions. In particular, the disclosed SLeX compounds can be used to prepare selectin binding ligand conjugates by linking them to a reporter moiety, such as a contrast agent, a radiodiagnostic agent, or a cytotoxic or chemotherapeutic agent. The SLeX compounds and conjugates of the invention exhibit binding to selectin that is similar to native Sialyl LeX, and are, therefore, useful for diagnosing and treating selectin-mediated disorders and related conditions.
摘要翻译： 本文公开了一类可连接的四糖化合物，其包括唾液酸基路易斯X（SLeX）的氨基苯基糖苷和相关类似物。 这些化合物具有可共轭的亲核基团，使其可用于制备多聚体SLeX组合物。 特别地，所公开的SLeX化合物可用于通过将选择蛋白结合配体缀合物连接到报告基因部分如造影剂，放射诊断剂或细胞毒性或化学治疗剂来制备。 本发明的SLeX化合物和缀合物显示出与天然唾液酸LeX相似的选择蛋白结合，因此可用于诊断和治疗选择素介导的病症和相关病症。
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公开(公告)号：US20110077302A1
公开(公告)日：2011-03-31
申请号：US12994008
申请日：2009-05-22
申请人： Frank Hollmann , Oliver Thum , Christoph Toelle , Angelo Provinzano , Cornelis Gerrit Nijs Korevaar
发明人： Frank Hollmann , Oliver Thum , Christoph Toelle , Angelo Provinzano , Cornelis Gerrit Nijs Korevaar
IPC分类号： A61K31/20 , C12P13/02 , C07C229/00
摘要： The invention relates to the enzymatic synthesis of sphingolipids and compositions that contain sphingolipids from lysosphingolipids and carbonic esters, and to cosmetic, dermatological or pharmaceutical formulations containing said sphingolipids or compositions.
摘要翻译： 本发明涉及鞘脂的酶促合成和含有来自溶血鞘脂和碳酸酯的鞘脂的组合物，以及含有所述鞘脂或组合物的化妆品，皮肤病学或药物制剂。
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公开(公告)号：US07863428B2
公开(公告)日：2011-01-04
申请号：US10540057
申请日：2003-12-26
申请人： Inge Dierynck , Jan Ludwig Goeman , Koenraad Lodewijk August Van Acker , Johan Theo André Van Der Eycken
发明人： Inge Dierynck , Jan Ludwig Goeman , Koenraad Lodewijk August Van Acker , Johan Theo André Van Der Eycken
CPC分类号： C07H15/00
摘要： This invention relates to hydrolase fluorogenic substrates with improved cell permeability, methods for the preparation thereof, and methods of measuring activities of hydrolases, particularly in cell-based assays. The substrates easily diffuse into the cells, where they are enzymatically processed to yield photostable fluorescent products, and are particularly fitted for visualising enzyme-derived activities in cell-based assays.
摘要翻译： 本发明涉及具有改善的细胞渗透性的水解酶荧光底物，其制备方法和测量水解酶活性的方法，特别是在基于细胞的测定中。 底物容易扩散到细胞中，在那里它们被酶处理以产生光稳定荧光产物，并且特别适用于在基于细胞的测定中可视化酶来源的活性。
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公开(公告)号：US07786315B2
公开(公告)日：2010-08-31
申请号：US12342321
申请日：2008-12-23
申请人： Rebecca J. Robbins , Mark A. Kelm , John P. Munafo
发明人： Rebecca J. Robbins , Mark A. Kelm , John P. Munafo
IPC分类号： C07D311/62
CPC分类号： C07D311/62 , C07H15/00
摘要： A process is described for selectively extracting cocoa procyanidins from an aqueous mixture of cocoa polyphenols by using a particular sequence of solvents to extract selected procyanidin monomers and/or oligomers. The solvents are n-butyl acetate, ethyl acetate, methyl acetate, diethyl ether, or mixtures of methyl acetate and diethyl ether. Preferably, the aqueous mixture of cocoa polyphenols is first extracted with n-butyl acetate. The mixtures of methyl acetate and diethyl ether are between 25:75 and 75:25 (v/v).
摘要翻译： 描述了通过使用特定的溶剂序列来提取选择的原花青素单体和/或低聚物来从可可多元酚的水性混合物中选择性提取可可原花青素的方法。 溶剂是乙酸正丁酯，乙酸乙酯，乙酸甲酯，乙醚或乙酸甲酯和乙醚的混合物。 优选地，可可多酚的含水混合物首先用乙酸正丁酯萃取。 乙酸甲酯和乙醚的混合物在25:75和75:25（v / v）之间。
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