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1. 发明授权

US08283326B2 Crystalline form of 4-(beta-D-glucopyranos-1-yl)-1-methyl-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a method for its preparation and the use thereof for preparing medicaments 有权
标题翻译： 4-（β-D-吡喃葡萄糖-1-基）-1-甲基-2- [4 - （（S） - 四氢呋喃-3-基氧基） - 苄基] - 苯的结晶形式，其制备方法和其用于制备药物
公开(公告)号：US08283326B2
公开(公告)日：2012-10-09
申请号：US12446003
申请日：2007-10-26
申请人： Matthias Eckhardt , Frank Himmelsbach , Tanja M. Butz , Hans-Juergen Martin
发明人： Matthias Eckhardt , Frank Himmelsbach , Tanja M. Butz , Hans-Juergen Martin
IPC分类号： A01N43/04 , A61K31/70 , C07H1/00
CPC分类号： C07H7/00 , C07D407/12 , C07H7/04
摘要： The invention relates to a crystalline form of 4-(β-D-glucopyranos-1-yl)-1-methyl-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.
摘要翻译：本发明涉及4-（（bgr。-D-吡喃葡萄糖-1-基）-1-甲基-2- [4 - （（S） - 四氢呋喃-3-基氧基） - 苄基] - 苯的结晶形式，其制备方法以及其制备药物的用途。

2. 发明申请

US20110046078A1 METHODS AND COMPOSITIONS FOR TREATING DISEASES AND DISORDERS ASSOCIATED WITH SIGLEC-8 有权
标题翻译：治疗与SIGLEC-8相关疾病和疾病的方法和组合
公开(公告)号：US20110046078A1
公开(公告)日：2011-02-24
申请号：US12824831
申请日：2010-06-28
申请人： Bruce Scott Bochner , Ronald L. Schnaar
发明人： Bruce Scott Bochner , Ronald L. Schnaar
IPC分类号： A61K31/726 , C07H7/00 , C07H15/12 , A61K31/715 , A61K31/702 , A61K31/7008 , A61P11/06 , A61P35/02 , A61P11/00
CPC分类号： C07H3/06 , C07H5/04 , C07H5/06 , C07H7/00 , C07H7/02 , C07H11/00
摘要： The invention provides therapeutic methods and compositions for the prevention and treatment of Siglec-8 associated diseases and disorders such as asthma and allergic reactions. In particular, the invention provides methods and compositions for the prevention and treatment of diseases and disorders associated with Siglec-8 expressing cells in humans, as well as other animals, through the administration of one or more novel, carbohydrate-based compounds.
摘要翻译：本发明提供了用于预防和治疗Siglec-8相关疾病和病症如哮喘和过敏反应的治疗方法和组合物。特别地，本发明提供了通过施用一种或多种新的基于碳水化合物的化合物来预防和治疗与人类以及其它动物中的Siglec-8表达细胞相关的疾病和病症的方法和组合物。

3. 发明申请

US20090318678A1 Stable C-Glycoside Sugar and C-Glycoconjugate Mimetics, Method for preparing same and uses Thereof in Particular in Cosmetics and Drugs 审中-公开
标题翻译：稳定的C-糖苷糖和C-糖缀合物模拟物，其制备方法及其在化妆品和药物中的用途
公开(公告)号：US20090318678A1
公开(公告)日：2009-12-24
申请号：US12226586
申请日：2007-04-23
申请人： Géraldine Castelot-Deliencourt-Godefroy , Jean-Charles Quirion , Philippe Jubault , Ludivine Zoute
发明人： Géraldine Castelot-Deliencourt-Godefroy , Jean-Charles Quirion , Philippe Jubault , Ludivine Zoute
IPC分类号： C07H7/00
CPC分类号： C07H7/00
摘要： The invention concerns a C-glycoside compound of formula (I); wherein: n is equal to 1 or 2; Y represents H or halogen; X is an alkyl chain bearing at least one amino, amide, acid, ester, carbonyl, alcohol, aryl function or a carbonyl, ester amide, amino, alcohol group; the R's, identical or different, represent a OH or OR′ group where R′ is an alkyl, benzyl, benzoyl, acetyl, pivaloyl, trialkylsilyl, tertiobutyldiphenylsilyl group or one or more sugars; R1 represents OR′, NR″R″′, N3, or a phthalamide with R″ and R″′, identical or different, represent H or an alkyl, aryl, benzyl, benzoyl, acetyl, alkoxycarbonyl, allyloxycarbonyl, benzyloxycarbonyl group; R2 represents H or halogen or a OH, OR, NR″R″′ or N3 group, as well as derivatives thereof in physiologically or pharmaceutically acceptable base, mineral or organic acid-addition salt, hydrate or solvate form. The invention is useful for preparing C-glycoside compounds or C-glycoconjugates applicable in particular in cosmetology, medical imagery, immunology for treating cancer, diabetes, hypertension.
摘要翻译：本发明涉及式（I）的C-糖苷化合物; 其中：n等于1或2; Y表示H或卤素; X是至少有一个氨基，酰胺，酸，酯，羰基，醇，芳基官能团或羰基，酯酰胺，氨基，醇基的烷基链; 苄基，苯甲酰基，乙酰基，新戊酰基，三烷基甲硅烷基，叔丁基二苯基甲硅烷基或一种或多种糖类，其中R'相同或不同，表示OH或OR'基团。 R1表示OR'，NR''R“'，N3或具有相同或不同的R”和R“'的邻苯二甲酰胺代表H或烷基，芳基，苄基，苯甲酰基，乙酰基，烷氧基羰基，烯丙氧基羰基，苄氧羰基 R2代表H或卤素或OH，OR，NR'R“或N3基团，以及其衍生物在生理或药学上可接受的碱，矿物或有机酸加成盐，水合物或溶剂合物形式中。本发明可用于制备适用于美容，医学影像，治疗癌症，糖尿病，高血压的免疫学的C-糖苷化合物或C-糖缀合物。

4. 发明申请

US20090304734A1 IMMUNOGENS FOR MENINGITIDIS-A VACCINES 有权
标题翻译：免疫球蛋白疫苗
公开(公告)号：US20090304734A1
公开(公告)日：2009-12-10
申请号：US11913765
申请日：2006-05-08
申请人： Stefan Oscarson , Peter Teodorovic , Paolo Costantino
发明人： Stefan Oscarson , Peter Teodorovic , Paolo Costantino
IPC分类号： A61K39/09 , C07H3/04 , C07K14/22 , A61K31/715
CPC分类号： C07H15/04 , C07H7/00 , C07H11/04 , C07H13/00
摘要： An oligosaccharide useful for a Meningitidis A vaccine contains a first mannose unit having a spacer in the alpha configuration at C-1, which spacer is capable of conjugating to a protein, and which is connected to a second mannose unit through a 1,6-linkage which connects C-6 of the first unit to C-1 of the second unit, wherein the 1,6-linkage comprises a phosphonate. Related methods of making such compounds, analogous compounds, or intermediates thereof are also disclosed.
摘要翻译：可用于脑膜炎奈瑟菌疫苗的寡糖含有第一甘露糖单元，其具有在C-1的α构型中的间隔基，该间隔基能够与蛋白质共轭，并且其通过1,6- 将第一单元的C-6与第二单元的C-1连接，其中该1,6-键包含膦酸酯。还公开了制备这些化合物，类似化合物或其中间体的相关方法。

5. 发明申请

US20080287667A1 Nucleic Acid Labeling Compounds 有权
标题翻译：核酸标记化合物
公开(公告)号：US20080287667A1
公开(公告)日：2008-11-20
申请号：US12163528
申请日：2008-06-27
申请人： Glenn McGall , Anthony D. Barone
发明人： Glenn McGall , Anthony D. Barone
IPC分类号： C07H21/00 , C07H19/04 , C07D413/04
CPC分类号： C12Q1/6816 , C07D239/47 , C07H7/00 , C07H7/06 , C07H19/06
摘要： Nucleic acid labeling compounds are disclosed. The compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofaranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.
摘要翻译：公开了核酸标记化合物。该化合物是通过将杂环衍生物与环状基团（例如核糖霜糖衍生物）缩合而合成的。标记化合物适合于在末端或内部酶促附着于核酸，以提供核酸检测机制。

6. 发明授权

US07375213B2 Methods of producing C-aryl glucoside SGLT2 inhibitors 有权
标题翻译：生产C-芳基葡萄糖苷SGLT2抑制剂的方法
公开(公告)号：US07375213B2
公开(公告)日：2008-05-20
申请号：US10745075
申请日：2003-12-23
申请人： Prashant P. Deshpande , Bruce A. Ellsworth , Janak Singh , Theodor W. Denzel , Chiajen Lai , Gerard Crispino , Michael E. Randazzo , Jack Z. Gougoutas
发明人： Prashant P. Deshpande , Bruce A. Ellsworth , Janak Singh , Theodor W. Denzel , Chiajen Lai , Gerard Crispino , Michael E. Randazzo , Jack Z. Gougoutas
IPC分类号： C07H15/203 , C07H15/20 , C07H1/00
CPC分类号： C07H23/00 , C07H5/04 , C07H5/06 , C07H7/00 , C07H15/207
摘要： Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.
摘要翻译：生产用于治疗糖尿病和相关疾病的C-芳基葡萄糖苷SGLT2抑制剂的方法。及其中间体。 C-芳基葡糖苷可以与形成氨基酸复合物的试剂络合。

7. 发明申请

US20070238866A1 METHODS OF PRODUCING C-ARYL GLUCOSIDE SGLT2 INHIBITORS 有权
标题翻译：生产C-ARYL GLUCOSIDE SGLT2抑制剂的方法
公开(公告)号：US20070238866A1
公开(公告)日：2007-10-11
申请号：US11764839
申请日：2007-06-19
申请人： Prashant Deshpande , Bruce Ellsworth , Janak Singh , Theodor Denzel , Chiajen Lai , Gerard Crispino , Michael Randazzo , Jack Gougoutas
发明人： Prashant Deshpande , Bruce Ellsworth , Janak Singh , Theodor Denzel , Chiajen Lai , Gerard Crispino , Michael Randazzo , Jack Gougoutas
IPC分类号： C07H15/20 , A61K31/70
CPC分类号： C07H23/00 , C07H5/04 , C07H5/06 , C07H7/00 , C07H15/207
摘要： Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.
摘要翻译：生产用于治疗糖尿病和相关疾病的C-芳基葡萄糖苷SGLT2抑制剂的方法。及其中间体。 C-芳基葡糖苷可以与形成氨基酸复合物的试剂络合。

8. 发明授权

US07049300B2 C-glycoside compounds for stimulating the synthesis of glycosaminoglycans 有权
标题翻译： C-糖苷化合物，用于刺激糖胺聚糖的合成
公开(公告)号：US07049300B2
公开(公告)日：2006-05-23
申请号：US10463323
申请日：2003-06-18
申请人： Maria Dalko , Lionel Breton
发明人： Maria Dalko , Lionel Breton
IPC分类号： A61K31/70 , A61K38/16
CPC分类号： A61K8/602 , A61Q19/08 , C07H7/00
摘要： C-glycoside compounds are suited for stimulating the synthesis of glycosaminoglycans containing a D-glucosamine and/or N-acetyl-D-glucosamine residue, advantageously hyaluronic acid, and/or proteoglycans, advantageously proteoglycans containing hyaluronic acid, by fibroblasts and/or keratinocytes.
摘要翻译： C-糖苷化合物适合于刺激含有D-葡糖胺和/或N-乙酰基-D-葡糖胺残基，有利的透明质酸和/或蛋白聚糖，有益的含有透明质酸的蛋白聚糖的成纤维细胞和/或角质形成细胞的糖胺聚糖的合成。

9. 发明申请

US20060019246A1 Synthetic C-glycolipid and its use for treating cancer, infectious diseases, and autoimmune diseases 有权
标题翻译：合成β-糖脂及其用于治疗癌症，感染性疾病和自身免疫性疾病的用途
公开(公告)号：US20060019246A1
公开(公告)日：2006-01-26
申请号：US11193852
申请日：2005-07-29
申请人： Moriya Tsuji , Guangwu Chen , Richard Franck , Guangli Yang
发明人： Moriya Tsuji , Guangwu Chen , Richard Franck , Guangli Yang
IPC分类号： C12Q1/70 , A61K31/739 , C08B37/00
CPC分类号： C07H5/06 , C07H7/00 , C07H15/10
摘要： The invention is directed to compounds of formula (I) wherein X is O or NH; R′ is a hydrocarbon chain; R3 and R4 are hydrogen, OH or a monosaccharide; R5 is hydrogen or a monosaccharide; Q′ is optionally present and may be a C1-10 hydrocarbon; X′ is optionally present and may be O, S or NR8; and Q3 may be a hydrocarbon or hydrogen. The invention is also directed to the use of the compounds for treating cancer, infectious diseases and autoimmune diseases. The invention is also directed to syntheses of the compounds of formula (I).
摘要翻译：本发明涉及其中X为O或NH的式（I）化合物; R'是烃链; R 3和R 4是氢，OH或单糖; R 5是氢或单糖; Q'任选存在，并且可以是C 1-10烃; X'任选存在，并且可以是O，S或NR 8; 和Q 3可以是烃或氢。本发明还涉及该化合物用于治疗癌症，感染性疾病和自身免疫性疾病的用途。本发明还涉及式（I）化合物的合成。

10. 发明申请

US20050059814A1 Alkylated c-sugars and uses thereof 审中-公开
标题翻译：烷基化的c-糖及其用途
公开(公告)号：US20050059814A1
公开(公告)日：2005-03-17
申请号：US10471328
申请日：2002-03-11
申请人： Arno Spatola , Jackie Spatola , Grant Taylor , Florence Brunel
发明人： Arno Spatola , Jackie Spatola , Grant Taylor , Florence Brunel
IPC分类号： C07H5/06 , C07H7/00 , C07H15/04
CPC分类号： C07H5/06 , C07H7/00 , C07H15/04
摘要： The present invention relates to alkylated C-sugars which are new carbohydrate derivatives based on the “C-Sugar” platform. These alkylated C-sugars are converted from hydrophilic, hydrogen-bonded saccaride derivatives and are very stable, highly soluble and relatively low molecular weight structures. These alkylated C-sugars can serve as effective bioconjugates and pharmaceutical carriers. The alkylated C-sugar have the formula wherein n=0, 1, 2, 3, 4, Rx=aryl, alkyl, or halogen-substituted aryl or alkyl, Y=(CH2)mNH2,(CH2)mCO2H,(CH2)mOH,(CH2)mCH, or (CH2)mCl, and m=0, 1, 2 or 3.
摘要翻译：本发明涉及基于“C-Sugar”平台的新的碳水化合物衍生物的烷基化C糖。这些烷基化的C-糖从亲水性，氢键合的saccaride衍生物转变而且是非常稳定的，高度可溶的和相对低分子量的结构。这些烷基化的C-糖可以作为有效的生物共轭和药物载体。烷基化C糖具有下式其中n = 0,1,2,3,4，Rx =芳基，烷基或卤素取代的芳基或烷基，Y =（CH 2）m NH 2，（CH 2）m CO 2 H，（CH 2） mOH，（CH 2）m CH或（CH 2）m Cl，m = 0,1,2或3。

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