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11. 发明授权

US06555665B1 Glycosidation of 4,5-epoxymorphinan-6-ols 失效
标题翻译： 4,5-环氧吗啡喃-6-ols的糖化
公开(公告)号：US06555665B1
公开(公告)日：2003-04-29
申请号：US09601358
申请日：2000-09-15
申请人： Arie Gutman , Genadi Nisnevitch , Lev Yudovitch , Igor Rochman
发明人： Arie Gutman , Genadi Nisnevitch , Lev Yudovitch , Igor Rochman
IPC分类号： C07H1500
CPC分类号： C07H17/00
摘要： Glycosidation of 4,5-Epoxymorphinan-6-ols with a Thioglycoside as a glycoside donor is disclosed. The process comprises reacting a 4,5-Epoxymorphinan-6-ol and a Thioglycoside in the presence of a thiophilic promoter under conditions capable of forming 4,5-Epoxymorphinan-6-glycosides. This novel approach was used for preparation of pharmaceutically important 4,5-Epoxymorphinan-6-&bgr;-D-glucuronides. The process provides both high stereo-selectivity and high yields.
摘要翻译：公开了以硫代糖苷作为糖苷供体的4,5-环氧基吗啡喃-6-ols的糖苷化。该方法包括在能够形成4,5-环氧吗啡喃-6糖苷的条件下，在一种嗜碱性启动子存在下使4,5-环氧吗啡喃-6-醇与硫代糖苷反应。该新方法用于制备药物重要的4,5-环氧吗啡喃-6-β-D-葡糖苷酸。该方法提供高立体选择性和高产率。

12. 发明授权

US06420538B1 Aromatic amides, preparation method and application as medicines 失效
标题翻译：芳香酰胺，药物的制备方法和应用
公开(公告)号：US06420538B1
公开(公告)日：2002-07-16
申请号：US09600053
申请日：2000-08-30
申请人： Jean-Luc Haesslein , Michel Klich , Patrick Laurin , Branislav Musicki , Anne-Marie Periers
发明人： Jean-Luc Haesslein , Michel Klich , Patrick Laurin , Branislav Musicki , Anne-Marie Periers
IPC分类号： C07H1500
CPC分类号： C07H17/075
摘要： A compound having a formula wherein the substituents are defined as in the specification and its non-toxic, pharmaceutically acceptable acid addition salts which are useful as antibiotics.
摘要翻译：在说明书中定义具有取代基的取代基的化合物及其无毒的药学上可接受的酸加成盐，其可用作抗生素。

13. 发明授权

US06395886B1 1-O-(2-propenyl)-6-deoxy-6-carbonylthiopyranosides 失效
标题翻译： 1-O-（2-丙烯基）-6-脱氧-6-羰基硫代吡喃糖苷
公开(公告)号：US06395886B1
公开(公告)日：2002-05-28
申请号：US09686701
申请日：2000-10-11
申请人： Takayuki Yamazaki , Fumio Sugawara , Keisuke Ohta , Kazuyoshi Masaki , Kotaro Nakayama , Kengo Sakaguchi
发明人： Takayuki Yamazaki , Fumio Sugawara , Keisuke Ohta , Kazuyoshi Masaki , Kotaro Nakayama , Kengo Sakaguchi
IPC分类号： C07H1500
CPC分类号： C07H13/00
摘要： 1-O-(2-propenyl)-6-deoxy-6-carbonylthiopyranoside represented by the formula wherein R1, R2 and R3 each independently represents an alkyl or a substituted silyl group, and R5 represents a hydrogen atom, or an alkyl or aryl group.
摘要翻译：由糠醛R 1，R 2和R 3表示的1-O-（2-丙烯基）-6-脱氧-6-羰基硫代吡喃糖苷各自独立地表示烷基或取代的甲硅烷基，R5表示氢原子或烷基或芳基。

14. 发明授权

US06340746B1 Prodrugs and conjugates of thiol- and selenol- containing compounds and methods of use thereof 失效
标题翻译：含硫醇和含硒化合物的前药和缀合物及其使用方法
公开(公告)号：US06340746B1
公开(公告)日：2002-01-22
申请号：US09485321
申请日：2000-07-20
申请人： Jeannette C. Roberts , Britta H. Wilmore , Pamela B. Cassidy , Pamela K. Dominick , Megan D. Short
发明人： Jeannette C. Roberts , Britta H. Wilmore , Pamela B. Cassidy , Pamela K. Dominick , Megan D. Short
IPC分类号： C07H1500
CPC分类号： C07H5/00 , C07D293/06 , C07H5/10 , C07H15/26 , C07H17/00
摘要： Disclosed are prodrugs as follows: (I) a prodrug of the formula where A is a sulfur or a selenium, and R is a mono- di- or oligo-saccharide; (II) a prodrug of the formula where A is sulfur or selenium, R′ is a sugar, or ═O, and the R″ groups are hydrogen, alkyl, alkoxy, carboxy; (III) a conjugate of an antioxidant vitamin and a thiolamine or selenolamine; (IV) a prodrug of the formula where A is sulfur or selenium, and R′ is a sugar, or an alkyl or aryl group, or ═O, and R‡ is an alkoxy, or an amine group; (V) a prodrug of the formula R is COOH or H, and R′ is a sugar or ═O.
摘要翻译：公开的前药如下：（I）所述方法A的前药是硫或硒，R是单 - 或低聚糖;（II）所述方法A的前药是硫或硒，R '是糖，或= O，R“基团是氢，烷基，烷氧基，羧基;（III）抗氧化维生素和硫醇胺或硒胺的共轭物;（Ⅳ）或硒，R'为糖或烷基或芳基，或= O，R‡为烷氧基或胺基;（Ⅴ）式R的前药为COOH或H，R'为糖或= O。

15. 发明授权

US06291657B1 Deoxygalactonojirimycin derivatives 失效
标题翻译：脱氧半乳甘露霉素衍生物
公开(公告)号：US06291657B1
公开(公告)日：2001-09-18
申请号：US08102654
申请日：1993-08-05
申请人： Frances M. Platt , Gabrielle R. Neises , Raymond A. Dwek , Terry D. Butters
发明人： Frances M. Platt , Gabrielle R. Neises , Raymond A. Dwek , Terry D. Butters
IPC分类号： C07H1500
CPC分类号： A61K31/131 , C07D211/46 , Y02A50/471
摘要： Novel N-alkyl derivatives of deoxygalactonojirimycin are provided in which said alkyl contains from 3-6 carbon atoms. These novel compounds are useful for selectively inhibiting glycolipid synthesis.
摘要翻译：提供脱氧半乳糖吉非霉素的新型N-烷基衍生物，其中所述烷基含有3-6个碳原子。这些新型化合物可用于选择性抑制糖脂合成。

16. 发明授权

US06831164B2 Process for the production of peracylated 1-0-glycosides 失效
标题翻译：过氧化1-0-糖苷的生产方法
公开(公告)号：US06831164B2
公开(公告)日：2004-12-14
申请号：US10192856
申请日：2002-07-11
申请人： Johannes Platzek , Klaus-Dieter Graske , Ulrich Niedballa
发明人： Johannes Platzek , Klaus-Dieter Graske , Ulrich Niedballa
IPC分类号： C07H1500
CPC分类号： C07H15/18 , C07H15/04 , C07H15/26
摘要： The invention relates to a process for the production of peracylated 1-O-glycosides of general formula I or salts thereof in which sugar1 is a monosaccharide that is functionalized in 1-OH-position, R represents methyl, ethyl, propyl, isopropyl, tbutyl, phenyl, n means 2, 3 or 4, X means —COO— or —NH—and L means a straight-chain, branched, saturated or unsaturated C1-C30 carbon chain, which optionally is interrupted or substituted by groups. The process according to the invention starts from economical starting materials, provides good yields and allows the production of peracylated saccharides with 1-O-functionalized side chains on an enlarged scale.
摘要翻译：本发明涉及一种制备通式I的过酰基化的1-O-糖苷或其盐的方法，其中1是在1-OH位官能化的单糖，R代表甲基，乙基，丙基，异丙基，叔丁基，苯基，n表示2,3或4，X表示-COO-或-NH-，并且L表示直链，支链，饱和或不饱和的C1-C30碳链，其任选被中间或被基团取代。根据本发明从经济起始材料开始，提供良好的产率并且允许以1-O官能化的侧链扩大生产过酰基化糖。

17. 发明授权

US06800742B2 Method for producing &bgr;-D-ribofuranose derivatives or optical isomers thereof 失效
标题翻译：制备β-D-呋喃核糖衍生物或其旋光异构体的方法
公开(公告)号：US06800742B2
公开(公告)日：2004-10-05
申请号：US10100909
申请日：2002-03-20
申请人： Yoshihito Koguchi , Takayoshi Torii , Kunisuke Izawa
发明人： Yoshihito Koguchi , Takayoshi Torii , Kunisuke Izawa
IPC分类号： C07H1500
CPC分类号： C07H15/18 , C07H15/04 , C07H19/16
摘要： The present invention provides a method for efficiently producing &bgr;-D-ribofuranose derivatives or optical isomers thereof, useful as synthetic intermediates of pharmaceutical nucleic acid-series products. The method comprises a step of producing 1-O-benzyl-&bgr;-D-ribofuranose-2,3,5-triacetate or an optical isomer thereof by allowing &bgr;-D-ribofuranose-1,2,3,5-tetraacetate or an optical isomer thereof to react with a benzyl alcohol in the presence of acid catalysts and a step of hydrolyzing the resulting 1-O-benzyl-&bgr;-D-ribofuranose-2,3,5-triacetate in the presence of a base to produce 1-O-benzyl-&bgr;-D-ribofuranose or an optical isomer thereof.
摘要翻译：本发明提供了有效生产β-D-呋喃核糖衍生物或其光学异构体的方法，其可用作药物核酸系列产品的合成中间体。该方法包括通过使β-D-呋喃核糖-1,2,3,5-四乙酸酯或其制备方法制备1-O-苄基-β-D-呋喃核糖-2,3,5-三乙酸酯或其旋光异构体的步骤其光学异构体在酸催化剂存在下与苄醇反应，并在碱的存在下水解所得的1-O-苄基-β-D-呋喃核糖-2,3,5-三乙酸酯以产生1 -O-苄基-β-D-呋喃核糖或其旋光异构体。

18. 发明授权

US06774113B2 Process for preparing solubilization adjuvants from fusel oils and saccharides 失效
标题翻译：从杂醇油和糖制备增溶助剂的方法
公开(公告)号：US06774113B2
公开(公告)日：2004-08-10
申请号：US10008791
申请日：2001-11-13
申请人： Jean Noël Bertho , Regis de Baynast
发明人： Jean Noël Bertho , Regis de Baynast
IPC分类号： C07H1500
CPC分类号： C11D1/662 , B01F17/0021 , B01F17/0028 , C07H15/04
摘要： Process for preparing a solubilization adjuvant, which comprises placing fusel oils in contact with one or more reducing sugars in the presence of an acid catalyst, at a temperature of between 50° C. and 130° C. and while removing the water from the reaction medium until a solution of alkyl glycosides is obtained, and separating the glycosides from this solution.
摘要翻译：制备增溶助剂的方法，其包括在50℃至130℃的温度下，在50℃至130℃的温度下将杂醇油与酸催化剂存在下的一种或多种还原糖接触，同时从反应中除去水培养基直到获得烷基糖苷的溶液，并从该溶液中分离糖苷。

19. 发明授权

US06767999B2 Anthocyantin coloring agent and method for the production thereof from organic matter 失效
标题翻译：花青素着色剂及其从有机物生产的方法
公开(公告)号：US06767999B2
公开(公告)日：2004-07-27
申请号：US10019194
申请日：2001-12-21
申请人： Vitaly Alekseevich Smirnov , Viktor Victorovich Sidorov , Valentina Vladimirovna Smirnova
发明人： Vitaly Alekseevich Smirnov , Viktor Victorovich Sidorov , Valentina Vladimirovna Smirnova
IPC分类号： C07H1500
CPC分类号： C09B61/00
摘要： Anthocyanic colorant made of vegetable primary material and process for its production relate to food, cosmetic, pharmaceutical and textile industry and may be used in production of alcoholic and soft drinks, confectionery, products made of sour milk, in coloring of tablet capsules, dying of children's underwear, toys, etc. According to the invention, pelargonidin glycoside was added to the composition of the natural colorant that contained cyanidin glycosides, peonidin glycosides, organic substance and mineral salts. The components percentage shall be as follows, %: cyanidin glycoside 0.1-8.6; peonidin glycoside 0.08-6.45 pelargonidin glycoside 0.005-4.3; organic substance and mineral salts—the rest. Due to the fact that the colorant solution contains pelergonidin glycoside further to cyanidin and peonidin glycosides, the proposed colorant obtained expanded color spectrum. Combination of these three anthocyans in the proposed colorant provides for the most rich spectrum of red colors. At the same time, the ratio of pelargonidin glycoside:peonidine glycoside:cyanidin glycoside must be 1:1.5:2, respectively, and it will provide for production of a colorant with a number of valuable physical properties. Namely, the colorant retains red color when pH of the environment is not more than 7, it is thermostable, photostable and maintains its properties during 2 (two) years, besides, its relative optical density is the highest when it is subjected to the light with wavelength of 505-515 nm. According to the invention, process of the colorant production implies that pre-dried vegetable maize-pulp containing anthocyan is grinded, extracted by a mix of aqueous solutions of hydrochloric and citric acids in the field of ultrasonic vibration. Then the extracted coloring matter is filtered and concentrated in vacuum. The primary material is additionally prepared for extraction by infusion of grinded material in extracting agent during 6-8 hours at the temperature of 35-40° C. Extraction may be performed in three steps. Processing for extraction of each lot shall be 30-40 minutes at the temperature of 35-40° C. The process makes the production technology easier and provides for additional source of primary materials. 2 independent claims, 8 dependent claims, 5 tables.

20. 发明授权

US06750332B1 Salicyl alcohol derivatives 失效
标题翻译：水杨醇衍生物
公开(公告)号：US06750332B1
公开(公告)日：2004-06-15
申请号：US09856835
申请日：2002-02-26
申请人： Ralf Otto , Albrecht Weiss
发明人： Ralf Otto , Albrecht Weiss
IPC分类号： C07H1500
CPC分类号： C07H15/04 , A61K8/602 , A61Q19/00 , C08B37/00 , C12P7/62 , C12P19/44
摘要： Novel salicyl alcohol derivatives having valuable cosmetically and pharmaceutically useful properties, such as prostaglandin synthesis inhibition, corresponding to the formula (I): R1—OCH2—Ph—O—Z—(R2)n (I), a method for producing the same and their utilization in cosmetics and pharmacy.
摘要翻译：新颖的水杨醇衍生物具有有价值的美容和药学上有用的性质，如前列腺素合成抑制，对应于式（I）：其制备方法及其在化妆品和药学中的应用。

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