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61. 发明授权

US4415731A Process for the preparation of methyl 2,6-dideoxy-.alpha.-D-arabino-hexopyranoside 失效
标题翻译： 2,6-二脱氧-α-D-阿拉伯 - 六吡喃甲酸甲酯的制备方法
公开(公告)号：US4415731A
公开(公告)日：1983-11-15
申请号：US248175
申请日：1981-03-30
申请人： Philippe L. Durette
发明人： Philippe L. Durette
IPC分类号： C07H15/04 , C07H5/02 , C07H1/00
CPC分类号： C07H15/04
摘要： Disclosed is a process for preparing methyl 2,6-dideoxy-.alpha.-D-arabino-hexopyranoside from methyl 2-deoxy-.alpha.-D-glucopyranoside.
摘要翻译：公开了一种由2-脱氧-α-D-吡喃葡萄糖甲酸甲酯制备甲基2,6-二脱氧-α-D-阿拉伯 - 六吡喃糖苷的方法。

62. 发明授权

US4367226A N-Sugar compounds, compositions and uses thereof 失效
标题翻译： N-糖化合物，组合物及其用途
公开(公告)号：US4367226A
公开(公告)日：1983-01-04
申请号：US212198
申请日：1980-12-02
申请人： William O. Foye
发明人： William O. Foye
IPC分类号： C07H13/12 , C07H17/00 , A61K31/70 , C07H5/02 , C07H19/00
CPC分类号： C07H13/12 , C07H17/00
摘要： Novel, water-soluble antimicrobial compounds are provided which contain a sugar moiety linked to a nitrogen atom of substituted thiourea or a thiazole. The compounds have the general formula: ##STR1## and the pharmaceutically acceptable salts thereof wherein Su is a sugar moiety, i.e., mono- or polysaccharide and preferably glucosyl or acylated (i.e. C.sub.2 to C.sub.6 alkanoyl e.g. acetyl, propionyl, butyroyl etc. or aroyl e.g. benzoyl or C.sub.1 to C.sub.4 alkyl or alkoxy substituted benzoyl) ribosyl; andin Formula I, R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1 to C.sub.8 alkyl or alkoxy; C.sub.1 to C.sub.8 .omega.-phenyl-(or substituted phenyl)-substituted C.sub.1 to C.sub.8 alkyl; C.sub.3 to C.sub.8 alkene, preferably allyl; ##STR2## wherein R.sub.3 and R.sub.4 are independently hydrogen or C.sub.1 to C.sub.8 alkyl, or the atoms to form a 5- or 6-membered heterocyclic [which may contain C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, halo (e.g., chloro, bromo or iodo), hydroxy, carboxamido, sulfonamido and the like] such as piperazino, methyl piperazino, pyrimidino, piperidino, morpholino, thiamorpholino, pyrrolyl, pyrrolidinyl, furyl, tetrahydrofuryl and the like, but only one of R.sub.1 and R.sub.2 is hydrogen, andin Formula II, R.sub.5 is oxy(C.sub.1 to C.sub.8)alkyl or substituted alkyl, phenyl or substituted phenyl or NR.sub.6 R.sub.7 wherein R.sub.6 and R.sub.7 are independently selected similarly as R.sub.1 and R.sub.2.The compounds are particularly useful in aqueous systems especially in cosmetic formulations for maintaining same in a septic state.Methods for making compounds of Formula I and II are also disclosed.
摘要翻译：提供新的水溶性抗微生物化合物，其含有与取代的硫脲或噻唑的氮原子连接的糖部分。化合物具有以下通式： I. II。其中Su是糖部分，即单糖或多糖，优选葡糖基或酰化（即C 2至C 6烷酰基，例如乙酰基，丙酰基，丁酰基等或芳酰基，例如苯甲酰基或C 1至C 4烷基或烷氧基取代的苯甲酰基）核糖基; 在式I中，R 1和R 2独立地是氢，C 1至C 8烷基或烷氧基; C1至C8ω-苯基 - （或取代的苯基） - 取代的C1至C8烷基; C3至C8烯烃，优选烯丙基; 其中R 3和R 4独立地为氢或C 1至C 8烷基，或原子形成5或6元杂环[其可以含有C 1至C 4烷基，C 1至C 4烷氧基，卤素（例如氯，溴或碘），羟基，甲酰氨基，亚磺酰氨基等]，例如哌嗪子基，哌嗪子基，嘧啶基，哌啶子基，吗啉代，吗啉代，吡咯基，吡咯烷基，呋喃基，四氢呋喃基等，但R1和R2中只有一个为氢，在式II中，R 5是氧基（C 1至C 8）烷基或取代的烷基，苯基或取代的苯基或NR 6 R 7，其中R 6和R 7与R 1和R 2类似地独立地选择。该化合物特别适用于含水体系，特别是用于在化妆品状态下保持其的化妆品制剂中。还公开了制备式I和II化合物的方法。

63. 发明授权

US4343934A Crystalline 4,1',6'-trichloro-4,1',6'-trideoxy-galactosucrose 失效
标题翻译：结晶4,1'，6'-三氯-4,1'，6'-三脱氧半乳糖
公开(公告)号：US4343934A
公开(公告)日：1982-08-10
申请号：US212897
申请日：1980-12-04
申请人： Michael R. Jenner , David Waite
发明人： Michael R. Jenner , David Waite
IPC分类号： C07H5/02 , C07H3/04
CPC分类号： C07H5/02
摘要： Crystalline 4,1',6'-trichloro-4,1',6'-trideoxy-galactosucrose exists as the orthorhombic anhydrous form and as the pentahydrate, both of which are more stable than amorphous TGS. Crystals are obtained from seeded aqueous solutions, above 38.degree. C. for the anhydrate; below 38.degree. C. for the pentahydrate.
摘要翻译：结晶4,1'，6'-三氯-4,1'，6'-三脱氧 - 半乳糖蔗糖作为斜方晶无水形式存在，作为五水合物存在，两者都比无定形TGS更稳定。晶体从接种的水溶液中获得，对于无水物质，高于38℃; 低于38℃的五水合物。

64. 发明授权

US4335100A Method of inhibiting dextransucrase and oral compositions for use therein 失效
标题翻译：抑制葡聚糖蔗糖酯和口服组合物用于其中的方法
公开(公告)号：US4335100A
公开(公告)日：1982-06-15
申请号：US175635
申请日：1980-08-06
申请人： John F. Robyt , John N. Zikopoulos
发明人： John F. Robyt , John N. Zikopoulos
IPC分类号： A23G3/34 , A61K8/60 , A61K8/69 , A61Q11/00 , C07H3/04 , C07H3/08 , C07H5/02 , C07H5/06 , C07H11/00 , A61K7/16 , A61K9/68 , A61K31/10
CPC分类号： C07H11/00 , A23G3/346 , A61K8/60 , A61K8/69 , A61Q11/00 , C07H3/08 , C07H5/02 , C07H5/06 , A23G2200/06 , A61K2800/782
摘要： Dextransucrase synthesis of dextran from sucrose is inhibited by substituted sucrose compounds which have an inhibiting group bonded to the 5-position ring carbon. Oral compositions containing such substituted sucrose compounds can be used to control dextran formation in the mouth, and dextran comprises the principal component of dental plaque.
摘要翻译：来自蔗糖的葡聚糖的葡聚糖蔗糖酶合成由具有与5位环碳键合的抑制基团的取代的蔗糖化合物抑制。含有这种取代的蔗糖化合物的口服组合物可用于控制口腔中的葡聚糖形成，并且葡聚糖包括牙斑的主要成分。

65. 发明授权

US4296139A Bittering agents 失效
标题翻译：苦涩剂
公开(公告)号：US4296139A
公开(公告)日：1981-10-20
申请号：US85402
申请日：1979-10-17
申请人： Riaz A. Khan , Michael R. Jenner
发明人： Riaz A. Khan , Michael R. Jenner
IPC分类号： A01N43/16 , A23K1/16 , A23L1/226 , A23L1/236 , C07H5/02 , C07H13/04 , C07H13/08 , C07H15/04 , A23L2/00 , A23L2/02
CPC分类号： C07H5/02 , A01N43/16 , A23K20/163 , A23L27/2052 , A23L27/37 , C07H13/04 , C07H13/08 , C07H15/04 , Y02P20/55
摘要： A new chlorinated sucrose derivative, 2,6,1',6'-tetrachloro-2,6,1',6'-tetradeoxy-mannosucrose, is used as a bittering agent, e.g. to replace quinine sulphate, in ingestible compositions such as Indian tonic water, and in non-ingestible compositions.

66. 发明授权

US4284763A Sugar acetals, their preparation and use 失效
标题翻译：糖缩醛，其制备和使用
公开(公告)号：US4284763A
公开(公告)日：1981-08-18
申请号：US133975
申请日：1980-03-26
申请人： Leslie A. W. Thelwall , Leslie Hough , Anthony C. Richardson
发明人： Leslie A. W. Thelwall , Leslie Hough , Anthony C. Richardson
IPC分类号： C07H17/00 , C07H5/02 , C07H9/04 , C07H13/00 , C07H13/06 , C07H15/04 , C07H9/02
CPC分类号： C07H5/02 , C07H13/00 , C07H13/06 , C07H15/04 , C07H9/04
摘要： Novel sugar acetals such as those of formula ##STR1## where R.sup.a is hydrocarbyl; R.sup.b and R.sup.c are hydrogen or hydrocarbyl; R.sup.3' R.sup.4' and R.sup.6' are hydrogen or R.sup.4' with R.sup.3' or R.sup.6' is ##STR2## are made from 1,4-linked reducing disaccharides by a new exchange acetalation process in which the solvent is omitted. The sugar acetals have free hydroxy groups on the ring which groups can be converted to other substituents, e.g. chlorodeoxy or fatty acid acyl. After deprotection, the corresponding derivative of the initial disaccharide is obtained.
摘要翻译：新型糖缩醛，例如其中R a为烃基的式（Ⅰ）化合物; Rb和Rc是氢或烃基; R 3'R 4'和R 6'是氢或R 4'，其中R 3'或R 6'是通过新的交换缩醛化方法由1,4-连接的还原二糖制成的，其中省略了溶剂。糖缩醛在环上具有游离羟基，这些基团可以转化成其它取代基，例如。氯代脱氧或脂肪酸酰基。脱保护后，得到初始二糖的相应衍生物。

67. 发明授权

US4225590A Male fertility-inhibiting compositions of 6-chlorodeoxy-saccharides 失效
标题翻译： 6-氯脱氧糖的男性生育抑制组合物
公开(公告)号：US4225590A
公开(公告)日：1980-09-30
申请号：US886531
申请日：1978-03-14
申请人： Geoffrey M. H. Waites , William C. L. Ford , Riaz A. Khan , Haydn F. Jones
发明人： Geoffrey M. H. Waites , William C. L. Ford , Riaz A. Khan , Haydn F. Jones
IPC分类号： A61K31/70 , C07H5/02
CPC分类号： A61K31/7004 , C07H5/02 , Y10S514/841
摘要： A male fertility-inhibiting composition in unit dosage form, contains as an active ingredient a 6-chlorodeoxy-saccharide containing a pyranose or furanose ring of the formula ##STR1## where A represents the remainder of the pyranose or furanose ring, and has the formula C.sub.4 H.sub.7 O.sub.4 X (where X represents a hydrogen atom or another pyranose or furanose ring) in association with a physiologically acceptable carrier or excipient. The saccharide preferably contains a pyranose ring or furanose ring of the formula ##STR2## Also a method of controlling fertility in men or male animals comprises administering thereto a 6-chlorodeoxy-saccharide as defined above.
摘要翻译：单位剂型中的雄性生育抑制组合物含有含有式（I）的吡喃糖或呋喃糖环的6-氯脱氧糖的活性成分，其中A代表吡喃糖或呋喃糖环的剩余部分，和具有与生理学上可接受的载体或赋形剂相关的式C4H7O4X（其中X表示氢原子或另一种吡喃糖或呋喃糖环）。糖类优选含有下式的吡喃糖环或呋喃糖环。另外，一种在男性或雄性动物中控制生育力的方法包括向其施用如上定义的6-氯脱氧糖。

68. 发明申请

US20230098432A1 SYNTHESIS OF GLYCOSYL FLUORIDES 有权
公开(公告)号：US20230098432A1
公开(公告)日：2023-03-30
申请号：US17801638
申请日：2021-02-24
申请人： CarboCode S.A.
发明人： Ferenc Horvath , Györgyi Osztrovszky , Gyula Dekany , Agathe Bronikowski , Piroska Kovacs-Penzes , Rafael Soares , Jorge Santos , Fabio Pereira , Osama Mahmoud , Nagy Csaba , Dário Jorge Silva Neves
IPC分类号： C12P19/18 , C07H5/02 , C12N9/10
摘要： The present invention relates to a method for producing a glycosyl fluoride of interest, the method comprising providing an internalized exogenous precursor and a genetically modified cell, wherein one or more glycosylation reactions can be performed on the exogenous precursor in the genetically modified cell, the genetically modified cell comprising one or more nucleic acid sequences encoding one or more glycosyltransferase enzymes. The present invention further relates to a compound of the following formula: 2b.

69. 发明授权

US11471394B2 Oral care compositions containing deoxy sugar antimetabolites 有权
公开(公告)号：US11471394B2
公开(公告)日：2022-10-18
申请号：US16884958
申请日：2020-05-27
申请人： Colgate-Palmolive Company , The Forsyth Institute
发明人： Lyndsay Schaeffer-Korbylo , Jorge Frias-Lopez
IPC分类号： A61K8/60 , A61Q11/00 , A61K8/69 , C07H5/06 , C07H5/02 , C07H3/08
摘要： Described herein are oral care compositions comprising a deoxy sugar antimetabolite and methods of inhibiting microbial biofilm formation and/or degrading a microbial biofilm in a subject.

70. 发明授权

US10899783B2 Liquid-liquid extraction of DMF 有权
公开(公告)号：US10899783B2
公开(公告)日：2021-01-26
申请号：US16450256
申请日：2019-06-24
申请人： Tate & Lyle Technology Limited
发明人： David Dentel , Thomas Eilers , Edward Micinski
IPC分类号： C07H5/02 , C07H1/00 , C07H1/06 , C07H13/04 , B01D11/04 , B01D11/00
摘要： The present invention relates to a method for the chlorination of a sucrose-6-acylate to produce a 4,1′,6′-trichloro-4,1′,6′-trideoxy-galactosucrose-6-acylate wherein said method includes steps of: (i) combining the sucrose-6-acylate with a chlorinating agent in a reaction vehicle comprising a tertiary amide to afford a mixture; (ii) heating said mixture for a heating period in order to provide chlorination of sucrose-6-acylate at the 4,1′ and 6′ positions thereof; and (iii) quenching the product stream of (ii) to produce a 4,1′,6′-trichloro-4,1′,6′-trideoxy-galactosucrose-6-acylate; wherein before said quenching, a portion of said tertiary amide is removed by extraction into a solvent in which said tertiary amide is at least partially soluble.

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