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1. 发明申请

WO2013063336A1 REGIOSELECTIVELY SUBSTITUTED CELLULOSE ESTERS AND EFFICIENT METHODS OF PREPARING THEM 审中-公开
标题翻译：选择性取代的纤维素酯和有效的制备方法
公开(公告)号：WO2013063336A1
公开(公告)日：2013-05-02
申请号：PCT/US2012/062011
申请日：2012-10-25
申请人： VIRGINIA TECH INTELLECTUAL PROPERTIES, INC.
发明人： EDGAR, Kevin, J. , XU, Daiqiang , ZHENG, Xueyan
IPC分类号： C08B3/06 , C08B3/00 , C08L1/10 , C08J5/18
CPC分类号： C08B3/24 , C08B3/00 , C08B3/06 , C08B3/08 , C08B3/16 , C08J5/18 , C08J2301/10 , C08L1/10
摘要： Embodiments of the invention provide regioselectively substituted carbohydrate and polysaccharide derivatives, such as cellulose esters, and methods for preparing them. Particular methods of the invention include deacylation of esters using tetrabutyl ammonium fluoride to obtain selective substitution at desired hydroxyl position(s) of the ester. Preferred is deacylation of an ester, which shows selectivity for removal of acyl groups from the ester of the secondary alcohols at C-2 and C-3, and which affords cellulose-6- O - esters with high regioselectivity by a simple one-step process employing no protective groups. Inventive regioselectively substituted cellulose esters can be prepared by such methods to obtain esters with the anhydroglucose repeating units (I), wherein R 1 , R 2 , and R 3 are each independently chosen from a hydrogen atom, and, whether substituted or unsubstituted, branched or unbranched, an alkanoyl group, an aroyl group and a hetero aroyl group. In embodiments, the alkanoyl, aroyl and hetero aroyl groups can comprise from 1-20 carbon atoms.
摘要翻译：本发明的实施方案提供区域选择性取代的碳水化合物和多糖衍生物，例如纤维素酯，以及制备它们的方法。本发明的具体方法包括使用四丁基氟化铵对酯进行脱酰化，以在酯的所需羟基位置获得选择性取代。优选的是酯的脱酰基，其表现出在C-2和C-3上从仲醇的酯中除去酰基的选择性，并且通过简单的一步提供具有高区域选择性的纤维素-6-O-酯不使用保护基的方法。本发明的区域选择性纤维素酯可以通过这样的方法制备，以获得具有脱水葡萄糖重复单元（I）的酯，其中R 1，R 2和R 3各自独立地选自氢原子，并且无论是取代或未取代的，支链或非支链的，烷酰基，芳酰基和杂芳酰基。在实施方案中，烷酰基，芳酰基和杂芳基可以包含1-20个碳原子。

2. 发明申请

WO2015048408A1 CROSS-METATHESIZED POLYSACCHARIDE DERIVATIVES AND PROCESSES FOR PREPARING THEM 审中-公开
标题翻译：交联金属多糖衍生物及其制备方法
公开(公告)号：WO2015048408A1
公开(公告)日：2015-04-02
申请号：PCT/US2014/057661
申请日：2014-09-26
申请人： VIRGINIA TECH INTELLECTUAL PROPERTIES, INC. , EDGAR, Kevin, J. , MENG, Xiangtao , MATSON, John
发明人： EDGAR, Kevin, J. , MENG, Xiangtao , MATSON, John
IPC分类号： C07C319/18
CPC分类号： C08B3/16 , A61K47/38 , C08B3/00 , C08B3/14 , C08B37/0018 , C08B37/0021
摘要： Methods for the cross-metathesis of polysaccharides with one or more olefin-terminated side chains and cross-metathesized products are described. In an exemplary embodiment, a method for the synthesis of cellulose ω-carboxyesters via olefin cross-metathesis is described. Conditions of the reactions were relatively mild and the olefin-substituted polysaccharides and the appropriate monomeric olefin partners appear to follow Grubbs rules as summarized herein. The compounds and methods may be useful for structure-property studies, particularly those aimed at developing polymers for drug delivery, such as for controlled-release drug delivery systems, controlled-release coatings, increasing bioavailability of drugs, and maintaining drug supersaturation in the GI tract.
摘要翻译：描述了多糖与一种或多种烯烃封端的侧链和交叉复合产物的交叉复分解方法。在一个示例性实施方案中，描述了通过烯烃交叉复分解合成纤维素ω-羧酸酯的方法。反应条件相对温和，烯烃取代的多糖和适当的单体烯烃合成物似乎遵循本文总结的Grubbs规则。化合物和方法可用于结构性质研究，特别是那些旨在开发用于药物递送的聚合物的那些，例如用于控制释放药物递送系统，控释包衣，药物的增加的生物利用度和维持GI中的药物过饱和度道。

3. 发明申请

WO2013058751A1 CELLULOSE DERIVATIVES FOR ENHANCING BIOAVAILABILITY OF FLAVONOIDS 审中-公开
标题翻译：用于增强黄酮生物利用度的纤维素衍生物
公开(公告)号：WO2013058751A1
公开(公告)日：2013-04-25
申请号：PCT/US2011/056946
申请日：2011-10-19
申请人： VIRGINIA TECH INTELLECTUAL PROPERTIES, INC. , EDGAR, Kevin, J. , LI, Bin , TAYLOR, Lynne , ILEVBARE, Grace , KONECKE, Stephanie
发明人： EDGAR, Kevin, J. , LI, Bin , TAYLOR, Lynne , ILEVBARE, Grace , KONECKE, Stephanie
IPC分类号： A61K9/14 , A61K47/38 , A61K47/30 , A61K31/12 , A61K31/05 , A61P35/00
CPC分类号： A61K31/12 , A61K9/1652 , A61K31/05 , A61K31/352 , A61K31/37
摘要： The present invention relates to delivery systems to enhance the bioavailability of flavonoids to improve human health. Flavonoids of interest include but are not limited to curcumin, resveratrol, ellagic acid, naringenin, and quercetin. Flavonoids are important in part because they are known to have beneficial effects on human health, including cardioprotective, antioxidant, and anticancer effects. Utility has been limited by low bioavailability, both in the sense of requiring high doses and in that it has been difficult to carry out proper dose-response studies in the absence of methods to control the actual dose administered. In addition to pharmaceutical applications, there are potential nutraceutical uses, for example in supplements that might be sold in health food stores and pharmacies.
摘要翻译：本发明涉及递送系统以提高类黄酮的生物利用度以改善人体健康。感兴趣的类黄酮包括但不限于姜黄素，白藜芦醇，鞣花酸，柚皮苷和槲皮素。黄酮类化合物很重要，部分原因是它们对人体健康有益，包括心脏保护作用，抗氧化剂和抗癌作用。实用性受到低生物利用度的限制，无论是在需要高剂量的意义上，并且在没有控制施用实际剂量的方法的情况下难以进行适当的剂量反应研究。除了制药应用之外，还有潜在的营养保健用途，例如可能在保健食品商店和药店销售的补充品。

4. 发明申请

WO2015139029A2 POLYSACCHARIDE DERIVATIVES AND CROSS-METATHESIS PROCESSES FOR PREPARING THEM 审中-公开
标题翻译：多糖衍生物和制备它们的跨金属过程
公开(公告)号：WO2015139029A2
公开(公告)日：2015-09-17
申请号：PCT/US2015/020726
申请日：2015-03-16
申请人： VIRGINIA TECH INTELLECTUAL PROPERTIES, INC. , EDGAR, Kevin, J. , MENG, Xiangtao , DONG, Yifan
发明人： EDGAR, Kevin, J. , MENG, Xiangtao , DONG, Yifan
IPC分类号： C08L33/08
CPC分类号： C08B3/16 , C08B3/02 , C08B3/22 , C08B11/193 , C08B11/20 , C08B37/00 , C08F290/10 , C08L33/02 , C08L33/12
摘要： Methods for the cross-metathesis of polysaccharides with one or more olefin-terminated side chains and cross-metathesized products are described. In an exemplary embodiment, a method for the synthesis of cellulose ω-carboxyesters via olefin cross-metathesis with acrylates is described. Conditions of the reactions were relatively mild and the olefin-substituted polysaccharides and the appropriate acrylate partners appear to follow Grubbs rules as summarized herein. Additionally, a method of hydrogenation of the cross-metathesized product is described. The compounds and methods may be useful for waterborne coating applications, adhesives, lubricants, or any product in need of dispersion in an aqueous media.
摘要翻译：描述了多糖与一种或多种烯烃封端的侧链和交叉复合产物的交叉复分解方法。在一个示例性实施方案中，描述了通过烯丙基交错复分解与丙烯酸酯合成纤维素ω-羧酸酯的方法。反应条件相对温和，烯烃取代的多糖和合适的丙烯酸酯配合物似乎遵循本文总结的Grubbs规则。另外，描述了交叉复合产物的氢化方法。化合物和方法可用于水性涂料应用，粘合剂，润滑剂或需要在水性介质中分散的任何产品。

5. 发明申请

WO2013106433A1 CELLULOSE DERIVATIVES FOR INHIBITING CRYSTALLIZATION OF POORLY WATER-SOLUBLE DRUGS 审中-公开
标题翻译：用于抑制不溶性水溶性药物结晶的纤维素衍生物
公开(公告)号：WO2013106433A1
公开(公告)日：2013-07-18
申请号：PCT/US2013/020835
申请日：2013-01-09
申请人： VIRGINIA TECH INTELLECTUAL PROPERTIES, INC. , PERDUE RESEARCH FOUNDATION
发明人： EDGAR, Kevin, J. , LI, Bin , TAYLOR, Lynne , ILEVBARE, Grace , WILLIAMS, Stephanie, M. , LIU, Haoyu
IPC分类号： A61K47/38 , A61K47/30 , A61K9/08 , A61K31/70
CPC分类号： A61K47/38 , A61K9/146 , A61K31/05 , A61K31/352 , A61K31/357 , A61K31/40 , A61K31/427 , A61K31/536 , A61K31/70 , C08B3/00
摘要： The present invention relates to the fields of chemistry and pharmaceuticals. Embodiments of the invention provide cellulose esters useful for inhibiting solution crystallization of drugs. Specific polymers of the invention include cellulose esters of formula (I) : wherein n of the ω-carboxyalkanoyl group, Formula (II), is 3, 4, 6, or 8 to provide a ω-carboxyalkanoyl group chosen from succinoyl, glutaroyl, adipoyl, sebacyl, and suberyl groups; and wherein R is chosen from : a hydrogen atom; and an alkanoyl group chosen from acetyl, propionyl, butyryl, valeroyl, hexanoyl, nonanoyl, decanoyl, lauroyl, palmitoyl, and stearoyl groups; wherein there is a total degree of substitution of the alkanoyl group and the ω-carboxyalkanoyl group of at least 2.0; and wherein the polymer comprises m repeating units where n = 1 to 1,000,000, or 10 to 100,000, or 100 to 1,000, such as 1 to 6,000. Embodiments further include compositions comprising cellulose esters and poorly water-soluble drugs, which compositions exhibit greater solubility and stability in solution as compared to the drugs alone. Drugs that can be used in combination with such polymers include but are not limited to ritonavir, efavirenz, etravirine, celecoxib, clarithromycin, curcumin, ellagic acid, quercetin, naringenin, and resveratrol. Methods for making and using the compounds and compositions are also included within the scope of the invention.
摘要翻译：本发明涉及化学和药物领域。本发明的实施方案提供了可用于抑制药物溶液结晶的纤维素酯。本发明的具体聚合物包括式（I）的纤维素酯：其中式（II）的ω-羧基烷酰基中的n为3,4,6或8，以提供选自琥珀酰基，戊酰基，己二酰基，癸二酰基和辛二酸基; 并且其中R选自：氢原子; 和选自乙酰基，丙酰基，丁酰基，戊酰基，己酰基，壬酰基，癸酰基，月桂酰基，棕榈酰基和硬脂酰基的烷酰基; 其中烷酰基和ω-羧基烷酰基的总取代度为至少2.0; 并且其中所述聚合物包含m个重复单元，其中n = 1至1,000,000，或10至100,000，或100至1,000，如1至6,000。实施方案还包括包含纤维素酯和水溶性差的药物的组合物，与单独的药物相比，该组合物在溶液中表现出更大的溶解度和稳定性。可以与这些聚合物组合使用的药物包括但不限于利托那韦，依法韦仑，依伐维林，塞来昔布，克拉霉素，姜黄素，鞣花酸，槲皮素，柚皮苷和白藜芦醇。制备和使用化合物和组合物的方法也包括在本发明的范围内。

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