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21. 发明授权

US06610671B2 Cyclodextrin sulfonates, guest inclusion complexes methods of making the same and related materials 失效
公开(公告)号：US06610671B2
公开(公告)日：2003-08-26
申请号：US10042306
申请日：2002-01-11
申请人： Charles M. Buchanan , Steven N. Falling , Juanelle L. Lambert , Shannon E. Large , Jozsef Szejtli , Lajos Szente , Laszlo Jicsinszky
发明人： Charles M. Buchanan , Steven N. Falling , Juanelle L. Lambert , Shannon E. Large , Jozsef Szejtli , Lajos Szente , Laszlo Jicsinszky
IPC分类号： A61K31724
CPC分类号： G01N30/482 , B01D15/3833 , B01J20/262 , B01J20/265 , B01J20/285 , B01J20/29 , B01J2220/54 , C07C309/08 , C08B37/0012 , C08B37/0015 , C08G63/6884
摘要： This invention relates to new cyclodextrin derivatives, processes for producing these cyclodextrin derivatives, and inclusion complexes comprised of the new cyclodextrin derivatives and guest molecules, as well as methods of making such materials and related materials and methods of using the same.

22. 发明授权

US06432928B1 Complexes and their compositions 失效
标题翻译：复合物及其组成
公开(公告)号：US06432928B1
公开(公告)日：2002-08-13
申请号：US08836390
申请日：1997-08-01
申请人： Lajos Szente , Jozsef Szejtli , Maria Vikmon nee Kiraly , Julia Szeman
发明人： Lajos Szente , Jozsef Szejtli , Maria Vikmon nee Kiraly , Julia Szeman
IPC分类号： A61K31715
CPC分类号： B82Y5/00 , A61K47/6951 , C07D305/14
摘要： This invention provides inclusion complexes of Taxol ((2aR-(a&agr;,4&bgr;,4&agr;&bgr;,6&bgr;,9&agr;(&agr;R*,&bgr;S*),11&agr;,12&agr;,12a&agr;,12b&agr;))-&bgr;-(benzoylamino)-&agr;-hydroxy-benzene-propanoic acid 6,12-b-bis(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclo-deca-(3,4)-benz-(1,2-b)-oxeth-9-yl-ester)) or Taxotere (butoxycarbonyl-10-desacetyl-N-debenzoyl-Taxol) or Taxus extracts formed with a cyclodextrin derivative and a co-solvent. This invention relates to pharmaceutical composition with increased water-solubility and stability. This invention provides the process for the preparation of an inclusion complex of Taxol or Taxotere or a brevifolia extract of Taxus formed with a cyclodextrin derivative and a co-solvent. This invention relates to pharmaceutical composition, containing as active ingredient an effective amount of an inclusion complex of Taxol or Taxotere or a Taxus brevifolia extract formed with a cyclodextrin derivative, preferably heptakis-2,6-0 dimethyl-&bgr;-cyclodextrin, random methylated &bgr;-cyclodextrin, succinylmethyl-&bgr;-cyclodextrin and a co-solvent together with usual filling, diluting and other auxiliaries generally used in the pharmaceutical industry.
摘要翻译：本发明提供了紫杉醇（（2aR-（aalpha，4beta，4alphabeta，6beta，9alpha（αR*，βS*），11alpha，12alpha，12aalpha，12bapha））-β-（苯甲酰氨基）-α-羟基 - 苯 - 丙酸6,12-b-双（乙酰氧基）-12-（苯甲酰氧基）-2a，3,4,4a，5,6,9,10,11,12,12a，12b-十二氢-4,11- 二羟基-4a，8,13,13-四甲基-5-氧代-7,11-亚甲基-1H-环十二烷基（3,4） - 苯并（1,2-b） - 氧代-9-基 - 酯））或泰索帝（丁氧羰基-10-脱乙酰基-N-脱苯甲酰基紫杉醇）或由环糊精衍生物和共溶剂形成的紫杉提取物。本发明涉及具有增加的水溶性和稳定性的药物组合物。本发明提供了制备紫杉醇或泰索帝的包合物的方法或由环糊精衍生物和助溶剂形成的紫杉属的短叶提取物的方法。本发明涉及药物组合物，其含有有效量的紫杉醇或泰索帝或用环糊精衍生物形成的短叶紫杉提取物的有效量的混合物，优选七 - 2,6-0-二甲基-β-环糊精，随机甲基化β 环糊精，琥珀酰基甲基-β-环糊精和共溶剂，以及通常在制药工业中使用的填充，稀释和其它助剂。

23. 发明授权

US5403840A Inclusion complexes of N-ethoxycarbonyl 1-3-morpholino-sydnonimine or salts formed with cyclodextrin-derivatives, preparation thereof and pharmaceutical compositions containing the same 失效
标题翻译： N-乙氧基羰基-3-吗啉代 - 脱水亚胺或与环糊精衍生物形成的盐的包合物，其制备方法和含有它们的药物组合物
公开(公告)号：US5403840A
公开(公告)日：1995-04-04
申请号：US807852
申请日：1992-01-02
申请人： Maria Vikmon , Jozsef Szejtli , Jozsef Gaal , Istvan Hermecz , Agnes Horvath , Katalin Marmarosi , Gabor Horvath , Iren Munkacsi
发明人： Maria Vikmon , Jozsef Szejtli , Jozsef Gaal , Istvan Hermecz , Agnes Horvath , Katalin Marmarosi , Gabor Horvath , Iren Munkacsi
IPC分类号： C07D413/04 , A61K31/41 , A61K31/42 , A61K31/4245 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K47/40 , A61K47/48 , A61P9/08 , A61P9/10 , C07D265/28 , C07D271/04 , C07D271/10 , C08B37/00 , C08B37/06 , C08B37/16 , C06B37/16
CPC分类号： C08B37/0015 , C07D271/04
摘要： The invention relates to inclusion complexes of N-ethoxycarbonyl-3-morpholino-sydnonimine or its salts formed with a cyclodextrin derivatives, preparation thereof and pharmaceutical compositions containing the same.The inclusion complex of N-ethoxycarbonyl-3-morpholino-sydnonimine or its salt formed with cyclodextrin derivative is prepared bya) reacting the N-ethoxycarbonyl-3-morpholino-sydnonimine or its salt and the cyclodextrin derivative in a solvent medium, and if desired recovering the complex from the solution by dehydration, orb) high energy milling of the N-ethoxycarbonyl-3-morpholino-sydnonimine or its salt and the cyclodextrin derivative.
摘要翻译： PCT No.PCT / HU91 / 00012 Sec。 371日期1992年1月2日 102（e）日期1992年1月2日PCT 1991年3月28日PCT公布。公开号WO91 / 14680 日本1991年10月3日。本发明涉及N-乙氧基羰基-3-吗啉代 - 脱水亚胺或其与环糊精衍生物形成的盐的包合络合物，其制备方法和含有它们的药物组合物。通过以下步骤制备N-乙氧基羰基-3-吗啉代 - 脱水亚胺或其与环糊精衍生物形成的盐的包合络合物：a）在溶剂介质中使N-乙氧基羰基-3-吗啉代 - 脱水亚胺或其盐与环糊精衍生物反应，如果需要通过脱水从溶液中回收配合物，或b）N-乙氧基羰基-3-吗啉代 - 脱水亚胺或其盐和环糊精衍生物的高能研磨。

24. 发明授权

US5198430A Inclusion complexes with silybinin, their preparation and pharmaceutical compositions containing them 失效
标题翻译：包含与苯乙烯，他们的制剂和含有他们的药物组合物的复合物
公开(公告)号：US5198430A
公开(公告)日：1993-03-30
申请号：US593933
申请日：1990-10-09
申请人： Umberto Valcavi , Vincenzo Monterosso , Roberto Caponi , Enrico Bosone , Wilfried Wachter , Jozsef Szejtli
发明人： Umberto Valcavi , Vincenzo Monterosso , Roberto Caponi , Enrico Bosone , Wilfried Wachter , Jozsef Szejtli
IPC分类号： C07D407/04 , A61K31/00 , A61K31/335 , A61K31/35 , A61K31/715 , A61K47/40 , A61P1/16 , C08B20060101 , C08B37/00 , C08B37/16
CPC分类号： C08B37/0015
摘要： The invention relates to inclusion complexes of Silybinin with a cyclodextrin selected from the group consisting of .alpha.-, .beta.- and .gamma.-cyclodextrin and a suitable derivative thereof and to the method for the preparation thereof. The inclusion complexes of Silybinin showed a highly improved bioavailability in comparison to Silybinin which makes them particularly interesting in the treatment of various hepatotoxic conditions.

25. 发明授权

US4542211A Process for the manufacture of heptakis-[2,6-di-O-methyl]-beta-cyclodextrin 失效
标题翻译：制备七 - [2,6-二-O-甲基] - β-环糊精的方法
公开(公告)号：US4542211A
公开(公告)日：1985-09-17
申请号：US586203
申请日：1984-03-05
申请人： Jozsef Szejtli , Andras Liptak , Pal Nanasi , Peter Fugedi , Ildiko Jodal , Lili Kandra , Lorant Janossy
发明人： Jozsef Szejtli , Andras Liptak , Pal Nanasi , Peter Fugedi , Ildiko Jodal , Lili Kandra , Lorant Janossy
IPC分类号： C08B37/16 , C08B37/00
CPC分类号： C08B37/0012
摘要： The invention relates to a process for the manufacture of heptakis-[2,6-di-O-methyl]-beta-cyclodextrin by methylating beta-cyclodextrin in an organic phase wherein beta-cyclodextrin is methylated with dimethylsulfate in the presence of an alkalihydroxide at temperatures of from -10.degree. to 0.degree. C.
摘要翻译：本发明涉及通过在有机相中甲基化β-环糊精制备七 - [2,6-二-O-甲基]-β-环糊精的方法，其中β-环糊精在碱金属氢氧化物存在下与硫酸二甲酯进行甲基化在-10℃至0℃的温度下

26. 发明授权

US4529608A Honey powder preserving its natural aroma components 失效
标题翻译：蜂蜜粉保存其天然香气成分
公开(公告)号：US4529608A
公开(公告)日：1985-07-16
申请号：US549205
申请日：1983-11-04
申请人： Jozsef Szejtli , Marta Tardy nee Lengyel
发明人： Jozsef Szejtli , Marta Tardy nee Lengyel
IPC分类号： A23L1/00 , A23L1/08 , A23L1/22
CPC分类号： A23L27/77 , A23L21/25 , A23L27/70 , A23P10/43
摘要： A process for the preparation of honey powder preserving its natural aroma substances comprises(a) kneading 1 part by weight of honey, 0.8 part by weight of starch, pre-hydrolyzed starch or flour and 0.1-0.3 part by weight of cyclodextrin to yield a homogeneous mixture, subjecting the mixture thus obtained to thermal treatment at 100.degree. C. for 20 minutes, disintegrating the hot product obtained after thermal treatment, drying the product at a temperature of 50.degree.-55.degree. C., for 10-50 hours, adding 0.01-1.0% by weight of hydrophobic colloidal silicic acid or alkali earth stearate and grinding it to a powder; or(b) admixing 1 part by weight of honey with 6 parts by weight of a hot saturated aqueous cyclodextrin solution, freezing the homogeneous solution thus obtained, subjecting the product to lyphilization, adding 0.01-1.0% by weight of hydrophobic colloidal silicic acid or alkali earth stearate to the lyophilized product and grinding it to a powder.The advantage of the invention is that the aroma substances of honey are preserved and set free only during consumption.
摘要翻译：制备保存其天然芳香物质的蜂蜜粉的方法包括（a）捏合1重量份蜂蜜，0.8重量份淀粉，预水解淀粉或面粉和0.1-0.3重量份环糊精，得到均匀混合，将得到的混合物在100℃下热处理20分钟，将热处理后得到的热产物分解，在50-55℃的温度下干燥产物10-50小时，加入0.01-1.0重量％的疏水性胶体硅酸或碱土金属硬脂酸盐，并研磨成粉末; 或（b）将1重量份蜂蜜与6重量份热饱和水性环糊精溶液混合，冷却由此获得的均匀溶液，使产物进行裂解，加入0.01-1.0重量％的疏水胶体硅酸或碱土金属硬脂酸盐加入到冻干产品中并研磨成粉末。本发明的优点是蜂蜜的芳香物质被保存并且仅在消费期间释放。

27. 发明授权

US4528271A Process for the intensification of microbiological conversions of steroids using cyclodextrin additives 失效
标题翻译：使用环糊精添加剂加强类固醇微生物转化的过程
公开(公告)号：US4528271A
公开(公告)日：1985-07-09
申请号：US423084
申请日：1982-09-24
申请人： Eva Udvardy Nagy nee Cserey Pechany , Istvan Bartho , Gabor Hantos , Maria Trinn , Zsuzsa Vida , Jozsef Szejtli , Agnes Stadler nee Szoke , Ilona Habon , Marta Balazs nee Czurda
发明人： Eva Udvardy Nagy nee Cserey Pechany , Istvan Bartho , Gabor Hantos , Maria Trinn , Zsuzsa Vida , Jozsef Szejtli , Agnes Stadler nee Szoke , Ilona Habon , Marta Balazs nee Czurda
IPC分类号： C12P33/00 , C12P1/00 , C12P33/02 , C12P33/08 , C12P33/16 , C12P33/04 , C12P33/06 , C12P33/10 , C12P33/12 , C12P33/14 , C12P33/18 , C12P33/20
CPC分类号： C12P33/08 , C12P1/00 , C12P33/02
摘要： Microbiological conversions of cyclodextrins are intensified by adding to the reaction mixture 0.2 to 3 moles of .alpha.-, .beta.- or .gamma.-cyclodextrin or an optical mixture thereof pro mole of the steroid substrate, before, at the beginning or during the conversion. The cyclodextrin if desired, can be removed after the reaction. In this way the reaction velocity can be increased, the reaction time is reduced, the substrate concentration in the solution, i.e. its solubility is increased or the so called product inhibition may be avoided. In certain cases of more alternatives the desired reaction can be catalyzed and in this manner the selectivity is increased.
摘要翻译：在开始之前或转化期间，通过向反应混合物中加入0.2至3摩尔的α，β或γ-环糊精或其光学混合物来促进环糊精的微生物转化。如果需要，可以在反应后除去环糊精。以这种方式，可以增加反应速度，反应时间减少，溶液中的底物浓度，即其溶解度增加或者可以避免所谓的产品抑制。在更多选择的某些情况下，可以催化所需的反应，并且以这种方式增加了选择性。

28. 发明授权

US4272276A Method for the control of germination of plant seeds and growth of the seedlings 失效
标题翻译：控制植物种子萌发和幼苗生长的方法
公开(公告)号：US4272276A
公开(公告)日：1981-06-09
申请号：US040957
申请日：1979-05-21
申请人： Jozsef Szejtli , Magda Tetenyi nee Erdosi , Peter Tetenyi
发明人： Jozsef Szejtli , Magda Tetenyi nee Erdosi , Peter Tetenyi
IPC分类号： A01N43/14 , A01N31/00 , A01N43/16 , A01P21/00
CPC分类号： A01N43/16
摘要： A method of controlling seed germination and growth of the seedlings which comprises contacting plant seeds with a liquid or solid dextrin.
摘要翻译：控制种子发芽和幼苗生长的方法，其包括使植物种子与液体或固体糊精接触。

29. 发明申请

US20090110734A1 QUATERNISED AMMONIUM CYCLODEXTRIN COMPOUNDS 审中-公开
标题翻译：季铵化合物CYCLODEXTRIN化合物
公开(公告)号：US20090110734A1
公开(公告)日：2009-04-30
申请号：US12238473
申请日：2008-09-26
申请人： Georg Ludwig Kis , Christian Schoch , Jozsef Szejtli
发明人： Georg Ludwig Kis , Christian Schoch , Jozsef Szejtli
IPC分类号： A61K9/10 , C07H15/04 , A61K31/7028 , A61K38/02
CPC分类号： A61K31/724 , A61K31/196 , A61K31/4535 , C08B37/0012
摘要： Use of a compound of formula (I): wherein the symbol represents a n-valent residue derived from a cyclodextrin compound by removing n of its hydroxyl groups; n is a number greater than 0 and represents the average number of substituents of formula per molecule of said compound; h is 0 or 1; R1 is a di-valent group selected from alkylene, hydroxy alkylene, halogeno alkylene, monocyclic aralkylene, cycloalkylene and phenylene; R2, R3 and R4 are each independently of one another a group selected from alkyl, cycloalkyl, aryl, aralkyl, and cycloheteryl; xm− is a m-fold negatively charged anion; m is an integer being equal or greater than 1; and k is n/m in the preparation of an anti-infective medicament, as preservative and penetration enhancer.
摘要翻译：式（I）化合物的用途：其中符号表示通过除去其羟基而衍生自环糊精化合物的n价残基; n是大于0的数，表示每分子所述化合物的式的取代基的平均数; h为0或1; R1是选自亚烷基，羟基亚烷基，卤代亚烷基，单环亚芳基，亚环烷基和亚苯基的二价基团; R2，R3和R4各自独立地为选自烷基，环烷基，芳基，芳烷基和环戊基的基团; xm-是m-带负电荷的阴离子; m是等于或大于1的整数; 在制备抗感染药物中，k为n / m，作为防腐剂和渗透促进剂。

30. 发明申请

US20080287553A1 PHARMACEUTICAL COMPOSITIONS COMPRISING PERANHYDROCYCLODEXTRIN 审中-公开
标题翻译：药物组合物包含肾上腺皮质激素
公开(公告)号：US20080287553A1
公开(公告)日：2008-11-20
申请号：US12173439
申请日：2008-07-15
申请人： Lajos Szente , Jozsef Szejtli , Laszlo Jicsinszky , Georg Ludwig Kis , Christian Schoch
发明人： Lajos Szente , Jozsef Szejtli , Laszlo Jicsinszky , Georg Ludwig Kis , Christian Schoch
IPC分类号： A61K47/40
CPC分类号： A61K9/0048 , A61K47/40
摘要： The present invention relates to a pharmaceutical composition comprising a peranhydrocyclodextrin, a drug and a carrier, to the use of a peranhydrocyclodextrin as a drug transport enhancer (e.g. permeation enhancer), and to the use of a peranhydrocyclodextrin in the preparation of a pharmaceutical composition as a synergistic adjunctive system.
摘要翻译：本发明涉及一种包含环戊二烯环糊精，药物和载体的药物组合物，以使用环戊二烯环糊精作为药物转运增强剂（例如渗透促进剂），以及在制备药物组合物中使用环糊精协同辅助系统。

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