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1. 发明授权

US06664426B1 Ether and ester derivatives of the perborate icosahedron 有权
标题翻译：过硼酸二十面体的醚和酯衍生物
公开(公告)号：US06664426B1
公开(公告)日：2003-12-16
申请号：US09592214
申请日：2000-06-12
申请人： M. Frederick Hawthorne , Toralf Peymann , Andreas Maderna
发明人： M. Frederick Hawthorne , Toralf Peymann , Andreas Maderna
IPC分类号： C07F502
CPC分类号： C07F5/027
摘要： New boron icosahedral ethers and esters formed from Cs2[closo-B12(OH)12],; Cs[closo-1-H-1-CB11(OH)11]; and closo-1,12-H2-1,12-C2B10(OH)10 are disclosed. Also set forth are their preparation by reacting the icosahedral boranes [closo-B12H12]2−, [closo-1-CB11H12]− and closo-1,12-(CH2OH)2-1,12-C2B10H10 with an acid anhdride or acid chloride to form the ester or an alkylating agent to form the ether.
摘要翻译：由Cs2 [closo-B12（OH）12]形成的新的二十二面体醚和酯; Cs [closo-1-H-1-CB11（OH）11]; 和closo-1,12-H2-1,12-C2B10（OH）10。还阐述了它们通过使二十面体硼烷[closo-B12H12] 2-，[closo-1-CB11H12] - 和closo-1,12-（CH2OH）2-1,12-C2B10H10与酸或酰氯形成酯或烷基化剂以形成醚。

2. 发明授权

US06323372B1 Synthesis of perhydroxydodecaborate salts and related species 有权
标题翻译：全羟基十二硼酸盐和相关物质的合成
公开(公告)号：US06323372B1
公开(公告)日：2001-11-27
申请号：US09546108
申请日：2000-04-10
申请人： M. Frederick Hawthorne , Toralf Peymann , Axel Hans-Joachim Herzog
发明人： M. Frederick Hawthorne , Toralf Peymann , Axel Hans-Joachim Herzog
IPC分类号： C07F502
CPC分类号： C07F5/027
摘要： New icosahedral borohydrates Cs2[closo-B12(OH)12]; Cs[closo-1-H-1-CB11(OH)11]; and closo-1,12-H2-1,12-C2B10(OH)10 are disclosed. Also set forth are their preparation by refluxing the icosahedral boranes [closo-B12H12]2−, [closo-1-CB11H12]− and closo-1,12-(CH2OH)2-1,12-C2B10H10 with a hydroxylating agent, preferably 30%w hydrogen peroxide.
摘要翻译：新二十面体硼氢化物Cs2 [closo-B12（OH）12]; Cs [closo-1-H-1-CB11（OH）11]; 和closo-1,12-H2-1,12-C2B10（OH）10。还阐述了它们的制备方法是通过将二十面体硼烷[closo-B12H12] 2-，[closo-1-CB11H12]和closo-1,12-（CH2OH）2-1,12-C2B10H10与羟基化剂，优选 30％w过氧化氢。

3. 发明授权

US06355840B1 Synthesis of permethyldodecaborate and paramagnetic dodecaborate salt 有权
标题翻译：十二硼酸十二硼酸盐和顺磁十二硼酸盐的合成
公开(公告)号：US06355840B1
公开(公告)日：2002-03-12
申请号：US09576842
申请日：2000-05-23
申请人： M. Frederick Hawthorne , Toralf Peymann
发明人： M. Frederick Hawthorne , Toralf Peymann
IPC分类号： C07F502
CPC分类号： C07F5/05
摘要： The dodecamethyl closo-borane dianion [closo-B12(CH3)12]2− and anion [closo-B12(CH3)12]− were synthesized and characterized. Dodecamethyl-closo dodecaborate (2−) was produced from [closo-B12H12]2−, using trimethylaluminum, and methyl iodide and modified Friedel-Crafts reaction conditions. The anion was produced from the dianion by chemical oxidation using ceric (4) ammonium nitrate in acetonitrile. The anion and dianion were both characterized by 1H and 11B NMR spectroscopy, high-resolution fast atom bombardment (FAB) mass spectrometry, cyclic voltammetry, and single-crystal X-ray diffraction. The “camouflaged” polyhedral borane anion [closo-B12(CH3)12]2−, can be used as a precursor to materials that offer a broad spectrum of novel applications ranging from drug applications and supramolecular chemistry to use as a weakly-coordinating dianion.
摘要翻译：合成并表征了十二甲基交联硼烷二价阴离子[closo-B12（CH3 )12] 2-和阴离子[closo-B12（CH3 )12]]。使用三甲基铝，甲基碘和改性的Friedel-Crafts反应条件，由[closo-B12H12] 2-制备十二甲基十八硼酸盐（2-）。通过使用硝酸铈（4）硝酸铵在乙腈中的化学氧化由二阴离子生成阴离子。阴离子和二阴离子均以1H和11B NMR光谱，高分辨率快速原子轰击（FAB）质谱，循环伏安法和单晶X射线衍射为特征。 “伪装”多面体硼烷阴离子[closo-B12（CH3）12] 2-）可用作材料的前体，提供广泛的新型应用范围，从药物应用和超分子化学到用作弱配位二价阴离子。

4. 发明申请

US20100178243A1 Novel method of stabilizing diagnostic and therapeutic compounds in a cationic carrier system 审中-公开
标题翻译：在阳离子载体体系中稳定诊断和治疗化合物的新方法
公开(公告)号：US20100178243A1
公开(公告)日：2010-07-15
申请号：US12654523
申请日：2009-12-22
申请人： Heinrich Haas , Thomas Fichert , Brita Schulze , Toralf Peymann , Uwe Michaelis , Michael Teifel
发明人： Heinrich Haas , Thomas Fichert , Brita Schulze , Toralf Peymann , Uwe Michaelis , Michael Teifel
IPC分类号： A61K9/127 , A61K49/04 , A61K49/18 , A61K49/22 , A61K51/12 , A61K49/00 , A61K38/43 , A61K31/337 , A61K31/475 , A61P35/00
CPC分类号： A61K9/1271 , A61K9/1272 , A61K31/00 , A61K31/335 , A61K31/47 , A61K31/4745 , A61K47/186 , A61K47/34 , A61K47/543 , A61K47/56 , A61K47/6911 , A61K49/1812 , B82Y5/00
摘要： The present invention relates to a method of stabilizing a low molecular weight compound in a cationic liposome, wherein said compound has a low solubility in a lipid membrane and/or a low permeability across a lipid membrane. Preferrably, the compound is modified in order to increase lipid membrane solubility and/or lipid membrane permeability. After delivery of the cationic liposome to a target site, particularly a target site in an organism, the modification is reversed and the low molecular weight compound may enact its desired activity.
摘要翻译：本发明涉及在阳离子脂质体中稳定低分子量化合物的方法，其中所述化合物在脂质膜中的溶解度低，和/或脂质膜上的低渗透性。优选地，化合物被修饰以增加脂质膜溶解度和/或脂质膜渗透性。将阳离子脂质体递送到靶位点，特别是生物体中的靶位点后，修饰被逆转，低分子量化合物可以产生其所需的活性。

5. 发明申请

US20050232984A1 Non-vesicular cationic lipid formulations 审中-公开
标题翻译：非囊泡阳离子脂质制剂
公开(公告)号：US20050232984A1
公开(公告)日：2005-10-20
申请号：US10525384
申请日：2003-08-25
申请人： Heinrich Haas , Toralf Peymann
发明人： Heinrich Haas , Toralf Peymann
IPC分类号： A61K9/127 , A61K31/335 , A61K31/47 , A61K31/4745 , A61K47/18 , A61K47/48 , A61K49/18
CPC分类号： A61K9/1272 , A61K31/335 , A61K31/47 , A61K31/4745 , A61K47/543 , A61K47/56 , A61K47/6911 , A61K49/1812 , B82Y5/00
摘要： The present invention relates to a non-vesicular preparation comprising at least one cationic amphiphile in an aqueous environment, its production and use and a cationic liposome suspension obtainable thereof with increase drug trap ratio and its areas of application such as pharmacology and medicine, particularly its use as carrier system for active substances.
摘要翻译：本发明涉及包含水性环境中的至少一种阳离子两亲物，其生产和使用的非囊泡制剂及其可获得的阳离子脂质体悬浮液，其具有增加的药物捕获比率及其应用领域如药理学和药物，特别是其用作活性物质的载体系统。

6. 发明申请

US20050181038A1 Novel method of stabilizing diagnostic and therapeutic compounds in a cationic carrier system 审中-公开
标题翻译：在阳离子载体体系中稳定诊断和治疗化合物的新方法
公开(公告)号：US20050181038A1
公开(公告)日：2005-08-18
申请号：US11018575
申请日：2004-12-22
申请人： Heinrich Haas , Thomas Fichert , Brita Schulze , Toralf Peymann , Uwe Michaelis , Michael Teifel
发明人： Heinrich Haas , Thomas Fichert , Brita Schulze , Toralf Peymann , Uwe Michaelis , Michael Teifel
IPC分类号： A61K47/18 , A61K9/127 , A61K31/00 , A61K31/335 , A61K31/337 , A61K31/47 , A61K31/4745 , A61K47/24 , A61K47/28 , A61K47/34 , A61K47/48 , A61K49/00 , A61K49/18 , A61K51/12 , A61P9/00 , A61P11/06 , A61P17/02 , A61P19/02 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00
CPC分类号： A61K9/1271 , A61K9/1272 , A61K31/00 , A61K31/335 , A61K31/47 , A61K31/4745 , A61K47/186 , A61K47/34 , A61K47/543 , A61K47/56 , A61K47/6911 , A61K49/1812 , B82Y5/00
摘要： The present invention relates to a method of stabilizing a low molecular weight compound in a cationic liposome, wherein said compound has a low solubility in a lipid membrane and/or a low permeability across a lipid membrane. Preferrably, the compound is modified in order to increase lipid membrane solubility and/or lipid membrane permeability. After delivery of the cationic liposome to a target site, particularly a target site in an organism, the modification is reversed and the low molecular weight compound may enact its desired activity.
摘要翻译：本发明涉及在阳离子脂质体中稳定低分子量化合物的方法，其中所述化合物在脂质膜中的溶解度低，和/或脂质膜上的低渗透性。优选地，化合物被修饰以增加脂质膜溶解度和/或脂质膜渗透性。将阳离子脂质体递送到靶位点，特别是生物体中的靶位点后，修饰被逆转，低分子量化合物可以产生其所需的活性。

7. 发明申请

US20120087975A1 Method of Producing A Cationic Liposomal Preparation Comprising A Lipophilic Compound 有权
标题翻译：产生包含亲脂性化合物的阳离子脂质体制备方法
公开(公告)号：US20120087975A1
公开(公告)日：2012-04-12
申请号：US13278801
申请日：2011-10-21
申请人： Carsten Mundus , Christian Welz , Oliver Schramel , Heinrich Haas , Thomas Fichert , Brita Schulze , Toralf Peymann , Uwe Michaelis , Michael Teifel , Friedrich Gruber , Gerhard Winter
发明人： Carsten Mundus , Christian Welz , Oliver Schramel , Heinrich Haas , Thomas Fichert , Brita Schulze , Toralf Peymann , Uwe Michaelis , Michael Teifel , Friedrich Gruber , Gerhard Winter
IPC分类号： A61K9/127 , A61K31/337 , A61K31/4375 , A61K31/427 , A61K31/685 , A61K31/56
CPC分类号： A61K31/337 , A61K9/127 , A61K9/1272 , A61K31/335 , A61K31/47 , A61K31/4745 , A61K47/34 , A61K47/543 , A61K47/56 , A61K47/6911 , A61K49/1812 , B82Y5/00 , C07D471/14
摘要： A method for producing a cationic liposomal preparation comprising a lipophilic active compound with physical and chemical stability during manufacturing, storing and reconstituting, and further a cationic liposomal preparation obtainable by this method as well as specific cationic liposomal preparations as well as pharmaceutical compositions are disclosed.
摘要翻译：公开了一种阳离子脂质体制剂的制备方法，其包括在制造，储存和重构过程中具有物理和化学稳定性的亲脂性活性化合物，以及可通过该方法获得的阳离子脂质体制剂以及特定的阳离子脂质体制剂以及药物组合物。

8. 发明申请

US20110038926A1 Method of producing a cationic liposomal preparation comprising a lipophilic compound 有权
公开(公告)号：US20110038926A1
公开(公告)日：2011-02-17
申请号：US12859000
申请日：2010-08-18
申请人： Carsten Mundus , Christain Welz , Oliver Schramel , Heinrich Haas , Thomas Fichert , Brita Schulze , Toralf Peymann , Uwe Michaelis , Michael Teifel , Friedrich Gruber , Gerhard Winter
发明人： Carsten Mundus , Christain Welz , Oliver Schramel , Heinrich Haas , Thomas Fichert , Brita Schulze , Toralf Peymann , Uwe Michaelis , Michael Teifel , Friedrich Gruber , Gerhard Winter
IPC分类号： A61K9/127 , A61K31/337 , A61P35/00
CPC分类号： A61K31/337 , A61K9/127 , A61K9/1272 , A61K31/335 , A61K31/47 , A61K31/4745 , A61K47/34 , A61K47/543 , A61K47/56 , A61K47/6911 , A61K49/1812 , B82Y5/00 , C07D471/14
摘要： A method for producing a cationic liposomal preparation comprising a lipophilic active compound with physical and chemical stability during manufacturing, storing and reconstituting, and further a cationic liposomal preparation obtainable by this method as well as specific cationic liposomal preparations as well as pharmaceutical compositions are disclosed.

9. 发明申请

US20070148221A1 Method of producing lipid complexed camptothecin-carboxylate 审中-公开
标题翻译：产生脂质复合喜树碱 - 羧酸盐的方法
公开(公告)号：US20070148221A1
公开(公告)日：2007-06-28
申请号：US10584349
申请日：2004-12-23
申请人： Heinrich Haas , Christian Welz , Thomas Fichert , Ralf Mehrwald , Toralf Peymann
发明人： Heinrich Haas , Christian Welz , Thomas Fichert , Ralf Mehrwald , Toralf Peymann
IPC分类号： A61K9/127 , A61K31/4745
CPC分类号： A61K31/4745 , A61K9/1272 , A61K9/1277
摘要： An improved method for producing a cationic liposomal preparation comprising a camptothecin drug with enhanced physical and chemical stability, a cationic liposomal preparation obtainable by this method and pharmaceutical compositions thereof are disclosed.
摘要翻译：公开了一种用于生产包含具有增强的物理和化学稳定性的喜树碱药物的阳离子脂质体制剂的改进方法，可通过该方法获得的阳离子脂质体制剂及其药物组合物。

10. 发明授权

US08663606B2 Method of producing a cationic liposomal preparation comprising a lipophilic compound 有权
标题翻译：制备包含亲脂性化合物的阳离子脂质体制剂的方法
公开(公告)号：US08663606B2
公开(公告)日：2014-03-04
申请号：US13278801
申请日：2011-10-21
申请人： Carsten Mundus , Christian Welz , Oliver Schramel , Heinrich Haas , Thomas Fichert , Brita Schulze , Toralf Peymann , Uwe Michaelis , Michael Teifel , Friedrich Gruber , Gerhard Winter
发明人： Carsten Mundus , Christian Welz , Oliver Schramel , Heinrich Haas , Thomas Fichert , Brita Schulze , Toralf Peymann , Uwe Michaelis , Michael Teifel , Friedrich Gruber , Gerhard Winter
IPC分类号： A61K9/127 , A61K31/685 , A61K31/56 , A61K31/4375 , A61K31/427 , A61K31/337
CPC分类号： A61K31/337 , A61K9/127 , A61K9/1272 , A61K31/335 , A61K31/47 , A61K31/4745 , A61K47/34 , A61K47/543 , A61K47/56 , A61K47/6911 , A61K49/1812 , B82Y5/00 , C07D471/14
摘要： A method for producing a cationic liposomal preparation comprising a lipophilic active compound with physical and chemical stability during manufacturing, storing and reconstituting, and further a cationic liposomal preparation obtainable by this method as well as specific cationic liposomal preparations as well as pharmaceutical compositions are disclosed.
摘要翻译：公开了一种阳离子脂质体制剂的制造方法，其包括在制造，储存和重构过程中具有物理和化学稳定性的亲脂性活性化合物，以及可通过该方法获得的阳离子脂质体制剂以及特定的阳离子脂质体制剂以及药物组合物。

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