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1.发明申请Novel method of stabilizing diagnostic and therapeutic compounds in a cationic carrier system 审中-公开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。
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公开(公告)号：US06323372B1
公开(公告)日：2001-11-27
申请号：US09546108
申请日：2000-04-10
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。
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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。
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4.发明申请Novel method of stabilizing diagnostic and therapeutic compounds in a cationic carrier system 审中-公开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。
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公开(公告)号：US06664426B1
公开(公告)日：2003-12-16
申请号：US09592214
申请日：2000-06-12
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。
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6.发明申请Method of Producing A Cationic Liposomal Preparation Comprising A Lipophilic Compound 有权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。
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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.
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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。
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9.发明授权Method of producing a cationic liposomal preparation comprising a lipophilic compound 有权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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10.发明授权Method of producing a cationic liposomal preparation comprising a lipophilic compound 有权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：US08075913B2
公开(公告)日：2011-12-13
申请号：US12859000
申请日：2010-08-18
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
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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