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公开(公告)号：US06326353B1
公开(公告)日：2001-12-04
申请号：US08035443
申请日：1993-03-23
IPC分类号： A61K3812
CPC分类号： A61K9/1271 , A61K47/62 , A61K47/6911 , Y10S530/812
摘要： A liposome composition comprising small, surface-bound effector molecules is disclosed. The liposomes have a surface layer of hydrophilic polymer chains, for enhanced circulation time in the bloodstream. The effector molecules are attached to the distal ends of the polymer chains. In one embodiment, the effector is polymyxin B, for treatment of septic shock.
摘要翻译： 公开了包含小的表面结合效应分子的脂质体组合物。 脂质体具有亲水性聚合物链的表面层，用于增强血流中的循环时间。 效应分子连接到聚合物链的末端。 在一个实施方案中，效应物是多粘菌素B，用于治疗败血性休克。
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公开(公告)号：US5939096A
公开(公告)日：1999-08-17
申请号：US865005
申请日：1997-05-29
IPC分类号： A61K9/127
CPC分类号： A61K9/1278
摘要： A method of stably encapsulating a weak acid drug in liposomes, at a high concentration, is disclosed. The method employs a proton shuttle mechanism involving the salt of a weak acid to generate a higher inside/lower outside pH gradient. The weak acid compound accumulates in liposomes in response to this gradient, and may be retained in the liposomes by cation-promoted precipitation or low permeability across the liposome transmembrane barrier. Also disclosed is a reagent combination for practicing the method, and a liposome composition formed by the method.
摘要翻译： 公开了一种在脂质体中以高浓度稳定地包封弱酸药物的方法。 该方法采用涉及弱酸盐的质子穿梭机制以产生较高的内/外外pH梯度。 弱酸化合物响应于该梯度而积聚在脂质体中，并且可以通过阳离子促进的沉淀或穿过脂质体跨膜屏障的低渗透性而保留在脂质体中。 还公开了用于实施该方法的试剂组合和通过该方法形成的脂质体组合物。
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公开(公告)号：US5542987A
公开(公告)日：1996-08-06
申请号：US364586
申请日：1994-12-27
申请人： Shimon Gatt , Yechezkel Barenholz , Herve Bercovier , Zvi Eldar
发明人： Shimon Gatt , Yechezkel Barenholz , Herve Bercovier , Zvi Eldar
CPC分类号： B09C1/10 , A62D3/02 , A62D2101/20 , A62D2101/22 , F02B2075/027 , H05K3/26
摘要： The invention provides a method for cleaning the surfaces of a motor vehicle which is contaminated with wastes containing organic or lipophilic deposits, comprising applying liposomes thereto, which liposomes modify the physical properties of the wastes to increase the polarity and wettability thereof.
摘要翻译： 本发明提供了一种清洁机动车辆的表面的方法，其被含有有机或亲油沉积物的废物污染，包括向其中施加脂质体，该脂质体改变废物的物理性质以增加其极性和润湿性。
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公开(公告)号：US08242089B2
公开(公告)日：2012-08-14
申请号：US10560932
申请日：2004-06-17
CPC分类号： A61K31/132 , A61K9/1272 , A61K38/47 , A61K39/39 , A61K48/0041 , A61K2039/543 , A61K2039/55555 , A61K2039/55561 , C07C271/20 , C12N15/88 , A61K2300/00
摘要： The present invention concerns the use of a sphingoid-polyalkylamine conjugate comprising a sphingoid backbone carrying, via a carbamoyl bond, at least one polyalkylamine chains as a capturing agent of nucleic acid molecules. The present invention also provides the use of the sphingoid polyalkylamine conjugate for the preparation of a pharmaceutical composition for the delivery of a nucleic acid molecule into a target cell. In a further aspect the invention provides a method for transfecting a nucleic acid into a target cell, the method comprises contacting said target cell with the sphingoid-polyalkylamine conjugate associated with a nucleic acid molecule, thereby transfecting said target cell with said nucleic acid molecule. Other aspects of the invention concern pharmaceutical compositions comprising said conjugate, therapeutic methods as well as kits, making use of the said conjugate. A preferred conjugate according to the invention is N-palmitoyl D-erythrosphingosyl-1-carbamoyl spermine.
摘要翻译： 本发明涉及包含通过氨基甲酰键携带至少一个聚烷基胺链作为核酸分子的捕获剂的鞘氨醇主链的鞘氨醇 - 多烷基胺缀合物的用途。 本发明还提供了鞘氨醇多烷基胺缀合物用于制备用于将核酸分子递送至靶细胞的药物组合物的用途。 在另一方面，本发明提供了将核酸转染到靶细胞中的方法，所述方法包括使所述靶细胞与与核酸分子相关联的类鞘氨醇 - 多烷基胺缀合物接触，由此用所述核酸分子转染所述靶细胞。 本发明的其它方面涉及包含所述缀合物的药物组合物，治疗方法以及使用所述缀合物的试剂盒。 根据本发明的优选的缀合物是N-棕榈酰基D-赤藻酰基-1-氨基甲酰基精胺。
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公开(公告)号：US20110097387A1
公开(公告)日：2011-04-28
申请号：US12746656
申请日：2008-12-07
CPC分类号： A61K9/0019 , A61K9/1271 , A61K31/337 , A61K31/475 , A61K31/555 , A61K31/704
摘要： The present invention provides methods for desensitization for prevention or diminishing hypersensitivity reactions including C activation-related pseudoallergy (CARPA) and other reactions to particulate medicines. The desensitization is performed via pretreatment using a drug-free vehicle or carrier to eliminate or diminish the clinical symptoms of hypersensitivity.
摘要翻译： 本发明提供了用于预防或减少包括C活化相关假性反应（CARPA）和其他对颗粒药物的反应的超敏反应的脱敏的方法。 通过使用无药物载体或载体的预处理来进行脱敏以消除或减少超敏反应的临床症状。
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公开(公告)号：US20090155345A1
公开(公告)日：2009-06-18
申请号：US12096652
申请日：2006-12-07
申请人： Yechezkel Barenholz , Avi Schroeder , Joseph Kost
发明人： Yechezkel Barenholz , Avi Schroeder , Joseph Kost
CPC分类号： A61K41/0028 , A61K9/127 , A61K9/1271 , A61K9/1277
摘要： The present invention provides methods for loading of agents and substances into per-formed liposomes, preferably a suspension of pre-formed liposomes as well as to methods for the controlled quantum (step-wise) release of agents and substances from liposomes. One of the principle features of the methods of the invention is to expose the liposomes to ultrasound irradiation having predefined parameters, resulting in an increase in permeability of the liposomes, thereby permitting, respectively, the loading and/or release of agents and substances into and/or from the liposomes.
摘要翻译： 本发明提供了将试剂和物质装载到成形的脂质体中，优选预先形成的脂质体的悬浮液以及从脂质体中受控量子（逐步）释放试剂和物质的方法。 本发明方法的主要特征之一是将脂质体暴露于具有预定参数的超声辐照，导致脂质体的渗透性增加，从而分别允许试剂和物质的加载和/或释放进入和 /或从脂质体。
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公开(公告)号：US20080112917A1
公开(公告)日：2008-05-15
申请号：US10561394
申请日：2004-06-17
IPC分类号： A61K31/787 , C07F9/02 , A61K31/685
CPC分类号： A61K31/132 , A61K9/1272 , A61K38/47 , A61K39/39 , A61K48/0041 , A61K2039/543 , A61K2039/55555 , A61K2039/55561 , C07C271/20 , C12N15/88 , A61K2300/00
摘要： The present invention concerns novel sphingolipid-polyalkylamines conjugates, a process for their preparation and pharmaceutical compositions comprising the same.In particular, the present invention concerns ceramide based polyalkylamine conjugates and its use as a capturing agent. A preferred ceramide polyalkylamine conjugate is a ceramide-spermine conjugate, more preferably, N-palmitoyl D-erythro sphingosyl-1-carbamoyl spermine.
摘要翻译： 本发明涉及新型鞘脂 - 多烷基胺缀合物，其制备方法和包含其的药物组合物。 特别地，本发明涉及神经酰胺基聚烷基胺共轭物及其作为捕获剂的用途。 优选的神经酰胺多烷基胺缀合物是神经酰胺精胺缀合物，更优选N-棕榈酰基D-赤藓糖鞘糖醇-1-氨基甲酰基精胺。
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48.发明申请Liposomal Formulations Comprising an Amphipathic Weak Base Like Tempamine for Treatment of Neurodegenerative Conditions 审中-公开包含两性弱碱的脂质体制剂，如Tempamine用于治疗神经退行性病症公开(公告)号：US20080063702A1
公开(公告)日：2008-03-13
申请号：US11662173
申请日：2005-09-11
CPC分类号： A61K31/45 , A61K9/1271 , Y02A50/411
摘要： The present invention provides the use of an amphipathic weak base having defined characteristics for the preparation of a pharmaceutical formulation for the treatment or prevention of neurodegenerative conditions. Preferably, the amphipathic weak base is encapsulated in a liposome. The invention also provides pharmaceutical formulations and methods of use thereof for the treatment or prevention of neurodegenerative conditions. A specific and preferred amphipathic weak base is tempamine (TMN). Further, preferably, tempamine is loaded in sterically stabilized liposomes (SSL-TMN).
摘要翻译： 本发明提供具有确定特征的两性弱碱的用途，用于制备用于治疗或预防神经变性病症的药物制剂。 优选地，两亲性弱碱被包封在脂质体中。 本发明还提供药物制剂及其用于治疗或预防神经变性病症的方法。 特异性和优选的两亲性弱碱是温胺（TMN）。 此外，优选地，将Temamine加载到空间稳定的脂质体（SSL-TMN）中。
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公开(公告)号：US20080058274A1
公开(公告)日：2008-03-06
申请号：US11667671
申请日：2005-11-15
CPC分类号： A61K9/1272 , A61K9/1273 , A61K9/1278 , A61K45/06
摘要： The present invention concerns a new medical treatment involving the combination of two active entities, as well as pharmaceutical compositions comprising the two active entities. Specifically, the invention provides a pharmaceutical composition comprising a stable lipid assembly comprising as a first active entity an apoptosis-affecting lipid which does not self-aggregate in a polar environment to form liposomes and a lipopolymer. The pharmaceutical composition further comprises, as the second active entity, a cytotoxic amphipathic weak base drug carried by the lipid assembly or by a different liposome. According to one embodiment, the apoptotic-affecting lipid is a pro-apoptotic lipid. A preferred pro-apoptotic lipid is ceramide, preferably C6-ceramide. The cytotoxic amphipathic weak base drug is preferably doxorubicin or a biologically active, anthracyline-based doxorubicin analog thereof.
摘要翻译： 本发明涉及涉及两种活性实体的组合的新药物治疗，以及包含两种活性物质的药物组合物。 具体地说，本发明提供一种药物组合物，其包含稳定的脂质组合物，其包含作为第一活性实体的细胞凋亡影响的脂质，其在极性环境中不自聚集以形成脂质体和脂质聚合物。 作为第二活性物质，药物组合物还包含由脂质组合或不同脂质体携带的细胞毒性两亲性弱碱性药物。 根据一个实施方案，凋亡影响脂质是促凋亡脂质。 优选的促凋亡脂质是神经酰胺，优选C6-神经酰胺。 细胞毒性两亲性弱碱药物优选为多柔比星或其生物活性的基于蒽环类的多柔比星类似物。
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公开(公告)号：US20080003276A1
公开(公告)日：2008-01-03
申请号：US11662174
申请日：2005-09-11
CPC分类号： A61K9/127 , A61K9/1271 , A61K31/573
摘要： The present invention provides the use of a glucocorticoid (GC) or of a GC derivative encapsulated in a liposome for the preparation of a pharmaceutical composition for the treatment of an inflammatory associated condition in a subject, provided that said condition is not associated with a neurodegenerative disease or disorder A specific use concerns a liposomal formulation comprising methylprednisolone sodium hemisuccinate (MPS) for the treatment of rheumatoid arthritis.
摘要翻译： 本发明提供糖皮质激素（GC）或包封在脂质体中的GC衍生物用于制备用于治疗受试者的炎症相关病症的药物组合物的用途，条件是所述病症与神经变性不相关 疾病或病症具体用途涉及包含用于治疗类风湿性关节炎的甲泼尼龙钠半琥珀酸钠（MPS）的脂质体制剂。
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