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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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公开(公告)号：US07771711B2
公开(公告)日：2010-08-10
申请号：US10561394
申请日：2004-06-17
IPC分类号： A61K31/74
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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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：US20060252718A1
公开(公告)日：2006-11-09
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：US10085940B2
公开(公告)日：2018-10-02
申请号：US14232332
申请日：2012-07-12
申请人： Alberto A. Gabizon , Yechezkel Barenholz , Hilary Shmeeda , John Maher , Ana Catarina Parente Pereira
发明人： Alberto A. Gabizon , Yechezkel Barenholz , Hilary Shmeeda , John Maher , Ana Catarina Parente Pereira
IPC分类号： A61K31/704 , A61K9/127 , A61K31/663 , A61K38/20 , A61K45/06 , A61K35/15 , A61K35/17 , A61K47/55 , A61K47/69 , A61K39/00
摘要： The present disclosure provides liposomes comprising a membrane and an intraliposomal aqueous water phase, the membrane comprising at least one liposome forming lipid and the intraliposomal aqueous water phase comprises a salt of a bisphosphonate together with an amphipathic weak base agent (PLAD). An example of a liposome is one comprising co encapsulated in the intraliposomal aqueous water phase N-containing bisphosphonate, such as alendronate, and an anthracycline such as doxorubicin which was shown to increase survival as compared to Doxil or to administrations of liposomal alendronate (PLA) and Doxil (separate liposomes). Such liposomes may carry a targeting moiety exposed at the liposome's outer surface, for example, conjugate of folic acid as a targeting moiety to folate receptor (FT-PLAD). Also provided by the present disclosure is a method of preparing the liposomes and methods of use of the liposomes, at times, in combination with additional active ingredients, such as γδ T-cells.
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公开(公告)号：US07985417B2
公开(公告)日：2011-07-26
申请号：US11246340
申请日：2005-10-07
IPC分类号： A61K9/127
CPC分类号： A61K9/1271 , A61K9/1277 , A61K47/6907 , A61K47/6913 , C07K16/32 , C07K2317/622
摘要： A method of inserting a lipid-linked moiety into a lipid assembly, such as a planar lipid monolayer or bilayer, a spherical lipid vesicle, a micelle, or an emulsion envelope monolayer is described. In the method, the lipid assembly and the lipid-linked moiety are contacted in the presence of microwave irradiation to permit the lipid-linked moiety to become associated with the lipid assembly. In one embodiment, the lipid assembly is a liposome and the lipid-linked moiety is a lipid-polymer. Compositions comprised of a lipid layer and of a lipid-linked moiety, prepared in accord with the method, are also described.
摘要翻译： 描述了将脂质连接的部分插入脂质组合物，例如平面脂质单层或双层，球形脂质囊泡，胶束或乳剂包膜单层中的方法。 在该方法中，脂质组装和脂质连接部分在微波照射的存在下接触以允许脂质连接部分与脂质组装相关联。 在一个实施方案中，脂质组合物是脂质体，脂质连接部分是脂质聚合物。 还描述了根据该方法制备的由脂质层和脂质连接部分组成的组合物。
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公开(公告)号：US20070087047A1
公开(公告)日：2007-04-19
申请号：US11633129
申请日：2006-12-01
CPC分类号： A61K9/0019 , A61K9/1271 , A61K31/00 , A61K38/12 , A61K38/1774 , A61K47/61 , A61K47/62 , A61K47/6911 , Y10S424/812 , A61K2300/00
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.
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公开(公告)号：US20070082043A1
公开(公告)日：2007-04-12
申请号：US11492695
申请日：2006-07-25
CPC分类号： A61K9/127 , A61K38/09 , A61K38/2207 , A61K38/24 , A61K38/27 , A61K39/0005 , A61K2039/55555 , A61K2039/6031
摘要： The invention provides liposomal vehicles for encapsulating relatively high levels of water-soluble substances including immunogens directed against gastrin and gonadotropin releasing hormone. The liposome encapsulating large amounts of immunogens can be injected parentally to induce effective immune responses without exhibiting significant adverse tissue reactogenicity.
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公开(公告)号：US20050169979A1
公开(公告)日：2005-08-04
申请号：US11036690
申请日：2005-01-14
CPC分类号： A61K9/127 , A61K38/09 , A61K38/2207 , A61K38/27
摘要： The invention provides liposomal vehicles for encapsulating relatively high levels of immunogenic protein substances including immunogens directed against hormones and hormone receptors, such as gastrin and gonadotropin releasing hormone and their receptors. The liposome encapsulating large amounts of immunogens can be injected parenterally to induce effective immune responses without exhibiting significant adverse tissue reactogenicity. Methods for production of the liposomal vaccines and methods of their administration for treatment of diseases and conditions associated with the cognate hormones are also provided.
摘要翻译： 本发明提供用于包封相对高水平的免疫原性蛋白质物质的脂质体载体，包括针对激素和激素受体的免疫原，例如胃泌素和促性腺激素释放激素及其受体。 包封大量免疫原的脂质体可以肠胃外注射以诱导有效的免疫应答，而不显示显着的不利组织反应原性。 还提供了用于生产脂质体疫苗的方法及其用于治疗与同类激素相关的疾病和病症的施用方法。
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公开(公告)号：US20050090478A1
公开(公告)日：2005-04-28
申请号：US10487154
申请日：2002-08-21
IPC分类号： C07D295/02 , A61K9/127 , A61K31/555 , A61P35/00 , A61P43/00 , C07D211/46 , C07D211/58 , C07F15/00
CPC分类号： C07F15/0093
摘要： The present invention concerns novel platinum complexes in which at least one of the amine ligand is a non-planar heterocyclic aliphatic amine. The platinum complexes may be in a trans or cis configuration and were found to posses therapeutic activites. Thus, the present concerns novel platinum complexes, pharmaceutical compositions comprising them and other uses thereof.
摘要翻译： 本发明涉及其中至少一种胺配体是非平面杂环脂族胺的新型铂络合物。 铂络合物可以是反式或顺式构型，并被发现具有治疗活性。 因此，本发明涉及新颖的铂络合物，包含它们的药物组合物和其它用途。
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