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1.发明授权
公开(公告)号：US5264618A
公开(公告)日：1993-11-23
申请号：US686746
申请日：1991-04-16
IPC分类号： A61K9/127 , A61K31/70 , A61K47/18 , A61K47/48 , A61K48/00 , A61P31/12 , C07C211/62 , C07D295/00 , C07D451/00 , C12N15/88 , C07C69/52
CPC分类号： A61K47/48315 , A61K47/186 , A61K47/48023 , A61K47/48053 , A61K9/0014 , A61K9/0019 , A61K9/1272 , C12N15/88
摘要： Disclosed are cationic lipids capable of facilitating transport of biologically active agents into cells, including the transfection of cells by therapeutic polynucleotides, the delivery of antiviral drugs, and the introduction of immunogenic peptides. The cationic lipids, comprising an ammonium group, have the general structure ##STR1## Also disclosed are adducts of these compounds comprising additional cationic sites that enhance the transfective or transport activity. Structure-activity correlations provide for the selection of preferred compounds to be synthesized for this purpose. Compositions disclosed for use of these cationic lipid include formulations for in vitro transfection and pharmaceutical formulations for parenteral and topical administration of therapeutic agents.
摘要翻译： 公开了能够促进生物活性剂转运到细胞中的阳离子脂质，包括通过治疗性多核苷酸转染细胞，递送抗病毒药物和引入免疫原性肽。 包含铵基的阳离子脂质具有一般结构（I）。还公开了这些化合物的加合物，其包含增强转染或转运活性的另外的阳离子位点。 结构活性相关性提供了为此目的合成的优选化合物的选择。 公开的用于这些阳离子脂质的组合物包括用于体外转染的制剂和用于胃肠外和局部施用治疗剂的药物制剂。
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公开(公告)号：US5151265A
公开(公告)日：1992-09-29
申请号：US514392
申请日：1990-04-25
CPC分类号： A61K47/12 , A61K38/217 , A61K47/26 , A61K9/0019
摘要： A liquid pharmaceutical composition comprising an effective amount of non-lyophilized gamma-interferon. The liquid pharmaceutical composition which additionally includes a buffer capable of maintaining the pH of the liquid composition within the range of 4.0 to 6.0, a stabilizing agent and a non-ionic detergent.
摘要翻译： 一种液体药物组合物，其包含有效量的非冻干γ-干扰素。 液体药物组合物另外包括能够将液体组合物的pH值保持在4.0-6.0范围内的缓冲剂，稳定剂和非离子型洗涤剂。
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3.发明授权
公开(公告)号：US5459127A
公开(公告)日：1995-10-17
申请号：US123757
申请日：1993-09-16
IPC分类号： A61K9/127 , A61K31/70 , A61K47/18 , A61K47/48 , A61K48/00 , A61P31/12 , C07C211/62 , C07D295/00 , C07D451/00 , C12N15/88 , A01N37/18 , A61K38/17
CPC分类号： A61K47/48315 , A61K47/186 , A61K47/48023 , A61K47/48053 , A61K9/0014 , A61K9/0019 , A61K9/1272 , C12N15/88
摘要： Disclosed are cationic lipids capable of facilitating transport of biologically active agents into cells, including the transfection of cells by therapeutic polynucleotides, the delivery of antiviral drugs, and the introduction of immunogenic peptides. The cationic lipids, comprising an ammonium group, have the general structure ##STR1## Also disclosed are adducts of these compounds comprising additional cationic sites that enhance the transfective or transport activity. Structure-activity correlations provide for the selection of preferred compounds to be synthesized for this purpose. Compositions disclosed for use of these cationic lipid include formulations for in vitro transfection and pharmaceutical formulations for parenteral and topical administration of therapeutic agents.
摘要翻译： 公开了能够促进生物活性剂转运到细胞中的阳离子脂质，包括通过治疗性多核苷酸转染细胞，递送抗病毒药物和引入免疫原性肽。 包含铵基的阳离子脂质具有一般结构（I）。还公开了这些化合物的加合物，其包含增强转染或转运活性的另外的阳离子位点。 结构活性相关性提供了为此目的合成的优选化合物的选择。 公开的用于这些阳离子脂质的组合物包括用于体外转染的制剂和用于胃肠外和局部施用治疗剂的药物制剂。
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