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1. 发明公开

EP0944399A2 COVALENT POLAR LIPID CONJUGATES FOR TARGETING 失效
标题翻译：靶向共价极性脂质KONJUKATE
公开(公告)号：EP0944399A2
公开(公告)日：1999-09-29
申请号：EP97913811.0
申请日：1997-10-27
申请人： OREGON HEALTH SCIENCES UNIVERSITY , Yatvin, Milton B. , Stowell, Michael H., B. , Meredith, Michael J.
发明人： YATVIN, Milton, B. , STOWELL, Michael, H., B. , MEREDITH, Michael, J.
IPC分类号： A61K47 , A61K31 , A61P25 , A61P43 , C07H19
CPC分类号： C07H19/06 , A61K31/00 , A61K47/543 , A61K47/544 , B82Y5/00 , C07H19/10
摘要： This invention herein describes a method of facilitating the entry of drugs into cells and tissues at physiologically protected sites at pharmicokinetically useful levels and also a method of targeting drugs to specific organelles within the cell. This polar lipid/drug conjugate targeting invention embodies an advance over other drug targeting methods known in the prior art, because the invention provides drug concentrations in such physiologically protected sites that can reach therapeutically-effective levels after administration of systemic levels much lower than are currently administered to achieve a therapeutic dose. This technology is appropriate for use with psychotropic, neurotropic and neurological drugs, agents and compounds, for rapid and efficient introduction of such agents across the blood-brain barrier. Further, the invention provides means for retention and prolonged enzymatic release of psychotropic, neurotropic and neurological drugs, agents and compounds comprising the conjugates of the invention, in the brain and central nervous system.

2. 发明申请

WO9817325A3 COVALENT POLAR LIPID CONJUGATES FOR TARGETING 审中-公开
标题翻译：用于靶向的共价极性磷脂缀合物
公开(公告)号：WO9817325A3
公开(公告)日：1998-06-04
申请号：PCT/US9719486
申请日：1997-10-27
申请人： UNIV OREGON HEALTH SCIENCES , YATVIN MILTON B , STOWELL MICHAEL H B , MEREDITH MICHAEL J
发明人： YATVIN MILTON B , STOWELL MICHAEL H B , MEREDITH MICHAEL J
IPC分类号： A61K47/48 , A61K31/00 , A61K31/196 , A61K31/198 , A61K31/513 , A61K31/519 , A61K31/55 , A61P25/00 , A61P43/00 , C07H19/06 , C07H19/10 , A61K97/48
CPC分类号： C07H19/06 , A61K31/00 , A61K47/543 , A61K47/544 , B82Y5/00 , C07H19/10
摘要： This invention herein describes a method of facilitating the entry of drugs into cells and tissues at physiologically protected sites at pharmicokinetically useful levels and also a method of targeting drugs to specific organelles within the cell. This polar lipid/drug conjugate targeting invention embodies an advance over other drug targeting methods known in the prior art, because the invention provides drug concentrations in such physiologically protected sites that can reach therapeutically-effective levels after administration of systemic levels much lower than are currently administered to achieve a therapeutic dose. This technology is appropriate for use with psychotropic, neurotropic and neurological drugs, agents and compounds, for rapid and efficient introduction of such agents across the blood-brain barrier. Further, the invention provides means for retention and prolonged enzymatic release of psychotropic, neurotropic and neurological drugs, agents and compounds comprising the conjugates of the invention, in the brain and central nervous system.
摘要翻译：本发明在此描述了一种促进药物进入细胞和组织的生理学保护位点的药物动力学有用水平的方法，以及将药物靶向细胞内特定细胞器的方法。该极性脂质/药物缀合物靶向发明体现了超过现有技术中已知的其他药物靶向方法的进步，因为本发明提供了药物浓度在这样的生理学保护位点，其可以在施用系统水平之后达到治疗有效水平，施用以达到治疗剂量。该技术适用于精神药物，神经营养药物和神经药物，药物和化合物，以便迅速有效地将这些药物引入整个血脑屏障。此外，本发明提供了用于在脑和中枢神经系统中保留和延长精神，神经和神经药物，包含本发明缀合物的药剂和化合物的酶促释放手段。

3. 发明申请

WO1998017325A2 COVALENT POLAR LIPID CONJUGATES FOR TARGETING 审中-公开
标题翻译：有价值的极乐团队
公开(公告)号：WO1998017325A2
公开(公告)日：1998-04-30
申请号：PCT/US1997019486
申请日：1997-10-27
申请人： OREGON HEALTH SCIENCES UNIVERSITY , YATVIN, Milton, B. , STOWELL, Michael, H., B. , MEREDITH, Michael, J.
发明人： OREGON HEALTH SCIENCES UNIVERSITY
IPC分类号： A61K97/48
CPC分类号： C07H19/06 , A61K31/00 , A61K47/543 , A61K47/544 , B82Y5/00 , C07H19/10
摘要： This invention herein describes a method of facilitating the entry of drugs into cells and tissues at physiologically protected sites at pharmicokinetically useful levels and also a method of targeting drugs to specific organelles within the cell. This polar lipid/drug conjugate targeting invention embodies an advance over other drug targeting methods known in the prior art, because the invention provides drug concentrations in such physiologically protected sites that can reach therapeutically-effective levels after administration of systemic levels much lower than are currently administered to achieve a therapeutic dose. This technology is appropriate for use with psychotropic, neurotropic and neurological drugs, agents and compounds, for rapid and efficient introduction of such agents across the blood-brain barrier. Further, the invention provides means for retention and prolonged enzymatic release of psychotropic, neurotropic and neurological drugs, agents and compounds comprising the conjugates of the invention, in the brain and central nervous system.
摘要翻译：本发明在此描述了一种促进药物进入生理学保护部位的细胞和组织的药学上有用水平的方法，以及将药物靶向细胞内的特定细胞器的方法。这种极性脂质/药物共轭靶向发明体现了先前技术中已知的其它药物靶向方法的进步，因为本发明提供了在这样的生理保护部位中的药物浓度，其在施用远低于目前的系统水平后达到治疗有效水平施用以达到治疗剂量。该技术适用于精神药物，神经营养因子和神经药物，药剂和化合物，用于快速有效地将这些药物引入血脑屏障。此外，本发明提供了在脑和中枢神经系统中保留和延长酶促释放精神药物，神经营养因子和神经药物，包含本发明缀合物的药剂和化合物的方法。

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