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1. 发明授权

US06339060B1 Conjugate of biologically active compound and polar lipid conjugated to a microparticle for biological targeting 失效
标题翻译：生物活性化合物和与微粒结合的极性脂质的缀合物用于生物靶向
公开(公告)号：US06339060B1
公开(公告)日：2002-01-15
申请号：US09573497
申请日：2000-05-16
申请人： Milton B. Yatvin , Michael H B Stowell , Vincent S. Gallicchio , Michael J. Meredith
发明人： Milton B. Yatvin , Michael H B Stowell , Vincent S. Gallicchio , Michael J. Meredith
IPC分类号： A01N3718
CPC分类号： A61K9/167 , A61K47/543 , A61K47/544 , A61K47/645 , A61K47/6929 , B82Y5/00 , C07H19/06 , C07H19/10 , Y10S530/811 , Y10S530/813 , Y10S530/814 , Y10S530/815
摘要： Methods and reagents are provided for specifically targeting biologically active compounds such as antiviral and antimicrobial drugs, or prodrugs containing the biologically active compound to specific sites such as specific organelles in phagocytic mammalian cells. The biologically active compound or prodrug is linked to a microparticle with a linker that is non-specifically or specifically cleaved inside a phagocytic mammalian cell. Alternatively, the biologically active compound or prodrug is impregnated into a porous microparticle or coated on a nonporous microparticle, and then coated with a coating material that is non-specifically or specifically degraded inside a phagocytic mammalian cell. The prodrug contains the biologically active compound linked to a polar lipid such as ceramide with a specific linker such as a peptide that is specifically cleaved to activate the prodrug in a phagocytic mammalian cell infected with a microorganism. A microparticle linked antimicrobial drug or prodrug may be used for killing a microorganism infecting a phagocytic mammalian cell in vivo or in vitro.
摘要翻译：提供方法和试剂用于将生物活性化合物如抗病毒和抗微生物药物或含有生物活性化合物的前药特异性靶向特定位点，例如吞噬哺乳动物细胞中的特定细胞器。生物活性化合物或前药与具有在吞噬的哺乳动物细胞内非特异性或特异性切割的接头的微粒连接。或者，生物活性化合物或前药被浸渍到多孔微粒中或涂覆在无孔微粒上，然后用在吞噬的哺乳动物细胞内非特异性或特异性降解的包被材料包被。前药包含与极性脂质例如神经酰胺连接的生物活性化合物，其具有特异性接头，例如特异性切割以在感染微生物的吞噬细胞哺乳动物细胞中活化前药的肽。微粒连接的抗微生物药物或前体药物可用于在体内或体外杀死感染吞噬哺乳动物细胞的微生物。

2. 发明授权

US5840674A Covalent microparticle-drug conjugates for biological targeting 失效
公开(公告)号：US5840674A
公开(公告)日：1998-11-24
申请号：US691891
申请日：1996-08-01
申请人： Milton B. Yatvin , Michael H. B. Stowell , Vincent S. Gallicchio , Michael J. Meredith
发明人： Milton B. Yatvin , Michael H. B. Stowell , Vincent S. Gallicchio , Michael J. Meredith
IPC分类号： A61K9/16 , A61K47/48 , C07H19/06 , C07H19/10 , C12N5/08 , A01N37/18 , A01N57/26
CPC分类号： A61K9/167 , A61K47/48046 , A61K47/48053 , A61K47/48315 , A61K47/48884 , B82Y5/00 , C07H19/06 , C07H19/10 , Y10S530/811 , Y10S530/813 , Y10S530/814 , Y10S530/815
摘要： This invention provides novel methods and reagents for specifically delivering biologically active compounds to phagocytic mammalian cells. The invention also relates to specific uptake of such biologically active compounds by phagocytic cells and delivery of such compounds to specific sites intracellularly. The invention specifically relates to methods of facilitating the entry of antiviral and antimicrobial drugs and other agents into phagocytic cells and for targeting such compounds to specific organelles within the cell. The invention specifically provides compositions of matter and pharmaceutical embodiments of such compositions comprising conjugates of such antimicrobial drugs and agents covalently linked to particulate carriers generally termed microparticles. In particular embodiments, the antimicrobial drug is covalently linked to a microparticle via an organic linker molecule which is the target of a microorganism-specific protein having enzymatic activity. Thus, the invention provides cell targeting of drugs wherein the targeted drug is only released in cells infected with a particular microorganism. Alternative embodiments of such specific drug delivery compositions also contain polar lipid carrier molecules effective in achieving intracellular organelle targeting in infected phagocytic mammalian cells. Particular embodiments of such conjugates comprise antimicrobial drugs or agents covalently linked both to a microparticle via an organic linker molecule and to a polar lipid compound, to facilitate targeting of such drugs or agents to particular subcellular organelles within the cell. Also provided are porous microparticles impregnated with antiviral and antimicrobial drugs and agents wherein the surface or outside extent of the microparticle is covered with a degradable coating that is specifically degraded within an infected phagocytic mammalian cell. Also provided are nonporous microparticles coated with an antiviral or antimicrobial drug and further coated wherein the surface or outside extent of the microparticle is covered with a degradable coating that is specifically degraded within an infected phagocytic mammalian cell. Methods of inhibiting, attenuating, arresting, combating and overcoming microbial infection of phagocytic mammalian cells in vivo and in vitro are also provided.

3. 发明授权

US5543391A Covalent microparticle-drug conjugates for biological targeting 失效
公开(公告)号：US5543391A
公开(公告)日：1996-08-06
申请号：US441770
申请日：1995-05-16
申请人： Milton B. Yatvin , Michael H. B. Stowell , Vincent S. Gallicchio , Michael J. Meredith
发明人： Milton B. Yatvin , Michael H. B. Stowell , Vincent S. Gallicchio , Michael J. Meredith
IPC分类号： A61K9/16 , A61K47/48 , C07H19/06 , C07H19/10 , C12N5/08 , A01N37/18 , A01N57/26
CPC分类号： A61K9/167 , A61K47/48046 , A61K47/48053 , A61K47/48315 , A61K47/48884 , B82Y5/00 , C07H19/06 , C07H19/10 , Y10S530/811 , Y10S530/813 , Y10S530/814 , Y10S530/815
摘要： This invention provides novel methods and reagents for specifically delivering biologically active compounds to phagocytic mammalian cells. The invention also relates to specific uptake of such biologically active compounds by phagocytic cells and delivery of such compounds to specific sites intracellularly. The invention specifically relates to methods of facilitating the entry of antimicrobial drugs and other agents into phagocytic cells and for targeting such compounds to specific organelles within the cell. The invention specifically provides compositions of matter and pharmaceutical embodiments of such compositions comprising conjugates of such antimicrobial drugs and agents covalently linked to particulate carriers generally termed microparticles. In particular embodiments, the antimicrobial drug is covalently linked to a microparticle via an organic linker molecule which is the target of a microorganism-specific protein having enzymatic activity. Thus, the invention provides cell targeting of drugs wherein the targeted drug is only released in cells infected with a particular microorganism. Alternative embodiments of such specific drug delivery compositions also contain polar lipid carrier molecules effective in achieving intracellular organelle targeting in infected phagocytic mammalian cells. Particular embodiments of such conjugates comprise antimicrobial drugs covalently linked both to a microparticle via an organic linker molecule and to a polar lipid compound, to facilitate targeting of such drugs to particular subcellular organelles within the cell. Also provided are porous microparticles impregnated with antimicrobial drugs and agents wherein the surface or outside extent of the microparticle is covered with a degradable coating that is specifically degraded within an infected phagocytic mammalian cell. Methods of inhibiting, attenuating, arresting, combatting and overcoming microbial infection of phagocytic mammalian cells in vivo and in vitro are also provided.

4. 发明授权

US5543390A Covalent microparticle-drug conjugates for biological targeting 失效
公开(公告)号：US5543390A
公开(公告)日：1996-08-06
申请号：US246941
申请日：1994-05-19
申请人： Milton B. Yatvin , Michael H. B. Stowell , Vincent S. Gallicchio , Michael J. Meredith
发明人： Milton B. Yatvin , Michael H. B. Stowell , Vincent S. Gallicchio , Michael J. Meredith
IPC分类号： A61K9/16 , A61K47/48 , C07H19/06 , C07H19/10 , C12N5/08 , A01N37/18
CPC分类号： A61K9/167 , A61K47/48046 , A61K47/48053 , A61K47/48315 , A61K47/48884 , B82Y5/00 , C07H19/06 , C07H19/10 , Y10S530/811 , Y10S530/813 , Y10S530/814 , Y10S530/815
摘要： This invention provides novel methods and reagents for specifically delivering biologically active compounds to phagocytic mammalian cells. The invention also relates to specific uptake of such biologically active compounds by phagocytic cells and delivery of such compounds to specific sites intracellularly. The invention specifically relates to methods of facilitating the entry of antimicrobial drugs and other agents into phagocytic cells and for targeting such compounds to specific organelles within the cell. The invention specifically provides compositions of matter and pharmaceutical embodiments of such compositions comprising conjugates of such antimicrobial drugs and agents covalently linked to particulate carriers generally termed microparticles. In particular embodiments, the antimicrobial drug is covalently linked to a microparticle via an organic linker molecule which is the target of a microorganism-specific protein having enzymatic activity. Thus, the invention provides cell targeting of drugs wherein the targeted drug is only released in cells infected with a particular microorganism. Alternative embodiments of such specific drug delivery compositions also contain polar lipid carrier molecules effective in achieving intracellular organelle targeting in infected phagocytic mammalian cells. Particular embodiments of such conjugates comprise antimicrobial drugs covalently linked both to a microparticle via an organic linker molecule and to a polar lipid compound, to facilitate targeting of such drugs to particular subcellular organelles within the cell. Also provided are porous microparticles impregnated with antimicrobial drugs and agents wherein the surface or outside extent of the microparticle is covered with a degradable coating that is specifically degraded within an infected phagocytic mammalian cell. Methods of inhibiting, attenuating, arresting, combatting and overcoming microbial infection of phagocytic mammalian cells in vivo and in vitro are also provided.

5. 发明授权

US6063759A Conjugate of biologically active compound and polar lipid conjugated to a microparticle for biological targeting 失效
公开(公告)号：US6063759A
公开(公告)日：2000-05-16
申请号：US60011
申请日：1998-04-14
申请人： Milton B. Yatvin , Michael H B Stowell , Vincent S. Gallicchio , Michael J. Meredith
发明人： Milton B. Yatvin , Michael H B Stowell , Vincent S. Gallicchio , Michael J. Meredith
IPC分类号： A61K9/16 , A61K47/48 , C07H19/06 , C07H19/10 , C12N5/08 , A01N37/18 , A61K9/127 , A61K47/00 , C07K17/00
CPC分类号： A61K9/167 , A61K47/48046 , A61K47/48053 , A61K47/48315 , A61K47/48884 , B82Y5/00 , C07H19/06 , C07H19/10 , Y10S530/811 , Y10S530/813 , Y10S530/814 , Y10S530/815
摘要： Methods and reagents are provided for specifically targeting biologically active compounds such as antiviral and antimicrobial drugs, or prodrugs containing the biologically active compound to specific sites such as specific organelles in phagocytic mammalian cells. The biologically active compound or prodrug is linked to a microparticle with a linker that is non-specifically or specifically cleaved inside a phagocytic mammalian cell. Alternatively, the biologically active compound or prodrug is impregnated into a porous microparticle or coated on a nonporous microparticle, and then coated with a coating material that is non-specifically or specifically degraded inside a phagocytic mammalian cell. The prodrug contains the biologically active compound linked to a polar lipid such as ceramide with a specific linker such as a peptide that is specifically cleaved to activate the prodrug in a phagocytic mammalian cell infected with a microorganism. A microparticle linked antimicrobial drug or prodrug may be used for killing a microorganism infecting a phagocytic mammalian cell in vivo or in vitro.

6. 发明授权

US06858582B2 Composition containing porous microparticle impregnated with biologically-active compound for treatment of infection 失效
标题翻译：含有浸渍有用于治疗感染的生物活性化合物的多孔微粒的组合物
公开(公告)号：US06858582B2
公开(公告)日：2005-02-22
申请号：US10050271
申请日：2002-01-15
申请人： Milton B. Yatvin , Michael HB Stowell , Vincent S. Gallicchio , Michael J. Meredith
发明人： Milton B. Yatvin , Michael HB Stowell , Vincent S. Gallicchio , Michael J. Meredith
IPC分类号： A61K9/16 , A61K47/48 , C07H19/06 , C07H19/10 , C12N5/08 , A01N37/18 , A61K9/127 , A61K47/00 , C07K17/00
CPC分类号： A61K9/167 , A61K47/543 , A61K47/544 , A61K47/645 , A61K47/6929 , B82Y5/00 , C07H19/06 , C07H19/10 , Y10S530/811 , Y10S530/813 , Y10S530/814 , Y10S530/815
摘要： Methods and reagents are provided for specifically targeting biologically active compounds such as antiviral and antimicrobial drugs, or prodrugs containing the biologically active compound to specific sites such as specific organelles in phagocytic mammalian cells. The biologically active compound or prodrug is linked to a microparticle with a linker that is non-specifically or specifically cleaved inside a phagocytic mammalian cell. Alternatively, the biologically active compound or prodrug is impregnated into a porous microparticle or coated on a nonporous microparticle, and then coated with a coating material that is non-specifically or specifically degraded inside a phagocytic mammalian cell. The prodrug contains the biologically active compound linked to a polar lipid such as ceramide with a specific linker such as a peptide that is specifically cleaved to activate the prodrug in a phagocytic mammalian cell infected with a microorganism. A microparticle linked antimicrobial drug or prodrug may be used for killing a microorganism infecting a phagocytic mammalian cell in vivo or in vitro.
摘要翻译：提供方法和试剂用于将生物活性化合物如抗病毒和抗微生物药物或含有生物活性化合物的前药特异性靶向特定位点，例如吞噬哺乳动物细胞中的特定细胞器。生物活性化合物或前药与具有在吞噬的哺乳动物细胞内非特异性或特异性切割的接头的微粒连接。或者，生物活性化合物或前药被浸渍到多孔微粒中或涂覆在无孔微粒上，然后用在吞噬的哺乳动物细胞内非特异性或特异性降解的包被材料包被。前药包含与极性脂质例如神经酰胺连接的生物活性化合物，其具有特异性接头，例如特异性切割以在感染微生物的吞噬细胞哺乳动物细胞中活化前药的肽。微粒连接的抗微生物药物或前体药物可用于在体内或体外杀死感染吞噬哺乳动物细胞的微生物。

7. 发明授权

US6024977A Covalent polar lipid conjugates with neurologically active compounds for targeting 失效
公开(公告)号：US6024977A
公开(公告)日：2000-02-15
申请号：US923015
申请日：1997-09-03
申请人： Milton B. Yatvin , Michael H. B. Stowell , Michael J. Meredith
发明人： Milton B. Yatvin , Michael H. B. Stowell , Michael J. Meredith
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 , A61K9/127 , A61K31/135 , A61K31/54 , A61K38/00
CPC分类号： C07H19/06 , A61K31/00 , A61K47/48046 , A61K47/48053 , 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.

8. 发明授权

US5827819A Covalent polar lipid conjugates with neurologically active compounds for targeting 失效
公开(公告)号：US5827819A
公开(公告)日：1998-10-27
申请号：US735977
申请日：1996-10-25
申请人： Milton B. Yatvin , Michael H. B. Stowell , Michael J. Meredith
发明人： Milton B. Yatvin , Michael H. B. Stowell , Michael J. Meredith
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 , A61K38/00 , A61K9/127 , A61K31/135
CPC分类号： C07H19/06 , A61K31/00 , A61K47/48046 , A61K47/48053 , 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.

9. 发明授权

US06436437B1 Covalent polar lipid conjugates with neurologically active compounds for targeting 失效
标题翻译：共价极性脂质偶联物与神经活性化合物靶向
公开(公告)号：US06436437B1
公开(公告)日：2002-08-20
申请号：US09503892
申请日：2000-02-15
申请人： Milton B. Yatvin , Michael H. B. Stowell , Michael J. Meredith
发明人： Milton B. Yatvin , Michael H. B. Stowell , Michael J. Meredith
IPC分类号： A61K9127
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可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。

10. 发明授权

US5543389A Covalent polar lipid-peptide conjugates for use in salves 失效
标题翻译：用于药膏的共价极性脂质 - 肽缀合物
公开(公告)号：US5543389A
公开(公告)日：1996-08-06
申请号：US142771
申请日：1993-10-26
申请人： Milton B. Yatvin , Michael H B Stowell
发明人： Milton B. Yatvin , Michael H B Stowell
IPC分类号： A61K9/16 , A61K31/00 , A61K47/48 , C07H19/06 , C07H19/10 , A61K31/685
CPC分类号： B82Y5/00 , A61K31/00 , A61K47/48046 , A61K47/48053 , A61K47/48315 , A61K47/48784 , A61K9/167 , C07H19/06 , C07H19/10 , Y10S514/863
摘要： This invention herein describes a method of facilitating the entry of drugs into cells at pharmokinetically useful levels and also a method of targeting drugs to specific organelles within the cell. This lipid/drug conjugate targeting invention embodies an advance over other drug targeting methods because through this method, intracellular drug concentrations may reach levels which are orders of magnitude higher than those achieved otherwise. Furthermore, it refines the drug delivery process by allowing therapeutic agents to be directed to certain intracellular structures. This technology is appropriate for use with antiproliferative drugs, in particular in combination with a multiplicity of other emolients and agents to make up topically-active substances such as salves, for rapid and efficient introduction of antiproliferative agents through the epidermis for treatment of skin diseases such as psoriasis.
摘要翻译：本发明在此描述了一种促进药物进入细胞的药学上有用水平的方法，还有一种将药物靶向细胞内的特定细胞器的方法。这种脂质/药物共轭靶向发明体现了超越其他药物靶向方法的进步，因为通过该方法，细胞内药物浓度可达到比其它药物浓度高数量级的水平。此外，它通过允许治疗剂被引导到某些细胞内结构来改善药物递送过程。该技术适用于抗增生药物，特别是与多种其他强力组合剂和药剂组合以形成局部活性物质如药膏，用于通过表皮快速有效地引入抗增生剂以治疗皮肤疾病，例如作为牛皮癣。

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