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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

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.

3. 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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