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1. 发明授权

US08796431B2 Efficient production of peptides 有权
标题翻译：有效生产肽
公开(公告)号：US08796431B2
公开(公告)日：2014-08-05
申请号：US12942450
申请日：2010-11-09
申请人： Michael H. B. Stowell , Jonathan Caruthers , Travis Nemkov , Brian Hiester , Leslie Boux , Mikhail Plam
发明人： Michael H. B. Stowell , Jonathan Caruthers , Travis Nemkov , Brian Hiester , Leslie Boux , Mikhail Plam
IPC分类号： C07K17/02 , C12P21/04 , C12P21/06 , C12N9/90 , C07K14/62 , C07K14/65 , C07K14/61 , C07K14/655 , C07K14/585 , C07K14/47 , C07K14/005 , C07K14/635 , C07K14/56 , C12N15/70 , C07K14/535 , C07K14/505 , C07K14/755 , G06Q99/00 , C07K14/605
CPC分类号： C12P21/06 , C07K1/04 , C07K1/12 , C07K14/005 , C07K14/4703 , C07K14/4711 , C07K14/505 , C07K14/535 , C07K14/56 , C07K14/585 , C07K14/605 , C07K14/61 , C07K14/62 , C07K14/635 , C07K14/65 , C07K14/655 , C07K14/755 , C07K2319/01 , C07K2319/20 , C07K2319/21 , C12N9/90 , C12N15/70 , C12N2740/16122 , C12Y503/03001 , G06Q99/00
摘要： The present invention relates to processes for the production of peptides, and the peptides produced accordingly. Peptides produced according to the invention may be produced more efficiently than peptides produced according to prior art processes. The production process of the invention may lead to advantages in yield, purity, and/or price. Methods of marketing peptides are also disclosed.
摘要翻译：本发明涉及生产肽的方法，并且相应地生产肽。根据本发明产生的肽可以比根据现有技术方法生产的肽更有效地生产。本发明的生产方法可以产生产量，纯度和/或价格的优点。还公开了销售肽的方法。

2. 发明申请

US20110112990A1 Efficient Production of Peptides 有权
标题翻译：肽的有效生产
公开(公告)号：US20110112990A1
公开(公告)日：2011-05-12
申请号：US12942450
申请日：2010-11-09
申请人： Michael H. B. Stowell , Jonathan Caruthers , Travis Nemkov , Brian Hiester , Leslie Boux , Mikhail Plam
发明人： Michael H. B. Stowell , Jonathan Caruthers , Travis Nemkov , Brian Hiester , Leslie Boux , Mikhail Plam
IPC分类号： C12P21/00 , C12N9/24 , C12N9/64 , C12N9/90 , C07K2/00 , C07K14/62 , C07K14/585 , C07K14/505 , C07K14/61 , C07K14/555 , C07K14/535 , C12N15/63 , C12N1/21 , C07K19/00 , C07K14/47 , G06Q90/00
CPC分类号： C12P21/06 , C07K1/04 , C07K1/12 , C07K14/005 , C07K14/4703 , C07K14/4711 , C07K14/505 , C07K14/535 , C07K14/56 , C07K14/585 , C07K14/605 , C07K14/61 , C07K14/62 , C07K14/635 , C07K14/65 , C07K14/655 , C07K14/755 , C07K2319/01 , C07K2319/20 , C07K2319/21 , C12N9/90 , C12N15/70 , C12N2740/16122 , C12Y503/03001 , G06Q99/00
摘要： The present invention relates to processes for the production of peptides, and the peptides produced accordingly. Peptides produced according to the invention may be produced more efficiently than peptides produced according to prior art processes. The production process of the invention may lead to advantages in yield, purity, and/or price. Methods of marketing peptides are also disclosed.
摘要翻译：本发明涉及生产肽的方法，并且相应地生产肽。根据本发明产生的肽可以比根据现有技术方法生产的肽更有效地生产。本发明的生产方法可以产生产量，纯度和/或价格的优点。还公开了销售肽的方法。

3. 发明授权

US06767483B2 Sol-gel encapsulation of lipid vesicles, lipid membranes and proteins 失效
标题翻译：脂质囊泡，脂质膜和蛋白质的溶胶 - 凝胶包封
公开(公告)号：US06767483B2
公开(公告)日：2004-07-27
申请号：US09934989
申请日：2001-08-21
申请人： Michael H. B. Stowell , Guangyang Wang , Sunney I. Chan
发明人： Michael H. B. Stowell , Guangyang Wang , Sunney I. Chan
IPC分类号： B01J1300
CPC分类号： A61K9/1273
摘要： Inorganic-organic hybrid mixture sol-gel encapsulated lipid vesicles which are composed of silyl lipids or a mixture of silyl lipids and phospholipids are provided. The present invention also provides encapsulated Langmuir Blogget (LB) membranes and biological macromolecules. The sol-gel encapsulated lipid vesicles, LB membranes and proteins possess a higher stability than conventional vesicles. Inorganic-organic hybrid mixture sol-gels are provided as novel sol-gel materials possessing desirable mechanical and physicochemical properties. Also provided are methods of preparing encapsulated lipid vesicles, LB membranes and proteins. Methods of performing renal dialysis using compositions of the invention are also provided.
摘要翻译：提供由甲硅烷基脂质或甲硅烷基脂质和磷脂的混合物组成的无机 - 有机杂化混合物溶胶 - 凝胶包封的脂质囊泡。本发明还提供封装的Langmuir Blogget（LB）膜和生物大分子。溶胶 - 凝胶包封的脂质囊泡，LB膜和蛋白质具有比常规泡囊更高的稳定性。提供无机 - 有机杂化混合物溶胶，作为具有理想的机械和物理化学性质的新型溶胶 - 凝胶材料。还提供了制备包封的脂质囊泡，LB膜和蛋白质的方法。还提供了使用本发明组合物进行肾透析的方法。

4. 发明授权

US06284163B1 Sol-gel encapsulation of lipid vesicles, lipid membranes and proteins 失效
标题翻译：脂质囊泡，脂质膜和蛋白质的溶胶 - 凝胶包封
公开(公告)号：US06284163B1
公开(公告)日：2001-09-04
申请号：US08788632
申请日：1997-01-24
申请人： Michael H. B. Stowell , Guangyang Wang , Sunney I. Chan
发明人： Michael H. B. Stowell , Guangyang Wang , Sunney I. Chan
IPC分类号： A61K950
CPC分类号： A61K9/1273
摘要： Inorganic-organic hybrid mixture sol-gel encapsulated lipid vesicles which are composed of silyl lipids or a mixture of silyl lipids and phospholipids are provided. The present invention also provides encapsulated Langmuir Blogget (LB) membranes and biological macromolecules. The sol-gel encapsulated lipid vesicles, LB membranes and proteins possess a higher stability than conventional vesicles. Inorganic-organic hybrid mixture sol-gels are provided as novel sol-gel materials possessing desirable mechanical and physicochemical properties. Also provided are methods of preparing encapsulated lipid vesicles, LB membranes and proteins. Methods of performing renal dialysis using compositions of the invention are also provided.
摘要翻译：提供由甲硅烷基脂质或甲硅烷基脂质和磷脂的混合物组成的无机 - 有机杂化混合物溶胶 - 凝胶包封的脂质囊泡。本发明还提供封装的Langmuir Blogget（LB）膜和生物大分子。溶胶 - 凝胶包封的脂质囊泡，LB膜和蛋白质具有比常规泡囊更高的稳定性。提供无机 - 有机杂化混合物溶胶，作为具有理想的机械和物理化学性质的新型溶胶 - 凝胶材料。还提供了制备包封的脂质囊泡，LB膜和蛋白质的方法。还提供了使用本发明组合物进行肾透析的方法。

5. 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.

6. 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.

7. 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.

8. 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。

9. 发明授权

US5256641A Covalent polar lipid-peptide conjugates for immunological targeting 失效
标题翻译：用于免疫靶向的共价极性脂质 - 肽缀合物
公开(公告)号：US5256641A
公开(公告)日：1993-10-26
申请号：US911209
申请日：1992-07-09
申请人： Milton B. Yatvin , Michael H. B. Stowell , Miroslav Malkovsky
发明人： Milton B. Yatvin , Michael H. B. Stowell , Miroslav Malkovsky
IPC分类号： A61K38/00 , A61K39/385 , A61K47/48 , A61P31/12 , A61P35/00 , A61P37/06 , C07F9/6558 , C07H19/06 , C07H19/10 , C07K14/00 , A61K31/00 , A61K31/19 , A61K31/685 , A61K37/02
CPC分类号： A61K47/48053 , A61K47/48046 , A61K47/48315 , C07H19/06 , C07H19/10 , Y10S514/885
摘要： This invention relates to methods of facilitating the entry of peptides into cells and targeting such peptides to specific organelles within the cell. The invention provides methods for delivering and specific targeting of antigenically-active peptides to cells for the specific production of immunological reactivity against such peptides, as well as compositions and pharmaceutical compositions of matter comprising such peptides. This invention thereby provides improved methods for vaccine production and in vivo vaccination against pathogenic microorganisms. Methods for alleviating autoimmune disease and ameliorating tissue and organ transplant rejection using such conjugates are also provided.
摘要翻译：本发明涉及促进肽进入细胞并将这些肽靶向细胞内的特定细胞器的方法。本发明提供了将抗原活性肽递送和特异性靶向细胞用于特异性产生对这种肽的免疫反应性的方法，以及包含这些肽的物质的组合物和药物组合物。因此，本发明提供了用于针对病原微生物的疫苗生产和体内疫苗接种的改进方法。还提供了使用这种缀合物来减轻自身免疫疾病和改善组织和器官移植排斥的方法。

10. 发明授权

US5149794A Covalent lipid-drug conjugates for drug targeting 失效
标题翻译：用于药物靶向的共价脂 - 药物偶联物
公开(公告)号：US5149794A
公开(公告)日：1992-09-22
申请号：US607982
申请日：1990-11-01
申请人： Milton B. Yatvin , David W. Parks , Ronald W. McClard , Michael H. B. Stowell , John F. Witte
发明人： Milton B. Yatvin , David W. Parks , Ronald W. McClard , Michael H. B. Stowell , John F. Witte
IPC分类号： A61K47/48 , C07H19/06 , C07H19/10
CPC分类号： C07H19/10 , A61K47/48046 , A61K47/48053 , A61K47/48338 , C07H19/06
摘要： This invention relates to a novel method of drug targeting which comprises covalently binding a drug to a lipid carrier. This composition has the unique ability to both enhance the rate at which an antineoplastic or antiviral drug crosses the plasma membrane, and to direct the drug within the cell to specific organelles. The versatility of these conjugates may be further enhanced by including a spacer group between the drug and the lipid which may act to modulate drug release at the target site.
摘要翻译：本发明涉及药物靶向的新方法，其包括将药物与脂质载体共价结合。该组合物具有提高抗肿瘤药物或抗病毒药物穿过质膜的速率以及将细胞内的药物引导至特定细胞器的独特能力。通过在药物和脂质之间包括间隔基团可以进一步增强这些缀合物的多功能性，所述间隔基团可以作用于调节靶位点的药物释放。

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