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1. 发明申请

WO2005020933A2 NANOPARTICLES FOR DRUG-DELIVERY 审中-公开
标题翻译：药物输送纳米脂
公开(公告)号：WO2005020933A2
公开(公告)日：2005-03-10
申请号：PCT/US2004/028995
申请日：2004-09-02
申请人： UNIVERSITY OF SOUTH FLORIDA , TUROS, Edward , SHIM, Jeung-Yeop
发明人： TUROS, Edward , SHIM, Jeung-Yeop
IPC分类号： A61K
CPC分类号： A61K9/5138 , A61K9/5192
摘要： This invention relates to a unique process for the preparation of polymeric nanoparticles with target molecules bonded to the surface of the particles and having sizes of up to 1000nm, preferably Inm to 400nm, more preferably Inm to 200nm, that are dispersed homogeneously in aqueous solution. To accomplish the above objective, the polymeric nanoparticles of the subject invention are prepared using a novel technique of microemulsion polymerization. The resulting aqueous solution of polymeric nanoparticles is comprised of about 1 to 100 parts per weight of water or buffer, about 1 to 80 parts per weight of polymeric nanoparticles, which the bio-active molecules are conjugated, about 0.001 to 10 parts per weight of emulsifier, and about 0.00001 to 5 parts per weight of radical initiator based on the weight of the solution. In the method of this invention, the target drug/target substance is covalently bonded to the polymeric nanoparticles to secure them from outer intervention in vivo or cell culture in vitro until they are exposed at the target site within the cell.
摘要翻译：本发明涉及用于制备聚合物纳米颗粒的独特方法，其中靶分子键合到颗粒的表面，并且具有均匀分散在水溶液中的高达1000nm，优选Inm至400nm，更优选Inm至200nm的尺寸。为了实现上述目的，使用微乳液聚合的新技术制备本发明的聚合物纳米颗粒。所得到的聚合物纳米颗粒水溶液由约1至100份/重量的水或缓冲剂组成，约1至80份/重量的聚合物纳米颗粒，生物活性分子共轭，约0.001至10份/ 乳化剂和基于溶液重量的约0.00001至5重量份的自由基引发剂。在本发明的方法中，目标药物/靶物质共价键合到聚合物纳米颗粒上以确保它们在体内不受外部介入或体外细胞培养，直到它们暴露于细胞内的靶位点为止。

2. 发明申请

WO2009055650A2 POLYACRYLATE NANOPARTICLE DRUG DELIVERY 审中-公开
标题翻译：聚丙烯酸纳米脂药物递送
公开(公告)号：WO2009055650A2
公开(公告)日：2009-04-30
申请号：PCT/US2008/081080
申请日：2008-10-24
申请人： UNIVERSITY OF SOUTH FLORIDA , TUROS, Edward , CORMIER, Ryan , KYLE, Dennis E.
发明人： TUROS, Edward , CORMIER, Ryan , KYLE, Dennis E.
IPC分类号： A61K9/18
CPC分类号： A61K9/5138 , A61K9/5192 , Y02A50/411
摘要： Drug delivery of resistance reversal agents by polyacrylate nanoparticles for treatment of drug (e.g. chloroquine) resistant malaria. Also provided are drug delivery by polyacrylate nanoparticles of ciprofloxacin for treatment of anthrax.
摘要翻译：用于治疗药物（例如氯喹）抗性疟疾的聚丙烯酸酯纳米颗粒的药物递送抗逆转剂。还提供了用于治疗炭疽的环丙沙星的聚丙烯酸酯纳米颗粒的药物递送。

3. 发明申请

WO2008033505A1 BIOCOMPOSITE FOR ARTIFICIAL TISSUE DESIGN 审中-公开
标题翻译：人工组织设计生物化学
公开(公告)号：WO2008033505A1
公开(公告)日：2008-03-20
申请号：PCT/US2007/020006
申请日：2007-09-13
申请人： UNIVERSITY OF SOUTH FLORIDA , TUROS, Edward , KOOB, Thomas, J. , GREENHALGH, Kerriann, Robyn
发明人： TUROS, Edward , KOOB, Thomas, J. , GREENHALGH, Kerriann, Robyn
IPC分类号： A61F2/10
CPC分类号： A61L27/54 , A61L27/48 , A61L2300/64 , C08L89/06
摘要： The present invention concerns a biocomposite useful in artificial tissue replacement, methods for its production, and methods of use. The biocomposite can be implanted into humans or animals as an artificial tissue for treatment of a tissue defect. The biocomposite can be formed or manipulated into a desired shape for implantation.
摘要翻译：本发明涉及可用于人造组织置换的生物复合物，其生产方法和使用方法。生物复合材料可以植入人或动物作为人造组织来治疗组织缺损。生物复合材料可以形成或操纵成所需的植入形状。

4. 发明申请

WO2007133706A3 ANTIBIOTIC-BOUND POLY (CAPROLACTONE) POLYMER 审中-公开
标题翻译：抗生物聚合物（CAPROLACTONE）聚合物
公开(公告)号：WO2007133706A3
公开(公告)日：2008-11-27
申请号：PCT/US2007011454
申请日：2007-05-11
申请人： UNIV SOUTH FLORIDA , TUROS EDWARD , LESLIE MICHELLE
发明人： TUROS EDWARD , LESLIE MICHELLE
IPC分类号： C07D405/12 , A61K31/787 , C07D313/04 , C08G63/08
CPC分类号： A61K31/21 , C07D313/04 , C07D405/12 , Y02P20/55
摘要： This invention is the design and synthesis of a caprolactone monomer which bears a pendant protected carboxyl group. This monomer has been copolymerized with caprolactone in varying ratios. After polymerization, the protecting group can be removed and an antibiotic can be attached as a new pendant group. The bioactivity of the antibiotic-bound poly(caprolactone) polymer is described.
摘要翻译：本发明是设计和合成具有侧基保护的羧基的己内酯单体。该单体已经以不同比例的己内酯共聚。聚合后，可以除去保护基，并且可以将抗生素作为新的侧基附着。描述了抗生素结合的聚（己内酯）聚合物的生物活性。

5. 发明申请

WO2008033278A1 HETEROSUBSTITUTED N-THIOLATED BETA-LACTAM COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：异噻唑啉衍生物的酯交酯化合物及其使用方法
公开(公告)号：WO2008033278A1
公开(公告)日：2008-03-20
申请号：PCT/US2007/019576
申请日：2007-09-07
申请人： UNIVERSITY OF SOUTH FLORIDA , TUROS, Edward , RAMARAJU, Praveen
发明人： TUROS, Edward , RAMARAJU, Praveen
IPC分类号： C07D205/08 , C07D403/12 , A61P31/04
CPC分类号： C07D403/12 , C07D205/085 , C07D209/48
摘要： The invention relates to heterosubstituted N-thiolated beta-lactams, compositions comprising these compounds, methods for their production, and methods of use as antibiotics to inhibit the growth of bacteria. The antibacterial agents of the invention can be administered to a human or animal to treat or inhibit bacterial infection, such as that of Staphylococcus species, including methicillin-resistant Staphylococcus aureus (MRSA).
摘要翻译：本发明涉及异取代的N-硫醇化β-内酰胺，包含这些化合物的组合物，其生产方法和用作抗生素以抑制细菌生长的方法。本发明的抗菌剂可以施用于人或动物以治疗或抑制细菌感染，例如包括耐甲氧西林金黄色葡萄球菌（MRSA）的葡萄球菌属物种。

6. 发明申请

WO2006121962A1 N-THIOLATED 2-OXAZOLIDONE ANTIBIOTICS 审中-公开
标题翻译： N-巯基二氧杂环丁烷抗生素
公开(公告)号：WO2006121962A1
公开(公告)日：2006-11-16
申请号：PCT/US2006/017605
申请日：2006-05-08
申请人： UNIVERSITY OF SOUTH FLORIDA , TUROS, Edward , MISHRA, Rajesh, Kumar
发明人： TUROS, Edward , MISHRA, Rajesh, Kumar
IPC分类号： C07D413/12 , C07D263/04 , A61K31/421
CPC分类号： C07D263/26 , C07D263/52
摘要： This invention describes the discovery and synthesis of N-thiolated 2-oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2- oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit potent anti-bacterial activity, including bacteriostatic properties against Staphylococcus spp., including methicillin resistant Staphylcoccus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.
摘要翻译：本发明描述了作为新类抗细菌剂的N-硫醇化2-恶唑烷酮的发现和合成。这些化合物可以由2-恶唑烷酮通过Nd保护和N-亚磺酰化合成。发现这些新物质表现出有效的抗细菌活性，包括对葡萄球菌属的抑菌性，包括耐甲氧西林金黄色葡萄球菌（MRSA）和芽孢杆菌属（Bacillus spp。），包括炭疽芽孢杆菌。

7. 发明申请

WO2005020933A3 NANOPARTICLES FOR DRUG-DELIVERY 审中-公开
标题翻译：用于药物递送的纳米颗粒
公开(公告)号：WO2005020933A3
公开(公告)日：2005-06-09
申请号：PCT/US2004028995
申请日：2004-09-02
申请人： UNIV SOUTH FLORIDA , TUROS EDWARD , SHIM JEUNG-YEOP
发明人： TUROS EDWARD , SHIM JEUNG-YEOP
IPC分类号： A61K20060101 , A61K9/14 , A61K9/51
CPC分类号： A61K9/5138 , A61K9/5192
摘要： This invention relates to a unique process for the preparation of polymeric nanoparticles with target molecules bonded to the surface of the particles and having sizes of up to 1000nm, preferably Inm to 400nm, more preferably Inm to 200nm, that are dispersed homogeneously in aqueous solution. To accomplish the above objective, the polymeric nanoparticles of the subject invention are prepared using a novel technique of microemulsion polymerization. The resulting aqueous solution of polymeric nanoparticles is comprised of about 1 to 100 parts per weight of water or buffer, about 1 to 80 parts per weight of polymeric nanoparticles, which the bio-active molecules are conjugated, about 0.001 to 10 parts per weight of emulsifier, and about 0.00001 to 5 parts per weight of radical initiator based on the weight of the solution. In the method of this invention, the target drug/target substance is covalently bonded to the polymeric nanoparticles to secure them from outer intervention in vivo or cell culture in vitro until they are exposed at the target site within the cell.
摘要翻译：本发明涉及一种制备聚合物纳米颗粒的独特方法，其中目标分子与颗粒表面结合并具有最高达1000nm，优选Inm至400nm，更优选Inm至200nm的尺寸，其均匀分散于水溶液中。为了实现上述目的，本发明的聚合物纳米颗粒使用微乳液聚合的新技术制备。所得到的聚合物纳米粒子的水溶液由约1至100重量份的水或缓冲剂，约1至80重量份的生物活性分子缀合的聚合物纳米粒子，约0.001至10重量份的乳化剂和约0.00001-5重量份的基于溶液重量的自由基引发剂。在本发明的方法中，目标药物/目标物质共价结合到聚合物纳米粒子上，以确保它们免于体外外部干预或体外细胞培养，直到它们暴露于细胞内的靶位点。

8. 发明申请

WO2012068476A2 POLY(VINYL BENZOATE) NANOPARTICLES FOR MOLECULAR DELIVERY 审中-公开
标题翻译： POLY（VINYL BENZOATE）NANOPARTICLES FOR MOLECULAR DELIVERY
公开(公告)号：WO2012068476A2
公开(公告)日：2012-05-24
申请号：PCT/US2011/061429
申请日：2011-11-18
申请人： UNIVERSITY OF SOUTH FLORIDA , TUROS, Edward , LABRUERE, Raphael , CORMIER, Ryan Scott , SICARD, Renaud
发明人： TUROS, Edward , LABRUERE, Raphael , CORMIER, Ryan Scott , SICARD, Renaud
IPC分类号： A61K47/34 , A61K47/30 , A61K9/16 , A61K9/14 , A61K49/06 , A61K49/12 , C08F18/04
CPC分类号： A61K9/146 , A61K9/0019 , A61K9/10 , A61K9/5138 , A61K47/10 , A61K47/489 , A61K47/6933 , A61K49/0039 , A61K49/0043 , A61K49/0093
摘要： The present invention comprises poly(vinyl benzoate) nanoparticle suspensions as molecular carriers. These nanoparticles can be formed by nanoprecipitation of poly(vinyl benzoate) in water using Pluronic F68 as surfactant, to create spherical nanostructures measuring about 200-250 nm in diameter which are stable in phosphate buffer and blood serum, and only slowly degrade in the presence of esterases. Kinetics experiments in phosphate buffer indicate that 78% of the coumarin-6 was encapsulated within the polymer matrix of the nanoparticle, and the residual 22% of coumarin-6 was surface-bound and quickly released. The nanoparticles are non-toxic in vitro towards human epithelial cells (IC 50 >1000 µg/mL) and primary bovine primary aortic endothelial cells (IC 50 >500 µg/mL), and exert non-observable bactericidal activity against a selection of representative test microbes (MIC >250 µg/mL). Poly(vinyl benzoate) nanoparticles are suitable carriers for molecular delivery of lipophilic small molecules such as drugs pharmaceutical and imaging agents.
摘要翻译：本发明包括作为分子载体的聚（苯甲酸乙烯酯）纳米颗粒悬浮液。这些纳米颗粒可以通过使用Pluronic F68作为表面活性剂在水中的聚（乙烯基苯甲酸酯）的纳米沉淀形成，以产生直径约200-250nm的球形纳米结构，其在磷酸盐缓冲液和血清中是稳定的，并且在存在下仅缓慢降解的酯酶。在磷酸盐缓冲液中的动力学实验表明，78％的香豆素-6被包封在纳米颗粒的聚合物基质内，剩余的22％的香豆素-6被表面结合并迅速释放。纳米颗粒在体外对人上皮细胞（IC50>1000μg/ mL）和原代牛主动脉内皮细胞（IC50>500μg/ mL）无毒性，并且对代表性测试微生物的选择施加不可观察的杀菌活性（MIC>250μg/ mL）。聚（苯甲酸乙烯酯）纳米颗粒是分子递送亲脂性小分子如药物药物和成像剂的合适的载体。

9. 发明申请

WO2008085556A2 SURFACTANT-FREE NANOPARTICLES FOR DRUG DELIVERY 审中-公开
标题翻译：用于药物递送的无表面活性剂的纳米颗粒
公开(公告)号：WO2008085556A2
公开(公告)日：2008-07-17
申请号：PCT/US2007/078289
申请日：2007-09-12
申请人： UNIVERSITY OF SOUTH FLORIDA , TUROS, Edward , GREENHALGH, Kerriann, Robyn , GARAY, Julio, Cesar
发明人： TUROS, Edward , GREENHALGH, Kerriann, Robyn , GARAY, Julio, Cesar
IPC分类号： A61K9/14 , A61K9/50
CPC分类号： A61K47/58 , A61K47/6905 , A61K47/6933 , B82Y5/00
摘要： The present invention concerns nanoparticles, compositions comprising the nanoparticles, methods for their production, and methods of using the nanoparticles for the delivery of biologically active agents ( e.g. , antibiotics or other drugs) to human or non-human subjects. In one embodiment, the nanoparticle is a "surfactant-free" nanoparticle in which the surfactant moiety is covalently attached to the backbone of the polymer.
摘要翻译：本发明涉及纳米颗粒，包含纳米颗粒的组合物，其制备方法以及使用纳米颗粒将生物活性剂（例如抗生素或其它药物）递送给人类或非人类受试者的方法。在一个实施方案中，纳米颗粒是“表面活性剂”纳米颗粒，其中表面活性剂部分共价连接到聚合物的主链上。

10. 发明申请

WO2007133706A2 ANTIBIOTIC-BOUND POLY (CAPROLACTONE) POLYMER 审中-公开
标题翻译：抗生物聚合物（CAPROLACTONE）聚合物
公开(公告)号：WO2007133706A2
公开(公告)日：2007-11-22
申请号：PCT/US2007/011454
申请日：2007-05-11
申请人： UNIVERSITY OF SOUTH FLORIDA , TUROS, Edward , LESLIE, Michelle
发明人： TUROS, Edward , LESLIE, Michelle
IPC分类号： B05D3/00 , B05D5/00
CPC分类号： A61K31/21 , C07D313/04 , C07D405/12 , Y02P20/55
摘要： This invention is the design and synthesis of a caprolactone monomer which bears a pendant protected carboxyl group. This monomer has been copolymerized with caprolactone in varying ratios. After polymerization, the protecting group can be removed and an antibiotic can be attached as a new pendant group. The bioactivity of the antibiotic-bound poly(caprolactone) polymer is described.
摘要翻译：本发明是负载侧保护的羧基的己内酯单体的设计和合成。该单体已经以不同比例的己内酯共聚。聚合后，可以除去保护基，作为新的侧基可以附着抗生素。描述了抗生素结合的聚（己内酯）聚合物的生物活性。

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