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1. 发明申请

WO2012068476A3 POLY(VINYL BENZOATE) NANOPARTICLES FOR MOLECULAR DELIVERY 审中-公开
标题翻译：用于分子递送的POLY（乙烯基苯甲酸酯）纳米粒子
公开(公告)号：WO2012068476A3
公开(公告)日：2012-08-30
申请号：PCT/US2011061429
申请日：2011-11-18
申请人： UNIV 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 , A61K9/14 , A61K9/16 , A61K47/30 , 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 (IC50 >1000 µg/mL) and primary bovine primary aortic endothelial cells (IC50 >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：本发明包含聚（苯甲酸乙烯酯）纳米颗粒悬浮液作为分子载体。这些纳米颗粒可以通过使用Pluronic F68作为表面活性剂在水中纳米沉淀聚（苯甲酸乙烯酯）以形成直径为约200-250nm的球形纳米结构，其在磷酸盐缓冲液和血清中稳定并且在存在时仅缓慢降解的酯酶。磷酸盐缓冲液中的动力学实验表明，香豆素-6的78％被包封在纳米粒子的聚合物基质内，并且剩余22％的香豆素-6被表面结合并且快速释放。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，并对选择的代表性测试微生物发挥不可观察的杀菌活性（MIC>250μg/ mL）。聚（苯甲酸乙烯酯）纳米粒子是用于分子递送亲脂性小分子的合适载体，例如药物药物和成像剂。

2. 发明申请

WO2004100888A2 METHODS FOR PREVENTING AND TREATING CANCER USING N-THIOLATED beta-LACTAM COMPOUNDS AND ANALOGS THEREOF 审中-公开
标题翻译：使用N-硫代β-乳糖化合物及其类似物预防和治疗癌症的方法
公开(公告)号：WO2004100888A2
公开(公告)日：2004-11-25
申请号：PCT/US2004014460
申请日：2004-05-06
申请人： UNIV SOUTH FLORIDA , DOU Q PING , TUROS EDWARD , SMITH DAVID M
发明人： DOU Q PING , TUROS EDWARD , SMITH DAVID M
IPC分类号： C07D205/08 , C07D491/04 , A61K
CPC分类号： C07D491/04 , C07D205/08
摘要： The subject invention concerns N-thiolated beta-lactam compounds, their analogs and pharmaceutically acceptable salts, esters and amides thereof. The subject invention also concerns methods for inducing tumor cell death or inhibiting tumor cell proliferation, and methods for inducing DNA damage, inhibiting DNA replication, activating p38 MAP kinase, or activating caspase cascade activation, or releasing cytochrome C from mitochondria into the cytoplasm in a tumor cell. Methods for treating cancer using N-thiolated beta-lactam compounds, as well as pharmaceutical compositions comprising the same are further disclosed.
摘要翻译：本发明涉及N-硫醇化的β-内酰胺化合物，其类似物和药学上可接受的盐，酯和酰胺。本发明还涉及诱导肿瘤细胞死亡或抑制肿瘤细胞增殖的方法，以及用于诱导DNA损伤，抑制DNA复制，激活p38 MAP激酶或激活胱天蛋白酶级联活化或将细胞色素C从线粒体释放到细胞质中的方法肿瘤细胞。使用N-硫醇化β-内酰胺化合物治疗癌症的方法以及包含其的药物组合物进一步公开。

3. 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。

4. 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。

5. 发明申请

WO2009055650A3 POLYACRYLATE NANOPARTICLE DRUG DELIVERY 审中-公开
标题翻译：聚丙烯酸纳米颗粒药物递送
公开(公告)号：WO2009055650A3
公开(公告)日：2009-06-04
申请号：PCT/US2008081080
申请日：2008-10-24
申请人： UNIV SOUTH FLORIDA , TUROS EDWARD , CORMIER RYAN , KYLE DENNIS E
发明人： TUROS EDWARD , CORMIER RYAN , KYLE DENNIS E
IPC分类号： A61F13/00
CPC分类号： A61K9/5138 , A61K9/5192
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：通过聚丙烯酸酯纳米颗粒用于治疗药物（例如氯喹）耐药性疟疾的药物递送抗性逆转剂。还提供了环丙沙星的聚丙烯酸酯纳米颗粒用于治疗炭疽的药物递送。

6. 发明申请

WO2008085556A3 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：WO2008085556A3
公开(公告)日：2008-10-16
申请号：PCT/US2007078289
申请日：2007-09-12
申请人： UNIV 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 , A61K9/16 , A61K9/50 , G03C1/498
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（例如抗生素或其他药物）递送至人类或非人类受试者的方法。在一个实施方案中，纳米粒子是“表面活性剂”纳米粒子，其中表面活性剂部分共价连接到聚合物的骨架上。

7. 发明公开

EP2867298A4 BIOCOMPATIBLE POLYACRYLATE COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：维生素BULKOMPATIBLE POLYACRYLATZUSAMMENSETZUNGEN UND VERFAHREN ZUR VERWENDUNG
公开(公告)号：EP2867298A4
公开(公告)日：2016-01-20
申请号：EP13809673
申请日：2013-03-13
申请人： UNIV SOUTH FLORIDA
发明人： GREENHALGH KERRIANN ROBYN , TUROS EDWARD , ESPINOSA JULIO
IPC分类号： A61L31/10 , A61L15/24 , A61L15/44 , A61L15/46 , A61L24/00 , A61L24/06 , A61L26/00 , A61L27/34 , A61L27/54 , A61L31/16
CPC分类号： A61L31/10 , A61L15/24 , A61L15/44 , A61L15/46 , A61L24/0015 , A61L24/06 , A61L26/0014 , A61L26/0019 , A61L26/0066 , A61L27/34 , A61L27/54 , A61L31/16 , A61L2300/624 , A61L2400/04 , A61L2400/08 , A61L2400/12 , C08F220/14 , C08F220/18 , C08L33/08

8. 发明专利

CA2607660A1 N-THIOLATED 2-OXAZOLIDONE ANTIBIOTICS 未知
公开(公告)号：CA2607660A1
公开(公告)日：2006-11-16
申请号：CA2607660
申请日：2006-05-08
申请人： UNIV SOUTH FLORIDA
发明人： MISHRA RAJESH KUMAR , TUROS EDWARD
IPC分类号： C07D413/12 , A61K31/421 , C07D263/04
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.

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