公开(公告)号：US10588860B2

公开(公告)日：2020-03-17

申请号：US15228686

申请日：2016-08-04

申请人： Edward Turos ,  Raphael Labruere ,  Ryan Scott Cormier ,  Renaud Sicard

发明人： Edward Turos ,  Raphael Labruere ,  Ryan Scott Cormier ,  Renaud Sicard

IPC分类号： A61K9/14 ,  A61K9/00 ,  A61K9/10 ,  A61K9/51 ,  A61K47/10 ,  A61K49/00 ,  A61K47/69

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.

公开(公告)号：US09433581B2

公开(公告)日：2016-09-06

申请号：US13897868

申请日：2013-05-20

申请人： Edward Turos ,  Raphael Labruere ,  Ryan Scott Cormier ,  Renaud Sicard

发明人： Edward Turos ,  Raphael Labruere ,  Ryan Scott Cormier ,  Renaud Sicard

IPC分类号： A61K9/14 ,  A61K9/00 ,  A61K9/10 ,  A61K9/51 ,  A61K47/10 ,  A61K47/48 ,  A61K49/00

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。

公开(公告)号：US20130211787A1

公开(公告)日：2013-08-15

申请号：US13835984

申请日：2013-03-15

申请人： Lee Kaufman ,  Mark Ayasse ,  Raymond Johnson ,  Raymond Dufresne ,  Scott Cormier ,  Vlad Mangeym

发明人： Lee Kaufman ,  Mark Ayasse ,  Raymond Johnson ,  Raymond Dufresne ,  Scott Cormier ,  Vlad Mangeym

IPC分类号： G05B23/00

CPC分类号： G05B23/00 ,  G06Q10/06315 ,  G06Q30/0203

摘要： A system allowing a user to respond to a series of options to generate survey data, associating system data with the survey data to generate a highly accurate report of the facility. The user may, customize the survey by selecting categories corresponding to certain series of options and be presented with a running total of costs associated with each selected action, a total cost for all selected actions, and an impact on the property FCI corresponding to the selected action. The option is further provided to take digital photos and/or videos and associate the photos/videos with selected facilities and facility systems.

摘要翻译： 一种允许用户响应一系列选项以生成测量数据的系统，将系统数据与调查数据相关联，以生成设备的高精度报告。 用户可以通过选择对应于某些系列选项的类别来定制调查，并且呈现与每个所选择的动作相关联的运行总成本，所有所选动作的总成本以及对所选择的动作的属性FCI的影响 行动。 该选项还被提供用于拍摄数字照片和/或视频，并将照片/视频与选定的设施和设施系统相关联。

公开(公告)号：US08143398B1

公开(公告)日：2012-03-27

申请号：US13031991

申请日：2011-02-22

申请人： Edward Turos ,  Burt E. Anderson ,  Ryan Scott Cormier ,  John C. Thomas ,  Rebecca J. Kapolka ,  Glenn Roma

发明人： Edward Turos ,  Burt E. Anderson ,  Ryan Scott Cormier ,  John C. Thomas ,  Rebecca J. Kapolka ,  Glenn Roma

IPC分类号： C07D241/04

CPC分类号： C07D241/04

摘要： Bartonella species are facultative intracellular pathogens responsible for a range of diseases in animals and in humans. A selection of N-acyl ciprofloxacin analogues, chemically synthesized from ciprofloxacin, have been tested in vitro for activity against Bartonella species as models for therapeutic development. Nine Bartonella strains, including five of B. henselae, two of B. quintana, and one each of B. elizabethae and B. vinsonii, have been tested for susceptibility to different N-acyl ciprofloxacin derivatives. Several techniques have been used to test the in vitro antibacterial activity of the derivatives. Seven of them, labeled RC4-125, RC4-143, RC4-147, RC5-28, RC5-29, RC5-32 and RC5-69 showed significant intracellular anti-Bartonella activity. These synthetically derived N-acyl ciprofloxacin derivatives may be useful in the therapeutic treatment of infections caused by Bartonella.

摘要翻译： 巴尔多奈属物种是造成动物和人类各种疾病的兼性细胞内病原体。 已经在体外测试了从环丙沙星化学合成的N-酰基环丙沙星类似物的选择，用于针对巴氏杆菌属物种的活性作为治疗发展的模型。 已经测试了九种巴尔通体菌株，其中包括五种B.henselae，两种金针菇，以及一种每种B. elizabethae和B.vinsonii，已经测试了对不同N-酰基环丙沙星衍生物的易感性。 已经使用几种技术来测试衍生物的体外抗菌活性。 其中7个标记为RC4-125，RC4-143，RC4-147，RC5-28，RC5-29，RC5-32和RC5-69，显示出显着的细胞内抗Bartonella活性。 这些合成衍生的N-酰基环丙沙星衍生物可用于治疗由巴氏杆菌引起的感染的治疗。

公开(公告)号：US20160338962A1

公开(公告)日：2016-11-24

申请号：US15228686

申请日：2016-08-04

申请人： Edward Turos ,  Raphael Labruere ,  Ryan Scott Cormier ,  Renaud Sicard

发明人： Edward Turos ,  Raphael Labruere ,  Ryan Scott Cormier ,  Renaud Sicard

IPC分类号： A61K9/14

CPC分类号： A61K9/146 ,  A61K9/0019 ,  A61K9/10 ,  A61K9/5138 ,  A61K47/10 ,  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。

公开(公告)号：US20130243832A1

公开(公告)日：2013-09-19

申请号：US13897868

申请日：2013-05-20

申请人： Edward Turos ,  Raphael Labruere ,  Ryan Scott Cormier ,  Renaud Sicard

发明人： Edward Turos ,  Raphael Labruere ,  Ryan Scott Cormier ,  Renaud Sicard

IPC分类号： A61K9/14

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无毒性（IC50> 1000mug / mL）和原代牛原发性主动脉内皮细胞（IC50> 500mug / mL），并对选择的代表性测试微生物施加不可观察的杀菌活性 （MIC> 250mug / 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。