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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 57. Отображено 57.
18-06-2009 дата публикации

DERIVATIVE N-THIOLATED 2-OXAZOLIDINONE ANTIBIOTICS

Номер: US2009156654A1
Принадлежит:

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 Staphylococcus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.

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04-11-2010 дата публикации

Polyacrylate Nanoparticle Drug Delivery

Номер: US20100278920A1
Принадлежит: University of South Florida

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.

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24-04-2018 дата публикации

N-alkylthio beta-lactams, alkyl-coenzyme A asymmetric disulfides, and aryl-alkyl disulfides as anti-bacterial agents

Номер: US0009949480B2

The present invention provides N-alkylthio β-lactams and disulfide compounds (e.g., alkyl-coenzyme A asymmetric disulfides or aryl-alkyl disulfides), compositions containing such compounds, and methods of their use as anti-bacterial agents.

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14-09-2021 дата публикации

Nanoparticles carrying antibiotics

Номер: US0011116725B2

The subject invention pertains to polyacrylate homopolymers produced from acrylolated drug monomers. The homopolymers can be produced in the form of nanoparticles. The nanoparticles comprising the homopolymers can be produced via a free radical-induced emulsion polymerization of the acrylolated drug monomers to produce an aqueous emulsion of uniformly sized nanoparticles. The homopolymers of the invention containing acrylolated antibiotic monomers can be active against Gram-positive and Gram-negative bacteria, such as Staphylococcus aureus and Escherichia coil. Accordingly, methods are provided of treating a disease, for example, an infection, by administering to a subject the homopolymers, homopolymeric nanoparticles, or emulsions containing homopolymeric nanoparticles of the invention.

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21-08-2014 дата публикации

N-ALKYLTHIO BETA-LACTAMS, ALKYL-COENZYME A ASYMMETRIC DISULFIDES, AND ARYL-ALKYL DISULFIDES AS ANTI-BACTERIAL AGENTS

Номер: US20140235565A1
Принадлежит: UNIVERSITY OF SOUTH FLORIDA

The present invention provides N-alkylthio β-lactams and disulfide compounds (e.g., alkyl-coenzyme A asymmetric disulfides or aryl-alkyl disulfides), compositions containing such compounds, and methods of their use as anti-bacterial agents.

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09-05-2019 дата публикации

NANOPARTICLES CARRYING ANTIBIOTICS

Номер: US20190133944A1
Принадлежит: University of South Florida

The subject invention pertains to polyacrylate homopolymers produced from acrylolated drug monomers. The homopolymers can be produced in the form of nanoparticles. The nanoparticles comprising the homopolymers can be produced via a free radical-induced emulsion polymerization of the acrylolated drug monomers to produce an aqueous emulsion of uniformly sized nanoparticles. The homopolymers of the invention containing acrylolated antibiotic monomers can be active against Gram-positive and Gram-negative bacteria, such as Staphylococcus aureus and Escherichia coil. Accordingly, methods are provided of treating a disease, for example, an infection, by administering to a subject the homopolymers, homopolymeric nanoparticles, or emulsions containing homopolymeric nanoparticles of the invention.

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10-07-2008 дата публикации

HETEROSUBSTITUTED N-THIOLATED BETA-LACTAM COMPOUNDS AND METHODS OF USE

Номер: US2008167285A1
Принадлежит:

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).

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06-06-2017 дата публикации

Antibiotic compositions and methods of use

Номер: US0009670179B1

Embodiments of the present disclosure provide for compositions including an antibiotic containing a N-thiolated beta-lactam moiety, pharmaceutical compositions including the antibiotic, methods of treatment of a condition (e.g., bacterial infection), methods of treatment using compositions or pharmaceutical compositions, and the like.

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30-06-2011 дата публикации

HETEROSUBSTITUTED N-THIOLATED BETA-LACTAM COMPOUNDS AND METHODS OF USE

Номер: US20110160178A1
Принадлежит: University of South Florida

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. In one embodiment, the compounds have the structure shown in formula (A) or formula (B) or formula (C): wherein the R groups are as defined in the specification. 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).

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03-01-2017 дата публикации

Menthol-based nanoparticles for drug delivery

Номер: US0009533051B2

The subject invention pertains to formulations comprising poly(menthyl acrylate) nanoparticles comprising at least one active ingredient contained in a plurality of hydrophobic carriers and dispersed in an aqueous medium. The subject invention further pertains to methods of polymerization of drug loaded nanoparticles made up of methyl acrylate monomers in an aqueous emulsion.

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10-01-2012 дата публикации

Method for producing biocomposite comprising collagen and polymer

Номер: US0008093027B2

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.

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15-11-2007 дата публикации

Antibiotic-Bound Poly(Caprolactone) Polymer

Номер: US2007265243A1
Принадлежит:

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.

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24-11-2016 дата публикации

POLY(VINYL BENZOATE) NANOPARTICLES FOR MOLECULAR DELIVERY

Номер: US20160338962A1
Принадлежит: University of South Florida

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.

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17-03-2020 дата публикации

Poly(vinyl benzoate) nanoparticles for molecular delivery

Номер: US0010588860B2

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.

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25-06-2013 дата публикации

Antibiotic-bound poly(caprolactone) polymer

Номер: US0008470958B1

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.

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27-03-2012 дата публикации

Activity of new N-acylated ciprofloxacin derivatives against faculative intracellular bacteria

Номер: US0008143398B1

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.

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13-05-2014 дата публикации

Asymmetric disulfides and aryl-alkyl disulfides as anti-bacterial agents

Номер: US0008722937B2

The present invention provides N-alkylthio -lactams and disulfide compounds (e.g., alkyl-coenzyme A asymmetric disulfides or aryl-alkyl disulfides), compositions containing such compounds, and method of their use as anti-bacterial agents.

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27-01-2009 дата публикации

N-thiolated 2-oxazolidinone-derived antibiotics

Номер: US0007482467B2

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 Staphylococcus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.

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09-04-2013 дата публикации

Nanoparticles with covalently bound surfactant for drug delivery

Номер: US0008414926B1

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.

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16-07-2019 дата публикации

Antibacterial S-heterosubstituted disulfides

Номер: US0010350177B2

Synthetically-derived S,S-heterodisubstituted disulfides that exhibit potent in vitro antibacterial activity against a variety of bacteria, including Staphylococcus aureus, methicillin-resistant Staphylococcus aureus and Francisella tularensis. The present invention provides compounds, methods and compositions effective to treat microbial/bacterial infections, and, especially, infections arising from bacteria which have developed resistance to conventional antibiotics.

Подробнее
04-08-2015 дата публикации

N-alkylthio beta-lactams, alkyl-coenzyme A asymmetric disulfides, and aryl-alkyl disulfides as anti-bacterial agents

Номер: US0009096635B2

The present invention provides N-alkylthio -lactams and disulfide compounds (e.g., alkyl-coenzyme A asymmetric disulfides or aryl-alkyl disulfides), compositions containing such compounds, and methods of their use as anti-bacterial agents.

Подробнее
22-04-2014 дата публикации

Derivative N-thiolated 2-oxazolidinone antibiotics

Номер: US0008703963B2

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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19-02-2008 дата публикации

N-thiolated 2 oxazolidone antibiotics

Номер: US0007332611B2

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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20-09-2005 дата публикации

N-thiolated beta-lactams: novel antibacterial agents for methicillin-resistant Staphylococcus aureus

Номер: US0006946458B2
Автор: Edward Turos, TUROS EDWARD

The invention relates generally to novel N-thiolated beta-lactams. More specifically, the invention relates to the use of these novel antibacterial agents in the treatment or inhibition of methicillin-resistant Staphylococcus aureus.

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06-09-2016 дата публикации

Poly(vinyl benzoate) nanoparticles for molecular delivery

Номер: US0009433581B2

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.

Подробнее
07-02-2012 дата публикации

Antibiotic-bound poly(caprolactone) polymer

Номер: US0008110678B2

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.

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16-08-2007 дата публикации

Nanoparticles for drug-delivery

Номер: US2007190160A1
Принадлежит:

This invention relates to polymeric nanoparticles useful for drug delivery with target molecules bonded to the surface of the particles and having sizes of up to 1000 nm, preferably 1 nm to 400 nm, more preferably 1 nm to 200 nm, that are dispersed homogeneously in aqueous solution. The target drug/target substance is covalently bonded to the novel 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. This invention also relates to microemulsion polymerization techniques useful for preparing the novel nanoparticles.

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14-06-2012 дата публикации

DERIVATIVE N-THIOLATED 2-OXAZOLIDINONE ANTIBIOTICS

Номер: US20120149911A1
Принадлежит: UNIVERSITY OF SOUTH FLORIDA

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.

Подробнее
07-12-2010 дата публикации

Heterosubstituted N-thiolated beta-lactam compounds and methods of use

Номер: US0007846920B2

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. In one embodiment, the compounds have the structure shown in formula (A) or formula (B) or formula (C): wherein the R groups are as defined in the specification. 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).

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17-05-2012 дата публикации

BIOCOMPOSITE FOR ARTIFICIAL TISSUE DESIGN

Номер: US20120121531A1
Принадлежит: UNIVERSITY OF SOUTH FLORIDA

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. 1. A synthetic biocomposite comprising a biotic material and an abiotic material.2. The biocomposite of claim 1 , wherein the biotic material is collagen and the abiotic material is a polymer.3. The biocomposite of claim 1 , wherein the biocomposite is a fiber comprising an intertwined polymer emulsion and fibrils.4. The biocomposite of claim 3 , wherein the fibrils are collagen fibrils.5. The biocomposite of claim 1 , wherein the abiotic material is a polymer emulsion.6. The biocomposite of claim 1 , wherein the abiotic material comprises a copolymer emulsion.7. The biocomposite of claim 6 , wherein the copolymer is ethyl acrylate-methyl methacrylate.8. The biocomposite of claim 1 , further comprising a biologically active agent.9. The biocomposite of claim 8 , wherein the biologically active agent is a cell.10. A device comprising a surface with a synthetic biocomposite comprising a biotic material and an abiotic material.11. The device of claim 10 , wherein the device is a medical implant.12. A method for producing a synthetic biocomposite claim 10 , comprising polymerizing a biotic material and an abiotic material by emulsion polymerization claim 10 , thereby forming the synthetic biocomposite.13. The method of claim 12 , wherein the biotic material is collagen and the abiotic material is a polymer.14. The method of claim 12 , wherein the biocomposite is a fiber comprising an intertwined polymer emulsion and fibrils.15. The method of claim 14 , wherein the fibrils are collagen fibrils.16. The method of claim 12 , wherein the abiotic material is a polymer emulsion.17. The method of claim 12 , wherein the abiotic material comprises a ...

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05-11-2002 дата публикации

N-thiolated beta-lactam antibiotics

Номер: US0006476015B1

Substituted monocyclic beta-lactam compounds that are N-1-thiolated monolactams, and which exhibit wide-ranging antibacterial activities, having a single 4-membered azetidinone ring in which: the N-1 nitrogen atom of the azetidinone ring is bonded to sulfur but is not sulfonated, of the formula:wherein R1-5 are independently hydrogen, alkyl, heteroalkyl, aryl, heteroaryl, alkenyl, or alkynyl; X is H, C, or O; and n=0-3. Chemical synthesis of these compounds by a [2+2]-imine-acid chloride cycloaddition, and methods for subsequent derivatization, are also disclosed. The compounds and compositions disclosed herein are useful as antibacterial and antibiotic agents.

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02-03-2017 дата публикации

ANTIBACTERIAL S-HETEROSUBSTITUTED DISULFIDES

Номер: US20170056337A1
Принадлежит: University of South Florida

Synthetically-derived S,S-heterodisubstituted disulfides that exhibit potent in vitro antibacterial activity against a variety of bacteria, including , methicillin-resistant and . The present invention provides compounds, methods and compositions effective to treat microbial/bacterial infections, and, especially, infections arising from bacteria which have developed resistance to conventional antibiotics. 2. The method of claim 1 , further comprising a pharmaceutically acceptable carrier.3. The method of claim 1 , wherein Xand Xare NH-phenyl.4. The method of claim 3 , wherein the compound is administered to reach a concentration of at least 0.5 μg/mL.5. The method of claim 1 , wherein Xand Xare S—R.6. The method of claim 5 , wherein Ris propyl claim 5 , or phenyl.7. The method of claim 6 , wherein the compound is administered to reach a concentration of at least 1 μg/mL where Ris propyl claim 6 , or at least 2 μg/mL where Ris phenyl.8. The method of claim 1 , wherein Xand Xare O—R.9. The method of claim 8 , wherein Ris butyl claim 8 , isopropyl claim 8 , or phenyl.10. The method of claim 9 , wherein the compound is administered to reach a concentration of at least 0.25 μg/mL where Ris butyl claim 9 , at least 0.5 μg/mL where Ris isopropyl claim 9 , or at least 1 μg/mL where Ris phenyl.11. The method of claim 1 , wherein the microbe is a bacterium.12Staphylococcus, Bacillus, Francisella, Micrococcus, Streptococcus, Neisseria, StreptomycesMycobacterium.. The method of claim 11 , wherein the bacteria is from a genus selected from the group consisting of claim 11 , and13Staphylococcus aureusStaphylococcus aureus, Francisella tularensisBacillus anthracis.. The method of claim 12 , wherein the bacteria is methicillin-susceptible or methicillin-resistant claim 12 , or14. A method for inhibiting microbial growth claim 12 , comprising contacting the microbe with an effective amount of a compound comprising an S-heterosubstituted disulfide a compound having the formula (I):{' ...

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27-12-2018 дата публикации

ANTIBACTERIAL S-HETEROSUBSTITUTED DISULFIDES

Номер: US20180369163A1
Принадлежит: University of South Florida

Synthetically-derived S,S-heterodisubstituted disulfides that exhibit potent in vitro antibacterial activity against a variety of bacteria, including , methicillin-resistant and . The present invention provides compounds, methods and compositions effective to treat microbial/bacterial infections, and, especially, infections arising from bacteria which have developed resistance to conventional antibiotics. 1. A method for treating or preventing a bacterial infection , comprising administering to a subject in need thereof an effective amount of a compound comprising an S-heterosubstituted disulfide having formula (I):{'sub': 1', '2, 'XSSX(I)'}{'sub': 1', '2', '1', '2, 'wherein each Xand Xare concurrently S—Ror N—R;'}{'sub': '1', 'wherein Ris isopropyl, butyl, s-butyl, or phenyl; and'}{'sub': '2', 'wherein Ris s-butyl.'}2. The method of claim 1 , further comprising a pharmaceutically acceptable carrier.3. The method of claim 1 , wherein Xand Xare S—R.4. The method of claim 3 , wherein Ris phenyl.5Staphylococcus aureus.. The method of claim 1 , wherein the bacteria is6Staphylococcus aureus.. The method of claim 5 , wherein the bacteria is methicillin-resistant7Francisella tularensis.. The method of claim 1 , wherein the bacteria is This application is a continuation of and claims priority to currently pending U.S. Nonprovisional application Ser. No. 15/349,475, entitled “Antibacterial S-Heterosubstituted Disulfides”, filed Nov. 11, 2016, which is a continuation of and claims priority to U.S. Nonprovisional application Ser. No. 12/765,272, entitled, “Antibacterial S-Heterosubstituted Disulfides”, filed Apr. 22, 2010, now U.S. Pat. No. 9,512,160, which is a continuation of and claims priority to International Application Number PCT/US2008/081125, entitled, “Antibacterial S-Heterosubstituted Disulfides”, filed Oct. 24, 2008, which claims priority to U.S. Provisional Patent Application No. 60/982,403 entitled, “Antibacterial S-Heterosubstituted Disulfides”, filed Oct. 24, ...

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25-09-2018 дата публикации

Antibacterial S-heterosubstituted disulfides

Номер: US0010080725B2

Synthetically-derived S,S-heterodisubstituted disulfides that exhibit potent in vitro antibacterial activity against a variety of bacteria, including Staphylococcus aureus , methicillin-resistant Staphylococcus aureus and Francisella tularensis . The present invention provides compounds, methods and compositions effective to treat microbial/bacterial infections, and, especially, infections arising from bacteria which have developed resistance to conventional antibiotics.

Подробнее
29-05-2008 дата публикации

Biocomposite for artificial tissue design

Номер: US2008124371A1
Принадлежит:

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.

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22-05-2008 дата публикации

N-THIOLATED 2-OXAZOLIDINONE -DERIVED ANTIBIOTICS

Номер: US2008119533A1
Принадлежит:

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 Staphylococcus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.

Подробнее
12-08-2010 дата публикации

ANTIBACTERIAL S-HETEROSUBSTITUTED DISULFIDES

Номер: US20100204337A1
Принадлежит: UNIVERSITY OF SOUTH FLORIDA

Synthetically-derived S,S-heterodisubstituted disulfides that exhibit potent in vitro antibacterial activity against a variety of bacteria, including Staphylococcus aureus, methicillin-resistant Staphylococcus aureus and Francisella tularensis. The present invention provides compounds, methods and compositions effective to treat microbial/bacterial infections, and, especially, infections arising from bacteria which have developed resistance to conventional antibiotics.

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03-07-2018 дата публикации

Antibiotic compositions and methods of use

Номер: US0010010545B1

Embodiments of the present disclosure provide for compositions including an antibiotic containing a N-thiolated beta-lactam moiety, pharmaceutical compositions including the antibiotic, methods of treatment of a condition (e.g., bacterial infection), methods of treatment using compositions or pharmaceutical compositions, and the like.

Подробнее
06-12-2016 дата публикации

Antibacterial S-heterosubstituted disulfides

Номер: US0009512160B2

Synthetically-derived S,S-heterodisubstituted disulfides that exhibit potent in vitro antibacterial activity against a variety of bacteria, including Staphylococcus aureus , methicillin-resistant Staphylococcus aureus and Francisella tularensis . The present invention provides compounds, methods and compositions effective to treat microbial/bacterial infections, and, especially, infections arising from bacteria which have developed resistance to conventional antibiotics.

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22-12-2009 дата публикации

Methods for preventing and treating cancer using N-thiolated beta-lactam compounds and analogs thereof

Номер: US0007635693B2

The subject invention concerns N-thiolated beta-lactam compounds of formula A, wherein R1 is a hydrocarbon group having 1-8 carbon atoms; R3 is an organothio group; and R4 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl, and 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.

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11-04-2006 дата публикации

Methods for preventing and treating cancer using N-thiolated beta-lactam compounds and analogs thereof

Номер: US0007026472B2

The subject invention concerns N-thiolated beta-lactam compounds of formula A, wherein R1 is a hydrocarbon group having 1-8 carbon atoms; R3 is an organothio group; and R4 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl, and 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.

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31-07-2008 дата публикации

N-alkylthio beta-lactams, alkyl-coenzyme a asymmetric disulfides, and aryl-alkyl disulfides as anti-bacterial agents

Номер: US2008182815A1
Принадлежит:

The present invention provides N-alkylthio beta-lactams and disulfide compounds (e.g., alkyl-coenzyme A asymmetric disulfides or aryl-alkyl disulfides), compositions containing such compounds, and method of their use as anti-bacterial agents.

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24-11-2016 дата публикации

BIOCOMPATIBLE POLYACRYLATE COMPOSITIONS AND METHODS OF USE

Номер: US20160338969A1
Принадлежит: University of South Florida

A biocompatible polymer material is described that exhibits mechanical and physical properties that are fundamental to many medical devices and treatment of many medical diseases and disorders. The material is composed of a combination of acrylate monomers polymerized via a microemulsion polymerization. Multiple applications of the polymer material are presented.

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26-03-2013 дата публикации

Heterosubstituted N-thiolated beta-lactam compounds and methods of use

Номер: US0008404671B2

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. In one embodiment, the compounds have the structure shown in formula (A) or formula (B) or formula (C): wherein the R groups are as defined in the specification. 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).

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09-06-2016 дата публикации

Menthol-based Nanoparticles for Drug Delivery

Номер: US20160158364A1
Принадлежит: University of South Florida

The subject invention pertains to formulations comprising poly(menthyl acrylate) nanoparticles comprising at least one active ingredient contained in a plurality of hydrophobic carriers and dispersed in an aqueous medium. The subject invention further pertains to methods of polymerization of drug loaded nanoparticles made up of methyl acrylate monomers in an aqueous emulsion. 1. A formulation comprising poly(menthyl acrylate) nanoparticles comprising at least one active ingredient contained in a plurality of hydrophobic carriers dispersed in an aqueous medium.2. The formulation of claim 1 , wherein the at least one active ingredient is an antibiotic.3. The formulation of claim 1 , wherein the at least one active ingredient is penicillin.4. The formulation of claim 1 , wherein the at least one active ingredient is about 1% to about 20% (w/w) of the formulation.5. The formulation of claim 1 , wherein the plurality of hydrophobic carriers are a surfactant.6. The formulation of claim 1 , wherein the plurality of hydrophobic carriers form micelles dispersed in the aqueous medium.7. The formulation of claim 1 , wherein the poly(menthyl acrylate) nanoparticles are poly(L-menthyl acrylate) nanoparticles.8. The formulation of claim 1 , wherein the poly(menthyl acrylate) nanoparticles are poly(D-menthyl acrylate) nanoparticles.9. A method of polymerization of drug loaded nanoparticles in an aqueous emulsion claim 1 , comprising:adding a plurality of methyl acrylate monomers to an aqueous medium;adding an active ingredient to the aqueous medium;adding a radical initiator for alkene polymerization of the methyl acrylate monomers in the presence of the active ingredient; andadding a surfactant to form the aqueous emulsion.10. The method of claim 9 , wherein the menthyl acrylate monomers are L-menthyl acrylate monomers.11. The method of claim 9 , wherein the menthyl acrylate monomers are D-menthyl acrylate monomers.12. The method of claim 9 , wherein the menthyl acrylate monomers ...

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06-10-2015 дата публикации

Nanoparticles for drug-delivery

Номер: US0009149440B2

This invention relates to polymeric nanoparticles useful for drug delivery with target molecules bonded to the surface of the particles and having sizes of up to 1000 nm, preferably 1 nm to 400 nm, more preferably 1 nm to 200 nm, that are dispersed homogeneously in aqueous solution. The target drug/target substance is covalently bonded to the novel 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. This invention also relates to microemulsion polymerization techniques useful for preparing the novel nanoparticles.

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21-03-2013 дата публикации

Nanoparticles with covalently bound surfactant for drug delivery

Номер: US20130071348A1
Принадлежит: UNIVERSITY OF SOUTH FLORIDA

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.

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13-06-2013 дата публикации

Antibiotic-Bound Poly(Caprolactone) Polymer

Номер: US20130150550A1
Принадлежит: UNIVERSITY OF SOUTH FLORIDA

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. This divisional application claims priority to U.S. Non-Provisional Application Ser. No. 11/746,706 filed on May 10, 2007 and U.S. Provisional Application No. 60/747,061 filed on May 11, 2006, entitled “Antibiotic-Bound Poly(Caprolactone) Polymer”.This invention was made with Government support under Grant No. RO1 A1 51351 awarded by the National Institutes of Health. The Government has certain rights in the invention.This invention relates to attaching one or more bioactive molecules to the same polymer, and also for attachment before or after polymerizationThe delivery of water-insoluble drugs to targets within the human body is a challenge that presently places strict limitations on what drugs can be applied clinically. The need for methods which overcome this is of high priority in the development of new therapeutics for treatment of human disease.The development of antibiotics for control of pathogenic bacteria has been of pressing need in this era of drug resistant infections. N-Methylthiolated b-lactams have been identified as a new family of antibacterial agents active against bacteria, including methicillin-resistant (MRSA). (See Turos, E.; Konaklieva, M. I.; Ren, R. X. F.; Shi, H.; Gonzalez, J.; Dickey, S.; Lim, D. 2000, 56, 5571; Bart Heldreth, Timothy E. Long, Seyoung Jang, Suresh K. R. Guntireddygari, Edward Turos, Sonja Dickey, Daniel V. Lim, “N-Thiolated b-Lactam Antibacterials: Effects of the N-Organothio Substituent on anti-MRSA Activity,” 14, 3775-3784 (2006); and Edward Turos, Jeung-Yeop Shim, Yang Wang, Kerriann Greenhalgh, G. Suresh Kumar Reddy, Sonja Dickey, Daniel ...

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19-09-2013 дата публикации

POLY(VINYL BENZOATE) NANOPARTICLES FOR MOLECULAR DELIVERY

Номер: US20130243832A1
Принадлежит: UNIVERSITY OF SOUTH FLORIDA

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>1000 μg/mL) and primary bovine primary aortic endothelial cells (IC>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. 1. A composition of nanoparticles comprising:at least one nanoparticle formed from poly(vinyl benzoate) and at least one surfactant;a pharmaceutically acceptable carrier; anda lipophilic molecule.2. The composition of claim 1 , wherein the surfactant is a pluronic.3. The composition of claim 2 , wherein the pluronic is Pluronic F68.4. The composition of claim 1 , wherein the at least one nanoparticle has a mean particle size of between about 50 nm and about 350 nm.5. The composition of claim 1 , wherein the at least one nanoparticle has a mean particle size of between about 200 nm and about 250 nm.6. The composition of claim 1 , wherein the size of the lipophilic molecule is up to about 5% by weight.7. The composition of claim 1 , wherein the lipophilic molecule is an antibacterial agent.8. The composition of claim 1 , wherein the lipophilic molecule is a drug.9. An in vivo molecular carrier comprising a poly(vinyl benzoate) ...

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02-01-2014 дата публикации

BIOCOMPATIBLE POLYACRYLATE COMPOSITIONS AND METHODS OF USE

Номер: US20140004204A1
Принадлежит:

A biocompatible polymer material is described that exhibits mechanical and physical properties that are fundamental to many medical devices and treatment of many medical diseases and disorders. The material is composed of a combination of acrylate monomers polymerized via a microemulsion polymerization. Multiple applications of the polymer material are presented. 113-. (canceled)14. A method of applying a composition to hard or soft tissue of a subject in need thereof , comprising applying the composition to the hard or soft tissue , wherein the composition comprises an emulsion of polymer and water , wherein the polymer comprises a copolymer of a base acrylate and a supporting monomer.15. The method of claim 14 , wherein the composition is applied to protect or cover a wound.16. The method of claim 14 , wherein the composition is applied to adhere and repair injuries to soft tissue.17. The method of claim 14 , wherein the composition is applied as a medical sealant or a medical adhesive.18. The method of claim 14 , wherein the composition is applied as a hemostatic agent.19. The method of claim 14 , wherein the composition is applied as a filler.20. The method of claim 14 , wherein the composition is applied to an absorbent material.21. The method of claim 14 , wherein the composition is applied to deliver an additive to the tissue.22. The method of claim 14 , wherein the polymer is a microemulsion polymerized nanoparticle.23. The method of claim 22 , wherein the nanoparticle comprises a copolymer of repeating units of a base acrylate monomer and a supporting monomer.24. The method of claim 23 , wherein the base acrylate is butyl acrylate claim 23 , methyl methacrylate claim 23 , methyl acrylate or ethyl acrylate claim 23 , and the supporting monomer is methyl methacrylate claim 23 , methacrylate claim 23 , styrene claim 23 , methacrylamide claim 23 , phenyl acrylate claim 23 , ethyl acrylate claim 23 , a combination of two or more of the foregoing claim 23 , or a ...

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19-11-2015 дата публикации

N-ALKYLTHIO BETA-LACTAMS, ALKYL-COENZYME A ASYMMETRIC DISULFIDES, AND ARYL-ALKYL DISULFIDES AS ANTI-BACTERIAL AGENTS

Номер: US20150327547A1
Принадлежит: UNIVERSITY OF SOUTH FLORIDA

The present invention provides N-alkylthio β-lactams and disulfide compounds (e.g., alkyl-coenzyme A asymmetric disulfides or aryl-alkyl disulfides), compositions containing such compounds, and methods of their use as anti-bacterial agents.

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30-08-2012 дата публикации

Poly(vinyl benzoate) nanoparticles for molecular delivery

Номер: WO2012068476A3
Принадлежит: UNIVERSITY OF SOUTH FLORIDA

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.

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30-04-2009 дата публикации

Polyacrylate nanoparticle drug delivery

Номер: WO2009055650A2
Принадлежит: UNIVERSITY OF SOUTH FLORIDA

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.

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04-06-2009 дата публикации

Polyacrylate nanoparticle drug delivery

Номер: WO2009055650A3

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.

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31-07-2008 дата публикации

N-alkylthio beta-lactams, alkyl-coenzyme a asymmetric disulfides, and aryl-alkyl disulfides as anti-bacterial agents

Номер: US20080182815A1
Автор: Edward Turos, Kevin Revell
Принадлежит: Individual

The present invention provides N-alkylthio β-lactams and disulfide compounds (e.g., alkyl-coenzyme A asymmetric disulfides or aryl-alkyl disulfides), compositions containing such compounds, and method of their use as anti-bacterial agents.

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30-12-2021 дата публикации

Nanoparticles carrying antibiotics

Номер: US20210401747A1
Принадлежит: UNIVERSITY OF SOUTH FLORIDA

The subject invention pertains to polyacrylate homopolymers produced from acrylolated drug monomers. The homopolymers can be produced in the form of nanoparticles. The nanoparticles comprising the homopolymers can be produced via a free radical-induced emulsion polymerization of the acrylolated drug monomers to produce an aqueous emulsion of uniformly sized nanoparticles. The homopolymers of the invention containing acrylolated antibiotic monomers can be active against Gram-positive and Gram-negative bacteria, such as Staphylococcus aureus and Escherichia coli . Accordingly, methods are provided of treating a disease, for example, an infection, by administering to a subject the homopolymers, homopolymeric nanoparticles, or emulsions containing homopolymeric nanoparticles of the invention.

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02-01-2024 дата публикации

Nanoparticles carrying antibiotics

Номер: US11857679B2
Принадлежит: UNIVERSITY OF SOUTH FLORIDA

The subject invention pertains to polyacrylate homopolymers produced from acrylolated drug monomers. The homopolymers can be produced in the form of nanoparticles. The nanoparticles comprising the homopolymers can be produced via a free radical-induced emulsion polymerization of the acrylolated drug monomers to produce an aqueous emulsion of uniformly sized nanoparticles. The homopolymers of the invention containing acrylolated antibiotic monomers can be active against Gram-positive and Gram-negative bacteria, such as Staphylococcus aureus and Escherichia coli . Accordingly, methods are provided of treating a disease, for example, an infection, by administering to a subject the homopolymers, homopolymeric nanoparticles, or emulsions containing homopolymeric nanoparticles of the invention.

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