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30results about How to "Improve membrane permeability" patented technology

Novel lactam compound

The present invention provides a lactam compound, a sugar transport enhancement agent containing this compound as an active ingredient, an agent for the prevention and / or treatment of diabetes mellitus, diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macrovascular disease, glucose tolerance anomaly, obesity and the like. In addition, the present invention also provides a preparation method for the novel lactam compound, and a preparation intermediate thereof.
Owner:AJINOMOTO CO INC

Curcumin self-microemulsion and preparation method thereof

The invention discloses a self-microemulsion, in particular to a curcumin self-microemulsion and a preparation method thereof. The curcumin self-microemulsion is characterized by the following components by weight percent: 0.05%-10% of curcumin, 1%-35% of oil phase, 20%-80% of surfactant, and 2%-40% of cosurfactant. The curcumin self-microemulsion and the preparation method thereof has the benefits that: a curcumin self-microemulsion release system increases the solubility of drugs, protects the drugs dissolved in oil drops, and improves the stability in a body; and the surfactant can change the flowability of cell membranes, improve membrane permeability of the drugs, enhance the absorption of the drugs in the body and increase the relative bioavailability of oral drugs.
Owner:SHANDONG LUNUO ANIMAL PHARMA

Methods and Compositions for Increasing Membrane Permeability

Methods and compositions for increasing membrane permeability are provided. One aspect provides protein resulting from a fusion between a membrane-active peptide and second peptide. Nucleic acids, and vectors encoding the, pore forming fusion proteins are also provided.
Owner:VIRGINIA COMMONWEALTH UNIV

1,3,4-oxadizaole structure unit-containing Rhodamine B pH fluorescence probe and applications thereof

The invention discloses a 1,3,4-oxadizaole structure unit-containing Rhodamine B pH fluorescence probe, the structure of which is shown as the formula (I) in the specification. The invention further discloses applications of the probe to monitoring the change of pH values and specifically marking lysocome in living cells. The probe does not emit fluoresce under the neutral and alkaline conditions; after the pH value is smaller than 7, the fluorescence intensity is fast enhanced along with the reduction of the pH value and can achieve the maximum value when the pH value is about 4.4; the pH sensitivity of the fluorescence detection ranges from 6.7 to 4.4, and the fluorescence intensity and the pH are in linear relation from pH 4.7 to 5.7; good capability of interference resistance to various metal ions can be achieved under acidity condition; and the probe is very suitable for monitoring the pH value under the complicated interior environment of the living cells in real time, especially specifically marking lysocome and monitoring the change of pH value in the lysocome.
Owner:SHANDONG UNIV

High permeance and high selectivity facilitated transport membranes for olefin/paraffin separations

The invention provides a high permeance and high selectivity facilitated transport membrane comprising a very small pore, nanoporous polyethersulfone (PES) / polyvinylpyrrolidone (PVP) blend support membrane, a hydrophilic polymer inside the very small nanopores on the skin layer surface of the support membrane, a thin, nonporous, hydrophilic polymer layer coated on the surface of the support membrane, and metal salts incorporated in the hydrophilic polymer layer coated on the surface of the support membrane and the hydrophilic polymer inside the very small nanopores, a method of making this membrane, and the use of this membrane for olefin / paraffin separations, particularly for propylene / propane and ethylene / ethane separations.
Owner:UOP LLC

Porous hydrophilic membranes

Porous hydrophilic membranes comprising a porous inert support on which an ionomer is deposited, said membranes being characterized in that they have an ionic conductivity and a water permeability higher than 1 l / (h.m2.Atm).
Owner:AUSIMONT SPA

Lactam compound, a method for producing the same, and a diabetic therapy by administering the same

The present invention provides a lactam compound, a sugar transport enhancement agent containing this compound as an active ingredient, an agent for the prevention and / or treatment of diabetes mellitus, diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macrovascular disease, glucose tolerance anomaly, obesity and the like. In addition, the present invention also provides a preparation method for the novel lactam compound, and a preparation intermediate thereof.
Owner:AJINOMOTO CO INC

Preparation method of polypeptide supramolecular Bcl-xL antagonist nano-drug with mitochondrial targeting property

The invention discloses a preparation method of a polypeptide supramolecular Bcl-xL antagonist nano-drug with mitochondrial targeting, and relates to the technical field of supramolecular nano-drugs. Based on peptide sequences with mitochondrial targeting and pH-responsive morphologic changes in the tumor microenvironment, a BH3 structural domain derived from pro-apoptotic protein and anti-cancer, anti-inflammatory and antibacterial drugs are connected to polypeptide through covalent bonds, and the supramolecular Bcl-xL antagonist nano-drug is obtained by co-assembling the BH3 structural domain, the anti-cancer, anti-inflammatory and antibacterial drugs and the polypeptide according to different component proportions. The polypeptide supramolecular Bcl-xL antagonist nano-drug disclosed by the invention has the advantages that the polypeptide supramolecular Bcl-xL antagonist nano-drug has excellent mitochondrial targeting property and tumor microenvironment pH responsive morphology transformation, and has good tumor targeting enrichment capacity and excellent anti-tumor treatment effect. The preparation method is simple, easy for industrial production and wide in application field range.
Owner:NANKAI UNIV

Methods and compositions for increasing membrane permeability

Methods and compositions for increasing membrane permeability are provided. One aspect provides protein resulting from a fusion between a membrane-active peptide and second peptide. Nucleic acids and vectors encoding the pore forming fusion proteins are also provided.
Owner:GEORGIA TECH RES CORP +1

Compound having detrusor muscle-contracting activity and urethral sphincter muscle-relaxing activity

ActiveUS8410281B2Reduced dysfunctionPreventing and/or treating underactive bladderBiocideOrganic active ingredientsSide effectDetrusor muscle
Since a compound represented by formula (I) wherein all of the symbols are the same as defined in the specification, a salt thereof, a solvate thereof, a prodrug thereof, a mixture with a diastereomer thereof in an arbitrary ratio, or a cyclodextrin clathrate thereof have a contracting activity of bladder detrusor and a relaxing activity of urethral sphincter, they can ameliorate bladder contraction dysfunction and / or urethral relaxation dysfunction, and for example, are effective for underactive bladder. Additionally, the compound of the present invention has little risk of side effects on the urinary system, the circulatory system and the digestive system, and exhibits excellent pharmacokinetics, such as oral absorbability etc. Therefore, the compound of the present invention is useful as a superior agent for preventing, treating and / or ameliorating underactive bladder.
Owner:ONO PHARMA CO LTD

Naphthalene-based two-photon fluorescent probes, preparation method and use thereof

ActiveUS20150079625A1Low fluorescence backgroundStrong and specific fluorescent signalMicrobiological testing/measurementNaphthalimide/phthalimide dyesSolubilityTwo-photon absorption
The present invention provides a novel category of naphthalene-based two-photon fluorescent probes having a general formula I, wherein: X is selected from the X1, X2, X3 and X4; The mentioned two-photon fluorescent probes have a low fluorescence background in the non-tumor cells and tissues, and have a strong and specific fluorescent signal in the tumor cells and tissues. These probes have a certain level of water-solubility, while having good membrane permeability. In addition, they have a bigger effective two-photon absorption cross section. The compounds of the present invention also have a lower biotoxicity, phototoxicity and photobleaching. There is sufficient difference between the spectral range thereof and that of a biological sample.
Owner:DALIAN UNIV OF TECH +1

Curcumin self-microemulsion and preparation method thereof

The invention discloses a self-microemulsion, in particular to a curcumin self-microemulsion and a preparation method thereof. The curcumin self-microemulsion is characterized by the following components by weight percent: 0.05%-10% of curcumin, 1%-35% of oil phase, 20%-80% of surfactant, and 2%-40% of cosurfactant. The curcumin self-microemulsion and the preparation method thereof has the benefits that: a curcumin self-microemulsion release system increases the solubility of drugs, protects the drugs dissolved in oil drops, and improves the stability in a body; and the surfactant can change the flowability of cell membranes, improve membrane permeability of the drugs, enhance the absorption of the drugs in the body and increase the relative bioavailability of oral drugs.
Owner:SHANDONG LUNUO ANIMAL PHARMA

Method of producing nylon

There is provided a method of producing aminohexanoic acid and / or aminohexanoic acid ester from synthesis gas, the method comprising:A. contacting the synthesis gas with at least one bacteria capable of carrying out the Wood-Ljungdahl pathway and the ethanol-carboxylate fermentation to produce hexanoic acid; andB. contacting the hexanoic acid with a genetically modified cell to produce aminohexanoic acid and / or aminohexanoic acid ester, wherein the genetically modified cell has an increased activity, in comparison with its wild type, of alkane monooxygenase, alcohol dehydrogenase, and ω-transaminase.
Owner:EVONIK OPERATIONS GMBH

Fermentation culture method for producing schizophyllan from schizophyllum commune

The invention belongs to the field of production of high-added-value products by microorganisms, and particularly relates to a fermentation culture method for producing schizophyllan from schizophyllum commune. The method comprises the following steps of: performing deep liquid culture on schizophyllum commune by using a basic culture medium, and then adding cyclopentanone fatty acid to continue culture. The fermentation culture medium and the cyclopentanone fatty acid additive provided by the invention can shorten the fermentation period of schizophyllum commune hyphae, and greatly improve the content of high-added-value products produced by unit mycelium.
Owner:WUZHOUFENG AGRI SCI & TECH

High permeance and high selectivity facilitated transport membranes for olefin/paraffin separations

The invention provides a high permeance and high selectivity facilitated transport membrane comprising a very small pore, nanoporous polyethersulfone (PES) / polyvinylpyrrolidone (PVP) blend support membrane, a hydrophilic polymer inside the very small nanopores on the skin layer surface of the support membrane, a thin, nonporous, hydrophilic polymer layer coated on the surface of the support membrane, and metal salts incorporated in the hydrophilic polymer layer coated on the surface of the support membrane and the hydrophilic polymer inside the very small nanopores, a method of making this membrane, and the use of this membrane for olefin / paraffin separations, particularly for propylene / propane and ethylene / ethane separations.
Owner:UOP LLC

(z)-β-trifluoromethyl dehydrotryptophan compound and its synthesis method and application

The invention belongs to the field of organic synthesis and relates to ( Z )- β ‑Trifluoromethyldehydrotryptophan compounds, especially (Z)‑β ‑Trifluoromethyl dehydrotryptophan compound and its synthesis method and application. Weigh 3-trifluoroacetylindole compounds, isocyanate compounds, catalysts and solvents in proportion, stir and react at 20-40°C for 15-60 hours, after the reaction is completed, obtain ( Z )- β ‑Trifluoromethyl dehydrotryptophans. The present invention uses 3-trifluoroacetyl indole as a trifluoromethyl source, and through the reaction with isocyanate, it is simple and efficient to construct ( Z )- β ‑Trifluoromethyl dehydrotryptophans. The introduction of trifluoromethyl groups can effectively improve the membrane permeability of cyclic active peptides containing dehydrotryptophan, increase the oil-water separation coefficient, enhance lipophilicity and metabolic stability, and improve the cyclic activity of dehydrotryptophan-containing peptides. Biological activity of active peptides.
Owner:SHANGQIU NORMAL UNIVERSITY

1,3,4-oxadizaole structure unit-containing rhodamine b ph fluorescence probe and applications thereof

The invention discloses a 1,3,4-oxadizaole structure unit-containing Rhodamine B pH fluorescence probe, the structure of which is shown as the formula (I) in the specification. The invention further discloses applications of the probe to monitoring the change of pH values and specifically marking lysocome in living cells. The probe does not emit fluoresce under the neutral and alkaline conditions; after the pH value is smaller than 7, the fluorescence intensity is fast enhanced along with the reduction of the pH value and can achieve the maximum value when the pH value is about 4.4; the pH sensitivity of the fluorescence detection ranges from 6.7 to 4.4, and the fluorescence intensity and the pH are in linear relation from pH 4.7 to 5.7; good capability of interference resistance to various metal ions can be achieved under acidity condition; and the probe is very suitable for monitoring the pH value under the complicated interior environment of the living cells in real time, especially specifically marking lysocome and monitoring the change of pH value in the lysocome.
Owner:SHANDONG UNIV

Taxanes Compounds, Preparation Method Therefor, and Uses Thereof

The present invention provides taxanes compounds with a formula (I) or formula (II) structure, a method for preparing the compounds, as well as the use of the compositions containing the compounds, pharmaceutically acceptable salts and solvates thereof as active ingredients in manufacturing oral antitumor medicaments,In formula (I), R1 is —COR6, —COOR6 or —CONR7aR7b; R2 is a C1-C6 alkyl, a C1-C6 alkenyl, a substituted hydrocarbon group, a heterocyclic group, an aromatic group or a substituted aromatic group; R3 is —OR6, —OCOOR6, —OCOSR6 or —OCONR7aR7b; R4 is —OR6, —OCOOR6, —OCOSR6, —OCONR7aR7b or H; wherein, R6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group; R7a and R7b are respectively hydrogen, a hydrocarbon group, a substituted hydrocarbon group or a heterocyclic group. In formula (II), R1 is —COR6 or —COOR6; R2 is an aromatic group; R3 is —OR6; wherein, R6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group.
Owner:JIANGSU TASLY DIYI PHARMA CO LTD

Taxanes compounds, preparation method therefor, and uses thereof

The present invention provides taxanes compounds with a formula (I) or formula (II) structure, a method for preparing the compounds, as well as the use of the compositions containing the compounds, pharmaceutically acceptable salts and solvates thereof as active ingredients in manufacturing oral antitumor medicaments,In formula (I), R1 is —COR6, —COOR6 or —CONR7aR7b; R2 is a C1-C6 alkyl, a C1-C6 alkenyl, a substituted hydrocarbon group, a heterocyclic group, an aromatic group or a substituted aromatic group; R3 is —OR6, —OCOOR6, —OCOSR6 or —OCONR7aR7b; R4 is —OR6, —OCOOR6, —OCOSR6, —OCONR7aR7b or H; wherein, R6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group; R7a and R7b are respectively hydrogen, a hydrocarbon group, a substituted hydrocarbon group or a heterocyclic group. In formula (II), R1 is —COR6 or —COOR6; R2 is an aromatic group; R3 is —OR6; wherein, R6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group.
Owner:JIANGSU TASLY DIYI PHARMA CO LTD

A kind of tetrazolium substituted quinolinone derivative and its preparation method and application

A tetrazole-substituted quinolinone derivative and a preparation method and application thereof belong to the technical field of organic compound preparation. Its structure is the compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein, R 1 is tetrazolium; R 2 is a hydrogen atom or a halogen atom; R 3 is a hydrogen atom, a halogen atom, a nitro group or a trifluoromethyl group. The product of the invention is a high-efficiency aldose reductase inhibitor with excellent membrane permeability, which can improve the availability of the inhibitor in vivo, thereby achieving the effect of treating diabetic complications.
Owner:YANCHENG LIMIN CHEM

Medicinal application of collagen protein peptide, cucurbitacin oral micelle, and preparation method thereof

The invention belongs to the technical field of medicines and especially relates to a medicinal application of collagen protein peptide, a cucurbitacin oral micelle, and a preparation method thereof.The application is that the collagen protein peptide is used as a medicine transmembrane tool in preparation of the oral medicine preparation, wherein the collagen protein peptide carries positive charges. The invention provides the cucurbitacin oral micelle containing the collagen protein peptide, which comprises, by weight, 8-15 parts of cucurbitacin, 30-70 parts of lecithin, 50-75 parts of octanoic decanoic polyethylene glycol glyceride, 25-50 parts of polyethylene glycol 15-hydroxystearate and 80-100 parts of the collagen protein peptide carrying the positive charges. The collagen proteinpeptide, cooperated with other carrier materials, can improve membrane-permeability of the medicine and reduce excretion of the medicine, so that the collagen protein peptide can be used as the medicine transmembrane tool. For solving problems about oral bioavailability of the cucurbitacin, the invention provides the technology of collagen protein peptide coating nano-micelle, wherein by means ofthe characters of the collagen protein peptide, the problem of low bioavailability of medicines, such as the cucurbitacin, is solved.
Owner:ZHEJIANG UNIV OF TECH

(Z)-beta-trifluoromethyl dehydrotryptophan compound and synthesis method and application thereof

The invention belongs to the field of organic synthesis, and relates to a (Z)-beta-trifluoromethyl dehydrotryptophan compound, in particular to a (Z)-beta-trifluoromethyl dehydrotryptophan compound and a synthesis method and application thereof. The synthesis method comprises the following steps of: weighing a 3-trifluoroacetyl indole compound, an isocyanate compound, a catalyst and a solvent according to a certain ratio, stirring and reacting for 15-60 h at a temperature of 20-40 DEG C, and after the reaction is finished, carrying out pressure reduction and separation to obtain the (Z)-beta-trifluoromethyl dehydrotryptophan compound. According to the synthesis method disclosed by the invention, the (Z)-beta-trifluoromethyl dehydrotryptophan compound is simply, conveniently and efficientlyconstructed by taking 3-trifluoroacetyl indole as a trifluoromethyl source and carrying out a reaction between the trifluoromethyl source and isocyanate. Due to the introduction of trifluoromethyl, the membrane permeation function of the dehydrotryptophan-containing cyclic active peptide is effectively improved, the oil-water separation coefficient is increased, the lipophilicity and metabolic stability are enhanced, and the biological activity of the dehydrotryptophan-containing cyclic active peptide is improved.
Owner:SHANGQIU NORMAL UNIVERSITY

A fluorescent carbon dot for nuclear staining and its application and method in nuclear imaging

ActiveCN109021971BLow membrane permeabilityVery good membrane permeability at low dosesNanoopticsNano-carbonGreen-lightSilica gel
A fluorescent carbon dot for cell nucleus staining. The carbon dot is prepared by the following steps: 1) dissolving folic acid and m-phenylenediamine in water and heating for reaction; 2) after the reaction, centrifugation, and silica gel column chromatography to collect yellow The green fluorescent part was evaporated, transferred to water, and freeze-dried. The carbon dots prepared by the invention emit green light under ultraviolet excitation, have a large Stokes shift, and the optimal excitation position is consistent with the existing commercial 405 laser, and can be well applied to laser confocal microscopy.
Owner:ZHENGZHOU UNIV

Naphthalene-based two-photon fluorescent probes, preparation method and use thereof

ActiveUS9182350B2Low fluorescence backgroundStrong and specific fluorescent signalOrganic chemistryNaphthalimide/phthalimide dyesSolubilityTwo-photon absorption
The present invention provides a novel category of naphthalene-based two-photon fluorescent probes having a general formula I, wherein: X is selected from the X1, X2, X3 and X4; The mentioned two-photon fluorescent probes have a low fluorescence background in the non-tumor cells and tissues, and have a strong and specific fluorescent signal in the tumor cells and tissues. These probes have a certain level of water-solubility, while having good membrane permeability. In addition, they have a bigger effective two-photon absorption cross section. The compounds of the present invention also have a lower biotoxicity, phototoxicity and photobleaching. There is sufficient difference between the spectral range thereof and that of a biological sample.
Owner:DALIAN UNIV OF TECH +1

Pharmaceutical application of collagen peptide, cucurbitacin oral micelles and preparation method thereof

The invention belongs to the technical field of medicines and especially relates to a medicinal application of collagen protein peptide, a cucurbitacin oral micelle, and a preparation method thereof.The application is that the collagen protein peptide is used as a medicine transmembrane tool in preparation of the oral medicine preparation, wherein the collagen protein peptide carries positive charges. The invention provides the cucurbitacin oral micelle containing the collagen protein peptide, which comprises, by weight, 8-15 parts of cucurbitacin, 30-70 parts of lecithin, 50-75 parts of octanoic decanoic polyethylene glycol glyceride, 25-50 parts of polyethylene glycol 15-hydroxystearate and 80-100 parts of the collagen protein peptide carrying the positive charges. The collagen proteinpeptide, cooperated with other carrier materials, can improve membrane-permeability of the medicine and reduce excretion of the medicine, so that the collagen protein peptide can be used as the medicine transmembrane tool. For solving problems about oral bioavailability of the cucurbitacin, the invention provides the technology of collagen protein peptide coating nano-micelle, wherein by means ofthe characters of the collagen protein peptide, the problem of low bioavailability of medicines, such as the cucurbitacin, is solved.
Owner:ZHEJIANG UNIV OF TECH

Process for preparing low-free-alkali sodium methoxide methanol solution based on alkaline method

The invention discloses a process for preparing a low-free-alkali sodium methoxide methanol solution based on an alkali method, and relates to the technical field of chemical synthesis; the process comprises the following steps: S1, adding solid sodium hydroxide into an alkali dissolving tank containing methanol in proportion, performing standing precipitation, then conveying clear liquor to an alkali liquor inlet at the upper part of a reaction stripping tower through a pump to enter a reaction tower, and after the reaction, discharging mixed steam from the top of the tower, and forming a product at the bottom of the tower; s2, heating the mixed steam discharged in the step S1 and feeding the steam into a rectification section to separate the methanol and water in the mixed steam through a steam permeable membrane; s3, obtaining a sodium methoxide-methanol solution at the tower bottom. According to the process method provided by the invention, the content of free alkali in the prepared sodium methoxide methanol solution is low; water generated in the reaction is separated and removed through an evaporation permeable membrane, so that the production efficiency of sodium methoxide is improved; methanol separated and recycled from mixed steam can continue to react, so that the utilization rate of raw materials is increased, and the cost is reduced.
Owner:NINGBO ZHETIE JIANGNING CHEM
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