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43results about How to "Enhance amphipathic" patented technology

Methods for delivery therapeutic compounds across the blood-brain barrier

The present invention relates to amphiphilic drug-oligomer conjugates capable of traversing the blood-brain barrier ("BBB") and to methods of making and using such conjugates. An amphiphilic drug-oligomer conjugates comprise a therapeutic compound conjugated to an oligomer, wherein the oligomer comprises a lipophilic moiety coupled to a hydrophilic moiety. The conjugates of the invention further comprise therapeutic agents such as proteins, peptides, nucleosides, nucleotides, antiviral agents, antineoplastic agents, antibiotics, etc., and prodrugs, precursors, derivatives and intermediates thereof, chemically coupled to amphiphilic oligomers.
Owner:BIOCON LTD

Methods of altering the binding affinity of a peptide to its receptor

The present invention relates to amphiphilic drug-oligomer conjugates capable of traversing the blood-brain barrier ("BBB") and to methods of making and using such conjugates. An amphiphilic drug-oligomer conjugate comprises a therapeutic compound conjugated to an oligomer, wherein the oligomer comprises a lipophilic moiety coupled to a hydrophilic moiety. The conjugates of the invention further comprise therapeutic agents such as proteins, peptides, nucleosides, nucleotides, antiviral agents, antineoplastic agents, antibiotics, etc., and prodrugs, precursors, derivatives and intermediates thereof, chemically coupled to amphiphilic oligomers.
Owner:BIOCON LTD

Natriuretic compounds, conjugates, and uses thereof

Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, enteral, subcutaneous, pulmonary, and intravenous forms of the compounds and conjugates may be prepared as treatments and / or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the natriuretic compound are also disclosed, having an amino acid sequence that is other than the native sequence.
Owner:BIOCON LTD

Natriuretic compounds, conjugates, and uses thereof

Modified n atriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, subcutaneous, and intravenous forms of the compounds and conjugates may be prepared as treatments and / or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the n atriuretic compound are also disclosed, having an amino acid sequence that is other than the native sequence.
Owner:BIOCON LTD

Natriuretic compounds, conjugates, and uses thereof

Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, subcutaneous, and intravenous forms of the compounds and conjugates may be prepared as treatments and / or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the natriuretic compound are also disclosed, having an amino acid sequence that is other than the native sequence.
Owner:BIOCON LTD

Preparation method of chiral nanometer copper oxide with optical activity

The invention discloses a preparation method of chiral nanometer copper oxide with optical activity. The preparation method comprises the following steps of: (1) dissolving an achiral anionic surface-active agent and a chiral small molecule into water at room temperature to obtain an achiral anionic surface-active agent and chiral small molecule water solution; (2) adding inorganic copper salt to the achiral anionic surface-active agent and chiral small molecule water solution, and stirring to react for 10-60 minutes; (3) adding alkali to reaction liquid obtained from the step (2), then increasing temperature to 100-200 DEG C, and reacting for 30 minutes-6 hours; (4) after the reaction is finished, centrifugalizing or filtering the reaction liquid obtained from the step (3), and washing and drying to obtain the chiral nanometer copper oxide with the optical activity. The prepared chiral nanometer copper oxide with the optical activity shows very uniform flower-shaped appearance and shows outstanding optical activity by having chirality.
Owner:SHANGHAI JIAO TONG UNIV

Polymer viscosity reducer for thickened oil and preparation method thereof

The invention relates to a polymer viscosity reducer for thickened oil. The polymer viscosity reducer is a hydrophobically modified polyacrylamide and has a structural formula shown as formula (I), wherein n represents the total number of polyacrylamide monomers, ranges from 60,000 to 100,000, preferably from 7,000 to 85,000; x represents the number of acrylic monomers, ranges from 10,000 to 40,000, preferably 20,000 to 350,000; m represents the number of hydrophobic monomers, and ranges from 4000 to 10000, preferably from 6000 to 8000. The invention also relates to a preparation method and application of the polymer viscosity reducer for thickened oil.
Owner:CHINA PETROLEUM & CHEM CORP +1

Bna Conjugates and Methods of Use

Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, decreasing arterial blood pressure and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, enteral, subcutaneous, pulmonary, and intravenous forms of the compounds and conjugates may be prepared as treatments and / or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the hBNP compound are also disclosed, having an amino acid sequence that is other than the native sequence.
Owner:JAMES KENNETH D

Antifungal agents and uses thereof

The invention features echinocandin class compounds. The compounds can be useful for the treatment of fungal infections.
Owner:CIDARA THERAPEUTICS

Antimicrobial agents

The application relates to antimicrobial agents against Gram-negative bacteria, in particular to fusion proteins composed of an enzyme having the activity of degrading the cell wall of Gram-negative bacteria and a peptide stretch fused to the enzyme at the N- or C-terminus, as well as pharmaceutical compositions comprising the same. Moreover, it relates to nucleic acid molecules encoding such a fusion protein, vectors comprising said nucleic acid molecules and host cells comprising either said nucleic acid molecules or said vectors. In addition, it relates to such a fusion protein for use as a medicament, in particular for the treatment or prevention of Gram-negative bacterial infections, as diagnostic means or as cosmetic substance. The application also relates to the treatment or prevention of Gram-negative bacterial contamination of foodstuff, of food processing equipment, of food processing plants, of surfaces coming into contact with foodstuff, of medical devices, of surfaces in hospitals and surgeries.
Owner:LYSANDO +1

Micromolecular heavy oil viscosity reduction polymer and preparation method thereof

The invention discloses a micromolecular thick oil viscosity reduction polymer and a preparation method thereof. The micromolecular thick oil viscosity reduction polymer comprises the following raw material components: 10 wt.% to 20 wt.% of an acrylamide (AM) monomer, 1 wt.% to 10 wt.% of a sodium acrylate monomer, 1 wt.% to 3 wt.% of a hydrophobic monomer, 1 wt.% to 3 wt.% of a temperature-resistant monomer, 0.5 wt.% to 2.5 wt.% of a surface active monomer, 0.7 wt.% to 2.5 wt.% of a chain transfer agent, 0.08 wt.% to 2 wt.% of an initiator and the balance being water. The micromolecular thick / oil viscosity reduction polymer has quick dissolving performance and good injection performance, can emulsify thick oil, has oil displacement and profile control performance at the same time, and canbe suitable for thick oil recovery of offshore oil reservoirs and low-permeability oil reservoirs.
Owner:CHINA UNIV OF PETROLEUM (EAST CHINA) +1

Double-targeted phthalocyanine anti-cancer photosensitizer and preparation method thereof

The invention discloses a double-targeted phthalocyanine anti-cancer photosensitizer and a preparation method thereof. Micromolecular target drugs N-(3-chloro-4-fluorophenyl)-7-methoxyl-6-(3-morpholine-4-propoxy) quinazoline-4-amine connected via alcoxyl long chains are introduced on a phthalocyanine parent ring in the axial direction to improve the amphipathy, biocompatibility and the targeting property of the photosensitizer; and a triphenylphosphine group is introduced at the other end of the phthalocyanine parent ring in the axial direction, thus, the photosensitizer can be selectively, accurately and intelligently positioned on mitochondria of tumor cells with overexpressed epidermal growth factor receptors (EGFR), and the photodynamic action efficiency is improved. The compound is single in structure and determined in composition, and does not have isomers, products are easy to separate and purify, meanwhile, the complexes are not easy to gather, and the cell uptake rate is increased favorably.
Owner:FUZHOU UNIV

Piperazine-modified phthalocyanine complex and preparation method thereof

The invention discloses a piperazine-modified phthalocyanine complex as well as a preparation method and an application thereof. Piperazine molecules are introduced into the macrocyclic periphery of a metal phthalocyanine so as to enhance the amphipathy, the biocompatibility and the targeting of the phthalocyanine. A piperazine group contains two N atoms, so that after the synthesized phthalocyanine complex enters a tissue, if the tissue is normal, the single excitation state of the phthalocyanine can be quenched by lone pair electrons on the N atoms of the piperazine group under a light irradiation condition. Thus, the generation of singlet oxygen is avoided. If the tumor tissue is in a weak acid state, the N atoms are protonated, so that the single excitation state of the phthalocyanine cannot be quenched. Therefore, the singlet oxygen is generated so as to kill tumor cells. Based on the theory, the selectivity of the photodynamic therapy of the phthalocyanine is improved due to the introduction of the piperazine group, so that the damage of the phthalocyanine to the normal tissue is reduced. The piperazine-modified phthalocyanine complex has a single structure and does not contain isomers, and is easy to purify and low in cost, thereby being favorable for industrial production.
Owner:FUZHOU UNIV

Poloxamer-adriamycin conjugate with anti-tumor effect and preparation method thereof

The invention discloses a poloxamer-adriamycin conjugate with an anti-tumor effect and a preparation method thereof. The poloxamer-adriamycin conjugate has micelle property, is a high-molecular polymer which contains terminal carboxyl group and is prepared by reaction between poloxamer and succinic anhydride, and the terminal carboxyl group in the polymer and primary amino radical in adriamycin are directly bound in an amido link way. Compared with an adriamycin raw material drug, the poloxamer-adriamycin conjugate has the following advantages: the anti-tumor activity of the covalent bonding adriamycin in the poloxamer-adriamycin conjugate is maintained, the drug resistance of tumor is reduced; the poloxamer-adriamycin conjugate has the property of self-assembly formed micelle, and the critical micelle concentration of the conjugate is lower than that of polyxamer; and the micelle of the poloxamer-adriamycin conjugate can be entrapped with other medicaments with the anti-tumor effect in a physical entrapping mode, so that the aim of combined treatment of anti-tumor medicaments can be achieved.
Owner:WENZHOU MEDICAL UNIV

Feed additive for improving growth performance of nursery pig, and preparation and application thereof

The invention discloses a feed additive for improving the growth performance of a nursery pig. The invention discloses a preparation method of the feed additive for improving the growth performance ofthe nursery pig, wherein the preparation method comprises the following steps: mixing Fuzhuan tea, jujube, star anise and raw ginger, crushing, adjusting the water content, adding a compound enzyme preparation, mixing evenly, carrying out enzymatic hydrolysis, and filtering to obtain a first material and an enzymatic hydrolysate; adding the first material into absolute ethyl alcohol, soaking, andcarrying out ultrasonic assisted reflux extraction to obtain an extract liquid and a filter residue; adding the filter residue to water, soaking, cooking and filtering to obtain a filtrate; mixing the enzymatic hydrolysate, the extract liquid and the filtrate, and drying at low temperature to obtain a second material; adding the second material, excipients and a cladding wall material into water,mixing evenly and spray-drying to obtain the feed additive for improving the growth performance of the nursery pig. The invention discloses an application of the feed additive for improving the growth performance of the nursery pig.
Owner:ANHUI AGRICULTURAL UNIVERSITY

Heparin nano-drug loading system for loading amino anti-tumor drug and preparation method of heparin nano-drug loading system

ActiveCN112121174AAvoid metabolic toxicityOvercoming the problem of poor biocompatibilityOrganic active ingredientsPharmaceutical non-active ingredientsNanoparticleDrug carrier
The invention discloses a heparin nano-drug loading system for loading an amido anti-tumor drug. The drug loading system is a conjugate for loading the amido anti-tumor drug on PEGylated heparin molecules. Natural polysaccharide heparin which is biodegradable, good in compatibility and high in availability is used as a drug carrier, and PEG modification and the amino anti-tumor drug are combined,so that nanoparticles show an anti-tumor treatment index and biological safety which are remarkably enhanced compared with those of a free drug in in-vivo treatment.
Owner:NANJING KING FRIEND BIOCHEM PHARMA CO LTD +1

PEGylated heparin nano-micelle for loading carboxylic acid anti-tumor drug and preparation method of PEGylated heparin nano-micelle

ActiveCN112121177AAvoid metabolic toxicityOvercoming the problem of poor biocompatibilityOrganic active ingredientsPharmaceutical non-active ingredientsCarboxylic acidAnti neoplastic
The invention discloses a PEGylated heparin nano-micelle for loading a carboxylic acid anti-tumor drug. A drug loading system is a conjugate for loading the carboxylic acid anti-tumor drug on PEGylated heparin molecules. Natural polysaccharide heparin which is biodegradable, good in compatibility and high in availability serves as a drug carrier, and PEG modification and the carboxylic acid anti-tumor drug are combined, so that nanoparticles show an anti-tumor treatment index and biological safety which are remarkably enhanced compared with those of a free drug in in-vivo treatment.
Owner:KINDOS PHARM CO LTD +1

Adamantane-containing quaternary ammonium salt ionic liquid and preparation method thereof

InactiveCN109879765AEnhance amphipathicWill not affect the subject-guest combinationOrganic compound preparationTransportation and packagingQuaternary ammonium cation1-adamantanecarbonyl chloride
The invention relates to an adamantane-containing quaternary ammonium salt ionic liquid and a preparation method thereof. The structural formula of the adamantane-containing quaternary ammonium salt ionic liquid designed and prepared by the invention is shown in the specification, and in the formula, n is equal to 6, 9 or 11. According to the adamantane-containing quaternary ammonium salt ionic liquid disclosed by the invention, 1-adamantanecarboxylic acid is used as a raw material, and the ionic liquid is prepared by the following three steps: firstly, carrying out acylating chlorination reaction on 1-adamantanecarboxylic acid and thionyl chloride to synthesize 1-adamantanecarbonyl chloride, carrying out esterification reaction on the 1-adamantanecarbonyl chloride and OH(CH2)nBr, and thencarrying out quaternization with N,N-dimethylbenzylamine to form the adamantane-containing quaternary ammonium salt ionic liquid. The adamantane-containing quaternary ammonium salt ionic liquid obtained in the invention has the characteristics of mild reaction conditions, easily available raw materials and high product purity, and has potential application prospects in the fields of supramolecular chemistry, catalysis, batteries, nano materials and the like.
Owner:HEZHOU UNIV

Amphiphilic cyclic phosphazene trimer, pharmaceutical formulation of hydrophobic drugs by micelle-encapsulation using the amphiphilic cyclic phosphazene trimer, and preparation methods thereof

The present invention relates to an amphiphilic cyclic phosphazene trimer which is biocompatible and a method for preparing the same. The present invention also relates to pharmaceutical formulations of hydrophobic drugs that are micelle-encapsulated by the amphiphilic cyclic phosphazene trimer and a method for preparing the same.
Owner:CNPHARM

Paclitaxel lipid nanoparticle preparation method

The invention belongs to the technical field of medicines, particularly relates to a paclitaxel lipid nanoparticle preparation method and provides a method for preparing paclitaxel lipid nanoparticles easy for intestinal mucosae to absorb. The method includes the steps: (1) preparing paclitaxel solid lipid nanoparticle according to a film dispersion method; (2) preparing SA-R8-PTX-SLN according to an incubation method, to be more specific, precisely weighing 10mg of SA-R8, adding into 5ml of PTX-SLN dispersion liquid, magnetically stirring, staying overnight at a temperature of 4 DEG C to obtain the SA-R8-PTX-SLN; (3) precisely weighing 10mg of paclitaxel, putting into a 100ml volumetric flask, dissolving in methyl alcohol to a certain volume, and well shaking to obtain a PTX methanol stock solution with the density being 100 microgram / ml; (4) putting 1ml of SLN containing paclitaxel in a dialysis bag (14000 in molecular weight), tightening two ends of the dialysis bag, respectively adding 100ml of dissolution media, observing paclitaxel release conditions under the conditions of 37 DEG C and 100r / min, taking 1ml of dialysis media, lyophilizing, adding 0.25ml of methanol, whirling, centrifuging at a high speed, and taking supernatant for sampling by 20 microlitres.
Owner:孙仁

DOX-P micelle with anti-tumor drug resistance and preparation method thereof

The invention discloses poloxamer-adriamycin conjugate (DOX-P) micelle with anti-tumor drug resistance and a preparation method of the DOX-P micelle. The synthetic process of the DOX-P comprises the steps of firstly, reacting poloxamer with succinic anhydride to obtain high-molecular polymer of which the tail end contains carboxyl; and then, directly bonding the carboxyl at the tail end of the polymer with primaquine group in the adriamycin in an amido bond mode. The DOX-P has the capability of forming the micelle; and compared with the adriamycin bulk drug, the adriamycin subjected to covalent binding in the DOX-P micelle has the advantages that the anti-tumor activity of the adriamycin is maintained, the drug resistance of the tumor is overcome, and the stability of the adriamycin is better than that of poloxamer micelle.
Owner:吴燕

Dihydroartemisinin higher fatty acid ester and preparation method thereof

The invention discloses a dihydroartemisinin higher fatty acid ester and a preparation method thereof. The method adopts lipase as a catalyst, carries out a structure modification on the 10th position carbon of dihydroartemisinin, and then subjecting the hydroxyl group on the 10th carbon of dihydroartemisinin to carry out an esterification reaction with higher fatty acid ester. Specifically, the preparation method takes lipase Novozyme 435 as the catalyst, stearic acid and lauric acid as the acyl group donors, tertiary butanol as the reaction solvent, and 4A molecular sieve as the water absorbing agent during the esterification reaction. The prepared artemisinin esterification product has an oil and water amphiphilicity, and shows a good specificity in the in-vitro antimicrobial tests. The dihydroartemisinin higher fatty acid ester and the preparation method thereof have an important meaning on improving artemisinin solubility in water and oil so as to make artemisinin into a proper dosage form.
Owner:中科蓝海测试(天津)科技有限公司

A kind of amphiphilic fluorescent conjugated polymer, preparation method and application

The invention relates to an amphiphilic fluorescent conjugated polymer, a preparation method and an application. The present invention adopts Sonogashira coupling and ester group hydrolysis reaction to obtain an amphiphilic conjugated macromolecule that contains both hydrophilic carboxylate groups and hydrophobic alkoxy side groups in a repeating unit, and dissolves it in In a mixed solvent with a volume ratio of tetrahydrofuran and water of 1:1, it is used for rapid sensing and detection of neomycin in water. The use of this amphiphilic fluorescent conjugated polymer can realize the specific detection of neomycin, and has a fluorescent color change that can be recognized by the naked eye, and the result can be obtained without the use of a large-scale instrument, and the operation is convenient. Realize more convenient, fast and efficient detection in practical application.
Owner:SUZHOU UNIV

Porphyrin-modified cell-penetrating peptide and preparation and application thereof

InactiveCN110922451AExtend the length of stayLong body retentionPolypeptide with localisation/targeting motifEnergy modified materialsCarboxyl radicalPorphyrin
The invention discloses porphyrin-modified cell-penetrating peptide and preparation and application thereof, and belongs to the technical field of design and synthesis of antitumor drugs. Carboxyl ofpyromagnesium chlorophyll a is utilized and is linked to cell-penetrating peptide with exposed amino through amidation. The pyromagnesium chlorophyll a which is a porphyrin derivative and has similarproperty to hemoporphyrin can be embedded into a cavity of human serum albumin, so that the in-vivo circulation time of polypeptide is prolonged. In combination with the photodynamic effect of porphyrin, the peptide has a more efficient killing effect on tumors. The compound is simple in synthetic method, easily available in raw materials, low in cost, less in side reaction, high in yield, easy topurify and beneficial to industrial production.
Owner:FUZHOU UNIV

High-gloss water-based paint and preparation method thereof

InactiveCN112175428AConvenient amountImprove hardening too fastCoatingsComposite materialAntifoam agent
The invention provides high-gloss water-based paint and a preparation method thereof.The water-based paint is prepared from modified ethyl acrylate, a filler, a modified dispersing agent, an antifoaming agent, a thickener, a leveling agent, a wetting agent, a modified curing agent and water, and the preparation method comprises the steps that mixing the modified dispersing agent, the modified ethyl acrylate and the water to prepare a first mixed solution; and adding the filler, the antifoaming agent, the thickener, the leveling agent and the wetting agent into the first mixed solution to prepare a second mixed solution, adding the modified curing agent into the second mixed solution, and uniformly stirring to obtain the high-gloss water-based paint. According to the invention, the phenomenon that prickly heat easily occurs on the surface of a paint film of conventional water-based paint is overcome, and meanwhile, the improved water-based paint still has good surface performance and has good application prospect.
Owner:湖北京海泰建材科技有限公司
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