2353 results about "Compound s" patented technology

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

Aspects of the disclosure relate to complexes and other aspects relate to formulations (e.g., aqueous, lyophilized forms) comprising such complexes comprising an oligonucleotide (e.g., useful for targeting DMPK) covalently linked to an antibody (e.g., anti-TfR1 antibody).

Disclosed herein are methods and compositions for preventing or reducing adverse events associated with administration of a RAS(ON) inhibitors. Thus, disclosed are compositions and methods for treating or preventing RAS(ON) inhibitor therapy-associated rash or mucositis. The methods involve administering a compound that binds to cyclophilin A (CypA) to compete with a RAS(ON) inhibitor for CypA binding, thereby reducing tri-complex formation in non-tumor tissues. These approaches may improve the tolerability of RAS(ON) inhibitor therapies without compromising efficacy.

The invention relates to the technical field of cosmetics, and discloses an anti-inflammatory soothing cosmetic composition which comprises the following components in percentage by weight: 0.5%-4% of a barrier repairing component, 0.5%-3% of an immunoregulation component, 0.3%-2.5% of a nerve soothing component, 0.3%-3% of an anti-inflammatory plant compound, 1%-10% of a moisturizing soothing enhancer and the balance of auxiliary materials. According to the components, through a five-dimensional synergistic mechanism of barrier repair, immune tolerance, nerve desensitization, anti-inflammatory itching relieving, moisturizing and stability maintaining, anti-inflammatory relieving and barrier repair are remarkably enhanced; ceramide, rare ginsenoside, phytosterol ester and free fatty acid are introduced to synergistically construct a bionic liposome which is closer to the composition of human cuticle lipid, so that the transdermal absorption and stability are enhanced, and the repair efficiency is remarkably improved; the dipotassium glycyrrhizinate, the tamarix chinensis flower extract, the purslane extract, the dinoflaxanthine and the baicalin cooperate to quickly resist inflammation and relieve itching and strengthen barrier repair, so that the composition is suitable for highly sensitive skin.

The invention discloses an anti-aging face cream suitable for sensitive skin and a preparation method of the anti-aging face cream. The anti-aging face cream comprises 1-10 wt% of a supramolecular eutectic compound, 10-30 wt% of an auxiliary material and the balance of deionized water, the supramolecular eutectic compound comprises an anti-aging component, a supramolecular eutectic agent and Neosol-Aqulio, wherein the supramolecular eutectic agent is used for forming a supramolecular eutectic with the anti-aging component, and the Neosol-Aqulio is dispersed in the supramolecular eutectic; wherein the anti-aging component comprises oleuropein and hydroxytyrosol, and the supramolecular eutectic agent is nicotinamide, or a mixture of capryloyl glycine and betaine. Neosol-Aqulio, a supramolecular eutectic agent and an anti-aging component are utilized to form a supramolecular eutectic, so that active component delivery is facilitated, efficient transdermal absorption is realized, permeability, stability and mildness of the anti-aging active component are improved, the problem of sensitive skin cuticle permeation is solved, irritation of a traditional penetration enhancer is avoided, and the penetration enhancer is suitable for clinical application. The double effects of efficient permeation and mild anti-aging are realized.

The invention relates to a composite reverse osmosis membrane acidic cleaning agent, a preparation method and a cleaning process thereof, and belongs to the technical field of environment-friendly water treatment. The cleaning agent comprises the following components in percentage by mass: 4-8% of inorganic acid, 20-40% of organic acid, 1-3% of a surfactant, 0.5-1% of a chelating agent, 0.5-1% of a compound corrosion inhibitor and the balance of deionized water. The composite corrosion inhibitor is formed by compounding 2-mercaptobenzothiazole and the like according to a specific mass ratio, the molecular weight of polyaspartic acid is 5000, and the molar ratio of Zn to Mo in the zinc-molybdate compound is 2: 1. The preparation method comprises the following four steps: firstly preparing a compound corrosion inhibitor premix, then preparing an acidic base solution, and then sequentially adding the components to finally obtain the cleaning solution. According to the cleaning process, a cleaning agent and deionized water are mixed, the membrane flux recovery rate is larger than or equal to 85% through cleaning of a specific process, the reverse osmosis membrane can be effectively cleaned, and the performance of the reverse osmosis membrane can be recovered.

The invention provides a hydroxytyrosol supramolecular compound and a preparation method and application thereof, and belongs to the technical field of cosmetics and biological medicine, the supramolecular compound comprises the following chemical components by mass: 0.01-10% of hydroxytyrosol, 2-45% of an amino acid compound, 2-20% of alpha hydroxy acid, 2-30% of urea, and 15-92% of water. The supramolecular compound can promote transdermal delivery of hydroxytyrosol and maintain the biological activity of hydroxytyrosol, shows high biocompatibility, and can be applied to product development in the antibacterial field, the regeneration field and the anti-aging field.

Aspects of the disclosure relate to complexes comprising a muscle-targeting agent covalently linked to a molecular payload. In some embodiments, the muscle-targeting agent specifically binds to an internalizing cell surface receptor on muscle cells. In some embodiments, the molecular payload promotes the expression or activity of a functional dystrophin protein. In some embodiments, the molecular payload is an oligonucleotide, such as an antisense oligonucleotide, e.g., an oligonucleotide that causes exon skipping in a mRNA expressed from a mutant DMD allele.

Methods and apparatus for determining a representation of a protein-protein complex, given a constituent target complex of the protein-protein complex are presented; where the constituent target complex is some subset of the protein-protein complex. A recursive transformer neural network is devised, wherein for each iteration of the recursion, a representation of the output constituent protein complexed with the input constituent target complex is passed into the transformer as input for the next iteration. Some embodiments of the invention include design and manufacturing of effective synthetic biologic drugs, monoclonal antibody (mAb) drug, Antibody Drug Conjugate (ADC), peptide ligand drug, and small molecule drugs (SMDs).

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The invention relates to the field of oral cavities, and particularly discloses a lasting antibacterial type composite tooth socket for medicine carrying and a preparation method thereof.The lasting antibacterial type composite tooth socket comprises an adsorption layer and an antibacterial membrane layer, the adsorption layer is used for adsorbing oral cavity treatment liquid medicine, and the antibacterial membrane layer comprises a nano-silver antibacterial layer and a chitosan antibacterial layer; the preparation method comprises the following steps: mixing a tea polyphenol-polylactic acid composite solution, a nano-silver-carboxylation modified cellulose compound and a polyvinyl alcohol solution, and carrying out electrostatic spinning to prepare a nano-silver antibacterial fiber membrane, so as to form the nano-silver antibacterial layer; mixing chitosan with hot water, adding cinnamyl aldehyde, glycerol and boric acid, stirring to obtain a mixed solution, coating one side of the nano-silver antibacterial layer with the mixed solution, and curing to form a chitosan antibacterial layer; the adsorption layer is attached to the side, away from the chitosan antibacterial layer, of the nano-silver antibacterial layer, and then the lasting antibacterial type composite tooth socket for carrying the medicine is prepared through hot-pressing compounding. The drug-loaded composite tooth socket has the characteristic of further improving the antibacterial property and the antibacterial durability of the drug-loaded composite tooth socket.

Aspects of the disclosure relate to methods of reducing expression or activity of DUX4 (e.g., DUX4 protein and / or mRNA) and / or methods of treating facioscapulohumeral muscular dystrophy (FSHD) in a subject. In some embodiments, the methods comprise administering to the subject a composition comprising complexes (e.g., muscle targeting complexes) comprising an oligonucleotide (e.g., an RNAi oligonucleotide such as an siRNA) covalently linked to an antibody (e.g., anti-TfRl antibody).

Aspects of the disclosure relate to complexes comprising an anti-TfR1 antibody covalently linked (e.g., via a linker such as a peptide linker) to a lysosomal enzyme (e.g., an acid alpha glucosidase enzyme), and methods of making and using the fusion complexes to treat a lysosomal storage disease (e.g., Pompe disease).

Aspects of the disclosure relate to complexes and other aspects relate to formulations (e.g., aqueous, lyophilized forms) comprising such complexes comprising an oligonucleotide (e.g., useful for targeting DMPK) covalently linked to an antibody (e.g., anti-TfR1 antibody).

Aspects of the disclosure relate to complexes comprising a muscle-targeting agent covalently linked to a molecular payload. In some embodiments, the muscle-targeting agent specifically binds to an internalizing cell surface receptor on muscle cells. In some embodiments, the molecular payload inhibits expression or activity of a DMPK allele comprising a disease-associated-repeat. In some embodiments, the molecular payload is an oligonucleotide, such as an antisense oligonucleotide or RNAi oligonucleotide.

The invention relates to the technical field of pharmaceutical preparations, in particular to a stable perindopril amlodipine tablet and a preparation method thereof, and the tablet comprises the following components in percentage by weight: 5.0% of arginine perindopril; 3.5% of amlodipine besylate; 20%-40% of pregelatinized starch; 40%-68% of a microcrystalline cellulose colloidal silicon dioxide compound; 2.5%-6% of a disintegrating agent, wherein the disintegrating agent is selected from one or more of ion exchange resin, sodium alginate and croscarmellose sodium; the pregelatinized starch and the microcrystalline cellulose colloidal silicon dioxide compound are selected as main diluents, so that the Maillard reaction possibly occurring between the lactose and the active pharmaceutical ingredients is completely avoided, the problem of increase of related substances is fundamentally solved, and the stability and the safety of the product are remarkably improved.

An oral amphetamine extended release solid dose is described. The compositions contain a combination of an uncoated amphetamine-cation exchange resin complex, a barrier coated amphetamine-cation exchange resin complex-matrix, and an uncomplexed amphetamine, wherein one or more of these components contains blends of different forms of amphetamines. Either the modified release coated and / or the uncoated amphetamine-cation exchange resin complex may have two forms of amphetamine in a complex with a single cation exchange resin. Following administration of a single dose of the composition, a therapeutically effective amount of amphetamine is reached by about one hour and the composition provides at least a thirteen hour effect post-dose.

The invention relates to a high-water-solubility denitroflavin covalent complex as well as a preparation method and application thereof, and belongs to the technical field of organic synthesis and medicinal chemistry. Comprising the following steps: (1) firstly, carrying out bromination reaction on 3-methyl-10-ethyl denitroflavin, so as to obtain 3-methyl-10-(1-bromoethyl) denitroflavin; and (2) coupling the 3-methyl-10-(1-bromoethyl) denitroflavin with vitamin C, so as to obtain the high-water-solubility denitroflavin covalent complex. According to the present invention, the prepared highly water-soluble denitrificin covalent complex has the two-phase solubility of the organic solvent and the water, such that the water solubility of the 3-methyl-10-ethyl-denitrificin is substantially enhanced, and the application range of the denitrificin is expanded. And meanwhile, the denitrified flavin covalent compound also has good antioxidant activity, and the antioxidant duration can be prolonged.

The invention discloses a sugar response hydrogel wound dressing based on Prussian blue nano-enzyme and bacterial cellulose as well as a preparation method and application of the sugar response hydrogel wound dressing, and belongs to the field of medical dressings and biological materials. The sugar-responsive hydrogel wound dressing is good in mechanical property, and can be subjected to cascade reaction to play antibacterial and anti-inflammatory roles. The preparation method comprises the following steps: preparing Prussian blue nano-enzyme (PBNPs) by adopting a one-pot method and utilizing a self-polymerization reaction, and preparing a Prussian blue nano-enzyme bacterial cellulose compound by utilizing an isotonic adsorption method; glucose oxidase (GOx) is loaded on BC coated PBNPs by adopting an in-situ polymerization method, the sugar response hydrogel wound dressing based on PBNPs and BC is obtained, the preparation method is simple in process, and the obtained sugar response hydrogel wound dressing is good in stability, suitable for factory production and hopeful to be applied to diabetes wound treatment. Meanwhile, the PBNPs are applied to the field of diabetic wound dressings, and the application direction of the PBNPs is widened.

The invention belongs to the technical field of drug delivery, and particularly relates to an M-coated PLGA-10BX compound as well as a preparation method and application thereof. The preparation method comprises the following steps: preparing 10B-enriched boron nitride (h-10BN); extracting a cell membrane of the macrophage RAW264.7; polylactic acid-glycolic acid copolymer (PLGA) nano particles loaded with h-10BN are prepared; and finally, the bionic nano platform M (at) PLGA-10BN based on the macrophage membrane is prepared. The bionic nano-platform prepared by the invention is uniform in particle size and morphology, has relatively high biological safety, and has no obvious damage to various tissues and visceral organs. The compound can be used as a general platform for boron compound delivery, can also be used as an immune activator, is suitable for intravenous injection administration, and expands the application of boron neutron capture therapy (BNCT) in treatment of glioblastoma (GBM).

The invention discloses an adipose-derived stem cell exosome compound loaded with silver nanoparticles and application of the adipose-derived stem cell exosome compound loaded with the silver nanoparticles, and ADSC-Exos loaded with the silver nanoparticles is developed by integrating AgNPs into an exosome of ADSCs. In vivo, the Exo-AgNPs can accelerate healing of infected wounds by reducing bacterial colonization and promoting collagen deposition, angiogenesis and M2 type macrophage polarization. In vitro, the Exo-AgNPs activates the functions of fibroblasts and vascular endothelial cells, and shows an excellent antibacterial property. In addition, the Exo-AgNPs induces polarization of M2 type macrophages and inhibits secretion of proinflammatory cytokines by activating autophagy. The results show that Exo-AgNPs is expected to become an ideal biological material for treating infected wounds.

The invention relates to the technical field of biological medicines and ophthalmic medicines, in particular to a herbal exosome composition for eye care and treatment and a preparation method thereof. The composition comprises a synergistic combination of herbal exosomes and mesenchymal stem cell exosomes, and further comprises a nano slow-release carrier system. Wherein the herbal exosome is extracted from a traditional herbal plant liquorice by combining gradient centrifugation with a molecular exclusion chromatography method, and herbal active ingredients, namely astragaloside and quercetin, are loaded in the exosome by adopting an electroporation method, so that the pharmacological activity of the exosome is enhanced. The nano slow-release carrier system is of a two-phase slow-release structure; an inner phase is a phospholipid complex loaded with herbal exosomes and mesenchymal stem cell exosomes, and an outer phase is temperature-sensitive hydrogel; the compound is in a liquid state at room temperature, and is rapidly converted into a gel state after being dropped into the ocular surface, so that the retention time of the medicine on the ocular surface is remarkably prolonged, the bioavailability is improved, and the targeting slow release capability aiming at ocular surface tissues is endowed to the compound.

The invention discloses a photocuring microneedle with ginseng exosome loaded berberine, a preparation method of the photocuring microneedle and application of the photocuring microneedle to tissue repair. A ginseng exosome loaded berberine compound is prepared through a microfluidic technology; filling a needle cavity of a microneedle mold with a needle tip layer preparation solution containing the compound, methylacryloylated hyaluronic acid and methylacryloylated gelatin through a centrifugal method; covering a backing layer preparation solution composed of hyaluronic acid and povidone K90, and centrifuging again; and finally, carrying out light curing, drying and demolding. The prepared composite microneedle is complete and sharp in needle shape and high in forming rate; the efficient entrapment of the active medicine is realized; the biocompatibility is good, and the irritation is low; a cross-linked network structure formed by photocuring is beneficial to realizing controlled release of drugs, the targeted repair function of the ginseng exosome is combined with the hypoglycemic effect of berberine, and a new strategy and technical approach with a prospect are provided for painless, efficient and long-acting treatment of diabetes mellitus.

Aspects of the present disclosure relate to conjugates comprising a muscle targeting agent covalently linked to a molecular payload. In some embodiments, the muscle targeting agent specifically binds to an internalized cell surface receptor on muscle cells. In some embodiments, the molecular payload promotes the expression or activity of functional dystrophin protein. In some embodiments, the molecular payload is an oligonucleotide, such as an antisense oligonucleotide, e.g., an oligonucleotide that causes exon skipping in mRNA expressed from a mutant DMD allele.

The peptide complex of the present invention promotes the expression of the SIRT1 gene, referred to as a longevity gene, promotes the expression of the FGF21 gene, and increases the phosphorylation of AMPK. In addition, the peptide complex of the present invention exhibits an anti-inflammatory effect. Therefore, the peptide complex of the present invention inhibits aging, promotes the expression of the longevity gene SIRT1 gene, and can be used for treating or preventing diseases associated with SIRT1.

The application relates to the technical field of traditional Chinese medicines, in particular to a uric acid reducing composition and a preparation method thereof. The uric acid reducing composition comprises 35-45 parts of a cyclodextrin inclusion compound, 25-35 parts of nano-liposomes, 20-30 parts of a chicory extract-phospholipid complex and 5-8 parts of an antioxidant complex; the preparation method of the cyclodextrin inclusion compound comprises the following steps: step 1, adding beta-cyclodextrin into water, stirring and dissolving, adding pueraria extract, drying after inclusion reaction, and obtaining inclusion compound a; step 2, adding hydroxypropyl-gamma-cyclodextrin into water, stirring, adding mulberry leaf extract, drying after inclusion, and obtaining inclusion compound b; and step 3, mixing the inclusion compound a and the inclusion compound b, and obtaining the product. The uric acid reducing composition can more comprehensively and efficiently reduce blood uric acid level, and has high safety, high stability and high bioavailability. The preparation method is simple, easy to industrialize and beneficial to large-scale industrial production.

The invention belongs to the technical field of contact lens care, and provides temperature-sensitive contact lens eye-moistening gel and a preparation method thereof. The temperature-sensitive contact lens eye-moistening gel is prepared from the following raw materials in parts by mass: a gel matrix, a surfactant, an osmotic pressure regulator, an active component, a chelating agent, a buffering agent and the balance of injection water, the composition of the gel matrix is defined. Chitosan, sodium hyaluronate and polyvinyl alcohol are compounded to serve as a gel matrix, a polyelectrolyte compound is formed, gelation time is shortened, gel strength and swelling resistance are improved, biocompatibility is improved, and drug-loaded delivery of active ingredients is achieved; the gel matrix and the surfactant are reasonably selected, the viscosity of the solution is increased, the gelation time is shortened, the excellent effect of relieving eye fatigue and dryness is achieved, the wearing comfort of the contact lens is remarkably improved, and the oxygen permeation effect of the contact lens is not obviously reduced after gel forming.

The invention relates to the technical field of detection kits, in particular to a blood coagulation reaction linked lupus anticoagulant fluorescence detection kit and application thereof, the kit contains a screening-confirmation integrated reagent, a calibration product, a quality control product and an anticoagulation interference inhibitor; the integrated reagent is divided into a reagent A and a reagent B, the reagent A contains a buffer solution, recombinant snake venom thrombin, composite phospholipid, a fluorescent substrate and other components, and the reagent B contains prothrombin, calcium ions, high-concentration composite phospholipid and other components; the composite phospholipid system is formed according to a specific proportion and modifies beta2-glycoprotein I, the fluorescence enhancement-stabilization system is formed by matching a Schiff base compound with a stabilizer, the calibrator is a series of lupus anticoagulant standard substances, and the quality control substance comprises simulants with different concentrations and negative control. The anti-interference capability is high, and the influence of anti-coagulant drugs and enzyme source fluctuation is reduced; the signal amplification effect is obvious, the detection sensitivity is high and the reagent stability is good; the operation is simple and convenient, screening and confirmation are integrally completed, and a conventional fluorescence detector is adapted.

The invention provides a nanocrystalline composite oral ulcer film agent as well as a preparation method and application thereof. The nanocrystalline composite oral ulcer film agent comprises a waterproof backing layer and a drug-loading adhesion layer coated on the waterproof backing layer, the drug-loaded adhesion layer comprises a macromolecular hydrogen bond compound formed by a weakly acidic polymer and a nonionic proton receptor polymer, and a nanocrystalline drug. Compared with the prior art, the preparation method has the advantages that the polyacrylic acid polymer and the nonionic cellulose polymer interact to form IPC serving as an adhesion layer film-forming material, the nanocrystals are loaded into the adhesion layer film-forming material, the waterproof backing layer is coated with the adhesion layer film-forming material, and the oral ulcer film agent is prepared after drying and cutting. The obtained film agent has good comfort and adhesive power, shows good drug stability and permeation promotion performance, can be used as a carrier of an oral administration route, prolongs the drug action time and improves the curative effect. The preparation method of the film agent is simple and easy for industrial mass production.