39 results about "Bioactive molecules" patented technology

The present disclosure relates to biologically active molecules comprising a single domain antibody (sdAb) that specifically binds to the extracellular domain of human gp130, compositions comprising such antibodies, and methods of use thereof.

An injectable liquid containing bioactive molecules released from a powder comprising a neo-synthesized extracellular matrix for use in the treatment or prevention of cancer, in particular in the local treatment of solid tumors.

A pharmaceutical combination for subcutaneous administration and use thereof are provided. The pharmaceutical combination as described herein for subcutaneous administration includes a hyaluronidase and an antibody-drug conjugate. The antibody-drug conjugate includes a fragment of a bioactive molecule, and the bioactive molecule has moderate toxicity. The pharmaceutical combination can achieve a larger volume and a larger dose of administration, and the side reaction is not enhanced.

Phthalide lactones, as an important class of benzopentolactone skeleton, are widely distributed in natural products, medicinal plants and bioactive molecules, and have significant pharmacological activities and synthetic application potential. This kind of structure not only shows various biological activities such as antibacterial, anti-inflammatory, antitumor, antioxidant, but also is an indispensable core structural unit in many drug molecules and lead compounds. At the same time, cyano is a very valuable functional group in the field of organic synthesis and medicinal chemistry, with strong electron-withdrawing properties, strong structural stability and other advantages, which can effectively improve the electronic distribution, lipid solubility and drug performance of the molecule. In view of the important significance of phthalide lactones and cyano in organic synthesis and drug research and development, the present invention develops a synthetic method for efficiently constructing cyano-containing alkyl chain substituted phthalide lactone compounds. It has important value in medicinal chemistry and organic synthesis.

The application discloses a tetra-substituted furanone compound and a preparation method and application thereof. The structural formula of the tetra-substituted furanone compound is shown in formula (III); wherein, R 1 is an aromatic group, a substituted aromatic group, an alkyl group or a substituted alkyl group; 2 R 3 is an aromatic group, a substituted aromatic group, an alkyl group, a substituted alkyl group or a heterocyclic group; R 4 is an aromatic group, a substituted aromatic group, an alkyl group, a substituted alkyl group or a heterocyclic group. The tetra-substituted furanone compound provided by the application is widely distributed in natural products and bioactive molecules, and can be used as a multi-purpose intermediate and precursor in organic synthesis. The tetra-substituted furanone compound is also a potential strong antiviral active molecule, and has a wide application prospect in the field of antiviral drug research and development.

The application belongs to the technical field of biological medicine and molecular biology, and particularly relates to application of umbilical cord blood plasma-derived extracellular vesicles and related bioactive molecules thereof in treatment of Alzheimer's disease. Specifically, the application isolates extracellular vesicles (UCBP-sEVs) from umbilical cord blood plasma, which has the effect of improving Alzheimer's disease. Further research finds that high enrichment of miR-16-2-3p therein is a key molecule for mediating treatment of Alzheimer's disease. miR-16-2-3p targets and inhibits expression of ROCK2, reduces phosphorylation level of TFEB and promotes nuclear translocation of the same, activates microglial autophagy-lysosome pathway, and thus promotes phagocytosis and degradation of intracerebral beta amyloid, and therefore has good practical application value.

The invention is directed to fertilizers and manufacturing methods using organically enhanced inorganic fertilizer granules that incorporate a coating of one or more layers containing a bioactive agent in a carrier. The bioactive agent may be an herbicide, pesticide, plant growth regulator, microorganism, or beneficial element. Manufacture of conventional fertilizers involves stresses such as pH, heat, and pressure that are overcome by providing a protective carrier that facilitates and extends functional survival / effectiveness. Many carriers, such as liquefied dried milk, bind actively to the granule surface and contribute to the total carbon base. The release of the bioactive agent from the coating and or the surface of the fertilizer granule preferably results in a two-phased release, a first fast release and a second extended or slow-release into the soil metering the bioavailability of the bioactive agent for crop growth or protection, and / or for controlling unwanted vegetation or pests.

The application belongs to the technical field of organic synthesis, and particularly relates to a kind of bromine-containing isoindoline-1-ketone compound and preparation method thereof.The preparation method of the bromine-containing isoindoline-1-ketone compound uses commercially available aldehyde-derived imine as raw material, is reacted with aryl bromide oxazoline compound under butyl lithium condition, and then is subjected to acid-mediated cascade cyclization process, to efficiently construct isoindoline-1-ketone skeleton.The isoindoline-1-ketone compound can be directly used as an organic catalyst, the N-H functional group remaining in the structure of the isoindoline-1-ketone compound has reactivity, can be coupled with other bioactive molecules as a key connection site, to construct functional derivatives, the amide carbonyl group thereof can be further reduced, to be converted into pyrrolidine structural unit, and the structure itself can be used as a catalytically active center, to expand its application in the field of catalysis.

The invention provides an S-adenosine homocysteine (SAH) analogue, an S-adenosine-L-methionine (SAM) analogue and application thereof. The preparation method comprises the following steps: synthesis of the SAH analogue and a fluoroalkyl SAM analogue, fluoromethylation modification of bioactive molecules by an HMT-MT cyclase cascade reaction system based on the fluoroalkyl SAM analogue, and construction of a fluoro derivative of a clinical drug synthesized by a one-pot enzymatic method. The SAH analogue adopted by the invention can effectively avoid spontaneous degradation of the corresponding SAM analogue, and is used for constructing a cascade reaction system based on HMT-MT cyclase, so that the yield of a fluoromethylation product is increased; it is confirmed that the fluoro-intermediate generated by MT can be accepted by downstream biosynthetase, so that a fluoro-derivative of a clinical drug synthesized by a one-pot enzymic method is constructed.

This invention belongs to the field of biomedical technology, specifically disclosing a scorpion-derived polypeptide for combating influenza virus and its applications. The scorpion-derived polypeptide has the amino acid sequence shown in SEQ ID NO:1, or is a functional variant obtained by substitution, deletion, and / or addition of one or more amino acids from the same sequence, retaining its anti-influenza virus activity. The scorpion-derived polypeptide provided by this invention can significantly inhibit the proliferation of influenza A virus and substantially reduce the expression levels of viral RNA and protein within a non-cytotoxic concentration range. It also effectively reduces viral load and inflammatory factor levels in mice infected with influenza A virus, exhibiting excellent anti-influenza A virus activity and being less likely to induce viral resistance. This invention provides a novel, highly efficient, and low-toxicity bioactive molecule for influenza prevention and control, which can be applied to the development of anti-influenza drugs.

The present disclosure describes conditioned water containing amphibian bioactive molecules and purified bioactive molecules obtained from the conditioned water of amphibians. The present disclosure also describes methods of isolating bioactive molecules from the conditioned water. Moreover, the present disclosure describes using the purified bioactive molecules for treating skin conditions.

The presently disclosed subject matter provides compositions, methods, and kits for transfecting adipose-derived mesenchymal stem cells (AMSCs) in freshly extracted adipose tissue using nanoparticles comprising biodegradable polymers self-assembled with nucleic acid molecules. The presently disclosed subject matter also provides methods for treating a neurological disease in a patient in need thereof, the method comprising administering the AMSCs transfected with the nucleic acid molecules to the patient, wherein the nucleic acid molecules encode one or more bioactive molecules functional in the treatment of a neurological disease, particularly wherein the neurological disease is a brain tumor.

This invention relates to compositions, and uses and methods thereof, with therapeutic deciparticles. Described herein are deciparticle (nanoparticle) compositions composed of an amphiphilic compound complexed with an auxiliary compound such as a biologically active molecule. Deciparticles of this invention are active drugs having potency for anti-tumor effects and for immunosuppression. This invention is also directed to amphiphilic compounds useful for making deciparticle complexes.

The invention relates to a formulation of a pharmaceutical and food product, based on the fruits of Diospyros kaki. The invention further relates to the use of this pharmaceutical and food product, according to the method of preparation which takes place in several successive phases: sorting, rinsing, drying at a temperature which oscillates between 40 and 50 °C, grinding, mixing, maceration with distilled water for 12 hours and filtration, freeze-drying for 48 hours, to obtain the freeze-dried product by removing the water from the frozen suspension. The invention further relates to the formulation of a pharmaceutical and food product based on the pure extract of Diospyros kaki fruit (crude extract) which is rich in bioactive molecules for the purpose of preventing and fighting against various associated digestive and hepatorenal diseases. The invention also consists of using the formulated food product in other applications in the field of pastry making such as the production of syrup, flavoured food additive, jam and also juices.

Disclosed herein are compositions comprising a hydrogel scaffold, methods of generating a hydrogel scaffold, and systems for and methods of using the hydrogel scaffold to produce biologically active molecules.

This invention relates to compositions, and uses and methods thereof, with therapeutic deciparticles. Described herein are deciparticle (nanoparticle) compositions composed of an amphiphilic compound complexed with an auxiliary compound such as a biologically active molecule. Deciparticles of this invention are active drugs having potency for anti-tumor effects. This invention is also directed to amphiphilic compounds useful for making deciparticle complexes.

The application discloses a kind of silicon dioxide-engineered extracellular vesicle composite nano-preparation for tendon-bone interface repair and its preparation method and application, the preparation includes carrier matrix and functional load component, functional load component is loaded in carrier matrix by the synergistic effect of physical adsorption and channel embedding;The carrier matrix is the bioactive silicon dioxide nanoparticle of core-shell structure, the mesoporous silicon dioxide with central radial channel is in the core, the shell is calcium phosphorus layer, and the nanoparticle surface is modified by bone targeting molecule;Functional load component is the engineered extracellular vesicle of bone marrow mesenchymal stem cell source preprocessed by the bioactive molecule with anti-inflammatory osteogenesis effect.The application is by the dual delivery strategy of " carrier + excretion component", on the one hand, active ion released by silicon dioxide carrier promotes osteogenesis, on the other hand, " high efficiency" exosome is stimulated, and local inflammatory microenvironment is adjusted, and the functional regeneration of tendon-bone interface is accelerated by synergistic effect.

This invention relates to the field of biomedicine, specifically to a class of prodrug structures with ROS signal-responsive properties, their preparation methods, and applications. The prodrug molecules with ROS signal-responsive properties developed in this invention can rapidly release bioactive molecules in ROS-rich environments, achieving targeted therapeutic effects. This method has good universality and has been verified to be able to prodrugize various molecules, including four approved drug molecules, improving drug solubility, biocompatibility, reducing cytotoxicity, and enhancing targeted therapeutic effects. Based on the structural characteristics of these molecules, they can also complex with PVA hydrogels to further achieve responsive and controllable drug release.

The present disclosure provides a compound comprising a modified tetracycline derivative, covalently coupled through a linker to a low-hydrophobicity bioactive molecule useful for treating neurodegenerative diseases, wherein the modified tetracycline derivative is optionally defined by the following formula:

This invention relates to novel ionizable amine lipids with one or more sulfur atoms introduced into their tails. These lipids can be used in combination with other components to form lipid nanoparticles with oligonucleotides. The invention describes the synthesis, nanoparticle formation, and characterization of lipids of formula (I), as well as biological experiments demonstrating that lipid nanoparticles prepared from these novel lipids can efficiently deliver their carriers (e.g., RNA, DNA, mRNA, siRNA, miRNA, pDNA, circular DNA, dsRNA, small bioactive molecules) into cells.

The application provides a polytetrafluoroethylene barrier film and its application and preparation method, and belongs to the technical field of biomedical materials. The polytetrafluoroethylene barrier film comprises a film body and a bioactive layer on the surface of the film body; wherein the material of the film body comprises polytetrafluoroethylene, and the outer surface of the film body has a polar group; the material of the bioactive layer comprises a hydrophilic bioactive molecule. In the polytetrafluoroethylene barrier film provided by the application, the polar group on the outer surface of the polytetrafluoroethylene film body interacts with and effectively combines with the hydrophilic bioactive molecule, the combination stability between the film body and the bioactive layer is improved, the adhesion and growth of osteoblasts can be realized, and then the new bone mass during the bone augmentation surgery using the polytetrafluoroethylene barrier film is improved. In addition, the hydrophilic bioactive molecule can also endow the polytetrafluoroethylene barrier film with multifunctionality due to its characteristics.

The invention provides a novel method for realizing conversion from tertiary alcohol to ester in one step through carbon-carbon bond oxidative cleavage. According to the method, the ester compound is prepared from the tertiary alcohol compound by reacting for 12-48 hours at 110-180 DEG C in the presence of a nitrate catalyst in an oxygen atmosphere, and the method has the following advantages: 1) the application range of a substrate is wide, and the yield of medium or above can be obtained; and 2) the method does not need additional addition of an initiator, an oxidant and the like, and has the advantages of simplicity in operation, high stability, capability of realizing gram-level scale amplification and the like. And 3) the method can realize functional group conversion of complex bioactive molecules.

To provide a method for forming a microneedle array, which may include the step of forming a microneedle array having one or more types of bioactive components. [Solution] A microneedle array may include a base and a plurality of microneedles extending from the base, and one or more bioactive ingredients may be present in higher concentrations within the microneedles than within the base. The systems and methods disclosed herein include a skin delivery platform based on a soluble microneedle array that can result in efficient, precise, and reproducible delivery of bioactive molecules to human skin. The microneedle array delivery platform can be used to deliver a wide range of bioactive ingredients to patients.

The utility model discloses a preparation system of functional penis dressing relates to the biological gel preparation technical field of penis dressing, the utility model discloses a base, inner layer tubular product and outer layer tubular product, and the inner layer tubular product and outer layer tubular product are concentric double -layer tubular structure, and both are fixed in the base with the mode of concentric shaft, wherein the inner layer tubular product and outer layer tubular product are provided with the inner and outer tube interlayer between, the piston is provided in the inner layer tubular product, and the piston is closely connected with the inner layer tubular product wall and does not leak air. The utility model discloses through the integration biological gel of basic material and active ingredient, adds the basic material and active ingredient separately at the same time, avoids the active influence of heating to active ingredient, and the functional penis dressing developed has the similar structure with penis, through the surface of penis is covered, plays the role of biological activity molecule slow -release, the preparation system process of the utility model is simple, and the reaction is easy to control, and the stability is good, and the industrialization is possible, has extensive popularization prospect.

The application belongs to the technical field of synthetic chemistry, and relates to an arylmethyl sulfone compound and a synthesis method thereof. The application takes an imidazopyridine compound as a reaction substrate, takes sodium sulfinate as a sulfone reagent, takes DMA as a methylene source, and directly obtains the arylmethyl sulfone compound through one-step reaction under the action of a catalyst and an oxidant. The synthesis method has the advantages of rapid reaction, low cost of raw materials, simple operation and high yield. The arylmethyl sulfone compound constructed by the application is an important skeleton of many drugs, bioactive molecules and natural products, and the synthesis method provides a widely applicable preparation method for the synthesis of the compounds.

The present invention relates to lipids of formula (I), compositions comprising lipids of formula (I), methods for producing lipids of formula (I) and / or compositions, lipids of formula (I) and / or compositions for use as pharmaceuticals, the use of lipids of formula (I) and / or compositions as vectors for delivering active ingredients to targets, organs, cells and / or tissues, methods for transfecting cells with nucleic acids and / or proteins and / or peptides and / or polysaccharides and / or lipids and / or small organic or inorganic molecules and / or any kind of bioactive molecules using lipids of formula (I) and / or compositions, transfected cells obtained by this method, and kits comprising lipids of formula (I) and / or compositions.

The present application relates to the field of cosmetic technology, and more particularly to a vitamin C derivative composition and its preparation and application. The vitamin C derivative composition comprises vitamin C derivative, antioxidant protective agent, non-ionic surfactant, structure aid, and water. The non-ionic surfactant of polyglycerol short-chain ester is selected as the structure carrier, the antioxidant protective agent is dispersed in the gel carrier of lamellar micelles, the structure aid is used as the lipophilic auxiliary surfactant to cooperate with the structure layer, the hydrophilic end exists in the water phase between layers in the form of the fusion of the vitamin C derivative active molecule and water, and finally the gel carrier with certain consistency can be constructed. As the gel matrix, the solid state characteristics are beneficial to reducing the risk of the stability decline and activity degradation of the vitamin C derivative, thereby providing a better solution for the stable application of the vitamin C derivative in cosmetics.

The invention relates to LipexSil® lipid-containing nanoparticle compositions, in which a silicon-containing ionizable lipid is combined with a certain ratio of other lipids consituting the lipid nanoparticles resulting in a remarkable T cell transfection. In certain embodiments, the formulation consists of four components (ionizable lipid, structural lipid, helper lipid, and shield lipid), while in other embodiments a fifth lipid component is included. This ionizable cationic lipid family is showing remarkably low in vitro toxicity on T cells. The invention describes the production and characterization of the lipid nanoparticles and in vitro experiments demonstrating that the corresponding formulations with the LipexSil® lipids [WO2024023174] are superior to the current approach, delivering their payload, or cargo (e.g. RNA, DNA, mRNA, microRNA, siRNA, pDNA, circular DNA, small biologically active molecules) into T cells.

This invention provides a lipid compound and its applications, the results of which are shown in Formula I. The lipid compound provided by this invention can be used for targeted delivery of bioactive molecules to splenic T cells, particularly suitable for transporting negatively charged nucleic acid molecules, such as mRNA, providing a potential delivery strategy for in vivo specific gene editing of T cells. This invention also provides a bioactive substance delivery system comprising the lipid compound, which is loaded with bioactive substances. The bioactive substance delivery system of this invention, after intravenous administration, can efficiently target spleen tissue and selectively deliver active substances to T cells within the spleen, achieving efficient T cell transfection and immune activation. The delivery system of this invention has a simple synthesis process and strong structural tunability, and has broad application prospects in the fields of T cell immunotherapy and gene therapy.

The application discloses a method for synthesizing alkenyl borate ester compounds through a series reaction of palladium-catalyzed cross-coupling and iron-catalyzed borohydration, and belongs to the field of organic synthesis. The method inserts multiple methylene units into the carbon-carbon sigma-bond of the alkenyl borate ester through a series reaction of palladium-catalyzed cross-coupling and iron-catalyzed borohydration, and meanwhile, a valuable C(sp 2 )‑B functional group is reserved. The method utilizes the universality of the alkenyl borate ester in the cross-coupling reaction, provides an efficient approach for modular and iterative synthesis of C(sp3) homologues of bioactive molecules containing olefin structures, and is expected to accelerate the drug discovery process, applied to efficient preparation of drug molecule homologues and complex organic compounds, and provides a powerful tool for realizing rapid structural derivatization of drug lead compounds.