8943 results about "Small molecule" patented technology

In various embodiments, the disclosure provides compositions, such as polypeptides, polynucleotides, gene editing systems, small molecules, vectors, or host cells, comprising and / or modulating the expression or activity of an immunomodulatory-related protein. In various embodiments, the disclosure also provides for the treatment of aging, senescence, fibrosis, metabolic diseases, cardiovascular diseases, endocrine-related disorders, genetic diseases, cancer, infections, immune diseases, and the like using agents comprising and / or modulating the expression or activity of an immunomodulatory-related protein. Methods of replacing an adaptation of therapy or combinations thereof with hormones, growth factors and / or proteins, as well as methods of identifying the agents.

Compounds of Formulae (I)-(VII) or their pharmaceutically acceptable salts can inhibit the G12C, G12D, G12V, and / or G13D mutants of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formulae (I)-(VII) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

To provide a medicine for treating a disease in a mammal.SOLUTION: Provided is a medicine for treating a disease in a mammal, comprising an expression cassette that is a first expression cassette comprising a chimeric gene operably linked to a first expression control element, the chimeric gene comprising a first portion comprising a minigene having an alternatively spliced exon and a second portion encoding a first RNA encoding a protein, the first portion being 5' to the second portion, the second portion lacking an initiation codon or start codon, the alternatively spliced exon comprising a translation initiation regulatory sequence, expression of the protein being controlled by inclusion of the alternatively spliced exon, and the medicine being used in combination with a small molecule splicing modifier that modulates splicing of the alternatively spliced exon.SELECTED DRAWING: Figure 1

The invention provides a photosensitive resin composition containing a photobleaching aminomethyl anthracene photosensitizer and application thereof.The structural main body anthracene ring of the photosensitizer introduces an aminomethyl functional group to the 9th and / or 10th site: through introduction of the aminomethyl functional group, while the electron cloud density of polycyclic aromatic hydrocarbon is maintained, the maximum absorption wavelength is subjected to red shift, and the photosensitive resin composition is especially suitable for a 405nm illumination system; the initiation efficiency is obviously improved; the exposure energy is reduced; compared with an existing DBA type photoinitiator, the problem of alkoxy carbon-oxygen bond breakage caused by p-pi conjugation of DBA is avoided, generation of small molecule fragments is effectively inhibited, defects are reduced, and the yield is increased. In addition, compared with DPHA and DAcOA, the photosensitizer also shows better solubility and formula compatibility. The preparation method has the characteristics of simple preparation process and low cost, and can be widely applied to the photocuring fields of dry films, paints, coatings, printing inks, forming materials and the like.

Compounds of Formula (I) or their pharmaceutically acceptable salts can inhibit the G12C, G12D, G12V, and / or G13D mutants of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

Compounds of Formula (I) or their pharmaceutically acceptable salts can inhibit the G12C, G12D, G12V, and / or G13D mutants of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

The invention provides a method and a system for screening and constructing a small molecule polypeptide simulant based on interaction between proteins, relates to the technical field of biology, and comprises the following steps: predicting an interaction model of RECK protein and ADAM10 protein through a molecular docking platform, and analyzing interaction sites of the RECK protein and the ADAM10 protein. And then, determining a KAZAL region of the RECK protein according to the interaction site, and predicting a sequence structure of the KAZAL region. And then carrying out molecular docking on the KAZAL region and ADAM10 protein, designing a plurality of peptide fragments with the length of 30 amino acids, and screening the peptide fragment sequence with the highest score as candidate polypeptide. And finally, performing species homology comparison and quality control detection on the candidate polypeptide, and verifying the binding capacity and biological function of the candidate polypeptide to ADAM10 protein through cell experiments. The invention provides a method for screening to obtain a polypeptide simulant specifically bound with ADAM10 protein. The polypeptide simulant can be used for treating ADAM10 related diseases.

The invention discloses an embolism part for peripheral arteriovenous vessels, the embolism part comprises an anchoring part and a blocking part fixedly connected with the anchoring part, the blocking part adopts polyurethane shape memory foam, the expansion rate of the polyurethane shape memory foam is 50-100 times, and a preparation method of the polyurethane shape memory foam comprises the following steps: step 1, preparing a polyurethane shape memory foam material; the preparation method comprises the following steps: preparing a polyurethane acrylate prepolymer from macromolecular polyol, diisocyanate, a chain extender containing disulfide bonds, other micromolecular chain extenders and an acrylate end-capping reagent; and 2, uniformly mixing the polyurethane acrylate prepolymer, a foaming agent, a foaming promoter and a photoinitiator to obtain a foaming solution, and sequentially carrying out light curing and foaming on the foaming solution to obtain the polyurethane shape memory foam. According to the embolism part, the polyurethane shape memory foam is adopted as the blocking part, the blocking part applies radial acting force to the wall of the blood vessel all the time based on the expansion trend of the blocking part, and the blocking part and the anchoring part jointly act and can be stably maintained in the blood vessel.

Compounds of Formulae (I)-(VII) or their pharmaceutically acceptable salts can inhibit the G12C, G12D, G12V, and / or G13D mutants of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formulae (I)-(VII) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

Compounds or their pharmaceutically acceptable salts can modulate the G12D mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds disclosed herein or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

The present invention provides a class of small molecule compounds for targeted degradation of a pan-KRAS protein, a preparation method therefor, and use thereof as a therapeutic agent for preventing and / or treating cancer. The compound of the present invention can effectively degrade and / or inhibit the pan-KRAS protein in cells, and can be used for preparing a drug for treating and / or preventing related diseases or disorders caused by pan-KRAS mediation.

The invention provides a nano transdermal delivery system based on superoxide dismutase, the nano transdermal delivery system is of a capsule composite structure of a small molecule active component-superoxide dismutase-polymer shell layer, the small molecule active component is loaded in superoxide dismutase, the surface of the superoxide dismutase is coated by the polymer shell layer, and the superoxide dismutase is loaded in the capsule composite structure. The diameter of the superoxide dismutase-based active ingredient transdermal delivery system is 20-100 nm, and the thickness of the polymer shell layer is 7.5-52.5 nm. In the delivery system, the polymer shell layer provides a protection effect for the superoxide dismutase and the micromolecular functional substances with the anti-oxidation effect, the capsule composite structure is in a nanogel form, and the nanogel not only promotes the penetration depth of the capsule, but also reduces the irritation effect of the capsule on the skin. The raw materials are biologically friendly, the preparation method is simple, the yield is high, and industrial large-scale production can be realized.

The invention discloses a deep eutectic solvent / bimetal organic framework co-catalyzed straw polyol as well as a preparation method and application thereof, the straw polyol is prepared by the following method: uniformly mixing straw powder, small molecular alcohol, an acid catalyst and a deep eutectic solvent in a nitrogen atmosphere, and reacting to obtain a reaction product; and adding a bimetal organic framework catalyst into the reaction product, and reacting to obtain the straw polyol. A green, natural and pollution-free eutectic solvent catalytic liquefaction technology is adopted, lignin and hemicellulose can be dissolved, the cross-linking effect between lignin and hemicellulose and cellulose is reduced, the crystalline structure of cellulose can be destroyed, the available surface area is increased, the contact with a liquefying agent is enhanced, the conversion efficiency is improved, and the residue rate is reduced; the bimetallic organic framework catalyst is added in the middle and later periods of the reaction, aldehydes, ketones and acid and ester substances can be reduced and upgraded into alcohols, the hydroxyl value of the liquefied polyol is greatly increased, and the film-forming crosslinking degree is improved.

The invention discloses an extraction preparation method and application of algae micromolecule PDRN, and relates to the technical field of biology. The invention establishes a process for extracting PDRN from microalgae, which comprises the following steps: carrying out cell disruption on microalgae liquid, and removing cell debris to obtain filtrate; the filtrate is subjected to DNA dissolution, DNA separation and DNA purification, and a PDRN solution is obtained; wherein the dry weight of the microalgae in the algae liquid is 0.1 to 0.333 g / mL. Through process optimization, the extraction efficiency and purity of the microalgae PDRN are improved, and the extracted PDRN has excellent anti-aging and anti-inflammatory effects.

Methods and apparatus for obtaining representations of proteins and small molecule drugs for synthesis; wherein pre-trained mixed modality protein and natural language fusion models are further trained by supervised fine tuning using reasoning-oriented query—chain-of-thought (CoT) response pairs. The resulting reasoning-oriented neural network is then used to obtain representations of output proteins or small molecule drugs, in response to mixed modality reasoning-oriented input queries specifying conditions on the output. In one embodiment, the neural network is an autoregressive multicapitate transformer whose decoder output heads correspond to the represented modalities. The method returns mixed modality output representations of proteins or small molecule drugs for synthesis or manufacture.

The invention provides a preparation method of cereal fermentation broth postbiotics and application of the cereal fermentation broth postbiotics in improvement of systemic chronic inflammation and reduction of cholesterol and low-density lipoprotein, and belongs to the technical field of fermentation engineering. The invention provides a preparation method of cereal fermentation broth metabiotics, which is characterized in that mixed cereals are used as raw materials, anaerobic fermentation is carried out by using compound enzymes and various bacteria, and polysaccharides and proteins in the cereal raw materials can be quickly converted into functional small molecular substances, such as polypeptides, total phenols and total flavonoids. The cereal fermentation broth metagen can inhibit secretion of a macrophage proinflammatory medium, inhibit generation of inflammatory factors of liver, heart and intestinal tissues, and improve activation of adipose tissue macrophages related to body inflammation. After the cereal fermentation liquor is subjected to post-biogen treatment, glucose and lipid metabolism disorder can be effectively improved, liver function damage can be relieved, and the intestinal barrier function can be effectively improved.

The present invention relates to novel compounds that inhibit Nav1.8 sodium channels, methods of making, and methods of using thereof. The present disclosure is further directed to administering the disclosed compounds as therapeutic solutions for acute, chronic, and neuropathic pain to a subject in need thereof.

Provided herein are lipid compounds, e.g., a compound of Formula (I) comprising an amine (heterocyclic) "head group" and a "hydrocarbon tail" moiety, and pharmaceutical compositions thereof. Also provided are lipid nanoparticles, each comprising a lipid compound of Formula (I), as a promising delivery vehicle for a variety of therapeutic agents, including small molecule drugs, proteins, and nucleic acids.

A three-dimensional scaffold for use in engineered tissue includes a repeated 3D geometry; and at least one of a hydrogel, a biocompatible polymer, and a bioprintable polymer. The repeated 3D geometry may include an open geometry including a plurality of interconnected nodes configured to be seeded with living cells. The scaffold may be formed via bioprinting. The three-dimensional scaffold may also be used for (1) 3D tissue modelling (for liver, kidney, gut, pancreas, heart, lung, spleen, etc.), (2) disease modeling of different tumor types such as breast, colorectal, lung, liver, brain, ovarian and others, (3) drug testing / therapeutic screening of small molecule drugs, peptides, proteins, antibodies, ADCs, gene therapies, RNA-based therapeutics, cell therapies, and tissue therapies, and (4) therapeutic / drug delivery (i.e., via delivery device that can be used to control drug release based on different patterns).

The invention discloses a novel application of a small molecule compound BRD4780 in resisting ricin, the small molecule compound BRD4780 has a remarkable effect of resisting ricin toxicity and can be used in development of anti-ricin drugs, a brand new candidate molecule is provided for development of the anti-ricin drugs, the drug research and development blank in the field is filled, and the application of the small molecule compound BRD4780 in resisting ricin is developed. The method has important significance in the aspects of clinical treatment, biological protection and immunotoxin treatment safety optimization, and is wide in application prospect.

Methods and apparatus for obtaining representations of proteins and small molecule drugs for synthesis; wherein pre-trained mixed modality protein and natural language fusion models are further trained by supervised fine tuning using reasoning-oriented query—chain-of-thought (CoT) response pairs. The resulting reasoning-oriented neural network is then used to obtain representations of output proteins or small molecule drugs, in response to mixed modality reasoning-oriented input queries specifying conditions on the output. In one embodiment, the neural network is an autoregressive multicapitate transformer whose decoder output heads correspond to the represented modalities. The method returns mixed modality output representations of proteins or small molecule drugs for synthesis or manufacture.

Disclosed are small molecule inhibitors of αvβ6 integrin, and methods of using them to treat a number of specific diseases or conditions.

The invention discloses an ulva lactuca composite wall-breaking enzymolysis fermentation product as well as a preparation method and application thereof, and relates to the field of cosmetics. The preparation method comprises the following steps: soaking ulva powder, and performing physical cell wall breaking treatment; mixed enzymes are added for an enzymolysis reaction, wherein the mixed enzymes comprise lipase, cell wall breaking enzyme, enzyme and protease; adding the enzymolysis product into a culture medium, and inoculating bacterial liquid for fermentation culture to obtain fermentation liquid. According to the application, active ingredients such as macromolecular polysaccharide and protein in the ulva lactuca are extracted and decomposed by adopting physical cell wall breaking, composite enzymolysis and bifidus yeast fermentation technologies, and the prepared fermentation product is rich in various composite micromolecular active ingredients such as oligosaccharide, polypeptide, amino acid, polyphenols and flavonoids, has high free radical scavenging capacity, and can be used for preparing the ulva lactuca beverage. The anti-wrinkle and anti-oxidation composition has good anti-wrinkle and anti-oxidation effects, is beneficial to skin absorption when being applied to cosmetics and has high absorption efficiency, and the prepared cosmetics have excellent anti-wrinkle, anti-oxidation, soothing and repairing effects.

An objective of the present disclosure is to provide anti-CD137 antigen-binding molecules which have immunocyte-activating effect, cytotoxic activity, or anti-tumor activity, and meanwhile have reduced effect on non-tumor tissues such as normal tissues and produce less side effects, and methods of using the same.Anti-CD137 antigen-binding molecules which have immunocyte-activating effect, cytotoxic activity, or anti-tumor activity, and meanwhile have reduced effect on non-tumor tissues such as normal tissues and produce less side effects, are provided by discovering and producing CD137 antigen-binding molecules whose binding activity to CD137 depends on various substances (for example, small molecule compounds) in target tissues. Methods of using the same, pharmaceutical formulations, and such are also provided.The present disclosure also provides an antigen-binding molecule whose binding activity to an antigen varies depending on a small molecule compound, a preparation method thereof, and uses thereof.

The invention belongs to the field of functional proteomics research, and particularly relates to a combined analysis method for analyzing interaction between a small molecule substance and a targeted protein, which is used for analyzing the small molecule substance and the protein by adopting LiP-MS (Limited Protein-Mass Spectrometry) technology and phosphorylated proteome combined analysis. According to the method, the optimized LiP-MS technology is adopted, the target protein can be directly recognized under the complex proteome background without enriching specific protein, and the problem that low-abundance protein is difficult to detect is solved; phosphorylated proteome abundance transformation protein is analyzed by combining high-resolution mass spectrometry, so that the recognition capability on a drug target and a shear variant thereof is enhanced, and the detection sensitivity is improved.

The invention provides a new drug molecule design method and device fusing convex optimization and evolutionary learning, and belongs to the field of biological information.The method comprises the steps that in a generative adversarial network, a generator is adopted to generate a small molecule sequence, and the generator is established by adding an attention mechanism model in a long-short-term memory network; evaluating the authenticity of the small molecule sequence by adopting a discriminator, wherein the discriminator is established by adopting a convolutional neural network improved based on convex optimization; updating the parameters of the generator by adopting a strategy gradient method, and updating the parameters of the discriminator by adopting a gradient descent method; and generating a final small molecule sequence by the generator corresponding to the final generator parameter. According to the method, the small molecules which are highly similar to original samples and have higher effectiveness and innovativeness can be generated, the diversity and quality of the generated molecules are improved, and particularly, the method has excellent performance in the aspect of generating molecules with specific functions.

The invention discloses application of a small molecule compound in preparation of a product for treating nervous system diseases. According to the application disclosed by the invention, it is determined for the first time that Chebulinic acid and 1, 1, 1-Kestohexenose are targeted PU.1 inhibitors, nerve cell activity decline caused by A beta deposition can be improved, and a new technical choice is provided for developing a treatment method for nerve injury diseases and protecting or improving nerve cell injury.

The invention provides a micromolecular multifunctional information peptide and application thereof, and belongs to the technical field of active peptide raw material development. The sequence of the small-molecule multifunctional information peptide is VHPYVPR, the small-molecule multifunctional information peptide can be effectively combined with a downstream receptor of EGF, the EGF function is simulated, and meanwhile the situation that use of existing cell growth factor raw materials in the field of cosmetics is limited due to the molecular weight problem is avoided. Experiments prove that the micromolecular multifunctional information peptide provided by the invention can promote the repair of skin damage phenomena such as scratches, inhibit the release of inflammatory factors, inhibit the activity of beta-galactosidase and promote the generation of I-type, III-type and XVII-type collagen, shows excellent repair, soothing and anti-aging functions, is high in permeability and has a wide application prospect.

Provided is an antibacterial peptide having an amino acid sequence X1KRFKKFFX2KLKKWV-NH2, wherein X1 is selected from any one or of amino acids A, C, D, E, F, G, H, K, L, N, M, P, Q, R, S, I, V, W, Y, and T or is absent; and X2 is an amino acid having an aromatic side chain or an amino acid having an alkaline side chain. In view of defects such as poor gastrointestinal fluid stability of antibacterial peptides in the prior art, a brand-new sequence design scheme and preparation method for an antibacterial peptide are provided. By means of a complete or partial D-amino acid substitution or structural derivatization of a peptide sequence, a series of antimicrobial peptides having stronger antibacterial activity and gastrointestinal stability as compared with the prior art are obtained, such that the antibacterial peptides have a wider application range and higher development potential value.

The invention relates to an adjusting system applied to continuous kidney replacement treatment of acute kidney injury patients. Comprising the following steps: capturing the blood flow velocity and vascular endothelial permeability of glomerular capillaries in real time by using a micro sensor or a nano-scale optical imaging technology; the method comprises the following steps: pre-judging a risk time point of insufficient tissue perfusion through dynamic modeling of a capillary structure and a functional relationship; combining the microcirculation data with conventional biochemical indexes of the patient to create an early intervention model; when it is monitored that microcirculation perfusion is greatly reduced or kidney oxygen supply is insufficient, continuous renal replacement therapy CRRT parameter fine adjustment is triggered in advance; the method comprises the following steps: collecting plasma toxins of different patients at clinical and molecular levels, and constructing a common toxin map of the acute kidney injury AKI; whether the specific toxin concentration exceeds the standard or not is judged by combining a real-time sensor, and the removal priority is output in real time; a membrane material with an adjustable aperture or a special coating is adopted, so that inflammatory mediators and bacterial endotoxin molecules are adsorbed or intercepted, and the permeability of micromolecular electrolyte is kept.