450results about "Dipeptide ingredients" patented technology

The present disclosure provides bifunctional compounds as HPK1 degraders via the ubiquitin proteosome pathway and methods for treating diseases modulated by HPK1. The present invention provides novel bifunctional compounds for proteolytically degrading hematopoietic progenitor kinase (HPK1) and methods for treating diseases modulated by HPK1. HPK1 can be targeted for degradation, thereby providing therapeutic opportunities in enhancing anti-tumor immunity and increasing responses to checkpoint receptor blockade.

Use of an active peptide in the manufacture of a product to improve the skin barrier and promote collagen expression and / or increase skin elasticity and suppleness and / or reduce wrinkles, characterized in that the active peptide has the structural formula HA-OH, wherein A comprises at least two amino acid residues, and the amino acid residues comprise at least one from Hyp, Gly, Pro and Ala.

To provide a compound that can be readily synthesized, exhibits antibacterial activity against Porphyromonas gingivalis being a pathogenic bacterium of periodontitis, with greater specificity, and exhibits increased stability against esterase as well as reduced cytotoxicity.SOLUTION: The present invention provides a compound represented by a general formula (1) [where R1 is a halogen atom or a nitro group, and R2 is an alkoxy group or an acylamino group] or a salt thereof or a solvate thereof.SELECTED DRAWING: None

The invention relates to a Pan KRAS protein degradation agent as well as a preparation method and application thereof. Specifically, the compound provided by the invention has a structure as shown in a formula I. The invention also discloses a preparation method of the compound and application of the compound in prevention and / or treatment of KRAS mutation related diseases.

Disclosed herein are compositions and methods for promoting weight loss and / or preventing obesity; enhancing athletic performance / endurance; enhancing muscle function; enhancing cognitive function; promoting weight management; enhancing cardiovascular health; enhancing blood flow; reducing inflammation; and / or regulating immunity.In certain embodiments, the disclosed method comprises administering to subject the composition comprising the combination of dileucine and paraxanthine, and / or dileucine and L-arginine, and / or dileucine and leucine.

The present invention relates to a compound, aprocitentan, {5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yl-oxy)-ethoxy]-pyrimidin-4-yl}-sulfamide; and its use as an endothelin receptor antagonist in a method of treating hypertension, including resistant hypertension in a subject, the use comprising administering to a subject in need thereof a pharmaceutical composition comprising a clinically effective amount of aprocitentan or a pharmaceutically acceptable salt thereof. 【Chemical 1】 TIFF2025519101000003.tif76153

An object of the present invention is to provide a small molecule compound (IL-17 activity inhibitor) having a more potent inhibitory effect on IL-17 activity than conventional compounds. The IL-17RA inhibitor of the present invention is, for example, a small molecule compound surrounded by Phe60, Gln87, Asp121, Pro122, Asp123, Gln124, Asp153, Cys154, Glu155, Lys160, Pro164, Cys165, Ser167, Ser168, Gly169, Ser170, Leu171, Trp172, Asp173, Pro174, Pro254, Phe256, Ser258, Cys259, Asp262, Cys263, Leu264, and His266, which are contained in the extracellular domain of human interleukin-17 receptor A (IL-17RA). The compound contains a compound having the effect of inhibiting the binding of interleukin-17A (IL-17A) to IL-17RA in humans, etc., or a pharmaceutically acceptable salt, solvate, or prodrug thereof, which can bind to IL-17RA through non-covalent interactions, including van der Waals forces acting between at least 13 of these amino acid residues in the space defined by the compound, and preferably further including at least one type of intermolecular interaction selected from the group consisting of ionic bond, hydrogen bond, C-H-π interaction, and hydrophobic interaction acting between predetermined ones of the amino acid residues.

The application discloses a pyrrolobenzodiazepine-anthracene imide hybrid molecule and a preparation method and application thereof, and belongs to the technical field of chemical medicines. In order to solve the problems of few kinds of warheads of an existing antibody drug conjugate, single action mechanism and drug resistance easily generated in long-term use, a pyrrolobenzodiazepine-anthracene imide hybrid molecule shown in formula I and a preparation method and application thereof are provided. Experimental results show that the compound has strong anti-proliferation activity in various tumor cells such as ovarian cancer cells, gastric cancer cells and breast cancer cells, and an antibody drug conjugate thereof has good in-vivo and in-vitro anti-tumor activity and good safety.

This disclosure provides methods and reagents useful for analyzing protein-protein interfaces, such as the interface between a presenter protein (e.g., a member of the FKBP family, a member of the cyclophyllin family, or PIN1) and a target protein. [Solution] In some embodiments, the target and / or presenter protein is an intracellular protein. In some embodiments, the target and / or presenter protein is a mammalian protein.

Bioactive walnut peptides and use of the bioactive walnut peptides for topical application to the scalp are described. The bioactive walnut peptides may be incorporated into a pharmaceutical or cosmetic composition for application to the scalp. The pharmaceutical or cosmetic compositions and the one or more bioactive walnut peptides in the compositions are particularly useful for treating or preventing hair loss, and treating scalp conditions, such as dandruff, scalp psoriasis, and acne.

Novel compounds that act as inhibitors of alpha4beta7 integrin are disclosed. Pharmaceutical compositions and methods of use of inhibitors of [alpha] 4 [beta] 7 integrin are disclosed. In particular, methods of using the [alpha] 4 [beta] 7 inhibitors in the treatment of diseases or conditions associated with inflammatory bowel diseases, including ulcerative colitis and Crohn's disease.

The application discloses a compound capable of inducing SOS1 protein degradation, a preparation method and purposes, and the structure of the compound is shown as formula I. The compound of the application can induce SOS1 protein degradation, is used as a SOS1 degrading agent, and is used for preventing and / or treating tumors. The SOS1 protein ligand-connecting group L-E3 ligase ligand (I).

The present invention relates to a cosmetic composition, advantageously an eco-biological cosmetic composition, comprising: - polyglutamic acid or a salt thereof; and - at least one peptide derivative represented by the general formula (I) in which: - R1 represents a hydrogen atom, an acyl radical or an acyloxy radical; and - R2 represents the side chain of an alpha-amino acid chosen from the group consisting of phenylalanine, glutamic acid, arginine, cysteine, methionine, histidine and tyrosine. The present invention also relates to the use of said cosmetic composition for combating skin redness and / or skin aging; to its use for preventing and / or combating cutaneous vascular hyperproliferation and / or cutaneous inflammation and / or rosacea; and to a method for selecting compounds suitable for preventing and / or combating these pathologies.

The present invention relates to a combination of a specific binding molecule that binds to human ANXA1 and a second active agent for use in the treatment of cancer. The second active agent includes thymidylate synthase inhibitors, nucleobase analogs, checkpoint inhibitors, proteasome inhibitors, taxanes, platinum-based chemotherapy agents, and nucleoside analogs. Suitable cancers for treatment include pancreatic cancer, colon cancer, breast cancer, lung cancer, myeloma, and mantle cell lymphoma. Also provided are related kits, products, and uses.

The present invention relates to novel use of a cathepsin L inhibitor Z-Phe-Tyr-CHO (C26H26N2O5), wherein the cathepsin L inhibitor Z-Phe-Tyr-CHO inhibits cancer progression and cachexia and muscle damage that are caused by cancer, and thus can be effectively used for preventing, ameliorating or treating cachexia and muscle loss, while having anticancer activity.

The application relates to the field of high polymer materials, in particular to an exosome composite material for treating periodontitis and a preparation method thereof. The exosome composite material comprises the following raw materials in parts by weight: 10-20 parts of a chitosan derivative, 10-20 parts of sodium hyaluronate, 1-5 parts of zein, 0.5-1 part of exosomes, 0.1-0.3 parts of phosphonodipeptide sodium and 60-70 parts of deionized water. The exosome composite material can inhibit periodontal pathogenic bacteria, reduce the expression of proinflammatory factors by inhibiting the signal pathways such as NF-kappa B, and thus relieve periodontal tissue inflammation.

The invention belongs to the technical field of biochemistry and functional polymer materials, and particularly relates to a polysaccharide-oligopeptide co-assembled intestinal flora regulation and control material and a preparation method thereof. The material is prepared from imine-boric acid ester double dynamic crosslinking modified chitosan, glycyl-tryptophan dipeptide, sodium lactate, citric acid, glycerol and a phosphate buffer solution. A reversible imine bond and a borate bond are introduced into chitosan molecules to construct a polysaccharide network with a double-dynamic crosslinking characteristic, and then the polysaccharide network and oligopeptide molecules are synergistically self-assembled to form a three-dimensional gel structure. The material has pH responsiveness, self-repairing property and slow-release function, and can realize continuous release of short peptides and selective regulation and control of probiotics in an intestinal environment. The prepared material is high in gel strength, good in structural stability and stable in oligopeptide release, and has remarkable promotion and inhibition selectivity on intestinal flora. The method provides an innovative co-assembly strategy for polysaccharide functionalization and micro-ecological intervention, and has a good application prospect.

The present invention provides topical compositions comprising a combination of an N-acyl dipeptide derivative and glycolic acid. The compositions provide enhanced penetration of the N-acyl dipeptide derivative into the skin.

The objective of this invention is to provide a highly safe, long-term-use, and excellent food-derived Netrin-1 production promoter. [Solution] White fungus exhibits excellent Netrin-1 production-promoting activity, and the combination of white fungus and imidazole dipeptide showed a particularly remarkable Netrin-1 production-promoting activity compared to white fungus and imidazole dipeptide alone. Therefore, white fungus, white fungus, and imidazole dipeptide can be used as foods, quasi-drugs, and pharmaceuticals with excellent Netrin-1 production-promoting activity.

The submicron sized particle is substantially spherical, comprising an oily core containing the peptide active and a wax shell that is solid at room temperature The particle is stabilized by an outer layer of a high-HLB non-ionic surfactant. The invention provides a method for obtaining an aqueous suspension of said particles with a satisfactory degree of encapsulation and improved long-term stability, for use in particular in the cosmetics industry. Peptide active associations can be considered, incorporated into the particles and adsorbed on the outside of the particles.

The invention relates to a controlled release granulate comprising: a microcrystalline cellulose core; a first coating comprising vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B9, vitamin B12, a source of Zn, R-lipoic acid, or an acceptable salt or racemate, L-carnosine or an acceptable salt, olive extract as hydroxytyrosol source, and at least one antioxidant, and a second coating deposited upon the first coating comprising a modified cellulose and / or an hydroalcoholic polymer. Also relates to a process to obtain such controlled release granulate and its use in a method to treat or prevent pain.

The present disclosure provides novel methods for treating or preventing amyotrophic lateral sclerosis (ALS), methods for delaying the onset of neurological symptoms associated with ALS, increasing survival in subjects afflicted with ALS, and attenuating the decline of muscle strength associated with ALS in a subject in need thereof. The present disclosure also provides methods for treating or preventing α-synucleinopathy or TDP-43 proteinopathy. The methods comprise administering to the subject an effective amount of a mitochondria-targeting peptidomimetic compound, such as (R)-2-amino-N-((S)-1-(((S)-5-amino-1-(3-benzyl-1,2,4-oxadiazol-5-yl)pentyl)amino)-3-(4-hydroxy-2,6-dimethylphenyl)-1-oxopropan-2-yl)-5-guanidinopentanamide, or a pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, and / or solvate thereof.

The application belongs to the field of pharmacy, and particularly relates to a whole-process targeting polypeptide molecule with the functions of targeting brain capillary endothelial cells, tumor neovascular endothelial cells, tumor pseudo vascular, tumor cells and tumor stem cells, a stable and optimized polypeptide molecule, and a modified complex and drug delivery system for tumor diagnosis and treatment. The application prepares a whole-process targeting polypeptide WVAP and a WVAP modified drug and high polymer carrier material, and applies the WVAP to the construction of a drug delivery system for tumor imaging and targeted therapy. The results show that the WVAP can cross the blood-brain barrier, target tumor neovascular and cross the blood-tumor barrier, target tumor pseudo vascular, tumor cells and tumor stem cells; and the nano drug delivery system constructed by the WVAP modified high polymer carrier material can effectively deliver the loaded drug to the brain, target tumor tissues, and significantly improve the anti-tumor efficacy.

Proteolytic targeting chimeras (PROTACs) are heterobifunctional degraders that specifically eliminate target proteins by hijacking the ubiquitin-proteasome system (UPS). Pharmaceutical compositions are provided that include a mixture of a PROTAC, a hydrophilic polymer, a surfactant, and optionally an acid and an adsorbent. Methods for preparing and using such pharmaceutical compositions are also described. In one aspect, an amorphous solid dispersion comprising a PROTAC is disclosed herein.

The present invention relates to monospecific or bispecific antibodies or antibody fragments or fusion proteins thereof capable of binding to the degradative portion (degron) of the VHL ligand VH032 (or derivatives thereof) of a targeted proteolytic chimera (PROTAC), and optionally to a target protein. The present invention also relates to conjugates of such antibodies or antibody fragments or fusion proteins with PROTACs (PAXs), as well as methods for their production, and their respective medical and non-medical uses.

The present disclosure provides, inter alia, compositions and methods for intranasal delivery of carnosine.

The present application relates to a kind of compound for targeted degradation GLI1 protein and its pharmaceutical use, belong to biological medicine technical field.The compound for targeted degradation GLI1 protein of the present application is composed of following three parts:G-L-E;E is the ligand of recruiting E3 ubiquitin ligase, L is connecting chain, G is the ligand combined with GLI1.The compound for targeted degradation GLI1 protein has excellent activity of targeted degradation GLI1 protein, has the prospect of developing into the drug of the disease treated or alleviated by targeted degradation GLI1 protein.

This invention belongs to the biomedical field and relates to the application of a compound in preventing the recurrence of calcium oxalate kidney stones. The application of the compound, or its pharmaceutically acceptable salts, esters, solvates, crystal forms, or prodrugs, in the preparation of reagents for preventing the recurrence of calcium oxalate kidney stones is described. The structure of the compound is as follows: [structure details missing]. The calcium oxalate kidney stones originate from Randall plaques. Extensive experimental evidence demonstrates that Benathin can enhance intercellular adhesion by repairing the adhesion protein network damaged by hydroxyapatite (HAP), thereby reversing epithelial damage, preventing epithelial cell detachment, and effectively protecting the renal papillary mucosal barrier, thus reducing the risk of stone formation and recurrence of calcium oxalate kidney stones.

The present invention relates to an IBAT inhibitor for use in the treatment of pruritus in certain chronic liver diseases such as non-alcoholic fatty liver disease (NAFLD) [newly reclassified as metabolic dysfunction-associated steatotic liver disease (MASLD)] which encompasses non- alcoholic fatty liver (NAFL) and non-alcoholic steatohepatitis (NASH) [newly reclassified as metabolic dysfunction-associated steatohepatitis (MASH)] with or without cirrhosis, and methods of treatment of pruritus in NAFLD (or MASLD), including NAFL and NASH (or MASH) with or without cirrhosis, comprising administering to said human a therapeutically effective amount of an IBAT inhibitor such as linerixibat.