128 results about "Active metabolite" patented technology

The invention discloses a method for improving beef quality, an action mechanism and an experimental method, in a cattle body, vitamin A can activate the expression of EBF2 through an active metabolite RA of the vitamin A, and the EBF2 can inhibit the transcription process of CYP26B1 in a targeted manner to maintain the activity of a retinol signal channel, so that PPAR gamma and downstream lipid metabolism related genes thereof are activated, and the activity of the retinol signal channel is improved. Fatty acid transport and lipid accumulation in fat cells in the cattle muscle are promoted, fat deposition in the cattle muscle is promoted, and the beef quality is improved. By constructing the molecular network for regulating and controlling the formation of the fat in the cattle muscle, a complex regulation and control mechanism for controlling the fat deposition in the cattle muscle can be understood more deeply, a method for improving the beef quality based on regulating and controlling the vitamin A mediated key factor EBF2 is provided, and a new way is provided for improving the beef quality in a targeted manner.

The present application relates to a sustained release delivery composition of a vesicular monoamine transporter type 2 (VMAT2) inhibitor, a deuterated derivative thereof, a pharmaceutically acceptable salt thereof, an active metabolite thereof, or a prodrug thereof for treatment of hyperkinetic movement disorders including, but not limited to, tardive dyskinesia (TD), Huntington's disease (HD) chorea, tremors, dystonia, chorea, tics, myoclonus, stereotypies, restless legs syndrome, and various other disorders with abnormal involuntary movements. The present application also relates to a sustained release delivery composition of an antipsychotic agent, a pharmaceutically acceptable salt thereof, an active metabolite thereof, or a prodrug thereof for treatment of schizophrenia, bipolar disorder, and other psychiatric diseases or disorders. The method of making or using the composition is also disclosed.

The invention discloses application of a plant lactobacillus CCFM1357 to conversion of anthocyanin to generate various active metabolites, inhibition of a cGAS-STING pathway and enhancement of improvement of brain aging, and belongs to the technical field of microorganisms and the technical field of medicines. The phytobacterium plantarum CCFM1357 fermented anthocyanin and the compound preparation thereof provided by the invention have the following effects: (1) a marker for relieving D-gal induced mouse brain senescence and a marker for relieving D-gal induced mouse brain senescence; (2) promoting and relieving D-gal induced mouse histopathologic characterization; (3) relieving D-gal induced mouse neuroinflammation; (4) relieving behavioral characterization of the D-gal induced aging mouse; and (5) a cGAS-STING signal channel is inhibited. The phytobacterium plantarum CCFM1357 fermented anthocyanin and the compound preparation thereof provided by the invention can be used for a product for relieving brain aging, and have a huge application prospect.

The invention belongs to the field of probiotics and application thereof, and particularly relates to a humanized bifidobacterium animalis probiotic strain and application thereof in preparation of drugs for preventing or treating melanoma. The preservation number of the humanized bifidobacterium animalis is GDMCC No: 65044, the preservation unit is called GDMCC for short, and the active metabolite of the humanized bifidobacterium animalis contains mannose. The composition contains the bifidobacterium animalis probiotic strain, and contains / does not contain metabolites of the bifidobacterium animalis probiotic strain and one or more physiologically acceptable excipients or carriers. The method has the advantages that the protective strain lacked by the melanoma patient is screened and separated from the intestinal tract of a healthy person, the strain can normally survive in the intestinal tract of the human body and has no toxic or side effect, and a new way is provided for prevention and treatment of the melanoma patient by supplementing the lacked protective strain and active metabolites of the patient in a targeted manner; and an innovative solution is provided for auxiliary immunotherapy of melanoma.

The invention discloses low-GI probiotic compound coarse cereal meal replacement powder and a preparation method thereof. The preparation method comprises the steps of raw material and auxiliary material treatment, starch enzymolysis, strain activation culture, fermentation, freeze drying, blending and packaging and the like. The black tartary buckwheat, the black beans, the black sesame, the black rice and the black mulberries are used as main raw materials, good growth conditions are created for lactic acid bacteria by means of an amylase enzymolysis technology, and further the cereals are subjected to synergistic fermentation by inoculating a strain suspension of lactobacillus reuteri and lactobacillus rhamnosus, so that the nutritional value is increased, bioactive metabolites are added, and the nutritional value is increased. And the flavor and taste of the grains are also improved. Compared with common commercially available meal replacement powder, the product realizes directional domestication fermentation of probiotics in a composite coarse cereal environment, so that the product has high viable organism stability, ensures the colonization ability of the probiotics in cereal powder, realizes synergistic improvement of nutrition and flavor, contains certain functional components, and has relatively good sugar controlling and stabilizing ability.

The invention relates to application of 9-cis-retinoic acid in preparation of products for treating, preventing or improving obesity, and belongs to the technical field of biological medicine. Experimental evaluation of obese mice induced by high-fat diet proves that the 9-cis-retinoic acid can reduce blood fat and improve the glycometabolism function, and lipid accumulation of the liver is improved mainly by increasing expression of main regulatory protein PPAR-alpha oxidized by liver beta, so that the 9-cis-retinoic acid can be used for preparing medicines for treating obesity. The traditional Chinese medicine composition can be used for treating, preventing or improving metabolic symptoms caused by high fat diet, and a new strategy is provided for treating obesity and related metabolic syndromes. Besides, 9-cis-retinoic acid is a natural active metabolite of vitamin A, does not show obvious toxic reaction in animal experiments, and has better biocompatibility.

The invention discloses a kit for simultaneously determining five liver cancer multi-kinase targeted drugs and active metabolites thereof based on LC-MS / MS. The kit comprises an internal standard solution, a standard substance solution, a protein precipitant and a solution used as a mobile phase, the internal standard solution is a gefitinib solution; the standard substance solution is a solution of sorafenib, sorafenib nitric oxide, lenvatinib, lenvatinib nitric oxide, dorafenib, dorafenib nitric oxide, regorafenib, regorafenib nitric oxide, cabozatinib and cabozatinib nitric oxide; the protein precipitant is an ice acetonitrile solution; the mobile phase comprises a mobile phase A and a mobile phase B, the mobile phase A is an aqueous solution containing formic acid, and the mobile phase B is an acetonitrile solution containing formic acid. The invention also discloses a method for determining the liver cancer multi-kinase targeted drug and the active metabolite thereof. The method can be used for monitoring drug concentration and preparing a drug time monitoring curve, and can simultaneously improve the sensitivity and selectivity of the method and shorten the analysis time so as to improve the analysis flux.

The invention relates to the technical field of medicines, and discloses an application of combination of bufalin and heme in preparation of a cancer treatment medicine. According to the invention, by means of an active metabonomics means, a key active metabolite-heme is locked through exogenous library screening and endogenous analysis, and the drug effect of bufalin is regulated by means of the active metabolite. Through verification, it is found that heme can cooperate with the synergistic drug effect in various cancer cell lines, and a new technical normal form based on an active metabolome for improving the drug effect of bufalin is provided. The pharmaceutical composition can improve the apoptosis induction ability of bufalin to different cancer cells, and provides powerful guiding significance for developing a novel treatment scheme in clinical medicine.

The present application relates to the field of traditional Chinese medicine, in particular to a composition, eye patch and preparation method thereof for preventing and treating eye dryness, blurred vision fatigue and dry eye, comprising a carrier vehicle and a matrix layer, selecting medicinal materials with the effects of improving eyesight and resisting oxidation, fermenting the medicinal materials with plant lactic acid bacteria, bacillus or yeast to decompose macromolecules into small molecule active substances and possibly produce new active metabolites, adopting temperature control during the fermentation process to avoid high temperature from destroying heat-sensitive components, compounding the fermented medicinal material extract with hyaluronic acid, menthol, carboxymethyl cellulose and glycerol to form an intelligent rheological regulation body, hyaluronic acid synergistically enhances the moisturizing effect with the fermented extract, carboxymethyl cellulose serves as a film-forming agent to ensure the stability of the matrix layer, and glycerol improves the moisturizing performance, adopting a green process of activation, fermentation, mixing, loading and sterilization, selecting plant fibers as the carrier vehicle, cutting and packaging after loading the matrix layer, and then sterilizing to ensure the safety and effectiveness of the product.

This invention provides a method for treating a pulmonary arterial hypertension with reduced incident of side effect using a controlled release pharmaceutical composition of selexipag or its active metabolite, wherein the controlled release pharmaceutical composition of selexipag or its active metabolite following oral administration with an alcoholic beverage reduces incidence of at least one side effect associated with the selexipag or its active metabolite compared to the immediate-release dosage form comprising the same amount of the selexipag or active metabolite thereof.

To provide a novel tetracycline derivative having reduced antimicrobial activity for use in treating disorders of the central nervous system.SOLUTION: Provided are novel molecules comprising a modified tetracycline molecule including Deamino Diacetyl Minocycline, Methyl Ether Minocycline, Ethyl Ether Minocycline, Propyl Ether Minocycline, Butyl Ether Minocycline, Butyl Ether Monoacetyl Minocycline, Butyl Ether Diacetyl Minocycline, Butyl Ether Triacetyl Minocycline, or Butyl Ether Tetra Acetyl Minocycline, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, and tautomers thereof, and methods for using the same to treat Alcohol Use Disorder (AUD), Substance Use Disorder (SUD), tobacco use, pain, or proinflammatory disorders.SELECTED DRAWING: None

BA-1049 (R) and its active metabolite are disclosed. Also disclosed are pharmaceutical formulations containing BA-1049 (R) or its active metabolite.

The invention discloses a strain of parateratomycosis aveosphaeroides and application thereof, and belongs to the technical field of microorganism and biological prevention and control. In order to screen new species of fungi and provide alternative strains for application of plant beneficial bacteria in agriculture, a fungus SGSF1293 is separated, and the fungus SGSF1293 is identified to be a new species of the cystis clavatum and is named as the parateratosis aveoensis, and the new species of the cystis clavatum is named as the parateratosis aveoensis. According to the present invention, the activity research results show that the strain SGSF1293 has rice root-knot nematode killing activity, plant pathogen resistance (Brassica oleracea black rot xanthomonas, Pseudomonas syringae, Ralstonia solanacearum and Fusarium oxysporum) resistance, oxidation resistance and phosphorus solubilizing activity; besides, the secondary metabolite of the strain is separated and identified, two active compounds, namely, wintergreen ambrotic acid and brefeldin A, are separated, and the wintergreen ambrotic acid has the activity of killing rice root-knot nematode. The discovery of the strain SGSF1293 and the active metabolite thereof has certain application value in the agricultural fields of plant disease control and the like.

Fatty acids with one or more unsaturations and an odd-numbered hydrocarbon chain are described, wherein these fatty acids have the chemical structure of the therapeutically active metabolites of alpha-hydroxylated mono- or polyunsaturated fatty acids with an even-numbered chain. The compositions comprising these fatty acids, their medical uses, and their use as indicators of a patient's efficacy and / or response to treatment with the alpha-hydroxylated mono- or polyunsaturated fatty acids with an even-numbered chain from which they are derived are also described.

The invention belongs to the technical field of medicines, and relates to a compound as shown in a formula I, a stereoisomer, a prodrug and a pharmaceutically active metabolite thereof, pharmaceutically acceptable salt, a solvate and a hydrate thereof, a pharmaceutical composition containing the compound, and application of the compound in preparation of medicines for preventing and / or treating diseases or symptoms related to virus infection.

The present invention relates to a compound of formula I or a pharmaceutically acceptable salt, a solvate, an active metabolite, a polymorph, an ester, an optical isomer or a prodrug thereof, a pharmaceutical composition comprising the compound of formula I, and use of the compound, as a Bruton's tyrosine kinase inhibitor with high selectivity for BTK(C481S) mutant, in the manufacture of a medicament for preventing or treating a heteroimmune disease, an autoimmune disease or a cancer.

The invention relates to the technical field of biological detection, and particularly discloses a method for simultaneously determining serum concentrations of an anti-epileptic drug and active metabolites thereof based on an LC-MS / MS (Liquid Chromatography-Mass Spectrometry / Mass Spectrometry) method. According to the method, the C18 chromatographic column with the filler particle size of 3.0 microns is selected for the first time, efficient separation of lamotrigine, levetiracetam, oxcarbazepine and active metabolites thereof is achieved, and the separation efficiency is equivalent to that of a small-particle-size column; a pretreatment process is simplified by precipitating protein through a single organic solvent, and accurate quantification of four components is completed by only using two isotope internal standard oxcarbazep-d4 and levetiracetam-d6, so that the cost is reduced. In the aspect of the detection range, the lower quantification limit of oxcarbazepine is broken through to 0.04 [mu] g.mL <-1 >, and the technical contradiction between oxcarbazepine and the upper quantification limit (as high as 50 [mu] g.mL <-1 >) of LEV across three orders of magnitude is overcome. According to the scheme, hardware requirements and reagent cost are reduced, and meanwhile, high sensitivity and a wide linear range are achieved.

Provided are a compound of formula (I), or a pharmaceutically acceptable salt, solvate, active metabolite, polymorph, isotopic label, isomer or prodrug thereof, and a use thereof. The above-mentioned compound has a very strong inhibitory effect on the FGFR4 kinase activity and the proliferative activity of Hep 3B cells with high FGFR4 expression.

The invention discloses a lactobacillus paragasseri strain capable of converting anthocyanin to generate various active metabolites, inhibiting NF-kappa B and cGAS-STING signals and enhancing inflammatory response relieving, and belongs to the technical field of microorganisms and the technical field of medicines. The lactobacillus paragasseri CCFM1499 provided by the invention can be used for converting anthocyanin into various active substances such as homovanillic acid, cyanidin, 3 ', 4'-dihydroxyphenylacetic acid and the like; fermentation supernate obtained by fermenting anthocyanin through the lactobacillus paragasseri CCFM1499 has the following effects: (1) the capability of reducing inflammatory factors of cells is achieved; (2) the cell senescence phenotypic capability is relieved; (3) the cGAS-STING signal channel capability is inhibited; and (4) inhibiting the NF-kappa B signal path capability. The lactobacillus paragasseri CCFM1499 fermented anthocyanin provided by the invention can be used for preparing a product for relieving inflammatory response, and has a huge application prospect.

This disclosure provides the use of valbenazine, its active metabolites, or pharmaceutically acceptable salts thereof in the preparation of megakaryocytes, wherein the preparation of megakaryocytes is carried out in vitro. The valbenazine, its active metabolites, or pharmaceutically acceptable salts thereof in this disclosure can promote megakaryocyte proliferation and platelet production, providing a promising strategy for megakaryocyte proliferation and platelet production.

A biphenyl derivative having a structure represented by formula I or a pharmaceutically acceptable salt, an ester, an amide, a solvate, an active metabolite, a polymorph, an isotopically labeled substance, an isomer or a prodrug thereof, and a pharmaceutical composition containing the same. The derivative is designed on the basis of a plurality of Wnt upstream kinases with similar structures, and can regulate the pathway by means of at least one Wnt upstream pathway. The derivative increases the expression of reprogramming core genes Oct4, Lin28A and c-Myc when existing independently, and can thus be well applied to cell reprogramming.

The present invention provides compounds of formula (I) and / or salts thereof and / or biologically active metabolites thereof and / or prodrugs thereof and / or solvates thereof and / or hydrates thereof and / or polymorphs thereof having affinity and selectivity for the gamma-aminobutyric acid A receptor subunit alpha 5 and act as GABAA α5 positive allosteric modulators, thereby useful in the treatment or prevention of diseases related to the GABAA α5 receptor, process for the preparation and intermediates of the preparation process thereof, pharmaceutical compositions comprising them alone or in combination with one or more other active ingredients and their use as medicaments.

The invention discloses a lactobacillus paracasei capable of converting anthocyanin to generate various active metabolites and enhancing the effect of relieving cognitive impairment and neuroinflammation, and belongs to the technical field of microorganisms and the technical field of medicines. The lactobacillus paracasei CCFM1497 obtained through screening is combined with anthocyanin intake in animal experiments, and by inhibiting a cGAS-STING signal channel, brain inflammatory response of senescence individuals is effectively relieved, senescence-related cognition and behavior degeneration performance is improved, and brain senescence is delayed. The lactobacillus paracasei CCFM1497 fermented anthocyanin and the compound preparation thereof provided by the invention can be used for products for relieving cognitive impairment and neuroinflammation, and have a huge application prospect.

The present invention provides compounds of formula (I) and / or salt thereof and / or biologically active metabolite thereof and / or prodrug thereof and / or solvate thereof and / or hydrate thereof and / or polymorph thereof having affinity and selectivity for the gamma-aminobutyric acid A receptor subunit alpha 5 and act as GABAA α5 negative allosteric modulators, thereby useful in the treatment or prevention of diseases related to the GABAA α5 receptor, process for the preparation and intermediates of the preparation process thereof, pharmaceutical compositions comprising them alone or in combination with one or more other active ingredients and their use as medicaments.

Provided is a pharmaceutical composition comprising a sulfonamide derivative represented by the following formula (1), a pharmaceutically acceptable salt thereof, or an active metabolite thereof, and having improved absorbability when orally administered. Disclosed is a self-emulsifying composition comprising: a sulfonamide derivative represented by the following formula (1), a pharmaceutically acceptable salt thereof, or an active metabolite thereof; and at least two solubilizers.

The invention discloses a two-way positioning release sustained-release pharmaceutical composition and a preparation method thereof, the pharmaceutical composition is a double-layer tablet, and the double-layer tablet comprises an upper-layer tablet and a lower-layer tablet. The upper-layer tablet is a slow-release intragastric positioning release preparation part and contains 1 / 3 marked amount of active ingredients; the lower-layer tablet is a quick-release gastrointestinal tract release preparation part and contains 2 / 3 labeled amount of active ingredients. A new preparation technology and a new dosage form are adopted, the lower-layer tablet in the double-layer tablet can enable the medicine to be rapidly disintegrated in the stomach, the disintegrated medicine forms a particle dispersion, and the particle dispersion can be rapidly emptied by the stomach to enter the intestinal tract, so that the absorption of the medicine is promoted; the upper-layer tablet floats in the stomach after absorbing water, then the medicine is slowly dissolved out, the medicine dissolved out of the preparation can be metabolized into active metabolite OP-1118 in an acid environment in the stomach, then the active metabolite OP-1118 is absorbed through the gastrointestinal tract, and part of the medicine can be absorbed immediately after uniformly and slowly entering the intestinal tract, so that the bioavailability is improved.

The present invention relates to a composition comprising a) at least one biological control agent which is a fungicidally active bacterium and / or a fungicidally active metabolite produced by the respective bacterium and b) one or more fatty acids or derivatives thereof selected from unsaturated and saturated C12-24 fatty acids, salts thereof, esters thereof or mixtures of any of the foregoing as well as methods of using this composition and related uses.

The invention discloses a Lactobacillus paracasei 1029 and application thereof, the preservation number of the Lactobacillus paracasei 1029 is CCTCC (China Center for Type Culture Collection) NO: M20251441, and the Lactobacillus paracasei 1029 is preserved in the China Center for Type Culture Collection on June 23, 2025. The fermentation product contains a plurality of active metabolites, such as pyruvic acid, pantothenic acid, proline and leucine, and the components synergistically enhance the effects of oxidation resistance, bacteriostasis and cell melanin inhibition. Compared with the prior art, the fermented product disclosed by the invention realizes integration of multiple effects, is high in safety (free of cytotoxicity) and simple in preparation process (standing for 6 days at 30 DEG C, filtering, centrifuging, freezing and drying), has wide application prospects including food additives, health-care products, cosmetics and pharmaceutical preparations, and can remarkably improve the bioavailability and market competitiveness of products.

The present application relates to the technical field of probiotic composition, and discloses a bacterial agent for regulating vaginal microbial flora and a preparation method thereof, which comprises the following steps: preparing Lactobacillus paracasei KFY202407 powder into a seed solution; performing segmented fermentation culture on the seed solution; obtaining bacterial slurry after centrifugal enrichment of the fermentation product; mixing the bacterial slurry with a composite freeze-drying protective agent and then performing freeze-drying to obtain freeze-dried bacterial powder; and performing gelatinization treatment on the freeze-dried bacterial powder to obtain the bacterial agent. The present application realizes rapid proliferation of bacterial cells and promotes accumulation of active metabolites by adopting a two-stage fermentation process of liquid-state fermentation followed by solid-state fermentation, thereby solving the technical problems of low active bacterial proliferation efficiency and insufficient metabolites in the prior art. Meanwhile, the present application adopts a freeze-drying process of two-stage pre-freezing and drying sublimation, so that ice crystals are removed in the form of sublimation instead of melting, thereby solving the technical problem of bacterial cell damage and uncontrollable inactivation due to ice crystals in the traditional freeze-drying technology.

A method for treating patients with NOTCH3 mutations using a rho kinase inhibitor has been disclosed. Abnormal NOTCH3 signaling is a pathological factor in cerebral small vessel diseases, including CADASIL. A preferred embodiment relates to treating patients orally with the rho kinase inhibitor fasudil or its active metabolite hydroxyfasudil.