55 results about "Aklanonic acid" patented technology

This invention discloses a method for synthesizing cefotiam, using 7-aminocephalosporanic acid (7-ACA) as the parent nucleus and introducing a 4-dimethylaminopyridine-dimethyl carbonate composite catalytic system. The reaction is carried out in a one-pot process involving 3-position nucleophilic substitution, 7-position amidation, and simultaneous deprotection in a green mixed solvent of ionic liquid [BMIM]BF₄-water with 1-(2-dimethylaminoethyl)-1H-5-mercapto-tetrazole and compound I. This method simplifies the process, improves selectivity, produces a high-purity product with stable yield, and is suitable for industrial production.

The invention discloses an agonist of a retinoic acid receptor beta and application of the agonist in preparation of a non-small cell lung cancer medicine in the technical field of biological medicine. The agonist of the retinoic acid receptor beta is saturated odd fatty acid heptadecanoic acid C17: 0; according to the research, the expression of a retinoic acid receptor beta can be up-regulated by adding heptadecanoic acid into the NSCLC cells, so that the sensitivity of the NSCLC cells to retinoic acid treatment is improved. When heptadecanoic acid and retinoic acid are combined for use, the activity and migration ability of NSCLC cells can be further inhibited, and apoptosis of the cells is promoted. The result shows that the heptadecanoic acid plays an important role in controlling the sensitivity of the NSCLC cells to the retinoic acid, the combined use of the heptadecanoic acid and the retinoic acid provides a new drug treatment means for treating the NSCLC, and the heptadecanoic acid and the retinoic acid have potential application value in preparing the drug for treating the non-small cell lung cancer.

The present invention relates to a liquid cleansing composition. Particularly, the present invention relates to a liquid cleansing composition that provides improved deposition of an active, an octadecanoic acid, when applied on to a surface. The composition comprises an octadecanoic acid and an organic acid with pKa from 2.5 to 4.9 wherein the organic acid is other than the octadecanoic acid.

The invention discloses application of a marker to preparation of a kit for diagnosing chronic obstructive pulmonary diseases. According to the application disclosed by the invention, the accuracy of diagnosing the chronic obstructive pulmonary disease by using (R)-3-hydroxytetradecanoic acid alone or in combination with the azelayl platelet activating factor is relatively high; on the basis of combination of (R)-3-hydroxytetradecanoic acid and an azelayl platelet activating factor, the compound is prepared. The compound can be further combined with one or two of 1-hexadecyl-2-(5-oxovaleryl)-sn-glycerol-3-phosphorylcholine, 1-O-hexadecyl-SN-glycerol-3-choline phosphoric acid, lauroyl-L-carnitine and beta-acetyl-gamma-O-alkyl-L-alpha-phosphatidylcholine to be used for diagnosing the chronic obstructive pulmonary disease. Therefore, a diagnostic kit for diagnosing the chronic obstructive pulmonary disease can be prepared on the basis of the scheme, and the kit contains a compound standard substance corresponding to the scheme and can also contain an internal standard compound for mass spectrum quantitative analysis.

This invention provides a physiological age prediction model that predicts the physiological age of a subject by detecting urinary proteins and metabolites in a urine sample. The aforementioned urinary proteins and metabolites are those that change significantly with age, including one or more selected from the following: cartilage intermediate layer protein (CILP2), collagen Alpha 1 chain (COFA1), myristic acid, 12-methyltridecanoic acid, CN family member 5 (CCN5), Sushi domain-containing protein 5 (SUSD5), procollagen C endopeptidase enhancer 1 (PCOLCE), and L-lactate oxidase (LOX), preferably including all of the aforementioned urinary proteins and metabolites.

This disclosure relates to hyaluronic acid nanoparticles containing an anticancer agent such as a NADPH oxidase (NOX) inhibitor for targeted delivery to cancerous cells or tumors. In certain embodiments, the nanoparticles are made up of hyaluronic acid conjugated to hydrophobic moieties. In certain embodiments, the hydrophobic moieties are steroid based compounds, such as 5beta-cholanic acid.

The present invention describes novel drug-carrying nanoparticles called bionanocarriers capable of modulating the cellular redox system and targeting the cancerous tumor.Specifically, the invention relates to a nanomedicine strategy for combating cancerous tumor cells, a strategy that aims to target the tumor, and consists of providing quercetin-linked magnetite nanoparticles (Q): (MNPs Q), and 3,5-dimaleylbenzoic acid-linked magnetite nanoparticles (A3'5DMB): (MNPs A3'5DMB)M; both types of nanoparticles were subsequently encapsulated with chitosan (Qs) and O-carboxymethyl chitosan (O-CMQs), functionalized with 11-mercaptoundecanoic acid (MUDA), and finally the anti-ABCC3 antibody was attached to the polymer phase, which was used as a selective driver of the delivery process of the encapsulated nanoparticles, thus carrying out the construction of the bionanocarriers: BNC-1: MNPs-Q-Ab; BNC-2: MNPs-a3'5DMB-Ab.Its manufacturing method and the tests of its biological functionality, its stability, the degradation of the encapsulation for the tumor microenvironment, the controlled release profile of the drugs Q and A3'5DMB, selective cell uptake, intracellular localization, cytotoxic effect on steroids of hepatocellular carcinoma cells with altered redox balance and induction of apoptosis, as well as its safety on normal cells, are described.

The application discloses citrullinated collagen type II polypeptide and application thereof. The amino acid sequence of the polypeptide is Ste-QYMCitADQAAGGLR (SEQ ID NO. 1), wherein the N terminal of glutamine Q in the sequence is connected with octadecanoic acid Ste, and the fourth position in the sequence is modified by citrullination. The citrullinated collagen type II polypeptide has a long drug half-life, can effectively treat rheumatoid arthritis, and has small side effects.

The present application relates to the field of cefoperazone acid, and discloses a preparation method of cefoperazone impurity A, which comprises the following steps: (1) performing acyl chloride treatment on oxypiperazine acid in the presence of an acyl chloride reagent to generate an acyl chloride compound of oxypiperazine acid; (2) performing silylation treatment on 7-aminocephalosporanic acid in the presence of a silylation reagent to generate a silylated compound of 7-aminocephalosporanic acid; (3) reacting the acyl chloride compound of oxypiperazine acid with the silylated compound of 7-aminocephalosporanic acid to generate an intermediate compound (I); (4) hydrolyzing the intermediate compound (I) under the action of penicillin acylase to generate an intermediate compound (II); and (5) performing esterification and cyclization reaction on the intermediate compound (II) in the presence of a first crystallization solvent, a first organic solvent and a cyclization reagent to obtain the cefoperazone impurity A. The method disclosed by the present application is simple in process, and can obtain the cefoperazone impurity A with high purity, which can be used as a control sample for cefoperazone detection.

This invention relates to the field of drug synthesis and microchemical technology, and discloses a method for synthesizing 6-bromopenicillinic acid based on continuous flow microreactors. The method includes dissolving 6-aminopenicillinic acid in ethanol and stirring until clear to obtain liquid A; preparing an aqueous solution of sodium nitrite and hydrobromic acid to obtain liquid B; mixing liquid A and liquid B in a first micromixer and then passing them into a microreactor pipeline for diazotization and bromination reactions, with inert gas purging the pipeline online to obtain a reaction effluent; extracting the reaction effluent with dichloromethane online in a second micromixer, then separating the organic phase using a membrane phase separator, and concentrating to obtain 6-bromopenicillinic acid. This invention utilizes the advantages of efficient mixing and precise temperature control in a continuous flow microreactor, combined with inert gas purging, to achieve continuous and stable preparation. It features safe operation, good batch stability, high production efficiency, and environmental friendliness, making it suitable for industrial production.

The application discloses a new type of hapten and fatty acid double modified long-acting hypoglycemic BimBH3 mimetic peptide compound targeting PTP1B as well as a preparation method and application thereof. The structural general formula of the Bim BH3 mimetic peptide is shown as formula I: wherein the compound is derived from a core region peptide segment of a Bim-BH3 domain, a non-natural amino acid is used to replace the second amino acid by site-specific substitution to increase the stability of the peptide segment against DPP-4 enzyme, and a long-chain fatty acid (hexadecanoic acid or octadecanedioic acid) is conjugated to the N terminal to modify to ensure better PTP1B inhibitory activity, so that the BimBH3 mimetic peptide has longer duration and higher activity and plays a role in hypoglycemia by inhibiting the target PTP1B. The compounds are prepared by using 2-CTC resin by polypeptide solid-phase synthesis method, and the crude product is cut, purified and freeze-dried to obtain a pure target compound.

The invention relates to the technical field of analysis and testing, and discloses a quality detection method for 6-aminopenicillanic acid, which can effectively detect coporphyrin I which is generated in a penicillin fermentation-enzyme method process and causes the 6-aminopenicillanic acid to become powder, and can be used for detecting the content of porphyrin in each main step of the process. The generation reasons and the effective removal steps are known, so that the technical process control is better guided; meanwhile, the chromatographic conditions can also be used for detecting the content of porphyrin in each main step of the process for producing 6-aminopenicillanic acid so as to understand the generation reasons and effective removal steps of the porphyrin, so that the process control is better guided.

The invention relates to a pyridazinic acid unit-containing cyclic ester peptide compound, a preparation method thereof, a pharmaceutical composition containing the compound, application of the compound in preparation of a medicine for inducing rupture and death of a tumor cell membrane, and application of the compound in preparation of a medicine for activating tumor immune response, and particularly relates to a pyridazinic acid unit-containing cyclic ester peptide compound and a pharmaceutical composition containing the pyridazinic acid unit-containing cyclic ester peptide compound. The invention also relates to application of the compound in preparation of medicines for treating diseases related to cell death in organisms.

The object of the present invention is to provide an absorption enhancer capable of introducing high-molecular weight compounds into cells.The object can be solved by a composition of the present invention comprising a polymer compound having a group represented by the following general formula (1) or the following general formula (2) at a side chain, and a compound to be administered with a molecular weight of 1,000 to 1,200,000.wherein X1 is a residue of neutral amino acid or ω-aminoalkanoic acid in which an end amino group and an end carboxyl group are removed, X2 is a residue of cell-penetrating peptide in which an end amino group and an end carboxyl group are removed, X3 is a hydroxyl group, an amino group, an alkoxyl group having 1 to 4 carbon atoms or a benzyloxy group, a is an integer of 0 to 50, and * denotes a bonding site.wherein X4 is a residue of neutral amino acid or ω-aminoalkanoic acid in which an end amino group and an end carboxyl group are removed, X5 is a residue of cell-penetrating peptide in which an end amino group and an end carboxyl group are removed, X6 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a benzyl group, an acyl group having 1 to 6 carbon atoms, an arylsulfonyl group or an oxycarbonyl group, b is an integer of 0 to 50, and * denotes a bonding site.

The application discloses an expandase mutant SEQ ID NO:3 which can efficiently catalyze the expandase reaction of a substrate to generate phenylacetyl-7-amino deacetoxycephalosporanic acid in a reaction system with a penicillin G concentration of up to 10 mM, and can be used for industrial production of G-7-ADCA.

This invention, entitled "A Composition Containing Pentadecanoic Acid, Parabacterium Species Outer Membrane Vesicles Containing the Composition, and Their Applications," belongs to the field of probiotics and microbial preparations technology. The technical problem this invention aims to solve is that beneficial live bacteria have weak colonization ability in the gut, are easily affected by the gastrointestinal environment, exhibit unstable individual responses, and struggle to simultaneously address immune regulation and barrier repair. This invention provides a composition containing pentadecanoic acid, Parabacterium Species-derived outer membrane vesicles, and their applications. The outer membrane vesicles are derived from *Parabacterium difficile* and are rich in pentadecanoic acid, palmitic acid, and octadecanoic acid. The composition and outer membrane vesicles prepared by this invention can significantly inhibit macrophage M1 polarization and reduce pro-inflammatory cytokines. TNF-α , IL-6 and IL-1 β It can lower the expression level of [something], reduce intracellular reactive oxygen species levels, improve mitochondrial function, significantly alleviate symptoms of colitis induced by sodium dextran sulfate, regulate the intestinal flora structure, and increase the abundance of beneficial bacteria.

The invention discloses a preparation method and application of a 1, 2, 4-oxadiazole compound containing a camphor alkanoic acid group, and the structural formula of the 1, 2, 4-oxadiazole compound containing the camphor alkanoic acid group is shown in the specification. According to the application of the camphor alkanoic acid group-containing 1, 2, 4-oxadiazole compound in prevention and treatment of agricultural meloidogyne incognita, the activity result shows that the compound provided by the invention has a relatively good prevention and treatment effect on the meloidogyne incognita and sclerotinia rot of colza.

The invention relates to the technical field of organic synthetic chemistry, in particular to 1-{2-[3-(4-hydroxyphenyl) propionyl] diazo alkyl} docosan-1-ketone as well as application and a preparation method of 1-{2-[3-(4-hydroxyphenyl) propionyl] diazo alkyl} docosan-1-ketone. According to the method, docosanoic acid and 3-(4-hydroxyphenyl) propanohydrazide are used as raw materials, and in a polar aprotic solvent, a benzotriazole coupling reagent and organic base are adopted for catalysis and a coupling reaction is carried out. According to the method, one-step coupling without protecting groups can be realized, the synthesis efficiency is remarkably improved, and the production cost is reduced; the method also has the advantages of mild conditions, high yield, excellent product purity, safety, environmental protection, suitability for large-scale popularization and the like.

The invention relates to an expansible ring enzyme mutant and application thereof in preparation of a cephalosporanic acid compound. Through technical means such as directed evolution, a series of enzyme mutants with a penicillin G ring expanding function are successfully screened out, and the mutants can efficiently convert penicillin G into G-7-ADCA. Therefore, the expansive ring enzyme mutants have important application value in industry.

Disclosed is a method and oral composition for treating a plurality of End stage diseases such as end-stage renal disease, chronic kidney disease, liver cirrhosis, chronic liver failure, end stage liver disease, Cancer, congestive Heart failure, pulmonary fibrosis, chronic obstructive pulmonary disease. In an embodiment of the invention, the composition comprises testosterone duodecanoate.

This invention relates to the field of biomedicine, disclosing a long-acting pTH polypeptide compound and its preparation and application. The polypeptide has an octadecanoic acid or eicosanoic acid and its derivatives modified by at least one amino acid residue at the 13th, 26th, and 27th amino acid residues of the pTH (1-34) parent peptide sequence, and is covalently bound to the polypeptide backbone via an AEEA-AEEA-γ-Glu linker. This invention significantly enhances the binding ability of the polypeptide to serum albumin and prolongs its half-life by utilizing fatty acid side chain modification. The long-acting pTH polypeptide compound of this invention exhibits significant osteogenic activity, promoting the proliferation of MC3T3-E1 cells and generating osteogenic markers and calcium nodules under osteogenic induction conditions, with a 2-6 fold increase in binding ability to serum albumin. This invention also provides a solid-phase synthesis method for this polypeptide compound and a pharmaceutical composition containing it, which can be used to treat osteoporosis and hypoparathyroidism, effectively solving the compliance problem of existing drugs requiring daily injections.

The application provides a synthesis process of cefquinome sulfate, and belongs to the technical field of heterocyclic compounds, and comprises the following steps: uniformly mixing 7-aminocephalosporanic acid, 2-methyltetrahydrofuran, hexamethyldisilazane and trimethylsilyl iodide and then reacting, sequentially adding pyrazole acid salt base C@MOF and trimethylsilyl iodide, 5,6,7,8-tetrahydroquinoline and methanol and then reacting, performing suction filtration, adding a hydrochloric acid solution, standing to separate phases, crystallizing, and drying to obtain 7-aminocephalosporanic acid; uniformly mixing 7-aminocephalosporanic acid, AE-active ester, 2-methyltetrahydrofuran and 4-vinylpyridine-styrene copolymer and then reacting, performing suction filtration, washing, collecting a filtrate, concentrating, dissolving in water, adding sulfuric acid, filtering, and drying to obtain cefquinome sulfate. The application can accelerate the reaction process, and improve the purity and yield of the target product.

The invention relates to the technical field of chemical synthesis, in particular to a preparation method of N-(4-hydroxyphenethyl) tetracosanamide. The method comprises the following steps: carrying out condensation reaction on tetracosanic acid and p-hydroxyphenylethylamine under the action of an onium salt condensing agent to obtain a product, and purifying the product to obtain N-(4-hydroxyphenethyl) tetracosanamide; the temperature of the condensation reaction is 40-50 DEG C. The method has the advantages of mild reaction conditions, high selectivity and few byproducts; the product is high in yield and high in purity, and can meet the large-scale requirements in the fields of medicines, materials and the like; the melting purification is realized by utilizing the melting point difference between the target product and impurities, multiple column chromatography or recrystallization is omitted, and the process route is short; the method has the advantages of safety, economy and easiness in expanded production, and provides powerful support for industrial development of N-(4-hydroxyphenethyl) tetracosanamide.

This invention discloses a method for heterologous production of 7-aminodeacetoxycephalosporanic acid using *Aspergillus nidulans*. This invention targets a *Aspergillus nidulans* strain that heterologously produces 7-aminodeacetoxycephalosporanic acid. Genes derived from the biosynthetic gene clusters pcbAB / C, isopentine N-acetyltransferase gene, and cefE gene, or their mutants, are assembled into a *Aspergillus nidulans* expression vector. Co-expression is performed in a *Aspergillus nidulans* basal cell strain to obtain a recombinant strain, successfully achieving heterologous expression of 7-aminodeacetoxycephalosporanic acid in filamentous fungi. Experiments show that the yield can reach 0.13 g / L at the shake-flask level. The strain constructed in this invention provides a good heterologous expression system for studying the synthesis and regulatory mechanism of 7-aminodeacetoxycephalosporanic acid.

This invention discloses a method for synthesizing H-AEEA-AEEA-OH, in which the side chains of smegglutinin and telpolide both contain the polyethylene glycol-modified H-AEEA-AEEA-OH, chemically named 17-amino-10-oxo-3,6,12,15-tetraoxa-9-azaheptadecanoic acid. The method of this invention features a short production cycle, mild reaction conditions, and is suitable for industrial production. The intermediates in each step of the reaction have high purity and high yield, with an overall yield exceeding 85%. The H-AEEA-AEEA-OH obtained by this method contains few impurities, and the specific impurities H-AEEA-OH and H-AEEA-AEEA-AEEA-OH are both small.

The application provides a composition and application of the composition in preparation of a product for maintaining blood lipid health level, the composition comprises 0.1-10 parts by weight of pentadecanoic acid, further comprises 1 part by weight of ginseng and / or 0.1-5 parts by weight of hawthorn, the composition is target-specific, components are mutually matched and synergistic, has the efficacy of maintaining blood lipid health level, realizes simultaneous effective intervention on two key indexes of total cholesterol and triglyceride; the composition has a clear mechanism, obvious synergistic effect, and outstanding advantages in safety, controllability of cost and feasibility of productization, and provides important material foundation and technical support for development of an efficient, balanced and easily popularized blood lipid health management scheme.

The application belongs to the technical field of medicine separation, and discloses a coupled crystallization method for preparing dichloris sodium superior product, wherein 6-amino penicillanic acid (6-APA) is used as a starting raw material, after acylation reaction and salt formation, finally, through evaporation-solvent-out coupled crystallization means, the dichloris sodium superior product with regular crystal morphology, large particle size (>200 μm), high crystallinity, high purity (up to 99.4%), process yield ≥80% and good stability can be obtained. The required equipment is simple, the processing scale is large, the operation is simple, and the industrial production is easy, so that the method has good technical economy and high industrial application value.

The invention relates to a random copolymer of structure (A) comprising, a carboxylic acid bearing repeat of structure (I), a 4-vinylbenzocyclobutene derived repeat unit of structure of structure (II), a styrenic repeat unit of structure (III), an alkyl acrylate or alkyl 2-methylenealkanoate derived repeat unit of structure (IV), a hydroxy functionalized alkyl acrylate or alkyl 2-methylenealkanoate derived repeat unit of structure (V), and two end groups as shown in structure (A) one of which is H and the other is a methyl moiety substituted with Rr, Rr1 and Rr2, wherein Rr1, is a C-1 to C-8 alkyl, Rr2 is selected from a C-1 to C-8 alkyl, a C-1 to C-8 alkylene hydroxy moiety (-alkylene-OH), a C-1-C-8 alkylenecarboxylic acid moiety (-alkylene-CO2H), or a benzylic alcohol comprising moiety of structure (B), Rr is a cyano moiety (—CN) or a carbonylalkyl moiety (—C(═O)—Ri), wherein Ri is a C-1 to C-8 alkyl or an aryl moiety.