62results about How to "Metabolic stability" patented technology

The present invention relates to a new formulation comprising a stabilized GLP-1 compound, such as an analog, fragment or derivative thereof for delivery across pulmonary tissue in vivo.

This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt, amide or ester thereof, wherein R1 represents a hydrogen atom or a halogen atom; R2 represents a hydrogen atom, etc.; R3 represents an alkyl group having from 1 to 10 carbon atoms; said alkyl group of R3 is substituted by at least one substituent selected from the group consisting of substituents α; said substituents α is aryl, hydroxy, oxo, etc.; said aryl having 6 to 10 carbon atoms; said aryl is unsubstituted or substituted by at least one alkyl group having from 1 to 6 carbon atoms; said heterocyclic and the heterocyclic moiety of said heterocycliccarbonyl, both of substituents α, are 5- to 10-membered cyclic groups containing from 1 to 4 heteroatoms selected from the group consisting of nitrogen atoms, oxygen atoms and sulfur atomsThese compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

The invention relates to a spiro compound serving as a FXR receptor agonist, whose chemical structure is shown in type I, pharmaceutically acceptable salts of the spiro compound, or the enantiomers, diastereomers, tautomers, racemates, solvates, N-oxide or amino acid conjugates and the pharmaceutical compositions of the spiro compound, and the use in preparing drugs for treatment of diseases mediated by the FXR receptor.

The invention discloses a genetically engineered bacterium for producing L-arginine and a construction method and application thereof. According to the invention, a gene for encoding carbamyl phosphate synthetase and a gene for encoding L-arginine biosynthetic pathway enzyme are integrated in escherichia coli; a synthetic route of arginine in escherichia coli and metabolic flux related to argininein a whole amino acid metabolic network are analyzed and reconstructed to obtain genetically engineered bacteria which are clear in genetic background, do not carry plasmids, are not mutated and canstably and efficiently produce L-arginine; and the genetically engineered bacteria have good L-arginine production capacity.

The invention discloses a fermented soybean meal with the function of complex enzymes and a preparation method for the fermented soybean meal. According to the invention, a mixed fermentation technology by multi-strains is adopted, non-transgenic soybean meal, microbial strain liquids, molasses and other raw materials are uniformly mixed and then subjected to solid-state fermentation, environmental conditions such as temperature, material moisture and the like in the processes of growth, metabolism and enzyme generation of microorganisms are controlled, so as to ensure the enzyme-generating capability of the microorganisms and enzyme preparation content accumulation during the fermentation process; after the fermentation is completed, the materials are dried at a low temperature. The fermented soybean meal prepared by the method disclosed in the invention contains a large amount of amino acids, active probiotics and other nutrients and has the greatest characteristic of being rich in different types of enzymes such as proteases, amylase, cellulase and xylanase, and is easily digested and absorbed by animals; the digestion and utilization rate of the fermented soybean meal is improved; the production cost is reduced.

The invention provides a genetically engineered strain for high yield of ergothioneine and application. The stain takes escherichia coli as a host, and a coding gene hisG* of a corynebacterium glutamicum ATP phosphoribosyl transferase HisG mutant is integrated on a genome of the host; the copy number of a histidine operon gene hisDBCHAFI is further increased on the genome of the host; a mycobacterium smegmatis ergothioneine operon gene egtBCDE is further integrated on the genome of the host; an Escherichia coli glutamylcysteine ligase encoding gene gshA is integrated on the genome of the host,so that the synthesis of the ergothioneine is promoted; a neurospora crassa C-S lyase coding gene egtE<ncr> is further integrated on the genome of the host, so that the synthesis of ergothioneine isfurther promoted; and a gene egtB*<msm> of a sulfoxide synthase mutant is integrated on a genome of the host, so that synthesis of ergothioneine is further promoted.

The invention discloses a spiro compound as well as a preparation method, a composition and application thereof. The spiro compound has a structure shown as a formula (I). The spiro compound disclosedby the invention can effectively treat Farnesol X receptor-mediated diseases and is more stable and long in half-life period.

The invention discloses a F-18 tagged P2X7 receptor imaging agent which is a compound 18F-{(2-chloro-3-trifluorophenyl)(1-(pyrimidin-2-yl)-6,7-dihydro-1H-[1,2,3]triazolo[4,5-c]pyridin-5(4H)-yl)methanone shown as formula I. The P2X7 receptor imaging agent is suitable for identifying and diagnosing pulmonary inflammation and tumors.

This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, whereinR1 represents a hydrogen atom or a halogen atom;R2 represents a methyl group or an ethyl group;R3 represents a branched alkyl group having from 3 to 6 carbon atoms or an alkyl group having from 3 to 6 carbon atoms substituted by an alkoxy group having from 1 to 6 carbon atoms;with the proviso that when the terminal carbon atom of said alkyl group of R3 is substituted by said alkoxy group, said alkyl group is a branched alkyl group.These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

Novel diagnostic and therapeutic peptides disclosed herein are somatostatin analogs backbone cyclized through metal complexation, and having improved somatostatin receptor subtype affinity and selectivity. These backbone cyclized peptide analogs possess unique and superior properties over other analogs, including chemical and metabolic stability, selectivity, increased bioavailability and improved pharmacokinetics. Pharmaceutical compositions that include these backbone cyclized somatostatin analogs, radiolabelled analogs, reagents for synthesizing same, and methods of using such compositions for diagnostic and therapeutic purposes are also disclosed.

The invention discloses a hypoxia-activated prodrug based on 2-nitroimidazole-1-alkanol. The 2-nitroimidazole-1-alkanol of the prodrug is connected to an antineoplastic drug through a carbonate bond. The prodrug has a structure shown in the formula I and in the formula, n represents 0, 1, 2 or 3, and R1, R2, R3 and R4 include but not limited to hydrogen, hydroxyl, chlorine, bromine, fluorine, C1-C6 alkyl, C1-C6 alkyl containing alkenyl and C1-C6 alkyl containing alkynyl. The prodrug can target the hypoxia region of the tumor and is reduced by the high expressed specific enzyme in the hypoxic tumor tissue so that the original drug is released. The prodrug is stable in vitro and in vivo, and the released drug can be specifically reduced in hypoxic tumor tissue so that the targeting of the anti-tumor drug is improved, toxic or side effects are reduced and the curative effect is improved.

The invention relates to a probiotics fermented Chinese yam and a preparation method thereof. The product is prepared from Chinese yam, a probiotics combination and ingredients; the pH value is smaller than 3.6; the coli group MPN of each gram of the product is less than or equal to 3, the nitrate content is less than or equal to 0.5 mg / kg, and the viable count of lactic acid bacteria is up to 108 CFU / g; the probiotics combination comprises lactobacillus plantarum and leuconostoc mesenteroides; the ingredients comprise table salt and sugar. The preparation method comprises the following steps: activating and cultivating lactic acid bacteria, removing peels of Chinese yam, cutting and segmenting, blanching, cooling and airing, preparing fermenting brine, and inoculating. The probiotics fermented Chinese yam disclosed by the invention has the advantages of promoting nutritional value and peculiar flavor of the Chinese yam and prolonging the shelf life of the Chinese yam.

The present invention provides a novel class of compounds that have the activity of inhibiting HSP90 enzyme and are useful as anti-cancer agents or such, and compounds that are useful as synthetic intermediates thereof. Specifically, the present invention provides compounds represented by the following formula (1), and pharmaceutically acceptable salts thereof:wherein X, R1, R2, R3, R4, R5, R6, R7, L1, L2, and L3 are as defined in the specification.

The invention discloses a low-temperature-resistant flowering phase prolonging nutrient solution. The solution is prepared from, by weight, 35-37 parts of laminaria residues, 10-12 parts of sawdust, 23-25 parts of silkworm excrement, 4-5 parts of sodium carboxymethyl starch, 3-4 parts of ferrous sulfate, 2-3 parts of sodium lignin sulfonate, 40-44 parts of grape skin, 3.5-3.8 parts of proline, 32-34 parts of pomegranate seeds, 2.0-2.2 parts of sodium hexametaphosphate, 25-27 parts of folium eucommiae, 1.9-2.3 parts of ethylenediaminetetraacetic acid, an appropriate amount of 50% ethanol solution, an appropriate amount of 65% ethanol solution and an appropriate amount of water. Since high-content polyhydric alcohols in grape skin fermentation liquor can be combined with in-vivo cells to form hydrates, and addition of highly-hydrophilic proline stabilizes plant in-vivo protoplasm colloid and in-tissue metabolic process, lowers a solidifying point and prevents cell dehydration, the occurrence rate of freezing injury in a flowering phase can be remarkably decreased on the whole, influences of low temperature on moistures in petals are reduced, and the flowering phase is prolonged.

The invention belongs to the technical field of medicines, provides a medicine purpose of a FXIa inhibitor compound or salt thereof, and particularly relates to the purpose of the FXIa inhibitor compound or the salt thereof in preparation of medicines used for preventing and / or treating artery thrombi and venous thrombi.

The invention provides an aloe-emodin nitrogen-heterocyclic derivative as well as a preparation method and application thereof, and belongs to the field of chemical medicines. The derivative is a compound shown as a formula I, or a salt thereof, or a stereoisomer thereof, or a solvate thereof, or a prodrug thereof, or a metabolite thereof. The compound provided by the invention can effectively inhibit macrophages from generating NO and inflammatory factors, and can also effectively inhibit the expression of iNOS and COX-2, so that the activation of an NF-kappa B signal path is inhibited, the inflammatory reaction is alleviated or the occurrence of the inflammatory reaction is inhibited; meanwhile, the compound has a good treatment effect on colitis, especially acute ulcerative colitis; thebiological activity of the compound 5r is remarkably superior to that of aloe-emodin. In addition, the compound is good in safety and stable in metabolism, and has important application value in research and development of anti-inflammatory drugs.

The invention discloses compounds with anti-thrombus activity shown in a formula I, a preparation method thereof and an application of the compounds as antithrombotic agents. A rat thrombus model is adopted to evaluate the anti-thrombus activity of the compounds shown in the formula I. Experiment results show that: the compounds shown in the formula I have excellent anti-thrombus activity, and can be used as the antithrombotic agent clinically.

The invention relates to a method for producing oxytetracycline calcium premix by streptomyces rimosus fermentation, and belongs to the technical field of veterinary drug. In the method, the technicalconditions of a seed preparation process are optimized, so that the prepared seed has the characteristics of stable metabolism, small batch difference, high hypha concentration, small protein content, less heat-source matters and the like. Meanwhile, according to the method, culture medium ingredients are optimized, the culture medium is used for culturing the seeds so as to be favorable for thesynthesis of an oxytetracycline special structure and the improvement of the yield of the oxytetracycline calcium premix and also be favorable for subsequently separating and purifying the oxytetracycline calcium premix. A high-pressure diaphragm sheet frame machine is adopted to filter, and a flash evaporation dryer is used for drying. Compared with the traditional production method for the oxytetracycline calcium premix, the method disclosed by the invention is characterized in that a fermentation unit and yield can be effectively improved, production cost is lowered, meanwhile, the use of chemical organic solvent is avoided, pollution caused by the organic solvent for the oxytetracycline is avoided, and harm on animals is avoided.

The invention belongs to the technical field of mixed feed additives, and particularly relates to a nutritional preservative for a total mixed ration and a preparation method for the nutritional preservative. The nutritional preservative for the total mixed ration is prepared from the following raw materials: lactobacillus plantarum powder, sodium diacetate, phytic acid, cinnamic acid, grape polyphenols, tea polyphenols, soybean oligopeptides, ginkgo leaves extract, allicin, herba inulae extract, yellow sweet clover extract and vitamin C. The nutritional preservative for the total mixed ration contains multiple natural antibacterial and anti-oxidation components, comprises environment-friendly components, and is free of drug resistance and toxic or side effects, and is used for replacing a large dose of a preservative or antibiotics required to be used at present, bacteria can be effectively killed, mildews can be effectively proofed, the respiratory decay of feeds can be suppressed, the yield of an animal product such as meat and milk can be improved, and the quality of the animal product can be improved; stepwise water addition is adopted in the preparation method, so that a uniformly dissolved preservative can be obtained more easily, and the effective utilization rate of the raw materials is increased.

The invention belongs to the field of solar cells, and discloses a high-performance environment-friendly lead-based perovskite solar cell and a preparation method thereof. According to the preparationmethod, a certain amount of a chelating agent disodium ethylene diamine tetraacetate or 2, 3-dimercaptosuccinic acid is introduced into a lead-based perovskite precursor solution so that the crystallinity and the crystal orientation of a lead-based perovskite thin film layer can be effectively optimized, the grain boundary of a perovskite thin film is passivated, and the energy conversion efficiency of the perovskite thin film is improved. Meanwhile, when the device is decomposed, the chelating agent can be combined with lead ions in time to form a stable and soluble complex, the complex canbe smoothly metabolized by a human body and discharged along with urine after being absorbed by the human body accidentally, and finally harm to the human body is remarkably reduced. Commercial development of the perovskite solar cell is facilitated, and particularly application of perovskite indoor photovoltaic as energy supply of the smart home terminal in the Internet of Things era is promoted.

The invention belongs to the technical field of beverage processing and in particular relates to a nutritional health-care radix stellariae beverage. The nutritional health-care radix stellariae beverage is prepared from the raw materials: radix stellariae pulp, fresh jasmine flower, buckwheat, mango pulp, saccharifying enzyme, fresh pitaya peel, fresh corn stigma, total saponin, sophocarpine, grape seed extract, fenugreek saponins extract, zymophyte and distilled water. The nutritional health-care radix stellariae beverage has uniform color and luster, is light green, has color and luster and has no sediment and floc after standing; the nutritional health-care radix stellariae beverage has rich and coordinated fresh jasmine flower flavor, radix stellariae flavor and buckwheat flavor, is sour, sweet and delicious and has no bitter and astringent taste; the nutritional health-care radix stellariae beverage has remarkable treatment effect on patients with long-time gastrectasia, dim and dark complexion and hypertension.

The invention discloses a modified hyaluronic acid injectable filling material and a preparation method thereof. The modified hyaluronic acid injectable filling material comprisesis prepared from freehyaluronic acidgel, cross-linked hyaluronic acid gel, water soluble cellulose and a buffering solution, wherein the hyaluronic-polyethylene glycol modifying material has the following structure: (shown in the description), wherein n is selected from 10 to 5000, and m is selected from 100 to 5000. The modified hyaluronic acid injectable filling material is good in injectability, stability and biological compatibility, applicable to soft tissue filling, restoration and surgical operation such as wrinkle removal, rhinoplastynose re-shaping and breast implanting, and also applicable to the anti-adhesion of the medical surgical operation and lubrication of bone joints.

The invention discloses a pyridine substituted chalcone type compound with a structure as shown in a general formula I or a medicinal salt thereof, and also discloses a preparation method and application of the compound or the medicinal salt thereof. The compound or the medicinal salt thereof disclosed by the invention has small toxic or side effects and strong water solubility, is not easy to generate drug resistance, can effectively inhibit the aggregation of tubulin, has stronger anti-tumor activity in vitro and in vivo, can ensure more stable metabolism and has good pharmacological prospects. The invention also discloses combined application of the pyridine substituted chalcone type compound or the medicinal salt thereof and a TACC3 inhibitor for effectively inhibiting the activity oftumor cells resistant to tubulin.

The invention belongs to the biotechnology field of biochemical industry and colorants, and particularly relates to a bacterium strain capable of producing haematochrome and a method for preparing the haematochrome. A bacterium XF 105 which is obtained through screening in soil and can produce the haematochrome is adopted as the bacterium strain, the bacterium strain is named as Paenibacillus agaridevorans XF 105 and preserved in China Center for Type Culture Collection, the preservation number is CCTCC:M2014644, and the preservation date is December 11, 2014, and the gene sequence of the bacterium strain is shown as SEQ ID No.1. The haematochrome can be stably produced and is natural in hue, the bacterium strain is easy to preserve, the preservation time is long, the survival rate is high, the bacterium strain can still survive after being preserved at a 4-degree bevel, and the extraction method of the haematochrome is low in cost.

The present invention relates to a chlorophyll-fixing freshness-preserving agent. The chlorophyll-fixing freshness-preserving agent comprises the following components: proline, glycine, glutamic acid,L-arginine, titanium citrate, calcium chloride, zinc acetate, cholesterol, methyl salicylate and water. Before use, 1-MCP pre-treatment fumigation, UVB post-irradiation and modified atmosphere storage are conducted. A freshness-preserving method can significantly increase chlorophyll content of green vegetables during storage, at the same time reduces weight loss rate, maintains storage quality of crispness and tenderness, etc. of the green vegetables, delays decay and deterioration, and is suitable for freshness-preserving of whole green vegetables or sliced green vegetables.

The invention discloses skin cold storage liquid and application thereof. The cold storage liquid comprises hydroxyethyl starch, tretinoin, uronic acid, monopotassium phosphate, magnesium sulfate, sodium hydroxide and an ROCK inhibitor, wherein the ROCK inhibitor is selected from one or two of Y-27632 and Y-27632 2HCl. The cold storage liquid provided by the invention can be used for human skin storage, so that the skin can keep biological activity, and under the in-vitro condition, skin cells can continuously survive for a long time. The requirement of stably storing the skin for a long timecan be met, and meanwhile, the skin can survive after being stored and can be cultured into a large number of fibroblasts.

The invention relates to a novel FFA1 and PPAR-alpha / gamma / delta quadruple agonist as shown in a formula (I), a preparation method thereof and a pharmaceutical composition containing the compound. As a medicine for treating, preventing or relieving one or more diseases or dysfunction, compared with the prior art, the agonist has better metabolic stability and stronger in-vivo pharmacological effect, and can be used for preparing medicines for treating, preventing or relieving one or more diseases or dysfunction; and the agonist has a wider application prospect.