62results about How to "Metabolic stability" patented technology

The present invention relates to compounds of the formula

and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.

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.

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 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.

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 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 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 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.