62results about How to "Metabolic stability" patented technology

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 present invention relates to compounds of the formulaand 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 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.

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.

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 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 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 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 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.