212 results about "Chromone" patented technology

The present invention describes the identification and purification of 7-hydroxychromes that exhibit potent antioxidant activity. In one embodiment the present invention includes a method for providing an antioxidant to a host in need thereof, comprising administering an effective amount of a 7-hydroxychrome or a mixture of 7-hydroxychromones. The present invention includes methods that are effective in inhibiting free radical and oxidation caused damage through the simultaneous suppression of free radical generation and the suppression of the production of reactive oxygen species (ROS). The present invention also includes methods for preventing and treating ROS mediated diseases and conditions and diseases and conditions associated with other oxidative processes. The method for preventing and treating ROS mediated diseases and conditions and diseases and conditions associated with other oxidative processes is comprised of administering to a host in need thereof an effective amount of a composition comprised of a 7-hydroxychrome or a mixture of 7-hydroxychromones and a pharmaceutically acceptable carrier. Included in this invention is an improved method to isolate and purify 7-hydroxychromones from plant sources.

This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof,wherein R1, Q, Y2, Y3, Y4, U5, U6, U8, and R2 are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides methods of treating diseases such as heart disease, multiple sclerosis, osteo- and rheumatoid arthritis, arthritis other than osteo- or rheumatoid arthritis, cardiac insufficiency, inflammatory bowel disease, heart failure, age-related macular degeneration, chronic obstructive pulmonary disease, asthma, periodontal diseases, psoriasis, atherosclerosis, and osteoporosis in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides combinations, comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, together with another pharmaceutically active component as described in the specification.

The present invention describes the identification and purification of 7-hydroxychromes that exhibit potent antioxidant activity. In one embodiment the present invention includes a method for providing an antioxidant to a host in need thereof, comprising administering an effective amount of a 7-hydroxychrome or a mixture of 7-hydroxychromones. The present invention includes methods that are effective in inhibiting free radical and oxidation caused damage through the simultaneous suppression of free radical generation and the suppression of the production of reactive oxygen species (ROS). The present invention also includes methods for preventing and treating ROS mediated diseases and conditions and diseases and conditions associated with other oxidative processes. The method for preventing and treating ROS mediated diseases and conditions and diseases and conditions associated with other oxidative processes is comprised of administering to a host in need thereof an effective amount of a composition comprised of a 7-hydroxychrome or a mixture of 7-hydroxychromones and a pharmaceutically acceptable carrier. Included in this invention is an improved method to isolate and purify 7-hydroxychromones from plant sources.

A general chromone extract of ledebouriella root includes proportionally cimifugin, 5-0-methylwestammiol, etc. It is prepared by solvent extracting method or macroreticular adsorption resin method.

The invention pertains to the technical field of medicaments, and relates to a new flavonoid compound extracted from Maackia amurensis. The invention uses various separation methods including silica gel column chromatography, macroporous adsorptive resins, sephadex LH-20 column chromatography, semi-preparation type high-efficiency liquid chromatography, and the like. 54 compounds and 14 flavonoid compounds are seperated from the maackia amurensis, wherein, 7 new chemical components are included, which are respectively Maackiaflavanone A, Maackiaflavanone B, Maackiapentone, Maackiapterocarpan A, Maackiapterocarpan B, Maackiaisoflavonoside and 8-3, 3-dimethylallyl-5-hydroxy-7-methoxy chromone. A preliminary activity study indicates that the compound has certain effect of inhibiting the proliferation of tumor cells, thereby providing a basis for the development and research in the future.

The present invention relates to chromones, novel chromone derivatives, and pharmaceutical formulations containing the same and methods of use thereof. Uses of the present invention include, but are not limited to, use for the prevention and treatment of septic shock, organ injury and other disorders. The compounds described herein can be salt forms and also water-soluble compounds.

The invention discloses a chromone-containing benzoyl hydrazone compound capable of suppressing growth of cyanobacteria in a general formula I, synthesis of the compound and an in-vivo experiment on the benzoyl hydrazone for suppressing the growth of the cyanobacteria. In the formula, an R<1> represents hydrogen, halogen, C1-C4 alkyl groups or hydroxyl groups, an R<2>, an R<3> and an R<4> respectively represent hydrogen, halogen, hydroxyl groups or trifluoromethyl, and substituent groups represented by the R<2>, the R<3> and the R<4> can be identical or different. In the in-vivo experiment on the compound to microcystis aeruginosa FACHB912 which is the main type of cyanobacteria, a half maximal effective concentration value EC<50> of the compound ranges from 0.17muM to 33.37muM, and thus the compound has a remarkable effect for suppressing the growth of the cyanobacteria and can be used as an effective ingredient of an algicide.

The invention belongs to heterocyclic compound technical field, concretely relating to a heterocyclic compound in which unhydrogenated six-member heterocyclic ring containing an only ring hetero atom of an oxygen atom fuses with other phenyl rings. The invention provides a synthetic method of an isoflavone compound. The method comprises the steps of adding a reactant (substituted) 3-iodine chromone and tetraarylated tin into a solvent for a chemical reaction, and using column chromatography and recrystallization methods to purify the above resultant to obtain the pure compound of the present invention. By using the method, medicinal isoflavone such as daidzein, genistein, Ipriflavone, puerarin, formononetin and the like is prepared, and a new technical route of industrialization production of the above medicaments is established. Simultaneously, a series of novel isoflavone compounds with potential physiological activity are prepared.

The invention relates to a process for extracting and separating radix euphorbiae ebracteolatae chromone from Daphnetin radix euphorbiae ebracteolatae and use thereof, wherein the preparation process comprises the steps of, using Daphnetin radix euphorbiae ebracteolatae as raw material, using 4-10 times weight of ethyl acetate or acetone or mixture of ethyl acetate and acetone as solvent, extracting three times continuously by adopting 30-55 deg. C ultrasonic wave under normal pressure, the time for each extraction being 30-50 mins, wherein 60%-90% radix euphorbiae ebracteolatae chromone can be prepared through filtering, concentrating and column chromatography chromatography.

The invention discloses a chromone compound as well as a preparation method and application thereof. The chromone compound is obtained by separating from tobacco rootstock, the molecular formula of the chromone compound is C14H13O4 and comprises the structure as shown in the specification. The preparation method of the chromone compound comprises the following steps: on the basis of using the tobacco rootstock as a raw material, extracting extractum, and performing silica column chromatography and high pressure liquid chromatographic separation. The method comprises the following specific steps: crushing the tobacco rootstock sample, extracting ethanol ultrasonic extraction, combining extracting solution, filtering, reducing pressure, and concentrating to obtain the extractum; performing initial chromatography analysis on the extractum by using silica gel dry column-packing; performing gradient elution by using a chloroform-acetone solution in volume ratio of (1:0)-(1:2); further purifying the 8:2 part of eluate by using high pressure liquid chromatographic separation to obtain the chromone compound. The test proves that the chromone compound have good cell activity to tobacco mosaic virus. The compound disclosed by the invention is simple in structure, easy for realization of artificial synthesis and good in activity, and can be used as guiding compound for preventing the tobacco mosaic virus.

The invention discloses application of chloro-substituted tetrahydrophenethyl chromone derivatives and a pharmaceutical composition thereof which are extracted and separated from agilawood in prevention or treatment of inflammation-related diseases, autoimmune diseases and organ transplantation rejection, especially prevention or treatment of systemic inflammatory response, pneumonia, bronchitis, hepatitis, enteritis, rheumatoid arthritis, systemic lupus erythematosus, kidney transplantation rejection, liver transplantation rejection and hematopoietic stem cell transplantation rejection.

A therapeutic compound has a modified phenolic compound of the general formula (I)wherein at least one of R, R1, R2, R3, and R4 is an electrophilic group chosen from halogen, aldehyde, haloalkane, alkene, butyryl, flurophenol, sulfonamide, flurophenol sulfoxide and the remaining R, R1, R2, R3, and R4 is are each independently hydrogen, a hydroxyl group, an alkoxy group, a rutinosyl group, a carboxyl group, chromone, benzopyran, a rhamnosyl group, a substituted alkoxy group or a substituted acyloxy group wherein the substituent is chosen from hydroxyl, alkoxy, aryloxy, phenyl, halogen, and amido group. The compound can be used in a therapeutic treatment of inflammatory related diseases and condition.

The present invention describes the identification and isolation of chromones and novel chromone compositions from plant sources that exhibit up-regulation of adiponectin production by adipocytes and the normalization of virtually hundreds of genes related to glucose and fatty acid metabolic and signaling pathways. The chromone compositions are effective in enhancing adiponectin production by adipocytes and regulating genes involved in fatty acid biosynthesis, mitochondrial β-oxidation of fatty acids, steroid biosynthesis, gluconeogenesis, fat transport, PPARα / RXRα liver signaling and xenobiotic metabolism. The chromone compositions can be used to increase insulin sensitivity, improve glucose tolerance, lower triglyceride levels and balance glucose levels in mammals. Included in the present invention are methods for the prevention and treatment of a variety of diseases and conditions including, but not limited to insulin resistance, glucose intolerance, hyperglycemia, metabolic syndromes, dyslipidemia, and hypertriglyceridemia.

The invention belongs to the technical field of agilawood quality detection, and particularly discloses detection method for detecting agilawood quality by using a high-performance liquid chromatography. The method comprises the operation steps of chromatographic condition setting, preparation of a mother liquor of a reference substance, sample analysis and calculation for the analysis result. Byadopting the detection method, five chromones including agarotetrol, 6-hydroxy-2-[2-(4'-methoxyl) phenethyl] chromone, 6-hydroxy-2-(2-phenethyl) chromone, 6,7-dimethoxy-2-[2-(4'-methoxyl) phenethyl] chromone and 6,7-dimethoxy-2-(2-phenethyl) chromone which are contained in agilawood can be detected at a time, the comprehensiveness of agilawood quality detection is effectively improved, the accuracy of detecting the agilawood quality is improved, and the method has the advantages that the operation is simple, and the detection efficiency is high.

The invention discloses a chromone derivative represented by a formula (I) and a synthesis method thereof. The chromone derivative represented by the formula (I) is synthesized from an o-bromoalkynone compound and an ethyl acetoacetate compound serving as raw materials in the presence of a catalyst and inorganic alkali. The synthesis method disclosed by the invention has the advantages that the raw materials are simple and easily available, the post-treatment is simple and convenient, the catalyst is inexpensive, the yield is good and the environmental friendliness is achieved and the like.

The invention relates to a method for separating and purifying sec-o-glucosylhamaudol, which is characterized in that the method is a method for separating and purifying the sec-o-glucosylhamaudol from wind-resisting chromone extractive by using macroporous resin adsorption and gel column chromatography. The method uses the commercially available wind-resisting chromone extractive as raw materials, and comprises the steps of solvent backflow dissolving, resin adsorption, organic solvent extraction, gel column chromatography separation purification, recrystallization and the like. The method is characterized in that carbinol, ethanol, acetone or their mixed solvent serve as dissolving solvent and are heated for backflow for 1-3 hours, portions enriching the sec-o-glucosylhamaudol are obtained through resin adsorption and separation, and then the sec-o-glucosylhamaudol is separated and purified through the gel column chromatography. The method for extracting the sec-o-glucosylhamaudol is simple in method, high in repeatability, low in drying temperature, good in product quality and high purity.

The invention relates to a method for synthesizing multi-substituted chromone compounds, which includes a step for generating a series of multi-substituted chromone compounds, namely, enabling 2,3-allenoic acid and benzyne generated on the spot to give an insertion / 1,2-addition / ring opening / 1,4-addition reaction in tetrahydrofuran. The method for synthesizing the multi-substituted chromone compounds is simple in operation, easily obtainable in raw materials and reagent, higher in reaction yield, capable of avoiding the shortcoming of difficulty in preparation and severe conditions of a traditional method precursor, easily separable and purificatory in products, and suitable for synthesizing the multi-substituted chromone compounds.

The invention discloses a chromone skeleton-containing polycyclic compound as well as a preparation method and application thereof. The preparation method comprises the following steps: with 3-iodochromone compounds and norbornene as building blocks and palladium acetate as a catalyst, carrying out a [2 + 2 + 1] domino cycloaddition reaction with benzyl bromide compounds in an organic solvent to obtain a series of polycyclic compounds containing chromone skeletons, wherein diastereostereoselective change of the product is realized by adjusting the solvent. The chromone skeleton-containing polycyclic compound contains a chromone skeleton with potential biological activity, can provide a compound source for biological activity screening, and has important application value for drug screeningand pharmaceutical industry. Meanwhile, tumor growth inhibition activity screening is carried out on human non-small cell lung cancer cells (A549) and human hepatoma carcinoma cells (HepG2) of two tumor cell strains by the compound, and the compound is found to have certain tumor cell growth inhibition activity and can be applied to preparation of anti-tumor drugs.

The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.

The invention belongs to the field of medical chemical engineering and relates to a chromone dipolymer derivative as well as a preparation method and application thereof. Specifically, the invention relates to a compound with formula I, wherein S and R respectively represent absolute configurations of corresponding marking carbon atoms; R1-R3 independently represent various substituent groups, respectively; R3 and H connected by a wavey line can orientate alpha or beta. The invention further relates to penicillium purpurogenum of the compound with the formula I. Experiments prove that the compound with the formula I has good anti-tumor activity, can be used for preparing biological reagents such as a tumor cell killing agent, a tumor cell proliferation inhibitor and an anti-tumor agent, and further can be used for preparing anti-tumor and anti-cancer drugs. The formula I is as shown in the specification.

The invention belongs to the field of medicaments, and relates to a 2-substituted chromone compound, as well as a preparation method and application thereof. In-vitro anti-HBV (hepatitis b virus) activity test results of the 2-substituted chromone compound prove that: the 2-substituted chromone compound has remarkable anti-HBV effect, low effective concentration and low cytotoxicity. A medicinal composition can be further prepared from the 2-substituted chromone compound to be used for treating or preventing infection of hepatitis b virus, and particularly for inhibiting replication of surface antigen and e-antigen of the hepatitis b virus. The medicinal composition provided by the invention can be given nasally, orally, transdermally, parenterally, or by venous or intramuscular injection.

The invention relates to a substituted pyrrole chromone compound, which adopts the following structure: R1, R2, R3 and R4 are selected from hydrogen, halogen, C1-3 alkyl, C1-3 substituted alkyl, alkoxy, acyl, a carboxylic acid group, carboxylate radical, a nitrogen group, a phosphorous group or a sulfur group; R5 is selected from a substituted or non-substituted cyclic group; and R6 is selected from hydrogen or C1-3 alkyl, acyl, carboxylic acid group, carboxylate radical group, nitrogen group, phosphorous group or sulfur group. A type-5 phosphodiesterase inhibitor can be used for preparing medicine for curing diseases related to type-5 phosphodiesterase and is particularly suitable for preparing medicine for cuing male sexual dysfunction or pulmonary hypertension diseases.

The invention discloses an inducer for promoting agilawood formation of agilawood trees, and belongs to the technical field of biology. The inducer comprises a strong oxidant, fungal fermentation polysaccharide, inorganic salt and plant hormone. The inducer is injected into a trunk of an agilawood tree by an injection method, and then brown and yellowish-brown color-changing xylem in the trunk is cut and dried in the shade to obtain the agilawood. Components of an existing agilawood inducer are adjusted, formic acid, acetic acid and the like in a traditional agilawood inducer are replaced with a strong oxidant, molecular oxygen is generated after the agilawood inducer is injected into a tree body, and the strong stimulation effect on the tree body is achieved. The fungal fermentation polysaccharide serving as a plant stimulator can stimulate an agilawood tree to generate a stress reaction, so that resin secretion is facilitated, the yield of agilawood is increased, the content of an alcohol-soluble extract, the relative content of agarotetrol and the total relative content of sesquiterpenoids and 2-(2-phenethyl)-chromone compounds are increased, and the quality of agilawood is improved. The inducer has good economic benefits and ecological benefits.

The invention discloses a preparation method of a trifluoromethyl chromone compound, which is prepared by carrying out trifluoromethylation and cyclization reaction on a compound as shown in a formulaI in the presence of organic alkali without irradiation of visible light to initiate reaction or action of a photo-catalyst. Compared with the prior art, the method has the advantages of simple operation, safety, reliability, easy amplification, environmental friendliness and the like. R is a mono-substituted or multi-substituted group at any position on a benzene ring, and can be halogen, alkyl,alkoxy and the like in the same or different manner.

The invention provides a Qi'nan agilawood fragrance type cigar tobacco leaf and a preparation method of a cigar. The tobacco leaves contain qi'nan agilawood with the mass fraction of 0.1%-3%. The total relative content of chromone compounds in the Qi'nan agilawood extract reaches 65% or above, and the sum of the relative content of the monomer 2-(2-phenethyl) chromone and the monomer 2-[2-(4-methoxy) phenethyl] chromone reaches 45% or above. The Qi'nan agilawood extract is found to have a good effect of removing DPPH, and the higher the content of chromone compounds is, the stronger the removing capacity is. The prepared Qi'nan agilawood fragrance type cigar tobacco and cigarette are fragrant in smell, mellow in taste and good in combustion and smoking satisfaction degree, have a certain anti-oxidation effect, can reduce harmful ingredients in the cigar tobacco, further have the effect of preventing oral cancer and lung cancer and achieve the purpose of health care, and the content of a cancerogenic substance benzo [alpha] pyrene in smoke is low.

The invention belongs to the technical field of heterocyclic compounds, and particularly relates to a heterocyclic non-hydrogenated heterocyclic compound containing a six-membered ring and taking an oxygen atom as the only heteroatom and condensed with other rings. The invention provides a new method for synthesizing isoflavone by a nickel-catalyzed Negishi cross coupling reaction at room temperature, which comprises the following steps of: adding reactants (substituted) 3-iodine chromone or (substituted) 3-bromine chromone and an aryl zinc reagent into a solvent, and performing a nickel-catalyzed reaction at room temperature; and after the reaction, performing column chromatographic separation and purification to obtain a pure product of the compound isoflavone. The method provided by the invention is used for preparing medical isoflavones such as ipriflavone, formononetin, isoflavoues aglycone, genistein, puerarin and the like, provides a new technical way to the industrial production of the medicines, and is also used for preparing a series of new isoflavone compounds with potential physiological activity.

The invention relates to a 3-formacyl chromone derivative preparing method, making bis(trichloromethyl) carbonate fully react with N,N-dimethylformamide in C1-C4 halogenated hydrocarbon solvent at 0-5 deg.C, then adding in C1-C4 halogenated hydrocarbon solution of 2-hydroxy acetophenone derivative, raising temperature to 25-30 deg.C to react for 12-16 hours, separating and purifying the resultant and obtaining the 3-formacyl chromone derivative. And it has advantages of raw materials easy to obtain, reacting conditions moderate, simple and convenient to operate, clean and less pollution, good product purity, and high product yield; and it is a chemical synthesizing method with better spreading application prospect.

The invention relates to a method to simply and efficiently prepare a 2-alkyl substituted chromanone compound and relates to the field of medicine, organic chemical industry and fine chemical industry. The method uses chromone compounds and fatty aldehyde compounds as materials, and the 2-alkyl substituted chromanone compound is synthesized in the presence of the free radical initiators. The reaction conditions include: heating to 100-150 DEG C for 10-15 hours; isopropanol, tertiary butanol, chlorobenzene, acetonitrile, dimethyl sulfoxide and acetone are used as reaction solvents; tert-butyl hydroperoxide, tert-butyl peroxybenzoate, hydrogen peroxide, dicumyl peroxide and benzoyl peroxide are used as free radical initiators. Simple post-treatment can be performed after the reaction so as to obtain a series of 2-primary, secondary or tertiary alkyl substituted chromanone compounds.

The invention relates to a determination method of a total 2-(2-phenethyl) chromone compound content, comprising the following steps of: extracting and filtering an agilawood sample to obtain a solution to be determined; by taking 6, 7-dimethoxy-2(2-phenethyl) chromone as a reference substance, dissolving the solution to be determined with a same solvent, preparing standard solutions with different concentrations, determining a light absorption value under 230nm, and establishing a standard curve; and determining the light absorption value under 230nm after the solution to be determined is diluted, the total 2-(2-phenethyl) chromone compound content in the solution to be determined is calculated by the standard curve and a dilution multiple, and finally calculating the total 2-(2-phenethyl) chromone compound content in the agilawood sample. According to the determination method disclosed by the invention, operation is convenient; and by utilizing the characteristics that a 2-(2-phenethyl) chromone compound has a 2-(2-phenethyl) chromone mother nucleus and determining the total 2-(2-phenethyl) chromone compound content in an agilawood substance by adopting an ultraviolet spectrophotometric method, pertinence is strong, stability is good, accuracy is high, and repeatability is good.