Abstract: The present application relates to a method (I) for preparing a brivaracetam intermediate, comprising the steps of dissolving the compound represented by B-P and 1S,2S-diphenylethylenediamine in a solvent for resolution, crystallizing, filtering, and recrystallizing to obtain the compound represented by B-Q, which is then converted to the brivaracetam intermediate represented by B-R. This method can effectively resolve the compound represented by B-P. The present application also provides a method for preparing brivaracetam using the compound represented by B-R. The method can separate the effective components only through simple steps such as extraction, washing, drying, and concentration without requiring use of chiral chromatography column to separate isomers in the preparation process, and thus the separation process is simple, greatly reducing the production cost of brivaracetam.

Abstract: The present invention provides flavone derivatives having the general formula (I) which are useful for the treatment of Hepatitis B Virus infection (HBV). The compounds act as cccDNA (covalently closed circular DMA) inhibitors.

Abstract: Provided is a method for decomposing a flavonoid glycoside, wherein a flavonoid glycoside-containing raw material is hydrothermally treated to decompose a flavonoid glycoside into a flavonoid.

Abstract: The present invention provides PI3K protein kinase modulators of Formula (I) wherein R, n, R1, R2, L1, Cy1 and Cy2 are as defined herein, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

Abstract: Method and system for the extraction of oils from a biomass with a liquid carbon dioxide using cosolvent. The system and method can be used to extract cannabinoids from Cannabis biomass by cryogenically freezing the biomass and exposing the Cannabis biomass to sub-cooled liquid carbon dioxide and capturing a first high-terpene extract fraction, and then exposing the Cannabis biomass with a mixture of superfluid carbon dioxide and a cosolvent to capture a high cannabinoid second fraction.

Abstract: Described are polymerizable high energy light absorbing compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and X are as described herein. The compounds absorb various wavelengths of ultraviolet and/or high energy visible light and are suitable for incorporation in various products, such as biomedical devices and ophthalmic devices.

Abstract: The invention is composition and methods that restore balance to the stress-related steroidal hormone cascade. Upon co-administration, the compounds of the invention restore balance to the cascade and promote or restore normal function in patients suffering from a disorder having a primary psychological stress component. The compositions include a selected combination of isoflavones, alpha lipoic acid, and L dopamine or a precursor thereof, and are preferably obtained from the natural sources disclosed herein. The uses of the invention include administration of the disclosed compositions to patients suffering from PTSD, fibromyalgia, endometriosis, and other disorders having a common chronic stress component.

Abstract: The present invention is direct to the treatment of Pompe disease by administration of an enzyme or nucleic acid encoding for said enzyme suitable for Enzyme Replacement Therapy for Pompe disease in combination with the administration of an antisense oligomeric compound that modulates the splicing of acid alpha-glucosidase (GAA) gene.

Abstract: 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.

Abstract: A method of producing an alkoxyflavone derivative involves a step of reacting hydroxyflavone derivative which is shown in the below chemical formula and dialkyl sulfate in the presence of dimethyl sulfoxide and an alkali hydroxide. Further, in the chemical formula below, R11-R14, R21-R25 and R3 are independently one of hydrogen, hydroxyl group, ester group, alkoxy group, alkylenedioxy group, sulfonyl group and alkyl group, respectively. However, at least two of R21-R25 and R3 are hydroxyl groups.

Abstract: Provided is a method for preparing hispidulin or a derivative thereof. The method includes selective protection of trihydroxybenzaldehyde, followed by regioselective iodination, selective protection, Stille coupling, Baeyer-Villiger oxidation and basic hydrolysis to obtain a protected intermediate compound. Then, alkylation, Claisen-Schmidt condensation, cyclization and deprotection of the protected intermediate compound are performed to obtain hispidulin or the derivative thereof. The present disclosure provides an efficient method for total synthesis of hispidulin or the derivative thereof with concise reaction steps and high yield.

Abstract: A method of separating oil-soluble pigment and water-soluble pigment from natural material using aerogels characterized in comprising the steps of: (A) immersing a natural material in a leaching solvent to extract a pigment; (B) mixing the leaching solution from which pigment is extracted in step (A) with aerogel to adsorb oil-soluble pigment to aerogels; (C) separating oil-soluble pigment adsorbed on the surface of aerogel in step (B); (D) drying and concentrating the pigment separated in step (C), enhancing a method of separating from natural material the initial substance for pharmaceuticals, food, cosmetics, etc. facilitating a safer and more efficient production process compared to the conventional separation method.

Abstract: The invention belongs to the field of medicine and chemical industry, and particularly relates to multiple crystal forms of scutellarin aglycone and preparation thereof. The invention also relates to use of said crystal forms of scutellarin aglycone in the manufacture of a medicament for preventing and/or treating a cardiovascular or cerebrovascular disease, rheumatic arthritis or stroke sequelae, etc. The crystal forms of scutellarin aglycone according to the invention have good stability, and can solve the problems concerning poor oral absorption and low bioavailability of scutellarin.

Abstract: The invention relates to a process for producing Nebivolol hydrochloride, (formula I) comprising the steps of: provision of a protected Nebivolol hydrochloride of the general formula (II), with P being an amine protecting group, and hydrogenation of said protected Nebivolol hydrochloride yielding Nebivolol hydrochloride of the formula (I).

Abstract: A process for synthesis of enatiomerically pure or enatiomerically enriched or racemic mixture of (+ and/or ?) epicatechin and its intermediates, comprising the steps of: (i) obtaining penta-protected quercetin; (ii) reducing the penta-protected quercetin obtained from step (i); (iii) optionally deprotecting the compound of step (ii); (iv) reducing the compound obtained from step (ii) or step (iii) in the presence of a chiral/achiral reducing agent to obtain a chiral intermediate; (v) deprotecting and/or hydrogenation of the chiral intermediate obtained from step (iv) to obtain (?)-epicatechin; (vi) optionally simultaneously deprotecting and by drogenation of the compound obtained from step (ii) to obtain racemic epicatechin.

Abstract: The present invention is directed to a novel use of prenylflavanone compounds for control of blood glucose and treatment or prevention of diabetes.

Abstract: Novel substituted chroman derivatives and intermediate compounds, compositions containing same, methods for their preparation and uses thereof as therapeutic agents particularly as anti-cancer and chemotherapeutic selective agents are described.

Abstract: The preparation of C-3 coupled biflavonoids and C-3 coupled biflavonoid analogs occurs from flavan-3-ones that are contacted with a compound having a nucleophilic aromatic moiety, in the presence of a Lewis acid where an intermediate compound is formed with a C-3 hydroxy group. A flavan-3-ol can be converted to a flavan-3-one as required. The intermediate compound is dehydrated to a flavene with a C-3-C-4 double bond. The flavene compound undergoes hydroboration-oxidation hydration to introduce a C-4 hydroxy group that can be oxidized to an oxo group or can be dihydroxylation to introduce hydroxy groups at the C-4 and C-3 carbons and dehydrated to a biflavonoid or biflavonoid analog having an oxo group at its C-4 carbon and substituted by the selected nucleophilic aromatic moiety on its C-3 carbon.

Abstract: 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.

Abstract: The present invention provides a kind of benzopyrone compounds having a structure of formula (I) and the pharmaceutically acceptable salts or prodrugs thereof, and the pharmaceutical compositions containing such compounds, which can be used to regulate the novel estrogen receptor ER-a36, and prevent and/or treat the related diseases mediated by the ER-a36 receptor, such as cancers, etc.

Abstract: Provided are compositions for treatment of cancers, including breast cancer, comprising at least one novel daidzein analog, as well as methods of using the same for preventing or treating cancer or tumor growth.

Abstract: The subject of the invention is genistein for use in non-enzymatic method of treatment and/or prevention of the lysosomal storage diseases (LSDs) i.e. diseases with the underlying defect in degradation and resulting accumulation of organic compounds in lysosomes, to reduce the level of storage of organic compounds by reducing the rate of efficiency of accumulating organic substances synthesis and/or by increasing the rate of efficiency of cellular deposits degradation.

Abstract: Compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering a 7,8-dihydroxyflavone derivative with modified flavone or heterocyclic ring to a subject in need thereof. Methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided.

Abstract: The disclosure relates to new crystalline forms of genistein. The disclosed crystalline forms include crystalline genistein sodium salt dihydrate; crystalline genistein potassium salt dihydrate; crystalline genistein calcium salt; crystalline genistein magnesium salt; crystalline genistein L-lysine salt; crystalline genistein N-methylglucamine salt; crystalline genistein N-ethylglucamine salt; crystalline genistein diethylamine salt; and crystalline genistein monohydrate. The disclosure also relates to the novel genistein salts represented by these crystalline forms. Therapeutic compositions containing at least one of these crystalline forms of genistein and/or a genistein salt and a pharmaceutically acceptable carrier are described.

Abstract: The present invention relates to compounds useful as pharmaceutical intermediates, to processes for preparing the intermediates, to intermediates used in the processes, and to the use of the intermediates in the preparation of pharmaceuticals. In particular, the present invention concerns enantiomerically pure optionally substituted 2-(1-hydroxy-alkyl)-chromen-4-one derivatives represented by formula (IA) and (IB), processes for preparing the alcohol derivatives and their use in preparing pharmaceuticals.

Abstract: There is described a method of isolating one or more of pectin, d-limonene, a flavour compound, a flavonoid, a soluble monosaccharide, a decomposition product of a monosaccharide and cellulose, from citrus material wherein said method comprises the microwave assisted hydrothermal low temperature treatment of citrus material.

Abstract: Subject of the invention is a method for the production of isoflavanes from isoflavones, whereby in a first reaction step (a) the 4-keto group of the isoflavone is reduced in a enantioselective manner, whilst the 2,3-double bond is maintained, to the 4-hydroxy compound.

Abstract: The present invention relates to flavone derivatives and to compositions containing one or more of these flavone derivatives. The present invention further relates to flavone derivatives or compositions for use in the treatment and/or prevention of a viral infection, and to a method of preventing or treating these infections.

Abstract: Provided are compositions for treatment of cancers, including breast cancer, comprising at least one novel daidzein analog, as well as methods of using the same for preventing or treating cancer or tumor growth.

Abstract: The present invention provides edible compositions comprising a sweet taste modulator of the present invention, food products comprising such edible compositions and methods of preparing such food products. The present invention also provides methods of reducing the amount of sugar in a food product, methods of reducing the caloric intake in a diet, and methods of enhancing sweet taste in a food product.

Abstract: A compound of formula I, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein either Q1, CR6a and optionally R6b together form a cyclic moiety wherein: Q1 is selected from C1-2 alkylene, C1-2 alkenylene, OC1 alkylene and OC1 alkenylene moieties optionally substituted by oxo; R6a is a single bond and R6b is H; or R6a and R6b together form a double bond; and Q2 and Q3 are independently selected from H, R1 and R2; or Q2 and Q3 together form a cyclic moiety in which one of Q2 and Q3 is a cyclic moiety selected from OC1 alkylene and OC1 alkenylene moieties optionally substituted by oxo or a group R5 as here in below defined for R2 and the other of Q2 and Q3 is a cyclic moiety selected from C1-2 alkylene, C1-2 alkenylene and OC1 alkylene optionally substituted by oxo; R6a and R6b are each H or a cyclic moiety as defined above; and Q1 is selected from H, R1 and R2 and a cyclic moiety as defined above; and R1-4 are H or substituen

Abstract: The present invention relates to new compounds which are inter alia derivable from hops for use in the treatment of (for treating)/prevention or healing of a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, in particular a disease which is associated with or characterized by degeneration and/or a destruction of cartilage (and/or for the prevention of aggrecan loss). Food products comprising these compounds for use in the treatment (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, in particular a disease which is associated with or characterized by degeneration and/or a destruction of cartilage, are also envisaged.

Abstract: A pharmaceutical composition for treating disorders associated with insulin resistance is disclosed, and the composition comprises at least one inhibitor which is an effective agent to suppress endothelin-1-stimulated resistin gene expression through decreasing the endothelin-1-stimulated phosphorylation of proteins downstream of endothelin type A receptor, wherein the downstream signaling molecules comprise ERK1/2, JNKs, AKT, and STAT3 proteins, and wherein the inhibitor is selected from at least one antagonist of the endothelin type A receptor or downstream signaling proteins.

Abstract: The present invention relates to a composition having antiviral activity for prophylaxis or treatment of flavivirus infection or a disease resulting therefrom in humans or animals, characterised in that said composition consisting of baicalein, or analogues, or derivatives thereof. The composition may further comprise a pharmaceutically acceptable carrier. The antiviral activity may include inhibition of virus attachment to host cells, inhibition of intracellular virus replication and direct virucidal activity. The flavivirus may comprise dengue virus type-1, dengue virus type-2, dengue virus type-3, dengue virus type-4 and Japanese encephalitis virus.

Abstract: The invention discloses the uses of hydroxyl polymethoxylflavones and derivative thereof that are relative to inhibit adipogenesis and lower lipid accumulation, wherein the hydroxyl polymethoxylflavones is obtained from the peels of Citrus genus plants. Therefore, the hydroxyl polymethoxylflavones that of a therapeutically effective amount not only can be a medical compound for treatment obesity or fatty liver, but also can be a food element.

Abstract: Substituted flavonoid compounds, and pharmaceutical formulations of flavonoid compounds are described. Also described are processes for preparing flavonid compounds, as are methods for treating cancer in mammals using the described flavonoid compounds or pharmaceutical formulations thereof.

Abstract: Flavone derivatives, preparative method of the derivatives and use thereof as medicaments for treating diabetes. The structure of the derivatives is presented by formula 1: In the structure, R1 and R2, which are identical or not, represent hydrogen atom, halogen, cyano, hydroxyl, trifluoromethyl, thio-methyl, benzyloxy. C1-C8 linear chain or branch chain alkyl, C1-C8 linear chain or branch chain alkoxy. The pharmacological test indicates that the flavone derivatives can significantly increase the glucose consumption of Hep-G2 cell with insulin resistance activity, promote translocation of glucose transporter 4 of skeletal muscle cells (L6GLUT4myc) at different level, and significantly increase glucose intake and utilization by cells.

Abstract: A method for producing 4?-demethylnobiletin or 4?-demethyltangeretin including fermenting a skin derived from at least one citrus fruit selected from citrus fruits belonging to section Acrumen in subgenus Metacitrus in genus Citrus or citrus fruits belonging to section Aurantium in subgenus Archicitrus in genus Citrus, or a water extract product thereof using one or more Aspergillus molds selected from Aspergillus kawachii, Aspergillus awamori, Aspergillus oryzae, Aspergillus sojae, Aspergillus saitoi, and Aspergillus usamii to obtain a fermented product.

Abstract: Provided are: a method for rapid fluoromethylation, by which a fluoromethyl group can be easily bonded to an aromatic-ring carbon of an aromatic compound with little generation of by-products; and a process for preparation of a PET tracer using the same. The method is characterized by cross-coupling an organoboron compound in which an aromatic ring is bonded to a boron atom with FCX2Br (wherein X is ordinary hydrogen or heavy hydrogen) in a solvent obtained by adding water to an aprotic polar solvent, in the presence of a palladium complex, a phosphine ligand, and a base.

Abstract: An extract of Citrus depressa, preferably an organic solvent extract of a fruit and/or leaf of Citrus depressa, a supercritical extract of a fruit and/or leaf of Citrus depressa, or a subcritical extract of a fruit and/or leaf of Citrus depressa, containing 0.3 mass % or more of a polymethoxyflavonoid in terms of solid matter, for example, 0.2 mass % or more of nobiletin and/or 0.1 mass % or more of tangeretin in terms of solid matter, or a polymethoxyflavonoid, such as nobiletin and tangeretin, is used as an active ingredient of a muscle atrophy inhibitor.

Abstract: The present invention provides a sirtuin activator with an active component composed of black ginger or a black ginger extract, which is easily obtainable, extremely safe, and eaten from old. The present invention further provides a sirtuin activator with an active component of polyalkoxyflavonoid compound represented by general formula (I) and having a sirtuin activation effect that is 10 folds that of resveratrol or higher: wherein, R1 to R7 are each independently a hydrogen atom, a hydroxyl group, or a C1 to C6 lower alkoxy group.

Abstract: Embodiments of the present disclosure related to compounds and compositions derived from G. buchananii baker and methods thereof.

Abstract: Disclosed is a daidzein derivative as represented by formula (I), or pharmaceutically acceptable salt thereof. Compared to the daidzein in the prior art, the daidzein derivative hydrochloride, in particular to the 7-O—N,N-diethyl-aminoacetyl daidzein hydrochloride, prepared by the daidzein derivative of the present invention, has better solubility and effect for treating cardiovascular diseases.

Abstract: Supplementation of the bioflavonoids such as epigallocatechin gallate, rutin, naringin, or genistein into mammalian cell culture media are shown to be effective in reduction of acidic species variants on recombinant antibodies. The demonstrated reduction in acidic species through the use of bioflavonoids, facilitates the manufacturing of a less heterogeneous product with potential improvements in antibody structure and function.

Abstract: The present invention is directed to a novel use of prenylflavanone compounds for control of blood glucose and treatment or prevention of diabetes.

Abstract: Isoflavone fatty acid ester derivatives of formula (I) or (II), the preparation method thereof and the pharmaceutical compositions containing such compounds are disclosed. The uses of such compounds in preparation of medicaments for preventing or treating hyperlipidemia, obesity or type II diabetes are also disclosed.

Abstract: The present invention provides a medicinal and/or a food usage of eupatilin for treating, improving, and/or preventing at least one condition selected from bone disease, menopausal disorder, cardiovascular disease, neurodegenerative disease, or obesity. Advantages of the present invention includes little or no possibility of side effects such as cancer, and effective treatment, improvement, and/or prevention of the at least one condition selected from bone disease, menopausal disorder, cardiovascular disease, neurodegenerative disease, and obesity.

Abstract: 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.

Abstract: The invention provides methods for one or more of enhancing energy metabolism, promoting healthy energy metabolism, maintaining healthy energy metabolism, preventing conditions that result in a decline or deficiency in energy metabolism, treating conditions that result in a decline or deficiency in energy metabolism, and preventing the accumulation of excess body fat in animals without reducing energy intake by the animals. The methods comprise administering isoflavones to the animals, preferably in amounts of from about 0.001 to about 10 g/kg/day.

Abstract: The present invention relates to biodegradable polymers (e.g., polyesters and polyester amides) derived from functionalized biologically active compounds that can provide site specific delivery of bioactive compounds upon biodegradation in a controlled manner.