86 results about "C glycosides" patented technology

The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and / or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.

C-glycoside compounds are suited for stimulating the synthesis of glycosaminoglycans containing a D-glucosamine and / or N-acetyl-D-glucosamine residue, advantageously hyaluronic acid, and / or proteoglycans, advantageously proteoglycans containing hyaluronic acid, by fibroblasts and / or keratinocytes.

A process for producing an azulene derivative useful as a Na+-glucose cotransporter inhibitor, which is high in yield, is simple in operation, is low in cost, is suited for environmental protection, and is advantageous industrially, the process being characterized by reducing and deprotecting at least one compound selected from penta-acyl compounds and tetra-acyl compounds or salts thereof to obtain a C-glycoside compound; and a useful intermediate for synthesis of such an azulene derivative, obtained in the course of the above process.

A cocrystal of (1S)-1,5-anhydro-1-[3-(1-benzothien-2-ylmethyl)-4-fluorophenyl]-D-glucitol and L-proline. It is a cocrystal of known compound A, which has a constant quality, is superior in storage stability, has no moisture absorptivity, and is suitable as a crystal of a drug substance used for preparing pharmaceuticals.

The present invention relates to compositions that are suitable for topical application to the skin or the scalp, containing, in a physiologically acceptable medium, at least one compound of a given formula. The invention also relates to a cosmetic treatment process comprising the topical application of these compositions and also to novel C-glycoside derivatives.

The present invention relates to novel C-glycoside compounds of given absolute configuration, to a process for synthesising them and to compositions containing them. The invention also relates to the cosmetic use of these C-glycoside compounds as agents to stimulate the synthesis of glycosaminoglycans containing a D-glucosamine and / or N-acetyl-D-glucosamine residue, advantageously hyaluronic acid, and / or of proteoglycans, advantageously proteoglycans containing hyaluronic acid, by fibroblasts and / or keratinocytes. The invention also relates to a cosmetic process for treating keratin materials using a composition containing at least one C-glycoside compound according to the invention.

C-glycoside compounds are suited for stimulating the synthesis of glycosaminoglycans containing a D-glucosamine and / or N-acetyl-D-glucosamine residue, advantageously hyaluronic acid, and / or proteoglycans, advantageously proteoglycans containing hyaluronic acid, by fibroblasts and / or keratinocytes.

The invention discloses an extraction and purification technology of four kinds of flavone C-glycosides in moso bamboo leaves. The active ingredients of moso bamboo leaves are extracted by a heat reflux extraction process, and the best extraction technology for obtaining four kinds of flavone C-glycosides through a single-factor experiment and an orthogonal experiment comprises the following steps: extracting with 75% ethanol for 2h at 70 DEG C according to a solid-liquid ratio of 1:20, and repeatedly extracting for 4 times; purifying the crude extract of flavone by use of macroporous resin, wherein D101 macroporous resin is the best choice according to comparison of static saturated adsorption capacity and desorption capacity; and further purifying the component by use of polyamide resin, wherein the particle size of the polyamide resin is 0.15-0.25mm according to the comparison of the dynamic adsorption screening results of three common kinds of polyamide resin, and a 40% ethanol solution is adopted for purifying the four kinds of flavone C-glycosides. Through the treatment, the final purity of the four kinds of flavone C-glycosides bamboo leaf flavone powder reaches 76.939mg.g<-1>.

The invention discloses choline eutectic solvents, a preparation method and an application in extraction of flavone C-glycoside of flos trollii. The choline eutectic solvents have the expression: [N(CH)33CH2CH2OH]+[X.zY]- and is prepared from choline bromide or choline chloride and ZnCl2, SnCl2 or AlCl3 through mixing in a certain mole ratio, wherein when X is Br, Y is ZnCl2 or SnCl2; when X is Cl, Y is AlCl3. By means of the provided choline eutectic solvents, three important flavone C-glycosides, namely, orientin, orientin-2''-O-beta-L-galactoside and vitexin in the flos trollii can be efficiently and selectively extracted; compared with conventional extraction with methanol solvents, the extraction rate of orientin, orientin-2''-O-beta-L-galactoside and vitexin can be improved, few impurities exist in an extract, silica gel columns are not required to be repeatedly used for separation when the extract serving as the raw material is used for preparing monomers of orientin, orientin-2''-O-beta-L-galactoside and vitexin, the separation and purification steps can be greatly reduced, and the separation and purification cost can be reduced.

The invention discloses a preparation method of a high-purity flavone C-glycoside extract. The preparation method mainly comprises the following steps of: selecting vegetable drugs rich in flavone C-glycoside, extracting by adopting water or an ethanol-water mixed solvent, and optionally further separating, purifying and concentrating as required to obtain a flavone C-glycoside extract concentrated solution, wherein the concentrated solution is dissolved and diluted into a defined amount of acid water or an alcohol-containing aqueous solution to carry out an acid hydrolysis reaction, the obtained extract hydrolysate is further separated and purified by adopting fillers such as macroporous resin and the like, and high-purity (more than 60%) flavone C-glycoside extract is obtained. The preparation method disclosed by the invention adopts an acid hydrolysis control technology, and other flavone C-glycoside derivatives in plants can be converted into corresponding flavone C-glycoside components, so that content and purity of a flavone C-glycoside component are obviously increased, a process is simple, operability is strong, and industrialization amplification is easy to achieve.

Composition, especially a cosmetic and / or dermatological composition, containing, in a physiologically acceptable medium, at least one of mannose, and rhamnose and at least one additional compound chosen from C-glycosides and C-glycoside derivatives. Use of such a composition, and also a device containing it.

The invention relates to a total flavone c-glycoside effective component extract separated from traditional Chinese medicine abrus mollis hance, belonging to natural medicine technical field, which mainly contains apigenin-6, 8-bis-C-glucoside, apigenin-6-C-glucose-8-C-arabinfuranoside and apigenin-6-C-arabinose-8-C-glucoside, whose flavone c-glycoside content is higher than 40%. The invention relates to an extraction method of the total flavone c-glycoside effective component extract. Pharmacodynamic tests prove that the abrus mollis hance total flavone c-glycoside extract can be used as active component to prepare the drugs for the prevention and treatment of acute and chronic hepatitis or the like.

A cocrystal of (1S)-1,5-anhydro-1-[3-(1-benzothien-2-ylmethyl)-4-fluorophenyl]-D-glucitol and L-proline. It is a cocrystal of known compound A, which has a constant quality, is superior in storage stability, has no moisture absorptivity, and is suitable as a crystal of a drug substance used for preparing pharmaceuticals.

C-glycoside compounds having the formula (I): are useful for depigmenting / whitening the skin and / or for the anti-browning thereof.

C-glycoside keto-amide derivatives, including C-glycoside keto-hydrazones and C-glycoside keto-oximes, may be prepared from plant or animal lipids and saccharides. These C-glycoside keto-amide derivatives are of the formula:wherein:R is a saccharide;Y is independently selected from H or a halogen;m is an integer greater than or equal to 1;X is NH (as in C-glycoside keto-hydrazones) or O (as in C-glycoside keto-oximes); andR2 is an acyl moiety derived from any lipid fatty acid of the formula —C(O)—R3, wherein R3 is a C5 to C22 straight or branched chain hydrocarbon which may be saturated or unsaturated. These C-glycoside keto-amide derivatives have potential applications as surfactants, detergents, liposomes, and bilayers.

The invention discloses a 6-halogenated glucose C-glycoside as well as a preparation method and application thereof. A structure of 6-halogenated glucose C-glycoside is shown in formula I; an intermediate can be synthesized efficiently with cheap and easily available raw materials; meanwhile, when the raw material is used for synthesizing Jardiance, dapagliflozin and the like, a reaction yield ishigh, and an obtained product has high purity and relatively high industrial application prospect.

The invention discloses C-glycoside with substituted aromatic ring, S-glycoside compounds, pharmaceutical compositions with effective dose compounds, and applications of the compounds and compositions for preparing cardio-cerebrovascular anti-hypoxic ischemia medicine and neuroprotection medicine. In the compounds are c-glycoside compounds when X represents CH2, wherein when Y represents CH2, n may be 0 or 1, when n is 0, m is 0, and when n is 1, m is 0 or 1; when Y represents NH, n=m=1; when X represents S, the compounds is S-glycoside compounds, wherein Y represents CH2, n may be 1, 2 or 3, and m is 0; R represents mono-substituted, disubstituted, tri-substituted hydrogen C1-C3 straight-chain or branched chain alkyl and hydroxyl, or C1-C3 straight-chain or carboxylic acid ester. 14 compounds found have better protective action to hypoxia-reoxygenation injury of myocardium than or equal to salidroside; 15 compounds have stronger neuroprotection activity than or equal to gastrodine.

The invention discloses novel application of composition with the content of flavone C-glycoside 2'-O-beta-L-galactopyranosyl orientin and 2'-O-beta-L-galactopyranosyl orientin between 30 and 90 percent in preparing medicaments for resisting angiocardiopathy such as myocardial ischemia and the like, and also describes a single component of the 2'-O-beta-L-galactopyranosyl orientin, a method for preparing the composition, and a medicinal preparation.

The present invention relates to a topical cosmetic and / or dermatological composition comprising, in a physiologically acceptable medium, at least one hyaluronic acid or a derivative thereof and at least one C-glycoside derivative.

C-glycoside compounds having the general formula (I): are useful for protecting and / or stimulating the activity and / or the proliferation of gamma-delta T lymphocyte cells (γδT cells), and are advantageously formulated into cosmetic / pharmaceutical compositions suited for promoting skin tissue repair, for re-equilibrating epidermal proliferation and differentiation disorders which appear with lack of sleep, and for improving the appearance of the head of hair and limiting hair loss.

The invention provides a preparation method of a flavone-C-glycoside 6'' hydroxyl-ester derivative. By taking a flavone-C-glycoside 6'' hydroxyl extract having wide source and low activity as a substrate, the method enables esterification reaction between the substrate and carboxylic acid in the presence of microorganism lipase and organic solvent so as to obtain a flavone-C-glycoside 6'' hydroxyl-ester derivative rarely seen in nature and having high activity through local specific synthesis. In the reaction process, monitoring is performed by a detection method of thin-layer chromatography or efficient liquid chromatography until all start raw materials are consumed; and after the reaction, lipase is filtered, and the esterified product is washed and purified by the organic solvent. The method has the advantages of easily available substrate, simple preparation technology, high specificity and mild reaction conditions; the obtained product is easy to purify; and sufficient raw material guarantee is provided to the application of flavone-C-glycoside 6'' hydroxyl-ester derivative in the fields of functional food, beverage, cosmetics, medicine and the like.

C-glycoside compounds having the general formula (1): are useful for stimulating the immune system of the skin and / or as immunoregulators, and are advantageously formulated into cosmetic / pharmaceutical compositions suited for preventing and / or limiting cutaneous immune imbalances, notably those resulting from environmental stresses.

The present invention provides a method for producing a C-glycoside derivative, which can produce the C-glycoside derivative at a high yield and at a low cost, which conforms to environmental protection, and which is applicable industrially. The C-glycoside derivative is useful for treating and preventing diabetes such as insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes) and the like and various diabetes-related diseases including insulin-resistant diseases and obesity.

The invention provides a method for improving the yield of homoorientin produced by recombinant bacteria through a coordinated regulation strategy. Based on the recombinant bacteria carrying a C-glycosides glycosyl transferase Gt6CGT gene, the yield of the homoorientin produced by the recombinant bacteria is greatly improved through regulation of supply of a UDP-glucose by introducing genes, optimization of an induction conversion strategy and control of acetic acid accumulation. Through the coordinated regulation strategy, the recombinant bacteria BL21-CGT-III homoorientin yield reaches 1371mg / L, the molar conversion rate of a substrate reaches 97.4% and is 40 times the current production peak, and the process for preparing the homoorientin is simple.

The invention relates to a carbon-glycoside glycolipid compound and the function thereof. The carbon-glycoside glycolipid compound has the structure as shown in a formula A or a formula B. The synthesized carbon-glycoside glycolipid compound of the invention has prominent anti-tumor activity, and the compound can be used for the preparation of anti-tumor medicines. R1 and R2 in the formula A and the formula B are respectively selected from H or one of the groups as shown in a formula C, and R1 and R2 have at least one group as shown in the formula C; R3 is H or acetyl; R4 and R5 in a formula C are respectively selected from H or one of C1-C6 alkyls; n is 0-15.

The invention relates to a gem-difluoride glycoconjugated compound with formula (I): where R represents II or a benzyl, acetyl, benzoyl alkyl group, R1 and R2 may be identical or different and represent H or an alkyl, benzyl, benzoyl, acetyl, pivaloyl, trialkylsilyl, tertiobutyldiphenylsilyl protective group or an acetal group of the CR′R′ type, where R′ and R′ may be identical or different and represent H or an alkyl, aryl, benzyl or thiophene group, R3 represents H or an alkyl, benzyl, benzoyl, acetyl, pivaloyl, trialkylsilyl or tertiobutyldiphenylsilyl protective group, R4 represents OR″, NGR′GR′, N3, or a phthalimide, where R″ represents H or an alkyl, benzyl, benzoyl, acetyl, pivaloyl, trialkylsilyl or tertiobutyldiphenylsilyl protective group, GR′ and GR′ may be identical or different and represent II or an alkyl, benzyl, benzoyl, acetyl, alkyloxycarbonyl, allyloxycarbonyl or benzyloxycarbonyl group, R5 represents a free or protected hydroxyl group or a halogen, R6 represents H or an alkyl, acetyl, benzyl, PO3H or PO3Na group. It is applicable to the preparation of compounds that can be used particularly for the treatment of cancer.

C-glycoside compounds having the formula (I):are useful for depigmenting / whitening the skin and / or for the anti-browning thereof.