198results about "Saccharide with carbocyclic radicals" patented technology

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

The present invention relates to processes for preparing a glucopyranosyl-substituted benzyl-benzene derivative of general formula III,wherein R1 is defined according to claim 1.

The present invention relates to a novel process for the preparation of compounds having inhibitory activity on sodium-dependent glucose transporter (SGLT) present in the intestine or kidney.

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 novel crystal form of 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate, and having favorable characteristics, is characterized by its x-ray powder diffraction pattern and / or by its infra-red spectrum.

Compositions and systems are provided for the high efficiency quenching small water-soluble oligomers, or oligofluors, of from about 1-10 kd in size, where the oligofluors comprise multiple excimeric or exciplex forming fluorophores arranged on a scaffold, which are efficiently quenched by a quencher entity linked to the oligomer through a cleavable moiety. Fluorophores of interest include, without limitation, aromatic fluorophores such as pyrenes, e.g. benzopyrene, perylene, pyrene, etc. In some embodiments the oligofluor / quencher combination provides for a Stern-Vollmer constant (KSV) of greater than about 106 M−1, and may be greater than about 107 M−1, greater than about 108 M−1, or more. In some embodiments of the invention, the scaffold is a phosphodiester / glycoside backbone, e.g. an analog of a polynucleotide. The system of oligofluors and quenchers can be used in qualitative and quantitative screening and detection methods to detect any enzymatic, chemical or catalytic activity that can cleave the moiety between the quencher and scaffold.

The invention relates to a crystalline form of 4-(β-D-glucopyranos-1-yl)-1-methyl-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.

The invention relates to a method for the preparation for a crystalline form of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene. In addition the invention relates to a crystalline form obtainable by this method, to a pharmaceutical composition and to the use thereof for preparing medicaments.

A novel crystal form of 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate, and having favorable characteristics, is characterized by its x-ray powder diffraction pattern and / or by its infra-red spectrum.

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

A novel N-acetyl-5-N,4-O-carbonyl-protected dibutyl sialyl phosphate donor for sialylation of both primary and sterically hindered secondary acceptors to prepare sialosides with high yield and α-selectivity is disclosed. Methods for making disaccharide building blocks comprising α(2→3), α(2→6), α(2→8), α(2→8) / α(2→9) alternate, and α(2→9) sialosides are provided. methods for one-pot synthesis of complex sialosides are disclosed. Libraries of sialosides and methods for using the libraries for detection and receptor binding analysis of surface glycoproteins or pathogens and cancer cells are disclosed. Methods for distinguishing between hemagglutinin (HA) from various strains of influenza are provided.

Compounds and pharmaceutical compositions comprising them are disclosed that may be useful for the treatment of diseases and disorders such as diabetes and obesity.

The present invention provides a method for making glycoside compounds including the steps of: (a) lithiating an aromatic reactant having a leaving group using a lithium reagent in a first microreactor under non-cryogenic conditions to form a lithiated anion species, and (b) coupling the lithiated anion species with a carbonyl substituted reactant to form a glycoside.

A compound represented by formula I, or a pharmaceutically acceptable salt, solvate, polymorph, enantiomer or racemic mixture thereof, wherein, R1 and R2 are independently hydrogen, -OH, alkyl, -CF3, -OCHF2, -OCF3 or halogen,R3 is cycloalkyl, -OCH2CF3, -OCH2CHF2, -OCH2CH2F or -OCH2CH3,R4 is hydrogen, -OH, -O aryl, -OCH2 aryl, alkyl, cycloalkyl, -CF3, -OCHF2, -OCF3, -OCH2CF3, -OCH2CHF2, -OCH2CH2F or halogen,A is -CX1X2, wherein X1 and X2 are independently H, F and Cl, and when both X1 and X2 are H, R3 is other than -OCH2CH3. The compound has an activity of inhibitors of sodium-dependent glucose transport protein. A method for preparing the compound. A pharmaceutical composition comprising the compound. A use of the compound and pharmaceutical composition thereof in the preparation of medicaments of SGLT2 inhibitors for treating a disease of interest.

The present invention relates to a novel compound with thiazole ring having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes.

Provided are processes for the preparation of complexes that are useful in purifying compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The processes can reduce the number of steps needed to obtain the target compounds and the complexes formed in the processes are typically provided in a crystalline form.

The invention relates to a crystalline complex of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(β-D-glucopyranos-1-yl)-benzene and a natural amino acid, to methods for the preparation thereof, as well as to uses thereof for preparing medicaments.

The invention discloses a method for extracting and refining hydroxysafflor yellow A from safflower. The hydroxysafflor yellow A is a compound with a chalcone monoside structure, and is abundant in traditional Chinese medicinal material safflower (CARTHAMI FLOS). The hydroxysafflor yellow A with content of over 80 percent is obtained through the following five steps of: extracting form the traditional Chinese medicine safflower; purifying through ion exchange resin; purifying through neutral polarity macro-porous adsorption resin; purifying through non-polar macro-porous adsorption resin; and freeze-drying, wherein the transfer rate is over 20 percent.

The present invention relates to one or more SGLT2 inhibitors or pharmaceutically acceptable forms thereof for use in the treatment and / or prevention of a metabolic disorder in a feline animal, preferably wherein the metabolic disorder is one or more selected from the group consisting of: ketoacidosis, pre-diabetes, diabetes mellitus type 1 or type 2, insulin resistance, obesity, hyperglycemia, impaired glucose tolerance, hyperinsulinemia, dyslipidemia, dysadipokinemia, subclinical inflammation, systemic inflammation, low grade systemic inflammation, hepatic lipidosis, atherosclerosis, inflammation of the pancreas, neuropathy and / or Syndrome X (metabolic syndrome) and / or loss of pancreatic beta cell function and / or wherein the remission of the metabolic disorder, preferably diabetic remission, is achieved and / or maintained.

The invention relates to a preparation method of bulk pharmaceutical chemicals used for curing the type 2 diabete, in particular to a eutectic preparation method of sodium-glucose cotransporter 2 bulk pharmaceutical chemicals. In the invention, the technical problems of the existing preparation method that reaction steps are more, the methoxy-removing condition is strict and the yield of the obtained main product with beta configuration is low are solved. The technical scheme in the invention is as follows: the eutectic preparation comprises the following steps: adding chiral component (X) inN-3((3R,4S,5S,6R)-2-(4-chloro-3-(4-ethoxylbenzyl)phenyl)-6-(hydroxymethyl)-2-methoxytetrahydro-2H-pyran-3,4,5-triol, performing selective complexation with reductant to remove methoxy, then reducing the temperature to perform eutectic preparation, and adopting the one-pot method to obtain dapagliflozin-X. The eutectic preparation method is mainly used to prepare the sodium-glucose cotransporter 2bulk pharmaceutical chemicals.