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56 results about "Glucokinase activity" patented technology

Alpha functionalization of cyclic, ketalized ketones and products therefrom

Methodologies for the alpha-monohalogenation of acid sensitive ketones, especially cyclic, acid-sensitive, ketalized ketones. As one approach, the ketone is reacted with a halogen donor compound, e.g., N-chlorosuccinimide, in anhydrous, highly polar organic reagents such as dimethylformamide (DMF). As another monohalogenation approach, it has been observed that organic salts generated from amines and carboxylic acids catalyze the monohalogenation of ketalized ketone in reagents comprising alcohol solvent (methanol, ethanol, isopropanol, etc.). The monohalogenation is fast even at −5° C. The salt can be rapidly formed in situ from ingredients including amines and / or carboxylic acids without undue degradation of the acid sensitive ketal. Aryl ketones are monooxygenated using iodosylbenzene. This methodology is applied to monohalogenation of an acid sensitive monoketal ketone. The ability to prepare monohalogenated, acid sensitive ketones facilitates syntheses using halogenated, acid sensitive ketones. As just one example, facile synthesis of halogenated, acid sensitive ketones provides a new approach to synthesize the S-ketal-acid S-MBA (S-methylbenzylamine) salt useful as an intermediate in the manufacture of a glucokinase activator. As an overview of this scheme, a monohalogenated, cyclic, ketalized ketone is prepared using monohalogenation methodologies of the present invention. The halogenated compound is then subjected to a Favorskii rearrangement under conditions to provide the racemic acid counterpart of the desired chiral salt. The desired chiral salt is readily recovered in enantiomerically pure form from the racemic mixture.
Owner:HARRINGTON PETER J +2

Utilization of the function of rare sugar as promoter for the migration of glucokinase from nucleus to cytoplasm

Screening for a glucokinase-activating substance among rare sugars and providing a composition for treating disordered conditions in association with glucokinase activity, the composition containing the glucokinase-activating substance as the active ingredient. A promoting agent of glucokinase transfer from nucleus to cytoplasm, the promoting agent containing D-psicose and / or D-tagatose as the active ingredient, or a composition for preventing the onset of disordered conditions in association with glucokinase activity or for therapeutically treating the disordered conditions, which is in a form selected from a group consisting of food additives, food materials, drinks and foods, health drinks and foods, pharmaceutical product and feeds in blend with D-psicose and / or D-tagatose as the active ingredient for use in preventing the onset of disordered conditions in association with glucokinase activity or for therapeutically treating the disordered conditions. The disordered conditions in association with glucokinase activity are selected from impaired glucose tolerance, type 2 diabetes mellitus, insulin resistance, abnormal lipidemia, the metabolic syndrome and obesity. The composition is in a pharmaceutical form, and contains D-psicose and / or D-tagatose together with one or more pharmaceutically acceptable carriers.
Owner:KAGAWA UNIVERSITY +1

Indazole compounds for activating glucokinase

InactiveUS20110301155A1Superior GK activating actionLow toxicityBiocideOrganic chemistryBenzeneAcyl group
The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like.
A compound represented by the formula (I):
wherein R1 is an optionally substituted 4- to 7-membered nitrogen-containing heterocyclic group, optionally substituted carbamoyl, or optionally substituted sulfamoyl; R2 is optionally substituted alkyl, optionally substituted alkoxy, an optionally substituted 3- to 7-membered cyclic group, —SR′, —SOR′, or —SO2R′ (R′ is a substituent); R3 is hydrogen, halogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxy, —O-Cy (Cy is an optionally substituted 3- to 7-membered cyclic group which may be condensed with benzene), —SR″, —SOR″, or —SO2R″ (R″ is a substituent), or an optionally substituted 3- to 7-membered cyclic group which may be condensed with benzene; R4 is hydrogen, or optionally substituted alkyl; provided that when R3 is hydrogen, halogen, or methoxy, then R2 is not optionally substituted alkyl, or optionally substituted alkoxy; further provided that 5-[5-{[(2S)-2-amino-3-phenylpropyl]oxy}-2-(3-furyl)pyridin-3-yl]-N-pyridin-4-yl-1H-indazol-3-amine and 5-[5-{[(2S)-2-amino-3-phenylpropyl]oxy}-2-(3-furyl)pyridin-3-yl]-1-(4-methoxybenzyl)-N-pyridin-4-yl-1H-indazol-3-amine are excluded; or a salt thereof.
Owner:TAKEDA PHARMA CO LTD +1
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