12 results about "Glucokinase activator" patented technology

The invention relates to solid compositions comprising {2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid, and methods of making and using such solid compositions.

The present invention relates to a crystal form of a free state of (R)-3-(3-((S)-2-(4-(2-chlorophenoxy)-2-oxo-2,5-dihydro-1H-pyrrol-1-yl)-4-methylpentanoylamino)-1H-pyrazol-1-yl)-2-hydroxypropylnicotinate (compound A) or a pharmaceutically acceptable salt thereof, a pharmaceutical composition and a preparation method thereof, and a use of the crystal form in the preparation of a medicament for treating diabetes and related symptoms.

Provided herein are pharmaceutical formulations comprising glucokinase activator, or a prodrug, or a pharmaceutically acceptable salt, an isotope labeled analogue, a crystalline form, a hydrate, a solvate, or a diastereomeric or enantiomeric form thereof and the use thereof for treating diseases; the pharmaceutical formulations are in the form of immediate-release formulations, extended-release formulations, or combination of immediate-release formulation and extended-release formulations. The pharmaceutical formulations achieved once-a-day therapy for some diseases, in particular, type II Diabetes Mellitus with obesity. The pharmaceutical formulations exhibit sustained 24 hours of glucose-lowering effects. The pharmaceutical formulations also achieved lower Cmax, extended T1 / 2 as well as maintained similar bioavailability and increased MRT compared with commercial Dorzagliatin tablet, enhanced the pharmacology effect of restoring the glucose stimulated GLP-1 secretion in diabetes with obesity.

The invention relates to therapeutic use of a glucokinase activator in combination with insulin or an insulin analogue. Methods of using glucokinase (GK) activators, particularly in combination with insulin or insulin analogs, are generally disclosed herein. In certain aspects, the disclosure provides methods of treating type 1 diabetes mellitus comprising administering a GK activator in combination with insulin or an insulin analogue. Also disclosed herein are uses of GK activators as medicaments, and the preparation of medicaments for such uses.

The invention relates to a crystal form of a free state or a pharmaceutically acceptable salt of (R)-3-(3-((S)-2-(4-(2-chlorophenoxy)-2-oxo-2, 5-dihydro-1H-pyrrole-1-yl)-4-methyl valeryl amino)-1H-pyrazole-1-yl)-2-hydroxy propyl nicotinate (compound A), a pharmaceutical composition of the crystal form and a preparation method of the crystal form. The invention also discloses application of the crystal form in preparation of medicines for treating diabetes and related symptoms.

A use of a glucokinase activator or a prodrug thereof, or a pharmaceutically acceptable salt, an isotopic label, a crystal form, a hydrate, a solvate, a diastereomer or an enantiomer in preventing, alleviating or treating cognitive disorders or neurodegenerative diseases in subjects, or delaying the progress of cognitive disorders or neurodegenerative diseases in subjects, or reducing the risk of cognitive disorders or neurodegenerative diseases in subjects.

The invention provides a new skeleton small molecule compound and application thereof, the new skeleton small molecule compound has a structure as shown in formula 1A: Formula 1A, and the new skeleton small molecule compound can be used as a glucokinase regulator, especially a glucokinase activator for treatment of diseases mediated by the activation.

The present invention relates to the free state of (R)-3-(3-((S)-2-(4-(2-chlorophenoxy)-2-oxo-2,5-dihydro-1H-pyrrole-1-yl)-4-methylpentanoylamino)-1H-pyrazole-1-yl)-2-hydroxypropylnicotinate (compound A) or crystalline forms of its pharmaceutically acceptable salts, pharmaceutical compositions and methods for preparing the same, and the use of the above crystalline form in the preparation of pharmaceuticals for the treatment of diabetes and related conditions. [C1] TIFF2026511448000095.tif36156

A glucokinase activator or a prodrug thereof; the pharmaceutical salt, the isotope label, the crystal form, the hydrate, the solvate, the diastereoisomer or the enantiomer can be used for preventing, relieving or treating cognitive impairment or neurodegenerative diseases in subjects, or delaying progression of cognitive impairment or neurodegenerative diseases in subjects. The invention also relates to the application in the aspect of reducing the risk of cognitive impairment or neurodegenerative diseases of subjects.

The present application relates to a kind of combination of glucose kinase activator and PI3K inhibitor.The present application finds that glucose kinase activator can not only alleviate the hyperglycemia caused by PI3K inhibitor, but also can enhance the anti-tumor effect of PI3K inhibitor, and promote the further clinical application of PI3K inhibitor.