63 results about "GPR120" patented technology

GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.

Aryl GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.

The invention discloses a detection method for the expression of a GPR120 gene based on eGFP. The detection method comprises the following steps: inserting an eGFP fragment to the specific site TAA of the termination codon of the GPR120 gene by using CRISPR / Cas 9 technology so as to obtain a transgenic model mouse with eGFP-labeled GPR120 positive cells; and carrying out excitation by using a fluorescence analyzer and determining the fluorescence intensity of the positive cells of the mouse. The method carries out real-time monitoring on the expression of the GPR120 gene so as to control and reduce errors among groups, guarantee the reliability of results and compensate for and overcome the problems of variability caused by comparison of different groups of histocytes and incapability of monitoring the changes of gene expression at a living cell level in the prior art. According to the invention, the expression level of the GPR120 gene can be immediately determined after collection of cells, and operations and reactions like RNA extraction, inverse transcription and PCR are omitted, so detection of the expression of the GPR120 gene is simpler.

GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.

Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) and Formula (II) as follows:wherein Y, R1, G, and Q are defined herein;andwherein R11, R21, R41, RB1 and G1, are defined herein.

Aryl GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.

The present invention provides compounds of Formula (I) or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.

The present invention provides compounds of Formula (I):or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.

The present invention is directed to bicyclic pyrrole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.

Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) as follows:wherein R1, G, and Q are defined herein.

The present invention provides compounds of Formula (I):or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.

The present invention relates to thioaryl derivatives of Formula 1 as defined in the specification, a method for preparing the same, a pharmaceutical composition comprising the same and use thereof. The thioaryl derivatives of Formula 1 according to the present invention promote GLP-1 formation in the gastrointestinal tract and improve insulin resistance in macrophages, pancreas cells, etc. due to anti-inflammatory action, and can accordingly be effectively used for preventing or treating diabetes, complications of diabetes, inflammation, obesity, non-alcoholic fatty liver, steatohepatitis or osteoporosis.

Fat taste receptors and methods for using the receptors to screen compounds that mimic fat taste are disclosed. The receptors can include G-protein coupled receptor proteins, such as GPR40 or GPR120. New methods for preparing foods are also disclosed that involve testing compounds in the assay system and then incorporating into foods the identified nonfat compounds that have the taste of fat.

The present invention relates to a compound of formula (I), or a tautomer, stereoisomer, geometrical isomer, prodrug, carboxylic acid isostere, solvate, polymorph, N-oxide, S-oxide or pharmaceutically acceptable salt thereof, which are GPR120 agonists. The present invention also relates to a pharmaceutical composition of a compound of formula (I) for the treatment of metabolic disorders, particularly Type 2 diabetes and associated diseases.

Fat taste receptors and methods for using the receptors to screen compounds that mimic fat taste are disclosed. The receptors can include G-protein coupled receptor proteins, such as GPR40 or GPR120. New methods for preparing foods are also disclosed that involve testing compounds in the assay system and then incorporating into foods the identified nonfat compounds that have the taste of fat.

The present invention provides a screening method for determining whether a substance of interest is a substance which alters GPR120 mediated cell stimulating activities, comprising using a substance of interest, a biomembrane containing GPR120, or cells containing said biomembrane, and phospholipase or salts thereof. According to a screening method of the present invention, the method can screen substances such as CCK and GLP-1 which are involved in the secretion of hormones in gastrointestinal tracts.

The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.

The present invention is directed to bicyclic pyrrole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.

GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.

The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.

GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.

The present invention relates to fused heterocyclic compound of Formula (I), a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, a prodrug, a polymorph, N-oxide, S-oxide, or a carboxylic acid isostere thereof; processes for their preparation; pharmaceutical compositions comprising said compounds; and their use for the treatment of the diseases or disorders mediated by GPR120 receptor.

The present invention provides compounds of Formula (I): (I) or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.

Provided is a mouse model construction method of eGFP-labeled GPR120 positive cells. A guideRNA target sequence aiming at a target locus genome is designed, and in vitro transcription is carried out to obtain guideRNA aiming at the genome; donor DNA recombinant plasmid is constructed; the guideRNA and the donor DNA recombinant plasmid are subjected to oosperm injection to obtain F0-generation mice, and the genotype of the F0-generation mice is identified to obtain positive F0-generation mice achieving correct homologous recombination; the F0-generation mice and wild type mice are copulated to obtain F1-generation mice, and the genotype of the F1-generation mice is identified to obtain positive F1-generation mice achieving correct homologous recombination; positive transgenic mice in the generation F1 are subjected to sib mating to obtain F2-generation mice, and homozygous transgenic mice are obtained through screening and identifying. According to the method, GPR120 expression cell express eGFP at the same time, and therefore GPR120 positive cells are distinguished under laser excitation.

The invention provides a GPR120 protein receptor inhibitor and preparation and application thereof, and particularly provides a compound as shown in the following formula I in the specification or pharmaceutically acceptable salt thereof. The compound disclosed by the invention has excellent GPR120 protein inhibition activity.

The present invention is directed to cycloalkenyl derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the GPR120 and / or GPR40 receptors. More particularly, the compounds of the present invention are agonists of GPR120 and / or GPR40, useful in the treatment of, for example, obesity, Type II Diabetes Mellitus, dyslipidemia, etc.

The present invention is directed to bicyclic pyrrole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.

The invention discloses the application of a GPR120 agonist TUG891 to the prevention and treatment of osteoporosis. High concentration TUG891 has significant osteogenic differentiation promotion effect on bone marrow mesenchymal stem cells, and can significantly improve the proliferation activity of bone marrow mesenchymal stem cells; and a low concentration group cannot ascend osteoblast differentiation and proliferation ability of cells, even partially reduce osteogenic differentiation and proliferation potential. In an ovariectomized mice osteoporosis model, TUG891 can improve microstructure of cancellous bone at the distal femur, and increase the mineral deposition rate at the distal femur, which indicate that TUG891 can promote the proliferation differentiation of bone marrow mesenchymal stem cells to improve bone microstructure and play the role of prevention and treatment of osteoporosis.

The invention relates to a GPR120 (G-protein Coupled Receptor 120) small-molecule fluorescent probe and application of the GPR120 small-molecule fluorescent probe. The general structural formula of the fluorescent probe is shown as a formula (I), wherein R represents various types of fluorophores and n represents that the number of carbon is 1 to 6. The fluorescent probe provided by the invention can be used for marking cells or tissues which have a high GPR120 expression level, and has good pharmaceutical activity; fluorescent light is remarkably enhanced when the polarity of the surrounding environment is reduced and the fluorescent probe can be used as a tool medicine for researching pharmacological and physiological characteristics of the GPR120. Furthermore, a preparation method of the compound is mature, reaction conditions are moderate, raw materials are cheap and easy to obtain and operation and post-treatment are convenient. The formula (I) is shown as the description.