73 results about "GPR119" patented technology

Provided herein are compounds of the formula (I):as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.

Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.

The present invention relates to methods of using GPR119 receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY, such as conditions modulated by stimulation of NPY Y2 receptor (Y2R). Agonists of GPR119 receptor are useful as therapeutic agents for treating or preventing a condition modulated by PYY, such as a condition modulated by stimulation of Y2R. Conditions modulated by PYY such as may be a condition modulated by stimulation of Y2R include bone-related conditions, metabolic disorders, angiogenesis-related conditions, ischemia-related conditions, convulsive disorders, malabsorptive disorders, cancers, and inflammatory disorders.

A compound of formula Ior a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as GPR119 modulators, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus, and pharmaceutical compositions containing them.

Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR 119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA.

Compounds of formula (I) or pharmaceutically acceptable salts thereof, are GPCR (GPR119) agonists and are useful as for the treatment of diabetes and obesity.

A method of modulating the activity of the GPR119 G protein-coupled receptor comprising administering to a mammalian patient in need thereof a therapeutically effective amount of at least one compound of Formula I or Formula IA and, optionally, an additional therapeutic agent.

Compounds of formula (I) or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful as regulators of satiety, e.g. for the treatment of obesity, and for the treatment of diabetes.

Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, D, Di, E, J, L, n, Q, R2 and R4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.

The present invention relates to a pharmaceutical composition containing a G protein coupled receptor 119 (GPR119) ligand as an active ingredient for preventing or treating non-alcoholic fatty liver disease. More particularly, it was confirmed that the GPR119 ligand, which has been developed as only an anti-diabetic drug, exhibits superior effects on the treatment of non-alcoholic fatty liver and the signal pathways in hepatocytes therefor differ from the signal pathways in the small intestine and the pancreas exhibiting anti-diabetic effects, whereby the GPR119 ligand can be useful to treat non-alcoholic fatty liver.

Compounds of Formula I that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.

The present invention is directed to therapeutic compounds which have dual activity as agonists of GPR119 and inhibitors of DPP-IV and are useful for the treatment of metabolic disorders including type II diabetes.

The present invention relates to compounds of Formula (I) that are useful for treating, preventing and / or managing the diseases, disorders, syndromes or conditions associated with the modulation of GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods of treating, preventing and / or managing diseases, disorders syndromes or conditions associated with the modulation of GPR119 receptor by using either alone or in combinations of Formula (I).

Novel compounds of structure Formula I:or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein n1, R1, R2, R3 and R4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.

The invention discloses bicycloheteroaryl compounds of formula (I), pharmaceutical compositions containing the compounds, application of the compounds in regulating the activity of GPR119 and preparing medicines for treating diseases associated with metabolism, and methods for treating diseases associated with metabolism.

Compounds of formula (I) wherein: X is (A) or (B); Y is O or a bond; R1 is —C(O)—O—R3 or R2 is hydrogen, cyano, C1-C6 alkyl, or C3-C6 cycloalkyl; R5 is hydrogen, cyano, nitro, C1-C6 fluoroalkyl, C1-C6 alkyl, C1-C6 alkoxy, fluoroalkoxy, or C3-C6 cycloalkyl; R6 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, —C(O)—NH2, or C1-C6 alkyl substituted with hydroxy or C1-C6 alkoxy; m is 1 or 2, wherein when m is 1 then R8 is hydrogen, C1-C6 alkyl, —CH2—(C1-C5)haloalkyl, C3-C6 cycloalkyl, or C1-C6 alkyl substituted with hydroxy; and when m is 2 then each R8 is independently C1-C3 alkyl or —CH2—(C1—C2)haloalkyl; modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.

The present invention relates to the use of GPR119 receptor agonists for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. The present invention further relates to the use of a GPR119 receptor agonist in combination with a dipeptidyl peptidase IV (DPP-IV) inhibitor for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. A GPR119 receptor agonist and the combination of a GPR119 receptor agonist and a DPP-IV inhibitor promote bone formation in an individual.

The present invention relates to the GPR119 receptor agonists: 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N,N-dimethylbenzamide; -fluoro-4-(5-fluoro-6-(4-(3-(2-fluoro-propan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N-methylbenzamide; and 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)benzamide, and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single pharmaceutical agent or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.

Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR (GPR119) agonists and are useful as for the treatment of diabetes and obesity.

The present invention relates to the use of GPR119 receptor agonists for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. The present invention further relates to the use of a GPR119 receptor agonist in combination with a dipeptidyl peptidase IV (DPP-IV) inhibitor for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. A GPR119 receptor agonist and the combination of a GPR119 receptor agonist and a DPP-IV inhibitor promote bone formation in an individual.

The present invention is directed to therapeutic compounds of the following formula (I)which have activity as agonists of GPR119 and are useful for the treatment of metabolic disorders including type II diabetes.

The present invention is directed to therapeutic compounds which have activity as agonists of GPR119 and are useful for the treatment of metabolic disorders including type II diabetes.

Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, D, Di, E, J, L, n, Q, R2 and R4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.

The present invention relates to the use of GPR119 receptor agonists for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. The present invention further relates to the use of a GPR119 receptor agonist in combination with a dipeptidyl peptidase IV (DPP-IV) inhibitor for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. A GPR119 receptor agonist and the combination of a GPR119 receptor agonist and a DPP-IV inhibitor promote bone formation in an individual.

Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPFM 19 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.