1,2,4-oxadiazole derivatives as drugs modulating the GLP-1 peptide receptor
Inventors
Rodríguez De Fonseca, Fernando Antonio • ROMERO CUEVAS, MIGUEL • Orio Ortíz, Laura • DECARA DEL OLMO, JUAN MANUEL • Alonso Scrignoli, Monica
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-9050347-B2
Publication Date
2015-06-09
Expiration Date
Abstract
The present invention relates to the use of a compound of formula (I): or a pharmaceutically acceptable solvate or salt thereof in the preparation of a medicinal product for the prevention and/or the treatment of a disease in which the GLP-1 receptor participates or mediates, such as eating disorders or diseases, for example, obesity, anorexia, lipid dysfunction, diabetes, hyperinsulinism and cardiovascular diseases or metabolic syndrome.
Core Innovation
Oxadiazole derivative compounds of formula (I) and related embodiments, including formula (II), are provided for modulating GLP-1 receptor functions. The compounds are described as capable of acting as GLP-1 receptor agonists, allosteric modulators, or antagonists, including pharmaceutically acceptable solvates and pharmaceutically acceptable salts. The description includes variable definitions for R1, R2, R3, y, and n, and defines broad structural classes and optional substituents for these variables.
The compounds of formula (I) are used in a method for the treatment of a disease in a mammal in which the GLP-1 receptor participates or mediates. The use includes reducing body fat inducing satiety and controlling intake, and treating diseases including eating disorders, obesity, anorexia, lipid dysfunction, diabetes, hyperinsulism, metabolic syndrome, and cardiovascular diseases. The method comprises administering an effective amount of a compound of formula (I) together with a pharmaceutically acceptable vehicle.
The patent document further enumerates example compounds including specific named formula (I) embodiments and explicitly considers stereoisomers, salts, and solvates. Experimental examples described in the document include assays related to intake control, insulin secretion and GLP-1 enhancement in rat insulinoma cells, and parenteral glucose overload tests in Wistar rats assessing glycemia.
Claims Coverage
The partial content provides one independent claim directed to a treatment method using a compound of formula (I) to modulate GLP-1 receptor functions for specified treatment contexts. The listed dependents focus on narrowing structural substituent options and on specifying particular named embodiments and optional salt/solvate forms, as well as narrowing one treatment context to obesity.
Method for treatment via GLP-1 receptor participation or mediation
A method for the treatment, in a mammal suffering or being susceptible to suffer from a disease in which the GLP-1 receptor participates or mediates, for reducing body fat inducing satiety and controlling intake, or for the treatment of an eating disorder and a disease selected from obesity, anorexia, lipid dysfunction, diabetes, hyperinsulism, metabolic syndrome and cardiovascular diseases, comprising administering to said mammal an effective amount of a compound of formula (I) together with a pharmaceutically acceptable vehicle.
Compound of formula (I) defined by R1, R2, R3 and y
The method uses a compound of formula (I) wherein R1 is selected from C6-C15 aryl, C3-C15 heteroaryl, C7-C15 arylalkyl and C3-C15 heteroarylalkyl; R2 is selected from hydrogen, C1-C6 alkyl and C2-C6 alkenyl; each R3 is independently selected from the listed heterocyclic and heteroaryl groups and additional defined substituent options; and y is 1, 2, 3, 4 or 5, with allowance for a pharmaceutically acceptable solvate or salt thereof.
Across the provided claim set, the core coverage is a GLP-1 receptor-targeted treatment method in mammals using compounds of formula (I) defined by the specified R1/R2/R3/y structural constraints, formulated with a pharmaceutically acceptable vehicle. Dependent claim refinements in the provided partial content restrict R1 choices, fix R2 to hydrogen, restrict y to 1 or 2, and specify named formula (I) embodiments including pharmaceutically acceptable solvate or salt forms, with one dependent narrowing to a cosmetic method for obesity.
Stated Advantages
Reducing body fat inducing satiety and controlling intake.
Treatment of diseases selected from an eating disorder and diseases comprising obesity, anorexia, lipid dysfunction, diabetes, hyperinsulism, metabolic syndrome and cardiovascular diseases.
Documented Applications
Methods for treatment in a mammal suffering or being susceptible to suffer from a disease in which the GLP-1 receptor participates or mediates, including reducing body fat inducing satiety and controlling intake, and treating eating disorders, obesity, anorexia, lipid dysfunction, diabetes, hyperinsulism, metabolic syndrome and cardiovascular diseases.
A cosmetic method to treat obesity in a mammal by administering an effective amount of a compound of formula (I) together with a pharmaceutically acceptable vehicle.
Interested in licensing this patent?