Compositions and methods for the treatment of metabolic and liver disorders
Inventors
Lian, Brian • Barker, Geoffrey E. • Barnes, Maureen • Yagiz, Kader • Stevens, Erland
Assignees
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Publication Number
US-12318426-B2
Publication Date
2025-06-03
Expiration Date
Abstract
Disclosed herein are small molecule GIP/GLP-1 dual receptor agonist compositions, pharmaceutical compositions, the use and preparation thereof.
Core Innovation
The disclosure relates to small-molecule GIP/GLP-1 dual receptor agonist pharmaceutical compositions for treating metabolic and fatty liver disorders. It provides pharmaceutical compositions comprising a pharmaceutically acceptable excipient and a compound, or a pharmaceutically acceptable salt thereof, wherein the compound has the structure of Formula I and is described as a non-macrocyclic functionalized peptide with defined variable substituent sets and explicit stereochemistry indicated by an asterisked chiral carbon configuration.
The chemical scope defines Formula I using multiple variable substituents including R1, R2, R7, X, Y, R4, R5, R6, Z1, and Z2. Each variable is constrained to specific structural classes, and the asterisked chiral carbon is specified to be either S configuration or R configuration. The disclosure also includes representative sub-formulas and an explicit relationship for X and Y as —OR4 in at least one set.
The disclosure further includes definitions for stereoisomers, racemates, polymorphs, tautomers, solvates/hydrates, and pharmaceutically acceptable acid/base salts, together with structural-convention clarifications for substituted groups and ring formation. It also includes non-limiting synthesis/preparation description and example schemes for intermediates and compounds, as well as example formulations and treatment indications tied to fatty liver diseases and GIP/GLP-1 dual receptor agonism.
Claims Coverage
The independent claim set provided here contains two independent claim themes, both directed to pharmaceutical compositions with defined compound structures. The inventive features are expressed through Formula I or a specified structural group and through stereochemical designation of a chiral carbon as S or R configuration.
Formula I compound in a pharmaceutical composition
A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound, or a pharmaceutically acceptable salt, having the structure of Formula I with defined variable substituents including R1, R2, R7, X, Y, R4, R5, R6, Z1, and Z2, and with at least one of Z1 and Z2 not hydrogen.
Specified structural group compound in a pharmaceutical composition with chiral notation
A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound having the structure selected from a specified group, or a pharmaceutically acceptable salt, wherein “*” indicates a chiral carbon with S configuration or R configuration.
The claimed inventive content is the pharmaceutical composition defined by a compound structure and stereochemical designation, with Formula I substituent constraints including R1/R2 choices, R7 substitution options, and X/Y/R4/R5/R6/Z1/Z2 substituent constraints, together with the explicit requirement that at least one of Z1 or Z2 is not hydrogen.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Treating non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH) and related fatty liver diseases.
Treating metabolic and fatty liver disorders including metabolic disorders and metabolic syndrome.
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