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US 8,013,015 B2Granted
Small molecule inhibitors of ghrelin O-acyltransferase
AssigneeBoard of Regents, The University of Texas System
InventorsPatrcik G. Harran, Michael S. Brown, Joseph L. Goldstein, Jing Yang, Tong-Jin Zhao
Life of this patent
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Abstract
Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules. Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.
Claims24
A pharmaceutical composition comprising a ghrelin O-acyltransferase (GOAT) inhibitor of the structure 1:
- wherein:
- R1, is selected from unsubstituted n-heptanyl, unsubstituted n-heptenyl, unsubstituted n-heptynyl and unsubstituted methyl-diethylene glycol (—CH2OCH2CH2OCH2CH3);
- R2-R5 are independently selected from hydrogen, optionally hetero-, optionally substituted alkyl, optionally hetero-, optionally substituted alkenyl, optionally hetero-, optionally substituted alkynyl, optionally hetero-, optionally substituted aryl, and an optionally substituted heteroatom;
- A is selected from NH, and N-alkyl;
- G is O;
- X is selected from hydroxyl, amino, alkylamino, and alkylthio;
- Y is C;
- and
- Z is selected from O, S, NH and N-alkyl,
- or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient, wherein said inhibitor inhibits said ghrelin O-acyltransferase (GOAT), and said composition is suitable for pharmaceutical use.
7 more elements
A pharmaceutical composition comprising a ghrelin O-acyltransferase (GOAT) inhibitor or a pharmaceutically acceptable salt thereof, wherein said inhibitor is selected from the group consisting of:
Dependencies are inferred from the claim text.