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US 11,377,452 B2Granted
Glutamate transporter activators and methods using same
AssigneeDrexel University
InventorsSandhya Kortagere, Andreia C. K. Mortensen, Ole V. Mortensen, Joseph M. Salvino
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Abstract
The present invention provides compounds useful for treating, ameliorating or preventing a disease or disorder that is caused, induced or characterized by abnormal reduction in glutamate transporter activity or abnormal increase in extracellular CNS glutamate concentration in a subject. In certain embodiments, the compound stimulates a glutamate transporter.
Claims9
A compound, or an enantiomer, diastereoisomer, salt or solvate thereof, having the structure of formula (I):
- wherein:
- R1 is selected from the group consisting of —(C2-C3 alkyl)-(C3-C6 cycloalkyl) and —(C0-C3 alkyl)-(C6-C10 aryl),
- wherein the cycloalkyl and aryl group are independently optionally substituted by at least one substituent selected from the group consisting of —C1-C6 alkyl, —OH, —C1-C6 alkoxy, halogen, —NH2, —N(CH3)2, —C(═O)OH, trifluoromethyl, —C≡N, —C(═O)O(C1-C4)alkyl, —C(═O)NH2, —SO2NH2, —C(═NH)NH2, and —NO2;
- each occurrence of R2 is independently selected from the group consisting of H, —C1-C6 alkyl, —OH, —C1-C6 alkoxy, halogen, —NH2, —N(CH3)2, —C(═O)OH, trifluoromethyl, —C≡N, —C(═O)O(C1-C4)alkyl, —C(═O)NH2, —SO2NH2, —C(═NH)NH2, and —NO2;
- n is 1;
- R3 is selected from the group consisting of —(C═O)0-1(C0-C3 alkyl)-(C3-C6 cycloalkyl) and —(C═O)0-1(C0-C3 alkyl)-(C6-C10 aryl),
- wherein the cycloalkyl, and aryl groups are independently optionally substituted by one substituent selected from the group consisting of —C1-C6 alkyl, —OH, —C1-C6 alkoxy, halogen, —NH2, —N(CH3)2, —C(═O)OH, trifluoromethyl, —C≡N, —C(═O)O(C1-C4)alkyl, —C(═O)NH2, —SO2NH2, —C(═NH)NH2, and —NO2;
- with the proviso that R1 is not —(C1 alkyl)-phenyl.
5 more elements
A compound selected from the group consisting of:
- 3-((4-cyclohexylpiperazin-1-yl)(1-phenethyl-1H-tetrazol-5-yl)methyl)-6-methoxy-quinolin-2(1H)-one (GT949)
- 6-methoxy-3-((1-phenethyl-1H-tetrazol-5-yl)(4-(3-(trifluoromethyl)phenyl)piperazin-1-yl)methyl)quinolin-2(1H)-one (GT951)
- 3-((4-(benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)(1-phenethyl-1H-tetrazol-5-yl)methyl)-6,7-dimethylquinolin-2(1H)-one (GT835)
- and
- 3-((4-(furan-2-carbonyl)piperazin-1-yl)(1-phenethyl-1H-tetrazol-5-yl)methyl)-6,8-dimethylquinolin-2(1H)-one (GT729)
- an enantiomer, diastereoisomer, salt or solvate thereof, and any mixtures thereof.
3 more elements
Dependencies are inferred from the claim text.