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US 11,447,453 B2Granted
Metabotropic glutamate receptor negative allosteric modulators (NAMs) and uses thereof
AssigneeSanford Burnham Prebys Medical Discovery Institute
InventorsNicholas David Peter Cosford, Dhanya Raveendra-Panickar, Douglas J. Sheffler, John Howard Hutchinson, Reto Andreas Gadient
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Abstract
Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.
Claims19
A compound, or a pharmaceutically acceptable salt thereof, having the structure of Formula (I):
- wherein:
- ring
- is thiazolyl, thiadiazolyl, or triazolyl;
- ring
- is an aryl ring or heteroaryl ring;
- R1 is —CO2H, —CN, —C(O)NHOH, —C(O)NHOMe, —C(O)NHSO2Me, —NHC(O)Me, —C(O)NHMe,
- each R2 is independently halogen, —OR5, substituted or unsubstituted C1-C6alkyl, or substituted or unsubstituted C1-C6fluoroalkyl;
- each R3 is independently substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C3-C6cycloalkyl, or substituted or unsubstituted aryl;
- each R4 is independently halogen, —OR5, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C3-C6cycloalkyl, or substituted or unsubstituted aryl;
- or two R4 taken together with the carbon atoms to which they are attached to form a substituted or unsubstituted C2-C8heterocycloalkyl;
- each R5 is independently hydrogen, or substituted or unsubstituted C1-C6alkyl;
- n is 0, 1, 2, or 3;
- m is 0 or 1;
- and
- p is 0, 1, 2, or 3.
12 more elements
A compound of having the structure:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.