Positive allosteric modulators of the α7 nicotinic acetylcholine receptor and uses thereof

摘要

The present invention relates to compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (α7nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of α7nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also inflammatory diseases.

主权项

1. A compound of formula (I) or a salt thereof: wherein
R1 is selected from optionally substituted aryl, optionally substituted heteroaryl (excluding optionally substituted porphyrins), or optionally substituted heterocyclyl; R2 is selected from C1-C4 alkyl, C3-C5 alkenyl, F, Br, Cl, CN, or C1-C4 haloalkyl;
R3 is selected from hydrogen, C1-C4 alkyl, C3-C5 alkenyl, F, Br, Cl, CN, or C1-C4 haloalkyl; orR2 and R3 together form C4-9 cycloalkyl or C4-9 cycloalkenyl;R4 is selected from optionally substituted heteroaryl, optionally substituted heterocyclyl, or optionally substituted aryl;R5 is selected from hydrogen or optionally substituted alkyl;wherein when both R2 and R3 are Cl, R4 is an optionally substituted heteroaryl or optionally substituted heterocyclyl, andprovided that the following compounds are excluded: