2-phenylimidazo[1,2-a]pyrimidines as imaging agents

Abstract

The present invention relates to compounds of general formula wherein R1 is (a) phenyl, optionally substituted by one or two substituents selected from 3H, halogen, lower alkyl, di-methyl-amino, NHC(O)-lower alkyl, C(O)O-lower alkyl, lower alkoxy, OC(3H)3, O11CH3, OCH2CH218F, lower alkoxy substituted by halogen, hydroxy, lower alkyl substituted by hydroxy, S-lower alkyl, (b) heterocyclyl group, (c) benzo[d][1,3]dioxol-5-yl, (d) 2,3-dihydrobenzo[b][1,4]dioxin-6-yl, (e) indolin-2-one, or (f) heteroaryl, selected from the group consisting of thiophenyl, benzofuranyl, benzothiophenyl, pyrazinyl, and benzothiazolyl; R2 is hydrogen, lower alkyl or lower alkyl substituted by halogen; R3 is lower alkyl, C(3H)3, 11CH3, lower alkyl substituted by halogen, —(CH2)2—O-lower alkyl substituted by halogen or cycloalkyl; or R2 and R3 form together with the N-atom to which they are attach a ring containing —CH2CH2CHRCH2CH2—, —CH2CH2CHRCH2—, —CH2CHRCH2—, —CH2CH2—NR—CH2CH2—, —CH2CH2—O—CH2CH2—, or, R is hydrogen, halogen, lower alkyl substituted by halogen or lower alkoxy; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds are suitable as imaging tool, which will improve diagnosis by identifying potential patients with excess of tau aggregates in the brain, which may be likely to develop Alzheimer's disease.

Dependencies are inferred from the claim text.