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2-PHENYLIMIDAZO[1,2-A]PYRIMIDINES AS IMAGING AGENTS
专利权人:
发明人:
Luca Gobbi,Henner Knust,Matthias Koerner,Dieter Muri
申请号:
US14945969
公开号:
US20170128598A1
申请日:
2015.11.19
申请国别(地区):
US
年份:
2017
代理人:
摘要:
The present invention relates to compounds of general formulawherein 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 Alzheimers disease.
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