公开(公告)号：EP2791113A1

公开(公告)日：2014-10-22

申请号：EP12813630.6

申请日：2012-12-13

申请人： GE Healthcare Limited

发明人： JONES, Clare ,  GLASER, Matthias Eberhard ,  WYNN, Duncan ,  NAIRNE, James ,  MOKKAPATI, Umamaheshwar P. ,  NEWINGTON, Ian, Martin ,  RANGASWAMY, Chitralekha ,  JOSE, Jinto ,  JOHANSSON, Saga

IPC分类号： C07D213/74 ,  C07D237/24 ,  C07D495/04 ,  C07C243/22 ,  A61K31/5025 ,  A61P25/00

CPC分类号： A61K51/0459 ,  A61K49/0052 ,  C07B59/002 ,  C07D213/74 ,  C07D237/24 ,  C07D495/04 ,  G01N33/6896 ,  G01N2800/2821

摘要： Pyridazinone compounds of Formula I: (I) wherein: R' is alkyl or Ar, optionally substituted with at least one alkyl, halo¬ gen, hydroxyl, alkoxy, haloalkoxy, acid, ester, amino, nitro, amide, or alkoxyhalo; 2 R is independently alkyi, alkynyl, ester, amino, amide, acid, aryl, heteroaryl, aminoalkyl, -C(=0)alkyl, -C(=0)aryl, -C(=0)heteroaryl, -C(=0)heterocycloalkyl, - C(=0)heterocycloalkylAr, -C(=0)(CH
2 )
n halo, -C(=0)(CH
2 )nheterocyclyl, or -SC^Ar, optionally substituted with at least one alkyi, alkylhalo, halogen, nitro, aryl, heteroaryl, or heteroaryl(CH
2 )nhalo; R
3 and R
4 are independently hydrogen, alkyi, alkenyl, alkynyl, aryl, heteroaryl; Ar is an aryl, heteroaryl, cycloalkyl, heterocycloalkyl group; n is an integer from 0-10; or a radiolabeled derivative thereof. The compounds are useful as imaging probes of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.