abstract |
Imaging agents of formulas (I)-(V) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formulas (I)-(V) capable of binding to tau proteins and β-amyloid peptides are presented herein. The invention also relates to methods of imaging Αβ and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formulas (I)-(V) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders. Formula (V) or a pharmaceutically acceptable salt thereof, and stereoisomers thereof, wherein: X 25 -X 28 are each independently CH, CR 11 , or N; X 29 is CH, N, O or S; X 30 is CH, C, or N; X 31-34 are each independently CH, CR 12 , CR 13 or N; RII-RU are each independently H, halogen, hydroxy, nitro, cyano, ammo, alkyl, alkylaryl, alkylamino, alkylamine, arylamine, arylamino, alkoxy,— (O-CH 2 - CH 2 ) n -, alkenyL alkynyl, aryloxy, NRl0COOalkyl, NRl0 COOaryU NRW COalkyl, NR 10 CO aryl, COOalkyl, COOaryl, COalkyl, COaryl, aryl, cycloalkyl, cycloalkylamino, cycloalkylamine, bicyclic, saturated heterocycle and unsaturated heterocycle, wherein at least one carbon of R 11 -R 13 is optionally replaced with N, Q, S, triazole, or halo, and, wherein at least one hydrogen is optionally replaced with halo, amine, amino, alkoxy, nitro, alkyl, alkenyL alkynyl, aryloxy, alkylaryl, alkylamino, alkylamine, NRioCOOalkyl, NR 10 COOaryl, NR 10 COalkyl, NR,0 CO aryl, COOalkyl, COOaryl, COalkyl, COaryl, aryl, cycloalkyl, cycloalkylamino, cycloalkylamine, bicyclic saturated heterocycle and unsaturated heterocycle, a leaving group, CN, OH or a radioactive isotope. |