abstract |
The present invention relates to imaging agents of formula (I) to (V) capable of binding to tau proteins and β-amyloid peptides and to nervous systems comprising administering to patients in need of such formulas (I) to (V). A method for detecting a disease. The invention also provides a method of imaging Aβ and tau aggregates, which incorporates a detectable amount of a pharmaceutical formulation comprising a radiolabeled compound of formula (I) to formula (V), and contains amyloid deposits in a patient and / or Or to a labeled compound associated with a tau protein. These methods and compositions allow preclinical diagnosis and monitoring of the progression of AD and other neurological diseases. In the compound of formula (V) or a pharmaceutically acceptable salt thereof and stereoisomer thereof, the group definitions are as follows: 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; R 11 -R 13 are each independently H, halogen, hydroxy, nitro, cyano, amino, alkyl, alkylaryl, alkylamino, alkylamine, arylamine, arylamino, alkoxy,-(0-CH 2 -CH 2) n -, alkenyl, alkynyl, aryloxy, NR 10 COO-alkyl, NR 10 COO aryl, NR 10 CO-alkyl, NR 10 CO aryl, COO alkyl, COO aryl, CO-alkyl, CO aryl, aryl, cycloalkyl , Cycloalkylamino, cycloalkylamine, bicyclic, saturated heterocycle and unsaturated heterocycle, wherein one or more carbons of R 11 -R 13 are optionally substituted with N, O, S, triazole or halo Where at least one hydrogen is halo, amine, amino, alkoxy, nitro, alkyl, alkenyl, alkynyl, aryloxy, alkylaryl, alkylamino, alkylamine, NR 10 COOalkyl, NR 10 COOaryl, NR 10 CO Alkyl, NR 10 COaryl, COOalkyl, COOaryl, COalkyl, COaryl, aryl, cycloalkyl, cycloalkylamino Optionally substituted with cycloalkylamine, bicyclic, saturated heterocycle and unsaturated heterocycle, leaving group, CN, OH or radioactive isotope: |