CASHION, DANIEL KURT,CHEN, GANG,KASI, DHANALAKSHMI,KOLB, HARTMUTH C.,LIU, CHANGHUI,SINHA, ANJANA,SZARDENINGS, ANNA KATRIN,WANG, ERIC,YU, CHUL,ZHANG, WEI,GANGADHARMATH, UMESH B.,WALSH, JOSEPH C.
申请号：
CA2794004
公开号：
CA2794004C
申请日:
2011.03.22
申请国别(地区):
CA
年份:
2016
代理人:
摘要：
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 ß-amyloid peptides are presented herein. The invention also relates to methods of imaging ?ß 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: X25-X28 are each independently CH, CR11, or N X29 is CH, N, O or S X30 is CH, C, or N X31-34 are each independently CH, CR12, CR13 or N RII-RU are each independently H, halogen, hydroxy, nitro, cyano, ammo, alkyl, alkylaryl, alkylamino, alkylamine, arylamine, arylamino, alkoxy, (O-CH2- CH2)n-, alkenyL alkynyl, aryloxy, NRl0COOalkyl, NRl0 COOaryU NRW COalkyl, NR10 CO aryl, COOalkyl, COOaryl, COalkyl, COaryl, aryl, cycloalkyl, cycloalkylamino, cycloalkylamine, bicyclic, saturated heterocycle and unsaturated heterocycle, wherein at least one carbon of R11-R13 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, NR10 COOaryl, NR10 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.
