Imaging agents for detecting neurological disorders

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 [beta]-amyloid peptides are presented herein. The invention also relates to methods of imaging A[beta] 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, NRl0 COO alkyl, NRl0 COO aryl NR10 CO alkyl, NR10 CO aryl, COO alkyl, COO aryl, CO alkyl, CO aryl, 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, NR 10COO alkyl, NR10 COO aryl, NR10 CO alkyl, NR10 CO aryl, COO alkyl, COO aryl, CO alkyl, CO aryl, aryl, cycloalkyl, cycloalkylamino, cycloalkylamine, bicyclic saturated heterocycle and unsaturated heterocycle, a leaving group, CN, OH or a radioactive isotope.

Description

[0001] Related Patent Applications [0002] This application is a continuation-in-part of USSN 12 / 661,777 (filed March 23, 2010), which is incorporated herein by reference in its entirety. USSN 12 / 661,777 is based on and claims priority from US Provisional Application 61 / 162,421 (filed March 23, 2009), which is incorporated herein by reference in its entirety. [0003] The above-mentioned application and all documents cited therein or during their prosecution (“Application Cited Documents”) and all documents cited or referenced in said Application Cited Documents and all documents cited or referenced therein (“in which Cited Documents") and all documents cited or referenced in said documents cited therein, as well as manufacturer's instructions, instructions, product descriptions, and together with the product brochure, are incorporated herein by reference and may be used in the practice of the present invention. technical field [0004] In general, the invention relates to ...

AI Technical Summary

Problems solved by technology

[0010] Unfortunately, understanding the link between the uptake of these tracers and the associated biochemical processes has remained unresolved for many years since AD ​​could not be confirmed in patients until histological examination was performed.

Images