ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
发明人:
Jon T. Njardarson,Isaac Chogii,David Townsend Smith,Edon Vitaku,Daniela C. Zarnescu
申请号：
US16515743
公开号：
US20190350902A1
申请日:
2019.07.18
申请国别(地区):
US
年份:
2019
代理人:
摘要：
The present invention provides compounds and methods for mitigating a clinical condition associated with a neurodegenerative disease or a locomotor dysfunction in a subject. In one particular aspect, the invention relates to compounds and methods for reducing TDP-43 aggregation or toxicity in a subject. The compounds of the invention include those having the following formulas:or a pharmaceutically acceptable salt thereof whereindenotes a chiral center；each of R and R3a is independently hydrogen or alkyl；Ra is —；CF3, —；ORa1, or —；NRb1Rb2；Ra1 is H or alkyl；each of Rb1 and Rb2 is independently H or alkyl；X is —；NR1a—；, wherein R1a is hydrogen, alkyl or a nitrogen protecting group；each of R1, R2 and R3 is independently hydrogen, alkyl, haloalkyl, halide, vinyl, alkynyl, —；CHO, —；C(═；O)R1b (ketone), —；CO2R1c (ester), —；OR1d, OSO2R1e, aryl and heteroaryl, wherein each of R1b, R1c, R1d and R1e is independently alkyl or aryl；R2a is hydrogen, alkyl, haloalkyl, aryl, aralkyl, alkenyl, aralkenyl, cycloalkyl, heteroalkyl, heteroaryl or ester functional group；R2b is alkyl, cycloalkyl, aralkyl, alkenyl, aralkenyl, heteroalkyl, or heteroaryl； andZ is a conjugated electron withdrawing group.
