Publication number: 20220064195
Abstract: Compounds of formula I, their respective mirror-image enantiomers, and mixtures—preferably racemic—of both enantiomers, wherein R1 is ethyl or phenyl; R2 is methyl, phenyl, monosubstituted phenyl, benzyl, or monosubstituted benzyl; R3 is selected from the group consisting of: (C1-C6)-alkyl, (C1-C6)-cycloalkyl, —[CH2]n-phenyl, —[CH2]n-1-naphtyl, —[CH2]n-2-naphtyl, and —[CH2]n-[substituted phenyl]; wherein [substituted phenyl] is a phenyl radical with one, two or three substituents independently selected from: F, Cl, Br, (C1-C3)-alkyl, (C1-C3)-alkyloxy, phenyl, phenoxy, —CF3, —OCF3, nitro, —CN, —CO—(C1-C3)-alkyl and benzoyl; and n is an integer between 0 and 4; have a high affinity for imidazoline receptors of the I2 type, i.e. they are I2-IR ligands. Consequently they are applicable in the prevention or treatment of brain disorders in animals, including humans, particularly of neurodegenerative disorders, and more particularly of Alzheimer's disease (AD).
Type:
Application
Filed:
December 19, 2018
Publication date:
March 3, 2022
Inventors:
María Carmen ESCOLANO MIRÓN, Mercè PALLÀS LLIBERIA, Cristian Gaspar GRIÑÁN FERRE, Sònia ABÁS PRADES, Luis-Felipe CALLADO HERNANDO, Jesús A. GARCÍA SEVILLA