4-IMIDAZOLINES AND THEIR USE AS ANTIDEPRESSANTS

摘要

The present invention relates to compounds of formula (I) wherein R1 is hydrogen, halogen or lower alkyl; R2 is hydrogen or amino; X-Y is -(CH2)n-, N(R)-CH2-, -O-CH2- or -S-CH2-; Ar is phenyl or naphthyl; n is 1 or 2; R is hydrogen or lower alkyl; and to their pharmaceutically active salts, with the exclusion of the racemic compound 4-benzyl-4,5-dihydro-lH-imidazole or its tautomer (CAS 131548-83-9). It has been found that the compounds of formula (I) have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.