abstract |
patent summary: "heterocyclic amine derivatives". The present invention relates to compounds of formula I wherein R1 is hydrogen, lower alkyl, halogen, halogen substituted lower alkyl, lower alkoxy, halogen substituted lower alkoxy, cyano, nitro, C3-6-cycloalkyl, -ch2- C3-6-cycloalkyl, -o-ch2-c3-6-cycloalkyl, -o- (ch2) 2-o-lower alkyl, s (o) 2ch3, sf5, -c (o) nh-lower alkyl, phenyl, -o-pyrimidinyl, optionally substituted by halogen substituted lower alkoxy, or is benzyl, oxetanyl or furanyl; m is 1 or 2; ar is aryl or heteroaryl, selected from the group consisting of phenyl, naphthyl, pyrimidinyl, pyridinyl, benzothiazolyl, quinolinyl, quinazolinyl, benzo [d] [1,3] dioxolyl, 5,6,7,8-tetrahydro-quinazolinyl, pyrazolyl pyrazinyl, pyridazinyl or 1,3,4-oxadiazolyl; y is a bond, -ch2-, -ch2ch2-, -ch (cf3) - or -ch (ch3) -; R2 is hydrogen or lower alkyl; a is cr or n; and r is hydrogen, cyano, halogen or lower alkyl; R 'is hydrogen or halogen; with the proviso that when r 'is halogen, then a is ch; b is ch or n; n is 0, 1 or 2; x is a bond, -ch2- or -o-; or a pharmaceutically active acid addition salt thereof. It has now been found that the compounds of formula I have a good affinity for 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 disorders such as parkinson's disease, neurodegenerative disorders. such as alzheimer's disease, epilepsy, hemicrania, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, energy assimilation and consumption disorders, body temperature homeostasis disorders and malfunctioning , sleep disorders and circadian rhythm, and cardiovascular disorders |