| abstract |
The invention relates to compounds of the formula: wherein: R is hydrogen or lower alkyl, R1 is - (CH2) n- (O) o-heterocycloalkyl or -C (O) -heterocycloalkyl, in which the heterocyclolakyl group is optionally substituted with lower alkyl, hydroxy, halogen or with - (CH2) p-aryl, n is 0, 1 or 2, or is 0 or 1, p is 0, 1 or 2, R2 is CF3, cycloalkyl, optionally substituted with lower alkoxy or halogen, or is indan-2-yl, or is heterocycloalkyl, optionally substituted with heteroaryl, or is aryl or heteroaryl, in which the aromatic rings are optionally substituted with one or two substituents, selected from lower alkyl, halogen , heteroaryl, hydroxy, CF3, OCF3, OCH2CF3, OCH2-cycloalkyl, OCH2C (CH2OH) (CH2Cl) (CH3), S-lower alkyl, lower alkoxy, CH2-lower alkoxy, lower alkynyl or cyano, or with -C (O ) -phenyl, -O-phenyl, -O-CH2-phenyl, phenyl or -CH2-phenyl, and in which the phenyl rings may optionally be substituted with halogen, -C (O) -alq lower uyl, -C (O) -OH or -C (O) -O-lower alkyl, or the aromatic rings are optionally substituted with heterocycloalkyl, OCH2-oxethan-3-yl or O-tetrahydropyran-4-yl, optionally substituted With lower alkyl, X is a bond, -NR'-, -CH2NH-, -CHR '' -, - (CHR '') qO-, -O- (CHR '') q- or - (CH2) 2- , Y is a bond or -CH2-R 'is hydrogen or lower alkyl, R' 'is hydrogen, lower alkyl, CF3, lower alkoxy, q is 0, 1, 2 or 3, or a pharmaceutically acceptable acid addition salt thereof. It has now been found that the compounds of formula I have a good affinity with the receptors associated with traces of amines (TAARs), especially with TAAR1. The compounds can 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 dysfunction of homeostasis of body temperature, sleep and circadian rhythm disorders, and cardiovascular disorders. |