F. HOFFMANN-LA ROCHE AG;GALLEY, Guido;NORCROSS, Roger;GHELLAMALLAH, Cédric;PFLIEGER, Philippe
发明人:
GALLEY, Guido,GHELLAMALLAH, Cédric,NORCROSS, Roger,PFLIEGER, Philippe
申请号：
EPEP2012/060627
公开号：
WO2012/168260A1
申请日:
2012.06.06
申请国别(地区):
EP
年份:
2012
代理人:
摘要：
The invention relates to compounds of formula wherein R1 is hydrogen or phenyl, optionally substitutes by halogen, CN or lower alkoxy or lower alkoxy substituted by halogen； R2 is hydrogen or lower alkyl； R3 is hydrogen or lower alkyl or is phenyl optionally substituted by one or more substituents, selected from halogen, cyano or lower alkoxy substituted by halogen, or is pyridinyl, optionally substituted by halogen or lower alkyl substituted by halogen, or is pyrimidinyl, optionally substituted by lower alkyl substituted by halogen, or is pyrazinyl, optionally substituted by halogen, cyano or lower alkyl substituted by halogen； R4 is hydrogen, lower alkyl or phenyl； Z is a bond, -CH2- or -O-； or to a pharmaceutically suitable acid addition salt thereof. It has now been found that the compounds of formulas IA and IB 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.La présente invention concerne des composés de formule dans laquelle R1 est un atome d'hydrogène ou un groupe phényle, facultativement substitué par un atome d'halogène, un groupe CN ou un groupe alcoxy inférieur ou un groupe alcoxy inférieur substitué par un atome d'halogène ； R2 est un atome d'hydrogène ou un groupe alkyle inférieur ； R3 est un atome d'hydrogène ou un groupe alkyle inférieur ou est un groupe phényle
