DIHYDROOXAZOL-2-AMINE DERIVATIVES
    3.
    发明公开
    DIHYDROOXAZOL-2-AMINE DERIVATIVES 有权
    二氢 - 2 AMINDERIVATE

    公开(公告)号:EP2635560A1

    公开(公告)日:2013-09-11

    申请号:EP11776154.4

    申请日:2011-10-26

    摘要: The invention relates to compounds of formula (I) wherein R
    1 is hydrogen or lower alkyl; R
    2 is hydrogen or is heteroaryl, optionally substituted by one or more halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, cyano, S-lower alkyl, S(O)-lower alkyl, S(O)
    2 -lower alkyl, C(O)-lower alkyl or C
    3-6 -cycloalkyl; R
    3 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, cyano, S-lower alkyl, S(O)-lower alkyl, S(O)
    2 -lower alkyl, C(O)-lower alkyl or C
    3-6 -cycloalkyl; R
    4 is hydrogen or lower alkyl; (A) is phenyl or pyridinyl, wherein the N-atom may be in different positions; X is a bond or CH(CF
    3 )-; Ar is aryl or heteroaryl, optionally substituted by one or more R
    3 ; or to a pharmaceutically suitable acid addition salt thereof. It has now 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.