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dihydro-oxazol-2-amine derivatives
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
ALESSANDRA POLARA,MATTHIAS NETTEKOVEN,ROGER NORCROSS
申请号:
BR112013010558
公开号:
BR112013010558A2
申请日:
2011.10.26
申请国别(地区):
BR
年份:
2016
代理人:
摘要:
dihydro-oxazol-2-amine derivatives. The present invention relates to compounds of formula (I) wherein R1 is hydrogen or lower alkyl; R2 is hydrogen or heteroaryl, optionally substituted by one or more halogen, lower alkyl, halogen substituted lower alkyl, lower alkoxy, halogen substituted lower alkoxy, cyano, lower alkyl, lower alkyl s (o) -2-lower alkyl, c (o) lower alkyl or C 3-6 cycloalkyl; R3 is hydrogen, halogen, lower alkyl, halogen substituted lower alkyl, lower alkoxy, halogen substituted lower alkoxy, cyano lower alkyl lower alkyl, lower alkyl 2-lower alkyl C 1 -C 6 lower alkyl or C 3-6 cycloalkyl; R4 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 a pharmaceutically suitable acid addition salt thereof. It has now been observed that the compounds of formula I have good affinity for 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 diseases such as alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetes complications, obesity, dyslipidemia, energy consumption and assimilation disorders, disorders and malfunction of homeostasis. body temperature, sleep and circadian rhythm disorders and cardiovascular disorders.derivados de di-hidro-oxazol-2-amina. a presente invenção refere-se aos compostos de fórmula (i) em que r^ 1^ é hidrogênio ou alquila inferior; r^ 2^ é hidrogênio ou é heteroarila, opcionalmente substituído por um ou mais halogêneo, alquila inferior, alquila inferior substituída por halogêneo, alcóxi inferior, alcóxi inferior
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