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DERIVES HETEROCYCLIQUES UTILISES COMME RECEPTEURS ASSOCIES A DES AMINES SOUS FORME DE TRACE (TAAR)
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
GALLEY, GUIDO,GOERGLER, ANNICK,NORCROSS, ROGER,PFLIEGER, PHILIPPE
申请号:
CA2856204
公开号:
CA2856204A1
申请日:
2013.01.08
申请国别(地区):
CA
年份:
2013
代理人:
摘要:
The present invention relates to compounds of formula (I) wherein R1 is a one or two membered heteroaryl group, selected from the group consisting of formula (a), (b), (c), (d), (e), (f), (g), (h), (i), (j); R2 is hydrogen or halogen; or R1 and R2 may form together with the carbon atoms to with they are attached the following rings formula (k), (l), (m), (n), (o). R3 is hydrogen, halogen or lower alkyl; n is 1 or 2; R4 is phenyl, optionally substituted by one or two substituents, selected from halogen or cyano, or is pyridinyl, optionally substituted by halogen, or is tetrahydropyran, or is -NH-C(O)-phenyl, optionally substituted by halogen; R5 is hydrogen or halogen; R6 R13 are phenyl, optionally substituted by halogen: R14 is NH-C(O)-phenyl, substituted by halogen; R15 is hydrogen, lower alkyl substituted by halogen or is halogen; R16 is hydrogen or lower alkoxy; R17 is pyridinyl, optionally substituted by lower alkoxy or lower alkyl substituted by halogen; or to a pharmaceutically suitable acid addition salt thereof, to all racemic mixtures, to all their corresponding enantiomers and/or optical isomers and to all tautomeric forms of compounds of formula I. 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.
来源网站:
中国工程科技知识中心
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