发明名称 4-IMIDAZOLINES AS TAAR'S LIGANDS
摘要 The invention relates to compounds of formula (I) wherein R is hydrogen, lower alkyl or amino; X-R1 is -CH2 -, -CH(lower alkoxy)- or -CH(OH)- and Y-R 2 is -CH2, -CH(lower alkyl)-, -CH(lower alkoxy)- -O-, -S-, -S(O)-, -S(O)2 -, -CH(phenyl)- or -C(lower alkyl)2 -; or X-R1 is -NH- and Y-R2 is -CH2, -CH(l ower alkyl)-, -CH(lower alkoxy)-, -CH(phenyl)- or -C(lower alkyl)2 -; Ar is phenyl, napthyl or benzofuranyl, which rings are unsubstituted or substitute d by one or more substituents, selected from the group consisting of lower a lkyl, lower alkyl substituted by halogen, halogen, lower alkoxy, lower alkox y substituted by halogen, hydroxy, amino, di-alkylamino, morpholinyl, phenyl , benzyl or by O-benzyl; or to pharmaceutically suitable acid addition salts . It has been found that the compounds of formula (I) have a good affinity t o the trace amine associated receptors (TAARs), especially for TAAR1. The co mpounds may be used for the treatment of depression, anxiety disorders, bipo lar disorder, attention deficit hyperactivity disorder (ADHD), stress-relate d disorders, psychotic disorders such as schizophrenia, neurological disease s 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, obesit y, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and cir cadian rhythm, and cardiovascular disorders.
申请公布号 CA2671838(A1) 申请公布日期 2008.06.26
申请号 CA20072671838 申请日期 2007.12.10
申请人 F. HOFFMANN-LA ROCHE AG 发明人 STALDER, HENRI;NORCROSS, ROGER;GALLEY, GUIDO;GROEBKE ZBINDEN, KATRIN
分类号 C07D233/64;A61K31/415;A61P9/00;A61P25/00 主分类号 C07D233/64
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