New substituted 1-alkyl-3-phenyl-naphthalene derivatives, are melatoninergic receptor ligands useful e.g. for treating sleeping disorders, depression, jet lag or appetite disorders

摘要

1-(Amido-, ureido- or carbamoyl-alkyl)-3-(substituted methyl-phenyl)-naphthalene derivatives (I) are new. Phenyl-naphthalene derivatives of formula (I) and their enantiomers, diastereomers and acid or base addition salts are new. A = -NR2-CO-R1, -NR2-CO-NR1R'1 or -CO-NR1R'1; R1, R'1 = 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, 3-8C cycloalkyl, (3-8C) cycloalkyl-(1-6C) alkyl, aryl, aryl-(1-6C) alkyl, heteroaryl or heteroaryl-(1-6C) alkyl; R2 = H or alkyl; or R1 + R2 = 3-6C linear or branched alkylene; R3 = 1-6C alkoxy; R4 = halo, OH, 1-6C alkoxy, NH2 or mono- or di-(1-6C alkyl)-amino; aryl moieties = phenyl, naphthyl or biphenylyl (all optionally substituted by 1-3 of 1-6C alkyl, 1-6C alkoxy, OH, COOH, CHO, NO2, CN, 1-6C polyhaloalkyl, alkoxycarbonyl or halo); p = 1-3; heteroaryl moieties = mono- or bicyclic aromatic group containing 1-3 of O, S and N as heteroatom(s) (optionally substituted as for aryl). Independent claims are included for: (a) the preparation of (I); and (b) new alkoxycarbonylphenyl-naphthalene derivative intermediates of formula (V) and their enantiomers, diastereomers and acid or base addition salts. R'5 = (1-6C) alkoxycarbonyl.