Ahmed Sabaouni,Daniel-Henri Caignard,Mark Millan,Michaël Spedding,Mohamed Ettaoussi,Pascal Berthelot,Philippe Delagrange,Said Yous
申请号：
BRPI0814407
公开号：
BRPI0814407A2
申请日:
2008.07.01
申请国别(地区):
BR
年份:
2019
代理人:
摘要：
Substituted naphthalene derivatives (I) and their enantiomers, diastereoisomers, or acid or base addition salts, are new. Substituted naphthalene derivatives of formula (I) and their enantiomers, diastereoisomers, or acid or base addition salts, are new. R 11-6C (halo)alkyl, 1-6C alkenyl, polyhalo1-6C alkyl, 3-8C cycloalkyl, cyclo(3-8C)alkyl(1-6C)alkyl, (hetero)aryl or 1-6C (hetero)arylalkyl, where aryl is phenyl, naphthyl or biphenyl, heteroaryl is mono or bicyclic aromatic group containing 1-3 heteroatom of O, S or N, and (hetero)aryl is optionally substituted by 1-3 group comprising 1-6C alkyl, 1-6C alkoxy, OH, carboxy, formyl, nitro, CN, halo(1-6C)alkyl, polyhalo1-6C alkyl, alkyloxycarbonyl or halo； and R 2F or 1-6C alkyl (substituted by one or more F), preferably F or fluoromethyl. Independent claims are included for the preparation of (I). [Image] ACTIVITY : Hypnotic； Tranquilizer； Antidepressant； Cardiovascular-Gen； Gastrointestinal-Gen； CNS-Gen； Muscular-Gen； Neuroleptic； Anorectic； Anticonvulsant； Antidiabetic； Antiparkinsonian； Nootropic； Antimigraine； Neuroprotective； Endocrine-Gen； Cytostatic； Dermatological； Vasotropic； Immunomodulator； Contraceptive； Analgesic. MECHANISM OF ACTION : Melatonin 1 receptor binder； Melatonin 2 receptor binder； 5-Hydroxytryptamine 2c receptor binder. The ability of (I) to bind melatonin 1 receptor was tested using 2-[ 125>；I]-iodomelatonin radioligand. The result showed that inhibitory constant of N-[3-fluoro-2-(7-methoxy-1-naphthyl) propyl]acetamide was 0.1 nM.
