SAID YOUS,MOHAMED ETTAOUSSI,AHMED SABAOUNI,PASCAL BERTHELOT,MICHAËL SPEDDING,PHILIPPE DELAGRANGE,DANIEL-HENRI CAIGNARD,MARK MILLAN
申请号：
BRPI0814402
公开号：
BRPI0814402A2
申请日:
2008.07.01
申请国别(地区):
BR
年份:
2015
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, polyhalo(1-6C)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 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, 1-6C polyhaloalkyl, alkyloxycarbonyl or halo； X : oxime NOR 2, which can be in Z or E configuration； and R 2H or 1-6C alkyl, preferably CH 3. An independent claim is 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 2 receptor was tested using 2-[ 125>；I]-iodomelatonin radioligand. The result showed that inhibitory constant of N-[(2E)-2-(hydroxyimino)-2-(7-methoxy-1-naphthyl)ethyl]acetamide was 0.8 nM.
