EP 2167460 A2 20100331 - NOVEL NAPHTHALENE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
Title (en)
NOVEL NAPHTHALENE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
Title (de)
()
Title (fr)
NOUVEAUX DERIVES NAPHTALENIQUES, LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT
Publication
Application
Priority
- FR 2008000932 W 20080701
- FR 0704747 A 20070702
Abstract (en)
[origin: FR2918372A1] 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.
IPC 8 full level
A61K 31/165 (2006.01); A61P 25/00 (2006.01); C07C 251/48 (2006.01)
CPC (source: EP US)
A61P 1/00 (2017.12 - EP); A61P 3/00 (2017.12 - EP); A61P 3/04 (2017.12 - EP); A61P 3/10 (2017.12 - EP); A61P 9/00 (2017.12 - EP); A61P 15/00 (2017.12 - EP); A61P 15/08 (2017.12 - EP); A61P 15/10 (2017.12 - EP); A61P 25/00 (2017.12 - EP); A61P 25/06 (2017.12 - EP); A61P 25/08 (2017.12 - EP); A61P 25/16 (2017.12 - EP); A61P 25/18 (2017.12 - EP); A61P 25/20 (2017.12 - EP); A61P 25/22 (2017.12 - EP); A61P 25/24 (2017.12 - EP); A61P 25/28 (2017.12 - EP); A61P 35/00 (2017.12 - EP); A61P 35/04 (2017.12 - EP); A61P 37/00 (2017.12 - EP); A61P 37/02 (2017.12 - EP); A61P 43/00 (2017.12 - EP); C07C 251/48 (2013.01 - EP US)
Citation (search report)
See references of WO 2009022063A2
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MT NL NO PL PT RO SE SI SK TR
Designated extension state (EPC)
AL BA MK RS
DOCDB simple family (publication)
FR 2918372 A1 20090109; FR 2918372 B1 20090828; AR 070005 A1 20100310; AU 2008288373 A1 20090219; AU 2008288373 B2 20110804; BR PI0814402 A2 20150804; CA 2691586 A1 20090219; CN 101687777 A 20100331; EA 201000083 A1 20100630; EP 2167460 A2 20100331; JP 2010531859 A 20100930; KR 20100029262 A 20100316; MA 31577 B1 20100802; UA 94828 C2 20110610; US 2010168244 A1 20100701; US 7947852 B2 20110524; WO 2009022063 A2 20090219; WO 2009022063 A3 20090416; ZA 201000024 B 20110428
DOCDB simple family (application)
FR 0704747 A 20070702; AR P080102856 A 20080702; AU 2008288373 A 20080701; BR PI0814402 A 20080701; CA 2691586 A 20080701; CN 200880022874 A 20080701; EA 201000083 A 20080701; EP 08827457 A 20080701; FR 2008000932 W 20080701; JP 2010514037 A 20080701; KR 20107002337 A 20080701; MA 32571 A 20100201; UA A201000635 A 20080701; US 45242908 A 20080701; ZA 201000024 A 20100104