EP 2167457 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)
NEUARTIGE NAPHTHALENDERIVATE, HERSTELLUNGSVERFAHREN DAFÜR UND PHARMAZEUTISCHE ZUSAMMENSETZUNGEN DAMIT
Title (fr)
NOUVEAUX DERIVES NAPHTALENIQUES, LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT
Publication
Application
Priority
- FR 2008000933 W 20080701
- FR 0704748 A 20070702
Abstract (en)
[origin: FR2918370A1] 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.
IPC 8 full level
C07C 233/18 (2006.01); A61K 31/165 (2006.01); A61P 25/00 (2006.01); C07C 233/60 (2006.01)
CPC (source: EP KR US)
A61K 31/165 (2013.01 - KR); A61P 1/00 (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 15/10 (2017.12 - EP); A61P 15/18 (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 37/02 (2017.12 - EP); A61P 43/00 (2017.12 - EP); C07C 233/18 (2013.01 - EP KR US); C07C 233/60 (2013.01 - EP KR US); C07C 2601/02 (2017.04 - EP US); C07C 2601/04 (2017.04 - EP KR US)
Citation (search report)
See references of WO 2009022064A2
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 2918370 A1 20090109; FR 2918370 B1 20090828; AR 070006 A1 20100310; AU 2008288374 A1 20090219; AU 2008288374 B2 20110804; BR PI0814407 A2 20190924; CA 2691593 A1 20090219; CN 101687772 A 20100331; EA 201000084 A1 20100630; EP 2167457 A2 20100331; JP 2010531860 A 20100930; KR 20100029263 A 20100316; MA 31578 B1 20100802; MX 2010000001 A 20100421; UA 94827 C2 20110610; US 2010137446 A1 20100603; WO 2009022064 A2 20090219; WO 2009022064 A3 20090416; ZA 201000025 B 20110428
DOCDB simple family (application)
FR 0704748 A 20070702; AR P080102857 A 20080702; AU 2008288374 A 20080701; BR PI0814407 A 20080701; CA 2691593 A 20080701; CN 200880022964 A 20080701; EA 201000084 A 20080701; EP 08827416 A 20080701; FR 2008000933 W 20080701; JP 2010514038 A 20080701; KR 20107002340 A 20080701; MA 32572 A 20100201; MX 2010000001 A 20080701; UA A201000634 A 20080701; US 45245608 A 20080701; ZA 201000025 A 20100104