PYRIDINE DERIVATIVES OF ALKYLOXINDOLES AS 5HT7 RECEPTOR ACTIVE AGENTS

3,3-Disubstituted indol-2-one compounds (I) and their acid addition salts are new. 3,3-Disubstituted indol-2-one compounds of formula (I) and their acid addition salts are new. R 1>H, halo or 1-7C alkyl; R 2>, R 3>H or 1-7C alkyl; either R 4>H; and R 5>benzene compounds of formula (a)...

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Hauptverfasser: KAPILLERNE DEZSOEFI RITA, LEVELEKI CSILLA, HARSING LASZLO GABOR DR, GACSALYI ISTVAN, LEVAY GYOERGY DR, VOLK BALAZS, SZENASI GABOR DR, SIMIG GYULA DR, BARKOCZY JOZSEF DR, SZIRAY NORA, MEZEI TIBOR DR, MORICZ KRISZTINA, PALLAGI KATALIN, GIGLER GABOR, EGYED ANDRAS DR
Format: Patent
Sprache:eng
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Zusammenfassung:3,3-Disubstituted indol-2-one compounds (I) and their acid addition salts are new. 3,3-Disubstituted indol-2-one compounds of formula (I) and their acid addition salts are new. R 1>H, halo or 1-7C alkyl; R 2>, R 3>H or 1-7C alkyl; either R 4>H; and R 5>benzene compounds of formula (a); or CR 4>R 5>phenyl or 5-6 membered heterocyclic ring containing S (optionally substituted with halo); either R 6>-R 8>H, halo, CF 3 or 1-7C alkyl; or R 6>R 7>ethylene dioxy; and m : 1-4. An independent claim is also included for the preparation of (I). [Image] ACTIVITY : CNS-Gen.; Antidepressant; Tranquilizer; Neuroleptic; Antimanic; Nootropic; Cerebroprotective; Vasotropic; Neuroprotective. MECHANISM OF ACTION : 5-Hydroxy tryptamine (5-HT)-7 receptor inhibitor. (I) were tested for 5-HT7 receptor inhibitory activity in Wistard rat. The median inhibitory concentration of 3-{4-[4-(3-trifluoromethyl-phenyl)-1,2,3,6-tetrahydropyridin-1-yl]-butyl}-1,3-dihydro-2H-indol-2-one (Ia) was less than 100 nM.