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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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. |
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