NOVEL TRIAZABENZO A NAPHTHO 2,1,8-CDE AZULENE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

摘要

Triazabenzo[a]naphtho[2,1,8-cde]azulene derivatives (I) are new. Triazabenzo[a]naphtho[2,1,8-cde]azulene derivatives of formula (I) are new. R 1H, 1-6C alkyl, 1-6C aminoalkyl or 1-6C hydroxyalkyl; R 2H; R 1+R 2 = a bond; R 3H; R 4H, Me, 3-6C alkyl, 1-6C aminoalkyl, 1-6C hydroxyalkyl, aryl(1-6C)alkyl or heterocycloalkyl(1-6C)alkyl; R 3+R 4a bond; R 5-R 8H, or R 5+R 6 and/or R 7+R 8 = O, S or NH; R 9H, halo, 1-6C alkyl (optionally substituted with Q), 1-6C alkoxy, OH, CN, NO 2, 1-6C polyhaloalkyl or NRR"; R, R" : H, 1-6C alkyl or 2-6C alkenyl; R 10, R 11H, halo, 1-6C alkyl, 1-6C alkoxy, OH, CN, NO 2, 1-6C polyhaloalkyl or NRR"; n : 0-4; m : 0-2; p : 0-3; X : NR 12; R 12H, 1-6C alkyl (optionally substituted with Q), 2-6C alkenyl (optionally substituted with Q), aryl(1-6C)alkyl, 1-6C polyhaloalkyl; aryl : optionally substituted phenyl or naphthyl; Q : halo, OH, 1-6C alkyl, 1-6C alkoxy, NH 2 or mono- or di(1-6C alkyl)amino. An independent claim is also included for a process for preparing (I). [Image] ACTIVITY : Antidepressant; Tranquilizer; Nootropic; Neuroprotective; Antiparkinsonian. MECHANISM OF ACTION : Tyrosine hydroxylase inducer. Administering (5aRS,12aSR,12bSR,12cSR)-7-chloro-2,3,5a,10,12a,12b,12c-hexahydro-1H,4H-3a,9b,11-triazabenzo[a]naphtho[2,1,8-cde]azulene-10,12(5H,11H)-dione to mice by intraperitoneal injection (20 mg/kg) gave a 53% increase in tyrosine hydroxylase level in an anterior section of the locus coeruleus.