NOVEL PIPERAZINYL ALKYLTHIO PYRIMIDINYL DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING SUCH ACTIVE INGREDIENTS AND PROCESS FOR PRODUCING THE ACTIVE INGREDIENTS

Piperazinyl-alkylthiopyramidines (I), useful for treating central nervous system diseases, are new. Piperazinyl-alkylthiopyramidines (I) and their acid addition salts are new: [Image] R 1hydrogen (H), 1-4C alkyl, 1-4C alkanoyl or di(1-4C alkyl)amino(1-4C alkyl); R 2H or benzyl substituted with 1-3 groups from 1-4C alkyl, 1-4C alkoxy, di(1-4C alkyl)amino, hydroxy or halo; and n : 2-4. Independent claims are made for: (1) pharmaceutical compositions comprising (I) or their acid addition salts and one or more conventional carriers; and (2) a process for making (I). ACTIVITY : Anxiolytic; neuroprotective. SPRD Male rats were subjected to an elevated plus-maze test to compare the anxiolytic effects of oral 6 diamino-2-[2-(1-piperazinyl)ethylthio]-5-(4-fluorobenzyl)-pyrimidine trihydrochloride hydrate (Ia) (a compound of (I)). The minimum effective doses were (Ia) 0.01 mg/kg and diazepam 1 mg/kg. MECHANISM OF ACTION : None stated.