PIPERAZINE DERIVATIVES OF DIALKYL-OXINDOLES

3,3-Dialkyl indol-2-one derivatives (I) and their acid addition salts are new. 3,3-Dialkyl indol-2-one derivatives of formula (I) and their acid addition salts are new. R 1>H, halo, 1-7C alkyl or sulfonamido; R 2>H or halo; R 3>1-7C alkyl (optionally substituted with aryl (optionally substituted with 1 or 2 halo substituents)) or H; R 4>1-7C alkyl; R 5>benzene derivative of formulae (IIa) or phenyl (optionally substituted by R 6>, R 7>, R 8>); Q, W 1>N or CH; either R 6>, R 7>H, halo, trifluoromethyl, 1-7C alkyl or alkoxy; or R 6>+R 7>ethylenedioxy; R 8>H, halo, trifluoromethyl, 1-7C alkyl or alkoxy; m : 0-2; a : single, double or triple bond; and n : 0-2. Independent claims are also included for: (1) the preparation of (I); (2) indolone derivative of formula (III); and (3) a process for the preparation of (III) comprises reacting an alkane compound (V) of formula (L-(CH 2) m-CH 2-a-CH 2-(CH 2) m-L a>) with substituted indolone derivative of formula (VI) in the presence of a strong base. L : halogen, hydroxy, arylsulfonyloxy or alkylsulfonyloxy group; and L a>leaving group. [Image] [Image] ACTIVITY : CNS-Gen.; Antidepressant; Neuroleptic; Tranquilizer; Antimanic; Nootropic; Cerebroprotective; Vasotropic; Neuroprotective; Gastrointestinal-Gen.; Cardiovascular-Gen.; Nephrotropic; Auditory. MECHANISM OF ACTION : 5-Hydroxy tryptamine receptor (5HT 2C) binder; Alpha receptor binder. The ability of (I) to bind 5HT 2C receptor was assessed using male wistar rats. The results showed that 5-chloro-3- {3-[4-(3-chlorophenyl)-piperazin-1-yl]-propyl}-3-ethyl-1,3-dihydro-2H-indol-2-one (Ia) exhibited a median inhibitory concentration value of less than 50 nmole.