RACEMIC OR OPTICALLY ACTIVE 5-(1-HYDROXY-2-PIPERIDINOPROPYL)- -2-(1H,3H)-INDOLONE DERIVATIVE, 5-(1-OXO-2-PIPERIDINOPROPYL)- -2-(1H,3H)-INDOLE AS AN INTERMEDIATE FOR THE PREPARATION THEREOF, PHARMACEUTICAL COMPOSITIONS THEREOF, THEIR USE

摘要

A racemic or optically active 5-(l-hydroxy-2- -piperidinopropyl)-2(1R,3H)-5-(l-hydroxy-2-piperidinopropyl)-2- -(lH,3H)-indolone derivative, defined by the formula (I), (II) and (III); wherein A is -C(=O)-CRR1-(Y)n-, -C(X)=CR-(Y)n-, -SO2-CRR1-(Y)n-, -C(=O)-O- or SO2-O-; n is 0 or 1; m is 0 or an integer from 1 - 6; R, R1 and R2 are each independently hydrogen or (Cl-C3)alkyl; R3 and R4 are taken separately and are each hydrogen, or taken together are ethylene; X is hydrogen or an alkoxy group; Y is CH2 or oxygen; Z and Z1 are each independently hydrogen, (C1-C3)alkyl, alkoxy, fluoro, chloro or bromo; or a pharmaceutically-acceptable acid addition salt thereof that are usable in treating stroke, traumatic brain injury or CNS degenerative diseases; pharmaceutical compositions using these compounds; the use of these compounds for the preparation of medicaments; and the intermediates usable in the preparation of said compounds.