GB994889A - Piperazine derivatives - Google Patents

Abstract

The invention comprises compounds of the formula <FORM:0994889/C2/1> and acid addition salts thereof, wherein R and R1 are hydrogen, halogen, lower alkyl or lower alkoxy, R2 is hydrogen lower alkyl, phenyl-lower alkyl or trityl, R3 and R4 are hydrogen or lower alkyl and m is 2 or 3 (the word "lower" indicating a group of 1-8 carbon atoms), and their preparation by reacting the corresponding benzophenone (optionally bearing substituents R and R1) with a reactive metal derivative of the appropriate propargyl piperazine or homopiperazine. Compounds wherein R2 is hydrogen may be prepared by reacting a propargyl piperazine or homopiperazine having a blocking group on the N4-nitrogen atom, such as trityl, with the benzophenone reactant and subsequently removing the blocking group, e.g. in the case of a trityl group by reaction with 50% acetic acid. Pharmaceutical preparations having analgesic, muscle relaxant, anticholinergic, anti-spasmodic and antisecretory activity comprise unit dosages containing 10-30 mg. of the above compounds, including salt such as the hydrochloride, sulphate, formate, citrate, maleate, succinate, tartrate, benzoate, furmarate, salicylate or acetylsalicylate and a carrier. The preparations suitably take the form of solutions, powders, tablets or capsules. The invention includes the process of treating animals with these preparations.