GB877623A - New phthalazinium compounds and their pseudo bases and the anhydrides thereof - Google Patents

Abstract

The invention comprises: (a) phthalazinium compounds of the general formula <FORM:0877623/IV (b)/1> (wherein A represents the anion of an acid and alk an alkylene radical of 2-10 carbon atoms with at least 2 carbon atoms separating the two phthalazinium rings) and their pseudobases and the anhydro-compounds of the latter; (b) the preparation thereof by the processes of the examples, which may be summarized as follows: (i) reacting a compound X-alk-Y (wherein X represents a halogen atom and Y a halogen atom or a hydroxy group) with phthalazine and reacting the resulting monophthalazinium compound, if necessary after replacement of a hydroxy group by a halogen atom, with a further amount of phthalazine; (ii) reacting o-phthalaldehyde with an alkylene-bis-hydrazine H2NHN-alk-NHNH2 or a salt thereof; (iii) converting a bis-phthalazinium salt into its pseudo-base or the anhydride thereof, or vice versa, by the action of alkalies or acids respectively; (c) the preparation of compounds (a) from the intermediate monophthalazinium compound in accordance with (i) above; (d) bacteriostatic compositions containing compounds (a) (see Group VI). Alkylene-bis-hydrazines of the formula given in (ii) above are prepared by reaction of the corresponding diamines with formaldehyde and hydrocyanic acid, hydrolysis of the products to bis-glycines, nitrosation, ring closure to bis-sydnones and decomposition thereof with acid.ALSO:Pharmaceutical or disinfectant preparations contain bis-phthalazinium salts of the general formula <FORM:0877623/VI/1> (wherein A represents the anion of an acid and alk an alkylene radical of 2-10 carbon atoms with at least 2 carbon atoms separating the two phthalazinium rings) or the corresponding pseudo-bases or the anhydro-compounds of the latter, in admixture or conjunction with a solid or liquid diluent or a vaccine (the formation of anti-bodies by which is intensified by the addition). The pharmaceutical preparations may take the form of tablets, dragees, salves, solutions, suspensions or emulsions, and may be sterilized and/or may contain preserving, stabilizing, melting or emulsifying agents, salts for varying the osmotic pressure, buffers, or other therapeutically valuable substances. Specified salts are halides, sulphates, nitrates, phosphates, acetates, propionates, oxalates, malates, tartrates, citrates, alkylsulphates, alkyl- and aryl-sulphonates, hydroxyethane-sulphonates, benzoates, salicylates, p-amino-salicylates, and naphthalenecarboxylates.