Pharmaceutical compositions
AssigneeNational Research Development Corporation
InventorsAndrew M. Creighton, William A. Jeffery
Life of this patent
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AssigneeNational Research Development Corporation
InventorsAndrew M. Creighton, William A. Jeffery
Estimating the term…
Compounds of the formula (II) ##STR1## wherein R.sub.1 and R.sub.2 are each separately selected from hydrogen, alkyl, alkenyl and alkynyl groups having up to a maximum of four carbon atoms and being unsubstituted, and alkyl, alkenyl and alkynyl groups having up to a maximum of three carbon atoms and being substituted by one, or in the case of fluoro by one or more, substitutents but with the proviso that when R.sub.1 is hydrogen then R.sub.2 is hydrogen or methyl, or R.sub.1 and R.sub.2 together constitute an ethylene bridging group, and R.sub.3 is a group which under physiological conditions undergoes elimination with the formation of a 3,5-dioxopiperazinyl ring, with the further proviso that the compound is in the meso or erythro configuration when each of R.sub.1 and R.sub.2 is the same or different unsubstituted or substituted alkyl, alkenyl or alkynyl group, and salts thereof with a physiologically acceptable inorganic or organic acid, are of value as prodrugs, particularly in the therapy of cancer and psoriasis.
A method for the treatment of a patient receiving an anthracycline drug in order to provide protection against any cardiotoxic effect of that drug, which method comprises administering to said patient a therapeutically effective amount of a compound of formula (II) ##STR8## wherein R.sub.1 and R.sub.2 are each separately selected from hydrogen, alkyl, alkenyl and alkynyl groups having up to a maximum of four carbon atoms and being unsubstituted, and alkyl, alkenyl and alkynyl groups having up to a maximum of three carbon atoms and being substituted by one phenyl, carboxy, alkoxycarbonyl, halogeno (other than fluoro), hydroxy or alkoxy group, or by one or more fluoro groups, but with the proviso that when R.sub.1 is hydrogen then R.sub.2 is hydrogen or methyl or R.sub.1 and R.sub.2 together constitute an ethylene bridging group, and R.sub.3 excludes any group in which the bonding carbon atom does not carry at least one hydrogen atom, R.sub.3 being selected from (a) alkyl, alkenyl and alkynyl groups having up to a maximum of ten carbon atoms and being either unsubstituted or substituted by one or more alkoxy, carboxy, halogeno, hydroxy, alkoxycarbonyl, benzyloxycarbonyl, cyano, amino, alkylamino, dialkylamino or oxo groups and (b) aralkyl, aralkenyl, and aralkynyl groups in which the aromatic part of the group may optionally be substituted by one or two substituents selected from halogen, lower alkyl, lower alkoxy, amino and nitro groups or by one methylenedioxy group, and in which the aliphatic part of the group has up to a maximum of ten carbon atoms and may optionally be substituted by one substituent selected from alkoxycarbonyl and cyano groups, with the further proviso that the compound is in the meso or erythro configuration when each R.sub.1 and R.sub.2 is the same or different unsubstituted or substituted alkyl, alkenyl or alkynyl group, and salts thereof with a physiologically acceptable inorganic or organic acid.
A method according to claim 1, in which the aralkyl group is a phenylalkyl group which may optionally be substituted as described in claim 51.
Dependencies are inferred from the claim text.