Bis(1-substituted biguanide) derivatives.

摘要

A bis( 1-substituted biguanide) derivative of the formula: R<3>R<4>N.C(:NR<5>)NH.C(:NH.C(:NR<9>)NR<1>-X-NR<2>.C(:NR<9>)-NH.C(:NR< 6>)-NR<7>R <8 > V or a tautomeric form thereof, wherein R<1>, R<2> and R<9>, which may be the same or different, are each hydrogen, a 1-16C alkyl radical, a 3-16C cycloalkyl radical, a (3-12C cycloalkyl)-1-(1-4C alkyl) radical, an optionally substituted phenyl or naphthyl radical, an optionally substituted phenyl(1-4C)alkyl or naphthyl(1-4C)alkyl radical or an optionally substituted diphenylmethyl radical, provided that at least one of R<1>, R<2> and R<9> is other than hydrogen; R<3>, R<4>, R<7> and R<8>, which may be the same or different are each hydrogen, or an alkyl, cycloalkyl, (cycloalkyl)alkyl, phenyl, naphthyl, phenylalkyl, naphthylalkyl, or diphenylmethyl radical as defined above, or a 2-16 alkoxyalkyl radical, or R<3>, R<4> and the nitrogen atom to which they are attached, or R<7> and R<8> and the nitrogen atom to which they are attached, which may be the same or different, are each a 1-azetidinyl, 1-pyrrolidinyl, piperidino, hexamethyleneimino, heptamethyleneimino, morpholino or 4-(1-8C alkanoyl)-1-piperazinyl radical, each of which may bear 1-3C alkyl substituents; R<5> and R<6>, which may be the same or different, are each hydrogen or a 1-8C alkyl radical; and X is a 2-16C linking group which is a straight chain alkylene radical, or a straight chain alkylene radical bearing one or more 1-16C alkyl substituents, of which any pair or pairs which are attached to different carbon atoms, may be joined so as to form, together with the intervening carbon atom or atoms of the alkylene radical, a (5-7C)-cycloalkyl radical or radicals; and the acid addition salts thereof, processes for their manufacture, and antibacterial and antifungal compositions and methods using said compounds.