发明授权
US4024270A Antimycotic compositions containing an imidazolylacetic acid amide or salt thereof as the active agent and the use thereof in the treatment of mycoses 失效
含有咪唑基乙酰胺或其盐作为活性剂的抗真菌组合物及其在治疗真菌病中的应用

Antimycotic compositions containing an imidazolylacetic acid amide or
salt thereof as the active agent and the use thereof in the treatment
of mycoses
摘要:
Pharmaceutical compositions useful for treating mycotic infections in humans and animals are produced which comprise an antimycotically effective amount of an imidazolylacetic acid amide of the formula: ##STR1## or pharmaceutically acceptable nontoxic salts thereof WHEREINEitherR.sup.1 is phenyl or cycloalkyl, unsubstituted or substituted by one or more substituents; andR.sup.2 is hydrogen;OrR.sup.1 and R.sup.2, together with the nitrogen atom to which they are attached, form a saturated 5 to 7-membered heterocyclic ring which ring may contain an --SO.sub.2 -- or --NY-- moiety wherein Y is alkoxycarbonyl, dialkylaminocarbonyl, or phenyl or diphenylmethyl, unsubstituted or substituted by one or more substituents and wherein said 5 to 7-membered heterocyclic ring itself is otherwise unsubstituted or substituted by one or more substituents; andX.sup.1, x.sup.2, x.sup.3 and X.sup.4 are the same or different and are each hydrogen or halogen,Are produced byA. reacting a halodiphenylacetic acid amide of the formula: ##STR2## wherein R.sup.1, R.sup.2, X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are as above defined, and Hal is hydrogen,With imidazole; orB. reacting a halodiphenylacetic acid halide of the formula: ##STR3## WHEREIN X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are as above defined and Hal is hydrogenWith imidazole to produce an imidazolide of the formula: ##STR4## wherein X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are as above definedwhich in turn is transaminated by reaction with an amine of the formula:NHR.sup.1 R.sup.2whereinR.sup.1 and R.sup.2 are as above defined.
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