A class of N-substituted (.alpha.-imidazolyl-toluyl)pyrrole compounds
described for use in treatment of circulatory disorders. Compounds of
particular interest are angiotensin II antagonists of the formula
##STR1##
wherein m is one; wherein each of R.sup.0 and R.sup.1 is independently
selected from hydrido, alkyl, hydroxyalkyl, formyl, halo, haloalkyl,
cycloalkylcarbonyl, alkoxy, aroyl, aryloxy, aralkoxy, alkylcarbonyl,
alkoxycarbonyl, cyano, nitro, carboxyl, alkylcarbonyloxy,
alkylcarbonyloxyalkyl, alkoxycarbonylalkyl, aralkoxycarbonylalkyl,
alkylsulfonyl, aralkylsulfonyl, arylsulfonyl; wherein R.sup.2 is selected
from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,
tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl,
cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl;
wherein each of R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8,
R.sup.9 and R.sup.10 is independently selected from hydrido, halo, nitro,
trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl;
with the proviso that at least one of R.sup.5 and R.sup.8 must be selected
from COOH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2
CF.sub.3,
##STR2##
wherein each of R.sup.42 and R.sup.43 is independently selected from
chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and
trifluoromethylsulfonyl; or a tautomer thereof or a
pharmaceutically-aceptable salt thereof. These compounds are particularly
useful in treatment or control of hypertension and congestive heart
failure.
Uma classe de n-substituted (compostos do alpha.-imidazolyl-toluyl)pyrrole descritos para o uso no tratamento de disorders circulatory. Os compostos do interesse particular são antagonistas do angiotensin II do ## do ## STR1 da fórmula wherein m é um; wherein cada um de R.sup.0 e de R.sup.1 é selecionado independentemente do hydrido, alkyl, hydroxyalkyl, formyl, halo, haloalkyl, cycloalkylcarbonyl, alkoxy, aroyl, aryloxy, aralkoxy, alkylcarbonyl, alkoxycarbonyl, cyano, nitro, carboxyl, alkylcarbonyloxy, alkylcarbonyloxyalkyl, alkoxycarbonylalkyl, aralkoxycarbonylalkyl, alkylsulfonyl, aralkylsulfonyl, arylsulfonyl; wherein R.sup.2 é selecionado de methyl, de ethyl, de n-propyl, o isopropil, o n-butyl, o segundo-sec-butyl, o isobutyl, o tert-tert-butyl, n-n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, e hydroxyalkyl; wherein cada um de R.sup.3, de R.sup.4, de R.sup.5, de R.sup.6, de R.sup.7, de R.sup.8, de R.sup.9 e de R.sup.10 é selecionado independentemente do hydrido, do halo, de nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl e methoxycarbonyl; com o proviso que ao menos um de R.sup.5 e de R.sup.8 deve ser selecionado de COOH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, ## do ## STR2 wherein cada um de R.sup.42 e de R.sup.43 é selecionado independentemente de chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl e trifluoromethylsulfonyl; ou um tautomer disso ou um sal pharmaceutically-aceptable disso. Estes compostos são particularmente úteis no tratamento ou no controle da falha do hypertension e de coração congestive.
