Diuretic and uricosuric imidazo-azole-acryl:amide derivs. - prepd. e.g. by condensation of imidazo-azole-carboxaldehyde or ketone deriv. with acetamide cpd.

摘要

Imidazo-azoleacrylamide derivs. (I), their stereoisomeric enantiomers, diastereomers and Z/E isomers and their acid addn. salts are new. X is N or CH; Y is S, O, NH or N-alkyl; R1, R2 are H, opt. cyclic alkyl, alkenyl or opt. substd. alkynyl (akyl opt. interrupted by O, S, NH or N-(ar)alkyl), phenyl, naphthyl, furyl, thienyl, pyrimidyl, pyrazinyl, (iso)quinolyl or opt. substd. pyridyl ring or -S(O)n-alkyl (where n is 0-2), -NR'R" or -CO-R'"; R', R" are H, (ar)alkyl or aryl (alkyl opt. interrupted by O, S, NH or N-alkyl), or NR'R" is a 5-7 membered ring opt. having one or two of O, S and N; R'" is H, OH, alkyl, alkoxy, alkenyl(oxy) alkynyl, aralkyloxy, aryloxy or NR'R"; R3 is H, CF3 or alkyl; R4 is H, CN, halogen, NO2, S(O)n-alkyl (where n is 0-2), alkoxy, -CO-R'", or opt. cyclic alkyl, alkenyl or alkynyl alkyl opt. substd. by halogen, CN and/or interrupted by O, S, NH, N-(ar)alkyl or N-aryl); R5 is an amino gp. -N(R6)(R7) where (a) R6, R7 are H, aryl or opt. satd. (a)cyclic aliphatic hydrocarbon residue opt. interrupted and/or substd. (the alkyl gps. opt. linked to form a 5- to 7-membered opt. substd. rings; or (b) -N(R6)(R7) is a 3-8 membered opt. satd. ring opt. carries 1-2 further heteroatoms and/or 1-4 substituents from alkyl, halogen, aryl, aralkyl, alkoxycarbonyl hydroxyalkyl, alkoxyalkyl or CF3, or which is opt. condensed with opt. substd. aromatic ring. (I) are diuretics and saluretics and can be used as antihypertensives.