| abstract |
The subject of the invention is compounds of formula: (CF DRAWING IN BOPI) in which: - R1 and R2 each independently represent H or (C1 -C6) alkyl, (C1 -C4) alkoxy, amino, aminomethyl, carboxy, alkoxycarbonyl , cyano, tetrazolyl, methylsulfonylamino, trifluoromethylsulfonylamino, trifluoromethylsulfonylaminomethyl, N-cyanoacetamide, N-hydroxy-acetamide, N - ((4-carboxy) thiazol-1,3-yl-2) acetamide, ureido, cyano-2-guanidin, 2-cyano guanidinomethyl, imidazol-1-yl-carbonyl, 3-cyano-2-methyl isothioureidomethyl, provided that at least one of the substituents R1 or R2 is other than hydrogen; - R3 represents H, (C1 -C6) alkyl, (C2 -C6) alkenyl, (C3 -C7) cycloalkyl, phenyl, phenylalkyl, phenylalkenyl; - R4 and R5 represent alkyl C1 -C6, (C3 -C7) cycloalkyl, phenyl, phenylalkyl; - or R4 and R5 linked together represent either (CH2) n, or (CH2) p Y (CH2) q, in which Y is 0 or S, or C substituted by (C1 -C4) alkyl, phenyl or phenylalkyl, or N-R6 where R6 represents H, (C1 -C4) alkyl, phenylalkyl, alkylcarbonyl, halo-alkylcarbonyl, polyhaloalkylcarbonyl, benzoyl, alpha-aminoacyl or an N-protecting group, or R4 and R5 together with the carbon atom to which they are linked to constitute an indane or an adamantane; - p + q = m; - n is an integer between 2 and 11; - m is an integer between 2 and 5; - X represents an N-R7 group or a C (CN) R8 group; - R7 represents a C1 -C4 alkyl or a cyano group; - R8 represents H, cyano, tetrazolyl, tert-butyltetrazolyl, phenylsulfonyl or a COR9 group; - R9 represents thienyl, furyl, alkoxy (C1 -C4), phenoxy, benzyloxy or phenyl; and its possible salts. Application: angiotensin II antagonists. |