New substituted bi:phenylyl derivs. are angiotensin II antagonsists

摘要

Substd. biphenyl derivs. of formula (I), and their salts are new. n = 0, 1, 2 or 3 and x is a bond; or n = 1, 2 or 3, and x is O, S or NR; R = 1-3C alkyl; A = 1,4-butadienylene which is substd. by R1 and R2 and in which an unsubstd. CH gp. is opt. N; R1 = H, F, Cl, Br, CF3, or R; R2 = (a) H, R, 2-5C alkoxy, (b) benzimidazol-2-yl imidazo (-2,1-6) thiazol-6-yl, imidazo (-1,2-a, 4,5-6 or 4,5-c) (c) pyridinyl or pyrrolidinyl or piperidyl (d) imidazol-4-yl (e) a gp. which may be converted to carboxy in vivo; (f) a carbonyl gp. or (g) R5NR4CONR3; Ar = phenyl (opt. mono- or disubstd. by F, Cl, CF3, Me or MeO); R3 = H, 1-5C alkyl, cyclohexyl or benzyl; R4 = H, 1-6C alkyl, allyl, cyclohexyl, benzyl or phenyl; R5 = H or R; or NR4R5 = a 4-6C unbranched cycloalkyleneimino gp. or a morpholino gp. or R3 + R4 = 2-3C alkylene; Ra = 1-5C alkyl, 3-5C cycloalkyl, RO, R5 or RNH R6 = (a) a gp. convertible to carboxy in vivo; (b) COOH, CN, hydroxysulphonyl, 1H-tetrazolyl, 1-triphenylmethyl-tetrazolyl or 2-triphenylmethyl-tetrazolyl; (c) 1-4C alkylcarbonylaminosulphonyl, benzoylaminosulphonyl 1-4C alkylsulponylaminocarbonyl, F3CSO2NHCO or phenylsulphonylaminocarbonyl; or (d) if X is a bond and n is 1, R6 may also be bis(hydroxycarbonyl)methyl or bis (1-4C alkoxycarbonyl)methyl; Rc = H, F, Cl, BR, 1-4C alkyl, RO, NO2, NH2, RNH or (R)2N; Phenyl gps. are opt. mono- or disubstd. by Cl, Br, Me or MeO.