BENZOYL-GUANIDINE DERIVATIVES SUBSTITUTED WITH AMINO-ACIDS, PROCESS FOR PRODUCING THEM, THEIR USE AS DIAGNOSTICA OR PHARMACEUTICALS, AND PHARMACEUTICAL COMPOSITINS CONTAINING THEM

摘要

Benzoyl guanine derivs. of formula(I) and their salts are new. One of the substits. R1-R3 = Y-Ph-Ä(CH2)k-CHR7-CO-R8Ü; and the others = 1-8C alkyl, 2-8C alkenyl, (CH2)mR14, SO2NHC(=Y')NR18R19, H, halo, CN, Z(CH2)p-CqF2q+1, SOuR22, CONR23R24, COR25, SO2NR26R27, OR35 or NR35R36; Ph = phenylene (opt. mono- or di-substd. by Fl, Cl, CF3, Me, OH, OMe or NR37R38); R37, R38 = H or Me; Y = a bond, O, S or NR9; R9 = H or 1-4C alkyl; R7 = OR10 or NR10R11; R10 = H 1-8C alkyl, 1-8C alkanoyl, 1-8C alkoxycarbonyl, benzyl, or benzyloxycarbonyl; R11 = as R10 or trityl; R8 = OR12 or NR12R13; R12, R13 = H, 1-8C alkyl or benzyl; R14 = 3-8C cycloalkyl or phenyl (both opt. substd. by 1-3 F, Cl, CF3, Me, OMe, or NR15R16); R15, R16 = H or Me; Y' = O, S or NR20; R18, R19 = H, 1-8C alkyl, 3-6C alkenyl or (CH2)tR21; or R18+R19 = A; R21 = 5-7C cycloalkyl or phenyl, (both opt. mono- to tri-substd. by F, Cl, OMe or 1-4C alkyl); R20 = as R18 or amidine; Z = a bond, O, S or NR28; R22 = 1-8C alkyl, 3-6C alkenyl, (CH2)nR29 or CF3; R23, R25, R26 = as R22 or H; R24, R27 = H or 1-4C alkyl; or R23+R24, R26+R27 = A; A = (CH2)4 or (CH2)5 (both opt. having a CH2 replaced by O, S, NH, NMe or N-benzyl; R28 = H or 1-3C alkyl; R29 = 3-7C cycloalkyl or phenyl (both opt. substd. by 1-3 F, Cl, CF3, Me, OMe or NR30R31; R30, R31 = H or 1-4C alkyl; R35, R36 = H or 1-6C alkyl; or R35+R36 = (CH2)y (opt. having a CH2 gp. replaced by O, S, NH, NMe or N-benzyl); R4, R5 = H, 1-4C alkyl, F, Cl, OR32, NR33R34 or CrF2r+1; R32-R34 = H or 1-3C alkyl; k, n, t = 0-4; m, u, p = 0-2; q = 1-6; r = 1-4; and y = 4-7.