Antagonists nonpeptide bradykinin basic and pharmaceutical compositions thereof.

2003 
Compounds of general formula (I): ** (See formula) ** in which - R1 is a hydrogen atom or a C1-C4 alkyl; - R2 and R3, which may be identical or different, are an alkyl group C1-C4, or R2 and R3 together with the carbon atom to which they are attached, form a cyclic aliphatic group having 3 to 7 carbon atoms or a heterocyclic aliphatic group having 3 to 7 atoms selected one or two of the same group N, O, S and the others being C atoms; - R4 and R5, which may be identical or different, are a hydrogen atom or a C1-C4 alkyl; - X is selected from the group consisting of halogen, OR1, SR1, CN, C1-C4 alkyl; - B has at least one amino group with basic characteristics or a tetraalkylammonium group and is selected from the group consisting of: ** (See formula) ** - R6 is a hydrogen atom, C1-C6 alkyl; - R7 and R8, which may be identical or different, are a hydrogen atom, a C1-C4 alkyl, or NR7R8 is a group selected from: guanidine i) optionally substituted with 1 or 2 alkyl groups C1-C4 alkyl, cyclohexyl, ii) a nitrogen heterocycle 5-7 membered optionally containing another heteroatom selected from O, N, S; - R9 is selected from the group consisting of hydrogen, - (CH2) q L wherein L is selected from the -OH group, -NR5R6, -NR14R18R19, amidine optionally substituted with 1 or 2 groups C1-C4 guanidine optionally substituted with 1 or 2 groups C1-C4; - R10 is selected from the group consisting of OR6, NR6R12; - R11 is selected from the group consisting of hydrogen, - (CH2) qL, - (CH2) p-NR 4 (CH 2) qL; - R12 is a hydrogen atom, C1-C6 alkyl COR6; - R13 is selected from the group consisting of H, -C1-C6 alkyl - (CH2) pW (CH2) qY1, -Y, -COY, -CH2-Y, wherein - Y is selected from hydrogen, ( CH2) pY1, (CH2) pNR6Y1, (CH2) pN (Y1) 2, NR5R6, NR6 (CH2) pY1 or the following residues: ** (See formula) ** - T is selected from the group -NR7R8, -NR14R18R19, -OR6; Y1 is selected from the group consisting of NR7R8, NR14R18R19 or the following residues: ** (See formula) ** - Z is selected from the group consisting of H, C1-C6 alkyl, OR6, SR6, CF3, OCOR6, COR10 , NHCOR 6, SO2R6, SOR6, CO2R6, N (R6) 2, Cl, Br, NO2, NH2, CN, F, imidazole, phenyl, amidine, guanidine, guanidilmetilo; - R14 is selected from the group consisting of alkyl groups linear or branched C1-C4 alkyl; - R15 is selected from the group consisting of hydrogen or C1-C4 linear or branched; - the -NR16R17 group is an aliphatic nitrogen heterocycle 5-7 membered optionally containing another heteroatom selected from O, S, N; - the -NR14R18R19 group is a quaternary ammonium group in which: R14 is selected from the group consisting of groups C1-C4 linear or branched, R18 and R19, which may be identical or different, alkyl, they are an alkyl group C1-C4 linear or branched, or -NR18R19 is a nitrogen heterocycle 5-7 membered optionally containing another heteroatom selected from O, N, S; - W = CH2, O, S, NR4, N (R4) 2; - p = 1-6. q = 1-6.
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