Sulfur-containing heterocyclic bradykinin antagonists, process for their preparation, and their use.

摘要

Sulphur-containing bradykinin antagonist compounds of formula (I) and their salts are claimed: one of X1-X3 = COR<2>, and the other X1-X4 = N, CR<1>; R<1>,R<3> = H, halo, 1-6C alkyl, OR<6>, SR<6>, NHR<6>, 6-12C aryl, (6-12C aryl)(1-3C alkyl), C(O)OR<6>, C(O)H, 2-5C alkenyl, NO2, SO3R<7>, CN, C(O)NHR<8>, where alkyl, aryl, alkenyl may be substituted by C(O)(O)o(1-5C alkyl), OR<6>, SR<7>, NO2, CN, NHR<8>, halo; R<2> = (II); R<4>,R<5> = e.g. H; R<6>-R<8> = H, 1-5C alkyl, 3-5C alkenyl, etc.; A = amino acid e.g. methionine, alanine, phenylalanine, etc.; R<9> = H, C(O)(O)o(1-5C alkyl), C(O)(O)o(11-3C alkyl)(6-10C aryl); R<10> = e.g. C(O)DE; D = 2-5C alkendiyl, 1-8C alkandiyl, (CH2)nYo(CH2)m, etc., where any of the groups are optionally substituted by e.g. OR<6>; E = H, 6-10C aryl, 1-9C heteroaryl, etc.;Y = O, S, NR<8>; n,m = 0-6; o = 0 or 1.