NOVEL ANTAGONIST TO SULFONAMIDE FIBRINOGEN ACCEPTOR

Sulphonamido-phenylalkanoic acid derivs. of formula (I), and their salts, are new. In (I), R1 = Het1 opt. substd. NR6R7, R6R7NC- (=NR6)- R6R7NC(=NR6)NH-, R6C(=NR7)NR7- or a gp. (a) or (b); Het1 = a 4-8 member heterocyclic ring contg. 1-4 heteroatoms from N, O, S; R6, R7 = H, 0-10C alkyl or cycloalkyl, both opt. substd. Het2 = 1-4C alkanoylamino, 1-6C alkoxycarbonyl, 0-6C alkylamino; 1-10C alkylsulphonylamino, 4-10C aralkylsulphonylamino, 4-10C aralkyl, 1-10 1-10C alkaryl, 1-10C alkylthio 4-10C aralkylthio, 1-10C alkylsulphinyl, 4-10C aralkylsulphinyl, 1-10C alkylsulphonyl, 4-10C aralkylsulphonyl, aminosulphonyl, 1-10C alkylaminosulphonyl, 4-10C aralkylsulphonylamino, oxo, thio, or 1- or 2-ethenyl or 3- propenyl, all opt. substd.; "alkyl" = from alkane, alkene or alkyne; alkoxy = O-alkyl; aralkyl and alkaryl contain alkyl as defined above and aryl defined below; Het2 = a 5 or 6 membered satd. heterocyclic ring contg. 1-4 heteroatoms from N, O, S; aryl = a mono- or poly-cyclic ring system of 5- and 6-membered aromatic rings contg. 0-4 heteroatoms from N, O, S; R2, R3 = H, aryl, or 0-10C alkyl or cycloalkyl both opt. substd.; R4 = aryl, 1-10C alkyl or cycloalkyl, 4-1UC aralkyl, 1-10C alkoxyalkyl, 1-10C alkaryl, 1-10C alkylthioalkyl, 1-10C alkoxythioalkyl, 1-10C alkylamino, 4-10C aralkylamino, 1-10C alkanoylamino, 4-10C aralkanoylamino, 1-10C alkanoyl, 4-10C aralkanoyl, or 1-10C carboxyalkyl opt. substd. R5 = Het1, COR8, or CSR8; R8 = e.g. OH, 1-10C alkyloxy, 1-10C alkaryloxy, etc. X. Y, Z are opt. substits. and = NR6, O, S, SO, CO, CS CH(OH), SO2, CR6=CR7, CC, Het1, (opt. substd. at any atom with R6), aryl, CONR6, NR6CO, NR6SO2, or SO2NR6; m = 0-10; n = 0-10; and p = 0-3.