3-Amino-propionoyl 2-ethyl benzofuran(s) and salts - antithrombotics and blood platelet aggregation inhibitors, which inhibit factor XIII and fibrin formation

摘要

3-R1R2N-CH2-CH2-CO 2-ethyl-benzofuran. (RX)n derivs. of formula (I) are new. In (I) NR1R2 is di(1-4C alkyl)amino(where the alkyl gps. are independently chosen), diallylamino, pyrrolidino, piperidino, perhydroazepino, morpholino, dimethylmorpholino, N-(1-4C alkyl)-piperazino, N-(2-hydroxyethyl)- piperazino, N-carbethoxypiperazino, N-benzyl-piperazino, N-methoxy-phenyl-piperazino or N-propynyl-piperazine; RX is an acceptable mineral or organic acid or an alkyl or aryl halide and n is 0, 1 or 2. Antithrombotics which are administered orally or parenterally in daily doses of 50-250 mg. Activity tests show (I) inhibit factor XIII and the formation of fibrin and are blood platelet aggregation inhibitors. In acute toxicity tests in mice, tested cpds. has oral LD50 values of 188-1400 mg/kg and I.V LD505 of 9.5-188.0mg/kg.