The present invention relates to a 5-amidino-N-(2-aminophenethyl)-2-hydroxybenzenesulfonamide derivative represented by the general formula: ##STR1##

wherein R¹ is a hydrogen atom or a lower alkyl group;

R² represents a hydrogen atom, an optionally substituted lower alkyl group, etc.;

R³ is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, etc.;

Q is a hydrogen atom or an optionally substituted lower alkyl group; and

Z is a hydrogen atom or a hydroxy group, etc.,

or a pharmaceutically acceptable salt thereof, which exerts a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.