N-(4-carbamimidoyl-phenyl)-glycine derivatives

A compound of the formula:

• wherein
• R1 is alkyl;
• R2 is hydrogen, hydroxyalkoxy, alkoxycarbonyloxyalkoxy, or halogenalkoxycarbonyloxyalkoxy;
• R3 is hydrogen, alkoxy, or heterocycloalkyloxy;
• R4 is hydrogen or the residue of an ester group which is cleavable under physiological conditions;
• R5 is hydrogen, hydroxy, alkoxycarbonyl, halogenalkoxycarbonyl, aryloxycarbonyl, arylalkoxycarbonyl, alkoxyalkoxycarbonyl, cycloalkyloxycarbonyl, alkynyloxycarbonyl, 5-methyl-2-oxo-[1,3] dioxol-4-ylmethoxycarbonyl, arylcarbonyloxy, alkylaminocarbonyloxy, arylaminocarbonyloxy, alkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, or arylaminocarbonyl;
• and
• X is F, Cl, or Br;
• or a hydrate or solvates thereof, or a physiologically acceptable salt thereof or a physiologically acceptable ester thereof,
• with the provisio that the compound of formula I is not selected from the group consisting of:
• (RS)-(4-carbamimidoyl-phenylamino)-(3,5-diethoxy-2-fluoro-phenyl)-acetic acid ethyl ester,
• (RS)-(4-carbamimidoyl-phenylamino)-(3,5-diethoxy-2-fluoro-phenyl)-acetic acid,
• (RS)-(4-carbamimidoyl-phenylamino)-(2-fluoro-3,5-dimethoxy-phenyl)-acetic acid, and
• (RS)-(4-carbamimidoyl-phenylamino)-(2-fluoro-3,5-dimethoxy-phenyl)-acetic acid ethyl ester.