TRYPSIN-LIKE SERINE PROTEASE INHIBITORS, AND THEIR PREPARATION AND USE

摘要

Glycylglycine derivatives with a benzylsulfonylamido group at one end of the chain and an amidino-organylamido group at the other end are new, including their racemates, crystal forms, hydrates and salts. Compounds (I) of the formula shown are new, and also their racemates, crystal forms, hydrates and salts with organic or inorganic acids. i : 0 or 1, preferably 0; R4H or OH, preferably H; A : 1,4-phenylene, 1,4-cyclohexylene, pyridine-2,5- or -3,6-diyl, or thiophene-2,5-diyl, preferably phenylene; R1H, COOH, COOR5, aminomethyl, halogen or pseudohalogen, preferably COOH; R5 : methyl or ethyl; R33-aminophenyl, 4-pyridylmethyl, 4-amidinophenylmethyl or 4-aminomethylphenylmethyl; R23-12C alkyl (optionally cycloalkyl-substituted), 6-14C aryl or aralkyl, heteroaryl or as 6-12C heteroarylalkyl with 1-3 hetero-atoms, -CH2-(CH2)p-phenylene-R6, -CH2-(CH2)p-cyclohexyl, -(CH2)p-(1- or 2-naphthyl) or -CH2-(CH2)p-CH2-NHCOO-CH2-phenyl; R6halogen or pseudohalogen; p : 0, 1 or 2 . [Image]