4-guanidinobenzoic acid phenyl ester derivatives, process...

Details 4-guanidinobenzoic acid phenyl ester derivatives, process... 4-guanidinobenzoic acid phenyl ester derivatives, process...

C - Chemistry, Metallurgy

07

C

C07C 279/18 (2006.01) A61K 31/245 (2006.01) A61K 31/255 (2006.01) C07C 309/67 (2006.01)

Patent

CA 2064462

ABSTRACT OF THE DISCLOSURE This invention provides a 4-guanidinobenzoic acid phenyl ester derivative represented by the following general formula (I) or a pharmacologically acceptable acid addition salt thereof, both having excellent proteolytic enzyme inhibition activities, a process for the production of the same, and a proteolytic enzyme inhibitor containing the same as the active ingredient; Image (I) wherein R1 is a hydrogen atom or a halogen atom; R2 is a trifluoromethoxy group, a group represented by OCOR3, a group represented by C(=NOR4)R5 or a styrene sulfonyl group; R3 is a substituted or unsubstituted C3-7 cycloalkyl group; R4 is a hydrogen atom, a C14 alkyl group, a C1-4 alkenyl group or a group represented by CH2COOR6; R5 is a hydrogen atom or a C1-4 alkyl group; and R6 is a hydrogen atom or a C1-4 alkyl group. - 28 -

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