To obtain the subject new compound clinically applicable and useful as a selective activated blood coagulation factor X (hereinafter abbreviated to Fxa) inhibitor.
This biphenylamidine derivative is represented by formula I [A1 is amidino; R1 is H, F, Cl, Br, hydroxyl group, amino, nitro, a 1-10C alkyl or the like; R2 is F, Cl, Br, hydroxyl group, amino, a 1-10C alkoxy or the like; R3 is H, F, Cl, Br, hydroxyl group, amino, nitro, a 1-10C alkyl or the like; X1 is NH-CO-NH or the like; Y1 is phenyl, naphthyl or the like; (m) is 1-3; (n) is 0-3], e.g. methyl 3-(3-amidinophenyl)-5-benzoylaminomethyl-benzoate. In the compound represented by formula I, a compound in which X1 is amide bond can be obtained by synthesizing a nitrile derivative which is a precursor using, e.g. a compound represented by formula II (R5 is H, a 1-10C alkyl or an aryl; R11 is F, Cl, Br or the like) and then carrying out the amidination reaction of the resultant nitrile derivative.
TAKANO YASUNOBU
SUGIURA SATOSHI
NAKADA TOMOHISA
HARA TAKAYUKI
NAKAI YASUHARU
TAKARADA REIKO
