| 摘要 |
An amidine compound or a salt thereof has the formula (I) wherein: R is a group of the formula (2); R1 to R3 are independently hydrogen, hydroxy, alkyl or aryl; R4 is hydrogen, hydroxy, alkyl, alkoxy or halogen; R5 is hydrogen, cyano, carboxy or alkoxycarbonyl; R6 is hydrogen, cycloalkyl, hydroxy, carboxy, alkoxycarbonyl or optionally substituted aralkyloxycarbonyl or nitro, amino, alkylamino, dialkylamino, or optionally substituted aryl or heteroaryl or R6 is an optionally substituted 5- to 7-membered saturated heterocycle having at least one nitrogen or a group of formula (3); X2 is oxygen, sulphur, -SO2-, -SO2NH- or a single bond; X3 is -(CH2)m-; X4 is -CO-, -C(=NH) -, -SO2-, -CONH-, -CSNH-, -SO2NH-, (CH2)rCONH-, (CH2)rCH(OH)-, single bond or pyridylene, pyridylene-NH-C(O)- or quinolinylene; X5 is alkylene, alkenylene or a single bond; R7 is hydrogen, alkyl or -C(=R9)-R10; R8 is hydrogen, alkyl, optionally substituted cycloalkyl, carboxy, alkoxycarbonyl or optionally substituted aryl, heteroaryl or aralkyl or 5 to 7-membered saturated heterocycle having at least one nitrogen, Y1 is oxygen or -NR12-; Y2 is oxygen, sulphur or a single bond; Y3 is a group of formula (4) or a single bond; Y4 is oxygen, -CO-, -CO2-, -SO2-, -CONH-, -CH=CH- or a single bond; Y5 is -(CH2)p-, -(CH2)p'-CHAk-(CH2)p''-, -(CH2)p'-C(Ak)(Ak')-(CH2)p''-, or a phenoxy; ring A is phenylene or optionally substituted piperidylene; R9 to R12, R14, Ak and Ak' are as defined in the specification; p' and p'' are independently 0 to 2; m, n, p and r are independently is 0 to 3; s and t are independently 1 to 3; j is 1 or 2 and k is 0 or 1; provided that when R8 is H, Y4 is a single bond, Y5 is -(CH2)p-,with p being 0 then n is not 0 The compounds are used as blood coagulation inhibitors or as factor Xa inhibitors.
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