Substituted biphenyl derivatives

Details Substituted biphenyl derivatives Substituted biphenyl derivatives

C - Chemistry, Metallurgy

07

C

C07C 317/40 (2006.01) A61K 31/155 (2006.01) A61P 7/02 (2006.01) C07C 251/24 (2006.01) C07C 257/18 (2006.01)

Patent

CA 2403500

The invention relates to compounds of general formula (I) where R1 = - C(=NH)NH2 optionally substituted with COA, -CO-, [C(R7)2]n-Ar', -COOA, OR7, OCOA, OCO-[C(R7)2]n-Ar', -OH or by a conventional amino protecting group, - NHC(=NH)-NH2, -CON=C(NH2)2, (II), or (III), substituted phenyl or naphthyl, optionally substituted with A, -OR6, -N(R6)2, -NO2, -CAN, -Hal, -NR5COA, - NR5COAr', -NR5SO2A, - NR5SO2Ar', -COOR5, -CON(R5)2, -COR7, -COAr' or S(O)nA; R2 = -S(O)nA, -CF3, -COOR7, -OA and R3, R4, R5, R6, R7 and X have the meanings given in the text. Said compounds have factor Xa and VIIa inhibitory effects and can thus be used for the treatment and prevention of thromboembolitic diseases such as thromboses, myocardial infarct, arterioscleroses, inflammations, apoplexy, angina pectoris, restenosis after angioplasty and intermittent claudication.

L'invention concerne des composés de formule (I) dans laquelle R?1¿, R?2¿, R?3¿, R?4¿ et X ont la signification indiquée dans la description. Ces composés constituent des inhibiteurs des facteurs Xa et VIIa, et peuvent être utilisés par conséquent pour le traitement et la prévention de maladies thrombo-emboliques telles que la thrombose, l'infarctus du myocarde, l'artériosclérose, les infections, l'apoplexie, l'angine de poitrine, la resténose après angioplastie et la claudication intermittente.

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