| 摘要 |
Amidino- or guanidino-aryl substituted aminosulfonyl-biphenyl derivatives (I) are new. Amidino- or guanidino-aryl substituted aminosulfonyl-biphenyl derivatives (I) are new. [Image] R1phenyl or naphthyl (both mono-substituted by Q and optionally further substituted by A, OR5, N(R5)2, NO2, CN, halo, NR5COA, NR5COAr', NR5SO2A, NR5SO2Ar', COOR5, CON(R5)2, CON(R5)Ar', COR6, COAr' or S(O)nA); Q : C(=NH)NH2 (optionally mono-substituted by COA, COC(R6)2Ar', COOA, OH or an amino-protecting group), NHC(=NH)NH2, 5-methyl-1,2,4-oxadiazol-3-yl or 5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl; R2N(R5)2, NR5COA, NR5COAr or NR5COOR5; R3, R4H, A, OR5, N(R5)2, NO2, CN, halo, NR5COA, NR5COAr', NR5SO2A, NR5SO2Ar', COOR5, CON(R5)2, CON(R5)Ar', COR6, COAr' or S(O)nA; R5H, A, -CR6R7-Ar' or -CR6R7-Het; R6, R7H, A or (CH2)rAr'; R8H or A; X : O, NR5, CONR5, N(SO2Ar) or N(SO2Het); W : (CR6R6)n, OCR6R7, 1,3- or 1,4-phenylene or 1,3- or 1,4-phenylene-C(R6)2; V : (C(R6)2)m; A : 1-20C alkyl (optionally having 1 or 2 CH2 replaced by O, S or CH=CH and optionally substituted by 1-7 F); Ar : phenyl or naphthyl (both optionally substituted by 1-3 of A, Ar', Het, OR5, N(R5)2, NO2, CN, halo, NR5COA, NR5COAr', NR5SO2A, NR5SO2Ar', COOR5, CON(R5)2, CON(R5)Ar', COR6, COAr' or S(O)nA); Ar' : phenyl or naphthyl (both optionally substituted by 1-3 of A, OR6, N(R6)2, NO2, CN, halo, NR6COA, NR5SO2A, COOR6, CON(R6)2, COR6, SO2NR6 or S(O)nA); Het : N- or C-bonded, mono- or bicyclic, saturated, unsaturated or aromatic heterocyclyl containing 1-4 of N, O and/or S (optionally substituted by 1-3 of A, OR6, N(R6)2, NO2, CN, halo, NR6COA, NR6SO2A, COOR6, CON(R6)2, COR6, SO2NR6, S(O)nA or =O); r : 0-5; m : 0 or 1, and n : 0-2. - ACTIVITY : Anticoagulant; thrombolytic; cardiant; antiarteriosclerotic; antiinflammatory; cerebroprotective; antianginal; vasotropic. - MECHANISM OF ACTION : Coagulation Factor Xa inhibitor; coagulation Factor VIIa inhibitor; serine protease inhibitor. No biological test data is given. |
