| 摘要 |
PCT No. PCT/EP95/05176 Sec. 371 Date Sep. 25, 1996 Sec. 102(e) Date Sep. 25, 1996 PCT Filed Dec. 22, 1995 PCT Pub. No. WO96/22976 PCT Pub. Date Aug. 1, 1996Novel hydrosoluble 3-arylidene-2-oxindole derivatives, having tyrosine kinase inhibitor activity, encompassed by general formula (I), wherein m is zero, 1 or 2; A is a bicyclic ring chosen from tetralin, naphthalene, quinoline and indole; R1 is hydrogen, C1-C6 alkyl or C2-C6 alkanoyl; one of R2 and R3 independently is hydrogen and the other is a substituent selected from: a C1-C6 alkyl group substituted by 1, 2 or 3 hydroxy groups; -SO3R4 in which R4 is hydrogen or C1-C6 alkyl unsubstituted or substituted by 1, 2 or 3 hydroxy groups; -SO2NHR5 in which R5 is as R4 defined above or a -(CH2)n-N(C1-C6 alkyl)2 group in which n is 2 or 3; -COOR6 in which R6 is C1-C6 alkyl unsubstituted or substituted by phenyl or by 1, 2 or 3 hydroxy groups or phenyl; -CONHR7 in which R7 is hydrogen, phenyl or C1-C6 alkyl substituted by 1, 2 or 3 hydroxy groups or by phenyl; -NHSO2R8 in which R8 is C1-C6 alkyl or phenyl unsubstituted or substituted by halogen or by C1-C4 alkyl; -N(R9)2, -NHR9 or -OR9 wherein R9 is C2-C6 alkyl substituted by 1, 2 or 3 hydroxy groups; -NHCOR10, -OOCR10 or -CH2OOCR10 in which R10 is C1-C6 alkyl substituted by 1, 2 or 3 hydroxy groups; -NHCONH2; -NH-C(NH2)=NH; -C(NH2)=NH; -CH2NHC(NH2)=NH; -CH2NH2; -OPO(OH)2; -CH2OPO(OH)2; -PO(OH)2; or (a), (b), (c), or (d) group, wherein p is 1, 2 or 3 and Z is -CH2-, -O- or (e), in which R11 is hydrogen or is as R9 defined above; and the pharmaceutically acceptable salts thereof, are disclosed.
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