| 摘要 |
The benzocycloheptapyridine derivative or a pharmaceutically acceptable salt thereof have the formula I wherein: one of a, b, c and d is N or NR9 and the remaining a, b, c and d are CR1 or CR2 or each of a, s, c and d are independently CR1 or CR2; R9 is O-, CH3 or -(CH2)nCO2H; n is 1 to 3; R1 and R2 are independently H, halo, CF3, OR10, COR10, SR10, -S(O)t R10, SCN, N(R10)2, NR10R11, NO2, OC(O)R10, CO2R10, OCO2R10, CN, NHC(O)R10, NHSO2R10, CONHR10, CONHCH2CH2OH, NR10COOR11, SR11C(O)OR11, SR11N(R75)2, benzotriazol-1-yloxy or optionally substituted tetrazol-5-ylthio, alkyl, alkynyl or alkenyl or a group of formula II; R3 and R4 are independently H, any of the substituents of R1 and R2 or together form an optionally saturated C5-7 fused ring to the benzene ring (ring III); R5 to R8 are independently H, CF3, COR10, or optionally substituted alkyl or aryl or together with R6 forms a =O or =S group and/or R7 and R8 together forms a =O or =S group; R10 is H, alkyl, aryl or aralkyl; R11 is alkyl or aryl; X is N, CH, or C which C may contain an optional double bond (represented by the dotted line) to carbon atom 11; the dotted line between carbon atoms 5 and 6 represent an optional double bond such that when a double bond is present A and B independently are R10, halo, OR11, OCO2R11 or OC(O)R10 and no double bond is present between carbons atoms 5 and 6, A and B are independently H2, (OR11)2, H and halo, dihalo, alkyl and H, H and OC(O)R10, H and OR10, -O, aryl and H, =NR10 or -O-(CH2)p-O- and p is 2 to 4; W is -CH2C(H)(OH)-CH2OH, -CH2C(O)-NR12R13, -CH2-C(O)-E, -CH2-C(O)-O-R14; E is a heterocycloalkyl comprising carbon atoms and optionally another heteroatom selected from NH, NR15, O or S and optionally an aryl ring is fused to E and the rest of the variables are as defined in the specification. A pharmaceutical composition thereof is useful for treating tumour cells, inhabiting the abnormal growth of cells and the inhibition of farnesyl protein tranferase.
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