| 摘要 |
The substituted benzocycloheptapyridine derivatives or pharmaceutically acceptable salts or solvates thereof have the formula I wherein: one of a, b, c or d is N or NR9 with R9 being O, CH3 or -(CH2)nCO2H and n is 1 to 3 and the remaining a, b, c or d are CR1 or CR2 or each of a, b, c, or d are independently CR1 or CR2; each of R1 and R2 are independently H, halo, CF3, COR10, SR10, S(O)tR11, SCN, N(R10)2, NR10R11, NO2, OC(O)R10, CO2R10, OCO2R11, CN, NHC(O)R10, NHSO2R10, CONHR10, CONHCH2CH2OH, NR10COOR11, SR11C(O)OR11, SR11N(R75)2, benzotriazol-1-yloxy, optionally substituted tetrazol-5-ylthio, alkynyl, alkenyl, alkyl or a group of formula II; R3 and R4 are independently H, or one of the substituents of R1 and R2 or together form an optionally substituted 5-7 membered carbocyclic ring fused to the benzene ring (ring III); R5, R6, R7 and R8 are independently H, CF3, COR10, or optionally substituted alkyl or aryl or R5 and R6 and/or R7 and R8 together form =O or =S; R10 is H, aralkyl, aryl or alkyl and 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 is an optional double bond such that when the double bond is present, A and B are independently R10, halo, OR11, OCO2R11 or OC(O)R10 or when no double bond is present between carbon atoms 5 and 6 A and B are independently H2, (OR11)2, H and halo, dihalo, alkyl and H, (alkyl)2, H and OC(O)R10, H and OR10, =O, aryl and H, =NOR10 or -O-(CH2)p-O-; W is CN, COR12, -C(=NR13)-OR14, -C(=NR13)-NR10R16, -C(=CHNO2)-NHR10 or a group of formula III and the rest of the variables are as defined in the specification. A pharmaceutical composition thereof useful in treating tumour cells or inhibiting farnesyl protein transferase.
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