发明名称 IMIDAZOLE DERIVATIVES AND THEIR USE AS FARNESYL PROTEIN TRANSFERASE INHIBITORS
摘要 <p>The present invention relates to a compound of Formula (1) wherein Ar1 represents: (A) or (B) or (C); R1 is hydrogen, C¿1-4?alkyl or C1-4alkanoyl; R?12 and R13¿ are independently hydrogen or C¿1-4?alkyl; Ar?2¿ is phenyl or heteroaryl; p is 0 or 1; Ar3 is of formula (I) wherein W, X, Y and Z are independently CH or N, provided that at least two of W, X, Y and Z are CH and R2 and -(CH¿2)nR?3 are attached to ring carbon atoms; R2 is a group of Formula (II) or R2 represents a lactone of Formula (III) the group of Formula (II) or (III) having L or D configuration at the chiral alpha carbon in the corresponding free amino acid; n is 0, 1 or 2; R3 is phenyl or heteroaryl; provided that: when n is 0, Ar3 is substituted by R2 in the 4-position and -(CH¿2)nR?3 in the 3- or 5-position; and when n is 1 or 2, Ar3 is substituted by R2 in the 3- or 5-position and -(CH¿2)nR?3 in the 4-position; and R5-R9, m and n are as defined in the specification; or a pharmaceutically-acceptable salt, prodrug or solvate thereof. Processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them. A particular use is in cancer therapy.</p>
申请公布号 WO1999020612(A1) 申请公布日期 1999.04.29
申请号 GB1998003115 申请日期 1998.10.19
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