发明名称 Imidazole derivatives and their use as farnesyl protein transferase inhibitors
摘要 The present invention relates to a compound of Formula (1) wherein Ar1 represent (A) or (B) or (C); R1 is hydrogen, C1-4alkyl or C1-4alkanoyl; R12 and R13 are independently hydrogen or C1-4alkyl; Ar2 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 -(CH2)nR3 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 -(CH2)nR3 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 -(CH2)nR3 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.
申请公布号 US6410539(B1) 申请公布日期 2002.06.25
申请号 US20000509476 申请日期 2000.03.24
申请人 ASTRAZENCA UK LIMITED;ZENECA PHARMA SA 发明人 ARNOULD JEAN-CLAUDE
分类号 A61K31/4174;A61P35/00;A61P43/00;C07D233/54;C07D233/61;C07D233/64;C07D401/12;C07D521/00;(IPC1-7):A61K31/50;C07D401/00;C07D421/00;C07D277/20 主分类号 A61K31/4174
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