- 专利标题: Triazoles as Farnesyl Transferase Inhibitors
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申请号: US11926858申请日: 2007-10-29
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公开(公告)号: US20080103150A1公开(公告)日: 2008-05-01
- 发明人: Ashis Saha , David End , Bart De Corte , Henry Breslin , Li Liu
- 申请人: Ashis Saha , David End , Bart De Corte , Henry Breslin , Li Liu
- 主分类号: A61K31/4196
- IPC分类号: A61K31/4196 ; A61K31/4439 ; A61K31/4709 ; A61K31/498 ; A61K31/506 ; A61K31/53 ; A61P35/00 ; C07D249/08 ; C07D401/12 ; C07D403/12
摘要:
a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(═O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; =Z1-Z2=Z3- represents a radical of formula ═N—N═CH— (a-1), ═N—CH═N— (a-2), ═CH—N═N— (a-3); X is SO2, (CH2), wherein n is 1 to 4, C(═O), C(═S), or a direct bond; R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio; R3 is aryl, —NR5R6, a substituted or unsubstituted C1-14heterocycle, or C2-4alkenediyl substituted with a substituted or unsubstituted C1-14heterocycle or aryl; R4 is hydrogen, aryl, C3-7cycloalkyl, C1-6alkyl or C1-6alkyl substituted with C3-7cycloalkyl, hydroxycarbonyl, C1-4alkyloxycarbonyl or aryl; R5 and R6 are each independently selected from hydrogen, a substituted or unsubstituted C1-14heterocycle, aryl, C1-12alkyl and C1-12alkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted C1-14heterocycle.
公开/授权文献
- US07592356B2 Triazoles as farnesyl transferase inhibitors 公开/授权日:2009-09-22
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