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    • 5. 发明申请
    • ARYL IMIDAZOLES AND THEIR USE AS ANTI-CANCER AGENTS
    • ARYL IMIDAZOLES及其作为抗癌剂的用途
    • WO2005047266A9
    • 2008-04-17
    • PCT/IB2004052433
    • 2004-11-15
    • LORUS THERAPEUTICS INCHUESCA MARIOAL-QAWASMEH RAEDYOUNG AIPING HLEE YOON
    • HUESCA MARIOAL-QAWASMEH RAEDYOUNG AIPING HLEE YOON
    • C07D233/54C07D235/02C07D401/04C07D401/14C07D403/04C07D403/14C07D405/14C07D409/14C07D471/04C07D471/14C07D471/16C07D495/04
    • A61K31/4184A61K31/4178A61K31/4188A61K31/4745C07D233/64C07D235/02C07D401/14C07D403/04C07D403/14C07D409/14C07D495/04
    • Therapeutically effective 2,4,5-trisubstituted imidazole compounds are provided. Also provided are methods -of preparing the compounds and pharmaceutical compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-cancer agents; wherein: R1 is aryl, substituted aryl, heterocycle, substituted heterocycle, heteroaryl, substituted hetéroaryl or amino; R2 and R3 are independently aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, or substituted heteroaryl or R2 and R3 when taken together along with the carbon atoms they are attached to, form aryl or substituted aryl, and R4 is hydrogen, halogen, hydroxyl, thiol, lower alkyl, substituted lower alkyl, lower alkenyl, substituted lower alkenyl, lower alkynyl, substituted lower alkynyl, alkylalkenyl, alkyl alkynyl, alkoxy, alkyithio, aryl, aryloxy, amino, amido, carboxyl, aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, heteroalkyl, cycloalkyl, substituted cycloalkyl, alkylcycloalkyl, alkylcyclobeteroalkyl, nitro, cyano or -S(O)o.2R wherein R is alkyl, substituted alkyl, aryl, substituted aryl, heterocycle, beteroaryl, substituted heterocycle, or substituted heteroaryl.
    • 提供了治疗上有效的2,4,5-三取代的咪唑化合物。 还提供了制备化合物和药物组合物的方法,所述药物组合物包含单独的化合物或与其它药剂组合。 本发明还提供了化合物作为抗癌剂的用途; 其中:R 1是芳基,取代的芳基,杂环,取代的杂环,杂芳基,取代的杂芳基或氨基; R2和R3独立地是芳基,取代的芳基,杂环,杂芳基,取代的杂环或取代的杂芳基,或者当R 2和R 3与它们连接的碳原子一起形成时,R 2和R 3,形成芳基或取代的芳基,且R 4是氢,卤素, 羟基,硫醇,低级烷基,取代的低级烷基,低级烯基,取代的低级烯基,低级炔基,取代的低级炔基,烷基烯基,烷基炔基,烷氧基,烷硫基,芳基,芳氧基,氨基,酰胺基,羧基,芳基,取代的芳基,杂环 杂芳基,取代的杂环,杂烷基,环烷基,取代的环烷基,烷基环烷基,烷基环烯基烷基,硝基,氰基或-S(O)o2R其中R是烷基,取代的烷基,芳基,取代的芳基,杂环, 取代的杂芳基。