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    • 1. 发明授权
    • Azatyrosine analogues
    • 酪氨酸类似物
    • US5869507A
    • 1999-02-09
    • US899859
    • 1997-07-24
    • Hui-Po WangOn LeeJin-Yuh ShewShui-Jane Lee
    • Hui-Po WangOn LeeJin-Yuh ShewShui-Jane Lee
    • A61K31/44A61K31/4418A61P35/00C07D213/65
    • C07D213/65
    • A novel anti-oncogenic azatyrosine analogues of formula (I) ##STR1## wherein R.sub.1 is C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, benzyl, or (C.sub.1-6 alkyl)carbonyl; R.sub.2 is C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, or C.sub.1-6 alkoxyl; and R.sub.3 is CONR.sub.4 R.sub.5, CONHNR.sub.4 R.sub.5, or COOR.sub.6, wherein each R.sub.4 and R.sub.5 independently is a hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, or C.sub.3-6 cycloalkyl, or R.sub.4 and R.sub.5 taken together with the nitrogen attached thereto form a C.sub.3-8 heterocyclic group; R.sub.6 is C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or benzyl. Also disclosed is a method of preparing such a novel anti-oncogenic azatyrosine analogues, as well as a pharmaceutical composition containing a compound of formula (I).
    • 式(I)的新型抗致癌性酪氨酸类似物其中R 1为C 1-6烷基,C 1-6卤代烷基,苄基或(C 1-6烷基)羰基; R2是C1-6烷基,C1-6卤代烷基或C1-6烷氧基; 并且R 3是CONR 4 R 5,CONHR 4 R 5或COOR 6,其中每个R 4和R 5独立地是氢,C 1-6烷基,C 2-6烯基,C 2-6炔基或C 3-6环烷基,或者R 4和R 5与氮一起 附着其形成C 3-8杂环基; R 6是C 1-6烷基,C 1-6卤代烷基,C 2-6烯基,C 2-6炔基,C 3-6环烷基或苄基。 还公开了制备这种新型抗致癌性酪氨酸类似物的方法,以及含有式(I)化合物的药物组合物。