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    • 10. 发明授权
    • Vinylthioacetamido oxacephalosporin derivatives
    • 乙烯基硫代乙酰氨基氧杂环孢菌素衍生物
    • US4529721A
    • 1985-07-16
    • US534147
    • 1983-09-21
    • Wataru NagataMitsuru YoshiokaYasuhiro NishitaniTsutomu AokiToshiro KonoikeTadatoshi Kubota
    • Wataru NagataMitsuru YoshiokaYasuhiro NishitaniTsutomu AokiToshiro KonoikeTadatoshi Kubota
    • A01N43/90C07D241/08C07D339/00C07D505/00C07D519/00C07F9/535A01N59/06C07D498/04
    • C07F9/5352C07C309/00C07C323/00C07D241/08C07D339/00C07D505/00Y02P20/55
    • A compound of the formula: ##STR1## wherein u represents hydrogen, carboxamido, N-hydroxycarboxamido, carboxy, azido, an aryl, an acylamino, a protected carboxy or an N-alkoxycarboxamido, or, together with v, can represent --S-- or --CH.sub.2 S--; v represents hydrogen, halogen, cyano or an alkylthio, or, together with u, can represent --S-- or --CH.sub.2 S--, or, together with w, can represent --(CH.sub.2).sub.3 CO--; w represents hydrogen, carboamoyl, cyano, carboxy, an N-alkylcarbamoyl, an alkyl, an aryl, a protected carboxy or a heterocycle, or, together with v, can represents --(CH.sub.2).sub.3 CO--; x represents halogen, trifluoromethyl, an alkylthio or an arylthio; y represents hydrogen, a light metal or a carboxylic acid protecting group; and z represents an acyloxy or a heterocycle-thio, each of the above radicals represented by the symbols u, v, w, x, y and z being optionally substituted by halogen or a carbon-, nitrogen-, oxygen- or sulfur-containing functional group, a process for preparing the compound, a pharmaceutical composition containing the compound, and a therapeutical use of the compound.A compound of the formula: ##STR2## wherein u, v, w and x are as defined above, useful as a starting compound for preparing the compound (I) is also provided.
    • 下式的化合物:其中u表示氢,甲酰氨基,N-羟基羧甲酰氨基,羧基,叠氮基,芳基,酰氨基,被保护的羧基或N-烷氧基羧酰胺基,或与v一起可代表 -S-或-CH2S-; v表示氢,卤素,氰基或烷硫基,或与u一起可以表示-S-或-CH 2 S-,或者与w一起可以表示 - (CH 2)3 CO-; w表示氢,氨甲酰基,氰基,羧基,N-烷基氨基甲酰基,烷基,芳基,保护的羧基或杂环,或与v一起可以表示 - (CH 2)3 CO-; x表示卤素,三氟甲基,烷硫基或芳硫基; y表示氢,轻金属或羧酸保护基; 和z表示酰氧基或杂环硫基,由符号u,v,w,x,y和z表示的上述基团中的每一个任选被卤素或含碳,氮,氧或硫的 官能团,制备该化合物的方法,含该化合物的药物组合物和该化合物的治疗用途。 还提供了下式化合物:其中u,v,w和x如上定义,可用作制备化合物(I)的起始化合物。