2,3-thiomorpholinedione-2-oxime derivatives and pharmaceutical
compositions containing them
    4.
    发明授权
    2,3-thiomorpholinedione-2-oxime derivatives and pharmaceutical compositions containing them 失效
    2,3-苯硫酚-2-氧化物衍生物和含有它们的药物组合物

    公开(公告)号:US5106846A

    公开(公告)日:1992-04-21

    申请号:US477999

    申请日:1990-07-10

    IPC分类号: A61K31/54 A61P1/04 C07D279/12

    CPC分类号: C07D279/12

    摘要: The present invention relates to compounds of the general formula (I), ##STR1## wherein R.sub.1 stands for hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or nitro group;R.sub.2 means a C.sub.1-7 alkyl group optionally substituted by: a hydroxyl or oxo group; or an ester group containing 1 to 4 carbon atoms in the alkoxy moiety; or a C.sub.1-4 alkoxy, cyano, amino, C.sub.1-4 alkylamino, or dialkylamino group; or an acyl group containing 1 to 7 carbon atoms in the alkyl moiety; orR.sub.2 means an aryl-C.sub.1-7 alkyl group optionally bearing the substituents defined above for R.sub.2 in the alkyl chain and optionally substituted by halogen, nitro, C.sub.1-4 alkyl or alkoxy group in the benzene ring; orR.sub.2 represents an allyl, phenylallyl or phenylsulfonyl group, both latter groups optionally being substituted by halogen or a C.sub.1-4 alkyl group in the benzene ring; orR.sub.2 stands for a carbamoyl group substituted by one or two C.sub.1-4 alkyl group(s) or phenyl group on the nitrogen atom.The compounds according to the invention show a cytoprotective and acid secretion-inhibiting action and are effective against gastric and duodenal ulcers.

    摘要翻译: PCT No.PCT / HU88 / 00080 Sec。 371日期1990年7月10日 102(e)日期1990年7月10日PCT提交1988年12月13日PCT公布。 出版物WO89 / 05805 日本时间1989年6月29日。本发明涉及通式(I),其中R1代表氢,卤素,C1-4烷基,C1-4烷氧基或硝基的通式(I)的化合物。 R 2表示任选被羟基或氧代基取代的C 1-7烷基; 或在烷氧基部分含有1至4个碳原子的酯基; 或C 1-4烷氧基,氰基,氨基,C 1-4烷基氨基或二烷基氨基; 或在烷基部分含有1至7个碳原子的酰基; 或R 2表示任选具有上述对烷基链中的R 2定义并且任选被苯环中的卤素,硝基,C 1-4烷基或烷氧基取代的取代基的芳基-C 1-7烷基; 或R 2表示烯丙基,苯基烯丙基或苯基磺酰基,后两个基团任选被苯环中的卤素或C 1-4烷基取代; 或R 2表示被一个或两个C 1-4烷基或氮原子上的苯基取代的氨基甲酰基。 根据本发明的化合物显示出细胞保护和酸分泌抑制作用,并且对胃和十二指肠溃疡有效。