Pyrimidine derivatives and processes for the preparation thereof
    124.
    发明授权
    Pyrimidine derivatives and processes for the preparation thereof 失效
    嘧啶衍生物及其制备方法

    公开(公告)号:US5750531A

    公开(公告)日:1998-05-12

    申请号:US776220

    申请日:1997-01-23

    CPC分类号: C07D401/04 C07D495/04

    摘要: The present invention relates to novel pyrimidine derivatives of the formulae (I-1) and (I-2) and pharmaceutically acceptable salts thereof which possess an excellent anti-secretory activity, pharmaceutical compositions containing same as an active ingredient, their novel intermediates, and processes for the preparation thereof: ##STR1## wherein: R.sub.4 and R.sub.5, which may be the same or different, are independently hydrogen or a C.sub.1 -C.sub.3 alkyl group, or jointly form a cyclopentyl or cyclohexyl ring; A is a group of formula(II): ##STR2## wherein R.sub.1 and R.sub.2 are, independently of each other, hydrogen or a C.sub.1 -C.sub.3 alkyl group, and R.sub.3 is hydrogen, a C.sub.1 -C.sub.3 alkyl group or a halogen; and B is 1-(substituted)-1,2,3,4-tetrahydroisoquinolin-2-yl of formula (III-1) or 7-(substituted)-4,5,6,7-tetrahydrothieno�2,3-c!pyridin-6-yl of formula (III-2) ##STR3## wherein R.sub.6 is hydrogen or a C.sub.1 -C.sub.3 alkyl group.

    摘要翻译: PCT No.PCT / KR95 / 00105 Sec。 371日期1997年1月23日 102(e)日期1997年1月23日PCT提交1995年8月10日PCT公布。 出版物WO96 / 05177 日期1996年2月22日本发明涉及具有优异抗分泌活性的式(I-1)和(I-2)的新颖的嘧啶衍生物及其药学上可接受的盐,其含有作为活性成分的药物组合物, (I-1)其中:R 4和R 5可以相同或不同,独立地是氢或C 1 -C 3烷基 或共同形成环戊基或环己基环; A是式(II)的基团:其中R 1和R 2彼此独立地为氢或C 1 -C 3烷基,R 3为氢,C 1 -C 3烷基或卤素 ; 和B是式(III-1)的1-(取代的)-1,2,3,4-四氢异喹啉-2-基或7-(取代的)-4,5,6,7-四氢噻吩并〔2,3- c]吡啶-6-基,其中R 6是氢或C 1 -C 3烷基。