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    • 100. 发明授权
    • Pyridonecarboxylic acid derivatives and intermediates for the synthesis
thereof
    • 吡啶酮羧酸衍生物及其合成中间体
    • US6017911A
    • 2000-01-25
    • US125765
    • 1998-08-25
    • Nobuhiko HoriuchiTakenori YonezawaKatsumi ChibaHiroaki Yoshida
    • Nobuhiko HoriuchiTakenori YonezawaKatsumi ChibaHiroaki Yoshida
    • C07D491/04C07D491/048C07D491/052C07D519/00A61K31/47A61K31/535C07D215/56C07D471/04
    • C07D491/04
    • This invention relates to pyridonecarboxylic acid derivatives of the following general formula, esters thereof and salts thereof, as well as pharmaceutical preparations containing them. ##STR1## wherein: R is cycloalkyl which may be substituted by halogen, or the like;X is hydrogen, lower alkyl, amino or the like;Y is hydrogen or halogen;A is nitrogen or a group of the formula C--Z in which Z is lower alkoxy that may be substituted by halogen, or the like;R.sub.1 and R.sub.2 may be the same or different and are each hydrogen or the like;R.sub.3 is hydrogen or lower alkyl;R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 may be the same or different and are each hydrogen, halogen or lower alkyl;m is 0 or 1; andn and p may be the same or different and are each 0 or 1.This invention also relates to bicyclic amine compounds useful as direct intermediates for the synthesis of the above-described pyridonecarboxylic acid derivatives.
    • PCT No.PCT / JP97 / 00530 Sec。 371日期:1998年8月25日 102(e)日期1998年8月25日PCT提交1997年2月25日PCT公布。 第WO97 / 31919号公报 1997年9月4日,本发明涉及以下通式的吡啶酮羧酸衍生物,其酯类及其盐,以及含有它们的药物制剂。 其中:R为可被卤素取代的环烷基等; X是氢,低级烷基,氨基等; Y是氢或卤素; A是氮或式C-Z的基团,其中Z是可被卤素取代的低级烷氧基等; R1和R2可以相同或不同,各自为氢等; R3是氢或低级烷基; R 4,R 5,R 6,R 7,R 8和R 9可以相同或不同,各自为氢,卤素或低级烷基; m为0或1; n和p可以相同或不同,各自为0或1.本发明还涉及可用作合成上述吡啶酮羧酸衍生物的直接中间体的双环胺化合物。