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    • 2. 发明授权
    • Antibacterial preparation or bactericide comprising 2-aminothiazole
derivative and/or salt thereof
    • 包含2-氨基噻唑衍生物和/或其盐的抗菌制剂或杀菌剂
    • US5856347A
    • 1999-01-05
    • US836924
    • 1997-05-23
    • Terushi HashiguchiToshio YoshidaToshio ItoyamaYasuaki Taniguchi
    • Terushi HashiguchiToshio YoshidaToshio ItoyamaYasuaki Taniguchi
    • A61P31/04C07D277/40C07D277/42C07D277/44C07D277/46C07D277/52C07D277/56C07D401/12C07D417/04C07D417/12A61K31/425
    • C07D401/12C07D277/46C07D277/52C07D277/56C07D417/04C07D417/12
    • An antibacterial agent or bactericide, comprising a 2-aminothiazole derivative represented by the following formula (I) and a salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 each represent a hydrogen atom; a halogen atom; a lower alkyl, lower cycloalkyl, substituted or unsubstituted phenyl, thiophene, benzoyl, benzoylmethyl, benzyl or substituted benzyl or p-pivaloyloxyphenyl group; --COOR wherein R.sub.3 is a hydrogen atom, a lower alkyl group; and --CH.sub.2 COOR.sub.4 wherein R.sub.4 is a hydrogen atom or a lower alkyl, benzyl or substituted benzyl group; and A.sup.1 and A.sup.2 each represent a hydrogen atom; a lower alkanesulfonyl, halo lower alkanesulfonyl, phenyl or substituted phenyl, substituted benzoyl, substituted benzyl, substituted or unsubstituted benzenesulfonyl, substituted or unsubstituted lower alkanoyl or amidino group; --CO--R.sub.5 wherein R.sub.5 is a lower alkyl, phenyl or substituted phenyl group, --(CH.sub.2).sub.m --COOH wherein m is an integer of 1 to 5, or --(CH.sub.2).sub.n --NH--R.sub.6 wherein n is an integer of 1 to 5 and R.sub.6 is a hydrogen atom or a tert-butoxycarbonyl, benzyloxycarbonyl group; and --(CH.sub.2).sub.Q --R.sub.7 wherein Q is an integer of 0 to 5 and R.sub.7 is a lower alkoxy, phenyl or substituted phenyl, pyridyl or substituted pyridyl, cyclic amino group; or A.sup.1 and A.sup.2 may combine with each other to form a cyclic amino group.
    • PCT No.PCT / JP95 / 02347 Sec。 371日期1997年5月23日 102(e)日期1997年5月23日PCT提交1995年11月16日PCT公布。 公开号WO96 / 16650 PCT 日本1996年6月6日,含有下述式(I)所示的2-氨基噻唑衍生物及其盐的抗菌剂或杀菌剂:其中R1和R2各自表示氢原子; 卤素原子; 低级烷基,低级环烷基,取代或未取代的苯基,噻吩,苯甲酰基,苯甲酰基甲基,苄基或取代的苄基或对新戊酰氧基苯基; -COOR,其中R3是氢原子,低级烷基; 和-CH 2 COOR 4,其中R 4是氢原子或低级烷基,苄基或取代的苄基; A1和A2各自表示氢原子; 苯基或取代的苯基,取代的苯甲酰基,取代的苄基,取代或未取代的苯磺酰基,取代或未取代的低级烷酰基或脒基;低级烷基磺酰基, -CO-R 5,其中R 5是低级烷基,苯基或取代的苯基, - (CH 2)m -COOH,其中m是1至5的整数,或 - (CH 2)n -NH-R 6,其中n是 1〜5,R6为氢原子或叔丁氧羰基,苄氧羰基; 和 - (CH 2)Q-R 7,其中Q为0至5的整数,并且R 7为低级烷氧基,苯基或取代的苯基,吡啶基或取代的吡啶基,环状氨基; 或者A1和A2可以相互结合形成环状氨基。