Cycloalkylaminomethylpyrrolidine derivatives
    22.
    发明授权
    Cycloalkylaminomethylpyrrolidine derivatives 失效
    环烷基氨基甲基吡咯烷衍生物

    公开(公告)号:US06194434B1

    公开(公告)日:2001-02-27

    申请号:US09171637

    申请日:1998-10-22

    IPC分类号: A61K3147

    CPC分类号: C07D401/04

    摘要: A quinolone derivative represented by formula (I): wherein R1 represents a cycloalkyl group; R2 represents a hydrogen atom, an amino group, a hydroxyl group, a thiol group, a halogenomethyl group, an alkyl group, an alkenyl group, an alkynyl group, or an alkoxyl group; R3 represents an amino group, a halogenomethyl group, a halogenomethoxyl group, an alkyl group, an alkenyl group, an alkynyl group, or an alkoxyl group; R4 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R5 represents a cycloalkyl group having 3 to 6 carbon atoms; the above R1 to R5 may be substituted; X represents a halogen atom or a hydrogen atom; and Y represents a hydrogen atom, a phenyl group, an acetoxymethyl group, a pivaloyloxymethyl group, an ethoxycarbonyl group, a choline group, a dimethylaminoethyl group, a 5-indanyl group, a phthalidinyl group, a 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl group, a 3-acetoxy-2-oxobutyl group, an alkyl group having 1 to 6 carbon atoms, an alkoxymethyl group having 2 to 7 carbon atoms, or a phenylalkyl group having 1 to 6 carbon atoms in the alkyl moiety thereof, or a salt thereof. The compound exhibits high and broad antimicrobial activity against various bacteria including bacteria resistant to drugs and high safety.

    摘要翻译: 由式(I)表示的喹诺酮衍生物:其中R1表示环烷基; R2表示氢原子,氨基,羟基,硫醇基,卤代甲基,烷基,烯基,炔基或烷氧基; R3表示氨基,卤代甲基,卤代甲氧基,烷基,烯基,炔基或烷氧基; R4表示氢原子或碳原子数1〜6的烷基。 R5表示碳原子数3〜6的环烷基; 上述R 1〜R 5可以被取代; X表示卤素原子或氢原子; Y表示氢原子,苯基,乙酰氧基甲基,新戊酰氧基甲基,乙氧基羰基,胆碱基,二甲基氨基乙基,5-二氢化茚基,苯酞基,5-烷基-2-氧代 - 1,3-二氧杂环戊烯-4-基甲基,3-乙酰氧基-2-氧代丁基,碳原子数1〜6的烷基,碳原子数2〜7的烷氧基甲基或碳原子数1〜6的苯基烷基 其烷基部分的原子,或其盐。 该化合物对各种细菌(包括对药物有抗性的细菌和高安全性)具有高而广的抗菌活性。