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50 条记录 (耗时 0.031 秒)

    Pyridonecarboxylic acid derivatives substituted by a bicyclic amino group as antibacterials
    1.
    发明授权
    Pyridonecarboxylic acid derivatives substituted by a bicyclic amino group as antibacterials 失效
    被双环氨基取代的吡啶酮羧酸衍生物作为抗菌剂

    公开(公告)号：US5849757A

    公开(公告)日：1998-12-15

    申请号：US875678

    申请日：1997-08-04

    申请人： Makoto Takemura ,  Youichi Kimura ,  Katsuhiro Kawakami ,  Kenichi Kimura ,  Hitoshi Ohki ,  Norikazu Matsuhashi ,  Haruko Kawato

    发明人： Makoto Takemura ,  Youichi Kimura ,  Katsuhiro Kawakami ,  Kenichi Kimura ,  Hitoshi Ohki ,  Norikazu Matsuhashi ,  Haruko Kawato

    IPC分类号： C07D401/04 ,  A61K31/435 ,  A61K31/47 ,  C07D471/04

    CPC分类号： C07D401/04

    摘要： This invention relates to a N.sub.1 -(halogenocyclopropyl)-substituted pyridonecarboxylic acid derivative represented by the following formula (I): ##STR1## wherein X.sup.1 is a halogen atom or a hydrogen atom; X.sup.2 is a halogen atom; R.sup.1 is a hydrogen atom, a hydroxyl group, a thiol group, a halogenomethyl group, an amino group, an alkyl group or an alkoxy group which may have a substituent group; R.sup.2 is a group represented by the following formula (II): ##STR2## wherein R.sup.3 and R.sup.4 are independently a hydrogen atom or an alkyl group and n is an integer of 1 or 2; A is a nitrogen atom or a partial structure of the following formula (III): ##STR3## wherein X.sup.3 is a hydrogen atom, a halogen atom, a cyano group, an amino group, an alkyl group, a halogenomethyl group, an alkoxyl group or a halogenomethoxyl group which may have a substituent group; and R is 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 phthalidynyl group, a 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl group, a 3-acetoxy-2-oxobutyl group, an alkyl group, an alkoxymethyl group or a phenylalkyl group, and provides a heterocyclic compound useful as antibacterial drugs.

    摘要翻译： PCT No.PCT / JP96 / 00208 Sec。 371日期：1997年8月4日 102（e）日期1997年8月4日PCT PCT 1996年2月1日PCT公布。 公开号WO96 / 23782 日本特开2006年8月8日本发明涉及由下式（I）表示的N1-（卤代环丙基） - 取代吡啶酮羧酸衍生物：其中X 1为卤原子或氢原子; X2是卤原子; R1是可以具有取代基的氢原子，羟基，硫醇基，卤代甲基，氨基，烷基或烷氧基; R2是由下式（II）表示的基团：其中R3和R4独立地是氢原子或烷基，n是1或2的整数; A是氮原子或下式（III）的部分结构：可以具有取代基的卤素原子，氰基，氨基，烷基，卤代甲基，烷氧基或卤代甲氧基 ; R为氢原子，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，邻苯二甲酰炔基，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，烷基，烷氧基甲基或苯基烷基，提供可用作抗菌药物的杂环化合物。

    Cycloalkylaminomethylpyrrolidine derivatives
    2.
    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

    申请人： Makoto Takemura ,  Youichi Kimura ,  Katsuhiro Kawakami ,  Hitoshi Ohki

    发明人： Makoto Takemura ,  Youichi Kimura ,  Katsuhiro Kawakami ,  Hitoshi Ohki

    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。

    Heterocyclic spiro-derivative
    3.
    发明授权
    Heterocyclic spiro-derivative 失效
    杂环螺衍生物

    公开(公告)号：US06469023B1

    公开(公告)日：2002-10-22

    申请号：US08875863

    申请日：1997-08-07

    申请人： Makoto Takemura ,  Youichi Kimura ,  Hitoshi Ohki

    发明人： Makoto Takemura ,  Youichi Kimura ,  Hitoshi Ohki

    IPC分类号： A61K3144

    CPC分类号： C07D401/04

    摘要： The present invention provides an antibacterial compound useful as medicines, animal drugs, fisheries drugs or antibacterial preservatives and to an antibacterial agent or preparation which contains the same, more particularly a compound which possesses high safety and excellent activity against a broad range of bacterial species including quinolone-resistant strains. A quinolone derivative of the following formula (I) which has a group derived from the heterocyclic spiro-compound at the 7-positioned R2 and the halogenocyclopropyl group at the N1-position, prefereably a compound of pure isomer, and an antibacterial agent containing the derivative compound.

    摘要翻译： 本发明提供了可用作药物，动物药物，渔业药物或抗菌防腐剂的抗菌化合物，以及含有该抗菌剂或抗菌剂的抗菌剂或制剂，更具体地，涉及对广泛的细菌种类具有高安全性和优异活性的化合物，包括 喹诺酮耐药株。 下述式（I）的喹啉酮衍生物，其具有衍生自7-位R2上的杂环螺环化合物和N1位上的卤代环丙基的基团，优选纯异构体的化合物和含有 衍生化合物。