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114 条记录 (耗时 0.048 秒)

    Pyridonecarboxylic acid derivatives substituted by a bicyclic amino group as antibacterials
    2.
    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
    3.
    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。

    Tricyclic amine derivatives
    6.
    发明授权
    Tricyclic amine derivatives 失效
    三环胺衍生物

    公开(公告)号：US06384050B1

    公开(公告)日：2002-05-07

    申请号：US09284871

    申请日：1999-04-22

    申请人： Makoto Takemura ,  Hisashi Takahashi ,  Kenichi Kimura ,  Rie Miyauchi ,  Hitoshi Ohki ,  Katsuhiro Kawakami

    发明人： Makoto Takemura ,  Hisashi Takahashi ,  Kenichi Kimura ,  Rie Miyauchi ,  Hitoshi Ohki ,  Katsuhiro Kawakami

    IPC分类号： C07D40104

    CPC分类号： C07D401/04 ,  C07D455/02 ,  C07D471/04 ,  C07D513/04

    摘要： The present invention relates to a compound having a tricyclic amine substituent which may have various substituents, the compound being represented by formula (I), a salt or hydrate thereof, and a hydrate of the salt and a drug containing them as an active ingredient. They exhibit excellent antimicrobial activity against Gram negative bacteria and Gram positive bacteria with a satisfactory fate and safety and are useful in the treatment of infectious diseases. wherein Q preferably represents the following partial structure which may have various substituents:

    摘要翻译： 本发明涉及可具有各种取代基的三环胺取代基的化合物，该化合物由式（I）表示，其盐或水合物，以及该盐的水合物和含有它们作为有效成分的药物。 它们对革兰氏阴性细菌和革兰氏阳性菌表现出优异的抗微生物活性，具有令人满意的命运和安全性，可用于治疗感染性疾病。其中Q优选表示以下可能具有各种取代基的部分结构：

    Bicyclic amine derivative
    7.
    发明授权
    Bicyclic amine derivative 失效
    双环胺衍生物

    公开(公告)号：US06191129B1

    公开(公告)日：2001-02-20

    申请号：US09147893

    申请日：1999-03-18

    申请人： Makoto Takemura ,  Hisashi Takahashi ,  Katsuhiro Kawakami

    发明人： Makoto Takemura ,  Hisashi Takahashi ,  Katsuhiro Kawakami

    IPC分类号： A61K315383

    CPC分类号： C07D498/06

    摘要： A pyridobenzoxazine derivative having a bicyclic amine derivative as its substituent, represented by the formula (I): exhibiting antimcrobial activity, and useful in treating infectious diseases and preserving food and agricultural products.

    摘要翻译： 由式（I）表示的具有双环胺衍生物作为取代基的吡啶并苯并恶嗪衍生物：具有抗菌活性，可用于治疗感染性疾病和保存食品和农产品。

    Aminomethylpyrrolidine derivatives having aromatic substituents
    8.
    发明授权
    Aminomethylpyrrolidine derivatives having aromatic substituents 失效

    公开(公告)号：US07186843B2

    公开(公告)日：2007-03-06

    申请号：US10834079

    申请日：2004-04-29

    申请人： Makoto Takemura ,  Hisashi Takahashi ,  Katsuhiro Kawakami ,  Toshiyuki Takeda ,  Rie Miyauchi

    发明人： Makoto Takemura ,  Hisashi Takahashi ,  Katsuhiro Kawakami ,  Toshiyuki Takeda ,  Rie Miyauchi

    IPC分类号： C07D207/09 ,  C07D401/12 ,  C07D403/12

    CPC分类号： C07D401/04 ,  C07D405/14

    摘要： This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of the same or a hydrate of both. In the formula, R2, R3: hydrogen atom, an alkyl group; R4, R5, R6: hydrogen atom, hydroxyl group, a halogen atom, carbamoyl group, an alkyl group, an alkoxyl group, an alkylthio group; R7, R8: hydrogen atom, an alkyl group; R9: an alkyl group, an alkenyl group, a halogenoalkyl group, a cyclic alkyl group, an aryl group, a heteroaryl group, an alkoxyl group having from 1 to 6 carbon atoms, an alkylamino group; R10:hydrogen atom, an alkylthio group; R11: hydrogen atom, amino group, hydroxyl group, thiol group, a halogenomethyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; X1: halogen atom, a hydrogen atom; A1: nitrogen atom, C—X2; X2: hydrogen atom, amino group, a halogen atom, cyano group, an halogenomethyl group, a halogenomethoxyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; A2, A3:>C═C (—A1═)—N(—R9)—, >N—C (—A1>)═C(—R9)—; R10 and R9 or R9 and X2 may be integrated to form a ring structure; and Y: hydrogen atom, ester forming group.

    Aminomethylpyrrolidine derivatives having aromatic substituents
    10.
    发明授权
    Aminomethylpyrrolidine derivatives having aromatic substituents 失效
    具有芳香取代基的氨基甲基吡咯烷衍生物

    公开(公告)号：US06762181B1

    公开(公告)日：2004-07-13

    申请号：US09936050

    申请日：2001-09-07

    申请人： Makoto Takemura ,  Hisashi Takahashi ,  Katsuhiro Kawakami ,  Toshiyuki Takeda ,  Rie Miyauchi

    发明人： Makoto Takemura ,  Hisashi Takahashi ,  Katsuhiro Kawakami ,  Toshiyuki Takeda ,  Rie Miyauchi

    IPC分类号： A61K314375

    CPC分类号： C07D401/04 ,  C07D405/14

    摘要： This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of the same or a hydrate of both. In the formula, R2, R3: hydrogen atom, an alkyl group; R4, R5, R6: hydrogen atoms, hydroxyl group, a halogen atom, carbamoyl group, an alkyl group, an alkoxyl group, an alkylthio group; R7, R8: hydrogen atom, an alkyl group; R9: an alkyl group, an alkenyl group, a halogenoalkyl group, a cyclic alkyl group, an aryl group, a heteroaryl group, an alkoxyl group having from 1 to 6 carbon atoms, an alkylamino group; R10: hydrogen atom, an alkylthio group; R11: hydrogen atom, amino group, hydroxyl group, thiol group, a halogenomethyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; X1: halogen atom, a hydrogen atom; A1: nitrogen atom, C—X2; X2: hydrogen atom, amino group, a halogen atom, cyano group, an halogenomethyl group, a halogenomethoxyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; A2, A3: >C═C(—A1═)—N(—R9)—, >N—C(—A1═)═C(—R9)—; R10 and R9 or R9 and X2 may be integrated to form a ring structure; and Y: hydrogen atom, ester forming group.

    摘要翻译： 本发明提供了一种喹诺酮衍生物，其具有对各种细菌的抗菌活性，包括耐药菌株，其为下式的化合物，其中R 1为任选取代的芳族基团，其两者的盐或两者的水合物。 式R 2，R 3：氢原子，烷基; R 4，R 5，R 6：氢原子，羟基，卤素原子，氨基甲酰基，烷基，烷氧基，烷硫基; R 7，R 8：氢原子，烷基; R 9：烷基，烯基，卤代烷基，环状烷基，芳基，杂芳基，碳原子数1〜6的烷氧基，烷基氨基， R 10：氢原子，烷硫基; R 11：氢原子，氨基，羟基，硫醇基，卤代甲基，烷基，烯基，炔基，烷氧基; X 1：卤素原子，氢原子; A 1：氮原子，C-X 2; X 2：氢原子，氨基，卤原子，氰基，卤代甲基，卤代甲氧基，烷基，烯基，炔基，烷氧基; A 2，A 3：C = C（-A 1 =）-N（-R 9） - ，> NC（-A 1）= C（-R 9） >） - ; R 10和R 9或R 9和X 2可以一体形成环结构; 和Y：氢原子，酯形成基团。