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29 条记录 (耗时 0.045 秒)

    Cis-substituted fluoromethylpyrrolidine derivative
    3.
    发明授权
    Cis-substituted fluoromethylpyrrolidine derivative 失效
    顺式取代的氟甲基吡咯烷衍生物

    公开(公告)号：US06656952B2

    公开(公告)日：2003-12-02

    申请号：US09446696

    申请日：1999-12-23

    申请人： Makoto Takemura ,  Hisashi Takahashi ,  Hitoshi Ohki ,  Kenichi Kimura ,  Rie Miyauchi ,  Toshiyuki Takeda

    发明人： Makoto Takemura ,  Hisashi Takahashi ,  Hitoshi Ohki ,  Kenichi Kimura ,  Rie Miyauchi ,  Toshiyuki Takeda

    IPC分类号： A61K3147

    CPC分类号： C07D401/04

    摘要： An antibacterial drug having potent antibacterial activities upon various bacteria including resistant strains and high safety is disclosed, which comprises as an active ingredient, quinolone derivatives represented by the following formula (I), its salts or hydrates thereof: wherein R1 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, R2 represents a halogenomethoxyl group or an alkoxyl group, R3 represents an alkyl group, an alkenyl group, a halogenoalkyl group, a cyclic alkyl group, a heteroaryl group, an alkoxyl group or an alkylamino group, and R4 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, 3-acetoxy-2-oxobutyl group, an alkyl group, an alkoxylmethyl group or a phenylalkyl group. These substituents may further have additional substituents.

    摘要翻译： 本发明公开了一种对各种细菌（包括耐药菌株）和高度安全性具有有效抗菌活性的抗菌药物，其包含作为活性成分的由下式（I）表示的喹诺酮衍生物，其盐或水合物：其中R 1表示 氢原子或碳原子数1〜6的烷基，R 2表示卤代甲氧基或烷氧基，R 3表示烷基，链烯基，卤代烷基，环状烷基，杂芳基 基团，烷氧基或烷基氨基，R 4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， 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。 这些取代基还可以具有另外的取代基。

    Tricyclic amine derivatives
    4.
    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：

    Substituted cyclobutylamine derivatives
    6.
    发明授权
    Substituted cyclobutylamine derivatives 失效
    取代的环丁胺衍生物

    公开(公告)号：US06448266B1

    公开(公告)日：2002-09-10

    申请号：US09424780

    申请日：1999-11-30

    申请人： Makoto Takemura ,  Hisashi Takahashi ,  Kazuyuki Sugita ,  Rie Miyauchi

    发明人： Makoto Takemura ,  Hisashi Takahashi ,  Kazuyuki Sugita ,  Rie Miyauchi

    IPC分类号： A61K3147

    CPC分类号： C07D401/04

    摘要： Substituted cyclobutylamine derivativesb with a novel structure represented by the following formula (I), wherein R1 to R4 and Q each represents a specific substituent and, in particular, Q represents a quinolone derivative having a specific structure. These derivatives are useful as antibacterial compounds which have excellent antibacterial activity against a wide scope of bacteria including Gram-negative and Gram-positive bacteria, exert potent antibacterial activity particularly against methicillin-resistant Staphylococcus aureus (MRSA) strains, penicillin-resistant pneumococcus strains and quinolone-resistant bacteria, and are also possessed of both excellent pharmacokinetics and high safety.

    摘要翻译： 具有由下式（I）表示的新结构的取代的环丁基胺衍生物b，其中R 1至R 4和Q各自表示特定取代基，特别是Q表示具有特定结构的喹诺酮衍生物。 这些衍生物可用作对广泛范围的细菌（包括革兰氏阴性和革兰氏阳性细菌）具有优异的抗菌活性的抗菌化合物，特别是耐甲氧西林金黄色葡萄球菌（MRSA）菌株，青霉素耐药性肺炎球菌菌株和 喹诺酮抗性细菌，也具有优异的药代动力学和高安全性。

    Cycloalkyl-substituted aminomethylpyrrolidine derivatives
    9.
    发明授权
    Cycloalkyl-substituted aminomethylpyrrolidine derivatives 失效
    环烷基取代的氨基甲基吡咯烷衍生物

    公开(公告)号：US06573260B1

    公开(公告)日：2003-06-03

    申请号：US09856631

    申请日：2001-05-24

    申请人： Makoto Takemura ,  Hisashi Takahashi ,  Rie Miyauchi ,  Toshiyuki Takeda ,  Isao Hayakawa

    发明人： Makoto Takemura ,  Hisashi Takahashi ,  Rie Miyauchi ,  Toshiyuki Takeda ,  Isao Hayakawa

    IPC分类号： A61K314709

    CPC分类号： C07D401/04

    摘要： This invention provides a quinolone derivative which exerts strong antibacterial action upon various bacteria and has high safety, and it relates to a compound having a structure of formula (I), its salts and hydrates thereof: {R1 and R2: hydrogen, alkyl; n: 1 to 4; Q: following structure (Ia): [R3: alkyl, alkenyl, halogenoalkyl, cyclic alkyl, aryl, heteroaryl, alkoxyl, alkylamino; R4: hydrogen, alkylthio; R5: hydrogen, amino, hydroxyl, thiol, halogenomethyl, alkyl, alkenyl, alkynyl, alkoxyl; X1: halogen, hydrogen, A1: nitrogen, structure of formula (II): (X2: hydrogen, amino, halogen, cyano, halogenomethyl, halogenomethyl, alkyl, alkenyl, alkynyl, alkoxyl; R4 and R3 or X2 and R3 may together form a cyclic structure; Y: hydrogen, various ester forming groups]}.

    摘要翻译： 本发明提供了一种喹诺酮衍生物，其对各种细菌具有强烈的抗菌作用并具有高度的安全性，它涉及具有式（I）结构的化合物及其盐和水合物：{R1和R2：氢，烷基; n：1到4; Q：以下结构（Ia）：[R3：烷基，烯基，卤代烷基，环烷基，芳基，杂芳基，烷氧基，烷基氨基; R4：氢，烷硫基; R5：氢，氨基，羟基，硫醇，卤代甲基，烷基，烯基，炔基，烷氧基; X1：卤素，氢，A1：氮，式（II）的结构：（X2：氢，氨基，卤素，氰基，卤代甲基，卤代甲基，烷基，烯基，炔基，烷氧基; R4和R3或X2和R3可以一起形成 环状结构; Y：氢，各种酯形成基团]}。

    Tri-, tetra-substituted-3-aminopyrrolidine derivative
    10.
    发明授权
    Tri-, tetra-substituted-3-aminopyrrolidine derivative 有权
    三取代的3-氨基吡咯烷衍生物

    公开(公告)号：US07563805B2

    公开(公告)日：2009-07-21

    申请号：US11413153

    申请日：2006-04-28

    申请人： Hisashi Takahashi ,  Hiroaki Inagaki ,  Satoshi Komoriya ,  Makoto Takemura ,  Rie Miyauchi

    发明人： Hisashi Takahashi ,  Hiroaki Inagaki ,  Satoshi Komoriya ,  Makoto Takemura ,  Rie Miyauchi

    IPC分类号： A01N43/42 ,  A61K31/47 ,  C07D215/00

    CPC分类号： C07D207/14 ,  Y02P20/55

    摘要： A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria, and which are also highly safe are provided. The compound provided is represented by following formula (I): wherein R1 and R2 represent hydrogen atom, or the like; R3 represents an alkyl group containing 1 to 6 carbon atoms, or the like; R4 and R5 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like, with the proviso that R4 and R5 do not simultaneously represent hydrogen atom; or the substituents R4 and R5 together represent (a) a 3- to 6-membered cyclic structure including the carbon atom shared by R4 and R5 to form a spirocyclic structure with the pyrrolidine ring; R6 and R7 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like; R8 represents a halogen-substituted alkyl group containing 1 to 6 carbon atoms, or the like; X1 represents hydrogen atom or a halogen atom; A represents nitrogen atom or a moiety represented by formula (II):

    摘要翻译： 提供喹诺酮合成抗菌剂和用于感染的治疗剂，其对革兰氏阳性和革兰氏阴性细菌都具有广谱和强抗菌活性，并且也是高度安全的。 所提供的化合物由下式（I）表示：其中R1和R2表示氢原子等; R3表示含有1〜6个碳原子的烷基等; R4和R5独立地表示氢原子，含有1至6个碳原子的烷基等，条件是R4和R5不同时表示氢原子; 取代基R 4和R 5一起表示（a）包含由R 4和R 5共有的碳原子与吡咯烷环形成螺环结构的3至6元环状结构; R6和R7独立地表示氢原子，含有1至6个碳原子的烷基等; R8表示含有1〜6个碳原子的卤素取代的烷基等; X1表示氢原子或卤素原子; A表示氮原子或由式（II）表示的部分：