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    Intermediates for pyridonecarboxylic acid derivatives
    7.
    发明授权
    Intermediates for pyridonecarboxylic acid derivatives 失效
    吡啶酮羧酸衍生物的中间体

    公开(公告)号：US5476950A

    公开(公告)日：1995-12-19

    申请号：US406594

    申请日：1995-03-20

    申请人： Isao Hayakawa ,  Shohgo Atarashi

    发明人： Isao Hayakawa ,  Shohgo Atarashi

    IPC分类号： C07D401/04 ,  A61K31/435 ,  A61K31/47 ,  A61P31/04 ,  C07D207/09 ,  C07D403/04 ,  C07D471/04

    CPC分类号： C07D401/04 ,  C07D471/04

    摘要： This invention provides novel pyridonecarboxylic acid derivatives having a quite high antimicrobial activity. The derivatives have the following formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 represent each a hydrogen or C.sub.1-C.sub.6 alkyl group; R.sup.4 represents an ethyl, 2-fluoroethyl, vinyl, isopropyl, isopropenyl or cyclopropyl group; and X represents CH, C--F, C--Cl or Ncharacterized in that R.sup.2 and R.sup.3 are not hydrogen at the same time.

    摘要翻译： 本发明提供具有相当高的抗微生物活性的新颖的吡啶酮羧酸衍生物。 衍生物具有下式：其中R 1，R 2和R 3各自表示氢或C 1 -C 6烷基; R4表示乙基，2-氟乙基，乙烯基，异丙基，异丙烯基或环丙基; X表示CH，C-F，C-Cl或N，其特征在于R2和R3不同时为氢。

    Optically active pyridobenzoxazine derivatives
    8.
    发明授权
    Optically active pyridobenzoxazine derivatives 失效
    光活性吡啶并苯并恶嗪衍生物

    公开(公告)号：US5463053A

    公开(公告)日：1995-10-31

    申请号：US183783

    申请日：1994-01-21

    申请人： Isao Hayakawa ,  Shohgo Atarashi ,  Yoichi Kimura ,  Katsuhiro Kawakami

    发明人： Isao Hayakawa ,  Shohgo Atarashi ,  Yoichi Kimura ,  Katsuhiro Kawakami

    IPC分类号： A61K31/535 ,  A61K31/00 ,  A61K31/5375 ,  A61K31/538 ,  A61K31/5383 ,  A61P31/00 ,  A61P31/04 ,  C07D498/06 ,  C07D215/56 ,  A61K31/47

    CPC分类号： C07D498/06

    摘要： An optically active pyridobenzoxazine derivative represented by formula (I): ##STR1## wherein R.sup.1 and R.sup.2 wherein R.sup.1 and R.sup.2, which may be the same or different, each represent an alkyl group having from 1 to 6 carbon atoms, a halogenated alkyl group having from 1 to 6 carbon atoms, a hydroxyalkyl group having from 1 to 6 carbon atoms, or an alkoxymethyl group having from 2 to 7 carbon atoms; R.sup.3 represents a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms, an acyl group having from 2 to 7 carbon atoms, a halogen-substituted or unsubstituted alkyloxycarbonyl group having from 2 to 7 carbon atoms, a phenylmethyloxycarbonyl group, or a phenylmethyloxycarbonyl group whose phenyl moiety is substituted with a halogen atom, a nitro group, or a methoxy group; R.sup.4 represents a methyl or fluoromethyl group which is in a .beta.-configuration; R.sup.5 represents a hydrogen atom, an amino group, a hydroxyl group, a methyl group, or a halogen atom; and X represents a fluorine atom or a chlorine atom, and a salt thereof are disclosed. These compounds exhibit potent antimicrobial activity with broad antimicrobial spectra and improved lipophilic properties.

    摘要翻译： 由式（I）表示的光学活性吡啶并苯并恶嗪衍生物：其中R 1和R 2其中R 1和R 2可以相同或不同，各自表示具有1至6个碳原子的烷基，卤代 具有1至6个碳原子的烷基，具有1至6个碳原子的羟基烷基或具有2至7个碳原子的烷氧基甲基; R3表示氢原子，具有1至6个碳原子的烷基，具有2至7个碳原子的酰基，卤素取代或未取代的碳原子数2〜7的烷氧基羰基，苯基甲氧基羰基或 苯基部分被卤素原子，硝基或甲氧基取代的苯基甲氧基羰基; R4代表β-构型的甲基或氟甲基; R5表示氢原子，氨基，羟基，甲基或卤素原子; 并且X表示氟原子或氯原子，及其盐。 这些化合物表现出强大的抗菌活性，具有广泛的抗菌谱和改善的亲脂性。