Optically active pyridobenzoxazine derivatives
    1.
    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

    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。

    Intermediates for pyridonecarboxylic acid derivatives
    2.
    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

    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。

    Pyridonecarboxylic acid derivatives
    9.
    发明授权
    Pyridonecarboxylic acid derivatives 失效
    吡咯烷酮羧酸衍生物

    公开(公告)号:US5098912A

    公开(公告)日:1992-03-24

    申请号:US449160

    申请日:1989-12-12

    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 N wherein (i) one of R.sup.1, R.sup.2 and R.sup.3 represents a hydrogen or C.sub.1 -C.sub.6 alkyl group, and (ii) either R.sup.1 forms a methylene chain having 2 to 4 carbon atoms together with R.sup.2 or R.sup.3, or R.sup.2 and R.sup.3 form together an alkylene chain having 2 to 5 atoms and R.sup.4 represents an ethyl, 2-fluorethyl, vinyl, isopropyl, isopropenyl or cyclopropyl group and X represents CH, C-F, or C-Cl and salt thereof.

    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; 并且X表示CH,CF,C-Cl或N,其中(i)R 1,R 2和R 3中的一个表示氢或C 1 -C 6烷基,和(ii)R 1一起形成具有2至4个碳原子的亚甲基链 R 2或R 3,或R 2和R 3一起形成具有2至5个原子的亚烷基链,并且R 4表示乙基,2-氟甲基,乙烯基,异丙基,异丙烯基或环丙基,X表示CH,CF或C-Cl和盐 其中。