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    • 1. 发明申请
    • PYRIDONECARBOXYLIC ACID DERIVATIVE
    • 吡咯烷酮羧酸衍生物
    • WO1992021659A1
    • 1992-12-10
    • PCT/JP1992000687
    • 1992-05-27
    • DAIICHI PHARMACEUTICAL CO., LTD.HAYAKAWA, IsaoKIMURA, YouichiTAKAHASHI, Hisashi
    • DAIICHI PHARMACEUTICAL CO., LTD.
    • C07D215/56
    • C07D487/04C07D215/56C07D401/04C07D471/04Y02P20/55
    • Known synthetic antibacterials having a condensed pyridonecarboxylic acid skeleton include quinolone derivatives having various substituents at various positions of the skeleton. The possibility of the presence of diastereoisomerism in these derivatives, however, gives rise to a mixture of at least four diastereomers having properties differing from one another, resulting in the difficulty in applying the same as such as a medicine. Under these circumstances the present invention provides an antibacterial 1-(1,2-cis-2-fluorocyclopropyl) quinolone derivative represented by general formula (I) comprising a single diastereoisomer even when there are various diastereoisomers thereof. In formula (I), R represents methyl, difluoromethyl, etc.; R represents a saturated nitrogenous heterocyclic group; A represents C-X or nitrogen; X and X represent each independently halogen; and X and Z represent each hydrogen, etc.
    • 具有缩合吡啶酮羧酸骨架的已知合成抗菌剂包括在骨架的各个位置具有各种取代基的喹诺酮衍生物。 然而,在这些衍生物中存在非对映异构体的可能性导致具有彼此不同的性质的至少四种非对映异构体的混合物,导致难以应用与药物相同的性质。 在这些情况下,本发明提供了即使存在各种非对映异构体也包含单一非对映异构体的由通式(I)表示的抗菌1-(1,2-顺式2-氟环丙基)喹诺酮衍生物。 在式(I)中,R 1表示甲基,二氟甲基等; R 2表示饱和含氮杂环基; A表示C-X 3或氮; X 1和X 2各自独立地表示卤素; X 3和Z代表每个氢等