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    • 5. 发明公开
    • Quinolinecarboxylic acid derivatives
    • Chinolincarbonsäurederivate。
    • EP0249043A2
    • 1987-12-16
    • EP87106953.0
    • 1987-05-13
    • NIPPON SHINYAKU COMPANY, LIMITED
    • Kise, MasahiroKitano, MasahikoOzaki, MasakuniKazuno, KenjiShirahase, IchiroTomii, YoshifumiSegawa, Jun Room 405
    • C07D513/04
    • C07D513/04
    • Quinolinecarboxylic acid derivatives represented by the following general formula (I) and physiologically-acceptable salts thereof.
      wherein R' is hydrogen, alkyl, or substituted or unsubstituted phenyl; R 2 is hydrogen, alkyl, alkoxy, hydroxy, halogen, nitro or substituted or unsubstituted amino; R 3 is hydrogen or optionally-substituted alkyl; R 4 and R 5 are same or different and are alkyl or hydroxyalkyl or R 4 and R 5 may be combined and may form a cyclic amino together with the adjacent nitrogen atom and said cyclic amino may also be substituted and may further contain nitrogen, oxygen or sulfur as heteroatoms therein; and X is halogen, have been found to be very effective antibacterial therapeutic agents for systemic and local infectious diseases caused by P. aeruginosa and Gram-positive and negative bacteria.
    • 由以下通式(I)表示的喹啉羧酸衍生物及其生理学上可接受的盐。 其中R 1为氢,烷基或取代或未取代的苯基; R 2是氢,烷基,烷氧基,羟基,卤素,硝基或取代或未取代的氨基; R 3是氢或任选取代的烷基; R 4和R 5相同或不同,并且是烷基或羟基烷基,或者R 4和R 5可以相互结合形成环状氨基并且所述环状氨基也可以是 并且可以进一步含有氮,氧或硫作为其中的杂原子; X为卤素。 已经被发现是非常有效的抗菌治疗剂,用于由铜绿假单胞菌和脾阳性和阴性细菌引起的全身和局部感染性疾病。