Fused substituted aminopyrrolidine derivative

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 401/04 (2006.01) A61K 31/47 (2006.01) A61P 31/04 (2006.01) C07D 401/14 (2006.01) C07D 491/052 (2006.01) C07D 498/04 (2006.01)

Patent

CA 2674369

A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure.

L'invention concerne un agent antibactérien synthétique de type quinolone présentant d'excellentes propriétés thérapeutiques, cet agent développant une forte activité antibactérienne, non seulement par rapport aux bactéries à Gram négatif, mais aussi par rapport aux cocci à Gram positif qui sont peut sensibles aux agents antibactériens de type quinolone, ledit agent présentant un niveau de sécurité élevé et d'excellentes propriétés de pharmacocinétique. L'invention concerne aussi un composé de formule (I) ou un sel de celui-ci ou bien un hydrate de celui-ci. L'invention porte en particulier sur un dérivé de quinolone de formule (I) dans laquelle les susbtituants R6 et R7, avec les atomes carbones auxquels ils sont liés, forment une structure cyclique qui peut contenir un atome d'oxygène en tant qu'atome constituant un noyau, la structure cyclique formant un substituant de pyrrolidinyle bicyclique lié par fusion 5-4, 5-5 ou 5-6, ce substituant étant lié à un squelette mère de quilonone Q comportant une structure pyridobenzoxazine: (I).

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