C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/04 (2006.01) A61K 31/4709 (2006.01) A61P 31/04 (2006.01)
Patent
CA 2536429
[PROBLEMS] To provide a novel quinolonecarboxylic acid compound which is safe, has potent antibacterial activity, and is effective against resistant bacteria which are less controlled by conventional antibacterials. [MEANS FOR SOLVING PROBLEMS] It is a 7-(4-substituted 3- cyclopropylaminomethylpyrrolidinyl)quinolonecarboxylic acid derivative represented by the general formula (I)(typical example: 1-cyclopropyl-7- [(3S,4S)-3-cyclopropyl~aminomethyl-4-fluoro-1-pyrrolidinyl]-6-fluoro-1,4- dihydro~8-methoxy-4-oxo-3-quinolinecarboxylic acid). The derivative has potent antibacterial activity against gram-positive bacteria, in particular, resistant bacteria such as MRSA, PRSP, and VRE, and is highly safe.
Problèmes : produire un nouveau composé acide quinolonecarboxylique dont l'innocuité est garantie, qui possèdent une activité antibactérienne puissante et qui est efficace contre des bactéries résistantes moins bien attaquées par des antibactériens classiques. Solutions : un dérivé d'acide quinolonecarboxylique 7-(4-substitué 3-cyclopropylaminométhyl-1-pyrrolidinyle) représenté par la formule générale (I):I Exemple typique: 1-cyclopropyl-7-[(3S, 4S)-3-cyclopropyl-aminométhyl-4-fluoro-1-pyrrolidinyl]-6-fluoro-1,4-dihydro-8-méthoxy-4-oxo-3-acide quinolinecarbocylique). Ce dérivé posède une activité antibactérienne puissante contre les bactérie gram positif, en particulier contre des bactéries résistantes telles que MRSA, PRSP, et VRE, et ce composé présente une très bonne innocuité.
Asahina Yoshikazu
Takei Masaya
Kyorin Pharmaceutical Co. Ltd.
Norton Rose Or S.e.n.c.r.l.,s.r.l./llp
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