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    • 1. 发明授权
    • Antibacterial optically pure benzoquinolizine carboxylic acids, processes, compositions and methods of treatment
    • 抗菌光学纯苯喹啉羧酸,方法,组合物和治疗方法
    • US06750224B1
    • 2004-06-15
    • US09640947
    • 2000-08-17
    • Mahesh Vithalbhai PatelShivkumar AgarwalSreenivas KandepuNitin ShettyDilip UpadhyayNishith ChaturvediAbraham ThomasNoel John De SouzaHabil Fakhruddin Khorakiwala
    • Mahesh Vithalbhai PatelShivkumar AgarwalSreenivas KandepuNitin ShettyDilip UpadhyayNishith ChaturvediAbraham ThomasNoel John De SouzaHabil Fakhruddin Khorakiwala
    • A61K3144
    • A61K31/4745C07B2200/07C07C279/14C07D455/04
    • The present invention relates to optically pure S-(−)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof, substantially free of their R-(+)-isomers, to processes for preparation of the optically pure S-(−)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof substantially free of their R-(+)-isomers, and to pharmaceutical compositions comprising the S(−)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof. These compounds and compositions can be used to systemically and topically treat bacterial Gram-positive, Gram-negative and anaerobic infections, specially resistant Gram-positive organism infections, Gram-negative organism infections, mycobacterial infections and emerging nosocomial pathogen infections, while avoiding toxic effects associated with the administration of the racemic mixture of RS-(±)-benzoquinolizine carboxylic acid. The compounds and compositions of this invention can also be used to treat diseases and disorders caused by Gram-positive, Gram-negative and anaerobic bacteria, and diseases and disorders caused by resistant Gram-positive organisms, Gram-negative organisms, mycobacteria and nosocomial pathogens.
    • 本发明涉及基本上不含其R - (+) - 异构体的光学纯的S - ( - ) - 苯并喹嗪羧酸,其衍生物,盐,假多晶型物,多晶型物和水合物,用于制备光学纯S - ( - ) - 苯并喹嗪羧酸,它们的衍生物,盐,假多晶型物,基本上不含其R - (+) - 异构体的多晶型物和水合物,以及包含S( - ) - 苯醌喹唑啉羧酸的衍生物, 盐,假多晶型物,多晶型物及其水合物。 这些化合物和组合物可用于全身和局部治疗细菌革兰氏阳性,革兰氏阴性和厌氧感染,特异性抗性革兰氏阳性生物感染,革兰氏阴性生物感染,分枝杆菌感染和新出现的医院病原体感染,同时避免毒性作用 与对 - (±) - 苯并喹嗪羧酸的外消旋混合物的给药相关。 本发明的化合物和组合物还可用于治疗由革兰氏阳性,革兰氏阴性和厌氧细菌引起的疾病和病症,以及由抗性革兰氏阳性生物,革兰氏阴性菌,分枝杆菌和医院病原体引起的疾病和病症 。