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    Antibacterial optically pure benzoquinolizine carboxylic acids, processes, compositions and methods of treatment
    32.
    发明授权
    Antibacterial optically pure benzoquinolizine carboxylic acids, processes, compositions and methods of treatment 有权
    抗菌光学纯苯喹啉羧酸，方法，组合物和治疗方法

    公开(公告)号：US06750224B1

    公开(公告)日：2004-06-15

    申请号：US09640947

    申请日：2000-08-17

    申请人： Mahesh Vithalbhai Patel ,  Shivkumar Agarwal ,  Sreenivas Kandepu ,  Nitin Shetty ,  Dilip Upadhyay ,  Nishith Chaturvedi ,  Abraham Thomas ,  Noel John De Souza ,  Habil Fakhruddin Khorakiwala

    发明人： Mahesh Vithalbhai Patel ,  Shivkumar Agarwal ,  Sreenivas Kandepu ,  Nitin Shetty ,  Dilip Upadhyay ,  Nishith Chaturvedi ,  Abraham Thomas ,  Noel John De Souza ,  Habil Fakhruddin Khorakiwala

    IPC分类号： A61K3144

    CPC分类号： A61K31/4745 ,  C07B2200/07 ,  C07C279/14 ,  C07D455/04

    摘要： 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.

    摘要翻译： 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 。

    Prodrugs of benzoquinolizine-2-carboxylic acid
    34.
    发明授权
    Prodrugs of benzoquinolizine-2-carboxylic acid 有权
    苯喹啉-2-羧酸的前药

    公开(公告)号：US07868173B2

    公开(公告)日：2011-01-11

    申请号：US11715921

    申请日：2007-03-09

    申请人： Mahesh Vithalbhai Patel ,  Vijaya Narayan Desai ,  Prasad Keshav Deshpande ,  Ravindra Dattatraya Yeole ,  Rajesh Prabhakar Kale

    发明人： Mahesh Vithalbhai Patel ,  Vijaya Narayan Desai ,  Prasad Keshav Deshpande ,  Ravindra Dattatraya Yeole ,  Rajesh Prabhakar Kale

    IPC分类号： C07D221/06 ,  A61K31/473

    CPC分类号： C07D455/04

    摘要： The instant invention relates to novel prodrugs of optically pure benzoquinolizine-2-carboxylic acid and pharmaceutical compositions that include the prodrugs. In particular, the present invention relates to the sulfonic acid salts of L-alanine and L-valine prodrugs of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid. The compounds and compositions of the invention can be used to treat bacterial Gram-positive, Gram-negative and anaerobic infections, especially infections caused by resistant Gram-positive organism and Gram-negative organism, mycobacterial infections and emerging nosocomial pathogen infections.

    摘要翻译： 本发明涉及光学纯苯醌喹唑啉-2-羧酸的新型前体药物和包含前药的药物组合物。 特别地，本发明涉及L-丙氨酸的磺酸盐和S - （ - ） - 9-氟-6,7-二氢-8-（4-羟基哌啶-1-基） - 5-甲基-1-氧代-1H，5H-苯并[i，j]喹嗪-2羧酸。 本发明的化合物和组合物可用于治疗细菌革兰氏阳性，革兰氏阴性和厌氧感染，特别是由抗性革兰氏阳性生物和革兰氏阴性生物，分枝杆菌感染和新出现的医院病原体感染引起的感染。