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    Antibacterial optically pure benzoquinolizine carboxylic acids, processes, compositions and methods of treatment
    1.
    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 。

    Synthetic amino acid-and/or peptide-containing graft copolymers
    3.
    发明授权
    Synthetic amino acid-and/or peptide-containing graft copolymers 失效
    合成氨基酸和/或含肽的接枝共聚物

    公开(公告)号：US4908404A

    公开(公告)日：1990-03-13

    申请号：US234896

    申请日：1988-08-22

    申请人： Christine V. Benedict ,  Nishith Chaturvedi

    发明人： Christine V. Benedict ,  Nishith Chaturvedi

    IPC分类号： A61L27/00 ,  C07K7/06 ,  C07K14/00 ,  C08F8/30 ,  C08G69/00 ,  C08G69/08

    CPC分类号： C08F8/30

    摘要： A water soluble cationic peptide-containing graft copolymer exhibiting a number average molecular weight of from about 30,000 to about 500,000 are provided comprising:(a) a polymeric backbone containing or capable of modification to include free primary or secondary amine functional groups for reaction with an amino acid or peptide graft and exhibiting a number average molecular weight from about 10,000 to about 250,000; and(b) an amino acid or peptide graft reacted with from at least about 5% to about 100% of the primary or secondary amine functional groups of the polymeric backbone, wherein said amino acid or peptide graft comprises at least one 3,4-dihydroxyphenylalaine (Dopa) amino acid or a precursor thereof capable of hydroxylation to the Dopa form.The peptide-containing graft copolymers of the present invention can vary in (a) molecular weight, cationicity, percent substitution of the amino acid or peptide unit grafted to the polymer backbone and (b) the chemical and physical structure of the peptide-containing graft copolymer itself, thereby enabling specific tailoring of the polymers of the present invention for particular end-use applications.