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    • 15. 发明授权
    • Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
    • 碳青霉烯抗菌化合物,含有这些化合物的组合物和治疗方法
    • US06294529B1
    • 2001-09-25
    • US09421690
    • 1999-10-07
    • Lovji D. CamaRonald W. RatcliffeRobert R. WilkeningKenneth J. WildongerWanying Sun
    • Lovji D. CamaRonald W. RatcliffeRobert R. WilkeningKenneth J. WildongerWanying Sun
    • C07D47714
    • C07D477/14
    • Compounds of formula I are disclosed. as well as pharmaceutically acceptable salts thereof. The naphthosultam is substituted with various substituent groups including at least one cationic group -A-Q-L-B, wherein A-Q-L-B represents a side chain wherein: A is a C1-6 alkylene group, straight or branched, and optionally interrupted or terminated by 1-2 of —O—, —S—, NRa—, —C(O)— and —CH═CH—; Q represents  in which: b is 2 or 3; and X− is a charge balancing group; L represents a C1-8 alkylene group, unsubstituted or substituted with 1-3 Rc groups, and is interrupted or terminated by 1-3 of —CH═CH—, —C(O)—, —C(O)NRd—, —Het(Re)—, —C(O)—Het(Re)—, —C(O)NRa—Het(Re)—, —O—,—S—, —S(O)—, —SO2—, —CO2—, NRa—, —N+(Ra)2— B represents The carbapenems of the invention are effective against susceptible bacterial organisms, including methicillin resistant Staphylococcus aureus (MRSA), methicillin resistant Staphylococcus epidermidis (MRSE), and methicillin resistant coagulase negative Staphylococci (MRCNS).
    • 公开了式I的化合物以及其药学上可接受的盐。 萘并磺胺被包括至少一个阳离子基团-AQLB的各种取代基取代,其中AQLB表示侧链,其中:A是直链或支链的C1-6亚烷基,并且任选地被1-2的-O-O - , - S - ,NR a - , - C(O) - 和-CH = CH-; Q表示其中:b为2或3; X为电荷平衡基团; L为C1-8亚烷基 并且被1-3个R c基团取代,并被1-3个-CH = CH-,-C(O) - , - C(O)NR d - , - H(Re) - , - C(O)-Het(Re) - , - C(O)NR a -Het(Re) - , - O - , - S - , - S(O) - , - SO 2 - , - -N +(Ra)2-B代表本发明的碳青霉烯类对敏感细菌生物有效,包括耐甲氧西林金黄色葡萄球菌(MRSA),耐甲氧西林葡萄球菌(MRSE)和耐甲氧西林凝固酶阴性葡萄球菌(MRCNS)。