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1. 发明申请

WO2005067939A1 THERAPEUTICALLY USEFUL ANTIBACTERIAL COMPOUNDS 审中-公开
标题翻译：可治疗有用的抗生素化合物
公开(公告)号：WO2005067939A1
公开(公告)日：2005-07-28
申请号：PCT/GB2005/000131
申请日：2005-01-17
申请人： OXOID LIMITED , BOVILL, Richard , DRUGGAN, Patrick
发明人： BOVILL, Richard , DRUGGAN, Patrick
IPC分类号： A61K31/662
CPC分类号： A61K31/662 , A61K47/54 , A61K47/6903 , A61K47/6943
摘要： Disclosed is a compound which has antibiotic activity in vivo in a mammalian, preferably a human, subject, the compound comprising an uptake moiety linked to a bactericidal or bacteriostatic toxic moiety, said uptake moiety facilitating uptake of the compound by bacteria on which the toxic moiety exerts a bactericidal or bacteriostatic effect, wherein: (a) the compound is non-toxic for mammalian subjects; (b) the linkage between the uptake moiety and the toxic moiety is one which is cleavable by an enzyme or enzymes produced by the bacteria to be killed/inhibited, but is not readily cleavable by enzymes produced by the subject and to which the compound is exposed prior to contacting the bacteria; and (c) the toxic moiety, when cleaved from the uptake moiety, is toxic for the bacteria, but not toxic for the subject.
摘要翻译：公开了一种在哺乳动物，优选人类受试者体内具有抗生素活性的化合物，该化合物包含与杀菌或抑菌毒性部分连接的摄取部分，所述吸收部分便于由细菌摄取化合物，其中毒性部分发挥杀菌或抑菌作用，其中：（a）该化合物对哺乳动物受试者无毒; （b）摄取部分和毒性部分之间的连接是可被酶杀死的酶或由被杀死/抑制的细菌产生的酶，但不容易被受试者产生的酶切割，并且化合物在接触细菌之前暴露; 和（c）当从摄取部分切割时，毒性部分对细菌是有毒的，但对受试者无毒性。

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