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2. 发明申请

WO2014179784A3 ANTIMICROBIAL POTENTIATORS 审中-公开
标题翻译：抗微生物电位
公开(公告)号：WO2014179784A3
公开(公告)日：2015-11-19
申请号：PCT/US2014036712
申请日：2014-05-03
申请人： MICROBIOTIX INC
发明人： OPPERMAN TIMOTHY J , NGUYEN SON T , KWASNY STEVEN M , DING XIAOYUAN
IPC分类号： A61K31/436
CPC分类号： C07D491/052 , A01N43/90 , A01N47/44 , A61K31/436 , A61K31/496 , A61K31/5377 , A61K31/5383 , A61K31/541 , A61K31/551 , A61K31/553 , A61K45/06 , C07D493/04 , C07D513/04 , A61K2300/00
摘要： Novel compounds are disclosed having the structure of Formula I. The compounds are potent bacterial efflux pump inhibitors (EPis). Such compounds are useful to potentiate the antimicrobial activity of antimicrobial compounds such as beta-lactam antibiotics and quinolone antibiotics against Gram-negative bacteria. These novel compounds are effective as antibiotic or antimicrobial potentiators. Structures of these compounds are distinctive from other reported efflux pump inhibitors and antibiotic potentiators. Also disclosed are methods for inhibiting bacterial efflux pumps with the novel compounds described herein. In another embodiment, the present invention discloses the use of these novel compounds for the inhibition of bacterial efflux pumps. In yet another embodiment, the present invention discloses the use of these novel compounds for treating or inhibiting bacterial infection.
摘要翻译：公开了具有式I结构的新型化合物。该化合物是有效的细菌外排泵抑制剂（EPis）。这些化合物可用于增强抗菌化合物如β-内酰胺抗生素和喹诺酮抗生素对革兰氏阴性菌的抗微生物活性。这些新型化合物作为抗生素或抗微生物增效剂是有效的。这些化合物的结构与其他报道的外排泵抑制剂和抗生素增强剂不同。还公开了用本文所述的新型化合物抑制细菌外排泵的方法。在另一个实施方案中，本发明公开了这些新型化合物用于抑制细菌外排泵的用途。在另一个实施方案中，本发明公开了这些新化合物用于治疗或抑制细菌感染的用途。

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