Invention Grant
- Patent Title: Antimicrobial potentiators
- Patent Title (中): 抗微生物增效剂
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Application No.: US14888022Application Date: 2014-05-03
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Publication No.: US09540389B2Publication Date: 2017-01-10
- Inventor: Timothy J. Opperman , Son T. Nguyen , Steven M. Kwasny , Xiaoyuan Ding
- Applicant: MICROBIOTIX, INC.
- Applicant Address: US MA Worcester
- Assignee: Microbiotix, Inc.
- Current Assignee: Microbiotix, Inc.
- Current Assignee Address: US MA Worcester
- Agency: Yankwich & Associates, P.C.
- Agent Leon R. Yankwich; David C. O'Brien
- International Application: PCT/US2014/036712 WO 20140503
- International Announcement: WO2014/179784 WO 20141106
- Main IPC: A61K31/5377
- IPC: A61K31/5377 ; C07D491/052 ; A61K31/551 ; C07D493/04 ; C07D513/04 ; A61K45/06 ; A61K31/436 ; A61K31/496 ; A61K31/541 ; A01N43/90 ; A01N47/44 ; A61K31/5383 ; A61K31/553

Abstract:
Novel compounds are disclosed having the structure of Formula I: wherein, n is an integer from 1 to 5; X is —CN, —F, —Cl, —Br, —I, —NO2; W is S, SO, SO2, O, NH, or NR5; R5 is alkyl, aralkyl, alkenyl, or alkynyl; Y is O, S; Z is NR1R2 or heterocycloalkyl; R1, R2 are, independently, hydrogen, alkyl, aralkyl, alkenyl, alkynyl, or cycloalkyl and may be optionally substituted with halo, hydroxy, alkoxy, amino, alkylamino, carboxy, alkoxycarbonyl, or nitrile groups; R3 and R4 are, independently, hydrogen, alkyl, aralkyl, alkenyl, alkynyl, or cycloalkyl and may be optionally substituted with halo, hydroxy, alkoxy, amino, alkylamino, carboxy, alkoxycarbonyl, or nitrile groups, and may together form a cyclic structure; and Ar is mono-, di-, or tri-substituted phenyl or heteroaryl, a pharmaceutically acceptable salts thereof. 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.
Public/Granted literature
- US20160075714A1 Antimicrobial Potentiators Public/Granted day:2016-03-17
Information query
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