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1. (WO2014179784) ANTIMICROBIAL POTENTIATORS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2014/179784    International Application No.:    PCT/US2014/036712
Publication Date: 06.11.2014 International Filing Date: 03.05.2014
Chapter 2 Demand Filed:    08.01.2015    
IPC:
A61K 31/436 (2006.01)
Applicants: MICROBIOTIX, INC. [US/US]; One Innovation Drive Worcester, MA 01605 (US)
Inventors: OPPERMAN, Timothy, J.; (US).
NGUYEN, Son, T.; (US).
KWASNY, Steven, M.; (US).
DING, Xiaoyuan; (US)
Agent: YANKWICH, Leon, R.; Yankwich & Associates, PC. 201 Broadway Cambridge, MA 02139 (US)
Priority Data:
61/819,054 03.05.2013 US
Title (EN) ANTIMICROBIAL POTENTIATORS
(FR) POTENTIALISATEURS ANTIMICROBIENS
Abstract: front page image
(EN)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.
(FR)L'invention concerne de nouveaux composés ayant la structure de la formule I dans laquelle : n est un nombre entier allant de 1 à 5; X est -CN, -F, -CI, -Br, -I, -NO2; W est S, SO, SO2, O, NH ou NR5; R5 est alkyle, aralkyle, alcényle ou alcynyle; Y est O, S; Z est NR1R2 ou hétérocycloalkyle; R1, R2 sont, indépendamment, hydrogène, alkyle, aralkyle, alcényle, alcynyle ou cycloalkyle et peuvent être facultativement substitués par des groupes halo, hydroxy, alcoxy, amino, alkylamino, carboxy, alcoxycarbonyle ou nitrile; R3 et R4 sont, indépendamment, hydrogène, alkyle, aralkyle, alcényle, alcynyle ou cycloalkyle et peuvent être facultativement substitués par des groupes halo, hydroxy, alcoxy, amino, alkylamino, carboxy, alcoxycarbonyle ou nitrile, et peuvent conjointement former une structure cyclique; Ar est phényle ou hétéroaryle mono-, di- ou tri-substitué, des sels de qualité pharmaceutique de ceux-ci. Les composés sont des inhibiteurs puissants de pompe à écoulement (EPI) bactériens. De tels composés sont utiles pour potentialiser l'activité antimicrobienne de composés antimicrobiens tels que des antibiotiques bêta-lactame et des antibiotiques quinilone contre des bactéries à gram négatif.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)