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1. (WO2017190116) SYNTHETIC LIGANDS THAT MODULATE THE ACTIVITY OF THE RHLR QUORUM SENSING RECEPTOR
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Pub. No.: WO/2017/190116 International Application No.: PCT/US2017/030314
Publication Date: 02.11.2017 International Filing Date: 30.04.2017
IPC:
C07D 307/33 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02
not condensed with other rings
26
having one double bond between ring members or between a ring member and a non-ring member
30
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
32
Oxygen atoms
33
in position 2, the oxygen atom being in its keto or unsubstituted enol form
Applicants: WISCONSIN ALUMNI RESEARCH FOUNDATION[US/US]; 614 Walnut Street Madison, WI 53726, US
Inventors: BLACKWELL, Helen; US
BOURSIER, Michelle, E.; US
MOORE, Joseph, D.; US
Agent: SULLIVAN, Sally, S.; US
Priority Data:
62/329,94229.04.2016US
62/376,29117.08.2016US
Title (EN) SYNTHETIC LIGANDS THAT MODULATE THE ACTIVITY OF THE RHLR QUORUM SENSING RECEPTOR
(FR) LIGANDS SYNTHÉTIQUES MODULANT L'ACTIVITÉ DU RÉCEPTEUR DE DÉTECTION DU QUORUM RHLR
Abstract:
(EN) RhlR modulators including agonist and antagonists which are useful for modulating QS phenotypes in Gram-negative bacteria. Certain compounds of general formula A-W-HG having various carbocyclic ad heterocyclic head groups (HG) and various tail groups (A), where -W- is -CO-NH-, -SO2-NH-, -CO-NH-CH2-, or -SO2-NH-CH2- are RhlR agonists or antagonists. The compounds are useful in methods of modulating quorum sensing in Gram-negative bacteria, particularly in Pseudomonas. Compositions including certain RhlR modulators are useful for decreasing the virulence of Gram-negative bacteria. Pharmaceutical compositions comprising certain RhlR modulators are useful for treatment of infections of Gram-negative bacteria.
(FR) L'invention concerne les modulateurs de RhlR comprenant des agonistes et des antagonistes qui sont utilisés pour moduler des phénotypes QS dans des bactéries à Gram négatif. Certains composés de formule générale A-W-HG ayant différents groupes de tête (HG) carbocycliques et hétérocycliques et divers groupes de queue (A), où -W- représente -CO-NH-, -SO2-NH-, -CO-NH-CH2-, ou -SO2-NH-CH2-, sont des agonistes ou des antagonistes de RhlR. Les composés sont utilisés dans des procédés de modulation de la détection de quorum dans des bactéries à Gram négatif, en particulier Pseudomonas. Des compositions comprenant certains modulateurs de RhlR sont utilisées pour diminuer la virulence des bactéries à Gram négatif. Des compositions pharmaceutiques comprenant certains modulateurs de RhlR sont utilisées pour le traitement d'infections par 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, DJ, 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, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, 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 (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (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)