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1. (WO2018162670) 2- OR 3-IMIDAZOLINES AS CARBAPENEMASES INHIBITORS
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Pub. No.: WO/2018/162670 International Application No.: PCT/EP2018/055820
Publication Date: 13.09.2018 International Filing Date: 08.03.2018
IPC:
C07D 233/20 (2006.01) ,A61K 31/4164 (2006.01) ,A61P 31/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
233
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
04
having one double bond between ring members or between a ring member and a non-ring member
20
with substituted hydrocarbon radicals, directly attached to ring carbon atoms
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4164
1,3-Diazoles
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04
Antibacterial agents
Applicants:
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) [FR/FR]; 3, rue Michel Ange 75016 PARIS, FR
UNIVERSITE PARIS-SUD [FR/FR]; 15, rue Georges Clémenceau 91400 ORSAY, FR
ASSISTANCE PUBLIQUE - HOPITAUX DE PARIS [FR/FR]; 3, avenue Victoria 75004 PARIS, FR
Inventors:
CARIOU, Kevin; FR
DODD, Robert H.; FR
ROMERO, Eugénie; FR
BENCHEKROUN, Mohamed; GB
IORGA, Bogdan; FR
NAAS, Thierry; FR
OUESLATI, Saoussen; FR
Agent:
CABINET LAVOIX; 2 Place d'Estienne d'Orves 75441 Paris Cedex 09, FR
Priority Data:
17305257.209.03.2017EP
Title (EN) 2- OR 3-IMIDAZOLINES AS CARBAPENEMASES INHIBITORS
(FR) 2- OU 3-IMIDAZOLINES UTILISÉES EN TANT QU'INHIBITEURS DE CARBAPÉNÉMASES
Abstract:
(EN) The present application relates tonovel 3-imidazolinesof formula (I')and (I)below: (I') (I) Wherein Ar1, Ar2, Ar3, and R1 to R6 are as defined in the claims. The 3-imidazolines of the invention are useful in antibiotic therapies, in particular as inhibitors of carbapenemases. They are also useful as antibiotics themselves. The present invention also concerns a method for preparing more specifically the 3-imidazolines of formula (I). The present invention further relates to conjugates of said compounds with known antibiotics.
(FR) La présente invention concerne de nouveaux 3-imidazolines de formule (I') et (I) ci-dessous : (I') (I) dans lesquelles Ar1, Ar2, Ar3 et R1 à R6 sont tels que définis dans les revendications. Les 3-imidazolines de l'invention sont utiles dans des thérapies antibiotiques, en particulier en tant qu'inhibiteurs de carbapénémases. Les 3-imidazolines de l'invention sont également utiles en tant qu'antibiotiques eux-mêmes. La présente invention concerne également un procédé de préparation de manière particulière, des 3-imidazolines de formule (I). La présente invention concerne en outre des conjugués desdits composés avec des antibiotiques connus.
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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, JO, 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)