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1. (WO2019063634) RADIOLABELED DARAPLADIB AND ANALOGS THEREOF AND THEIR USE AS IMAGING COMPOUNDS
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Pub. No.: WO/2019/063634 International Application No.: PCT/EP2018/076163
Publication Date: 04.04.2019 International Filing Date: 26.09.2018
IPC:
C07D 239/70 (2006.01) ,A61K 51/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70
condensed with carbocyclic rings or ring systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51
Preparations containing radioactive substances for use in therapy or testing in vivo
02
characterised by the carrier
04
Organic compounds
Applicants:
INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE) [FR/FR]; 101 Rue de Tolbiac 75013 PARIS, FR
UNIVERSITE DE LA REUNION [FR/FR]; 15 Avenue René Cassin 97490 SAINT DENIS, FR
Inventors:
MEILHAC, Olivier; FR
JESTIN, Emmanuelle; FR
GUIBBAL, Florian; FR
BENARD, Sébastien; FR
Agent:
CABINET PLASSERAUD; 66 rue de la Chaussée d'Antin 75440 PARIS CEDEX 09, FR
Priority Data:
17306272.026.09.2017EP
Title (EN) RADIOLABELED DARAPLADIB AND ANALOGS THEREOF AND THEIR USE AS IMAGING COMPOUNDS
(FR) DARAPLADIB RADIOMARQUÉ, SES ANALOGUES ET LEUR UTILISATION EN TANT QUE COMPOSÉS D'IMAGERIE
Abstract:
(EN) The present inventors have developed new radiolabeled Darapladib and analogs thereof which can be used for the specific detection of vulnerable atherosclerotic plaques by targeting lipoprotein-associated phospholipase A2 (Lp-PLA2) which is a biomarker of choice concerning inflammation and atherosclerosis progression. Thus, the present invention relates to radiolabeled Darapladib and analogs thereof and their use as imaging compounds.
(FR) La présente invention se rapporte à la mise au point de nouveaux darapladib radiomarqués et des analogues de ceux-ci, qui peuvent être utilisés pour la détection spécifique de plaques d'athérosclérose vulnérables en ciblant la phospholipase A2 associée aux lipoprotéines (Lp-PLA2) qui est un biomarqueur de choix concernant l'inflammation et la progression de l'athérosclérose. La présente invention concerne un darapladib radiomarqué et des analogues de celui-ci ainsi que leur utilisation en tant que composés d'imagerie.
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)