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Pub. No.: WO/2017/176216 International Application No.: PCT/SG2017/050198
Publication Date: 12.10.2017 International Filing Date: 06.04.2017
C09K 11/06 (2006.01) ,B82Y 40/00 (2011.01) ,G01N 33/52 (2006.01) ,A61K 49/18 (2006.01)
Applicants: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH[SG/SG]; 1 Fusionopolis Way, #20-10 Connexis North Tower, Singapore 138632, SG
NATIONAL UNIVERSITY OF SINGAPORE[SG/SG]; 21 Lower Kent Ridge Road, Singapore 119077, SG
Inventors: NG, Lai Guan; SG
LIU, Bin; SG
RENIA, Laurent; SG
LI, Jackson Liang Yao; SG
FENG, Guangxue; SG
Agent: SPRUSON & FERGUSON (ASIA) PTE LTD; P.O. Box 1531 Robinson Road Post Office Singapore 903031, SG
Priority Data:
Abstract: front page image
(EN) This invention relates to a nanoparticle comprising a fluorophore, an amphiphilic copolymer and a cyclic chelating agent, wherein the fluorophore and amphiphilic copolymer form a nanodot core, and wherein the cyclic chelating agent is conjugated onto the nanodot core. In particular, the fluorophore is selected from the group consisting of 2,3-bis[4- (diphenylamino)phenyl]fumaronitrile (TPAFN), 2,3-bis(4-(phenyl(4-(1,2,2-triphenylvinyl)phenyl)amino)phenyl) fumaronitrile (TPETPAFN), tetraphenylethylene (TPE); the amphiphilic copolymer is selected from 1,2-distearoyl-sn- glycero-3-phosphoethanolamine-N-[amino(polyethylene glycol)-2000], 1,2-distearoyl-sn-glycero-3- phosphoethanolamine-N-[maleimide(polyethylene glycol)-2000]; and the cyclic chelating agent is 2,2',2"-(10-(2-((2,5- dioxopyrrolidin-1 -yl)oxy)-2-oxoethyl)-1,4,7, 10-tetraazacyclododecane-1,4,7-triyl)triacetic acid. The invention also relates to a method of preparing such a nanoparticle, the use of such a nanoparticle for vascular imaging and a method for in vivo imaging of blood vessels using such nanoparticles.
(FR) La présente invention concerne une nanoparticule comprenant un fluorophore, un copolymère amphiphile et un agent chélateur cyclique, le fluorophore et le copolymère amphiphile formant un noyau de nanopoint, et l'agent de chélation cyclique étant conjugué sur le noyau de nanopoint. En particulier, le fluorophore est choisi dans le groupe constitué des 2,3-bis[4- (diphénylamino)phényl]fumaronitrile (TPAFN), 2,3-bis(4-(phényl(4-(1,2,2-triphénylvinyl)phényl)amino)phényl)fumaronitrile (TPETPAFN), tétraphényléthylène (TPE); le copolymère amphiphile est choisi parmi les 1,2-distéaroyl-sn-glycéro-3-phosphoéthanolamine-N-[amino(polyéthylèneglycol)-2000], 1,2-distéaroyl-sn-glycéro-3-phosphoéthanolamine-N-[maléimide(polyéthylèneglycol)-2000] ; et l’agent chélateur cyclique est l’acide 2,2',2"-(10-(2-((2,5-dioxopyrrolidin-1-yl)oxy)-2-oxoéthyl)-1,4,7,10-tétraazacyclododécane-1,4,7-triyl)triacétique. L'invention concerne en outre un procédé de préparation d'une telle nanoparticule, l'utilisation d'une telle nanoparticule pour l'imagerie vasculaire et un procédé d'imagerie in vivo de vaisseaux sanguins utilisant de telles nanoparticules.
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)