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1. (WO2019011829) IMPROVED PROCESS FOR PREPARING IMETELSTAT
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Pub. No.: WO/2019/011829 International Application No.: PCT/EP2018/068485
Publication Date: 17.01.2019 International Filing Date: 09.07.2018
IPC:
C07H 1/00 (2006.01) ,C07H 21/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
1
Processes for the preparation of sugar derivatives
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
21
Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
04
with deoxyribosyl as saccharide radical
Applicants:
GERON CORPORATION; 149 Commonwealth Drive Menlo Park, CA 94025, US
Inventors:
MUSLEHIDDINOGLU, Jale; BE
GALA, Dinesh; BE
ALBANEZE-WALKER, Jennifer, Elizabeth; BE
Agent:
BASSIL, Nicholas Charles; GB
Priority Data:
17180426.310.07.2017EP
Title (EN) IMPROVED PROCESS FOR PREPARING IMETELSTAT
(FR) PROCÉDÉ AMÉLIORÉ POUR PRÉPARER DE L'IMETELSTAT
Abstract:
(EN) The present invention relates to a process for preparing the telomerase inhibitor imetelstat using a 3 steps per cycle solid- phase support bound process comprising the steps of deprotection of the 3'-amino group of the support-bound oligonucleotide, coupling with a 5'-phosphoramidite, and sulfurization with an acyl disulfide, characterized by the absence of an additional capping step in each cycle that is used to prevent unreacted 3'-amino oligonucleotide groups from reacting during subsequent cycles. Imetelstat has formula below.
(FR) La présente invention concerne un procédé de préparation d'un inhibiteur de télomérase, l'imetelstat, à l'aide d'un procédé de liaison de support en phase solide en 3 étapes par cycle comprenant les étapes de déprotection du groupe 3'-amino de l'oligonucléotide lié à un support, de couplage avec un 5'-phosphoramidite, et de sulfuration avec un disulfure d'acyle, l'invention étant caractérisée par l'absence d'une étape supplémentaire de coiffage dans chaque cycle qui est utilisée pour empêcher des groupes 3'-amino-oligonucléotide n'ayant pas réagi de réagir pendant des cycles ultérieurs. L'imetelstat a la formule ci-dessous.
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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)