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1. (WO2017032726) LNA-G PROCESS
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Pub. No.: WO/2017/032726 International Application No.: PCT/EP2016/069765
Publication Date: 02.03.2017 International Filing Date: 22.08.2016
IPC:
C12N 15/11 (2006.01) ,C07D 473/18 (2006.01)
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
N
MICRO-ORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICRO-ORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
15
Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
09
Recombinant DNA-technology
11
DNA or RNA fragments; Modified forms thereof
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
02
with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6
18
one oxygen and one nitrogen atom, e.g. guanine
Applicants:
ROCHE INNOVATION CENTER COPENHAGEN A/S [DK/DK]; Fremtidsvej 3 2970 Hørsholm, DK
Inventors:
HANSEN, Dennis Jul; DK
HOERNSCHEMEYER, Joerg; CH
RAVN, Jacob; DK
ROSENBOHM, Christoph; DK
Agent:
TURNER, Mark; CH
Priority Data:
15182172.524.08.2015EP
Title (EN) LNA-G PROCESS
(FR) PROCÉDÉ LNA-G
Abstract:
(EN) Recent advancements in LNA oligonucleotides include the use of amine linkers to link an LNA antisense oligonucleotide to a conjugate group. For example please see WO2014/118267. The present invention originates from the identification of a problem when de-protecting LNA oligonucleotides which comprise an aliphatic amine group and DMF protected LNA G nucleoside, which results in the production of a +28 Da impurity. This problem is solved by using acyl protection groups on the exocyclic nitrogen of the LNA-G residue, rather than the standard DMF protection group.
(FR) Des avancées récentes concernant les oligonucléotides LNA se rapportent à l’utilisation de lieurs aminés pour la liaison d’un oligonucléotide LNA antisens à un groupe conjugué. Des exemples sont présentés dans le brevet WO2014/118267. La présente invention provient de l’identification d’un problème survenant lors de la déprotection des oligonucléotides LNA qui comprennent un groupe amine aliphatique et un nucléoside LNA G protégé au DMF, qui résulte en la production d’une impureté de plus de 28 Da. Ce problème est résolu en utilisant des groupes de protection acyle sur l’azote exocyclique du résidu LNA-G, plutôt que le groupe de protection DMF standard.
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, 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, KN, KP, KR, 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)