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1. (WO2019027368) METHOD OF PREPARING STAPLED PEPTIDES
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Pub. No.: WO/2019/027368 International Application No.: PCT/SG2018/050388
Publication Date: 07.02.2019 International Filing Date: 31.07.2018
IPC:
C07K 1/04 (2006.01) ,C07K 7/08 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
1
General processes for the preparation of peptides
04
on carriers
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
7
Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
04
Linear peptides containing only normal peptide links
08
having 12 to 20 amino acids
Applicants:
AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH [SG/SG]; 1 Fusionopolis Way #20-10 Connexis North Tower, Singapore 138632, SG
Inventors:
YUEN, Tsz Ying; SG
JOHANNES, Charles William; SG
HILINSKI, Gerard; US
Agent:
SPRUSON & FERGUSON (ASIA) PTE LTD; P.O. Box 1531, Robinson Road Post Office Singapore 903031, SG
Priority Data:
10201706224X31.07.2017SG
Title (EN) METHOD OF PREPARING STAPLED PEPTIDES
(FR) PROCÉDÉ DE PRÉPARATION DE PEPTIDES AGRAFÉS
Abstract:
(EN) Described herein is an operationally simple, one-pot solid-supported preparation of saturated stapled peptides. Following completion of ruthenium-catalysed metathesis, solid-phase transfer hydrogenation was achieved using triethylhydrosilane at elevated temperatures. The utility of the method has been demonstrated on 14-and 16-mer peptides to yield the corresponding cyclic a- helix stabilised stapled peptides.
(FR) L'invention concerne une préparation à support solide, monotope, à fonctionnement simple de peptides agrafés saturés. Après l'achèvement de la métathèse catalysée par du ruthénium, une hydrogénation par transfert en phase solide a été réalisée à l'aide de triéthylhydrosilane à des températures élevées. Le procédé selon la présente invention s'avère utile sur des peptides 14 et 16-mer pour produire les peptides agrafés stabilisés cycliques en hélice a correspondants.
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)