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1. (WO2018104922) SYNTHESIS OF LIRAGLUTIDE
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Pub. No.: WO/2018/104922 International Application No.: PCT/IB2017/057763
Publication Date: 14.06.2018 International Filing Date: 09.12.2017
IPC:
C07K 4/00 (2006.01) ,C07K 1/10 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
4
Peptides having up to 20 amino acids in an undefined or only partially defined sequence; Derivatives thereof
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
1
General processes for the preparation of peptides
10
using coupling agents
Applicants:
BIOCON LIMITED [IN/IN]; 20th KM, Hosur Road, Electronic City, Karnataka, Bangalore 560 100, IN
Inventors:
GANGA, Ramu, Vasanthakumar; IN
PATIL, Nitin; IN
CHARYULU, Palle Venkata, Raghavendra; IN
JASMINE, Castelino, Roopa; IN
MACHANI, Rambabu; IN
SUVARNA, Deepa, Shankar; IN
Agent:
MAJUMDAR, Subhatosh; IN
GANGULI, Dr., Sanchita; IN
SEN, Abhishek; IN
VENKATESH, Mythili; IN
MAJUMDAR, Amrita; IN
KUNDU, Subarna; IN
CHAUBEY, Priyanka; IN
Priority Data:
20164104225210.12.2016IN
Title (EN) SYNTHESIS OF LIRAGLUTIDE
(FR) SYNTHÈSE DE LIRAGLUTIDE
Abstract:
(EN) The present invention relates to the efficient solid-phase synthesis of liraglutide represented by Formula-I. The present invention relates to an efficient process for the preparation of liraglutide by sequential coupling employing solid phase approach. It involves sequential coupling of protected amino acids to prepare backbone of liraglutide and upon completion of linear sequence, synthesis was extended from lysine side chain by adding γ-glutamic acid and palmitic acid, followed by removal of protective groups, cleavage of the peptide from solid support and purification of crude liraglutide obtained. The present invention also involves the usage of inorganic salts during the coupling, wash with HOBt in DMF solution after Fmoc-deprotection step to suppress the aggregation of peptides and ensure reactions are going for completion, and thus avoid deletion sequences and improve the process yield.
(FR) La présente invention concerne la synthèse efficace en phase solide de liraglutide représentée par la formule I. La présente invention concerne également un procédé efficace pour la préparation de liraglutide par couplage séquentiel utilisant une approche en phase solide. L'invention implique un couplage séquentiel d'acides aminés protégés pour préparer le squelette de liraglutide et lors de l'achèvement de la séquence linéaire, la synthèse a été étendue à partir de la chaîne latérale de la lysine par ajout d'acide gamma-glutamique et de l'acide palmitique, suivi par l'élimination de groupes protecteurs, le clivage du peptide à partir du support solide et la purification du liraglutide brut obtenu. La présente invention concerne également l'utilisation de sels inorganiques pendant le couplage, le lavage avec HOBt dans une solution DMF après l'étape de déprotection Fmoc pour supprimer l'agrégation de peptides et assurer l'achèvement des réactions, évitant ainsi des séquences de suppression, tout en améliorant le rendement du processus.
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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)