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1. (WO2019064220) SYNTHESIS OF ICATIBANT
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Pub. No.: WO/2019/064220 International Application No.: PCT/IB2018/057498
Publication Date: 04.04.2019 International Filing Date: 27.09.2018
IPC:
C07K 7/06 (2006.01)
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
06
having 5 to 11 amino acids
Applicants:
BIOCON LIMITED [IN/IN]; 20th KM, Hosur Road, Electronic City post, Karnataka Bangalore 560 100, IN
Inventors:
RAMU, Vasanthakumar, Ganga; IN
PATIL, Nitin, Sopanrao; IN
PALLE, Venkata, Raghavendracharyulu; IN
YOGESHA; 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:
20174103431427.09.2017IN
Title (EN) SYNTHESIS OF ICATIBANT
(FR) SYNTHÈSE DE L'ICATIBANT
Abstract:
(EN) The present invention relates to the efficient solid-phase synthesis of Icatibant represented by Formula (I). The present invention relates to an efficient process for the preparation of Icatibant by sequential coupling employing solid phase approach. It involves sequential coupling of protected amino acids to prepare Icatibant. The present invention also involves the usage of inorganic salts during the coupling, wash with HOBt in DMF solution after Fmoc-deprotection step to ensure complete removal of piperidine and reactions are going for completion, and thus avoid addition/deletion sequences and also improve the process yield.
(FR) La présente invention concerne la synthèse efficace en phase solide de l'Icatibant représenté par la formule (I). La présente invention concerne un procédé efficace pour la préparation de l'Icatibant par couplage séquentiel utilisant une approche en phase solide. Il implique un couplage séquentiel d'acides aminés protégés pour préparer l'Icatibant. La présente invention implique également l'utilisation de sels inorganiques pendant le couplage, le lavage avec du HOBt dans une solution de DMF après l'étape de déprotection du Fmoc pour garantir l'élimination totale de la pipéridine et que les réactions soient complètes, et éviter ainsi des séquences d'addition/délétion et améliorer également le rendement du procédé.
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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)