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1. (WO2017091568) ADDITIVE SYSTEMS FOR USE IN PROTEIN PEGYLATION
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/091568 International Application No.: PCT/US2016/063313
Publication Date: 01.06.2017 International Filing Date: 22.11.2016
IPC:
C07K 1/107 (2006.01) ,A61K 47/60 (2017.01) ,C07K 14/50 (2006.01) ,C07K 14/64 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
1
General processes for the preparation of peptides
107
by chemical modification of precursor peptides
[IPC code unknown for A61K 47/60]
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
14
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435
from animals; from humans
475
Growth factors; Growth regulators
50
Fibroblast growth factor (FGF)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
14
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435
from animals; from humans
575
Hormones
64
Relaxins
Applicants:
BRISTOL-MYERS SQUIBB COMPANY [US/US]; Route 206 and Province Line Road Princeton, New Jersey 08543, US
Inventors:
HICKEY, Matthew R.; US
RAMIREZ, Antonio; US
Agent:
LIU, Hong; US
CLAUSS, Isabelle; US
D'AMICO, Stephen C.; US
DELAUNEY, Ashton; US
FARQUHARSON-TORRES, Serena; US
FRANK, Eve; US
GOLIAN, Paul D.; US
GREENBLATT, Gary D.; US
GUO, Z. Angela; US
HADAD, Henry; US
JACOBSEN, Barry H.; US
KORSEN, Elliott; US
LU, Yong; US
PARLET, Nickki L.; US
VANATTEN, Mary K.; US
VOM WEGE, Julia; US
WALSH, Brian J.; US
EPPERSON, James; US
MINGO, Pamela A.; US
VOLLES, Warren; US
BELLOMY, Gregory R.; US
CHAO, Yuan; US
HAI, Bing; US
Priority Data:
62/258,64423.11.2015US
Title (EN) ADDITIVE SYSTEMS FOR USE IN PROTEIN PEGYLATION
(FR) SYSTÈMES D'ADDITIFS POUR PÉGYLATION DE PROTÉINES
Abstract:
(EN) The present disclosure provides an additive system for use in protein PEGylation. The additive system includes p-aminobenzoic hydrazide used either alone or in combination with aromatic amines, such as 3,5-diaminobenzoic acid, or with ammonium salts such as ammonium chloride or ammonium acetate. The disclosed additive combination provides several benefits including increased reaction rates, higher yields and reduction in the aminoxy-PEG equivalents required to complete the conjugation reaction. Typical reactions can be run by combining the additive or additive system with a solution of a protein and aminoxy-PEG reagent. The solution is adjusted to pH 4 and held at 20-25 °C without stirring until completion, typically within 24 hours.
(FR) L'invention concerne un système d'additifs pour la pégylation de protéines. Le système d'additifs comprend de l'hydrazide aminobenzoïque utilisé seul ou en combinaison avec des amines aromatiques, tels que l'acide 3,5-diaminobenzoïque, ou avec des sels d'ammonium tels que le chlorure d'ammonium ou l'acétate d'ammonium. Le mélange d'additifs fournit plusieurs avantages incluant l'accroissement des vitesses de réaction, des rendements supérieurs et une diminution des équivalents aminoxy-PEG nécessaires à l'achèvement de la réaction de conjugaison. Les réactions habituelles peuvent être réalisées par combinaison de l'additif ou du système d'additifs avec une solution d'une protéine et d'un réactif aminoxy-PEG. La solution est ajustée au pH 4 et maintenue à 20-25 °C sans agitation jusqu'à la fin, habituellement au bout de 24 heures.
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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, JP, KE, KG, 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 Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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)
Also published as:
KR1020180081610CN108350025EP3380487