Patent SG-11201407597X-A (SG)
Title: Nucleophilic catalysts for oxime linkage
Inventor: SIEKMANN JUERGEN
IPC: A61K47/48
Filed: 2013-05-16
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 21 November 2013 (21.11.2013) WIPOIPCT (10) International Publication Number WO 2013/173543 A1 (51) International Patent Classification: A61K 47/48 ( 2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/US2013/041280 16 May 2013 (16.05.2013) English English (30) Priority Data: 61/647,814 13/488,043 16 May 2012 (16.05.2012) US 4 June 2012 (04.06.2012) US (71) Applicants: BAXTER INTERNATIONAL INC. [US/US]; One Baxter Parkway, Deerfield, IL 60015 (US). BAXTER HEALTHCARE SA [CH/CH]; Thurgauer- strasse 130, CH-8152 Glattpark (Opfikon) (CH). (72) Inventors: SIEKMANN, Juergen; Gerasdorfer Strasse 153/209, A-1210 Vienna (AT). HAIDER, Stefan; Moz- artstrasse 2, A-3385 Prinzersdorf (AT). ROTTENSTEIN- ER, Hanspeter; Haidgasse 10/17, A-1020 Vienna (AT). TURECEK, Peter; Weidling, Hauptstrasse 59g, A-3400 Klosterneuburg (AT). (74) Agents: BRUSCA, Eric, M. et al.; Marshall, Gerstein & Borun LLP, 233 S. Wacker Drive, 6300 Willis Tower, Chicago, IL 60606-6357 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available)'. 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, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, 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, 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. (84) Designated States (unless otherwise indicated, for every kind of regional protection available)'. ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (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), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: — as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(H)) — as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) Published: — with international search report (Art. 21(3)) — with sequence listing part of description (Rule 5.2(a)) •t m i> i-H cn i-H o CJ o & (54) Title: NUCLEOPHILIC CATALYSTS FOR OXIME LINKAGE (57) Abstract: The invention relates to materials and methods of conjugating water soluble polymer a to an oxidized carbohydrate moiety of a therapeutic protein comprising contacting the oxidized carbohydrate moiety with an activated water soluble polymer un­ der conditions that allow conjugation. More specifically, the present invention relates to the aforementioned materials and methods wherein the water soluble polymer contains an active aminooxy group and wherein an oxime or hydrazone linkage is formed between the oxidized carbohydrate moiety and the active aminooxy group on the water soluble polymer, and wherein the conjuga - tion carried is out in the presence of nucleophilic a catalyst.