Patent SG-11201804666Q-A (SG)
Title: Factor viii with extended half-life and reduced ligand-binding properties
Inventor: TURECEK PETER
IPC: C07K14/755
Filed: 2016-12-05
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau 1111111111111111111111111111111111111111111111111111111111111111111111111R111111111111111 (10) International Publication Number WO 2017/096383 Al WIPO I PCT (43) International Publication Date 8 June 2017 (08.06.2017) (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, 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. (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, ST, 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, KM, ML, MR, NE, SN, TD, TG). Published: with international search report (Art 21(3)) (51) International Patent Classification: C07K 14/755 (2006.01) A61K 47/61 (2017.01) (21) International Application Number: PCT/US2016/064979 (22) International Filing Date: 5 December 2016 (05.12.2016) English English (25) Filing Language: (26) Publication Language: (30) Priority Data: 62/262,674 3 December 2015 (03.12.2015) US (71) Applicants: BAXALTA INCORPORATED [US/US]; 1200 Lakeside Drive, Bannockburn, IL 60015 (US). BAX- ALTA GMBH [CH/CH]; Thurgauerstrasse 130, 8152 Glattpark (Opfikon) (CH). (72) Inventors; and (71) Applicants : TURECEK, Peter [AT/AT]; Hauptstrasse 59g, 3400 Klosterneuburn-Weidling (AT). SCHRENK, Gerald [AT/AT]; Flachsweg 12, 1220 Vienna (AT). SIEKMANN, Juergen [AT/AT]; Gerasdorfer Strasse 153/209, 1210 Vienna (AT). (74) Agents: MANN, Jeffry, S. et al.; Morgan, Lewis & Bocki- us LLP, One Market, Spear Street Tower, San Francisco, CA 94105 (US). (54) Title: FACTOR VIII WITH EXTENDED HALF-LIFE AND REDUCED LIGAND-BINDING PROPERTIES 180 rFVIII, n=4 160 PSA-rF1/111 preclinical BDS, n=3 PSA-rFVIII clinical phase 1 BDS, n=3 PSA-rFVIII preclinical FDP, n=3 —j— PsA-rFv111 clinical phase 1 FDP, n=1 140 120 100 80 60 40 20 0 W O 20 17 /096383 Al 200 400 600 800 1000 1200 Chip-immobilized VWF (RU) FIGURE 1 (57) : The invention relates to materials and methods of conjugating a water soluble polymer 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 a modified, recombinant Factor VIII (FVIII) with extended half-life and reduced ligand-binding properties.