Patent SG-11201809830W-A (SG)
Title: Selective reduction of cysteine-engineered antibodies
Inventor: COUMANS RUDY GERARDUS ELISABETH
IPC: A61K47/50
Filed: 2017-02-13
Abstract: OMeVii), P SO H (II) (I) (V) S031 - 1 (vi) W O 20 17 / 137 6 28 Al (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2017/137628 Al 17 August 2017 (17.08.2017) WIPO I PCT (51) International Patent Classification: A61K 47/50 (2017.01) (21) International Application Number: PCT/EP2017/053157 (22) International Filing Date: 13 February 2017 (13.02.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 16155481.1 12 February 2016 (12.02.2016) EP 16206761.5 23 December 2016 (23.12.2016) EP (71) Applicant: SYNTHON BIOPHARMACEUTICALS B.V. [NL/NL]; Microweg 22, 6545CM Nijmegen (NL). (72) Inventors: COUMANS, Rudy Gerardus Elisabeth; Syn- thon Biopharmaceuticals B.V., Microweg 22, 6545 CM Nijmegen (NL). SPIJKER, Henri Johannes; Synthon Biopharmaceuticals B.V., Microweg 22, 6545 CM Nijme- gen (NL). (74) Agent: VISSCHER, Inge; P.O. BOX 7071, 6503 GN Nijmegen (NL). (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, 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. (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). Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii)) 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)) (54) Title: SELECTIVE REDUCTION OF CYSTEINE-ENGINEERED ANTIBODIES (57) : The present invention relates to a process for the selective reduction of cysteine- engineered antibodies comprising reacting an antibody comprising one or more engineered cysteines at positions selected from HC40, HC41,HC42, HC89, HC152, HC153, HC155, HC171, LC40, LC41, LC165, and LC168 with a compound according to formula (I), (II), (III), (IV), (V), (VI) or (VII): (I) (II) (III) (IV) (V) (VI) (VII), and to a process for the preparation of antibody conjugates, including antibody-drug conjug - ates (ADCs). 1111111111111101110111111111110101111101110111011111111111110111110111111111110111111