Patent SG-11201806478P-A (SG)
Title: Efficient process for preparing cell-binding agent-cytotoxic agent conjugates
Inventor: LAI KATHARINE
IPC: C07K1/13
Filed: 2017-02-03
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization M1111101110101011111 HO 11111 0111011100111011101011100 111110 ill OEN 11 International Bureau ... .jd .... ....\" (10) International Publication Number (43) International Publication Date WO 2017/136623 Al 10 August 2017(10.08.2017) WIPO I PCT (51) International Patent Classification: AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, A61K 47/69 (2017.01) CO7K 1/13 (2006.01) 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, (21) International Application Number: HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, PCT/US2017/016344 KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, (22) International Filing Date: MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, 3 February 2017 (03.02.2017) 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, (25) Filing Language: English TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, (26) Publication Language: English ZA, ZM, ZW. (30) Priority Data: (84) Designated States (unless otherwise indicated, for every 62/292,018 5 February 2016 (05.02.2016) US kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, (71) Applicant: IMMUNOGEN, INC. [US/US]; 830 Winter TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, Street, Waltham, MA 02451 (US). TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, (72) Inventors: LAI, Katharine, C.; 6 Wychwood Drive, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, Littleton, MA 01460 (US). HERBST, Robert, W.; 31 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, Hollis Avenue, Braintree, MA 02184 (US) HILDER- GW, KM, ML, MR, NE, SN, TD, TG). BRAND, Scott, Alan; 19 Lawrence Terrace, Swampscott, MA 01907 (US). Published: Agents: LU, Yu McCarter & English, LLP, 265 — with international search report (Art. 21(3)) (74) et al.; Franklin Street, Boston, MA 02120 (US). — with sequence listing part of description (Rule 5.2(a)) (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, 1-1 M ei M 1-1 (54) Title: EFFICIENT PROCESS FOR PREPARING CELL-BINDING AGENT-CYTOTOXIC AGENT CONJUGATES I N (57) : The present invention provides a novel method for preparing a cell-binding agent cytotoxic agent conjugate. The 1-1 C method comprises the step of reacting a cell-binding agent with a cytotoxic agent or a cytotoxic agent-linker compound having a re- el active group capable of forming a covalent bond with the cell-binding agent at a pH between 4 to 9 in the presence of a buffer solu - 0 tion with high ionic strength, wherein the cell-binding agent comprises a lysine c-NH 2 group that forms a covalent bond with the cytotoxic agent or the cytotoxic agent-linker compound having an amine-reactive group. The cell-binding agent-cytotoxic agent con- jugates prepared according to the methods described herein are also included in the present invention.