Patent SG-11201807537R-A (SG)
Title: Process for the preparation of an antibody-rifamycin conjugate
Inventor: BACHMANN STEPHAN
IPC: C07D498/04
Filed: 2017-03-03
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization IIIM141101110101011111 HO 11111011101111101010 111111111100111110 1111 III N International Bureau ... .jd .... ..or::,„, (10) International Publication Number (43) International Publication Date WO 2017/152083 Al 8 September 2017 (08.09.2017) WIP0 I PCT (51) International Patent Classification: (72) Inventors: BACHMANN, Stephan; c/o F. Hoffmann-La C07D 498/04 (2006.01) CO7C 215/78 (2006.01) Roche AG, Grenzacherstrasse 124, 4070 Basel (CH). FANTASIA, Serena Maria; c/o F. Hoffmann-La Roche (21) International Application Number: AG, Grenzacherstrasse 124, 4070 Basel (CH). JANSEN, PCT/US2017/020711 Michael; c/o F. Hoffmann-La Roche AG, Grenzacher- (22) International Filing Date: strasse 124, 4070 Basel (CH). KOENIG, Stefan; c/o Gen- 3 March 2017 (03.03.2017) entech, Inc., 1 DNA Way, South San Francisco, California 94080 (US). LINGHU, Xin; c/o Genentech, Inc., 1 DNA (25) Filing Language: English Way, South San Francisco, California 94080 (US). RI- (26) Publication Language: English ETH, Sebastian; c/o F. Hoffmann-La Roche AG, Gren- zacherstrasse 124, 4070 Basel (CH). SEGRAVES, Nath- (30) Priority Data: aniel L.; c/o Genentech, Inc., 1 DNA Way, South San 62/303,556 4 March 2016 (04.03.2016) US Francisco, California 94080 (US). ZOGG, Andreas; c/o F. (71) Applicant (for all designated States except AL, AT, BE, Hoffmann-La Roche AG, Grenzacherstrasse 124, 4070 BG, CH, CN, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, Basel (CH). HR, HU, IE, IN, IS, IT, LT, LU, LV, MC, MK, MT, NL, (74) Agents: ANDRUS, Alex et al.; Genentech, Inc., 1 DNA NO, PL, PT, RO, RS, SE, SI, SK, SM, TR): GENENTECH, Way, MS 49, South San Francisco, California 94080 (US). INC. [US/US]; 1 DNA Way, South San Francisco, Califor- nia 94080 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, (71) Applicant (for AL, AT, BE, BG, CH, CN, CY, CZ, DE, DK, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, EE, ES, FI, FR, GB, GR, HR, HU, IE, IN, IS, IT, LT, LU, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, = LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, SM, TR only): F. HOFFMANN-LA ROCHE AG HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, — [CH/CH]; Grenzacherstrasse 124, 4070 Basel (CH). KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, [Continued on next page] (54) Title: PROCESS FOR THE PREPARATION OF AN ANTIBODY-RIFAMYCIN CONJUGATE (57) : Processes are described for the preparation of = F-benzoxazinorifamycin I: and intermediates for conjugation with an antibody. — ' = = = Ulf. (.1 .o) — s Batch-reactor . \"I = nah Oxidant 02, I Rmn sv etc benroquinone, RIKA , . n g .1 1-1 0 0— o en GC HO ° Op (;,0,p N 0 0 0 Ho,, HN 0 kr) Il IN Il 0 N O WO 2017/152083 Al MIDEDIMOMOIDEIR0101311101011MMODEVOIMIE MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, 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. GN, GQ, GW, KM, ML, MR, NE, SN, TD, Published: TG). (84) Designated States (unless otherwise indicated, for every with international search report (Art. 21(3)) 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, — before the expiration of the time limit for claims and to be republished in the event amendments (Rule 48.2(h)) amending of receipt the of