Patent SG-11201906414V-A (SG)
Title: Calicheamicin derivatives and antibody drug conjugates thereof
Inventor: AHMAD OMAR KHALED
IPC: C07H15/00
Filed: 2018-01-10
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 02 August 2018 (02.08.2018) WI P0 I P C T oil1 oil muoin Imo oimIE (10) International Publication Number WO 2018/138591 Al (51) International Patent Classification: C07H 15/00 (2006.01) A61K 47/64 (2017.01) (21) International Application Number: PCT/IB2018/050153 (22) International Filing Date: 10 January 2018 (10.01.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/449,839 24 January 2017 (24.01.2017) US (71) Applicant: PFIZER INC. [US/US]; 235 East 42nd Street, New York, New York 10017 (US). (72) Inventors: AHMAD, Omar Khaled; 200 Exchange Street, Unit 512, Providence, Rhode Island 02903 (US). BROWN, Stephen Paul; 19 Walter Fish Avenue, Mystic, Connecti- cut 06355 (US). DIRICO, Kenneth John; 8 Melanie Lane, Gales Ferry, Connecticut 06335 (US). DUSHIN, Russell; 15 Jericho Drive, Old Lyme, Connecticut 06371 (US). FILZEN, Gary Frederick; 125 Markley Road, Sch- wenksville, Pennsylvania 19473 (US). PUTHENVEETIL, Sujiet; 10 Catherine Avenue, Franklin, Massachusetts 02038 (US). STROP, Pavel; 461 West 25th Avenue, San Mateo, California 94403 (US). SUBRAMANYAM, Chakrapani; 314 Great Pond Road, South Glastonbury, Connecticut 06073 (US). TUMEY, Lawrence N.; 37 William Street, Pawcatuck, Connecticut 06379 (US). (74) Agent: WALDRON, Roy F.; PFIZER INC., 235 East 42nd Street, MS 235/9/S20, New York, NY 10017 (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, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, 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)) before the expiration of the time limit for amending the claims and to be republished in the event of receipt of amendments (Rule 48.2(h)) with sequence listing part of description (Rule 5.2(a)) 1-1 1-1 GC 1-1 1-1 0> (57) : The present invention is directed to novel calicheamicin derivatives useful as payloads in antibody-drug-conjugates \" (ADC's), and to payload-linker compounds and ADC compounds comprising the same; to pharmaceutical compositions comprising the 0 same and to methods for using the same to treat pathological conditions such as cancer. (54) Title: CALICHEAMICIN DERIVATIVES AND ANTIBODY DRUG CONJUGATES THEREOF