Patent SG-11201909563V-A (SG)
Title: Quaternized nicotinamide adenine dinucleotide salvage pathway inhibitor conjugates
Inventor: NEUMANN CHRISTOPHER SCOTT
IPC: C07D401/12
Filed: 2018-04-27
Abstract: untreated - 0- eAC10-5 1 mg/kg - 0- cAC1 0-12 1 mg/kg -El - cAC10-26 1 mg/kg 10 20 days 30 40 800 --- 600 E '' a 400 E > 200 1-1 N GC O O 1-1 00 O O 1-1 (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 01 November 2018 (01.11.2018) WIPO I PCT IiiimmomiolollmonolooloiollmoionmommovoimIE (10) International Publication Number WO 2018/201087 Al (51) International Patent Classification: A61K 47/68 (2017.01) C07D 401/12 (2006.01) A61P 35/00 (2006.01) C07H 15/203 (2006.01) (21) International Application Number: PCT/US2018/030018 (22) International Filing Date: 27 April 2018 (27.04.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/490,733 27 April 2017 (27.04.2017) US 62/573,987 18 October 2017 (18.10.2017) US (71) Applicant: SEATTLE GENETICS, INC. [US/US]; 21823 30th Drive SE, Bothell, Washington 98021 (US). (72) Inventors: NEUMANN, Christopher Scott; 21823 30th Drive SE, Bothell, Washington 98021 (US). OLIVAS, Kathleen; 21823 30th Drive SE, Bothell, Washington 9021 (US). LYON, Robert; 21823 30th Drive SE, Bothell, Washington 98021 (US). WANG, Kung-Pern; 21823 30th Drive SE, Bothell, Washington 98021 (US). (74) Agent: CASTELLINO, Angelo et al.; SEATTLE GENETICS, INC., 21823 30TH Drive SE, Bothell, Wash- ington 98021 (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). (54) Title: QUATERNIZED NICOTINAMIDE ADENINE DINUCLEOTIDE SALVAGE PATHWAY INHIBITOR CONJUGATES L540cy xenog raft model FIGURE 1 (57) : Compounds and compositions are disclosed in which a NAMPT Drug Unit is conjugated to a targeting Ligand Unit through quaternization by a Linker Unit from which a NAMPT inhibitor compound or derivative thereof is released at the targeted site of action. Methods for treating diseases characterized by the targeted abnormal cells, such as those of cancer or an autoimmune disease, using the compounds and compositions of the invention are also disclosed. [Continued on next page] WO 2018/201087 Al MIDEDIMOMMIDEFIEHNOIRMIIMEHMEMOIMIE Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(H)) 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))