Patent SG-11201804268R-A (SG)
Title: Conjugates of quaternized tubulysin compounds
Inventor: BURKE PATRICK J
IPC: C07K19/00
Filed: 2016-12-02
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, -, Organization 111111110111101110101011111010111111111011101101110110111011111101111011111 International Bureau .. .... ..Yejd (10) International Publication Number (43) International Publication Date ..... ...:;.1 WO 2017/096311 Al 8 June 2017 (08.06.2017) W I P0 I P CT (51) International Patent Classification: (74) Agents: CASTELLINO, Angelo et al.; Seattle Genetics, A61K 38/04 (2006.01) CO7K 19/00 (2006.01) Inc., 21823 30TH Drive SE, Bothell, Washington 98021 A61K 38/06 (2006.01) CO7K 5/078 (2006.01) (US). A61K 38/07 (2006.01) C07K 5/10 (2006.01) CO7K 5/02 (2006.01) (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, (21) International Application Number: AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, PCT/US2016/064834 BZ, DO, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DZ, EC, EE, EG, ES, FL GB, GD, GE, GH, GM, GT, (22) International Filing Date: HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, 2 December 2016 (02.12.2016) KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, (25) Filing Language: English MG, OM, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, (26) Publication Language: English SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, (30) Priority Data: TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, 62/263,578 4 December 2015 (04.12.2015) US ZW. 62/263,587 4 December 2015 (04.12.2015) US (84) Designated States (unless otherwise indicated, for every 62/309,448 16 March 2016 (16.03.2016) US kind of regional protection available): ARIPO (BW, GH, 62/309,462 17 March 2016 (17.03.2016) US GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, (71) Applicant: SEATTLE GENETICS, INC. [US/US]; TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, 21823 30th Drive SE, Bothell, Washington 98021 (US). TJ, DK, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, (72) Inventors: BURKE, Patrick J.; 21823 30th Drive SE, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, Bothell, Washington 98021 (US). COURTER, Joel; SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, 21823 30th Drive SE, Bothell, Washington 98021 (US). GW, KM, ML, MR, NE, SN, TD, TG). [Continued on next page] (54) Title: CONJUGATES OF QUATERNIZED TUBULYSIN COMPOUNDS L540cy HL xenograft model - ADCs loaded at 4-drugs/mAb, single dose ip -w untreated ^ 1000 -4,- cAC10-15, 0.6 mg/kg ' ' ' E -e- cAC10-15, 2 mg/kg • g- 800 1/5 cures -40- cAC10-82, 0.6 mg/kg E -is- cAC 10-57, 0.6 mg/kg ' 600 0:7 > * 8 400 E = c 200 E ,. 21 r, ct s 1-1 0 20 40 60 80 .4 days post implant 1-1 1-1 M c:r © Figure 1 IN 1-1 (57) : Compounds and compositions are disclosed in which a quaternized drug unit is linked to a targeting ligand unit from 0 which a tertiary amine-containing drug is released at the targeted site of action. Methods for treating diseases characterized by the \" targeted abnormal cells, such as cancer or an autoimmune disease using the compounds and compositions of the invention are also 0 disclosed. WO 2017/096311 Al MIDEDItitililliMEMEDICHHIMUMOVOIMIE Declarations under Rule 4.17: Published: — as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii)) — with international search report (Art 21(3)) — as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(0)