Patent SG-11201908721T-A (SG)
Title: Conjugation of a cytotoxic drug with bis-linkage
Inventor: ZHAO ROBERT YONGXIN
IPC: A61P31/00
Filed: 2017-04-06
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 11 October 2018 (11.10.2018) WIPO I PCT 0111111010 0111 °nolo OH H imomiono oimIE (10) International Publication Number WO 2018/185526 Al (51) International Patent Classification: C07D 417/14 (2006.01) A61P 31/00 (2006.01) (21) International Application Number: PCT/IB2017/051977 (22) International Filing Date: 06 April 2017 (06.04.2017) (25) Filing Language: English (26) Publication Language: English (71) Applicant: HANGZHOU DAC BIOTECH CO., LTD [CN/CN]; Building 12, ZhengTaiZhongZi Tech. Park, No. 260 Sixth Street, HEDA, Hangzhou, Zhejiang 310018 (CN). (72) Inventors: ZHAO, Robert Yongxin; 7Loring Street, 7Loring Street, Lexington, Massachusetts 02421 (US). HUANG, Yuanyuan; Room 401, Building 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). YANG, Qingliang; Room 401, Building 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). GAL Shun; Rm 303, Bildg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). YE, Hangbo; Rm 402, Bldge 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). ZHAO, Linyao; Rm 403, Bldge 12, No. 260 Sixth Street, Hangzhou, Zhe- jiang 310018 (CN). YANG, Chengyu; Rm 402, Bldge 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). XU, Yifang; Rm 402, Bldg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). GUO, Huihui; Rm 304, Bldg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). CHAO, Minjun; Rm 304, Bildg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). TONG, Qian- qian; Rm 302, Bildg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). LI, Wenjun; Rm 405, Bildg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). CAI, Xiang; Rm 304, Bildg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). ZHOU, Xiaomai; Rm 2006, Bildg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). XIE, Hongsheng; Rm 2005, Bildg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). JIA, Junxiang; Rm 301, Bildg 12, No. 260 Sixth Street, Hangzhou, Zhe- jiang 310018 (CN). ZHU, Haifeng; Rm 305, Bildg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). GUO, Zhixiang; Rm 102,Bildg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). GAO, Shuihong; Rm 305, Bildg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). WANG, Chunyan; Rm 305, Bildg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). LIN, Chen; Rm 301, Bildg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). YANG, Yanlei; Rm 103, Bildg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). YE, Zhicang; Rm 303, Bildg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). PENG, Jie; Rm 104, Bildg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). XU, Jun; Rm 301, Bildg 12, No. 260 Sixth Street, Hangzhou, Zhejiang 310018 (CN). ZUO, Xiaotao; Rm 402, Building 12, 260 Sixth Street, HEDA, Hangzhou, Zhejiang 310018 (CN). SU, Qingyu; Rm 303, Building 12, 260 Sixth Street, HEDA, Hangzhou, Zhejiang 310018 (CN). (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, 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 the identity of the inventor (Rule 4.170) as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii)) of inventorship (Rule 4.17(iv)) Published: with international search report (Art. 21(3)) 1-1 (54) Title: CONJUGATION OF A CYTOTOXIC DRUG WITH BIS-LINKAGE (57) : What provided is the conjugation of cytotoxic to a cell-binding molecule with a bis-linker(dual-linker) as shown in 0 Formula (I). It provides bis-linkage methods of making a conjugate of a cytotoxic drug molecule to a cell-binding agent in a specific \" manner. It also relates to application of the conjugates for the treatment of a cancer, or an autoimmune disease, or an infectious disease. C