SG11201908721TA - Conjugation of a cytotoxic drug with bis-linkage - Google Patents

Conjugation of a cytotoxic drug with bis-linkage

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Publication number
SG11201908721TA
SG11201908721TA SG11201908721TA SG11201908721TA SG 11201908721T A SG11201908721T A SG 11201908721TA SG 11201908721T A SG11201908721T A SG 11201908721TA SG 11201908721T A SG11201908721T A SG 11201908721TA
Authority
SG
Singapore
Prior art keywords
street
hangzhou
zhejiang
bildg
international
Prior art date
Application number
Inventor
Robert Yongxin Zhao
Yuanyuan Huang
Qingliang Yang
Shun Gai
Hangbo Ye
Linyao Zhao
Chengyu Yang
Yifang Xu
Huihui Guo
Minjun Chao
Qianqian Tong
Wenjun Li
Xiang Cai
Xiaomai Zhou
Hongsheng Xie
Junxiang Jia
Haifeng Zhu
Zhixiang Guo
Shuihong Gao
Chunyan Wang
Chen Lin
Yanlei Yang
Zhicang Ye
Jie Peng
Jun Xu
Xiaotao Zuo
Qingyu Su
Original Assignee
Hangzhou Dac Biotech Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hangzhou Dac Biotech Co Ltd filed Critical Hangzhou Dac Biotech Co Ltd
Publication of SG11201908721TA publication Critical patent/SG11201908721TA/en

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    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
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    • A61K47/6807—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug or compound being a sugar, nucleoside, nucleotide, nucleic acid, e.g. RNA antisense
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    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
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    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
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    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
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    • C07—ORGANIC CHEMISTRY
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    • C07D513/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/32—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products of oncogenes
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    • C07K2317/00—Immunoglobulins specific features
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    • C07K2317/94—Stability, e.g. half-life, pH, temperature or enzyme-resistance

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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

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
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