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31. 发明专利

SG11201908721TA CONJUGATION OF A CYTOTOXIC DRUG WITH BIS-LINKAGE 未知
公开(公告)号：SG11201908721TA
公开(公告)日：2019-10-30
申请号：SG11201908721T
申请日：2017-04-06
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： ZHAO ROBERT YONGXIN , HUANG YUANYUAN , YANG QINGLIANG , GAI SHUN , YE HANGBO , ZHAO LINYAO , YANG CHENGYU , XU YIFANG , GUO HUIHUI , CHAO MINJUN , TONG QIANQIAN , LI WENJUN , CAI XIANG , ZHOU XIAOMAI , XIE HONGSHENG , JIA JUNXIANG , ZHU HAIFENG , GUO ZHIXIANG , GAO SHUIHONG , WANG CHUNYAN , LIN CHEN , YANG YANLEI , YE ZHICANG , PENG JIE , XU JUN , ZUO XIAOTAO , SU QINGYU
IPC分类号： C07D417/14 , A61P31/00
摘要： 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

32. 发明专利

PH12019501056A1 CONJUGATION LINKERS, CELL BINDING MOLECULE-DRUG CONJUGATES CONTAINING THE LIKERS, METHODS OF MAKING AND USES SUCH CONJUGATES WITH THE LINKERS 未知
公开(公告)号：PH12019501056A1
公开(公告)日：2019-09-09
申请号：PH12019501056
申请日：2019-05-14
申请人： HANGZHOU DAC BIOTECH CO LTD , SUZHOU M CONJI BIOTECH CO LTD
发明人： ZHAO YONGXIN ROBERT , YANG QINGLIANG , HUANG YUANYUAN , GAI SHUN , YE HANGBO , ZHAO LINYAO , YANG CHENGYU , GUO HUIHUI , ZHOU XIAOMAI , XIE HONGSHENG , ZHU HAIFENG , XU YIFANG , TONG QIANQIAN , JIA JUNXIANG , CAO MINJUN , LI WENJUN , GAO SHUIHONG , GUO ZHIXIANG , BAI LU , LI CHEN , YANG YANLEI , WANG CHUNYAN , YE ZHICHANG
IPC分类号： A61K31/10
摘要： The present invention relates to linkers having a group of propiolyl, substituted acryl (acryloyl), or disubstituted propanoyl, and using such linkers for the conjugation of compounds, in particular, cytotoxic agents to a cell-binding molecule.

33. 发明专利

ZA202110803B A CONJUGATE OF A CYTOTOXIC AGENT TO A CELL BINDING MOLECULE WITH BRANCHED LINKERS 未知
公开(公告)号：ZA202110803B
公开(公告)日：2022-09-28
申请号：ZA202110803
申请日：2021-12-22
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： ZHAO ROBERT YONGXIN , YANG QINGLIANG , ZHAO LINYAO , HUANG YUANYUAN , YE HANGBO , GAI SHUN , JIA JUNXIANG , BAI LU , LI WENJUN , GUO ZHIXIANG , LIN CHEN , ZHENG JUN , GUO HUIHUI , CAO MINJUN , KONG XIANGFEI , DU YONG , XU YIFANG , ZHOU XIAOMAI , XIE HONGSHENG , ZHANG XIUZHEN , CHEN MIAOMIAO , LIU XIAOLEI , CAI XIANG , CHEN BINBIN , YANG YANLEI , ZHANG LINGLI
摘要： Provided is a conjugation of cytotoxic drug to a cell-binding molecule with a side-chain linker. It provides side-chain linkage methods of making a conjugate of a cytotoxic molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and immunological disorders.

34. 发明专利

CL2021000901A1 Enlazadores de conjugación que contienen el grupo 2,3-diaminosuccinilo 未知
公开(公告)号：CL2021000901A1
公开(公告)日：2022-03-04
申请号：CL2021000901
申请日：2021-04-12
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： ZHAO ROBERT YONGXIN , ZHUO XIAOTAO , YANG QINGLIANG , ZHAO LINYAO , HUANG YUANYUAN , YE HANGBO , YANG CHENGYU , LEI JUN , GAI SHUN , GUO HUIHUI , JIA JUNXIANG , BAI LU , XIE HONGSHENG , ZHOU XIAOMAI , GUO ZHIXIANG , LI WENJUN , ZHENG JUN , YANG YANLEI , XU YIFANG , TONG QIANQIAN , CHAO MINGJUN , TONG YANHONG , YE ZHICANG , LIN CHEN , CHEN BINBIN
IPC分类号： A61P31/00 , C07D417/14
摘要： Se provee un conjugado de una molécula o fármaco citotóxicos con una molécula de unión a células con un enlazador bis (enlazador dual) que contiene un grupo 2,3-diaminosuccinilo, . También se hace referencia a la preparación del conjugado de un fármaco o molécula citotóxicos con una molécula de unión a células con un enlazador bis, en particular cuando el fármaco tiene grupos de amino, hidroxilo, diamino, amino-hidroxilo, dihidroxilo, carboxilo, hidrazina, aldehído y tiol para su conjugación con el enlazador bis en una forma específica, así cómo también al uso terapéutico de los conjugados.

35. 发明专利

AU2020301115A1 A formulation of a conjugate of a tubulysin analog to a cell-binding molecule 未知
公开(公告)号：AU2020301115A1
公开(公告)日：2022-02-10
申请号：AU2020301115
申请日：2020-02-18
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： ZHAO ROBERT , YANG QINGLIANG , HUANG YUANYUAN , GAI SHUN , YE HANGBO , ZHAO LINYAO , GUO HUIHUI , BAI LU , LI WENJUN , JIA JUNXIANG , GUO ZHIXIANG , ZHENG JUN , CHEN XIAOXIAO , KONG XIANGFEI , LIN CHEN , DU YONG , ZHANG YU , ZHOU LEI , ZHANG XIOUZHENG , ZHENG XIOUHONG , CHEN BINGBING , YANG YANLEI , DAI MENG , XU YIFANG , FANG ZHONGLIANG , ZHOU XIAOMAI , JIANG XINGYAN , CHEN MIAIMIAO , ZHANG LINGLI , LI YANHUA
IPC分类号： A61K47/68 , A61K9/08 , A61K31/426 , A61P35/00 , C07D277/56
摘要： A formulation of conjugates of tubulysin analogs with a cell-binding molecule having a structure represented by Formula (I), wherein T, L, m, n, -----, R

36. 发明专利

AU2018430758B2 Cross-linked pyrrolobenzodiazepine dimer (PBD) derivative and its conjugates 未知
公开(公告)号：AU2018430758B2
公开(公告)日：2022-01-27
申请号：AU2018430758
申请日：2018-07-05
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： ZHAO ROBERT YONGXIN , ZHUO XIAOTAO , YANG QINGLIANG , ZHAO LINYAO , HUANG YUANYUAN , YE HANGBO , YANG CHENGYU , LEI JUN , GAI SHUN , GUO HUIHUI , JIA JUNXIANG , BAI LU , XIE HONGSHENG , ZHOU XIAOMAI , GUO ZHIXIANG , LI WENJUN , CAO MINGJUN , ZHENG JUN , YE ZHICHANG , YANG YANLEI
IPC分类号： C07D487/04 , A61K31/5517 , A61P35/00
摘要： A novel cross-linked cytotoxic agents, pyrrolobenzo-diazepine dimer (PBD) derivatives, and their conjugates to a cell-binding molecule, a method for preparation of the conjugates and the therapeutic use of the conjugates.

37. 发明专利

SG11202107876VA A CONJUGATE OF AN AMANITA TOXIN WITH BRANCHED LINKERS 未知
公开(公告)号：SG11202107876VA
公开(公告)日：2021-08-30
申请号：SG11202107876V
申请日：2019-01-31
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： ZHAO ROBERT YONGXIN , YANG QINGLIANG , LEI JUN , HUANG YUANYUAN , ZHAO LINYAO , YE HANGBO , GAI SHUN , CAO MINGJUN , TONG QIANQIAN , BAI LU , GUO ZHIXIANG , YANG CHENGYU , ZHOU XIAOMAI , XIE HONGSHENG , XU YIFANG , GUO HUIHUI , JIA JUNXIANG , ZHENG JUN , LIN CHENG , ZHUO XIAOTAO , LI WENJUN , DU YONG , KONG XIANGFEI , CHEN BINBIN , YANG YANLEI , TONG YANHONG , CHEN XIAOXIAO , LI YANHUA , ZHANG XIUZHENG , LAI JUAN
IPC分类号： A61K47/50 , A61P35/00 , C07K7/64
摘要： Provided herein is the conjugation of an amanita toxin compound to a cell-binding molecule with branched linkers for having better targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of an amanita molecule to a cell-binding ligand, as well as methods of using the conjugate in targets treatment of cancer, infection and autoimmune disease.

38. 发明专利

AU2021200562A1 Conjugation Linkers, Cell Binding Molecule-Drug Conjugates Containing the linkers, methods of making and uses such conjugates with the linkers 未知
公开(公告)号：AU2021200562A1
公开(公告)日：2021-02-25
申请号：AU2021200562
申请日：2021-01-29
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： ZHAO YONGXIN ROBERT , YANG QINGLIANG , HUANG YUANYUAN , GAI SHUN , YE HANGBO , ZHAO LINYAO , YANG CHENGYU , GUO HUIHUI , ZHOU XIAOMAI , XIE HONGSHENG , ZHU HAIFENG , XU YIFANG , TONG QIANQIAN , JIA JUNXIANG , CAO MINJUN , LI WENJUN , GAO SHUIHONG , GUO ZHIXIANG , BAI LU , LI CHEN , YANG YANLEI , WANG CHUNYAN , YE ZHICHANG
IPC分类号： C07K14/00 , A61K31/10
摘要： The present invention relates to linkers having a group of propiolyl, substituted acryl (acryloyl), or disubstituted propanoyl, and using such linkers 5 for the conjugation of compounds, in particular, cytotoxic agents to a cell binding molecule.

39. 发明专利

CA3128264A1 A CONJUGATE OF AN AMANITA TOXIN WITH BRANCHED LINKERS 未知
公开(公告)号：CA3128264A1
公开(公告)日：2020-08-06
申请号：CA3128264
申请日：2019-01-31
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： ZHAO ROBERT YONGXIN , YANG QINGLIANG , LEI JUN , HUANG YUANYUAN , ZHAO LINYAO , YE HANGBO , GAI SHUN , CAO MINGJUN , TONG QIANQIAN , BAI LU , GUO ZHIXIANG , YANG CHENGYU , ZHOU XIAOMAI , XIE HONGSHENG , XU YIFANG , GUO HUIHUI , JIA JUNXIANG , ZHENG JUN , LIN CHENG , ZHUO XIAOTAO , LI WENJUN , DU YONG , KONG XIANGFEI , CHEN BINBIN , YANG YANLEI , TONG YANHONG , CHEN XIAOXIAO , LI YANHUA , ZHANG XIUZHENG , LAI JUAN
IPC分类号： A61K47/50 , A61P35/00 , C07K7/64
摘要： Provided herein is the conjugation of an amanita toxin compound to a cell-binding molecule with branched linkers for having better targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of an amanita molecule to a cell-binding ligand, as well as methods of using the conjugate in targets treatment of cancer, infection and autoimmune disease.

40. 发明专利

AU2017408164A1 Conjugation of a cytotoxic drug with bis-linkage 未知
公开(公告)号：AU2017408164A1
公开(公告)日：2019-10-03
申请号：AU2017408164
申请日：2017-04-06
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： ZHAO ROBERT YONGXIN , HUANG YUANYUAN , YANG QINGLIANG , GAI SHUN , YE HANGBO , ZHAO LINYAO , YANG CHENGYU , XU YIFANG , GUO HUIHUI , CHAO MINJUN , TONG QIANQIAN , LI WENJUN , CAI XIANG , ZHOU XIAOMAI , XIE HONGSHENG , JIA JUNXIANG , ZHU HAIFENG , GUO ZHIXIANG , GAO SHUIHONG , WANG CHUNYAN , LIN CHEN , YANG YANLEI , YE ZHICANG , PENG JIE , XU JUN , ZUO XIAOTAO , SU QINGYU
IPC分类号： C07D417/14 , A61P31/00
摘要： What provided is the conjugation of cytotoxic to a cell-binding molecule with a bis-linker(dual-linker) as shown in 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.

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