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1. 发明申请

WO2016147031A3 NOVEL HYDROPHILIC LINKERS AND LIGAND-DRUG CONJUGATES THEREOF 审中-公开
标题翻译：新型亲水链接剂和配体 - 药物偶联物
公开(公告)号：WO2016147031A3
公开(公告)日：2016-11-10
申请号：PCT/IB2015052011
申请日：2015-03-19
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： SUN SANXING , ZHAO ROBERT YONGXIN , LI XING , GUO HUIHUI , JIA JUNXIANG , XIE HONGSHENG , ZHOU XIAOMAI , HUANG YUANYUAN , YANG QINGLIANG , ZHUO XIAOTAO , YE HANGBO , GAI SHUN , QU LAN , LI WENJUN , LIN CHEN
IPC分类号： C07D207/404 , A61K47/48 , A61P35/00 , C07D207/327 , C07F9/38 , C07K16/28
CPC分类号： C07D207/46 , A61K47/6803 , A61K47/6851 , A61K47/6889 , C07F9/5721 , C07F9/65583
摘要： The present invention provides hydrophilic linkers that are useful for linking drugs to cell-binding ligands in ligand-drug conjugates, such as antibody-drug conjugates. The ligand- drug conjugate comprises a cell -binding ligand capable of binding to a particular cell population, and a drug connected to the ligand by a hydrophilic linker. The hydrophilic linker comprises one or more hydrophilic groups that render the linker hydrophilic. The hydrophilic linker may also comprise functional groups at the two termini for coupling to the drug and the cell-binding ligand respectively.
摘要翻译：本发明提供了用于将药物与配体 - 药物缀合物如抗体 - 药物缀合物中的细胞结合配体连接的亲水性接头。配体 - 药物缀合物包含能够结合特定细胞群的细胞结合配体和通过亲水性接头与配体连接的药物。亲水性连接体包含一个或多个赋予连接体亲水性的亲水性基团。亲水性接头还可以在两个末端包含官能团以分别与药物和细胞结合配体偶联。

2. 发明申请

WO2015151079A3 AURISTATIN ANALOGUES AND THEIR CONJUGATES WITH CELL-BINDING MOLECULES 审中-公开
标题翻译：胰岛素类似物及其与细胞结合分子的结合
公开(公告)号：WO2015151079A3
公开(公告)日：2016-05-06
申请号：PCT/IB2015054653
申请日：2015-06-20
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： YANG QINGLIANG , ZHAO ROBERT Y , YE HANGBO , GAI SHUN , JIA JUNXIANG , HUANG YUANYUAN , LI XING , GUO HUIHUI , XIE HONGSHENG , LI WENJUN , ZHOU XIAOMAI , YANG CHENGYU , ZHUO XIAOTAO , ZHAO LINYAO , CAO MINJUN , LIN CHEN , PENG JIE , YE ZHICANG , XU JUN
IPC分类号： A61K47/48 , A61K39/395 , A61P35/00 , C07K5/02
CPC分类号： C07D403/12 , A61K47/6803 , A61K47/6855 , A61K47/6869 , C07D405/14
摘要： Provided are analogues of auristatins, in particular monomethyl auristatin F (MMAF), as cytotoxic agents, conjugates of such agents with a cell-binding agent, the preparation and the therapeutic uses of these cytotoxic agents and conjugates thereof to arrest or retard abnormal cell growth and /or proliferation.
摘要翻译：提供了auristatin的类似物，特别是单甲基auristatin F（MMAF），作为细胞毒性剂，这些试剂与细胞结合剂的缀合物，这些细胞毒性剂的制备和治疗用途及其结合物来阻止或延缓异常细胞生长和/或增殖。

3. 发明专利

CA2978857C NOVEL HYDROPHILIC LINKERS AND LIGAND-DRUG CONJUGATES THEREOF 未知
公开(公告)号：CA2978857C
公开(公告)日：2021-04-20
申请号：CA2978857
申请日：2015-03-19
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： SUN SANXING , ZHAO ROBERT YONGXIN , LI XING , GUO HUIHUI , JIA JUNXIANG , XIE HONGSHENG , ZHOU XIAOMAI , HUANG YUANYUAN , YANG QINGLIANG , ZHUO XIAOTAO , YE HANGBO , GAI SHUN , QU LAN , LI WENJUN , LIN CHEN
IPC分类号： C07D207/404 , A61P35/00 , C07D207/327 , C07F9/38 , C07K16/28
摘要： The present invention provides hydrophilic linkers that are useful for linking drugs to cell-binding ligands in ligand-drug conjugates, such as antibody-drug conjugates. The ligand- drug conjugate comprises a cell -binding ligand capable of binding to a particular cell population, and a drug connected to the ligand by a hydrophilic linker. The hydrophilic linker comprises one or more hydrophilic groups that render the linker hydrophilic. The hydrophilic linker may also comprise functional groups at the two termini for coupling to the drug and the cell-binding ligand respectively.

4. 发明专利

PL3271329T3 NOWE ŁĄCZNIKI HYDROFILOWE I ICH KONIUGATY LIGAND-LEK 未知
公开(公告)号：PL3271329T3
公开(公告)日：2022-01-17
申请号：PL15885301
申请日：2015-03-19
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： SUN SANXING , ZHAO ROBERT YONGXIN , LI XING , GUO HUIHUI , JIA JUNXIANG , XIE HONGSHENG , ZHOU XIAOMAI , HUANG YUANYUAN , YANG QINGLIANG , ZHUO XIAOTAO , YE HANGBO , GAI SHUN , QU LAN , LI WENJUN , LIN CHEN
IPC分类号： A61P35/00 , A61K47/68 , C07D207/327 , C07D207/404 , C07D207/46 , C07F9/572 , C07F9/6558 , C07K16/00 , C07K16/28

5. 发明专利

AU2020200566A1 Novel Hydrophilic Linkers and Ligand-Drug Conjugates Thereof 未知
公开(公告)号：AU2020200566A1
公开(公告)日：2020-02-13
申请号：AU2020200566
申请日：2020-01-26
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： SUN SANXING , ZHAO ROBERT YONGXIN , LI XING , GUO HUIHUI , JIA JUNXIANG , XIE HONGSHENG , ZHOU XIAOMAI , HUANG YUANYUAN , YANG QINGLIANG , ZHUO XIAOTAO , YE HANGBO , GAI SHUN , QU LAN , LI WENJUN , LIN CHEN
IPC分类号： C07D207/404 , A61P35/00 , C07D207/327 , C07F9/38 , C07K16/28
摘要： The present invention provides hydrophilic linkers that are useful for linking drugs to cell-binding ligands in ligand-drug conjugates, such as antibody-drug conjugates. The 5 ligand- drug conjugate comprises a cell -binding ligand capable of binding to a particular cell population, and a drug connected to the ligand by a hydrophilic linker. The hydrophilic linker comprises one or more hydrophilic groups that render the linker hydrophilic. The hydrophilic linker may also comprise functional groups at the two termini for coupling to the drug and the cell-binding ligand respectively.

6. 发明专利

AU2019203316B2 Novel Hydrophilic Linkers and Ligand-Drug Conjugates Thereof 未知
公开(公告)号：AU2019203316B2
公开(公告)日：2020-05-14
申请号：AU2019203316
申请日：2019-05-13
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： SUN SANXING , ZHAO ROBERT YONGXIN , LI XING , GUO HUIHUI , JIA JUNXIANG , XIE HONGSHENG , ZHOU XIAOMAI , HUANG YUANYUAN , YANG QINGLIANG , ZHUO XIAOTAO , YE HANGBO , GAI SHUN , QU LAN , LI WENJUN , LIN CHEN
IPC分类号： C07D207/404 , A61P35/00 , C07D207/327 , C07F9/38 , C07K16/28
摘要： The present invention provides hydrophilic linkers that are useful for linking drugs to cell-binding ligands in ligand-drug conjugates, such as antibody-drug conjugates. The 5 ligand- drug conjugate comprises a cell -binding ligand capable of binding to a particular cell population, and a drug connected to the ligand by a hydrophilic linker. The hydrophilic linker comprises one or more hydrophilic groups that render the linker hydrophilic. The hydrophilic linker may also comprise functional groups at the two termini for coupling to the drug and the cell-binding ligand respectively.

7. 发明专利

AU2015386647A1 Novel hydrophilic linkers and ligand-drug conjugates thereof 未知
公开(公告)号：AU2015386647A1
公开(公告)日：2017-08-31
申请号：AU2015386647
申请日：2015-03-19
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： SUN SANXING , ZHAO ROBERT YONGXIN , LI XING , GUO HUIHUI , JIA JUNXIANG , XIE HONGSHENG , ZHOU XIAOMAI , HUANG YUANYUAN , YANG QINGLIANG , ZHUO XIAOTAO , YE HANGBO , GAI SHUN , QU LAN , LI WENJUN , LIN CHEN
IPC分类号： C07D207/404 , A61P35/00 , C07D207/327 , C07F9/38 , C07K16/28
摘要： The present invention provides hydrophilic linkers that are useful for linking drugs to cell-binding ligands in ligand-drug conjugates, such as antibody-drug conjugates. The ligand- drug conjugate comprises a cell -binding ligand capable of binding to a particular cell population, and a drug connected to the ligand by a hydrophilic linker. The hydrophilic linker comprises one or more hydrophilic groups that render the linker hydrophilic. The hydrophilic linker may also comprise functional groups at the two termini for coupling to the drug and the cell-binding ligand respectively.

8. 发明专利

CA2978857A1 NOVEL HYDROPHILIC LINKERS AND LIGAND-DRUG CONJUGATES THEREOF 未知
公开(公告)号：CA2978857A1
公开(公告)日：2016-09-22
申请号：CA2978857
申请日：2015-03-19
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： SUN SANXING , ZHAO ROBERT YONGXIN , LI XING , GUO HUIHUI , JIA JUNXIANG , XIE HONGSHENG , ZHOU XIAOMAI , HUANG YUANYUAN , YANG QINGLIANG , ZHUO XIAOTAO , YE HANGBO , GAI SHUN , QU LAN , LI WENJUN , LIN CHEN
IPC分类号： C07D207/404 , A61P35/00 , C07D207/327 , C07F9/38 , C07K16/28
摘要： The present invention provides hydrophilic linkers that are useful for linking drugs to cell-binding ligands in ligand-drug conjugates, such as antibody-drug conjugates. The ligand- drug conjugate comprises a cell -binding ligand capable of binding to a particular cell population, and a drug connected to the ligand by a hydrophilic linker. The hydrophilic linker comprises one or more hydrophilic groups that render the linker hydrophilic. The hydrophilic linker may also comprise functional groups at the two termini for coupling to the drug and the cell-binding ligand respectively.

9. 发明专利

AU2014384434A1 Charged linkers and their uses for conjugation 未知
公开(公告)号：AU2014384434A1
公开(公告)日：2016-05-19
申请号：AU2014384434
申请日：2014-02-28
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： ZHAO ROBERT YONGXIN , LI XING , HUANG YUANGYUANG , YANG QINGLIANG
IPC分类号： C07F9/30 , A61K31/662 , A61K47/48 , A61P31/00 , A61P35/00 , A61P37/00
摘要： Cell binding agent-drug conjugates comprising phosphinate-based charged linkers and methods of using such linkers and conjugates are provided.

10. 发明专利

ES2897706T3 Nuevos enlazadores hidrófilos y conjugados ligando-fármaco de los mismos 未知
公开(公告)号：ES2897706T3
公开(公告)日：2022-03-02
申请号：ES15885301
申请日：2015-03-19
申请人： HANGZHOU DAC BIOTECH CO LTD
发明人： SUN SANXING , ZHAO ROBERT YONGXIN , LI XING , GUO HUIHUI , JIA JUNXIANG , XIE HONGSHENG , ZHOU XIAOMAI , HUANG YUANYUAN , YANG QINGLIANG , ZHUO XIAOTAO , YE HANGBO , GAI SHUN , QU LAN , LI WENJUN , LIN CHEN
IPC分类号： A61K47/68 , A61P35/00 , C07D207/327 , C07D207/404 , C07D207/46 , C07F9/572 , C07F9/6558 , C07K16/00 , C07K16/28
摘要： Un conjugado ligando-fármaco de Fórmula (2): **(Ver fórmula)** donde: D representa un fármaco citotóxico; L representa un ligando de unión a células; V representa un grupo polar o cargado seleccionado del grupo que consiste en aminos [-N (R) -], ureas que son -N (CONR1R2) -, carboxilos [-Q (COOH) - o -Q (ZCOOH) -], carbamatos que son-N (COOR) -, guanidinas [-N (R1) C = N (COOR2)N(R3) -], sulfonamidas [-N (SO2R) -], ácidos sulfónicos [-Q (ZSO2OH) -] , ácidos sulfámicos [-N (SO2OH) -], fosfonatos {-Q [ZPO (OR)2] -}, ácidos fosfónicos {-Q [ZPO (OH)2] -}, ácidos fosforamídicos {-N[PO (OH)2] -}, ácidos fosforodiamídicos {-N [PO (NH2)(OH)] -} y triamidas fosfóricas {-N [PO (NH2)2] -}, donde R, R1, R2 y R3 son independientemente H o alquilo C1-C8; Q es CH o N; Z es 1-5 unidades de metileno; U' representa un grupo funcional que permite un enlace covalente con el fármaco citotóxico; el grupo funcional que permite un enlace covalente con el fármaco citotóxico seleccionado del grupo que consiste en tioles, disulfuros, aminos, carboxilos, aldehídos, cetonas, maleimidas, grupos haloacetilo, grupos alquenilo, grupos alquinilo, hidrazinas e hidroxilos, por lo que el enlace covalente con el fármaco citotóxico puede ser un enlace disulfuro, un enlace tioéter, un enlace tioéster, un enlace amida, un enlace éster, un enlace carbono-nitrógeno, un enlace carbono-carbono, un enlace hidrazina, un enlace hidrazida, un enlace hidrazona, un enlace éter, enlace carbamato o enlace carbonato; W' representa un grupo funcional que permite un enlace covalente con el ligando de unión a células L, donde dicho grupo funcional W' se selecciona de (a) grupos funcionales que permiten un enlace covalente con un grupo amino en el ligando de unión a células, dichos grupos funcionales W' se seleccionan del grupo que consiste en ésteres de N- hidroxisuccinimida, ésteres de N-sulfosuccinimidilo, ésteres de nitrofenilo, ésteres de dinitrofenilo, ésteres de pentafluorofenilo, ésteres de tetrafluorofenilo, cloruros de acilo, anhídridos, cloruros de sulfonilo, cloroformiatos, isocianatos, isotiocianatos, aldehídos y cetonas, y (b) grupos funcionales que permiten un enlace covalente con el grupo tiol en el ligando de unión a células, dichos grupos funcionales W' se seleccionan entre disulfuros, por ejemplo piridildisulfuros y nitropiridildisulfuros; maleimidas; cloruros de acilo; grupos haloacetilo, por ejemplo yodoacetamida y bromoacetamida; alquenil piridinas; isocianatos; e isotiocianatos; X representa un componente compuesto por una, dos o tres unidades de metileno, donde las unidades de metileno pueden estar opcionalmente sustituidas con grupos alquilo, halo, hidroxilo o alcoxi; Y representa un componente compuesto por una, dos o tres unidades de metileno, donde las unidades de metileno pueden estar opcionalmente sustituidas con grupos alquilo, halo, hidroxilo o alcoxi; n es un número entero de 1 a 100, donde si n> 1, los valores de cada V, X e Y en los corchetes repetidos de la Fórmula (2) son independientes y no tienen por qué ser idénticos.

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