Novel Hydrophilic Linkers and Ligand-Drug Conjugates Thereof

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 conne...

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Bibliographic Details
Main Authors ZHAO, Robert Yongxin, LI, Wenjun, ZHUO, Xiaotao, GAI, Shun, SUN, Sanxing, HUANG, Yuanyuan, JIA, Junxiang, LI, Xing, YANG, Qingliang, ZHOU, Xiaomai, GUO, Huihui, LIN, Chen, QU, Lan, XIE, Hongsheng, YE, Hangbo
Format Patent
LanguageEnglish
Published 21.05.2020
Subjects
ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary: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. WO 2016/147031 PCT/IB2015/052011 1200 - -0- PBS -U- T-DM1 E oDX-111 E *- DX-112 a) 0 5 10 15 20 25 30 35 40 Days after Initiation of Treatment Figure 1
Bibliography:Application Number: AU20200200566