Invention Grant
- Patent Title: Heterocyclic self-immolative linkers and conjugates
- Patent Title (中): 杂环自我消失的接头和共轭体
-
Application No.: US12764821Application Date: 2010-04-21
-
Publication No.: US07989434B2Publication Date: 2011-08-02
- Inventor: Bainian Feng
- Applicant: Bainian Feng
- Applicant Address: US WA Bothell
- Assignee: Seattle Genetics, Inc.
- Current Assignee: Seattle Genetics, Inc.
- Current Assignee Address: US WA Bothell
- Main IPC: A61K31/395
- IPC: A61K31/395 ; A61K31/435 ; A61K31/495 ; A61K31/53 ; C07K16/00

Abstract:
The present invention provides heterocyclic linker compounds useful for linking drug moieties to ligands. The compounds also include drug-ligand conjugates comprising a ligand capable of targeting a selected cell population, and a drug connected to the ligand by a heterocyclic linker moiety. The linker moiety comprises a peptide sequence that is a substrate for an intracellular enzyme, for example a cathepsin, that cleaves the peptide at an amide bond. The peptide further contains a self-immolating moiety which connects the drug and the protein peptide sequence. Upon cleavage of the peptide sequence by an intracellular enzyme the self-immolating moiety cleaves itself from the drug moiety such that the drug moiety is in an underivatized and active form.
Public/Granted literature
- US20100273843A1 HETEROCYCLIC SELF-IMMOLATIVE LINKERS AND CONJUGATES Public/Granted day:2010-10-28
Information query