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US07754681B2 Heterocyclic self-immolative linkers and conjugates 有权
杂环自我消失的接头和共轭体

  • 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.: US11925659
    Application Date: 2007-10-26
  • Publication No.: US07754681B2
    Publication Date: 2010-07-13
  • 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: A61K38/00
  • IPC: A61K38/00
Heterocyclic self-immolative linkers and conjugates
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.
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