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US 12,678,518 B2Granted
Theranostic probe and its use for targeting and/or labeling the EGFR kinase and/or the cells expressing EGFR or its family members
AssigneeTianjin University
InventorsLizhi Mi, Xingxing Wang, Peng Liu, Xiaohong Qin, Zhiqun Shang
Life of this patent
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Abstract
The present application is directed to a theranostic probe and its use for targeting and/or labeling the EGFR kinase and/or the cells expressing EGFR or its family members.
Claims9
A theranostic probe represented by formula (1):
- Module 2-L-Module 1 (1)
- wherein
- L is a linker;
- Module 1 is a moiety targeting the EGFR kinase and is represented by formula (2):
- wherein
- R1 in formula (2) is H, halogen or C2-6alkynyl;
- R2 in formula (2) is H, halogen, C6-10arylC1-6 alkyloxy or 5- to 6-membered heteroarylC1-6alkyloxy, wherein the C6-10aryl and 5- to 6-membered heteroaryl are optionally substituted with halogen, and the 5- to 6-membered heteroaryl comprises 1, 2, 3 or 4 heteroatoms selected from the group consisting of O, S and N;
- R3 in formula (2) is H, C1-6alkyloxy optionally substituted with C1-6alkyloxy, or 5- to 6-membered heterocycloalkyloxy, wherein the 5- to 6-membered heterocycloalkyl comprises 1 or 2 heteroatoms selected from the group consisting of O, S and N;
- R4 in formula (2), as the attachment point of Module 1 to L, is —(CH2)n—;
- and
- n in formula (2) is 0, 1, 2, 3, 4, 5 or 6;
- and
- Module 2 is an imaging probe selected from the group consisting of fluorescent, MRI and radioactive probes;
- or a theranostically acceptable salt thereof.
11 more elements
Dependencies are inferred from the claim text.