Back to results
US 2021/0060190 A1Published application
Residualizing linkers and uses thereof
AssigneeCentre for Probe Development and Commercialization
InventorsJohn Fitzmaurice Valliant, Eric Steven Burak, Neil Grant Cockbum, Alla Darwish, Joe Adamson Drewry, John Richard Forbes, Meiduo Hu, Ryan Wayne Simms, Karin Ann Stephenson, Tao Wu
Life of this patent
Estimating the term…
Abstract
The present invention relates to conjugates including a residualizing linker, methods for their production, and uses thereof.
Claims37
A conjugate comprising a polypeptide linked to a detection agent, the conjugate having the structure:
- or a salt thereof,
- wherein A-NH— is a polypeptide;
- L1 and L2 are independently absent, optionally substituted C1-C6 alkyl, optionally substituted C1-C6 heteroalkyl optionally substituted C3-C10 cycloalkyl, optionally substituted aryl, optionally substituted C2-C100 polyethylene glycol;
- L3 is absent or optionally substituted C1-C6 alkyl;
- m is 0 or 1;
- R1 is hydrogen and R2 is —CH2CO2H or —CH2CH2CO2H, or R is —CH2CO2H or —CH2CH2CO2H and R2 is hydrogen;
- each R3 and R4 is hydrogen or R3 and R4 combine to form C═O;
- n is 0 or 1;
- o is 3;
- R5 is hydrogen or L4-B;
- R6 and R7 are independently hydrogen, optionally substituted C1-C6 heteroalkyl, or L4-B;
- L4 is optionally substituted C1-C6 alkyl, or optionally substituted C1-C6 heteroalkyl;
- B is an organic moiety comprising a detection agent;
- at least one of L1 and L2 is present and when L1 or L2 is absent, m is 0;
- and one and only one of R5, R6, and R7 is L4-B,
- wherein B has the structure:
- in which R8 is a radionuclide selected from the group consisting of 18F, 75Br, 76Br, 77Br, 123I, 124I, 125I, 131I, and 211At:
- or
- B has the structure:
- to which a metal is chelated.
17 more elements
2-17. (canceled)
19-20. (canceled)
23-24. (canceled)
37-39. (canceled)
41-46. (canceled)
48-51. (canceled)
54-57. (canceled)
60-131. (canceled)
136-141. (canceled)
143-156. (canceled)
Dependencies are inferred from the claim text.