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US 11,446,292 B2Granted
Compounds and conjugates thereof
AssigneeMedImmune, LLC
InventorsPhilip Wilson Howard, Niall Dickinson, Thais Cailleau, Luke Masterson, William Goundry
Life of this patent
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Abstract
A conjugate comprising the following topoisomerase inhibitor derivative (A*): with a linker for connecting to a Ligand Unit, wherein the linker is attached in a cleavable manner to the amino residue. The Ligand Unit is preferably an antibody. Also provided is A* with the linking unit attached, and intermediates for their synthesis, as well as the released warhead.
Claims15
A compound with the formula I:
- and salts and solvates thereof, wherein RL is (Ia):
- wherein
- Q is:
- (a) a dipeptide residue selected from:
- NH-Phe-Lys-C═O,
- NH-Val-Ala-C═O,
- NH-Val-Lys-C═O,
- NH Ala-Lys-C═O,
- NH-Val-Cit-C═O,
- NH-Phe-Cit-C═O,
- NH-Leu-Cit-C═O,
- NH-Ile-Cit-C═O,
- NH-Phe-Arg-C═O,
- NH-Trp-Cit-C═O, and
- NH-Gly-Val-C═O;
- or
- (b) a tripeptide residue selected from:
- NH-Glu-Val-Ala-C═O,
- NH-Glu-Val-Cit-C═O,
- NH-αGlu-Val-Ala-C═O, and
- NH-αGlu-Val-Cit-C═O;
- or
- (c) a tetrapeptide residue selected from:
- NH-Gly-Gly-Phe-GlyC═O;
- and
- NH-Gly-Phe-Gly-GlyC═O;
- X is:
- where a=0 to 5, b1=0 to 16, b2=0 to 16, c1=0 or 1, c2=0 or 1, d=0 to 5,
- wherein at least b1 or b2=0 and at least c1 or c2=0;
- and
- GL, is selected from:
28 more elements
Dependencies are inferred from the claim text.