PSMA binding ligand-linker conjugates and methods for using
First Claim
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1. A compound of the formula
B-L-Dor a salt thereof, whereinB is a ligand of prostate specific membrane antigen (PSMA) comprising a urea of two amino acids, wherein each amino acid is independently an aminoalkylcarboxylate substituted with alkyl, hydroxyalkyl, sulfhydrylalkyl, aminoalkyl, or carboxyalkyl;
- L is a linker comprising a carbonyl and a divalent radical selected from the group consisting of alkane, alkene, alkyne, cycloalkane, arylene, and imide and the linker has a molecular weight of 30 to 300 g/mol; and
D is a radioisotope covalently bound to the linker.
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Abstract
Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.
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Citations
15 Claims
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1. A compound of the formula
B-L-Dor a salt thereof, wherein B is a ligand of prostate specific membrane antigen (PSMA) comprising a urea of two amino acids, wherein each amino acid is independently an aminoalkylcarboxylate substituted with alkyl, hydroxyalkyl, sulfhydrylalkyl, aminoalkyl, or carboxyalkyl; -
L is a linker comprising a carbonyl and a divalent radical selected from the group consisting of alkane, alkene, alkyne, cycloalkane, arylene, and imide and the linker has a molecular weight of 30 to 300 g/mol; and D is a radioisotope covalently bound to the linker. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14)
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15. A compound of the formula
B-L-Dor a salt thereof, wherein B is a ligand of prostate specific membrane antigen (PSMA) comprising a urea of two amino acids, wherein each amino acid is independently an aminoalkylcarboxylate substituted with alkyl, hydroxyalkyl, sulfhydrylalkyl, amino alkyl, or carboxyalkyl; -
L is a linker comprising a carbonyl and a divalent radical selected from the group consisting of alkane, alkene, alkyne, cycloalkane, arylene, and imide and the linker does not have an arylalkyl sidechain; and D is a radioisotope covalently bound to the linker.
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Specification