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US 2026/0158175 A1Published application
Radiolabeled amino acids for cancer imaging, therapy and corresponding labeling methods thereof
OwnerAnthony Casarez, David A. Nicewicz +1inventors
InventorsAnthony Casarez, David A. Nicewicz, Zibo Li
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Abstract
The disclosure relates to double halogenated phenylalanine derivatives, which can be radiolabeled with PET or SPECT radioisotopes, and their use in treating and/or imaging cancer.
Claims21
A compound of Formula (I):
- wherein:
- X is —O—, —NH—, —N[(C3-C6) cycloalkyl]-, or —N[(C1-C6) alkyl]-;
- R1 and R2 are independently selected from the group consisting of —H, -PG, —CH2Ar, —(C1-C4) alkyl, and —(C3-C7) cycloalkyl;
- or X and R1 together form a (C3-C5) heterocycle;
- R3 is a radioisotope R* selected from the group consisting of [210]At and [211]At, wherein R3 is in the 2-position on the phenyl ring;
- R4 is —F, or radioisotope [18]F;
- R5 is -PG, —(C1-C6) alkyl, or —(C3-C6) cycloalkyl;
- R6 and R7 are independently selected from the group consisting of —H, -PG, —CH2Ar, —(C1-C4) alkyl, and —(C3-C6) cycloalkyl;
- or R6 and R7 together form a (C3-C5) heterocycle;
- PG, in each instance, is a protecting group;
- m is 1, 2, or 3;
- and
- n is 0, 1, or 2;
- or any stereoisomer and/or pharmaceutically acceptable salt thereof.
11 more elements
A compound of Formula (I):
- wherein:
- X is —O—, —NH—, —N[(C3-C6) cycloalkyl]-, or —N[(C1-C6) alkyl]-;
- R1 and R2 are independently selected from the group consisting of —H, -PG, —CH2Ar, —(C1-C4) alkyl, and —(C3-C7) cycloalkyl;
- or X and R1 together form a (C3-C5) heterocycle;
- R3 is a radioisotope R* selected from the group consisting of [210]At and [211]At;
- R4 is —H, —F, or radioisotope [18]F;
- R5 is -PG, —(C1-C6) alkyl, or —(C3-C6) cycloalkyl;
- R6 and R7 are independently selected from the group consisting of —H, -PG, —CH2Ar, —(C1-C4) alkyl, and —(C3-C6) cycloalkyl;
- or R6 and R7 together form a (C3-C5) heterocycle;
- PG, in each instance, is a protecting group;
- m is 0, 1, 2, or 3;
- and
- n is 1 or 2;
- or any stereoisomer and/or pharmaceutically acceptable salt thereof.
11 more elements
Dependencies are inferred from the claim text.