Therapeutic radiolabelled conjugates and their use in therapy
AssigneesCentenary Institute of Cancer Medicine and Cell Biology, The University of Sydney
InventorsPhilip HOGG, Ivan HO SHON
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Abstract
The invention relates to compounds according to Formula (I) wherein A is —As(OH)2 or an arsenoxide equivalent group; each of R1, R2, R3 and R4 is independently selected from H, X, OH, NH2, CO, SCN, —CH2NH, —NHCOCH3, —NHCOCH2X or NO, and X is a halogen; R5 is —NHCH2COOH, OH or OR6, wherein R6 is a C1-5 straight or branched alkyl group; and Z is a therapeutic radioisotope, or a pharmaceutically acceptable salt, ester, prodrug or solvate thereof, uses of said compounds, and methods of preparing said compounds. The invention also relates to therapeutic methods utilizing said compounds. The invention further relates to processes for preparing compounds according to Formula (I) wherein Z is a radioisotope.
Claims28
A compound according to Formula (I)
- wherein A is —As(OH)2 or an arsenoxide equivalent group;
- each of R1, R2, R3 and R4 is independently selected from H, X, OH, NH2, CO, SCN, —CH2NH, —NHOOCH3, —NHCOCH2X or NO, and X is a halogen;
- R5 is —NHCH2COOH, OH or OR6, wherein Re is a C1-5 straight or branched alkyl group;
- and Z is a therapeutic radioisotope,
- or a pharmaceutically acceptable salt, ester, prodrug or solvate thereof.
7-13. (canceled)
30-35. (canceled)
37-49. (canceled)
A process for preparing a compound according to Formula (I)
- wherein A is —As(OH)2 or an arsenoxide equivalent group;
- each of R1, R2, R3 and R4 is independently selected from H, X, OH, NH2, CO, SCN, —CH2NH, —NHOOCH3, —NHCOCH2X or NO, and X is a halogen;
- R5 is —NHCH2COOH, OH or OR6, wherein R6 is a C1-5 straight or branched alkyl group;
- and Z is a radioisotope,
- or a pharmaceutically acceptable salt, ester, prodrug or solvate thereof,
- said process comprising adding the radioisotope to a compound according to Formula (II)
- wherein A is —As(OH)2 or an arsenoxide equivalent group;
- each of R1, R2, R3 and R4 is independently selected from H, X, OH, NH2, CO, SCN, —CH2NH, —NHCOCH3, —NHCOCH2X or NO, and X is a halogen;
- R5 is —NHCH2COOH, OH or OR6, wherein R6 is a C1-5 straight or branched alkyl group;
- or a pharmaceutically acceptable salt, ester, prodrug or solvate thereof, wherein the radioisotope is added to the compound of Formula (II) in the presence of glutathione.
51-56. (canceled)
Dependencies are inferred from the claim text.