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US 2023/0406847 A1Published application
Ligands of prostate specific membrane antigen (psma) containing heteroaromatic linker building blocks
AssigneeAbx Advanced Biochemical Compounds GmbH
InventorsAlexander HOEPPING, Hans-Joachim LANKAU, Ronny HESSE, Klaus KOPKA, Ulrike BAUDER WÜST, Christian LIS, René SMITS, Jan MOLLITOR, Kristine SCHEIBE, Alexandra GEISSLER
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Abstract
The present invention relates to novel compounds that bind to the prostate-specific membrane antigen (PSMA)-binding and their use in the diagnosis and treatment of certain diseases where PSMA is upregulated.
Claims21
A compound of Formula I
- wherein
- C is represented by any of the structures selected from the group consisting of
- 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA),
- N,N″-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N″-diacetic acid (HBED-CC),
- 1,4-bis(carboxymethyl)-6-[bis(carboxymethyl)]amino-6-methylperhydro-1,4-diazepine (AAZTA),
- 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA),
- 2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl)pentanedioic acid (DOTAGA),
- N4-[5-[[4-[[5-(acetylhydroxyamino)pentyl]amino]-1,4-dioxobutyl]hydroxyamino]pentyl]-N1-(5-aminopentyl)-N1-hydroxybutanediamide (DFO),
- N1-[5-(acetylhydroxyamino)pentyl]-N26 -(5-aminopentyl)-N26,5,16-trihydroxy-4,12,15,23-tetraoxo-5,11,16,22-tetraazahexacosanediamide (DFO*), or
- 5-[(2-mercapto-2-methylpropyl)[2-[(2-mercapto-2-methylpropyl)amino]ethyl]amino]pentanoic acid (BAT),
- L is C1-C5-heteroaryl, optionally substituted with C1-C6 alkyl,
- X is NH or CH2,
- k is 0, 1 or 2,
- m is an integer from 1 to 7,
- n is an integer from 0 to 6,
- p is 0 or 1,
- R1 is phenyl, phenyl-NH—, benzothiophenyl or naphthyl,
- wherein phenyl and phenyl-NH— is optionally substituted with 1, 2 or 3 groups each independently selected from halo, OH and NO2, and
- R2 is aryl, aryl-C(O)—, or heteroaryl-C(O)—, optionally substituted with 1, 2 or 3 groups each independently selected from halo, OH, C1-C6-alkyl, OCH3 and NO2,
- wherein C1-C5-heteroaryl contains 1, 2, 3 or 4 heteroatoms, each independently selected from N, O or S,
- or a pharmaceutically acceptable salt thereof or a solvate thereof or a solvate of a salt thereof.
18 more elements
Dependencies are inferred from the claim text.