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US 2019/0336622 A1Published application
Labeled inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer
AssigneesDeutsches Krebsforschungszentrum, Ruprecht-Karls-UniversitäT Heidelberg
InventorsMatthias EDER, Klaus KOPKA, Martin SCHÄFER, Ulrike BAUDER-WÜST, Uwe HABERKORN, Michael EISENHUT, Walter MIER, Martina BENESOVA
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Abstract
The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).
Claims14
A compound of Formula (Ia) or (Ib):
- with:
- n:
- 0,1
- m:
- 1,2,3,4
- Z:
- —CO2H, —SO2H, —SO3H, —SO4H, —PO2H, —PO3H,
- —PO4H2
- X:
- Naphthyl, Phenyl, Biphenyl, Indolyl (=2,3-benzopyrrolyl),
- Benzothiazolyl
- Y:
- Aryl, Alkylaryl, Cyclopentyl, Cyclohexyl, Cycloheptyl
- Che-
- 1,4,7,10-tetraazacyclododecane-N,N′,N″,N′″-tetraacetic acid
- lator:
- (=DOTA),
- N,N″-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-
- N,N″-diacetic acid (=HBED-CC),
- 1,4,7-triazacyclononane-1,4,7-triacetic acid (=NOTA),
- 2-(4,7-bis(carboxymethyl)-1,4,7-triazonan-1-yl)pentanedioic acid
- (NODAGA),
- 2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-
- yl)pentanedioic acid
- (DOTAGA),
- 1,4,7-triazacyclononane phosphinic acid (TRAP),
- 1,4,7-triazacyclononane-1-[methyl(2-carboxyethyl)phosphinic
- acid]-4,7-bis[methyl(2-hydroxymethyl)phosphinic acid] (NOPO),
- 3,6,9,15-tetraazabicyclo[9.3.1.]pentadeca-1(15),11,13-triene-3,6,9-
- triacetic acid (=PCTA),
- N′-{5-[Acetyl(hydroxy)amino]pentyl}-N-[5-({4-[(5-
- aminopentyl)(hydroxy)amino]-4-oxobutanoyl}amino)pentyl]-N-
- hydroxysuccinamide (DFO),
- Diethylenetriaminepentaacetic acid (DTPA)
- Trans-cyclohexyl-diethylenetriaminepentaacetic acid (CHX-DTPA)
- 1-oxa-4,7,10-triazacyclododecane-4,7,10-triacetic acid (oxo-Do3A)
- p-isothiocyanatobenzyl-DTPA (SCN-Bz-DTPA)
- 1-(p-isothiocyanatobenzyl)-3-methyl-DTPA (1B3M)
- 2-(p-isothiocyanatobenzyl)-4-methyl-DTPA (1M3B)
- 1-(2)-methyl-4-isocyanatobenzyl-DTPA (MX-DTPA)
37 more elements
Dependencies are inferred from the claim text.