18F-tagged inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer

Patent metadata

Field	Value
Publication number	US-10016519-B2
Application number	US-201715463059-A
Country	US
Kind code	B2
Filing date	Mar 20, 2017
Priority date	Oct 20, 2014
Publication date	Jul 10, 2018
Grant date	Jul 10, 2018

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.

First claim

What is claimed is:

1. A compound of formula (la) or (lb):

with:

n is 0 or 1;

m is 0, 1, 2, 3 or 4, with the proviso that m + n > 0;

Z is —CO 2 H, —SO 2 H, —SO 3 H, —SO 4 H, —PO 2 H, or —PO 4 H 2 ;

X is naphthyl, phenyl, biphenyl, indolyl (=2,3-benzopyrrolyl),

or benzothiazolyl;

Y is aryl, alkylaryl, cyclopentyl, cyclohexyl, or cycloheptyl; and

18 F-Tag is

With:

x = 1-5

wherein the carbohydrate is

With:

x = 1-5

wherein the carbohydrate is

Assignees

• Deutsches Krebsforsch
• Univ Heidelberg Ruprecht Karls
• Deutsches Krebsforschungszentrium

Inventors

• Kopka Klaus
• Benesova Martina
• Cardinale Jens
• Eder Matthias
• Schäfer Martin
• Bauder-Wüst Ulrike
• Haberkorn Uwe
• Eisenhut Michael

Classifications

• C07B59/002

  Heterocyclic compounds · CPC title

• C07D213/82

  in position 3 · CPC title

• C07C275/16

  being further substituted by carboxyl groups · CPC title

• C07B2200/05

  Isotopically modified compounds, e.g. labelled · CPC title

• A61K51/0402

  carboxylic acid carriers, fatty acids (amino acids A61K51/0406) · CPC title