US 12,064,490 B2
Radiolabeled GRPR-Antagonists for Diagnostic Imaging and Treatment of GRPR-Positive Cancer
Theodosia Maina-Nock, Athens (GR); Berthold Artur Nock, Athens (GR); and Marion de Jong Hendriks, TN Vlaardingen (NL)
Assigned to Advanced Accelerator Applications International SA, Geneva (CH)
Filed by Advanced Accelerator Applications International SA, Geneva (CH)
Filed on Jul. 23, 2021, as Appl. No. 17/383,567.
Application 17/383,567 is a continuation of application No. 16/580,990, filed on Sep. 24, 2019, granted, now 11,083,805.
Application 16/580,990 is a continuation of application No. 15/817,776, filed on Nov. 20, 2017, abandoned.
Application 15/817,776 is a continuation of application No. 14/431,096, granted, now 9,839,703, issued on Dec. 12, 2017, previously published as PCT/US2013/061712, filed on Sep. 25, 2013.
Prior Publication US 2022/0008568 A1, Jan. 13, 2022
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 51/08 (2006.01); C07B 59/00 (2006.01)
CPC A61K 51/088 (2013.01) [A61K 51/08 (2013.01); C07B 59/008 (2013.01)] 9 Claims
 
1. A radiolabeled GRPR-antagonist of a formula MC-S-P wherein:
M is a radiometal and C is a metal chelator that binds M,
S is a spacer covalently linked between C and P of formula:

OG Complex Work Unit Chemistry
wherein S is covalently attached to the N-terminus of P;
and P is DPhe-Gln-Trp-Ala-Val-Gly-His-NH—CH[CH2—CH(CH3)2]2 (SEQ ID NO: 1);
wherein M is 177Lu.