IP Library › Granted Patent US 12,485,179
Granted Patent B2
US 12,485,179 · App. 17/739,873 · Granted Dec 2, 2025

Cholecystokinin B receptor targeting for imaging and therapy

Inventors: Philip Stewart Low (West Lafayette, IN); Charity Wayua (West Lafayette, IN)
Assignee: Purdue Research Foundation
A61K47/545A61K31/4409A61K31/475A61K38/06A61K38/07A61K49/0052A61K51/02A61K51/0468A61K51/047C07D243/12C07D405/12
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Quick Facts
Patent No.
US 12,485,179
App. No.
17/739,873
Granted
Dec 2, 2025
Kind
B2
Abstract

Conjugates are described herein where CCK2R targeting ligands are attached to an active moiety, such as therapeutic agent or an imaging agent, through a linker. The conjugates can be used in the detection, diagnosis, imaging and treatment of cancer.

Claims (29)

1 . A method for detecting a tumor in a subject, comprising administering a conjugate of formula B-L-D, or a pharmaceutically acceptable salt thereof, to a subject suspected of having a tumor and detecting the conjugate in the subject, wherein:

B is a targeting ligand of Formula I

wherein the wavy line represents the point of connection of B to L;

L is a releasable polyvalent linker; and

D is an optical dye.

2 . The method of claim 1 , wherein the optical dye is of Formula II

wherein

X is selected from the group consisting of oxygen, —NH, and sulfur, and X is attached to the linker L;

Y is selected from the group consisting of OR a , NR a 2 , and NR a 3 + ;

Y′ is selected from the group consisting of O, NR a , and NR a 2 + ;

each R is independently selected from the group consisting of H, fluoro, sulfonic acid, sulfonate, and salts thereof; and

R a is hydrogen or alkyl.

3 . The method of claim 2 , wherein X is —NH.

4 . The method of claim 2 , wherein each R is H.

5 . The method of claim 2 , wherein Y is H.

6 . The method of claim 2 , wherein Y′ is O.

7 . The method of claim 1 , wherein the optical dye is of Formula III

wherein X is selected from the group consisting of oxygen, nitrogen, and sulfur, and X is attached to linker L.

8 . The method of claim 2 , wherein X is nitrogen.

9 . The method of claim 1 , wherein the optical dye is selected from the group consisting of fluorescein (FITC), rhodamine, S0456, IR800CW, and LS288.

10 . The method of claim 1 , wherein the linker L comprises at least one amino acid.

11 . The method of claim 1 , wherein the linker L comprises glutamic acid.

12 . The method of claim 1 , wherein the linker L comprises a carbamate moiety.

13 . The method of claim 1 , wherein the linker L is L1, L2 or L3

—HN-Glu-Arg-Asp-CO—  L1

—HN-Glu-PS-Glu-PS—CO—  L2

—HN-Octanoyl-Glu-PS-Glu-PS—CO—  L3

wherein PS is a radical of formula:

14 . The method of claim 1 , wherein the conjugate is of formula

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 3, 2023
From: LOW, PHILIP STEWART; WAYUA, CHARITY
To: PURDUE RESEARCH FOUNDATION
Reel/Frame 063208/0047 →
Continuity (5)
Continuation 16942537 · Jul 29, 2020
Continuation 16105734 · Aug 20, 2018
Continuation 14380273
Provisional Application 61602831 · Feb 24, 2012
Related Publication 20220273803A1 · Sep 1, 2022
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