# US 2025/0375540 A1 · Fibroblast activation protein targeting precursor and radiotracer

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- Number: US 2025/0375540 A1
- Document ID: US20250375540A1
- Status: Published application
- Kind: A1
- Application number: 18/877,137
- Filed: 2023-06-22
- Published: 2025-12-11
- Earliest claimed: 2022-06-28
- Assignees: ITM Oncologics GmbH
- Applicants: Itm Oncologics GmbH
- Inventors: Frank RÖSCH; Marian MECKEL; Euy Sung MOON
- Web page: https://patentgrep.com/patent/US20250375540A1

## CPC

- A61K 51/0455: {having six-membered rings with one nitrogen as the only ring hetero atom}
- C07D 401/14: containing three or more hetero rings
- A61K 51/0497: {conjugates with a carrier being an organic compounds}
- C07B 59/002: {Heterocyclic compounds}
- A61K 2123/00: Preparations for testing in vivo
- C07B 2200/05: Isotopically modified compounds, e.g. labelled
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)

## Abstract

A precursor compound and radiotracer for targeting fibroblast activation protein comprise a chelator Ch and ligand TV with Ch=(Formula) with R═|—CH3 or |—CH2COOH; and TV=(Formula).

## Claims

### Claim 1

Precursor compound for radiotracer having structure Ch-L1-B-L2-TV, wherein
L1 is a bifunctional linker moiety;
L2 is a bifunctional linker moiety;
B is absent or a bifunctional linker moiety;
L1 is configured to covalently bind to Ch and L2 or to Ch and B, if B is present;
B, if present, is configured to covalently bind to L1 and to L2; and
L2 is configured to covalently bind to L1 and TV or to TV and B, if B is present.

### Claim 2 (depends on 1)

Precursor compound according to claim 1, characterized in that

### Claim 3 (depends on 1)

Precursor compound according to claim 1, characterized in that absent,

### Claim 4 (depends on 1)

Precursor compound according to claim 1, characterized in that
with m=1, 2, 3, 4, 5, 6, 7, 8, 9 or 10.

### Claim 5 (depends on 4)

Precursor compound according to claim 4, characterized in that m=4.

### Claim 6 (depends on 1)

Precursor compound according to claim 1, characterized in that
with n=1, 2, 3, 4, 5, 6, 7, 8, 9 or 10.

### Claim 7 (depends on 6)

Precursor compound according to claim 6, characterized in that n=4.

### Claim 8 (depends on 1)

Precursor compound according to claim 1, characterized in that

### Claim 9 (depends on 1)

Precursor compound according to claim 1, characterized in that

### Claim 10 (depends on 1)

Precursor compound according to claim 1, characterized in that

### Claim 11 (depends on 1)

Precursor compound according to claim 1, characterized in that

### Claim 12 (depends on 1)

Precursor compound according to claim 1, characterized in that it has the structure

### Claim 13 (depends on 1)

Precursor compound according to claim 1, characterized in that it has the structure

### Claim 14 (depends on 1)

Precursor compound according to claim 1, characterized in that it has the structure

### Claim 15 (depends on 1)

Precursor compound according to claim 1, characterized in that it has the structure

### Claim 16 (depends on 1)

Precursor compound according to claim 1, characterized in that it has the structure

### Claim 17 (depends on 1)

Radiotracer comprised of the precursor compound according to claim 1 and therewith complexed radioisotope 68Ga.