# US 10,870,629 B2 · 18F-labelled compound for prostate cancer diagnosis, and use thereof

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- Number: US 10,870,629 B2
- Document ID: US10870629B2
- Status: Granted
- Kind: B2
- Application number: 16/622,518
- Filed: 2018-06-18
- Published: 2020-07-02
- Granted: 2020-12-22
- Earliest claimed: 2017-06-19
- Assignees: Futurechem Co., Ltd.
- Applicants: Futurechem Co., Ltd.
- Inventors: Dae Yoon Chi; Byoung Se Lee; So Young Chu; Woon Jung Jung; Hyeon Jin Jeong; Min Hwan Kim; Mi Hyun Kim; Kyo Chul Lee; Yong Jin Lee; Ji Ae Park; Ran Ji Yoo; Sang Moo Lim
- Web page: https://patentgrep.com/patent/US10870629B2

## CPC

- A61K 51/0402: {carboxylic acid carriers, fatty acids (amino acids A61K51/0406)}
- C07D 249/04: 1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
- A61K 49/085: {conjugated systems}
- A61K 49/10: Organic compounds
- A61K 51/04: Organic compounds
- A61K 51/0497: {conjugates with a carrier being an organic compounds}
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- 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)

## Abstract

The present invention relates to an 18F-labelled compound, and a use thereof. The compound selectively binds to a prostate-specific membrane antigen (PSMA), and enables the acquisition of clear prostate cancer images in a short time when used in positron emission tomography (PET).

## Claims

### Claim 1

A compound represented by the following formula 1:
wherein,
Y is C1-C5 alkylene;
Z is —CH2—(CH2—O—CH2)n—CH2—, wherein n is an integer of 0 to 5;
R is hydrogen or C1-C2 alkyl having a substituent, wherein the substituent is C6-C12 aryl or C4-C10 heteroaryl containing one or more elements selected from the group consisting of O, S and N; and
F is 18F or 19F.

### Claim 2 (depends on 1)

The compound according to claim 1, wherein Y is C1-C2 alklylene and F is 18F.

### Claim 3

A compound represented by A the following formula 11:
wherein,
Y is C1-C5 alkylene; and
R is hydrogen or C1-C2 alkyl having a substituent, wherein the substituent is C6-C12 aryl or C4-C10 heteroaryl containing one or more elements selected from the group consisting of O, S and N.

### Claim 4 (depends on 3)

The compound according to claim 3, wherein Y is C1-C2 alkylene.

### Claim 5 (depends on 1)

A pharmaceutical composition for treating or diagnosing prostate cancer comprising a compound of claim 1 or a pharmaceutically acceptable salt thereof as an active ingredient.

### Claim 6 (depends on 1)

A radiopharmaceutical for imaging diagnosis of prostate cancer comprising a compound of claim 1 or a pharmaceutically acceptable salt thereof as an active ingredient.

### Claim 7 (depends on 6)

The radiopharmaceutical according to claim 6, wherein the imaging diagnosis includes magnetic resonance imaging (MRI) or positron emission tomography (PET).

### Claim 8 (depends on 5)

A method for treating or diagnosing prostate cancer in a subject, said method comprising administering to the subject the pharmaceutical composition of claim 5.

### Claim 9 (depends on 6)

A method for diagnostically imaging prostate cancer in a subject, said method comprising administering to the subject the radiopharmaceutical of claim 6.