# US 10,500,292 B2 · PSMA-binding agents and uses thereof

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- Number: US 10,500,292 B2
- Document ID: US10500292B2
- Status: Granted
- Kind: B2
- Application number: 15/864,236
- Filed: 2018-01-08
- Published: 2018-08-23
- Granted: 2019-12-10
- Earliest claimed: 2008-08-01
- Assignees: The Johns Hopkins University
- Applicants: The Johns Hopkins University
- Inventors: Martin G. Pomper; Ronnie Charles Mease; Ying Chen
- Web page: https://patentgrep.com/patent/US10500292B2

## CPC

- A61K 51/0455: {having six-membered rings with one nitrogen as the only ring hetero atom}
- A61K 9/127: Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
- A61K 51/0402: {carboxylic acid carriers, fatty acids (amino acids A61K51/0406)}
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 35/00: Antineoplastic agents
- C07C 275/16: being further substituted by carboxyl groups
- C07C 275/18: of a saturated carbon skeleton containing rings
- C07D 213/61: Halogen atoms or nitro radicals
- C07D 213/74: Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
- C07D 213/82: in position 3
- C07F 7/2208: {Compounds having tin linked only to carbon, hydrogen and/or halogen}
- C07B 2200/05: Isotopically modified compounds, e.g. labelled
- Y02P 20/55: Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)
- Y02P: CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS

## Abstract

Prostate-specific membrane antigen (PSMA) binding compounds having radioisotope substituents are described, as well as chemical precursors thereof. Compounds include pyridine containing compounds, compounds having phenylhydrazine structures, and acylated lysine compounds. The compounds allow ready incorporation of radionuclides for single photon emission computed tomography (SPECT) and positron emission tomography (PET) for imaging, for example, prostate cancer cells and angiogenesis.

## Claims

### Claim 1

A method of preparing a compound of the formula:
the method comprising contacting a compound of the formula:
with TFA, wherein each instance of PMB is p-methoxybenzyl.

### Claim 2 (depends on 1)

The method of claim 1 further comprising contacting a compound of the formula:
with a compound of the formula:
to provide the compound of the formula:

### Claim 3

A method of preparing a compound of the formula:
the method comprising contacting a compound of the formula:
with K18F and K222.

### Claim 4 (depends on 3)

The method of claim 3 further comprising contacting a compound of the formula:
with a compound of the formula:
and NEt3 to provide the compound of the formula: