# US 12,006,302 B2 · Tau PET imaging ligands

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- Number: US 12,006,302 B2
- Document ID: US12006302B2
- Status: Granted
- Kind: B2
- Application number: 17/450,212
- Filed: 2021-10-07
- Published: 2022-01-27
- Granted: 2024-06-11
- Earliest claimed: 2016-07-18
- Assignees: Janssen Pharmaceutica NV
- Applicants: Janssen Pharmaceutica NV
- Inventors: José Ignacio Andrés-Gil; Guy Maurits R. Bormans; Lieven Denis Herwig Declercq; Katleen Fierens; Joseph Elisabeth Leenaerts; Diederik Willem Elisabeth Moechars; Frederik Jan Rita Rombouts; Hartmuth Kolb; Wei Zhang
- Web page: https://patentgrep.com/patent/US12006302B2

## CPC

- C07D 401/12: linked by a chain containing hetero atoms as chain links
- A61K 51/0455: {having six-membered rings with one nitrogen as the only ring hetero atom}
- C07B 59/002: {Heterocyclic compounds}
- A61K 2123/00: Preparations for testing in vivo
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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)
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)

## Abstract

The present invention relates to novel, selective radiolabelled tau ligands which are useful for imaging and quantifying tau aggregates, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue or a subject, in vitro or in vivo, and to precursors of said compounds.

## Claims

### Claim 1

A compound according to Formula (P-1)
wherein
R2 is methyl, R1 is H and R3 is selected from the group consisting of Br, —NO2, —[N(CH3)3]+, and 4-CH3—Ph—SO2—O;
or a pharmaceutically acceptable salt or a solvate thereof.

### Claim 2 (depends on 1)

The compound according to claim 1, wherein the compound is
or a pharmaceutically acceptable salt or a solvate thereof.