EGFR inhibitor for the treatment of cancer

Patent metadata

Field	Value
Publication number	US-12344613-B2
Application number	US-202017620239-A
Country	US
Kind code	B2
Filing date	Jun 19, 2020
Priority date	Jun 21, 2019
Publication date	Jul 1, 2025
Grant date	Jul 1, 2025

Abstract

The application relates to a compound of formula (I) containing a thiazole ring, an indazol ring and a 6,7-dihydro-5H-pyrrolo[1,2-c]imidazole ring system, to pharmaceutical compositions containing it and its medical use. The compounds are described as selective allosteric inhibitors of T790M/L858R, T790M/L858R/C797S, L858R, L858R/C797S containing EGFR mutants and thus useful for the treatment of cancer, in particular non-small cell lung cancer.

First claim

The invention claimed is:

1. A compound or a pharmaceutically acceptable salt thereof of formula (I)

2. A compound of formula (I)

3. A pharmaceutical composition comprising the compound or pharmaceutically acceptable salt thereof of claim 1 and a therapeutically inert carrier.

4. A method for treating a cancer in a patient in need thereof, the method comprising administering an effective amount of the compound or pharmaceutically acceptable salt of claim 1 to the patient with cancer, wherein the cancer comprises one or more Epidermal Growth Factor Receptor (EGFR) mutations selected from T790M, L858R, and C797S.

5. A method for treating a non-small cell lung cancer (NSCLC) in a patient in need thereof, the method comprising administering an effective amount of the compound or pharmaceutically acceptable salt of claim 1 to the patient with NSCLC, wherein the NSCLC comprises one or more Epidermal Growth Factor Receptor (EGFR) mutations selected from T790M, L858R, and C797S.

6. A pharmaceutical composition comprising the compound of claim 2 and a therapeutically inert carrier.

7. A method for treating a cancer in a patient in need thereof, the method comprising administering an effective amount of the compound of claim 2 to the patient with cancer, wherein the cancer comprises one or more Epidermal Growth Factor Receptor (EGFR) mutations selected from T790M, L858R, and C797S.

8. A method for treating a non-small cell lung cancer (NSCLC) in a patient in need thereof, the method comprising administering an effective amount of the compound of claim 2 to the patient with NSCLC, wherein the NSCLC comprises one or more Epidermal Growth Factor Receptor (EGFR) mutations selected from T790M, L858R, and C797S.

9. The method according to claim 4 , wherein the cancer comprises EGFR mutations at T790M/L858R, T790M/L858R/C797S, L858R, or L858R/C797S.

10. The method according to claim 5 , wherein the NSCLC comprises EGFR mutations at T790M/L858R, T790M/L858R/C797S, L858R, or L858R/C797S.

Assignees

• Hoffmann La Roche

Inventors

• Dolente Cosimo
• Goergler Annick
• Hewings David
• Jaeschke Georg
• Kuhn Bernd
• Nagel Yvonne Alice
• Obst-Sander Christa Ulrike
• Ricci Antonio
• Rueher Daniel
• Steiner Sandra

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• C07D519/00

  Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00 · CPC title

• A61K47/12

  Carboxylic acids; Salts or anhydrides thereof · CPC title

• A61K47/10

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title

• A61K9/4866

  Organic macromolecular compounds · CPC title