Thiocarbamate derivatives as A2A inhibitors, pharmaceutical composition thereof and combinations with anticancer agents

US11376255B2 · kind B2 · utility

Assignee

• iTeos Belgium SA · BE

Inventors

• Stefano Crosignani · Nivelles, BE
• Erica Joke Katelijne Heleen Houthuys · Petit Enghien, BE
• Reece Gerrad Marillier · Chaumont-Gistoux, BE
• Chiara Martinoli · Milano, IT
• Oliver De Henau · Watermael-Boitsfort - Watermaal-Bosvoorde, BE
• Gregory Driessens · Ottignies, BE

Key dates

• Filing date: Sep 9, 2020
• Grant date: Jul 5, 2022
• Expiry date: Sep 9, 2040

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K2317/76
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to thiocarbamate derivatives of Formula (I) which are useful as A2A adenosine receptor (A2AR) inhibitorsEspecially, the present invention relates to a pharmaceutical composition comprising an A2A inhibitor of Formula (I) and a lipid carrier such as lauroyl macrogol-32 glycerides, D-α-tocopherol-polyethylene glycol-1000 succinate or a mixture thereof. The pharmaceutical composition of the invention is particularly useful for oral dosing in the treatment of cancers. The present invention also relates to a combination comprising an A2A receptor inhibitor of Formula (I) and an anticancer agent. The anticancer agent is for example an immunotherapeutic agent, such as a checkpoint inhibitor. The invention further relates to a pharmaceutical composition and a kit of parts comprising such combination. Additionally, the combination of the invention is particularly useful for the treatment and/or prevention of cancers.