Invention Grant
- Patent Title: Thiocarbamate derivatives as A2A inhibitors, pharmaceutical composition thereof and combinations with anticancer agents
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Application No.: US17015850Application Date: 2020-09-09
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Publication No.: US11376255B2Publication Date: 2022-07-05
- Inventor: Stefano Crosignani , Erica Joke Katelijne Heleen Houthuys , Reece Gerrad Marillier , Chiara Martinoli , Oliver De Henau , Gregory Driessens
- Applicant: iTeos Belgium SA
- Applicant Address: BE Gosselies
- Assignee: iTeos Belgium SA
- Current Assignee: iTeos Belgium SA
- Current Assignee Address: BE Gosselies
- Agency: Goodwin Procter LLP
- Priority: BE2018/0103 20180911,BE2018/0114 20180927
- Main IPC: A61K31/519
- IPC: A61K31/519 ; A61P35/00 ; A61K31/5377 ; A61K33/243 ; A61K9/48 ; A61K31/704 ; A61K39/395

Abstract:
The present invention relates to thiocarbamate derivatives of Formula (I) which are useful as A2A adenosine receptor (A2AR) inhibitors Especially, 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.
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