Thiocarbamate derivatives as A2A inhibitors, pharmaceutical composition thereof and combinations with anticancer agents
申请人:iTeos Belgium SA
公开号:US11376255B2
公开(公告)日:2022-07-05
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.
本发明涉及可用作 A2A 腺苷受体(A2AR)抑制剂的式 (I) 硫代氨基甲酸酯衍生物
特别是,本发明涉及一种药物组合物,该组合物包含式(I)的 A2A 抑制剂和脂质载体,例如月桂酰基大环醇-32 甘油酸酯、D-α-生育酚-聚乙二醇-1000 丁二酸酯或它们的混合物。本发明的药物组合物特别适用于治疗癌症的口服剂量。本发明还涉及一种由式(I)的 A2A 受体抑制剂和抗癌剂组成的组合物。抗癌剂例如是免疫治疗剂,如检查点抑制剂。本发明还涉及一种药物组合物和包含这种组合物的部件试剂盒。此外,本发明的组合物特别适用于治疗和/或预防癌症。