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Thiocarbamate derivatives as a2a inhibitors, pharmaceutical composition thereof and combinations with anticancer agents

A composition and solvate technology, applied in pharmaceutical compositions, A2A adenosine receptor inhibitors, oral administration in the treatment of cancer, pharmaceutical compositions and component kits, in the field of treatment and/or prevention of cancer, capable of Addressing issues such as specific combinations of A2AR inhibitor anticancer agents that have not yet been reported

Pending Publication Date: 2021-08-06
ITEOS BELGIUM SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0021] Specific combinations of A2AR inhibitors (especially thiocarbamate derivatives disclosed in WO2018 / 178338) with other anticancer agents have not been reported

Method used

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  • Thiocarbamate derivatives as a2a inhibitors, pharmaceutical composition thereof and combinations with anticancer agents
  • Thiocarbamate derivatives as a2a inhibitors, pharmaceutical composition thereof and combinations with anticancer agents
  • Thiocarbamate derivatives as a2a inhibitors, pharmaceutical composition thereof and combinations with anticancer agents

Examples

Experimental program
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Embodiment Construction

[0136] A2AR inhibitor

[0137] The present invention relates to pharmaceutical compositions and combinations of anticancer agents comprising at least one A2A adenosine receptor (A2AR) inhibitor. A2AR inhibitors are thiocarbamate derivatives, especially those as disclosed in PCT / EP2018 / 058301. More preferably, the A2AR inhibitor is a thiocarbamate derivative of formula (I) as described below.

[0138] In one embodiment, the thiocarbamate derivative A2AR inhibitor has formula (I):

[0139]

[0140] or a pharmaceutically acceptable salt or solvate thereof, wherein:

[0141] R 1 Represents 5 or 6 membered heteroaryl or 5 or 6 membered aryl, wherein heteroaryl or aryl is optionally replaced by one or more selected from C1-C6 alkyl (preferably methyl) and halogen (preferably fluorine or chlorine) substituent substitution; preferably, R 1 represents a 5-membered heteroaryl group; more preferably, R 1 represents a furyl group;

[0142] R 2 Represents 6-membered aryl or 6-me...

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Abstract

The present invention relates to thiocarbamate derivatives of Formula (I) which are useful as A2A adenosine receptor (A2AR) inhibitors (I). 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-alpha-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.

Description

[0001] field of invention [0002] The present invention relates to thiocarbamate derivatives which are useful as A2A adenosine receptor (A2AR) inhibitors. [0003] In particular, the present invention relates to a pharmaceutical composition comprising a thiocarbamate derivative as an adenosine A2A receptor inhibitor. The pharmaceutical composition of the present invention is especially suitable for oral administration in the treatment of cancer. [0004] The present invention also relates to a combination comprising an A2A adenosine receptor (A2AR) inhibitor and an anticancer agent. Said A2AR inhibitor is a thiocarbamate derivative of formula (I) as defined below. The anticancer agent is eg an immunotherapeutic agent, like eg a checkpoint inhibitor. The invention further relates to pharmaceutical compositions and kits of parts comprising said combinations. The combinations according to the invention are especially suitable for the treatment and / or prevention of cancer. [...

Claims

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Application Information

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IPC IPC(8): A61K31/519C07D497/14A61K31/337A61K31/513A61K31/555A61K31/704A61K31/7068A61K45/06A61K47/10A61K47/12A61K47/14A61K47/22A61K9/20A61K9/16A61K9/48A61P35/00
CPCA61K9/4858A61K9/4866A61K31/337A61K31/513A61K31/519A61K31/555A61K31/704A61K31/7068A61K45/06A61P35/00C07D513/14A61K31/5377A61K33/243A61K39/3955C07K16/2803C07K16/2818C07K16/2827C07K2317/76A61K2300/00A61K9/4825A61K47/10A61K47/20
Inventor S.格罗西格纳尼P.迪金森M.德马塔斯E.J.K.H.豪奇斯R.G.马里利尔C.马蒂诺利O.德亨奥G.德里森斯
Owner ITEOS BELGIUM SA
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