US 11,376,255 B2 · Thiocarbamate derivatives as A2A inhibitors, pharmaceutical composition thereof and combinations with anticancer agents

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.

Claims6

Dependent claims

A method of treating cancer in a patient in need thereof, the method comprising administering to the patient a therapeutically acceptable effective amount of a combination comprising:

(S)-5-amino-3-(2-(4-(2,4-difluoro-5-(2-(methylsulfinyl)ethoxy)phenyl)piperazin-1-yl)ethyl)-8-(furan-2-yl)thiazolo[5,4-e][1,2,4]triazolo[1,5-c]pyrimidin-2(3H)-one, or a pharmaceutically acceptable salt thereof;
and
a checkpoint inhibitor selected from the group consisting of a PD-1 antibody and a PD-L1 antibody.

Dependencies are inferred from the claim text.

Facts

Application

17/015,850Filed 9 Sep 2020 · continuation

Priority

BE 2018/010311 Sep 2018

Published

US 2021/0069196 A111 Mar 2021

Granted

5 Jul 2022

Term ends

Not estimatedThe source records don’t support an estimate.

Classification24 codes

A61K 31/519
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim: ortho- or peri-condensed with heterocyclic rings
A61K 9/4858
Filling excipients; Inactive ingredients: organic compounds
A61K 9/4866
Filling excipients; Inactive ingredients: organic macromolecular compounds
A61K 31/337
Having oxygen as the only ring hetero atom, e.g. fungichromin: having four-membered rings, e.g. taxol

Family

Application62/729,808Us provisional application · filed 11 Sep 2018

Application62/737,723Us provisional application · filed 27 Sep 2018

PCT/EP2019/074208Parent of this continuation · filed 11 Sep 2019

US 2021/0069196 A1Pre-grant publication · published 11 Mar 2021

US 11,376,255 B2This patent

From the US filing history. Foreign family members aren’t listed.

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

Life of this patent

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

Life of this patent

Abstract

Claims6