The present invention is directed to compounds of Formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein the substituents A, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b and n are as defined herein. The inventions also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds and methods of preparing the compounds.

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

##STR00001##

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.

Provided are a pyrazole-containing polycyclic derivative inhibitor, a preparation method therefor and an application thereof. In particular, provided are a compound as represented by formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and an application thereof as a P2X3 inhibitor in treatment of P2X3 receptor function disorders, particularly in treatment of neurogenic diseases, wherein the substituents in the formula (I) are the same as those in the description in definition.

##STR00001##

Provided are a pyrazole-containing polycyclic derivative inhibitor, a preparation method therefor and an application thereof. In particular, provided are a compound as represented by formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and an application thereof as a P2X3 inhibitor in treatment of P2X3 receptor function disorders, particularly in treatment of neurogenic diseases, wherein the substituents in the formula (I) are the same as those in the description in definition.

##STR00001##

In accordance with the present disclosure, macrocyclic compounds of formula (I) have been discovered that bind to PD-L1 and are capable of inhibiting the interaction of PD-L1 with PD-1 and CD80. These macrocyclic compounds exhibit in vitro immunomodulatory efficacy thus making them therapeutic candidates for the treatment of various diseases including cancer and infectious diseases.

##STR00001##

In accordance with the present disclosure, macrocyclic compounds of formula (I) have been discovered that bind to PD-L1 and are capable of inhibiting the interaction of PD-L1 with PD-1 and CD80. These macrocyclic compounds exhibit in vitro immunomodulatory efficacy thus making them therapeutic candidates for the treatment of various diseases including cancer and infectious diseases.

##STR00001##

The present invention provides solid forms of an MK2 inhibitor, compositions thereof, and methods of using the same.

The present invention relates to compounds of Formula I

##STR00001##

or pharmaceutically acceptable salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as A2A inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer. The invention also relates to a process for manufacturing compounds of Formula I.

The present invention relates to compounds of Formula I

##STR00001##

or pharmaceutically acceptable salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as A2A inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer. The invention also relates to a process for manufacturing compounds of Formula I.

A method for synthesizing a compound comprising forming a liquid mixture by adding a CH-acid, 2-Mercaptobenzimidazole, and a benzaldehyde component to an ionic liquid of trihexyltetradecylphosphonium bromide. The method may further comprise mixing the liquid mixture at a temperature between 20° C. and 30° C. for a time duration between 17 and 30 minutes, and forming the compound by adding an ethanol-water solution to the mixed liquid mixture with a volume ratio (ethanol-water solution:mixed liquid mixture) between 1:1 and 1.5:1.