The present invention concerns a compound of following formula (I): where: —R.sub.1 is H or OH, —R.sub.2 is a (C.sub.1-C.sub.6)alkyl, COOH, COO—((C.sub.1-C.sub.6)alkyl) or thiazolyl group, —R.sub.3 is H or a (C.sub.1-C.sub.6)alkyl group, and —R.sub.4 is: .square-solid.a straight-chain or branched, saturated or unsaturated hydrocarbon group having 1 to 8 carbon atoms substituted by one or more groups chosen from among OH and NR.sub.5R.sub.6, .square-solid.—(CH.sub.2CH.sub.2X.sub.1)(CH.sub.2CH.sub.2X.sub.2).sub.a2(CH.sub.2CH.sub.2X.sub.3).sub.a3(CH.sub.2CH.sub.2X.sub.4).sub.a4(CH.sub.2CH.sub.2X.sub.5).sub.a5R.sub.7, .square-solid.an aryl-(C.sub.1-C.sub.8)alkyl group substituted by one or more groups chosen from among OH and NR.sub.9R.sub.10 groups, or .square-solid.a heterocycle-(C.sub.1-C.sub.8)alkyl group optionally substituted by one or more groups chosen from among (C.sub.1-C.sub.6)alkyl, OH and NR.sub.12R.sub.13 groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.

##STR00001##

The present invention concerns a compound of following formula (I): where: —R.sub.1 is H or OH, —R.sub.2 is a (C.sub.1-C.sub.6)alkyl, COOH, COO—((C.sub.1-C.sub.6)alkyl) or thiazolyl group, —R.sub.3 is H or a (C.sub.1-C.sub.6)alkyl group, and —R.sub.4 is: .square-solid.a straight-chain or branched, saturated or unsaturated hydrocarbon group having 1 to 8 carbon atoms substituted by one or more groups chosen from among OH and NR.sub.5R.sub.6, .square-solid.—(CH.sub.2CH.sub.2X.sub.1)(CH.sub.2CH.sub.2X.sub.2).sub.a2(CH.sub.2CH.sub.2X.sub.3).sub.a3(CH.sub.2CH.sub.2X.sub.4).sub.a4(CH.sub.2CH.sub.2X.sub.5).sub.a5R.sub.7, .square-solid.an aryl-(C.sub.1-C.sub.8)alkyl group substituted by one or more groups chosen from among OH and NR.sub.9R.sub.10 groups, or .square-solid.a heterocycle-(C.sub.1-C.sub.8)alkyl group optionally substituted by one or more groups chosen from among (C.sub.1-C.sub.6)alkyl, OH and NR.sub.12R.sub.13 groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.

##STR00001##

The present invention provides compounds, compositions thereof, and methods of using the same.

The present invention provides compounds, compositions thereof, and methods of using the same.

Provided are compounds of Formula (I): (I) and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

##STR00001##

The present invention provides a compound of Formula (I): (I); an enantiomer, diastereoisomer, atropisomer thereof, a mixture thereof, or a pharmaceutically acceptable salt thereof, that inhibits voltage-gated sodium channels, in particular NaV1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders, cough, and itch. Also provided are pharmaceutical compositions containing the compounds of the present invention. Also further provided is an atropi-selective preparation of said compounds of Formula (I), and intermediate thereof.

##STR00001##

The present invention provides a compound of Formula (I): (I); an enantiomer, diastereoisomer, atropisomer thereof, a mixture thereof, or a pharmaceutically acceptable salt thereof, that inhibits voltage-gated sodium channels, in particular NaV1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders, cough, and itch. Also provided are pharmaceutical compositions containing the compounds of the present invention. Also further provided is an atropi-selective preparation of said compounds of Formula (I), and intermediate thereof.

##STR00001##

Improved processes for the preparation of tubulysin compounds, tubulysin drug linker compounds, and their intermediates are disclosed.

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or prodrug, and/or tautomer, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same. Formula (I).

##STR00001##

The present disclosure is directed to use of MrgprX2 antagonists in the treatment of inflammatory disorders, e.g., inflammatory disorders of the skin. This invention is also directed to pharmaceutical compositions comprising a MrgprX2 antagonist and a pharmaceutically acceptable carrier for topical or oral administration.