Described are methods for preparing a deuterated aldehyde using with a photocatalyst and a hydrogen atom transfer agent in a H.sub.2O free solvent comprising D.sub.2O and an organic solvent under an inert gas. The methods may be used to convert a wide variety of aldehydes (e.g., aryl, alkyl, or alkenyl aldehydes) to C-1 deuterated aldehydes under mild reaction conditions.

The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds.

The present invention provides compounds that have antimalarial activity. More in particular, the present invention provides novel compounds that are analogues of pantothenamides. The pantothenamide analogues of this invention have particularly low IC.sub.50 values against the asexual blood stages and gametocytes of malaria parasites. Furthermore, the pantothenamide analogues of this invention are characterized by low hepatic metabolism. Therefore, pantothenamide analogues of the invention are particularly suitable for use in therapeutic and/or prophylactic treatment of protozoan infections in a human or animal subject in need thereof. The invention further provides pharmaceutical formulations comprising the pantothenamide analogues as well as the therapeutic and/or prophylactic uses of the pantothenamide analogues and pharmaceutical formulations comprising them.

The present invention provides compounds that have antimalarial activity. More in particular, the present invention provides novel compounds that are analogues of pantothenamides. The pantothenamide analogues of this invention have particularly low IC.sub.50 values against the asexual blood stages and gametocytes of malaria parasites. Furthermore, the pantothenamide analogues of this invention are characterized by low hepatic metabolism. Therefore, pantothenamide analogues of the invention are particularly suitable for use in therapeutic and/or prophylactic treatment of protozoan infections in a human or animal subject in need thereof. The invention further provides pharmaceutical formulations comprising the pantothenamide analogues as well as the therapeutic and/or prophylactic uses of the pantothenamide analogues and pharmaceutical formulations comprising them.

Methods are provided for modulating MRGPRX2 generally, or for treating a MRGPRX2 dependent condition more specifically, by contacting the MRGPRX2 or administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I):

##STR00001##

or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein D, W, Z, R.sup.1, R.sup.2 and R.sup.3 are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

Methods are provided for modulating MRGPRX2 generally, or for treating a MRGPRX2 dependent condition more specifically, by contacting the MRGPRX2 or administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I):

##STR00001##

or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein D, W, Z, R.sup.1, R.sup.2 and R.sup.3 are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder. ##STR00001##

Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder. ##STR00001##

Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound or composition described herein.

Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound or composition described herein.