Nucleoside or nucleotide derivatives, and uses thereof

Inventors

Kim, Kyungjin • Kim, Meehyein • KIM, Uk-Il • Go, Yun Young • NAM, Hwajung • BANG, Hyung Tae • Shin, Jin Soo • Yoon, Jihye • Jang, Yejin

Assignees

ST Pharm Co Ltd

Abstract

The present disclosure relates to a novel nucleoside or nucleotide derivative, a racemate thereof, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition for preventing or treating viral infection-associated diseases, containing the same as an active ingredient.

Core Innovation

The invention relates to a class of compounds represented by Chemical Formula 1, including a racemate, a stereoisomer, or a pharmaceutically acceptable salt thereof. The structure is defined through substituent variables including Y and groups R1 to R6, where Y is heterocyclyl or —NHC(O)R3 and R3 is heteroaryl with defined unsubstituted or substituted options. The allowed heterocyclyl and heteroaryl ring types are enumerated, including tetrahydrofuranyl and related heterocyclic groups, and 5- to 10-membered heteroaryl rings containing nitrogen, oxygen, sulfur, or combinations thereof.

The disclosed structures include stereochemically defined small-molecule examples featuring a substituted tetrahydrofuran-dihydropyrimidin-yl nicotinamide/picolinamide/pyridazine/pyrazole/pyrimidinone/imidazolidinone/pyrrolidinone motif. Representative compounds include nicotinamide and picolinamide amide derivatives bearing difluoro-substituted tetrahydrofuran and dihydropyrimidinone cores, as well as defined phosphonate/phosphate nucleotide ester examples. The disclosure also includes a phosphate ester form and provides the pharmaceutically acceptable forms of these compounds.

The disclosed derivatives are described as antiviral agents intended for preventing or treating viral infection-associated diseases using pharmaceutical compositions containing the Chemical Formula 1 compound. The document enumerates virus targets and disease contexts including HIV, HBV, HCV, influenza, picorna, flavi, alpha virus, phlebovirus, ebola, and coronavirus.

Claims Coverage

The independent claims define a Chemical Formula 1 scaffold with detailed substituent and ring limitations, and include pharmaceutical composition claims using the compound as an active ingredient for viral infection-associated diseases. The independent claims include 3 inventive features.

Overall, the independent claims define Chemical Formula 1 with detailed substituent and ring enumerations and allow racemate, stereoisomer, and pharmaceutically acceptable salt forms. The composition claims use the Chemical Formula 1 compound as the active ingredient for treating enumerated viral infection-associated diseases, with additional formulation components optionally included.

Stated Advantages

Documented Applications