Highly Selective TREX1 Inhibitors from Constellation Pharmaceuticals

This article highlights the key drug discovery patents published in August 2024, including AKR1C3-dependent KARS (not KRAS!) inhibitors for NRF2/KEAP1-mutated cancers and DHX9 helicase inhibitors of MSI-high tumors. It also covers the development of MK2 degraders for inflammatory diseases and small molecule IL-17A inhibitors that show promise in modulating inflammation. Additionally, we cover Roche’s take on Revolution Medicines’ macrocyclic pan-KRAS inhibitors, which show improved PK profiles, and novel non-hydroxamate LpxC inhibitors for treating Gram-negative bacterial infections.

This article highlights million-dollar molecules that were recently in the news with related patent applications that give clues to their structures and properties. This edition includes Maze’s glycogen synthase 1 (GYS1) inhibitors that were recently licensed to Sanofi, allosteric androgen receptor (AR) modulators that may be of interest to targeted protein degradation researchers, brain-penetrant HER2 and ROCK2 inhibitors, and MDM2 degraders.

In March 2024, the landscape of patent disclosures continued to reflect the rapid pace of advances against key therapeutic targets. The Drug Hunter team has curated a searchable database encompassing over 200 patents pertinent to the field of drug discovery. This resource is further enriched with insightful spotlight on some of the most promising molecules and targets, including OX2R agonists, TEAD covalent inhibitors, NaV1.8 inhibitors, and selective PI3Kγ inhibitors, among others. This round-up provides a valuable tool for drug hunters to navigate the most recent trends in drug discovery.

This article highlights a patent application from AstraZeneca and Mitsubishi Tanabe, and Astellas Pharma that discloses the biological activity of compounds that act as NLRP3 inhibitors, providing a summary of key data for selected molecules disclosed in the patent application.

To help you quickly scan the patent literature, we’ve distilled down thousands of new documents into a searchable table of over 200 selected patents focused on key areas in drug discovery, all published in June 2024. This resource is enriched with detailed highlights on selected molecules targeting high-interest areas such as synthetically lethal Polθ inhibitors, SARM1 inhibitors for neurodegenerative indications, and our best guess at the identity of Gilead’s small molecule GLP-1R agonist GS-4571