Patent Highlight: Tau-Targeting Heterobifunctional Degraders from Arvinas for Neurological Diseases

Check out our searchable, annotated database featuring our curated selection of the most important drug discovery patents published in October 2024.

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.

From WRN helicase to KRAS G12V, there were numerous hot targets of interest with patent applications published in January 2024. Here, we curated a searchable table comprising key information for more than 200 patents from January 2024 of potential interest to drug hunters, along with highlights from some of our favorites, including several degraders and molecules targeting Nrf2, KRAS G12V, MAGL, WRN, among others.

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.

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.