IP Library Granted Patent US 12,459,920
Granted Patent B2
US 12,459,920 · App. 19/183,531 · Granted Nov 4, 2025

Targeted protein degradation

Inventors: Elisa Liardo (Basel, CH); Laura Ann McAllister (Basel, CH); Bernhard Fasching (Basel, CH)
Assignee: Monte Rosa Therapeutics AG
C07D401/12A61K31/506A61P29/00C07B2200/09
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 12,459,920
App. No.
19/183,531
Granted
Nov 4, 2025
Kind
B2
Abstract

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt thereof) that degrade and/or otherwise modulate (e.g., inhibit) NIMA Related Kinase 7 (NEK7). Said chemical entities are useful, e.g., for treating a subject (e.g., a human subject) having one or more disorders or diseases associated with NLRP3 inflammasome activation. Said disorders or diseases include but are not limited to, autoinflammatory and autoimmune disorders (e.g., gout, inflammatory bowel disease, rheumatoid arthritis, multiple sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease), cardiovascular and metabolic disorders (eg. pericarditis, atherosclerosis, Type 2 diabetes, obesity, and metabolic syndrome), fibrotic disorders (e.g. interstitial lung disease, chronic kidney disease), hematology (eg, anemia of inflammation) and eye disorders (eg. macular degeneration). In embodiments, and while not wishing to be bound by theory, it is believed that the chemical entities described herein directly target (e.g., directly bind to) NEK7, thereby altering (e.g., attenuating) the inflammatory response modulated by the NLRP3 inflammasome. This disclosure also features compositions containing the same as well as methods of using and making the same.

Claims (9)

1 . A compound having the structure:

or a pharmaceutically acceptable salt thereof.

2 . The compound according to claim 1 having the structure:

or a pharmaceutically acceptable salt thereof.

3 . The compound according to claim 1 having the structure:

or a pharmaceutically acceptable salt thereof.

4 . The compound according to claim 1 , or a pharmaceutically acceptable salt thereof,

wherein the compound is in racemic mixture.

5 . A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 11, 2025
From: LIARDO, ELISA; MCALLISTER, LAURA ANN; FASCHING, BERNHARD
To: MONTE ROSA THERAPEUTICS AG
Reel/Frame 071681/0062 →
Continuity (3)
Continuation PCTUS2024039292 · Jul 24, 2024
Provisional Application 63528823 · Jul 25, 2023
Related Publication 20250243180A1 · Jul 31, 2025
References Cited (41)
US 20220313827A1 · Phillips et al. · 2022 [cited by applicant]
US 20240374738A1 · Su et al. · 2024 [cited by applicant]
US 20250041429A1 · Lee et al. · 2025 [cited by applicant]
US 20250059162A1 · Yang et al. · 2025 [cited by applicant]
EP 2308838A1 · 2011 [cited by applicant]
EP 3455219A1 · 2019 [cited by applicant]
EP 3641762A1 · 2020 [cited by applicant]
EP 3684366A1 · 2020 [cited by applicant]
EP 3817822A1 · 2021 [cited by applicant]
EP 3897631A1 · 2021 [cited by applicant]
EP 4031243A1 · 2022 [cited by applicant]
EP 4039688A2 · 2022 [cited by applicant]
EP 4114392A1 · 2023 [cited by applicant]
EP 4334302A1 · 2024 [cited by applicant]
JP 2011157349A · 2011 [cited by applicant]
WO 2022161414A1 · 2022 [cited by applicant]
WO 2022235698A1 · 2022 [cited by applicant]
WO 2022268052A1 · 2022 [cited by applicant]
WO 2022272074A1 · 2022 [cited by applicant]
WO 2023072270A1 · 2023 [cited by applicant]
WO 2023080732A1 · 2023 [cited by applicant]
WO 2023098656A1 · 2023 [cited by applicant]
WO 2023116835A1 · 2023 [cited by applicant]
WO 2023125907A1 · 2023 [cited by applicant]
WO 2023143249A1 · 2023 [cited by applicant]
WO 2023177451A1 · 2023 [cited by applicant]
WO 2023192578A1 · 2023 [cited by applicant]
WO 2023227080A1 · 2023 [cited by applicant]
WO 2023245327A1 · 2023 [cited by applicant]
WO 2024073871A1 · 2024 [cited by applicant]
WO 2024188209A1 · 2024 [cited by applicant]
WO 2025016457A1 · 2025 [cited by applicant]
WO 2025024521A1 · 2025 [cited by applicant]
Devant, P., et al., “Molecular mechanisms of gasdermin D pore-forming activity”, Nature Immunology, 24:1064-1075 (2023). [cited by applicant]
Fu, J., et al., “Structural Mechanisms of NLRP3 Inflammasome Assembly and Activation”, Annual Review of Immunology, 41:301-16 (2023). [cited by applicant]
International Search Report and Written Opinion for International Patent Application No. PCT/US2024/039292, mailed Nov. 27, 2024. [cited by applicant]
Mangan, M. S. J., et al. “Targeting the NLRP3 inflammasome in inflammatory diseases”, Nat. Rev. Drug Discov., 17:588-606 (2018). [cited by applicant]
McKee, C. M., et al., “NLRP3 inflammasome priming: A riddle wrapped in amystery inside an enigma”, J. Leuk. Biol., 108:937-952 (2020). [cited by applicant]
Mullard, A., “NLRP3 inhibitors stoke anti-inflammatory ambitions”, Nat. Rev. Drug Discov., 18:405-407 (2019). [cited by applicant]
Sharif, H., et al., “Structural mechanism for NEK7-licensed activation of NLRP3 inflammasome”, Nature, 570(7761):338-343 (2019). [cited by applicant]
Taldo, S., et al., “Targeting The NLRP3 Inflammasome In Cardiovascular Diseases”, Pharmacology & Therapeutics, 236(108053):1-20 (2022). [cited by applicant]