Pyrazole-based radionuclide-containing neurotensin receptor ligands
Pyrazole-based neurotensin receptor ligands address the limitations of existing NTSR1-targeted RLTs by enhancing selectivity and stability, improving cancer treatment through optimized tumor targeting and biodistribution.
WO2026136398A1PCT designated stage Publication Date: 2026-06-25ELI LILLY & CO
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Patent Information
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- ELI LILLY & CO
- Filing Date
- 2025-12-16
- Publication Date
- 2026-06-25
AI Technical Summary
Technical Problem
Existing neurotensin receptor 1 (NTSR1)-targeted radioligand therapies (RLTs) lack improved selectivity, potency, stability, and biodistribution for effective cancer treatment.
Method used
Development of pyrazole-based neurotensin receptor ligands with specific structural components, including various substituents and linkers, to enhance targeting and stability, allowing for improved tumor localization and therapeutic efficacy.
Benefits of technology
The pyrazole-based neurotensin receptor ligands demonstrate enhanced selectivity and stability, leading to improved cancer treatment outcomes by optimizing tumor targeting and biodistribution.
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Figure US2025059895_25062026_PF_FP_ABST
Abstract
The present invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, Z, Q, X1, Cy1, X2, L1, Ch1, and M1 are as defined herein. The present invention also provides pharmaceutical compositions including the compounds, methods of using the compounds for the treatment of disease, and methods of making the compounds.
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