Substituted phenyl-1H-pyrrolo[2,3-c]pyridine derivatives

JP2024521879A5Pending Publication Date: 2026-07-03JANSSEN PHARMA NV
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
JANSSEN PHARMA NV
Filing Date
2022-05-30
Publication Date
2026-07-03

AI Technical Summary

Technical Problem

Current therapeutic approaches for chromosomal rearrangements affecting mixed lineage leukemia (MLL) and related diseases such as leukemia, myelodysplastic syndrome (MDS), and myeloproliferative neoplasms (MPN) are inadequate, highlighting the need for new strategies to target the menin/MLL protein interaction.

Method used

Development of substituted phenyl-1H-pyrrolo[2,3-c]pyridine derivatives that act as menin/MLL protein interaction inhibitors, potentially disrupting the oncogenic activity of MLL fusion proteins and inhibiting HOX/MEIS1 gene expression.

Benefits of technology

These compounds demonstrate improved metabolic stability, oral bioavailability, and extended in vivo half-life, effectively inhibiting tumor growth and reducing HOX/MEIS1 gene expression, offering a promising therapeutic option for leukemia and other cancers with MLL gene rearrangements.

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Abstract

The present invention relates to medicaments useful for the treatment and / or prevention in mammals, pharmaceutical compositions comprising such compounds, and their use as menin / MLL protein / protein interaction inhibitors useful in the treatment of diseases such as cancer, including but not limited to leukemia, myelodysplastic syndrome (MDS), and myeloproliferative neoplasm (MPN); and diabetes.
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