PRMT5 inhibitors for cancer treatment

ChangeBridge: Patent Grants - Organic Chemistry (C07D)

Published April 7th, 2026

Detected April 7th, 2026

Summary

USPTO granted patent US12595248B2 to Merck Sharp & Dohme LLC covering PRMT5 inhibitor compounds of Formula I and their use in treating cancer, sickle cell disease, and hereditary persistence of foetal hemoglobin (HPFH). The patent includes 32 claims covering the compound compositions, methods of making, pharmaceutical formulations, and treatment methods.

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What changed

USPTO granted patent US12595248B2 to Merck Sharp & Dohme LLC for PRMT5 (protein arginine methyltransferase 5) inhibitor compounds. The patent claims 32 items covering compounds of Formula I, their pharmaceutically acceptable salts, esters, and prodrugs, along with methods of manufacturing and pharmaceutical compositions.

For pharmaceutical companies developing oncology therapeutics, this patent establishes intellectual property barriers for PRMT5 inhibitor compounds with similar structures or uses. Competitors in the cancer therapeutics space should review this patent landscape before proceeding with R&D in this area to assess freedom-to-operate implications.

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Source document (simplified)

← USPTO Patent Grants

PRMT5 inhibitors

Grant US12595248B2 Kind: B2 Apr 07, 2026

Assignee

Merck Sharp & Dohme LLC

Inventors

Michelle Machacek, Michael D. Altman, Chunghui Huang, Michael H. Reutershan, David L. Sloman, Phieng Siliphaivanh, Sebastian E. Schneider, Charles S. Yeung, David J. Witter, Craig R. Gibeau, Yingchun Ye

Abstract

The present invention provides a compound of Formula (I) and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are PRMT5 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.