Selective inhibitor of protein arginine methyltransferase 5 (PRMT5)

Abstract

The disclosure is directed to crystalline forms of the compound of Formula I, pharmaceutically acceptable salts of the compound of Formula I, and crystalline forms thereof. Pharmaceutical compositions comprising said crystalline forms and salts, as well as methods of their use and preparation, are also described.

Description

[0001] CROSS-REFERENCE TO RELATED APPLICATIONS [0002] This application claims the benefit of priority to U.S. Provisional Patent Application No. 62 / 805,175, filed February 13, 2019, and U.S. Provisional Patent Application No. 62 / 805,726, filed February 14, 2019. Each of these applications is hereby incorporated by reference in its entirety. technical field [0003] The present disclosure relates to PRMT5 inhibitors and methods of use thereof. Background technique [0004] Protein arginine methylation is a common post-translational modification that regulates many cellular processes including gene transcription, mRNA splicing, DNA repair, protein cellular localization, cell fate determination and signal transduction. There are three types of methylarginine species: ωNG monomethylarginine (MMA), ωNG, NG asymmetric dimethylarginine (ADMA) and ωNG, N'G symmetric dimethylarginine amino acid (SDMA). The formation of methylated arginine is catalyzed by the protein arginine me...

AI Technical Summary

Problems solved by technology

PRMT5 can directly modify histones H3 and H4, leading to repression of gene expression

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