Bromodomain inhibitor

Abstract

Described herein is the bromodomain inhibitor 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one, including crystalline forms, amorphous forms, solvates, and hydrates thereof, as well as pharmaceutical compositions that include this bromodomain inhibitor. In some embodiments, the pharmaceutical composition comprises 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one that has been processed by micronization or spray dried dispersion. In some embodiments, the pharmaceutical composition further comprises at least one polymer. In some embodiments, the pharmaceutical composition comprises a solid polymer matrix comprising 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one and at least one polymer. Pharmaceutical compositions comprising 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one are useful for the treatment of cancer or neoplastic disease.

1 - 22 . (canceled) 
     
     
         23 . A method of modulating epigenetic regulation in a subject mediated by one or more proteins comprising acetyl-lysine recognition motifs or a mutant thereof, the method comprising administering to the subject a pharmaceutical composition comprising 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one. 
     
     
         24 . A method of inhibiting the activity of a bromodomain-containing protein or a mutant thereof in a subject, the method comprising administering to the subject a pharmaceutical composition comprising 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one. 
     
     
         25 . The method of  claim 23 , wherein the one or more proteins comprise a BET (bromodomain and extra-terminal domain) protein. 
     
     
         26 . The method of  claim 25 , wherein the BET (bromodomain and extra-terminal domain) protein is BRD4. 
     
     
         27 . The method of  claim 24 , wherein the bromodomain-comprising protein comprises a BET (bromodomain and extra-terminal domain) protein. 
     
     
         28 . The method of  claim 27 , wherein the BET (bromodomain and extra-terminal domain) protein is BRD4.