Solid state forms of mavacamten and process for preparation thereof

Abstract

The present disclosure encompasses solid state forms of Mavacamten, in embodiments crystalline polymorphs of Mavacamten, processes for preparation thereof, and pharmaceutical compositions thereof.

1 . A crystalline form of Mavacamten designated as Form 1, characterized by an X-ray powder diffraction pattern having peaks at 11.7, 16.3, 18.7, 20.0 and 23.4 degrees 2-theta±0.2 degrees 2-theta. 
     
     
         2 . The crystalline Form 1 of Mavacamten according to  claim 1 , characterized by an XRPD having peaks at: 11.7, 16.3, 18.7, 20.0 and 23.4 degrees 2-theta±0.2 degrees 2-theta; and further characterized by having one, two or three additional peaks selected from 17.4, 29.1 and 31.6 degrees 2-theta±0.2 degrees 2-theta. 
     
     
         3 . The crystalline Form 1 of Mavacamten according to  claim 2 , wherein said crystalline Form 1 is characterized by an XRPD having peaks at: 11.7, 16.3, 17.4, 18.7, 20.0, 23.4, 29.1 and 31.6 degrees 2-theta±0.2 degrees 2-theta. 
     
     
         4 . The crystalline form of Mavacamten according to  claim 1 , characterized by the X-ray powder diffraction pattern substantially as depicted in  FIG.  1   . 
     
     
         5 . The crystalline Form 1 of Mavacamten according to  claim 1 , wherein said form is an anhydrous form. 
     
     
         6 . A crystalline form of Mavacamten designated as Form 5, characterized by an X-ray powder diffraction pattern having peaks at 13.4, 14.8, 21.8, 23.8 and 24.6 degrees 2-theta±0.2 degrees 2-theta. 
     
     
         7 . The crystalline Form 5 of Mavacamten according to  claim 6 , wherein said crystalline is characterized by an XRPD having peaks at: 13.4, 14.8, 21.8, 23.8 and 24.6 degrees 2-theta±0.2 degrees 2-theta; and further characterized by having one, two, three or four additional peaks selected from 11.9, 15.8, 18.9 and 20.1 degrees 2-theta±0.2 degrees 2-theta. 
     
     
         8 . The crystalline Form 5 of Mavacamten according to  claim 7 , wherein said crystalline Form 5 is characterized by an XRPD having peaks at: 11.9, 13.4, 14.8, 15.8, 18.9, 20.1, 21.8, 23.8 and 24.6 degrees 2-theta±0.2 degrees 2-theta. 
     
     
         9 . The crystalline Form 5 of Mavacamten according to  claim 6 , characterized by the X-ray powder diffraction pattern substantially as depicted in  FIG.  5   . 
     
     
         10 . The crystalline Form 5 of Mavacamten according to  claim 6 , wherein said form is an anhydrous form. 
     
     
         11 . A pharmaceutical composition comprising the crystalline Form 1 of Mavacamten according to  claim 1  and at least one pharmaceutically acceptable excipient. 
     
     
         12 . (canceled) 
     
     
         13 . A process for preparing the pharmaceutical composition according to  claim 11 , comprising combining the crystalline Form 1 of Mavacamten according to  claim 1  with at least one pharmaceutically acceptable excipient. 
     
     
         14 . A medicament comprising the crystalline Form 1 of Mavacamten according to  claim 1 . 
     
     
         15 . (canceled) 
     
     
         16 . A method of treating obstructive hypertrophic cardiomyopathy (oHCM), comprising administering a therapeutically effective amount of the crystalline Form 1 of Mavacamten according to  claim 1  to a subject in need of the treatment. 
     
     
         17 . A pharmaceutical composition comprising the crystalline Form 5 of Mavacamten according to  claim 7  and at least one pharmaceutically acceptable excipient. 
     
     
         18 . A process for preparing a pharmaceutical composition comprising combining the crystalline Form 5 of Mavacamten according to  claim 7  with at least one pharmaceutically acceptable excipient. 
     
     
         19 . A medicament comprising the crystalline Form 5 of Mavacamten according to  claim 7 . 
     
     
         20 . A method of treating obstructive hypertrophic cardiomyopathy (oHCM), comprising administering a therapeutically effective amount of the crystalline Form 5 of Mavacamten according to  claim 7  to a subject in need of the treatment.