Substituted aminopurine compounds, compositions thereof, and methods of treatment therewith

A method for treating or preventing a cancer characterized by a beta-catenin mutation, the method comprising administering to a subject having cancer characterized by a beta-catenin mutation an effective amount of an Aminopurine Compound of formula (I):

• or a pharmaceutically acceptable salt, tautomer, stereoisomer, enantiomer, or isotopologue thereof,
• wherein:
• R1 is substituted or unsubstituted C1-8 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, or substituted or unsubstituted non-aromatic heterocyclyl;
• R2 is H or substituted or unsubstituted C1-3 alkyl;
• and
• R3 is phenyl, substituted with one or more halogen, optionally further substituted with one or more substituents independently selected from substituted or unsubstituted C1-3 alkyl, CN, and —OR′, wherein each R′ is independently substituted or unsubstituted C1-3 alkyl.

A method for treating or preventing a cancer characterized by an activated beta-catenin pathway, the method comprising administering to a subject having cancer characterized by an activated beta-catenin pathway an effective amount of an Aminopurine Compound of formula (I):

• or a pharmaceutically acceptable salt, tautomer, stereoisomer, enantiomer, or isotopologue thereof,
• wherein:
• R1 is substituted or unsubstituted C1-8 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, or substituted or unsubstituted non-aromatic heterocyclyl;
• R2 is H or substituted or unsubstituted C1-3 alkyl;
• and
• R3 is phenyl, substituted with one or more halogen, optionally further substituted with one or more substituents independently selected from substituted or unsubstituted C1-3 alkyl, CN, and —OR′, wherein each R′ is independently substituted or unsubstituted C1-3 alkyl.

A method for modulating the levels of a biomarker in a subject having a cancer, the method comprising administering to the subject an effective amount of a Aminopurine Compound of formula (I):

• or a pharmaceutically acceptable salt, tautomer, stereoisomer, enantiomer, and isotopologue thereof,
• wherein:
• R1 is substituted or unsubstituted C1-8 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, or substituted or unsubstituted non-aromatic heterocyclyl;
• R2 is H or substituted or unsubstituted C1-3 alkyl;
• and
• R3 is phenyl, substituted with one or more halogen, optionally further substituted with one or more substituents independently selected from substituted or unsubstituted C1-3 alkyl, CN, and —OR′, wherein each R′ is independently substituted or unsubstituted C1-3 alkyl.