Creatine prodrugs, compositions and methods of use thereof
AssigneeFarmington Pharma Development
InventorWilliam F. Brubaker
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Abstract
The invention describes membrane permeable creatine prodrugs, pharmaceutical compositions comprising membrane permeable creatine prodrugs, and methods of treating diseases such as ischemia, heart failure, neurodegenerative disorders and genetic disorders affecting the creatine kinase system comprising administering creatine prodrugs or pharmaceutical compositions thereof. The invention also describes treating a genetic disease affecting the creatine kinase system, such as, for example, a creatine transporter disorder or a creatine synthesis disorder comprising administering creatine prodrugs or pharmaceutical compositions thereof.
Claims20
A compound of Formula (VI), or a pharmaceutically acceptable salt, or tautomer thereof, wherein:
- R is —CH3 or —CD3;
- R10 is hydrogen, C1-12 alkyl, substituted C1-12 alkyl, C1-12 heteroalkyl, substituted C1-12 heteroalkyl, C3-12 cycloalkyl, substituted C3-12 cycloalkyl, C4-20 cycloalkylalkyl, substituted C4-20 cycloalkylalkyl, C4-20 heterocycloalkylalkyl, substituted C4-20 heterocycloalkylalkyl, C5-12 aryl, substituted C5-12 aryl, C5-12 heteroaryl, substituted C5-12 heteroaryl, C6-20 arylalkyl, substituted C6-20 arylalkyl, C6-20 heteroarylalkyl, or substituted C6-20 heteroarylalkyl;
- R11 is hydrogen or —OR13;
- and
- R12 is hydrogen, —OR13 or —C(O)R5, with the proviso that both R11 and R12 cannot be hydrogen;
- R13 is independently hydrogen, C1-12 alkyl, or substituted C1-12 alkyl;
- and
- R5 is hydrogen, C2-12 alkyl, substituted C2-12 alkyl, C1-12 heteroalkyl, substituted C1-12 heteroalkyl, C3-12 cycloalkyl, substituted C3-12 cycloalkyl, C4-20 cycloalkylalkyl, substituted C4-20 cycloalkylalkyl, C4-20 heterocycloalkylalkyl, substituted C4-20 heterocycloalkylalkyl, C5-12 aryl, substituted C5-12 aryl, C5-12 heteroaryl, substituted C5-12 heteroaryl, C6-20 arylalkyl, substituted C6-20 arylalkyl, C6-20 heteroarylalkyl or substituted C6-20 heteroarylalkyl.
Dependencies are inferred from the claim text.