Quinazoline inhibitors of egfr tyrosine kinase
AssigneeAuspex Pharmaceuticals, Inc.
InventorsThomas G. Gant, Sepehr Sarshar
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Abstract
The present invention relates to new quinazoline inhibitors of EGFR tyrosine kinase, pharmaceutical compositions thereof, and methods of use thereof.
Claims59
A compound of structural Formula I
- or a pharmaceutically acceptable salt thereof, wherein:
- R1-R24 are independently selected from the group consisting of hydrogen and deuterium;
- at least one of R1-R24 is deuterium;
- and
- if R17-R24 are deuterium, then at least one of R1-R16 is deuterium.
A pharmaceutical composition comprising a pharmaceutically acceptable carrier together with a compound of structural Formula I
- or a pharmaceutically acceptable salt thereof, wherein:
- R1-R24 are independently selected from the group consisting of hydrogen and deuterium;
- and
- at least one of R1-R24 is deuterium.
A method of treatment of an EGFR tyrosine kinase-mediated disorder comprising the administration, to a patient in need thereof, of a therapeutically effective amount of a compound of structural Formula I
- or a pharmaceutically acceptable salt thereof, wherein:
- R1-R24 are independently selected from the group consisting of hydrogen and deuterium;
- and
- at least one of R1-R24 is deuterium.
A compound for use as a medicament, having structural Formula I
- or a pharmaceutically acceptable salt thereof, wherein:
- R1-R24 are independently selected from the group consisting of hydrogen and deuterium;
- and
- at least one of R1-R24 is deuterium.
A compound for use in the manufacture of a medicament for the prevention or treatment of a disorder ameliorated by inhibiting EGFR tyrosine kinase activity, said compound having structural Formula I
- or a pharmaceutically acceptable salt thereof, wherein:
- R1-R24 are independently selected from the group consisting of hydrogen and deuterium;
- and
- at least one of R1-R24 is deuterium.
A compound of Formula II:
- or a pharmaceutically acceptable salt thereof, wherein:
- R8-R24 are independently selected from the group consisting of hydrogen and deuterium;
- and
- when R8-R16 are all H, then at least one of R17-R24 is deuterium.
Dependencies are inferred from the claim text.