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US 10,590,111 B2Granted
Substituted 2-anilinopyrimidine derivatives as EGFR modulators
AssigneeBeta Pharma, Inc.
InventorsJirong Peng, Michael John Costanzo, Michael Nicholas Greco, Michael Alan Green, Victoria Lynn Wilde, Don Zhang
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Abstract
This application discloses novel substituted 2-anilinopyrimidine derivatives, and pharmaceutically acceptable salts, solvates, prodrugs, and compositions thereof, which are useful for the treatment or prevention of diseases or medical conditions mediated by epidermal growth factor receptors (EGFRs), including but not limited to a variety of cancers.
Claims39
A compound of formula I:
- or a pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein:
- G is selected from substituted or unsubstituted 1H-indol-3-yl, substituted or unsubstituted 1H-indazol-3-yl, substituted or unsubstituted 2H-indazol-3-yl, and substituted or unsubstituted pyrazolo[1,5-a]-pyridin-3-yl, and substituted or unsubstituted 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridin-3-yl;
- X is selected from oxygen, sulfur, and methylene;
- R1 is selected from hydrogen, halogen, methyl, trifluoromethyl, and cyano;
- R2, R3, and R4 are the same or different and are independently selected from hydrogen, halogen, and trifluoromethyl;
- provided, however, when X is oxygen and all of R2, R3, and R4 are hydrogen, then said substituted or unsubstituded 1H-indol-3-yl is
- and G is not pyrazolo[1,5-a]-pyridin-3-yl;
- R5 is selected from lower alkyl, optionally substituted 3- to 6-membered heterocyclyl, R7R8N-(lower alkyl), and R7R8N-(cycloalkylalkyl), wherein R7 and R8 are the same or different and are independently selected from hydrogen and lower alkyl;
- and
- R6 is selected from lower alkoxy and lower alkyl.
7 more elements
Dependencies are inferred from the claim text.