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US 2016/0257682 A1Published application
Azaindazole compounds as inhibitors of t790m containing egfr mutants
AssigneeGenentech, Inc.
InventorsMarian C. Bryan, Bryan Chan, Francois Diederich, Jennafer Dotson, Emily Hanan, Timothy Heffron, Michael Lainchbury
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Abstract
This invention relates to novel compounds which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.
Claims23
A compound of Formula (I)
- wherein,
- R1 is C3-C7heterocycloalkyl, heteroaryl, —O(C1-C6alkyl), or —NRaRb, wherein said C3-C7heterocycloalkyl and heteroaryl may be further substituted with one to five Rf groups;
- R2 is hydrogen, C1-C6alkyl, C3-C7cycloalkyl or C3-C7heterocycloalkyl;
- R3 is C1-C6alkyl, C3-C7heterocycloalkyl, C3-C7cycloalkyl, —O(C1-C6alkyl), CN, —NRaRb, —NHC(O)(C1-C3alkyl), —C(O)NRaRb or heteroaryl;
- wherein each Rf is independently selected from the group consisting of C1-C3alkyl, alkoxy, amino, hydroxy, alkylamino, amide, urea, oxo, halo, pyrazolyl, imidazolyl, triazolyl, CN, —NHC(O)(C1-C3alkyl), acyl, sulfonyl, sulfoxide, sulfonamide, sulfoximinyl, —(CH2)mC3-C7heterocycloalkyl, —O(C1-C6alkyl), —C(O)ORa;
- wherein each Ra is independently H or C1-C6alkyl, each Rb is independently H, C1-C6alkyl, alkoxy, amino, —(CH2)mC(O)NH2, —(CH2)mC3-C7cycloalkyl, —(CH2)mC3-C7heterocycloalkyl or —(CH2)mheteroaryl, or Ra and Rb together may form a C3-C7cycloalkyl, C3-C7heterocycloalkyl or heteroaryl ring, wherein said C3-C7cycloalkyl, C3-C7heterocycloalkyl and heteroaryl may each be further substituted with one to three groups selected from the group consisting of halo, hydroxy, C1-C3alkyl, amino, oxo, amide, sulfonyl, sulfoxide, sulfoximinyl, sulfonamide, alkoxy, CN and acyl;
- each m is independently 0, 1, 2 or 3;
- or a pharmaceutically acceptable salt thereof.
5 more elements
Dependencies are inferred from the claim text.