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US 2015/0087664 A1Published application
Quinazoline compounds as serine/threonine kinase inhibitors
AssigneesGenentech, Inc., Array BioPharma Inc.
InventorsJames F. Blake, Huifen Chen, Mark Joseph Chicarelli, Jason Demeese, Rustam Ferdinand Garrey, John Gaudino, Lewis Gazzard, Robert J. Kaus, Samuel Kintz, Peter J. Mohr, David A. Moreno, Jacob Schwartz, Christopher S. Siedem, Eli M. Wallace
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Abstract
Compounds having the formula (I) wherein R1, R2, R3 and Ar as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
Claims29
A compound according to formula I
- wherein:
- R1 is heterocyclyl or heteroaryl optionally substituted with one to three substituents independently selected from the group consisting of C1-6 alkyl, C1-6 hydroxyalkyl, halogen, hydroxyl and oxo;
- Ar is phenyl or pyridinyl optionally substituted by 1 to 5 groups independently selected from the group consisting of C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C3-6 cycloalkyl, halogen, C1-6 haloalkoxy, C1-6 alkylthio, C1-6 acylamino, cyano and nitro;
- R2 is selected from the group consisting of (a) C1-10 alkyl, (b) C1-6 haloalkyl, (c) heterocyclyl or heterocyclyl-C1-6 alkyl wherein said heterocycle or heterocyclyl-C1-6 alkyl is selected from the group consisting of tetrahydropyranyl, tetrahydrofuranyl,2-oxabicyclo[2.2.1]heptan-5-yl, oxetanyl, piperidinyl, N—C1-6 alkyl-piperidinyl, 1,1-dioxothietan-3-yl, thietan-3-yl, and N—C1-6 alkyl-2-oxo-pyrrolidinyl and wherein said heterocyclyl or heterocyclyl-C1-6 alkyl is optionally substituted by 1 to 3 groups independently selected from the group consisting of C1-6 alkyl, C1-6 haloalkyl, C1-4 acyloxy-C1-2 alkyl, halogen, hydroxyl, phenyl, C1-3 hydroxyalkyl and oxo, (d) C3-7 cycloalkyl or C3-7 cycloalkyl-C1 alkyl wherein said cycloalkyl or C3-7 cycloalkyl-C1-6 alkyl are optionally substituted by one to three hydroxyl, C1-3 alkoxy or halo groups, (e) C1-6 heteroalkyl wherein the heteroalkyl moiety at least includes C1-6 hydroxyalkyl or C1-3 alkoxy-C1-6 alkoxy, (f) heteroaryl wherein said heteroaryl is selected from the group consisting of pyrazolyl and pyridinyl wherein said heteroaryl is optionally independently substituted with one to three groups selected from the group consisting of C1-6 alkyl groups, C1-6 haloalkyl and halogen. and (g) C1-3 cyanoalkyl;
- R3 is hydrogen or halogen;
- or,
- a stereoisomer, tautomer or pharmaceutically acceptable salt thereof.
4 more elements
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Dependencies are inferred from the claim text.