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US 10,882,848 B2Granted
2-benzopyrazinyl-n-heteroaryl-2-phenyl-acetamide compounds
AssigneeHoffmann-La Roche Inc.
InventorsMartin Duplessis, Georg Jaeschke, Bernd Kuhn, Kiel Lazarski, Yanke Liang, Yvonne Alice Nagel, Antonio Ricci, Daniel Rueher, Sandra Steiner
Life of this patent
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Abstract
The present invention provides compounds which are selective allosteric inhibitors of T790M and C797S containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.
Claims15
A compound of formula I,
- wherein
- R1 is each independently selected from the group consisting of
- i) amino,
- ii) C1-6-alkyl,
- iii) C1-6-alkoxy,
- iv) cyano,
- v) halogen,
- vi) halogen-C1-6-alkyl,
- vii) halogen-C1-6-alkoxy, and
- viii) hydroxy;
- R2 is each independently selected from the group consisting of
- i) amino,
- ii) aryl substituted with (R3)k,
- iii) C1-6-alkyl,
- iv) C1-6-alkoxy,
- v) C2-6-alkynyl substituted with (R5)p,
- vi) cyano,
- vii) halogen,
- viii) halogen-C1-6-alkyl,
- ix) halogen-C1-6-alkoxy,
- x) heteroaryl substituted with (R4)l,
- xi) heterocyclyl substituted with (R7)r and
- xii) hydroxy;
- R3 is each independently selected from the group consisting of
- i) amino,
- ii) C1-6-alkyl,
- iii) C1-6-alkoxy,
- iv) cyano,
- v) halogen,
- vi) halogen-C1-6-alkyl,
- vii) halogen-C1-6-alkoxy, and
- viii) hydroxy;
- R4 is each independently selected from the group consisting of
- i) amino,
- ii) C1-6-alkyl,
- iii) C1-6-alkoxy,
- iv) cyano,
- v) halogen,
- vi) halogen-C1-6-alkyl,
- vii) halogen-C1-6-alkoxy,
- viii) heterocyclyl substituted with (R8)s, and
- ix) hydroxy;
- R5 is independently selected from the group consisting of
- i) heteroaryl substituted with (R6)q, and
- ii) C1-6-alkyl;
- R6 is independently selected from the group consisting of
- i) amino, and
- ii) C1-6-alkyl;
- R7 is independently selected from the group consisting of
- i) amino, and
- ii) C1-6-alkyl;
- R8 is independently selected from the group consisting of
- i) amino, and
- ii) C1-6-alkyl;
- Het is heteroaryl;
- k is 0, 1, 2 or 3;
- l is 0, 1 or 2;
- n is 0, 1, 2 or 3;
- m is 0, 1 or 2;
- p is 0, 1 or 2;
- q is 0, 1 or 2;
- r is 0, 1 or 2;
- s is 0, 1 or 2;
- or a pharmaceutically acceptable salt thereof.
61 more elements
Dependencies are inferred from the claim text.