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US 12,427,153 B2Granted
1,2,4-triazin-3(2H)-one compounds for the treatment of hyperproliferative diseases
AssigneesBayer Aktiengesellschaft, The Broad Institute, Inc.
InventorsStefan Nikolaus Gradl, Manuel Ellermann, Philip Lienau, Charlotte Christine Kopitz, Martin Lange, Adrian Tersteegen, Detlev Sülzle, Timothy A. Lewis, Heidi Greulich, Xiaoyun Wu
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Abstract
The present invention includes name compounds of general formula (I): (I) in which R1, R2, R3 and R4 are as defined herein, methods for their preparation, pharmaceutical compositions and combinations comprising said compounds, and their use for the treatment of hyperproliferative diseases.
Claims8
A compound of formula (I)
- wherein
- R1 is a hydrogen atom, a halogen atom, a C1-C3-alkyl group, or a C1-C3-haloalkyl group;
- R2 is a hydrogen atom, or a halogen atom;
- with the proviso that both, R1 and R2, may not be a hydrogen atom at the same time with the exception if R3 is an ortho substituted phenyl group, both, R1 and R2, may also be a hydrogen atom;
- R3 is
- a C1-C3-alkyl group which is substituted one or more times with a group independently selected from a C1-C3-alkyl group, a C1-C3-alkoxy group, a heterocycloalkyl group, and an amino group which is substituted once or twice with a C1-C3-alkyl group,
- a C2-C6-alkenyl group, which is optionally substituted with a C1-C3-alkoxy group,
- a C5-C6-cycloalkenyl group,
- a phenyl group which is substituted one or more times with a group independently selected from halogen atom, C1-C3-alkyl group, and a C1-C3-haloalkyl group,
- a 4- to 6-membered heterocycloalkyl group which is substituted one or more times with a group independently selected from a fluorine atom, a hydroxy group, and a C1-C3-alkyl group,
- a
- group, a
- group, a
- group,
- a 5- to 10-membered heteroaryl group which is substituted one or more times with a group independently selected from an amino group, a halogen atom, and a C1-C3-haloalkyl group,
- a C1-C6-alkoxy group which is optionally substituted with a group independently selected from C1-C3-haloalkyl group, a hydroxy group, a C1-C3-alkyoxy group, a C4-C6-cycloalkyl group, a 4- to 6-membered heterocycloalkyl group, a 5- to 6-membered heteroaryl group, with the proviso that an unsubstituted methoxy group is excluded;
- a NR5R6 group, and
- a
- group,
- R4 is a hydrogen atom or a C1-C3-alkyl group;
- R5 is a hydrogen atom
- R6 is selected from
- a C1-C3-alkyl group which is substituted one or more times with a group selected from a 5- to 6-membered heteroaryl group, a C1-C3-alkoxy group, a hydroxy group, a C1-C3-haloalkyl group, and a C4-C6-cycloalkyl group which itself is optionally substituted with a C1-C3-hydroxyalkyl group,
- and
- a C5-C6-cycloalkyl group;
- or a stereoisomer, a tautomer, an N-oxide, or a salt thereof, or a salt of a stereoisomer, a salt of a tautomer, a salt of an N-oxide or a mixture of same.
23 more elements
Dependencies are inferred from the claim text.