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US 8,476,267 B2Granted
Imidazo-, pyrazolopyrazines and imidazotriazines and their use
AssigneeBayer Intellectual Property GmbH
InventorsStephan Siegel, Andreas Wilmen, Susanne Röhrig, Niels Svenstrup, Mark Jean Gnoth, Stefan Heitmeier, Ulrich Rester, Adrian Tersteegen, Michael Gerisch
Life of this patent
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Abstract
The invention relates to substituted imidazo-, pyrazolopyrazines and imidazotriazines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of hematological disorders, preferably of leukopenias and neutropenias.
Claims7
A compound of the formula,
- characterized in that
- either
- U represents N,
- V represents CR12,
- W represents CH,
- A represents CR15,
- or
- U represents CH,
- V represents CR12,
- W represents N,
- A represents CR15,
- or
- U represents CR16,
- V represents N,
- W represents CR17,
- A represents N,
- where
- R12 represents hydrogen, hydroxycarbonyl, aminocarbonyl, methyl, ethyl, C1-C4-alkylcarbonyl, C1-C4-alkoxycarbonyl, C1-C4-alkylaminocarbonyl, C1-C4-alkylcarbonylamino, pyrrolidinylcarbonyl, piperidinylcarbonyl, piperazinylcarbonyl, morpholinylcarbonyl or —CH2R13′
- where pyrrolidinylcarbonyl, piperidinylcarbonyl, piperazinylcarbonyl and morpholinylcarbonyl may be substituted by 1 to 2 substituents, where the substituents independently of one another are selected from the group consisting of oxo, methyl and ethyl,
- and
- where alkylcarbonyl, C2-C4-alkoxycarbonyl and C2-C4-alkylaminocarbonyl may be substituted by a substituent, where the substituent is selected from the group consisting of hydroxyl, amino, C1-C4-alkylamino, pyrrolidinyl, piperidinyl, piperazinyl and morpholinyl,
- where pyrrolidinyl, piperidinyl, piperazinyl and morpholinyl may be substituted by 1 to 2 substituents, where the substituents independently of one another are selected from the group consisting of oxo, methyl and ethyl,
- and
- where
- R13 represents hydroxyl, amino, hydroxycarbonyl, aminocarbonyl, C1-C4-alkoxy, C1-C4-alkylamino, pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl,
- where pyrrolidinyl, piperidinyl, piperazinyl and morpholinyl may be substituted by 1 to 2 substituents, where the substituents independently of one another are selected from the group consisting of oxo, methyl and ethyl,
- R15 represents hydrogen,
- R16 represents hydrogen or methyl,
- R17 represents hydrogen or methyl,
- R1 represents a group of the formula
- where
- * is the point of attachment to the heterocycle,
- n represents the number 0,
- X represents NR10,
- where
- R10 represents hydrogen,
- Y represents NR11,
- where
- R11 represents hydrogen or methyl,
- R3 represents 2-pyridyl, pyrimid-2-yl, 2-aminopyrimid-4-yl, 1,3-thiazol-2-yl or 1,3-thiazol-4-yl, where 2-pyridyl, pyrimid-2-yl, 1,3-thiazol-2-yl and 1,3-thiazol-4-yl are substituted by 1 or 2 substituents, where the substituents independently of one another are selected from the group consisting of fluorine, chlorine, cyano, nitro, amino and trifluoromethyl,
- and
- where 2-aminopyrimid-4-yl may be substituted by a substituent, where the substituent is selected from the group consisting of fluorine, chlorine, cyano, nitro, amino and trifluoromethyl,
- R4 represents hydrogen,
- R5 represents hydrogen or methyl,
- R6 represents hydrogen,
- R7 represents hydrogen or methyl,
- R8 represents hydrogen,
- R9 represents hydrogen or methyl,
- R2 represents phenyl, thienyl, pyrazolyl or pyridyl,
- where phenyl, thienyl, pyrazolyl and pyridyl may be substituted by 1 to 2 substituents, where the substituents independently of one another are selected from the group consisting of halogen, trifluoromethyl, trifluoromethoxy, aminocarbonyl, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkoxycarbonyl, C1-C4-alkylaminocarbonyl, pyrrolidinyl, piperidinyl, morpholinyl and morpholinylcarbonyl,
- or one of its salts.
48 more elements
Dependencies are inferred from the claim text.