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US 8,541,576 B2Granted
Substituted pyrazolo-quinazoline derivatives as kinase inhibitors
AssigneeNerviano Medical Sciences S.R.L.
InventorsFrancesco Casuscelli, Claudia Piutti, Antonella Ermoli, Daniela Faiardi
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Abstract
The present invention relates to substituted pyrazolo[4,3-h]quinazoline compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular PIM kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
Claims2
A compound selected from the group consisting of:
- 1-(2-hydroxyethyl)-8-(methylsulfanyl)-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;
- 1-tert-butyl-N-methyl-8-(methylsulfanyl)-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;
- 1-(2-aminoethyl)-8-(methylsulfanyl)-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;
- 8-(methylsulfanyl)-1-(piperidin-4-ylmethyl)-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;
- 1-(2-hydroxyethyl)-8-[4-(4-methylpiperazin-1-yl)phenoxy]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;
- 1-tert-butyl-8-[4-(4-methylpiperazin-1-yl)phenoxy]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;
- 1-tert-butyl-8-(methylsulfanyl)-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
- 8-(methylsulfanyl)-1-(piperidin-4-yl)-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;
- 8-(methylsulfanyl)-1-(piperidin-3-yl)-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;
- 1-(4-aminocyclohexyl)-8-(methylsulfanyl)-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;
- 8-(methylsulfanyl)-1-(piperidin-3-ylmethyl)-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;
- 8-methoxy-1-(piperidin-4-yl)-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;
- 1-[(3-exo)-8-azabicyclo[3.2.1]oct-3-yl]-8-(methylsulfanyl)-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;
- 1-(4-aminobutan-2-yl)-8-(methylsulfanyl)-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;
- 1-(1-azabicyclo[2.2.2]oct-3-yl)-8-(methylsulfanyl)-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;
- 8-(methylsulfanyl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;
- 1-[trans-3-(hydroxymethyl)cyclobutyl]-8-(methylsulfanyl)-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;
- and
- 1-[cis-3-(hydroxymethyl)cyclobutyl]-8-(methylsulfanyl)-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide.
16 more elements
Dependencies are inferred from the claim text.