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US 2015/0306102 A1Published application
Substituted pyrazolopyrimidines as akt kinase inhibitors
AssigneesBayer Intellectual Property GmbH, Bayer Pharma Aktiengesellschaft
InventorsLars BÄRFACKER, William SCOTT, Andrea HÄGEBARTH, Hartmut REHWINKEL, Oliver POLITZ, Roland NEUHAUS, Ulf BÖMER
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.
Claims14
A compound of formula (I)
- in which
- R1 is hydrogen, a 1-6C-alkyl group,
- wherein said group being optionally substituted, one or more times, identically or differently, with a substituent selected from:
- hydroxy, halogen, 1-6C-alkyl, 1-4C-haloalkyl, 1-6C-alkoxy, —NR7R8, cyano, (═O), —C(O)NR7R8, —C(O)OR9, —NHC(O)R10, —NHS(O)2R10, heteroaryl,
- R2 is hydrogen, or a 1-6C-alkyl group
- wherein said group is optionally substituted, one or more times, identically or differently, with a substituent selected from:
- hydroxy, halogen, 1-6C-alkyl, 1-4C-haloalkyl, 1-6C-alkoxy, —NR7R8, cyano, —C(O)NR7R8, —C(O)OR9, —NHC(O)R10, —NHS(O)2R10, —NH-(1-6C-alkylen)-O-(1-6C-alkyl),
- R3 is hydrogen, 1-6C-alkyl which is optionally substituted one or more times with halogen,
- R4 is phenyl optionally substituted by 1-6C-alkyl, halogen, cyano,
- R5 is hydrogen, halogen,
- R6 is hydrogen, 1-6C-alkyl,
- X is —CH2—,
- Y is —CH2—, —CH(OH)—,
- R7, R8 which can be the same or different, is hydrogen, hydroxy, 3-7C-cycloalkyl or a group selected from 1-4C-alkyl, 1-6C-alkoxy, wherein said group is optionally substituted, one or more times, identically or differently, with a substituent selected from:
- halogen, hydroxy, mono- or di-(1-4C-alkylamino), 1-4C-alkoxy, or 3-7C-cycloalkyl or,
- R7 and R8 together with the nitrogen to which they are attached may also form a saturated or unsaturated 3-6C-heterocyclic ring,
- which is optionally substituted by (═O)
- R9 is hydrogen, 1-6C-alkyl,
- R10 is 1-4C-alkyl (optionally substituted in the same way of differently one or more times with halogen, hydroxy) or 3-7C-cycloalkyl,
- or an N-oxide, a salt, a tautomer or a stereoisomer of said compound, or a salt of said N-oxide, tautomer or stereoisomer.
17 more elements
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Dependencies are inferred from the claim text.