- The lab oddity prevails: Discovery of Pan-CDK inhibitor (R)-S-Cyclopropyl-S-(4-{[4-{[(1R,2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulfoximide (BAY1000394) for the treatment of cancer
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Lead optimization of a high-throughput screening hit led to the rapid identification of aminopyrimidine ZK304709, a multitargeted CDK and VEGF-R inhibitor that displayed a promising preclinical profile. Nevertheless, ZK304709 failed in phaseI studies due
- Luecking, Ulrich,Jautelat, Rolf,Krueger, Martin,Brumby, Thomas,Lienau, Philip,Schaefer, Martina,Briem, Hans,Schulze, Julia,Hillisch, Alexander,Reichel, Andreas,Wengner, Antje Margret,Siemeister, Gerhard
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p. 1067 - 1085
(2013/07/26)
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- ALKYNYLPYRIMIDINES AS TIE2 KINASE INHIBITORS
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The invention relates to alkynylpyrimidines according to the general formula (I) in which A, R1, R2, R3, R4, R5, and R6 are as defined in the claims, to pharmaceutical compositions comprising said alkynylpyrimidines, to methods of preparing said alkynylpyrimidines, as well as to uses thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 and VEGFR2 signalling.
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Page/Page column 70
(2009/01/23)
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- SULFOXIMINE-SUBSTITUTED PYRIMIDINES , THEIR PREPARATION AND USE AS DRUGS
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The invention relates to sulfoximine-substituted pyrimidines of the general Formula (I) processes for the preparation thereof and their use as kinase inhibitors for treating for example cancer or inflammation.
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Page/Page column 109
(2010/11/27)
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- Sulfoximine-substituted pyrimidines, processes for production thereof and use thereof as drugs
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The invention relates to sulfoximine-substituted pyrimidines of the general formula I processes for the preparation thereof and their use as drugs.
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Page/Page column 42
(2010/11/28)
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