851008-74-7Relevant academic research and scientific papers
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
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
, p. 1067 - 1085 (2013/07/26)
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
SULFOXIMINE-SUBSTITUTED ANILINOPYRIMIDINE DERIVATIVES AS CDK INHIBITORS, THE PRODUCTION THEREOF, AND USE AS MEDICINE
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, (2011/12/13)
The invention relates to sulfoximine-substituted anilino-pyrimidine derivatives of formula (I). methods of production thereof, and use thereof as medication for the treatment of various diseases.
Sulfoximine-substituted trifluoromethylpyrimidine analogs as inhibitors of proline-rich tyrosine kinase 2 (PYK2) show reduced hERG activity
Walker, Daniel P.,Zawistoski, Michael P.,McGlynn, Molly A.,Li, Jian-Cheng,Kung, Daniel W.,Bonnette, Peter C.,Baumann, Amy,Buckbinder, Leonard,Houser, Janet A.,Boer, Jason,Mistry, Anil,Han, Seungil,Guzman-Perez, Li Xing and Angel
scheme or table, p. 3253 - 3258 (2010/03/31)
The synthesis, in vitro properties, and in vivo pharmacokinetics for a series of sulfoximine-substituted trifluoromethylpyrimidines as inhibitors of proline-rich tyrosine kinase, a target for the possible treatment of osteoporosis, are described. These co
ALKYNYLPYRIMIDINES AS TIE2 KINASE INHIBITORS
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Page/Page column 70, (2009/01/23)
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.
SULFOXIMINE-SUBSTITUTED PYRIMIDINES , THEIR PREPARATION AND USE AS DRUGS
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Page/Page column 108, (2010/11/27)
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.
Sulfoximine-substituted pyrimidines, processes for production thereof and use thereof as drugs
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Page/Page column 41, (2010/11/28)
The invention relates to sulfoximine-substituted pyrimidines of the general formula I processes for the preparation thereof and their use as drugs.
