389606-35-3Relevant academic research and scientific papers
Changing for the Better: Discovery of the Highly Potent and Selective CDK9 Inhibitor VIP152 Suitable for Once Weekly Intravenous Dosing for the Treatment of Cancer
Lücking, Ulrich,Kosemund, Dirk,B?hnke, Niels,Lienau, Philip,Siemeister, Gerhard,Denner, Karsten,Bohlmann, Rolf,Briem, Hans,Terebesi, Ildiko,B?mer, Ulf,Sch?fer, Martina,Ince, Stuart,Mumberg, Dominik,Scholz, Arne,Izumi, Raquel,Hwang, Stuart,Von Nussbaum, Franz
, p. 11651 - 11674 (2021/07/31)
Selective inhibition of exclusively transcription-regulating positive transcription elongation factor b/CDK9 is a promising new approach in cancer therapy. Starting from atuveciclib, the first selective CDK9 inhibitor to enter clinical development, lead optimization efforts aimed at identifying intravenously (iv) applicable CDK9 inhibitors with an improved therapeutic index led to the discovery of the highly potent and selective clinical candidate VIP152. The evaluation of various scaffold hops was instrumental in the identification of VIP152, which is characterized by the underexplored benzyl sulfoximine group. VIP152 exhibited the best preclinical overall profile in vitro and in vivo, including high efficacy and good tolerability in xenograft models in mice and rats upon once weekly iv administration. VIP152 has entered clinical trials for the treatment of cancer with promising longterm, durable monotherapy activity in double-hit diffuse large B-cell lymphoma patients.
Synthetic method of chloro 2-methoxy -4-5- methoxy-methyl-ethyl-phenyl-pyrimidine (by machine translation)
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Paragraph 0021; 0023; 0026; 0028; 0031; 0033; 0036; 0038, (2019/11/28)
Compared with the prior art, 4 - the 2 - 20% method has the advantages that the yield and purity are high 2, the pollution is small, and the process reaction flow is 2,4 - short 2,4 - 2 - 2 - 2 . (by machine translation)
SULFOXIMINE-SUBSTITUTED PYRIMIDINES , THEIR PREPARATION AND USE AS DRUGS
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Page/Page column 213, (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 87, (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.
SUBSTITUTED 2-ANILINOPYRIMIDINES AS CELL CYCLE KINASE INHIBITORS OR RECEPTOR TYROSINE KINASE INHIBITORS, PRODUCTION OF SAID SUBSTANCES AND USE OF THE LATTER AS MEDICAMENTS
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Page/Page column 52, (2010/10/20)
The invention relates to pyrimidine derivatives of general formula (I), in which R1, R2, R3, R4, A and D are defined as cited in the description, said derivatives being used as inhibitors of cyclin-dependent kin
Macrocyclic pyrimidines, their production and use as pharmaceutical agents
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Page column 20, (2010/02/08)
Macrocyclic pyrimidine derivatives of general formula I in which R1 to R5, X, Y, A, B, m and n have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinase, their processes for production as well as their use as medications for treating various diseases are described.
Pyrimidine derivatives
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, (2008/06/13)
Compounds of formula (I), wherein R1, p, R2, q, R3 and R4 are defined within, and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their prepara
