954221-72-8

Upstream product

• 1193-21-1 4,6-dichloropyrimidine 
• 179899-07-1 4-fluoro-2-methoxyphenylboronic acid 

Downstream Products

• 1603922-98-0 (2-{[6-(4-fluoro-2-methoxyphenyl)pyrimidin-4-yl]amino}pyridin-4-yl)methanol 
• 1603922-92-4 6-(4-fluoro-2-methoxyphenyl)-N-{6-fluoro-4-[(methylsulfonyl)methyl]pyridin-2-yl}pyrimidin-4-amine 
• 1603923-00-7 N-[4-(chloromethyl)pyridin-2-yl]-6-(4-fluoro-2-methoxyphenyl)pyrimidin-4-amine 
• 1603922-85-5 6-(4-fluoro-2-methoxyphenyl)-N-{4-[(methylsulfonyl)methyl]pyridin-2-yl}pyrimidin-4-amine 
• 1603922-96-8 6-(4-fluoro-2-methoxyphenyl)-N-{4-[(methylsulfanyl)methyl]pyridin-2-yl}pyrimidin-4-amine 
• 1610462-79-7 (rac)-N-{4-[(S-ethylsulfonimidoyl)methyl]pyridin-2-yl}-6-(4-fluoro-2-methoxyphenyl)pyrimidin-4-amine 
• 1610462-89-9 (rac)-N-{ethyl[(2-{[6-(4-fluoro-2-methoxyphenyl)pyrimidin-4-yl]amino}pyridin-4-yl)methyl]-λ⁴-sulfanylidene}-2,2,2-trifluoroacetamide 
• 1610462-71-9 (R)-6-(4-fluoro-2-methoxyphenyl)-N-{4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl}pyrimidin-4-amine 
• 1610462-70-8 (S)-6-(4-fluoro-2-methoxyphenyl)-N-{4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl}pyrimidin-4-amine 
• 1610462-69-5 (rac)-6-(4-fluoro-2-methoxyphenyl)-N-{4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl}pyrimidin-4-amine 
• 1610462-81-1 2,2,2-trifluoro-N-{[(2-{[6-(4-fluoro-2-methoxyphenyl)pyrimidin-4-yl]amino}pyridin-4-yl)methyl](methyl)oxido-λ⁶-sulfanylidene}acetamide 
• 1610462-80-0 2,2,2-trifluoro-N-{[(2-{[6-(4-fluoro-2-methoxyphenyl)pyrimidin-4-yl]amino}pyridin-4-yl)methyl](methyl)-λ⁴-sulfanylidene}acetamide 

Relevant 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

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.

Synthesis and evaluation of phosphorus containing, specific CDK9/CycT1 inhibitors

Although there is a significant effort in the design of a selective CDK9/CycT1 inhibitor, no compound has been proven to be a specific inhibitor of this kinase so far. The aim of this research was to develop novel and selective phosphorus containing CDK9/CycT1 inhibitors. Molecules bearing phosphonamidate, phosphonate, and phosphinate moieties were synthesized. Prepared compounds were evaluated in an enzymatic CDK9/CycT1 assay. The most potent molecules were tested in cell-based toxicity and HIV proliferation assays. Selectivity of shortlisted compounds against CDKs and other kinases was tested. The best compound was shown to be a highly specific, ATP-competitive inhibitor of CDK9/CycT1 with antiviral activity.

N-(PYRIDIN-2-YL)PYRIMIDIN-4-AMINE DERIVATIVES CONTAINING A SULFONE GROUP

The present invention relates to N-(pyridin-2-yl)pyrimidin-4-amine derivatives containing a sulfone group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorder

N-(PYRIDIN-2-YL)PYRIMIDIN-4-AMINE DERIVATIVES CONTAINING A SULFOXIMINE GROUP

The present invention relates to disubstituted N-(pyridin-2-yl)pyrimidin-4-amine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/ or prophylaxis of disorders, in particular of hyper- proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).

NOVEL 4,6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES HAVING BOTH AROMATIC AND HALOGENIC SUBSTITUENTS

Certain 4,6-disubstituted aminopyrimidine derivatives having both aromatic and halogenic substituents.

4, 6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES AS INHIBITORS OF PROTEIN KINASES

The present invention relates to inhibitors of general Formula (I) of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to compounds for preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases.