54093-09-3

Upstream product

• 5424-21-5 2,4-dichloro-6-methylpyrimidine 
• 108-91-8 cyclohexylamine 

Downstream Products

• 73029-73-9 CyPPA 
• 1070897-34-5 2-ethylamino-4-cyclohexylamino-6-methylpyrimidine 
• 1207424-87-0 C₁₇H₂₉N₅ 
• 1207424-94-9 C₁₆H₂₁N₅ 
• 1348084-98-9 C₂₁H₃₀N₄O₃ 
• 1207424-89-2 C₂₃H₃₃N₅ 
• 1207424-86-9 C₁₈H₃₂N₄ 
• 1207424-88-1 C₂₂H₃₄N₄ 
• 1207424-47-2 C₁₉H₂₆N₄ 
• 1207424-48-3 C₁₉H₂₆N₄ 
• 934495-03-1 2-ethylamino-4-cyclohexylamino-5-iodo-6-methylpyrimidine 
• 934495-07-5 8-cyclohexyl-2-(ethylamino)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one 
• 934495-09-7 6-bromo-8-cyclohexyl-2-(ethylamino)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one 
• 934495-05-3 (E)-ethyl 3-(4-(cyclohexylamino)-2-(ethylamino)-6-methylpyrimidin-5-yl)acrylate 

Relevant academic research and scientific papers

Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain

The large GTPase dynamin mediates membrane fission during clathrin-mediated endocytosis (CME). The aminopyrimidine compounds were reported to disrupt dynamin localization to the plasma membrane via the PH domain and implicate this mechanism in the inhibition of CME. We have used a computational approach of binding site identification, docking, and interaction energy calculations to design and synthesize a new library of aminopyrimidine analogues targeting site-2 of the pleckstrin homology (PH) domain. The optimized analogues showed low micromolar inhibition against both dynamin I (IC50 = 10.6 ± 1.3 to 1.6 ± 0.3 μM) and CME (IC50(CME) = 65.9 ± 7.7 to 3.7 ± 1.1 mM), which makes this series among the more potent inhibitors of dynamin and CME yet reported. In CME and growth inhibition cell-based assays, the data obtained was consistent with dynamin inhibition. CEREP ExpresS profiling identified off-target effects at the cholecystokinin, dopamine D2, histamine H1 and H2, melanocortin, melatonin, muscarinic M1 and M3, neurokinin, opioid KOP and serotonin receptors.

Synthesis and antiplasmodial activity of novel 2,4-diaminopyrimidines

Two sets of diaminopyrimidines, totalling 45 compounds, were synthesized and assayed against Plasmodium falciparum. The SAR was relatively shallow, with only the presence of a 2-(pyrrolidin-1-yl)ethyl group at R2 significantly affecting activity. A subsequent series addressed high Log D values by introducing more polar side groups, with the most active compounds possessing diazepine and N-benzyl-4-aminopiperidyl groups at R1/R2. A final series attempted to address high in vitro microsomal clearance by replacing the C6-Me group with CF3, however antiplasmodial activity decreased without any improvement in clearance. The C6-CF3 group decreased hERG inhibition, probably as a result of decreased amine basicity at C2/C4.

METHODS OF TREATING CANCER USING PYRIDOPYRIMIDINONE INHIBITORS OF PI3K ALPHA

The present invention provides methods of treating cancer by administering a compound of Formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with other cancer treatments. (Formula I)

PYRIDO [2, 3-D] PYRIMIDIN-7-ONE COMPOUNDS AS INHIBITORS OF PI3K-ALPHA FOR THE TREATMENT OF CANCER

The invention is directed to a Compound of Formula I, II, or III. The invention provides compounds that inhibit, regulate, and/or modulate PI3K that are useful in the treatment of hyperproliferatives diseases, such as cancer.

PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα

The invention is directed to Compounds of Formula I and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.

Selective positive modulation of the SK3 and SK2 subtypes of small conductance Ca2+-activated K+ channels

Background and purpose: Positive modulators of small conductance Ca 2+-activated K+ channels (SK1, SK2, and SK3) exert hyperpolarizing effects that influence the activity of excitable and non-excitable cells. The prototype compound 1

Identification of aminopyrimidine regioisomers via line broadening effects in1H and13C NMR spectroscopy

Substituted mono- and diamino-pyrimidines were synthesized as part of our medicinal chemistry programmes. Primary amines substituted at the 4-position exhibited room-temperature line broadening effects in both 1H and 13C NMR spectros

Pyrimidines and process of making the same

A compound of the formula SPC1 Wherein X is a member of the group consisting of H and Br, and R is a member of the group consisting of straight-chain and branched-chain alkyl radicals and cycloalkyl radicals having from 5 - 8 C-atoms. The invention also relates to the preparation of the new compounds. The pyrimidines of the invention are useful pesticides, particularly herbicides and fungicides.