40503-91-1

Upstream product

• 40503-16-0 4-hydroxy-4-(3-methoxy-phenyl)-cyclohexanone 
• 365553-76-0 8-(3-methoxyphenyl)-1,4-dioxaspiro[4.5]decane 
• 147678-65-7 8-(3-methoxyphenyl)-1,4-dioxaspiro[4.5]dec-7-ene 
• 4746-97-8 cyclohexanedione monoethylene ketal 
• 365553-73-7 8-(3-methoxy-phenyl)-1,4-dioxa-spiro[4.5]decan-8-ol 
• 147678-66-8 C₁₃H₁₄O₂ 
• 2398-37-0 3-methoxyphenyl bromide 
• 195436-65-8 4-methyl-N'-(1,4-dioxaspiro[4.5]decan-8-ylidene)benzenesulfonohydrazide 
• 36282-40-3 (3-methoxyphenyl)magnesium bromide 

Downstream Products

• 868142-49-8 8-(3-methoxy-phenyl)-2,4-dioxo-1,3-diaza-spiro[4.5]decane-1,3-dicarboxylic acid di-tert-butyl ester 
• 945399-14-4 1-[2-(2,4-dichlorophenyl)ethylamino]-4-(3-methoxyphenyl)cyclohexanecarbonitrile 
• 1254342-82-9 (S)-5,7-dibromo-2-(3-methoxyphenyl)-1,2,3,4-tetrahydroacridine 
• 1297474-30-6 C₁₆H₁₈N₂O₂S 
• 1402080-49-2 5-(3-methoxyphenyl)oxepan-2-one 
• 1297474-48-6 C₂₈H₂₄N₂O₆S 
• 1297474-39-5 C₁₆H₁₄N₂O₂S 
• 868142-19-2 8-(3-methoxy-phenyl)-1,3-diaza-spiro[4.5]decane-2,4-dione 

Relevant academic research and scientific papers

Desymmetrizing Isomerization of Alkene via Thiazolinyl Iminoquinoline Cobalt Catalysis

We report a cobalt-catalyzed desymmetrizing isomerization of exo-cyclic alkenes to generate chiral 1-methylcyclohexene derivatives with good yields and enantioselectivities. A novel chiral thiazolinyl iminoquinoline ligand and its cobalt complex were desi

NOVEL HETEROCYCLIC DERIVATIVES USEFUL AS SHP2 INHIBITORS

Provided is a compound of formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, provided is a pharmaceutical composition comprising the said compound.

Optimization of TRPV6 calcium channel inhibitors using a 3D ligand-based virtual screening method

Herein, we report the discovery of the first potent and selective inhibitor of TRPV6, a calcium channel overexpressed in breast and prostate cancer, and its use to test the effect of blocking TRPV6-mediated Ca2+-influx on cell growth. The inhib

Design and synthesis of novel small molecule CCR2 antagonists: Evaluation of 4-aminopiperidine derivatives

A novel N-(2-oxo-2-(piperidin-4-ylamino)ethyl)-3-(trifluoromethyl)benzamide series of human CCR2 chemokine receptor antagonists was identified. With a pharmacophore model based on known CCR2 antagonists a new core scaffold was designed, analogues of it synthesized and structure-affinity relationship studies derived yielding a new high affinity CCR2 antagonist N-(2-((1-(4-(3-methoxyphenyl)cyclohexyl)piperidin-4-yl)amino)-2-oxoethyl)-3-(trifluoromethyl)benzamide.

Enantioselective baeyer-villiger oxidation: Desymmetrization of meso cyclic ketones and kinetic resolution of racemic 2-arylcyclohexanones

Catalytic enantioselective Baeyer-Villiger (BV) oxidations of racemic and meso cyclic ketones were achieved in the presence of chiral N,N'-dioxide-Sc III complex catalysts. The BV oxidations of prochiral cyclohexanones and cyclobutanones afforded series of optically active μ- and γ-lactones, respectively, in up to 99% yield and 95% ee. Meanwhile, the kinetic resolution of racemic 2-arylcyclohexanones was also realized via an abnormal BV oxidation. Enantioenriched 3-aryloxepan-2-ones, whose formation is counter to the migratory aptitude, were obtained preferentially. Both the lactones and the unreacted ketones were obtained with high ee values.

Enantioselective baeyer-villiger oxidation: Desymmetrization of meso cyclic ketones and kinetic resolution of racemic 2-arylcyclohexanones

Catalytic enantioselective Baeyer-Villiger (BV) oxidations of racemic and meso cyclic ketones were achieved in the presence of chiral N,N'-dioxide-Sc III complex catalysts. The BV oxidations of prochiral cyclohexanones and cyclobutanones afforded series of optically active μ- and γ-lactones, respectively, in up to 99% yield and 95% ee. Meanwhile, the kinetic resolution of racemic 2-arylcyclohexanones was also realized via an abnormal BV oxidation. Enantioenriched 3-aryloxepan-2-ones, whose formation is counter to the migratory aptitude, were obtained preferentially. Both the lactones and the unreacted ketones were obtained with high ee values.

Aryl extensions of thienopyrimidinones as fibroblast growth factor receptor 1 kinase inhibitors

Optimization of thienopyrimidinone derivatives as FGFR1 kinase inhibitors is being pursued. The present results confirm predictions of computational modeling that an aryl substituent can be introduced at the 2-position in structure 3. The substituent is anticipated to project deeper into the binding site and provide opportunities for enhanced activity and selectivity. The most potent analog reported herein, 13, has a 4-hydroxyphenyl substituent and yields an IC50 of 6 μM for inhibition of phosphorylation by FGFR1 kinase. It was also found that the western anisole-containing substituent in 3 can be replaced by a propionic acid group with no loss in potency and with potentially significant gains in pharmacologically relevant properties.

1-Cyclohexyl-4-(4-arylcyclohexyl)piperazines: Mixed σ and Human Δ8-Δ7 Sterol Isomerase Ligands with Antiproliferative and P-Glycoprotein Inhibitory Activity

Many new chemotherapeutic agents are under preclinical investigation and, despite efforts to more selectively target cancer cells, limitations such as toxicity and inherent resistance are often encountered. Therefore, alternative strategies are needed to treat cancer and overcome such limitations. We describe novel cyclohexylpiperazine derivatives, designed as mixed affinity ligands for sigma (σ) receptors and human Δ8-Δ7 sterol isomerase (HSI) ligands, which also exhibit P-glycoprotein (P-gp) inhibitory activity, with the aim of exploiting the antiproliferative effects mediated by σ and HSI sites while overcoming P-gp-mediated resistance. All of the compounds displayed high affinities for σ receptors and HSI sites, P-gp inhibitory activity, and σ2 receptor agonist antiproliferative activity. Antiproliferative activity was also tested in PC-3 cells to establish σ1 and HSI contribution. Compound cis-11, which displayed the best antiproliferative and P-gp inhibitory activities, was co-administered with 0.1 μM doxorubicin in MDCK-MDR1 cells. Compound cis-11 caused 70 % and 90 % cell death when co-administered at 30 μM and 50 μm, respectively. When administered alone, cis-11 resulted in 50 % cell death, demonstrating its single agent antitumor properties in a tumor cell line overexpressing P-gp.Synergistic mixed activity: A series of cyclohexylpiperazines with mixed σ and HSI affinities and P-gp inhibitory activity were synthesized. Their antiproliferative activity, combined with P-gp inhibitory activity, shows the potential of these compounds to be used as antitumor agents devoid of P-gp-mediated resistance, or in association with classic antitumor agents susceptible to P-gp activity.

SPIRO IMIDAZOLE DERIVATIVES AS PPAR MODULATORS

The invention provides compounds (Ia), (Ib) and (Ic), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated