57825-29-3

Upstream product

• 871887-29-5 4-(2-ethylbenzyl)morpholine 
• 506-68-3 bromocyane 
• 767-90-8 (2-ethylphenyl)methanol 
• 50-00-0 formaldehyd 
• 100-41-4 ethylbenzene 
• 10035-10-6 hydrogen bromide 
• 22927-13-5 2-ethylbenzaldehyde 
• 612-19-1 2-ethylbenzoic acid 
• 40391-19-3 (1R*,1'RS*)-1-cyclohex-2-enylethanol 
• 89-95-2 2-methyl-benzyl alcohol 

Downstream Products

• 15255-92-2 N-(2-Ethyl-benzyloxy)-carbamidsaeure-ethylester 
• 5553-49-1 N-(2-Ethyl-benzyl)-N-(2-ethyl-benzyloxy)-carbamidsaeure-ethylester 
• 911405-99-7 C₂₆H₃₅N₃O₃ 
• 1257335-34-4 (E)-3-(1-(2-ethylbenzyl)-2-oxo-1, 2-dihydropyridin-3-yl)-N-hydroxyacrylamide 
• 74533-20-3 2-(2-ethylphenyl)acetonitrile 
• 1400902-37-5 (E)-2-(2-ethylbenzyl)-3-oxo-3-(4-phenylcyclohexyl)-propionic acid ethyl ester 
• 1001096-01-0 C₂₄H₃₀NO₄P 

Relevant academic research and scientific papers

ALKOXYBENZO-FIVE-MEMBERED (SIX-MEMBERED) HETEROCYCLIC AMINE COMPOUND AND PHARMACEUTICAL USE THEREOF

The invention relates to alkoxybenzeno five- or six-member heterocyclic amines compounds as scheme I , in which the R1, R2 and R3 are consistent with the detailed description in the patent claim. The compounds can act as selective sphingomyelin synthase 2 (SMS2) inhibitors to treat diseases caused by abnormal increasing of sphingomyelin (SM). This invention also includes compounds as scheme I , including pharmaceutically acceptable salts, pharmaceutical compositions as the active ingredients, and their application in drugs which can prevent and cure diseases caused by abnormal increasing of SM. These diseases caused by abnormal increasing of SM include atherosclerosis, type II diabetes, fatty liver, obesity, metabolic syndromes, enteritis and other inflammatory diseases.

Discovery, synthesis and anti-atherosclerotic activities of a novel selective sphingomyelin synthase 2 inhibitor

The sphingomyelin synthase 2 (SMS2) is a potential target for pharmacological intervention in atherosclerosis. However, so far, few selective SMS2 inhibitors and their pharmacological activities were reported. In this study, a class of 2-benzyloxybenzamides were discovered as novel SMS2 inhibitors through scaffold hopping and structural optimization. Among them, Ly93 as one of the most potent inhibitors exhibited IC50 values of 91 nM and 133.9 μM against purified SMS2 and SMS1 respectively. The selectivity ratio of Ly93 was more than 1400-fold for purified SMS2 over SMS1. The in vitro studies indicated that Ly93 not only dose-dependently diminished apoB secretion from Huh7 cells, but also significantly reduced the SMS activity and increased cholesterol efflux from macrophages. Meanwhile, Ly93 inhibited the secretion of LPS-mediated pro-inflammatory cytokine and chemokine in macrophages. The pharmacokinetic profiles of Ly93 performed on C57BL/6J mice demonstrated that Ly93 was orally efficacious. As a potent selective SMS2 inhibitor, Ly93 significantly decreased the plasma SM levels of C57BL/6J mice. Furthermore, Ly93 was capable of dose-dependently attenuating the atherosclerotic lesions in the root and the entire aorta as well as macrophage content in lesions, in apolipoprotein E gene knockout mice treated with Ly93. In conclusion, we discovered a novel selective SMS2 inhibitor Ly93 and demonstrated its anti-atherosclerotic activities in vivo. The preliminary molecular mechanism-of-action studies revealed its function in lipid homeostasis and inflammation process, which indicated that the selective inhibition of SMS2 would be a promising treatment for atherosclerosis.

Propionic Acid Derivatives and Methods of Use Thereof

Provided herein are compounds and pharmaceutical compositions of formula I where R1, R2, R3, R4, R5, X and R6 are as described herein. Also provided pharmaceutically acceptable salts or stereoisomer(s) of these compounds. In addition methods are provided for antagonizing the action of an α4-integrin to treat various pathophysiological conditions.

Amide-Directed C?H Sodiation by a Sodium Hydride/Iodide Composite

A new protocol for amide-directed ortho and lateral C?H sodiation is enabled by sodium hydride (NaH) in the presence of either sodium iodide (NaI) or lithium iodide (LiI). The transient organosodium intermediates could be transformed into functionalized aromatic compounds.

ANTIVIRAL PHOSPHINATE COMPOUNDS

The invention is related to anti-viral phosphinate compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

5-Benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators

A series of 5-benylidene-1,2-dihydrochromeno[3,4-f]quinolines (4) were synthesized and tested in bioassays to evaluate their progestational activities, receptor- and tissue-selectivity profiles as selective progesterone receptor modulators (SPRMs). Most of the new analogues exhibited as highly potent progestins with more than 100-fold receptor selectivity over other steroid hormone receptors and LG120920 (7b) demonstrated tissue selectivity toward uterus and vagina versus breasts in a rodent model after oral administration.

Stereo- and enantioselective routes to functionalised cyclohexenes via heterodiene cycloadditions of 6-oxocyclohexene-1-carbaldehydes with ketene acetals

Various substituted cyclohexenes related to α-cyclocitral have been prepared using the heterodiene cycloadditions of 2-formyl-4,4-dimethyl-2- cyclohexen-1-one 4 with ketene acetals as the pivotal step. The key intermediates are accessible in homochiral form via an auxiliary-based sequence in which a C2-symmetric ketene acetal derived from 1,2-bis(2- methylphenyl)ethane-1,2-diol 2a serves as the 2π component. The diol 2a can be recovered in optically pure form.

REACTIVITE DES GEM-DIBROMOCYCLOPROPANES-IV; OUVERTURE ACIDO-CATALYSEE DE GEM-DIHALOGENOCYCLOPROPYLCARBINOLS

By acid catalysis, gem-dihalogenocyclopropylcarbinols are converted into homoallylic α-dihalogenated cations which in general eliminate the hydrogen halide and lead to the 3-halogenopentadienyl cations from which cyclopentenones can be formed by cyclisation.For bicycloheptanes, aromatisation of the 3-halogenopentadienyl cation in benzyl bromide is observed.