119999-22-3Relevant academic research and scientific papers
Competitive Binding Assay with an Umbelliferone-Based Fluorescent Rexinoid for Retinoid X Receptor Ligand Screening
Yamada, Shoya,Kawasaki, Mayu,Fujihara, Michiko,Watanabe, Masaki,Takamura, Yuta,Takioku, Maho,Nishioka, Hiromi,Takeuchi, Yasuo,Makishima, Makoto,Motoyama, Tomoharu,Ito, Sohei,Tokiwa, Hiroaki,Nakano, Shogo,Kakuta, Hiroki
, p. 8809 - 8818 (2019/10/11)
Ligands for retinoid X receptors (RXRs), "rexinoids", are attracting interest as candidates for therapy of type 2 diabetes and Alzheimer's and Parkinson's diseases. However, current screening methods for rexinoids are slow and require special apparatus or facilities. Here, we created 7-hydroxy-2-oxo-6-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)-2H-chromene-3-carboxylic acid (10, CU-6PMN) as a new fluorescent RXR agonist and developed a screening system of rexinoids using 10. Compound 10 was designed based on the fact that umbelliferone emits strong fluorescence in a hydrophilic environment, but the fluorescence intensity decreases in hydrophobic environments such as the interior of proteins. The developed assay using 10 enabled screening of rexinoids to be performed easily within a few hours by monitoring changes of fluorescence intensity with widely available fluorescence microplate readers, without the need for processes such as filtration.
aromatic compound having fused cyclic substituent in aromatic ring and organic light-emitting diode including the same
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Paragraph 0295-0297, (2019/01/06)
The present invention relates to a compound having a cyclic substituent fused with a cyclic ring and an organic light emitting diode including the same, and more particularly, to a compound for an organic light emitting diode represented by chemical formula A and an organic light emitting diode including the same. In chemical formula A, X is a substituent having structural formula X, Y is a substituent of structural formula Y1, n is an integer from 1 to 4, and structural formulas X and Y1 are the same as described in detailed description of the present invention.
The synthesis of lactone-bridged 1,3,5-triphenylbenzene derivatives as pi-expanded coumarin triskelions
Hintz, Heather A.,Sortedahl, Nicholas J.,Meyer, Samantha M.,Decato, Daniel A.,Dahl, Bart J.
supporting information, p. 4703 - 4708 (2017/11/17)
Two triply lactone-bridged 1,3,5-triphenylbenzene derivatives with solubilizing moieties have been synthesized in five and six steps from commercially available starting materials. Compounds containing the 1,3,5-triphenylbenzene core with two atom bridges are relatively unknown. This new class of pi-expanded coumarins contain triskelion architectures and X-ray crystallographic studies of one of the triskelions indicates that the 1,3,5-triphenylbenzene core adopts a near-planar geometry. This is the only known example of a two atom-bridged 1,3,5-triphenylbenzene derivative to adopt a planar structure.
aromatic compound having fused cyclic substituent in aromatic ring and organic light-emitting diode including the same
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Paragraph 0307; 0308, (2016/10/10)
The present invention refers to to the aromatic ring-fused ring withdrawing substituent and a compound having an same relates to organic light emitting device including, more specifically a represented by [formula A] an alkali-soluble polymer resin compound for an organic light-emitting device including organic light emitting device is characterized in that the. [Formula A] In said [formula A], X has a dementia drug; and shows strong X having substituted group, Y has a dementia drug; and shows strong formula selected from the group consisting Y1 to Y5 having one of substituted group, the n being integers, of 4 to 1, the Y5 formula to Y1 formula and X formula detailed description of the invention is described. (by machine translation)
Selective arylation and vinylation at the α position of vinylarenes
Zou, Yinjun,Qin, Liena,Ren, Xinfeng,Lu, Yunpeng,Li, Yongxin,Zhou, Jianrong
supporting information, p. 3504 - 3511 (2013/07/05)
In intermolecular Heck reactions of styrene and vinylarenes, the aryl and vinyl groups routinely insert at the β position. However, selective insertion at the α position has been very rare. Herein, we provide a missing piece in the palette of Heck reaction, which gave >20:1 α selectivity. The key to our success is a new ferrocene 1,1′-bisphosphane (dnpf) that carries 1-naphthyl groups. Our mechanistic studies revealed that the high α selectivity is partly attributable to the steric effect of dnpf. The rigid and bulky 1-naphthyl groups of dnpf sterically disfavor β insertion. What the Heck! In intermolecular Heck reactions, insertion at the β position of aromatic olefins is very common, but reversal of the selectivity for selective α insertion has been a longstanding problem. A general method to couple aryl and vinyl triflates with aromatic olefins in >20:1 α selectivity is presented. The key to this successful approach is a new ferrocene bisphosphane with naphthyl groups on the phosphorus atom (see scheme; OTf=triflate). Copyright
Modeling, synthesis, and biological evaluation of potential retinoid X receptor (RXR) selective agonists: Novel analogues of 4-[1-(3,5,5,8,8- Pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic Acid (Bexarotene) and (E)-3-(3-(1,2,3,4-tetrahydro-1,1,
Jurutka, Peter W.,Kaneko, Ichiro,Yang, Joanna,Bhogal, Jaskaran S.,Swierski, Johnathon C.,Tabacaru, Christa R.,Montano, Luis A.,Huynh, Chanh C.,Jama, Rabia A.,Mahelona, Ryan D.,Sarnowski, Joseph T.,Marcus, Lisa M.,Quezada, Alexis,Lemming, Brittney,Tedesco, Maria A.,Fischer, Audra J.,Mohamed, Said A.,Ziller, Joseph W.,Ma, Ning,Gray, Geoffrey M.,Van Der Vaart, Arjan,Marshall, Pamela A.,Wagner, Carl E.
, p. 8432 - 8454 (2013/12/04)
Three unreported analogues of 4-[1-(3,5,5,8,8-pentamethyl-5-6-7-8- tetrahydro-2-naphthyl)ethynyl]benzoic acid (1), otherwise known as bexarotene, as well as four novel analogues of (E)-3-(3-(1,2,3,4-tetrahydro-1,1,4,4,6- pentamethylnaphthalen-7-yl)-4-hydr
THERAPEUTIC COMPOUNDS
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Page/Page column 36, (2013/03/28)
The invention provides compounds of formulae (I), (II), (III), and (IV): and salts thereof, as well as pharmaceutical compositions comprising such compounds. The compounds are useful for treating cancers and Alzheimer's disease.
Retinoid compounds and their use
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, (2012/11/06)
The invention relates to retinoid compounds of the formula (I): wherein V is a hydrophobic group;W is a non-polyenic linker; andX is a polar group comprising a hydrogen bond donor; or a salt thereof, and to the use of such compounds in the control of cell differentiation.
Process for preparing retinoid compounds
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Page/Page column 6-7, (2008/06/13)
The application claims a process for the preparation of a RAR modulator according to formula Ia or Ib comprising to sequential Heck couplings steps to elaborated the disubstituted olefin.
Retinoid compounds (I)
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, (2008/06/13)
The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.
