186374-96-9Relevant academic research and scientific papers
Catalytic nucleophilic fluorination by an imidazolium ionic liquid possessing trialkylphosphine oxide functionality
Paramanik, Minakshmi,Singh, Rekha,Mukhopadhyay, Sulekha,Ghosh, Sunil K.
, p. 47 - 55 (2015)
Abstract The synthesis of a new alkylmethylimidazolium ionic liquid wherein the alkyl group is functionalized with dihexylphosphine oxide moiety at the terminal position has been achieved in four steps from 1-methylimidazole. This hybrid ionic liquid effectively catalyzed the nucleophilic fluorination of primary alkyl mesylates under mild conditions using CsF as the fluoride source with a faster rate compared to butylmethylimidazolium mesylate. The hybrid catalyst was recycled 5 times without compromising the yield and purity of the product. The nucleophilic fluorination has been used for the synthesis of diethyl 2-(5-fluoropentyl)-2-methyl malonate, a precursor of 18F isotopomer of an apoptosis imaging agent and the protected form of O-(2'-fluoroethyl)-l-tyrosine, a 18F isotopomer of a tumor imaging agent.
Self-assembling behaviour of chiral calamitic monoacrylates targeted for polymer stabilisation of polar smectic phases in chiral liquid crystals
Dmochowska, Ewelina,Herman, Jakub,Czerwiński, Micha?,Stulov, Sergei,Bubnov, Alexej,Kula, Przemys?aw
, (2021/03/03)
The stabilisation and control of synclinic and anticlinic chiral liquid crystalline phases remain an actual and highlighted task. This work presents the design and mesomorphic properties of new chiral calamitic reactive mesogens, monoacrylates, based on biphenyl benzoate and phenyl biphenyl-4-carboxylate cores with reactive terminal groups placed far from the chiral chain. The compound's structures, compatible with the components of modern ferroelectric and antiferroelectric liquid crystalline mixtures, are confirmed by mass spectrometry (electron ionization) analysis and proton/carbon nuclear magnetic resonance. All the reactive mesogens possess the self-assembling, i.e. liquid crystalline behaviour with high tendency to create smectic phases in a broad temperature range, which was confirmed by a polarizing optical microscopy, differential scanning calorimetry and broad-band dielectric spectroscopy. Doping of advanced multicomponent mixtures possessing the chiral smectic phases by the designed monoacrylates with further cross-linking procedure, can be an effective and functional tool for stabilising ferroelectric and antiferroelectric phases in various states and hence, can allow the symmetrisation of the switching times in the modes employed surface stabilised geometry; this is a very highlighted task for optoelectronics. Moreover, an evident considerable tendency for thermal polymerisation of specific reactive mesogens can reduce the drawbacks of polymer stabilisation.
COMPOUNDS AND METHODS TO ATTENUATE TUMOR PROGRESSION AND METASTASIS
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Paragraph 0284-0285, (2020/05/28)
This invention relates to certain compounds or pharmaceutically acceptable salts thereof, and for the use of the compounds to treat cancer. In another aspect, the disclosure relates to a pharmaceutical composition comprising a compound of Formula (1), For
Small-Molecule Covalent Modification of Conserved Cysteine Leads to Allosteric Inhibition of the TEAD?Yap Protein-Protein Interaction
Bum-Erdene, Khuchtumur,Zhou, Donghui,Gonzalez-Gutierrez, Giovanni,Ghozayel, Mona K.,Si, Yubing,Xu, David,Shannon, Harlan E.,Bailey, Barbara J.,Corson, Timothy W.,Pollok, Karen E.,Wells, Clark D.,Meroueh, Samy O.
, p. 378 - 13,389 (2019/03/19)
The Hippo pathway coordinates extracellular signals onto the control of tissue homeostasis and organ size. Hippo signaling primarily regulates the ability of Yap1 to bind and co-activate TEA domain (TEAD) transcription factors. Yap1 tightly binds to TEAD4
LEPTIN mRNA COMPOSITIONS AND FORMULATIONS
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Paragraph 0386; 0387; 0388, (2015/07/07)
A formulation comprising a modified synthetic messenger RNA and a delivery agent. The modified synthetic messenger RNA encodes a leptin protein, is non-replicating and is translation-ready. The formulation can be delivered to a subject with congenital leptin deficiency, lipodystrophy or other condition where circulating leptin level is low.
LIPIDS AND LIPID COMPOSITIONS FOR THE DELIVERY OF ACTIVE AGENTS
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Page/Page column 126-127, (2015/07/07)
This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, n and p are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
LIPIDS AND LIPID COMPOSITIONS FOR THE DELIVERY OF ACTIVE AGENTS
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Page/Page column 92-93, (2015/07/07)
This invention provides for a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R3, n, p, L1 and L2 are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
New glucocerebrosidase inhibitors by exploration of chemical diversity of N -substituted aminocyclitols using click chemistry and in situ screening
Díaz, Lucía,Casas, Josefina,Bujons, Jordi,Llebaria, Amadeu,Delgado, Antonio
supporting information; experimental part, p. 2069 - 2079 (2011/06/10)
A library of aminocyclitols derived from CuAAC reaction between N-propargylaminocyclitol 4 and a series of azides [1′25] is described and tested against GCase. Azides have been chosen from a large collection of potential candidates that has been filtered
Indol-3-ylcycloalkyl ketones: Effects of N1 substituted indole side chain variations on CB2 cannabinoid receptor activity
Frost, Jennifer M.,Dart, Michael J.,Tietje, Karin R.,Garrison, Tiffany R.,Grayson, George K.,Daza, Anthony V.,El-Kouhen, Odile F.,Yao, Betty B.,Hsieh, Gin C.,Pai, Madhavi,Zhu, Chang Z.,Chandran, Prasant,Meyer, Michael D.
experimental part, p. 295 - 315 (2010/06/11)
Several 3-acylindoles with high affinity for the CB2 cannabinoid receptor and selectivity over the CB1 receptor have been prepared. A variety of 3-acyl substituents were investigated, and the tetramethylcyclopropyl group was found to lead to high affinity CB2 agonists (5, 16). Substitution at the N1-indole position was then examined. A series of aminoalkylindoles was prepared and several substituted aminoethyl derivatives were active (23-27, 5) at the CB2 receptor.Astudy of N1 nonaromatic side chain variants provided potent agonists at the CB2 receptor (16, 35-41, 44-47, 49-54, and 57-58). Several polar side chains (alcohols, oxazolidinone) were well-tolerated for CB2 receptor activity (41, 50), while others (amide, acid) led to weaker or inactive compounds (55 and 56). N1 aromatic side chains also afforded several high affinity CB2 receptor agonists (61, 63, 65, and 69) but were generally less potent in an in vitro CB2 functional assay than were nonaromatic side chain analogues.
3-CYCLOALKYLCARBONYL INDOLES AS CANNABINOID RECEPTOR LIGANDS
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Page/Page column 63, (2008/06/13)
The present invention provides novel compounds of Formula (I), which are CB2 selective ligands useful for the treatment of pain.
