2655-84-7Relevant academic research and scientific papers
ARYL AND HETEROARYL COMPOUNDS, AND THERAPEUTIC USES THEREOF IN CONDITIONS ASSOCIATED WITH THE ALTERATION OF THE ACTIVITY OF GALACTOCEREBROSIDASE
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Page/Page column 83, (2021/06/04)
The application is directed to compounds of formulae (IA) and (IB): (IA) and (IB), and their salts and solvates, wherein R1a, R2a, A1, A2, A3, A4, R1b, R2b, B1, B2, B3, and G are as set forth in the specification, as well as to methods for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or prevention of, e.g., lysosomal storage diseases, such as Krabbe's disease, and α-synucleinopathies, such as Parkinson's disease.
LIQUID CRYSTAL COMPOUND HAVING BENZOTHIOPHENE, LIQUID CRYSTAL COMPOSITION AND LIQUID CRYSTAL DISPLAY DEVICE
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Paragraph 0209, (2018/10/30)
A compound, represented by formula (1): In formula (1), R1 is hydrogen, alkyl or the like; ring A1 and ring A2 are independently 1,4-cyclohexylene, 1,4-phenylene or the like; Z1, Z2 and Z3
Base Mediated Synthesis of Alkyl-aryl Ethers from the Reaction of Aliphatic Alcohols and Unsymmetric Diaryliodonium Salts
Sundalam, Sunil K.,Stuart, David R.
, p. 6456 - 6466 (2015/06/30)
The base mediated coupling of aliphatic alcohol pronucleophiles with unsymmetric diaryliodonium salt electrophiles is described. This metal-free reaction is operationally simple, proceeds at mild temperature, and displays broad substrate scope to generate industrially important alkyl-aryl ethers in moderate to excellent yield. The synthetic utility of these reactions is demonstrated, and aspects of sustainability are highlighted by the use of unsymmetric aryl(mesityl)iodonium arylating reagents.
3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands
Hewings, David S.,Wang, Minghua,Philpott, Martin,Fedorov, Oleg,Uttarkar, Sagar,Filippakopoulos, Panagis,Picaud, Sarah,Vuppusetty, Chaitanya,Marsden, Brian,Knapp, Stefan,Conway, Stuart J.,Heightman, Tom D.
supporting information; experimental part, p. 6761 - 6770 (2011/12/04)
Histone-lysine acetylation is a vital chromatin post-translational modification involved in the epigenetic regulation of gene transcription. Bromodomains bind acetylated lysines, acting as readers of the histone-acetylation code. Competitive inhibitors of this interaction have antiproliferative and anti-inflammatory properties. With 57 distinct bromodomains known, the discovery of subtype-selective inhibitors of the histone-bromodomain interaction is of great importance. We have identified the 3,5-dimethylisoxazole moiety as a novel acetyl-lysine bioisostere, which displaces acetylated histone-mimicking peptides from bromodomains. Using X-ray crystallographic analysis, we have determined the interactions responsible for the activity and selectivity of 4-substituted 3,5-dimethylisoxazoles against a selection of phylogenetically diverse bromodomains. By exploiting these interactions, we have developed compound 4d, which has IC50 values of 5 μM for the bromodomain-containing proteins BRD2(1) and BRD4(1). These compounds are promising leads for the further development of selective probes for the bromodomain and extra C-terminal domain (BET) family and CREBBP bromodomains.
DIMESYLATE SALTS OF NEUROPEPTIDE Y LIGANDS
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Page 6-7, (2010/11/30)
The dimesylate salt of cis-1-(3-ethoxyphenyl)-1-(4-phenylpiperazin-1-yl)4-methyl-cyclohexane has superior properties and is useful to treat physiological disorders associated with an excess of neuropeptide Y.
One-step preparation of some 3-substituted anisoles
Zilberman, Joseph
, p. 303 - 305 (2013/09/06)
A one-step preparation of 3-bromoanisole, 3-chloroanisole, and 3-trifluoromethylanisole from the corresponding 3-substituted nitrobenzenes is carried out by nucleophilic aromatic substitution of the nitro group with sodium or potassium methoxide, employing an effective amount of a phase-transfer catalyst (PTC), in a medium of a nonpolar aprotic solvent, under aerobic conditions, at a temperature of 50-65°C. The alkali methoxide used can be a pre-prepared solid, or it can be prepared in situ from the alkali hydroxide and methanol. The methoxydenitration proved to be very sensitive to the type of PTC. The effect of the solvent on the reaction is discussed. The targeted anisoles are obtained in yields of more than 80% and purities of greater than 99%.
Anilide derivative, production and use thereof
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, (2008/06/13)
This invention is to provide a compound of the formula: wherein R1is an optionally substituted 5- to 6-membered ring; the ring A is an optionally substituted 6- to 7-membered ring; the ring B is an optionally substituted benzene ring; n is an integer of 1 or 2; Z is a chemical bond or a divalent group; R2is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, (2) an optionally substituted nitrogen-containing heterocyclic ring group which may contain a sulfur atom or an oxygen atom as ring constituting atoms and wherein a nitrogen atom may form a quaternary ammonium, (3) a group binding through a sulfur atom or (4) a group of the formula: ?wherein k is 0 or 1, and when k is 0, a phosphorus atom may form a phosphonium; and R5and R6are independently an optionally substituted hydrocarbon group, an optionally substituted hydroxy group or an optionally substituted amino group, and R5and R6may bind to each other to form a cyclic group together with the adjacent phosphorus atom, or a salt thereof , which is useful for antagonizing CCR5 and also for the prevention and treatment of infectious disease of HIV.
DIMESYLATE SALTS OF NEUROPEPTIDE Y LIGANDS
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, (2008/06/13)
The dimesylate salt of cis-1-(3-ethoxyphenyl)-1-(4-phenylpiperazin-1-yl)4-methyl-cyclohexane has superior properties and is useful to treat physiological disorders associated with an excess of neuropeptide Y.
