402-51-7Relevant academic research and scientific papers
COMPOUND HAVING BET INHIBITORY ACTIVITY AND PREPARATION METHOD AND USE THEREFOR
-
Paragraph 0439-0440, (2020/12/22)
The invention relates to the field of pharmaceutical chemistry. Specifically, the present invention relates to a series of BET (bromodomain and extra-terminal domain) inhibitors having a novel structure, particularly inhibitors targeting BRD4 (Bromodomain-containing protein 4), and a preparation method and use therefor. The structure thereof is shown in the following general formula (I). Said compounds or a stereoisomer, racemate, geometric isomer, tautomer, prodrug, hydrate, solvate, or crystal form thereof, or a pharmaceutically acceptable salt thereof, and the pharmaceutical compsosition thereof can be used for the treatment and/or prevention of related diseases mediated by bromodomain proteins.
Synthesis of trifluoromethylated α-hydroxy acids and their derivatives based on alkyl trifluoropyruvates
Vasilyeva,Vorobyeva
, p. 1426 - 1432 (2018/10/31)
The reactions of trifluoropyruvates with nitromethane and arylmagnesium bromides leading to trifluoromethyl-containing α-hydroxy acid esters were studied and various derivatives of the acids were obtained.
COMPOSITIONS FOR TREATING NEURODEGENERATIVE DISEASES
-
Paragraph 0322, (2018/12/12)
The present disclosure relates to novel compounds, pharmaceutical compositions containing the compounds and methods of using the compounds and pharmaceutical compositions for treating neurodegerative diseases, including Alzheimer's disease and cognitive decline. Methods for inhibiting synapse number decline or membrane trafficking abnormalities associated with exposure of a neuronal cell to Abeta species are also disclosed.
Preparation of Trifluoromethylphenyl Magnesium Halides in the Presence of LiCl and Synthesis of 2′-Trifluoromethyl-Aromatic Ketones
Nakatani, Jiro,Nozoe, Tatsuhiro
, p. 1633 - 1636 (2016/09/23)
The effect of LiCl-promoted insertion of magnesium turnings into halogenated-trifluoromethylbenzenes for Grignard reagent synthesis was investigated. In the presence of less than 1.0 equiv of LiCl, chloro(trifluoromethyl)benzene Grignard reagents were easily generated. The 2-trifluoromethylphenyl magnesium chloride Grignard reagent was obtained in high yield and 2′-trifluoromethyl-substituted aromatic ketone was synthesized through reaction of the obtained Grignard reagent with a carboxylic anhydride in an 83% yield.
Palladium-catalyzed aerobic oxidative double allylic C-H oxygenation of alkenes: A novel and straightforward route to α,β-unsaturated esters
Yang, Wanfei,Chen, Huoji,Li, Jianxiao,Li, Chunsheng,Wu, Wanqing,Jiang, Huanfeng
supporting information, p. 9575 - 9578 (2015/06/08)
A mild tandem oxidative functionalization of allyl aromatic hydrocarbons was accomplished using the catalytic system of Pd(OAc)2/DMA under 1 atm O2. The green twofold C-O bond formation involving double allylic C-H oxygenation unlocks opportunities for markedly different synthetic strategies. Moreover, the reaction affords aryl α,β-unsaturated esters directly from readily available terminal olefins in moderate to good yields with excellent chemo- and stereoselectivities.
Novel Sulfonaminoquinoline Hepcidin Antagonists
-
Page/Page column 158, (2012/09/05)
The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases.
meso-Substituted bisanthenes as soluble and stable near-infrared dyes
Li, Jinling,Zhang, Kai,Zhang, Xiaojie,Huang, Kuo-Wei,Chi, Chunyan,Wu, Jishan
experimental part, p. 856 - 863 (2010/04/30)
(Chemical Equation Presented) Three meso-substituted bisanthenes, 4-6, were prepared in a short synthetic route from the bisanthenequinone. They exhibit largely improved stability and solubility in comparison to the parent bisanthene. All of these compoun
Use of73Ge NMR Spectroscopy and X-ray Crystallography for the Study of electronic interactions in substituted tetrakis(phenyl)-, -(phenoxy)-, and -(thiophenoxy)germanes
Yoder, Claude H.,Agee, Tamara M.,Griffith, Allison K.,Schaeffer Jr., Charles D.,Carroll, Mary J.,Detoma, Alaina S.,Fleisher, Adam J.,Gettel, Cameron J.,Rheingold, Arnold L.
experimental part, p. 582 - 590 (2010/04/25)
NMR chemical shifts of 1H, 13C, and 73Ge, molecular modeling, and single-crystal X-ray diffraction results are reported for a series of substituted tris- and tetrakis(phenyl)germanes of the type (XC6H4)3GeY and (XC6H 4)4Ge, where X = o-, m-, and p-OCH3, o-, m-, and p-OC2H5, m- and p-CF3, H, p-C(CH 3)3, p-Cl; and Y = Cl and H. Chemical shifts and X-ray data are also reported for o-CH3 and o-OCH3 tetrakis(phenoxy)- ((XC6H4O)4Ge) and thiophenoxygermanes ((XC6H4S)4Ge). For tetrakis derivatives, 73Ge resonances are observed for all but the o-methoxyphenoxy compound, for which the inability to detect a resonance is attributed to rapid quadrupolar relaxation caused by intramolecular interactions of the methoxy oxygen with the central atom. The observation of a relatively broad, slightly upfield 73Ge resonance in the analogous phenyl and thiophenoxy derivatives suggests, as do the results of molecular modeling, that in these compounds there is some hypercoordination. The solid-state structures show bond angles at the aromatic carbon bearing the alkoxy group that suggest an interaction of the alkoxy oxygen with germanium. Oxygen-germanium bond distances are about 17% shorter than the sum of the van der Waals radii.
Asymmetric bromolactonization catalyzed by a C3-symmetric chiral trisimidazoline
Murai, Kenichi,Matsushita, Tomoyo,Nakamura, Akira,Fukushima, Shunsuke,Shimura, Masato,Fujioka, Hiromichi
supporting information; experimental part, p. 9174 - 9177 (2011/02/26)
A productive alliance: In an enantioselective organocatalytic bromolactonization of 5-substituted hex-5-enoic acids (see scheme), it appears that the formation of an ion pair through interaction of the trisimidazoline catalyst 1 with the substrate both cr
Vanilloid receptor ligands and their use in treatments
-
Page/Page column 11; 13; 27; 30; 33; 35, (2009/04/24)
Bicyclic 3,4-fused piperidine compounds, and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotizing agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
