- Organoarsenic probes to study proteins by NMR spectroscopy
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Arsenical probes enable structural studies of proteins. We report the first organoarsenic probes for nuclear magnetic resonance (NMR) and electron paramagnetic resonance (EPR) spectroscopy to study proteins in solutions. These probes can be attached to ir
- Adekoya, Ibidolapo,Huber, Thomas,Mahawaththa, Mithun C.,Nitsche, Christoph,Orton, Henry W.,Otting, Gottfried
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p. 701 - 704
(2022/01/25)
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- Design, synthesis and identification of silicon-containing HCV NS5A inhibitors with pan-genotype activity
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Modification of a HCV NS5A inhibitor, ombitasvir, led to the identification of 10d with improved pan-genotype NS5A inhibition and better pharmacokinetic properties. The key structural changes to ombitasvir include bioisosteric replacement of carbon with silicon atom. Compared with ombitasvir, the activity of anti-HCV genotypes (GT 1 to 6) of 10d is increased to some extent, especially the inhibitory activity against genotype 3a and 6a is increased by more than seven times, and the dog's in vivo pharmacokinetics properties were also superior to ombitasvir. Further drug evaluation showed that 10d was similar to ombitasvir on plasma protein binding and liver distribution profiles, with no cytotoxicity and no inhibitory effect on both CYP 450 and hERG ligand binding. However, permeability assay results indicated that 10d was not the substrate of P-gp or BCRP transporter, which is different from that of ombitasvir. The results of a 14-day repeat-dose toxicity study identified no toxicity with 10d. Our findings in preclinical tests suggest that the silicon-containing compound 10d could be worthy of continued study as a potential drug candidate.
- Liu, Baomin,Gai, Kuo,Qin, Hui,Liu, Xushi,Cao, Yuan,Lu, Qin,Lu, Dandan,Chen, Deyang,Shen, Hengqiao,Song, Wei,Zhang, Yang,Wang, Xiaojin,Xu, Hongjiang,Zhang, Yinsheng
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- AMIDE COMPOUND
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The present invention relates to compound (I) or a salt thereof which has a RORγt inhibitory action. In the formula (I), each symbol is as defined in the specification.
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Paragraph 0466
(2016/08/17)
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- Heterocyclic compound
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The present invention relates to compound (I) or a salt thereof which has a ROR γ t inhibitory action. wherein each symbol is as defined in the specification.
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Paragraph 0548
(2016/10/08)
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- Assembly of Primary (Hetero)Arylamines via CuI/Oxalic Diamide-Catalyzed Coupling of Aryl Chlorides and Ammonia
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A general and practical catalytic system for aryl amination of aryl chlorides with aqueous or gaseous ammonia has been developed, with CuI as the catalyst and bisaryl oxalic diamides as the ligands. The reaction proceeds at 105-120°C to provide a diverse set of primary (hetero)aryl amines in high yields with various functional groups.
- Fan, Mengyang,Zhou, Wei,Jiang, Yongwen,Ma, Dawei
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supporting information
p. 5934 - 5937
(2015/12/11)
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- Mild and highly selective palladium-catalyzed monoarylation of ammonia enabled by the use of bulky biarylphosphine ligands and palladacycle precatalysts
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A method for the Pd-catalyzed arylation of ammonia with a wide range of aryl and heteroaryl halides, including challenging five-membered heterocyclic substrates, is described. Excellent selectivity for monoarylation of ammonia to primary arylamines was achieved under mild conditions or at rt by the use of bulky biarylphosphine ligands (L6, L7, and L4) as well as their corresponding aminobiphenyl palladacycle precatalysts (3a, 3b, and 3c). As this process requires neither the use of a glovebox nor high pressures of ammonia, it should be widely applicable.
- Cheung, Chi Wai,Surry, David S.,Buchwald, Stephen L.
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supporting information
p. 3734 - 3737
(2013/08/23)
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- Direct stereospecific amination of alkyl and aryl pinacol boronates
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The direct amination of alkyl and aryl pinacol boronates is accomplished with lithiated methoxyamine. This reaction directly provides aliphatic and aromatic amines, stereospecifically, and without preactivation of the boronate substrate.
- Mlynarski, Scott N.,Karns, Alexander S.,Morken, James P.
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supporting information
p. 16449 - 16451,3
(2020/09/15)
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- Ipso-Fluorination of aryltrimethylsilanes using xenon difluoride
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Reaction of aryltrimethylsilanes with xenon difluoride in C 6F6/Pyrex at room temperature gives aryl fluorides in good yield. The reaction is inhibited when acetonitrile is used as solvent but proceeds well in CFCl3/Pyrex or CH 2Cl2/Pyrex. Pyrex appears to be a very effective heterogeneous catalyst for this ipso-fluorination. The reaction does not proceed in PTFE, quartz, soda glass or glassy-carbon flasks or Pyrex flasks pre-rinsed with 2 M NaOH. Aryltrimethylstannanes and arylboronic acids and their esters do not undergo ipso-fluorination under similar conditions. Plausible mechanisms involving electrophilic addition of polarised xenon difluoride [FXeδ+?F→Pyrex δ-] followed by ligand coupling are discussed.
- Lothian, Aileen P.,Ramsden, Christopher A.,Shaw, Maxine M.,Smith, Rachel G.
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p. 2788 - 2793
(2011/05/02)
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- PYRROLE-3-CARBOXAMIDE DERIVATIVES FOR THE TREATMENT OF OBESITY
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The present invention relates to compounds of Formula (I) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.
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Page/Page column 12; 34
(2010/02/13)
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- Diphenylphosphinophenolate: A ligand for the palladium-catalysed silylation of aryl halides activating simultaneously both palladium and silicon
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Diphenylphosphinophenolate was found to be an effective ligand for the palladium-catalysed silylation of aryl halides, activating not only palladium but also silicon of a disilane, where aryl bromides and iodides having such substituents as methyl, methoxy, amino, ethoxycarbonyl, trifluoromethyl, formyl or phenyl are applicable to the reaction with hexamethyldisilane to give the corresponding trimethylsilylarenes.
- Shirakawa,Kurahashi,Yoshida,Hiyama
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p. 1895 - 1896
(2007/10/03)
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- Palladium-catalysed synthesis of monodisperse, controlled-length, and functionalized oligoanilines
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The palladium-catalyzed animation of aryl halides, in conjunction with an orthogonal protective group scheme, forms the basis of two routes to oligoaniline precursors. One method consists of a bidirectional chain growth from a symmetric core piece, wherea
- Sadighi, Joseph P.,Singer, Robert A.,Buchwald, Stephen L.
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p. 4960 - 4976
(2007/10/03)
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- Radiosynthesis, Cerebral Distribution, and Binding of -1-(p-Iodophenyl)-3-(1-adamantyl)guanidine, a Ligand for ? Binding Sites
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An analog of 1,3-di-o-tolylguanidine (DTG), -labeled 1-(p-iodophenyl)-3-(1-adamantyl)guanidine (PIPAG), was synthesized as a potential ligand for cerebral ? binding sites.Data from in vitro binding experiments and in vivo experiments on brain distribution suggested that PIPAG binds to ? binding sites with high affinity (Kd in low nanomolar range) as determined by Scatchard analysis and relative potencies of ?-specific drugs.Haloperidol had the highest potency to inhibit PIPAG binding.It was followed by DTG, BMY 14802, and (+)-N-allylnormetazocine.Compounds with high affinities for dopamine receptors (but low affinity for ? binding sites), for opioid receptors, for nicotinic acetylcholine receptors, and for phencyclidine receptors were ineffective inhibitors of PIPAG binding.
- Kimes, Alane S.,Wilson, Alan A.,Scheffel, Ursula,Campbell, Bruce G.,London, Edythe D.
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p. 4683 - 4689
(2007/10/02)
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