- NOVEL PYRIDIN-2(1H)ONE DERIVATIVES, THEIR PREPARATION AND THEIR USE FOR THE TREATMENT OF PAIN
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The present invention concerns novel pyridin-2(1H)one derivatives, their process of preparation and their use in therapeutics, in particular as agents for treating and/or preventing pain.
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Page/Page column 15; 22-23
(2021/04/10)
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- Pyridin-2(1H)one derivatives: A possible new class of therapeutics for mechanical allodynia
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Mechanical Allodynia (MA), a frequent chronic pain symptom caused by innocuous stimuli, constitutes an unmet medical need, as treatments using analgesics available today are not always effective and can be associated with important side-effects. A series of 3,5-disubstituted pyridin-2(1H)-ones was designed, synthesized and evaluated in vivo toward a rat model of inflammatory MA. We found that the series rapidly and strongly prevented the development of MA. 3-(2-Bromophenyl)-5-(phenylamino)pyridin-2(1H)-one 69, the most active compound of the series, was also able to quickly reverse neuropathic MA in rats. Next, when 69 was evaluated toward a panel of 50 protein kinases (PK) in order to identify its potential biological target(s), we found that 69 is a p38α MAPK inhibitor, a PK known to contribute to pain hypersensitivity in animal models. 3,5-Disubstituted pyridin-2(1H)-ones thus could represent a novel class of analgesic for the treatment of MA.
- Abrunhosa-Thomas, Isabelle,Anizon, Fabrice,Artola, Alain,Dallel, Radhouane,Descheemaeker, Amélie,Giraud, Francis,Moreau, Pascale,Nauton, Lionel,Pinto-Pardo, Nicolas,Théry, Vincent,Visseq, Alexia
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- NITROGENATED AROMATIC COMPOUND, ORGANIC SEMICONDUCTOR MATERIAL, AND ORGANIC ELECTRONIC DEVICE
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Provided are a nitrogen-containing aromatic heterocyclic compound useful as an organic semiconductor material and an organic electronic device using this compound. The nitrogen-containing aromatic heterocyclic compound has a fused indole skeleton represented by the following formula (1), the organic semiconductor material contains the said compound, and the organic electronic device uses the said organic semiconductor material. In general formula (1), X is N-A', O, S, or Se; A is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group exclusive of a fused heterocycle consisting of 4 rings or more; and R is a hydrogen atom, an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group exclusive of a fused heterocycle consisting of 4 rings or more.
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Paragraph 0126; 0129
(2013/07/31)
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- NITROGENATED AROMATIC COMPOUND, ORGANIC SEMICONDUCTOR MATERIAL, AND ORGANIC ELECTRONIC DEVICE
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Provided are a novel nitrogen-containing aromatic heterocyclic compound and an organic electronic device using the compound. This nitrogen-containing aromatic compound is represented by the general formula (1). Further, the present invention relates to or
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Paragraph 0146
(2013/09/11)
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- Synthesis of (3-indolyl)heteroaromatics by Suzuki-Miyaura coupling and their inhibitory activity in lipid peroxidation
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A variety of (3-indolyl)heteroaromatic compounds were synthesized by Suzuki-Miyaura coupling of 3-indolylboronic acid and halogenated heteroaromatics. 2-(3-Indolyl)thiophene showed potent inhibitory activity against lipid peroxidation by rat liver microsome.
- Nishida, Atsushi,Miyashita, Naoki,Fuwa, Mihoko,Nakagawa, Masako
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p. 473 - 476
(2007/10/03)
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- A Highly Enantioselective Asymmetric Hydrogenation Route to β-(2R,3S)-Methyltryptophan
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Asymmetric hydrogenation of a protected (Z)-dehydro-β-methyltryptophan derivative 2 with (R,R)-Me-DuPHOS-Rh catalysis was achieved in 97percent ee.Deprotection then afforded (2R,3S)-β-methyltryptophan 1.
- Hoerrner, R. Scott,Askin, David,Volante, R. P.,Reider, Paul J.
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p. 3455 - 3458
(2007/10/03)
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