- 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; 24-25
(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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- Synthesis of nonsymmetrical 5-Aryl-2-indolopyrrole derivatives via controlled mono Suzuki-Miyaura cross-coupling on N-Boc-2,5-dibromopyrrole
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The first example of mono Suzuki-Miyaura cross-coupling of N-Boc-2,5-dibromopyrrole with a boronic acid (indol-2-ylboronic acid) is reported. The resulting 2-indolyl-5-bromopyrrole derivative was in turn coupled with a variety of aryl- or heteroarylboronic acids thereby providing the corresponding non-symmetrical 2,5-disubstituted pyrroles in good to excellent yields. The tert-butoxycarbonyl (Boc) groups could be easily removed to give the completely deprotected products. Georg Thieme Verlag Stuttgart - New York.
- Beaumard, Floriane,Dauban, Philippe,Dodd, Robert H.
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experimental part
p. 4033 - 4042
(2011/02/22)
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- Nicotinamide n-oxide derivatives as vanilloid-1 receptor modulators
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The present invention relates to vanilloid receptor modulators of formula (I) wherein X is selected from phenyl, naphthyl, pyridine, quinoline or isoquinoline and Y is optionally substituted phenyl or pyridyl ring, to processes for the preparation thereof
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Page/Page column 4
(2009/05/29)
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- BIARYLCARBOXYARYLAMIDES AS VANILLOID-1 RECEPTOR MODULATORS
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The present invention provides compounds of formula (I): wherein A and Z are as defined in the description, along with methods for preparing such derivatives and their use for the treatment of inflammatory diseases such as neuropathic pain.
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Page/Page column 5-6
(2008/06/13)
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- Synthesis of quinolyl- and isoquinolyl heteroarylamines using palladium catalyzed suzuki cross-coupling reaction
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Quinolyl- and isoquinolylboronic acids are prepared from 5-bromoquinoline and 5-bromoisoquinoline, respectively, via halogen-metal exchange. Suzuki cross-coupling of these compounds with haloheteroarylamine leading to the corresponding heteroarylamine derivatives is described.{A figure is presented}.
- Lee, Ihl Young Choi,Jung, Myung Hee,Lim, Hee-Jeong,Lee, Hyo Won
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p. 2505 - 2511
(2007/10/03)
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- MODULATORS OF THE GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-KB ACTIVITY AND USE THEREOF
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A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) its stereoisomers thereof, or a solvate thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Z is CONR1R2 or CH2NR1R2 and where at least one of X1 - X8 is N, and R, Ra, Rb, Rc and Rd are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
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Page/Page column 61
(2008/06/13)
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