C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 275/24 (2006.01) A61K 31/17 (2006.01) A61P 29/00 (2006.01)
Patent
CA 2673219
The invention relates to compounds of formula (I) in which R is selected from halogen, alkyl, alkoxy, aryl and heteroaryl; R1 is selected from 2-hydroxyethyl, 2,3-dihydroxypropyl, 3-hydroxypropyl, 2,2-dihydroxyethyl, 3,3-dihydroxypropyl, 1,3-dioxolane- ethyl, 1,3-dioxane-methyl, 1,3-dioxolane-methyl, 1,3-dioxane-ethyl, 3-fluoro- 2-hydroxypropyl, 3-carboxy-2-hydroxy-propyl, 3-chloro-2-hydroxypropyl, 2-hydroxypropyl, 2-hydroxy-propen-2-yl, morpholinoethyl, piperazinoethyl, hydroxymethyl, benzyl, 4-(hydroxymethyl)benzyl, 4-chlorobenzyl, 4-fluorobenzyl, and 4-hydroxybenzyl. R2 is te/t-butyl or trifluoromethyl; R3 is independently selected from hydrogen, carboxy, cyano, alkyl or hydroxyalkyl, The compounds of formula (I) can be used for the preparation of pharmaceutical compositions for the therapy of inflammatory states, such as chronic neuropathic pain, over-active bladder syndrome, tumor pain, haemorrhoids, inflammatory hyperalgesia, post-intervention pain, dental extraction, airway and gastro-intestinal diseases.
La présente invention concerne des composés de formule (I) dans laquelle R est choisi parmi un halogène, un alkyle, un alcoxy, un aryle et un hétéroaryle ; R1 est choisi parmi le 2-hydroxyéthyle, le 2,3-dihydroxypropyle, le 3-hydroxypropyle, le 2,2-dihydroxyéthyle, le 3,3-dihydroxypropyle, le 1,3-dioxolane-éthyle, le 1,3-dioxane-méthyle, le 1,3-dioxolane-méthyle, le 1,3-dioxane-éthyle, le 3-fluoro-2-hydroxypropyle, le 3-carboxy-2-hydroxy-propyle, le 3-chloro-2-hydroxypropyle, le 2-hydroxypropyle, le 2-hydroxy-propén-2-yle, le morpholinoéthyle, le pipérazinoéthyle, l'hydroxyméthyle, le benzyle, le 4-(hydroxyméthyl)benzyle, le 4-chlorobenzyle, le 4-fluorobenzyle et le 4-hydroxybenzyle ; R2 est le te/t-butyle ou le trifluorométhyle ; R3 est choisi indépendamment parmi l'hydrogène, un carboxy, un cyano, un alkyle ou un hydroxyalkyle. Les composés de formule (I) peuvent être utilisés dans la préparation de compositions pharmaceutiques destinées au traitement de conditions inflammatoires telles que la douleur neuropathique chronique, le syndrome de vessie hyperactive, la douleur d'origine tumorale, les hémorroïdes, l'hyperalgésie inflammatoire, la douleur post-chirurgicale, l'extraction dentaire et les maladies des voies respiratoires ou gastro-intestinales.
Baraldi Pier Giovanni
Borea Pier Andrea
Fruttarolo Francesca
Geppetti Pierangelo
Pavani Maria Giovanna
Kirby Eades Gale Baker
Pharmeste S.r.l.
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