Blood-brain barrier disruption inhibitor

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 231/26 (2006.01) A61K 31/4152 (2006.01) A61P 7/00 (2006.01) A61P 9/00 (2006.01) A61P 25/00 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2513042

The invention aims at providing blood-brain barrier disruption inhibitors. The invention provides blood-brain barrier disruption inhibitors containing as the active ingredient pyrazolone derivatives represented by the general formula (I), physiologically acceptable salts thereof, or hydrates or solvates of the same: (I) wherein R1 is hydrogen, aryl, alkyl, or alkoxycarbonylalkyl, and R2 is hydrogen, aryloxy, arylmercapto, alkyl, or hydroxyalkyl, or R1 and R2 may be united to form alkylene; and R3 is hydrogen, alkyl, cycloalkyl, hydroxyalkyl, benzyl, naphthyl, phenyl, or phenyl which is mono- to tri- substituted with one or more members selected from the group consisting of alkyl, alkoxy, hydroxyalkyl, alkoxycarbonyl, alkylmercapto, alkylamino, dialkylamino, halogeno, trifluoromethyl, carboxyl, cyano, hydroxyl, nitro, amino, and acetamido.

La présente invention concerne des inhibiteurs de rupture de la barrière hémato-encéphalique, et plus particulièrement, de ceux utilisant comme principe actif des dérivés pyrazoloniques représentés par la formule générale (I), certains de leurs sels, hydrates ou solvates physiologiquement admis. Dans cette formule, R?1¿ est hydrogène, aryle, alkyle, ou alcoxy-carbonylalkyle, et R?2¿ est hydrogène, aryloxy, arylmercapto, alkyle, ou hydroxyalkyle. Mais aussi, R?1¿ et R?2¿ peuvent être unis pour former un alkylène; enfin, R?3¿ est hydrogène, alkyle, cycloalkyle, hydroxyalkyle, benzyle, naphtyle, phényle éventuellement mono, bi ou tri-substituté par au moins un élément choisi dans le groupe des alkyle, alcoxy, hydroxyalkyle, alcoxycarbonyle, alkylmercapto, alkylamino, dialkylamino, halogène, trifluorométhyle, carboxyle, cyano, hydroxyle, nitro, amino, et acétamide.

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