Substituted (4-aminocyclohexen-1-yl)phenyl and...

Details Substituted (4-aminocyclohexen-1-yl)phenyl and... Substituted (4-aminocyclohexen-1-yl)phenyl and...

C - Chemistry, Metallurgy

07

C

C07C 233/80 (2006.01) A61K 31/165 (2006.01) A61K 31/44 (2006.01) A61P 25/06 (2006.01) C07D 213/75 (2006.01)

Patent

CA 2549007

The present invention relates to compounds of formula (I) or a pharmaceutically acceptable acid addition salt thereof, where; X is -C(R4)= or -N=; Ar is phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R1 and R2 are independantly hydrogen or C1-C3 alkyl; R3 is hydrogen, fluoro, or methyl; when X is -C(R4)=, R4 is hydrogen, fluoro, or methyl, provided that no more than one of R3 and R4 may be other than hydrogen; and R5 is hydrogen, methyl, or ethyl. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting dural protein extravasation, and for the treatment or prevention of migraine in a mammal.

L'invention concerne des composés de formule (I) ou un sel d'ajout d'acide pharmaceutiquement acceptable de celui-ci. Dans cette formule, X désigne -C(R?4¿)= ou -N=; Ar désigne phényle, phényle substitué, hétérocycle, ou hétérocycle substitué; R?1¿ et R?2¿ désignent indépendamment hydrogène ou alkyle C¿1?-C¿3?; R?3¿ désigne hydrogène, fluor ou méthyle; lorsque X désigne -C(R?4¿)=, R?4 ¿désigne hydrogène, fluor, ou méthyle, à condition que seul un élément parmi R?3¿ et R?4¿ soit différent de l'hydrogène; et R?5¿ désigne hydrogène, méthyle ou éthyle. Les composés de l'invention sont utiles pour activer des récepteurs de 5-HT¿1F?, pour inhiber une extravasation protéinique durale, et pour traiter ou pour prévenir une migraine chez un mammifère.

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