N-phenyl-n-(4-piperidinyl) amides useful as analgesics

Details N-phenyl-n-(4-piperidinyl) amides useful as analgesics N-phenyl-n-(4-piperidinyl) amides useful as analgesics

C - Chemistry, Metallurgy

07

D

167/232, 260/292

C07D 211/58 (2006.01) A61K 31/445 (2006.01) C07D 211/66 (2006.01)

Patent

CA 2010011

N-Phenyl-N-piperdinyl)amide derivatives are disclosed having the general formula (I). (see fig.I) wherein: X is a member selected from the group consisting of: alkoxy-carbonyl-lower alkyl, lower alkyl-carbor-lyloxy-lower alkyl, alkenyloxy-carbonyl-lower alkyl, and (C1-2)alkoxy-(C1-2)alkoxy-carbonyl-lower alkyl. Ar is a member selected from the group consisting of phenyl, mono-, di- and tri-substituted phenyl, wherein each subtitutuent is independently selected from the group consisting of halo, lower alkyl, lower alkoxy and trifluoromethyl; R is a member selected from the group consisting of lower alkyl, and lower alkoxy-lower alkyl; R1 is a member selected from the group consisting of hydrogen, lower alkoxy-carbonyl, and methoxymethyl; and R2 is a member selected from the group consisting of hydrogen and methyl; and the diastereomeric and enantiomeric isomers thereof, and the acid addition salts of said compounds and isomers. The compounds exhibit analgesic activity having relatively short durations of analgesic action. The invention embraces the compounds (I), pharmaceutical compositions of (I) and methods of providing analgesia with (I). Also included are certain novel intermediates for making (I).

Dérivés de N-phényl-N-pipéridinyl)amide de formule générale (I) (voir fig. I) où X est choisi parmi les groupes suivants : alcoxy-carbonyl-alkyle inférieur, alkyle inférieur-carbor-lyloxy-alkyle inférieur, alcényloxy-carbonyl-alkyle inférieur et alcoxy(C1-2)-alcoxy(C1-2)-carbonyl-alkyle inférieur. Ar est choisi parmi les groupes suivants : phényle, phényle avec mono-, di- et trisubstitution, où chaque substituant est choisi indépendamment l'un de l'autre parmi les groupes suivants : halo, alkyle inférieur, alcoxy inférieur et trifluorométhyle; R est choisi parmi un alkyle inférieur et un alcoxy inférieur-alkyle inférieur; R1 est choisi parmi un hydrogène, un alcoxy inférieur-carbonyle et un méthoxyméthyle; R2 est choisi parmi l'hydrogène et un groupe méthyle; leurs diastéréoisomères et énantiomères, ainsi que leurs sels d'addition avec un acide et les isomères correspondants. Ces composés ont des propriétés d'analgésiques avec une durée d'effet analgésique relativement courte. L'invention englobe les composés (I), les compositions pharmaceutiques de (I), ainsi que des méthodes d'analgésie utilisant les composés (I). L'invention donne également certains nouveaux intermédiaires pour la préparation des composés (I).

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