3-(2-pyrrolidinylmethyl)-indole compounds having 5-ht6 affinity

Details 3-(2-pyrrolidinylmethyl)-indole compounds having 5-ht6 affinity 3-(2-pyrrolidinylmethyl)-indole compounds having 5-ht6 affinity

C - Chemistry, Metallurgy

07

D

C07D 403/06 (2006.01) A61K 31/40 (2006.01) C07D 401/14 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01)

Patent

CA 2287551

Described herein are compounds with affinity for the 5-HT6 receptor, which have general formula (I) wherein: R1 is selected from the group consisting of H and C1-4alkyl; R2 is selected from the group consisting of H, C1-4alkyl and benzyl; R3 is selected from the group consisting of COR5, SO2R5, CONHC1-4alkyl and C(S)SR6; R4a is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; R4b is selected from the group consisting of H, hydroxy, halo, C3- 7cycloalkyloxy, C1-4alkoxy; C1-4alkyl, benzyloxy, phenoxy, trifluoromethyl, trifluoromethoxy and vinyl; R4c is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; R4d is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; R5 is selected from the group consisting of phenyl, pyridyl, thienyl, quinolinyl and naphthyl which are optionally substituted with 1-4 substituents selected from C1-4alkoxy, C1-4alkyl, halo, nitro, trifluoromethyl, trifluoromethoxy, 1,2-methylenedioxy, C1-4alkylcarbonyl, C1- 4alkoxycarbonyl and C1-4alkylS-; and R6 is selected from C1-4alkyl, allyl, propargyl and optionally substituted benzyl wherein the benzyl group is optionally substituted with 1-4 substituents selected from cyano, C1-4alkyl and halo. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.

La présente invention concerne des composés qui présentent une affinité pour le récepteur 5-HT6, de formule générale (I), dans laquelle R<1> est choisi parmi les groupes H et alkyle en C1-4; R<2> est choisi parmi les groupes H, alkyle en C1-4 et benzyle; R<3> est choisi parmi les groupes COR<5>, SO2R<5>, CONHC1-4 alkyle et C(S)SR<6>; R<4a> est choisi parmi les groupes H, OH, halo, alkyle en C1-4 et alcoxy en C1-4; R<4b> est choisi parmi les groupes H, hydroxy, halo, cycloalkyloxy en C3-7, alcoxy en C1-4, alkyle en C1-4, benzyloxy, phénoxy, trifluorométhyle, trifluorométhoxy et vinyle; R<4c> est choisi parmi les groupes H, OH, halo, alkyle en C1-4 et alcoxy en C1-4; R<4d> est choisi parmi les groupes H, OH, halo, alkyle en C1-4 et alcoxy en C1-4; R<5> est choisi parmi les groupes phényle, pyridyle, thiényle, quinolinyle, et naphtyle, éventuellement substitués par des substituants en 1-4 choisis parmi les groupes alcoxy en C1-4, alkyle en C1-4, halo, nitro, trifluorométhyle, trifluorométhoxy, 1,2-méthylènedioxy, alkylecarbonyle en C1-4, alcoxycarbonyle en C1-4, et alkyleS- en C1-4; et R<6> est choisi parmi les groupes alkyle en C1-4, alkyle, propargyle, et éventuellement benzyle substitué dans lequel le groupe benzyle est éventuellement substitué par des substituants en 1-4 choisis parmi les groupes cyano, alkyle en C1-4 et halo. La présente invention concerne aussi l'utilisation de ces composés en tant que médicaments destinés au traitement des troubles dans lesquels se manifeste une inhibition du récepteur 5-HT6, tels que la schizophrénie.

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