4-aminoalkoxy-1,3-dihydrobenzoimidazol-2-thiones...

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 235/28 (2006.01) A61K 31/415 (2006.01) A61K 31/47 (2006.01) C07D 401/12 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2278718

This invention relates to a novel series of compounds having potency at the dopamine D2 receptor which are illustrated by formula (I) wherein R1 is hydrogen or C1-C6 alkyl; R2 is hydrogen or C1-C6 alkyl; R3 is selected from hydrogen, straight-chain and branched alkyl group having up to 10 carbon atoms, cyclohexylmethyl or -(CH2)mAr where Ar is phenyl, naphthyl, thienyl, furanyl or pyridinyl, each optionally substituted by one or two substituents selected independently from C1-C6 alkyl, halogen, C1-C6 alkoxy and trifluoromethyl; or NR2R3 is 1,2,3,4-tetrahydroquinolin-1-yl or 1,2,3,4- tetrahydroisoquinolin-2-yl; m is 1-5; n is 1 or 2; Y is halogen, C1-C6 alkyl, and C1-C6 alkoxy; or a pharmaceutically acceptable salt thereof.

L'invention concerne une nouvelle série de composés présentant une activité au niveau du récepteur de la dopamine D¿2?, qui sont illustrés par la formule (I), ou bien un sel pharmaceutiquement acceptable de ceux-ci. Dans cette formule, R?1¿ est hydrogène ou alkyle C¿1?-C¿6?; R?2¿ est hydrogène ou alkyle C¿1?-C¿6?; R?3¿ est choisi parmi hydrogène, un groupe alkyle à chaîne droite et ramifié possédant jusqu'à dix atomes de carbone, cyclohexylméthyle ou bien -(CH¿2?)¿m?Ar où Ar est phényle, naphtyle, thiényle, furanyle ou pyridinyle, éventuellement substitués par un ou deux substituants choisis indépendamment parmi alkyle C¿1?-C¿6?, halogène, alcoxy C¿1?-C¿6? et trifluorométhyle; ou bien NR?2¿R?3¿ est 1,2,3,4-tétrahydroquinoléin-1-yle ou 1,2,3,4-tétrahydroisoquinoléin-2-yle; m vaut 1-5; n vaut 1 ou 2; Y est halogène, alcyle C¿1?-C¿6? et alcoxy C¿1?-C¿6?.

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