Halo substituted aminotetralins

C - Chemistry – Metallurgy – 07 – C

Patent

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260/329.3, 260/5

C07C 217/74 (2006.01) C07C 211/42 (2006.01) C07C 211/60 (2006.01) C07C 323/38 (2006.01)

Patent

CA 2026775

This invention is therapeutically useful tetralins and pharmaceutically acceptable acid addition salts thereof of the formula (see fig.I) wherein X1 is -OR3; wherein R3 is alkyl(C1-C8); alkenyl(C1-C8), -CH2-cycloalkyl(C3-C8) or benzyl; wherein R4 is alkyl(C1-C3); wherein X2 is hydrogen, CF3 or halogen; wherein R7 is hydrogen or methyl; wherein R1 is hydrogen, alkyl(C1-C3), or cyclopropylmethyl; wherein R2 is -CH2-cycloalkyl(C3-C8), alkyl(C1-C8), -(CH2)q-R5 or -CH2CH2-Z-(CH2)rCH3; wherein R5 is phenyl, 2-thiophene or 3-thiophene; wherein Z is oxygen or sulfur; and wherein p is one or 2, q is 2 or 3, and r is zero to 3; with the proviso that when p is 2, X1 is at the 5- or 8- position. These compounds are useful to treat central nervous system disorders.

Tétralines et leurs sels d'addition acceptables en pharmacie, agents thérapeutiques, de formule (voir fig. I), où X1 est -OR3; R3 est un alkyle (C1-C8), un alcényle (C1-C8), un -CH2-cycloalkyle (C3-C8) ou un benzyle; R4 est un alkyle (C1-C3); X2 est un hydrogène, CF3 ou un halogène; R7 est un hydrogène ou un méthyle; R1 est un hydrogène, un alkyle (C1-C3) ou un cyclopropylméthyle; R2 est un -CH2-cycloalkyle (C3-C8), un alkyle (C1-C8), -(CH2)q-R5 ou -CH2CH2-Z-(CH2)rCH3; R5 est un phényle, un 2-thiophène ou 3-thiophène; Z est un oxygène ou un soufre; p est 1 ou 2, q est 2 ou 3, et r est un entier de 0 à 3; à la condition que lorsque p est 2, X1 est en position 5- ou 8-. Ces composés sont utiles pour traiter les troubles du système nerveux central.

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