Therapeutically useful tetralin derivatives

C - Chemistry – Metallurgy – 07 – C

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C07C 217/74 (2006.01) C07C 323/25 (2006.01) C07C 323/38 (2006.01) C07D 333/20 (2006.01)

Patent

CA 1331191

ABSTRACT This invention is therapeutically useful tetralins and pharmaceuticallyacceptable acid addition salts thereof of the formula Image wherein YR1 is OR1 at the 8 position where R1 is -CH2-(C3-8 cycloalkyl); R2 is hydrogen or C1-3 alkyl; R3 is -CH2-(C3-8 cycloalkyl); R4 is hydrogen, C1-8 alkyl, -CH2-(C3-4 cycloalkyl), -(CH2)m-R5 or -CH2-CH2-X-(CH2)nCH3, n is zero to 3 and m is 2 or 3; X is oxygen or sulfur; R5 is phenyl, C1-3 alkoxy, C1-3 alkyl, 2-thiophene, 3-thiophene, or phenyl substituted with one or two substituent groups selected from chlorine, bromine or fluorine; and with the proviso that when R3 contains more than four carbon atoms and R4 is alkyl, said alkyl contains from 1 to 3 carbon atoms. Alternatively, -YR1 is -S-(C1-3 alkyl) at the 5, 6, 7 or 8 position of the aromatic ring or OR1 at the 8 position where R1 is selected from the group consisting of C1-8 alkyl, C2-8 alkenyl, -CH2-(C3-8 cycloalkyl) or benzyl; R2 is hydrogen or (C1-C3) alkyl; R3 is -CH2-(C3-C8) cycloalkyl; R4 is -(CH2)m-(2-thiophenyl or 3-thiophenyl); and m is 2 or 3.

593340

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