Benzosulfone derivatives

Details Benzosulfone derivatives Benzosulfone derivatives

C - Chemistry, Metallurgy

07

D

C07D 239/38 (2006.01) A61K 31/44 (2006.01) A61K 31/4439 (2006.01) A61K 31/496 (2006.01) A61P 25/00 (2006.01) C07C 317/36 (2006.01) C07D 213/71 (2006.01) C07D 401/04 (2006.01)

Patent

CA 2258454

The present invention relates to novel compounds of the general formula (see formula I) wherein R1 is hydrogen; R2 is hydrogen, trifluoromethyl or lower alkyl; R3 is hydrogen or amino; or R1 and R2 or R3 and R2 taken together are -CH=CH-CH=CH-; Z is pyrimidin-4-yl, pyridin-4-yl, pyridin-2-yl or phenyl; R4, R5 are each independently hydrogen, lower alkyl, trifluoromethyl, halogen, lower alkoxy, nitrilo, amino, lower alkyl-amino, di-lower alkyl-amino, piperazinyl, morpholinyl, pyrrolidinyl, vinyl, C3-C6 cycloalkyl, C3-C6 cycloalkenyl, t-buthylethinyl, hydroxyalkylethinyl, phenylethinyl, naphthyl, thiophenyl, or phenyl, which may be substituted by halogen, lower alkoxy, lower alkyl, trifluoromethyl or nitro, or a group -NH(CH2)n NR6R7, -N(CH3)(CH2)n NR6R7, -NH(CH2)n-morpholin-4-yl or -NH(CH2)n OH; n is 2-4 R6 and R7 are each independently hydrogen or lower alkyl, and to their pharmaceutically acceptable salts. It has been found that the compounds of formula I possess a selective affinity to 5HT-6 receptors.

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