| 摘要 |
Benzenesulphonamide compounds or salts thereof of Formula I wherein: P is phenyl, naphthyl, anthracenyl, a bicyclic heterocyclic ring, a tricyclic heteroaromatic ring or is a 5- to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulphur; A is a single bond, a C1-6alkylene or a C1-6 alkenylene group; B is SO2; R1 is halogen, C1-6 alkyl optionally substituted by one or more fluorine atoms, C3-6 cycloalkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkanoyl, C1-6 alkoxy, OCF3, hydroxy, hydroxyC1-6 alkyl, hydroxyC1-6 alkoxy, C1-6 alkoxyC1-6 alkoxy, nitro, cyano, NR10R11 where R10 and R11 are independently hydrogen, C1-6 alkyl or optionally substituted phenyl, SR11 where R11 is defined as above or R1 is optionally substituted phenyl, naphthyl, a bicyclic heterocyclic ring or is a 5- to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulphur, or R1 together with a second R1 substituent forms a group -O-CH2-O-, OCH2CH2O-, -CH2CH2CH2- or -CH2CH2CH2CH2-; n is 0, 1, 2, 3, 4, 5 or 6; R2 is hydrogen, C1-6 alkyl, arylC1-6 alkyl or together with group P form a 5- to 8-membered ring optionally substituted with one or more C1-6 alkyl groups; R3 is hydrogen, halogen, C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkanoyl, C1-6 alkoxy, optionally substituted with one or more fluorine atoms, hydroxy, hydroxyC1-6 alkyl, hydroxyC1-6 alkoxy, C1-6 alkoxyC1-6 alkoxy, nitro, trifluromethyl, cyano or aryl or together with the group R5 forms a group (CH2)2O or (CH2)3O optionally substituted with 1 or more C1-6 alkyl groups; R4 is-X(CH2)p-R6 where X is a single bond, CH2, O, NH or N-alkyl and p is 0 to 6 and R6 is an optionally substituted 4- to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from nitrogen, sulphur or oxygen, or R6 is NR7R8 where R7 and R8 are independently hydrogen, C1-6 alkyl or arylC1-6 alkyl; and R5 is a group R3 or together with R3 forms a group (CH2)2O or (CH2)3O optionally substituted with 1 or more C1-6 alkyl groups. - having pharmacological activity (5-HT6 receptor antagonists), processes for their preparation, compositions containing them, and their use in the treatment of anxiety and/or depression.
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