HETEROCYCLIC ARYL SULPHONES, SUITABLE FOR TREATING DISORDERS RESPONSIVE TO 5HT₆ RECEPTOR MODULATION

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to novel compounds of formula (I) ; , where: n equals 0, 1, 2; G denotes CH₂, CHR³; R¹ denotes H, C₁-C₆-alkyl, C₃-C₆-alkenyl, -CH₂Ph; R², R³, R⁴ independently denote H, CH₃, -CH₂F, -CHF₂, CF₃; A denotes 1,4-Ph, 1,3-Ph, which can be optionally substituted with 1-4 substitutes selected from halogen, C₁-C₄-alkyl, C₁-C₄alkoxy, fluorinated C₁-C₄-alkyl and fluorinated C₁-C₄alkoxy; E denotes NR⁵, where R⁵ denotes H, C₁-C₃-alkyl; Ar denotes a radical of formula ; and ;where: R^a denotes halogen, C₁-C₆-alkyl, fluorinated C₁-C₆-alkyl, C₁-C₆-alkoxy, fluorinated C₁-C₆-alkoxy, phenyl sulphonyl, CN, -NR⁶R⁷, where R⁶ and R⁷, together with an N atom, form a 5- or 6-member saturated ring or denotes a 5-member saturated or unsaturated aromatic or non-aromatic heterocyclic ring containing, as ring members, 1, 2 or 3 heteroatoms selected from N, O and S, and where the heterocyclic ring can carry 1, 2 or 3 substitutes selected from halogen and C₁-C₆-alkyl, or denotes a 6-member saturated heterocyclic ring containing, as ring members, one N and one O atom; R^b and R^c independently denote H, halogen, CH₃, OCH₃, CH₂F, OCH₂F, CHF₂, OCHF₂, CF₃, OCF₃, CH₂CH₂F, OCH₂CH₂F, CH₂CHF₂, OCH₂CHF₂, CH₂CF₃ or OCH₂CF₃; R^d denotes R^a or a 5- or 6-member heteroaromatic ring containing, as ring members, 1, 2 or 3 heteroatoms selected from N, O and S, and where the heteroaromatic ring can carry 1 substitute selected from C₁-C₆-alkyl and C₁-C₆-alkylthio; R^e denotes H or is defined as R^a; R^f is defined as R^a; k equals 0, 1, 2, 3; j equals 0, 1, 2, 3, 4; provided that R^a does not denote F, CH₂F, CHF₂, CF₃, OCF₃, if A denotes 1,4-Ph, Ar denotes a radical of formula (A) and R^b and R^c denote H, halogen; except compounds, where R¹ denotes propyl, G denotes CH₂, n equals 1, A denotes 1,4- Ph, E denotes NH, Ar denotes a radical of formula (F) and R^d denotes halogen, C₁-C₆-alkyl, C₂-C₆-alkenyl or a 5-member heteroaromatic ring; and physiologically acceptable acid addition salts thereof.;EFFECT: compounds exhibit 5HT₆ receptor simulating activity, which allows for their use in a pharmaceutical composition.;25 cl, 6 tbl, 107 ex