| 摘要 |
The use of amino-naphthalene N-phenylsulfonamide derivatives (I) as medicaments having 5-HT6 receptor antagonist activity is new. The use of amino-naphthalene N-phenylsulfonamides derivatives of formula (I) or their salts is claimed in the production of medicaments for the prevention and/or treatment of diseases treatable with 5-HT6 receptor antagonists is new. R1 = H or -CO-T; R2 = T substituted by C- or N-bonded 5- or 6-membered heterocyclyl containing 1-3 of O, S and/or N as heteroatom(s); or -CO-R4, -SO2R5, -COOR6, -S(O)T or -C(=NH)-R8; NR1R2 = up to 6C saturated or unsaturated ring, optionally having 1 or 2 ring C replaced by O, S, SO, CO or NR16 and optionally fused with a phenyl ring; R1 and R2 may both = H, if A or J = SO2T; R3 = -NHCOR17 or -CONHR17; R4 = T (optionally substituted by NH2, NHCOOT or C- or N-bonded 5- or 6-membered saturated heterocyclyl containing 1-3 of O, S and/or N as heteroatom(s)); 5- or 6-membered heteroaryl containing 1-3 of O, S and/or N as heteroatom(s); or 3-7C cycloalkyl, COOT or NR9R10; R9, R10 = H, T (optionally substituted by 1-3 of halo, OH, COOH and OT), 7-20C alkyl or phenyl (optionally substituted by COOH); NR9R10 = up to 7C saturated or unsaturated ring, optionally having 1 or 2 ring C replaced by O, S, SO, CO or NR11; R11 = H or T; R5 = T (optionally substituted by CF3, C2F5 or C- or N-bonded 5- or 6-membered saturated heterocyclyl containing 1-3 of O, S and/or N as heteroatom(s)), 3-7C cycloalkyl or NR12R13; R12, R13 = T; NR12R13 = up to 6C saturated or unsaturated ring, optionally having 1 or 2 ring C replaced by O, S, SO, CO or NR11; R6 = -CH2CH2-OCH2CH2-OT; C- or N-bonded 5- or 6-membered saturated heterocyclyl containing 1-3 of O, S and/or N as heteroatom(s) (optionally substituted by T); or T (optionally substituted by OH, OT or C- or N-bonded 5- or 6-membered saturated, unsaturated or aromatic heterocyclyl containing 1-3 of O, S and/or N as heteroatom(s)); R8 = NH2, NHT or NT2; R16 = H, T (optionally substituted by halo) or -CO-T (optionally substituted by 1-3 halo); R17 = T (optionally substituted by 1-3 of OH, halo or (1-4C) alkoxycarbonyl); A, D, E, G = H, halo, NO2, CN, OH, COOH, CF3, OCF3, T, OT, OCOT, COOT or SO2T; and T = 1-6C alkyl.
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