COMPOSTO DE ARILSULFONAMIDAS E ANÁLOGOS, BEM COMO COMPOSIÇÃO FARMACÊUTICA E USO DOS MESMOS

Aryl sulphonamides (I) and their salts are new: R1-A-D-E-G-L-R2 (I) R1 = 6-10C aryl; quinolyl; isoquinolyl; or a group of formula (a); Q = group of formula (i)-(vii): a = 1 or 2; R3 = H; 2-6C alkenyl; 1-6C alkyl; 1-6C acyl; -(CO)b-NR4R5 or -NR6-SO2-R7; b = 0 or 1; R4, R5 = H; phenyl; 1-6C acyl; 4-7C...

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Hauptverfasser: KLAUS-HELMUT MOHRS, MICHAEL MATZKE, ARNO FRIEDL, JOACHIM MITTENDORF, JEAN-MARIE-VIKTOR DE VRY, FRANK MAULER, MICHAEL-HAROLD ROCK, JOACHIM SCHUMACHER, ERVIN HORVATH, REINHARD JORK, JUERGEN DRESSEL, JUERGEN FRANZ, PETER SPREYER, SIEGFRIED RADDATZ, VERENA VOEHRINGER, JOERG KELDENICH
Format: Patent
Sprache:por
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Zusammenfassung:Aryl sulphonamides (I) and their salts are new: R1-A-D-E-G-L-R2 (I) R1 = 6-10C aryl; quinolyl; isoquinolyl; or a group of formula (a); Q = group of formula (i)-(vii): a = 1 or 2; R3 = H; 2-6C alkenyl; 1-6C alkyl; 1-6C acyl; -(CO)b-NR4R5 or -NR6-SO2-R7; b = 0 or 1; R4, R5 = H; phenyl; 1-6C acyl; 4-7C cycloacyl; benzoyl; or 1-6C alkyl optionally substituted by NH2, NH(1-6C alkyl) or N(1-6C alkyl)2; or NR4R5 = 5- or 6-membered saturated heterocycle optionally containing S and/or O and/or NR8; R6 = H; phenyl; 1-6C alkyl; or 1-6C acyl; R7 = phenyl or 1-6C alkyl; R8 = H; 1-6C alkyl; or 1-6C acyl; rings in R1 and alkenyl, alkenyl and acyl groups in R3 are optionally geminally substituted by 1 or more halo, COOH, OH, phenyl, 1-6C alkoxy, 1-6C alkoxycarbonyl or 1-8C alkyl (itself optionally substituted by halo, 1-6C alkylsulphonyloxy, N3, NH2, NH(1-6C alkyl), N(1-6C alkyl)2 or OH); A, E = bond or 1-4C alkylene; D = O ; S(O)c; or N(R9); c = 0-2; R9 = H; 1-6C alkyl; or 1-6C acyl; G = divalent 6-10C aryl or 5-7-membered heteroaryl (containing 1-3 S, N and/O) optionally substituted by 1 or more OH, CF3, COOH, halo, 1-6C alkyl, 1-6C hydroxyalkyl, 1-6C alkoxy, 1-6C alkoxycarbonyl, -CO-O-(CH2)d-NR4R5, -NR6-SO2R7, -(CH2)e-(CO)f-NR14R15 and/or OR16; R14, R15 = R4 and R5 or -(CH2)g-NR4R5; d, g = 1-4; e, f = 0 or 1; R16 = 6-10C aryl; L = O; NH; N(R19)-SO2; N(R20)-SO; N(R21)-SO2O; N(R22)-SO2-N(R23); N(R24)-CO; SO2-N(R25); OSO2; N(R26)-P(O)(OR27); or N(OH)-SO2 (bonding to G is via the left hand atom); R19-R27 = H or 1-4C alkyl or R19 = SO2R2; R2 = 6-10C aryl or 5-7-membered saturated or aromatic heterocycle (containing 1-3 S, N and/or O) optionally substituted by 1 or more halo, CF3, NO2, NH2 and/or 1-6C alkyl; a group of formula (b): morpholinyl; 3-8C cycloalkyl; 1-12C alkyl, 2-12C alkenyl or 2-12C alkynyl optionally substituted by 1 or more halo, CF3, OH, CN, N3, 1-6C alkoxy (optionally substituted by 1 or more F); phthalimido and/or NR4R5; or phenyl or 5- or 6-membered heteroaryl (containing 1-3 S, N and/O) and both optionally substituted by 1 or more halo, NO2, OH, 1-6C alkyl, 1-6C alkoxy and/or NR30R31; or L and R2 together form a group of formula (c): R30, R31 = H; 1-6C alkyl; or 1-6C acyl. Also claimed are (1) starting materials of formula (II) (see 'Preparation'); (2) compounds of formulae (XV): R48-SO2-(CH2)h-U-(CH2)i-CR49R50-CF2-R51 (XV) R48 = leaving group; U = O or single bond; R49, R50 = H; F; Cl; or CF3; R51 = H; F; Cl; or Br; h = 1 or 2; i = 0 or 1; compounds are