Pharmaceutically Active Benzensulphonyl-Indols

A compound of formula

• wherein
• R1 is branched (C4-12)alkyl, (C1-12)alkoxy, (C3-12)cycloalkyl, optionally fused with heterocyclyl, (C5-12)cycloalkenyl, optionally fused with heterocyclyl, (C6-18)aryl, optionally fused with heterocyclyl, heterocyclyl, chloro or fluoro, halo(C1-4)alkyl, (C1-4)alkoxy, halo(C1-4)alkoxy, (C1-4)alkylthio,
• wherein heterocyclyl is aliphatic or aromatic heterocyclyl comprising 3 to 12 ring members and 1 to 4 heteroatoms selected from N, O, S, optionally anellated with another ring system,
• wherein cycloalkyl, cycloalkenyl, aryl or heterocyclyl are unsubstituted or substituted by one or more halogen, halo(C1-4)alkyl, halo(C1-4)alkoxy, (C1-4)alkyl, (C1-4)alkoxy or
• (C1-4)alkylthio,
• R2 and R3 are different from each other and independently are hydrogen, hydroxycarbonyl, alkoxycarbonyl, e.g. (C1-4)alkoxycarbonyl, cyano,
• aminocarbonyl, wherein amino is NH2, one- or twofold substituted amino or a cyclic amine, with the proviso that if R2 is 4-methyl-piperazin-1-yl-carbonyl, then R2 is in position 3 of the ring system,
• chloro, halo(C1-4)alkyl, such as CF3, (C1-4)alkyl, (C1-4)alkoxy, (C1-4)alkylthio
• with the PROVISO that
• a compound of formula
• and a compound of formula
• are EXCLUDED.

A compound from the group selected from consisting of

• 1-(4-tert.Butyl-benzenesulfonyl)-5-chloro-1H-indole-2-carboxylic acid,
• 1-(4-tert.Butyl-benzenesulfonyl)-1H-indole-6-carboxylic acid,
• 1-(4-tert.Butyl-benzenesulfonyl)-1H-indole-7-carboxylic acid methyl ester,
• 1-(4-tert.Butyl-benzenesulfonyl)-1H-indole-3-carboxylic acid,
• 5-Chloro-1-(4-morpholin-4-yl)-benzenesulfonyl)-1H-indole-3-carboxylic acid,
• 1-(4-tert.Butyl-benzenesulfonyl)-5-chloro-1H-indole-3-carboxylic acid,
• 5-Chloro-1-(4-oxazol-5-yl)-benzenesulfonyl)-1H-indole-3-carboxylic acid,
• 5-Chloro-1-(4-trifluoromethyl-benzenesulfonyl)-1H-indole-3-carboxylic acid,
• 5-Chloro-1-(4-chloro-benzenesulfonyl)-1H-indole-3-carboxylic acid,
• 5-Chloro-1-(4-morpholin-4-yl-benzenesulfonyl)-1H-indole-2-carboxylic acid,
• 1-(4-tert.Butyl-benzenesulfonyl)-1H-indole-2-carboxylic acid,
• 1-(4-Morpholin-4-yl-benzenesulfonyl)-1H-indole-6-carboxylic acid methyl ester,
• 1-(4-Morpholin-4-yl-benzenesulfonyl)-1H-indole-6-carboxylic acid,
• 1-(4-tert.Butyl-benzenesulfonyl)-5-chloro-1H-indole-2-carboxylic acid amide,
• [1-(4-tert.Butyl-benzenesulfonyl)-5-chloro-1H-indol-3-yl]-morpholin-4-yl-methanone,
• 2-{[1-(4-tert.Butyl-benzenesulfonyl)-5-chloro-1H-indole-3-carbonyl]amino}-2-methyl-propionic acid,
• [1-(4-tert.Butyl-benzenesulfonyl)-5-chloro-1H-indol-3-yl]-(4-methyl-piperazin-1-yl)-methanone,
• 1-(4-tert.Butyl-benzenesulfonyl)-5-chloro-1H-indole-3-carboxylic acid methylamide,
• 1-(4-tert.Butyl-benzenesulfonyl)-5-chloro-1H-indole-3-carboxylic acid dimethylamide,
• [1-(4-tert.Butyl-benzenesulfonyl)-5-chloro-1H-indole-3-yl]-piperidin-1-yl-methanone,
• 1-(4-tert.Butyl-benzenesulfonyl)-5-chloro-1H-indole-3-carboxylic acid amide,
• 1-(4-tert.Butyl-benzenesulfonyl)-5-chloro-1H-indole-3-carboxylic acid isopropylamide,
• 1-(4-tert.Butyl-benzenesulfonyl)-1H-indole-6-carbonitrile,
• 1-(4-tert.Butyl-benzenesulfonyl)-5-chloro-1H-indole-2-carbonitrile,
• 1-(4-tert.Butyl-benzenesulfonyl)-1H-indole-3-carbonitrile,
• 1-(4-tert.Butyl-benzenesulfonyl)-1H-indole-6-carboxylic acid amide and
• 4-tert.Butyl-N-[1-(4-tert-butyl-benzenesulfonyl)-1H-indole-6-carbonyl]-benzenesulfon-amide,