Arylsulfonamides with analgetic activity

摘要

Pyridin-piperazin-phenyl derivatives (I) or their enantiomers, diastereomers or salts, preferably salts with organic or inorganic acid or base, are new. Pyridin-piperazin-phenyl derivative (I) of formula (R 5>-A-R 4>-B 1>-R 3>-A-D-Y 1>-N(R 2>)-SO 2-R 1>) or their enantiomers, diastereomers or salts, preferably salts with organic or inorganic acid or base, are new. A : a bond or 1-4C alkylene; B 1>a bond, 1-3C alkylene, -O- or -C(O)-; D : amine group of formula (-N(R 2>)-C(O)-) or (-C(O)-N(R 2>)-); Y 1>1-4C-alkylene optionally substituted by R 2>, where a methylene group can be replaced in addition by Y 2>; Y 2>-O-, -S-, -S(O)-, -N(R 2>)-, -N(R 2>)-C(O)-, -C(O)-N(R 2>)-, -C(O)-, -CH(aryl)- or -S(O) 2-; R 1>3-7C-cycloalkyl- or aryl-, heteroaryl- or aryl-1-3C-alkyl- (all substituted with 1-4 R1a); R 2>H or 1-3C-alkyl, where each methylene group is substituted with up to two F and each methyl group is replaced with up to 3 F; R 3>arylene, heteroarylene, saturated 4-7-membered heterocyclic ring, unsaturated 5-7 membered heterocyclic ring (all substituted with 1 or 2 R3a) or 1-6C-alkylene; R 4>arylene, heteroarylene, saturated 4-7-membered heterocyclic ring, unsaturated 5-7 membered heterocyclic ring (all substituted with 1 or 2 R4a), -O-, -C(O)O-, -C(O)NR 2>-, -NR 2>-, -NR 2>-NR 2>-, -3-7C-cycloalkylene- or -1-6C-alkylene-; R 5>heteroaryl, 4-7 membered saturated heterocyclic ring (both substituted with 1 or 2 R5a), H, 1-8C alkyl, 3-7C-cycloalkyl (optionally substituted with 1-3C alkyl), H 2N-, 1-4C-alkyl-NH-, (1-4C-alkyl) 2N- or H 2N-C(O)-; and R1a, R3a, R4a, R5a : H, F, Cl, Br, I, 1-3C-alkyl-, HO-, 1-3C-alkyl-O- or 1-3C-alkyl-O-2-4C-alkylene-O-. An independent claim is included for pyridin-piperazin-phenyl salts with inorganic or organic acids or bases. - ACTIVITY : Analgesic; Antimigraine; Neuroprotective; Dermatological; Cerebroprotective; Vasotropic; Antiallergic; Immunosuppressive; Gastrointestinal-Gen; Respiratory-Gen; Antiasthmatic; Antiinflammatory; Antiarthritic; Osteopathic. - MECHANISM OF ACTION : None given.