| 摘要 |
Sulfonylamino-benzene derivatives (A), as pure stereoisomers (particularly enantiomers or diastereomers), racemates or mixtures in any proportions, optionally as salts and/or solvates are new. Sulfonylamino-benzene derivatives of formula (A), as pure stereoisomers (particularly enantiomers or diastereomers), racemates or mixtures in any proportions, optionally as salts and/or solvates are new. X : O, S or -NCN; Y : amino, NHR 30>, NR 31>R 32>, or (un)saturated optionally substituted (OS) 1-10C aliphatic group; n : 0-4; R 1>-R 4>H, F, Cl, Br, I, SF 5, nitro, CF 3, CN, amino, OH, SH, CONH 2, SO 2NH 2, CONHOH, COOH, CHO, SO 2OH, NHR 11>, NR 12>R 13>, OR 14>, SR 15>, CONHR 16>, CONR 17>R 18>, SO 2NHR 19>, SO 2NR 20>R 21>, COOR 22>, COR 23>, SOR 24>, SO 2R 24> or (un) saturated OS 1-10C aliphatic group; R 5>R 1>, CF 2Cl, or (un)saturated OS 3-9 membered cycloaliphatic ring, attached via C atom, optionally including 1 or more heteroatoms in the ring; either Q : a group of formula (a)-(g); R 6>, R 7>, R 9>R 1>, CF 2Cl, or OS 6-10 membered aryl, optionally attached via OS 1-6C alkylene, 2-6C alkenylene or 2-6C alkynylene; R 8>R 1>, CF 2Cl, amidino, C(=NH)-NHR 27>, guanidino, or N=C(NHR 28>)(NHR 29>); or (un)saturated OS 3-9 membered cycloaliphatic ring, attached via C atom, optionally including 1 or more heteroatoms in the ring, optionally fused with (un)saturated OS mono- or poly-cyclic ring system and/or attached via OS 1-6C alkylene, 2-6C alkenylene or 2-6C alkynylene; or OS 5-14 membered (hetero)aryl group, optionally fused with (un)saturated OS mono- or poly-cyclic ring system and/or attached via OS 1-6C alkylene, 2-6C alkenylene or 2-6C alkynylene; R 10>SF 5, nitro, CF3, CF2Cl, CN, amino, OH, SH, CONH2, SO2NH2, CONHOH, COOH, CHO, SO 2OH, NHR 11>, NR 12>R 13>, OR 14>, SR 15>, CONHR 16>, CONR 17>R 18>, SO 2NHR 19>, SO 2NR 20>R 21>, COOR 22>, COR 23>, SOR 24>, SO 2R 24>, amidino, C(=NH)-NHR 27>, guanidino, or N=C(NHR 28>)(NHR 29>); or 1-10C (un)saturated aliphatic group (OS by 1-9 T); unsubstituted 2-10C alkenyl or 2-10C alkynyl; or (un)saturated OS 3-9 membered cycloaliphatic ring, attached via C atom, optionally including 1 or more heteroatoms in the ring, optionally fused with (un)saturated OS mono- or poly-cyclic ring system and/or attached via OS 1-6C alkylene; or OS 5-14 membered (hetero)aryl group, optionally fused with (un)saturated OS mono- or poly-cyclic ring system and/or attached via OS 1-6C alkylene; T : CN, nitro, OH, amino, SH, 1-5C alkoxy, 1-5C alkylthio, (di) 1-5C alkylamino, CF 3O or CF 3S; either R 11>-R 24>, R 27>-R 29>(un)saturated OS 1-10C aliphatic group; (un)saturated OS 3-9 membered cycloaliphatic ring, optionally including 1 or more heteroatoms in the ring, optionally fused with (un)saturated OS mono- or poly-cyclic ring system and/or attached via OS 1-6C alkylene or 2-6 membered heteroalkylene; or OS 5-14 membered (hetero)aryl group, optionally fused with (un)saturated OS mono- or poly-cyclic ring system and/or attached via OS 1-6C alkylene or 2-6 membered heteroalkylene; or NR 12>N 13>(un)saturated OS 4-9 membered heterocycloaliphatic group (optionally containing a further heteroatom), optionally fused to (un)saturated OS mono- or poly-cyclic ring system; either R 25>(un)saturated OS 1-10C aliphatic group; OS 5-14 membered (hetero)aryl, optionally fused with (un)saturated OS mono- or poly-cyclic ring system and/or attached via OS 1-6C alkylene, 2-6C alkenylene or 2-6C alkynylene group; or (un)saturated OS 3-9 membered cycloaliphatic ring, optionally including at least one heteroatom in the ring; and R 26>H or R 25>; or CR 25>R 26>(un)saturated OS 3-6 membered cycloaliphatic group; R 30>-R 32>(un)saturated OS 1-10C aliphatic group. All optionally substituted groups may be mono- or polysubstituted. An independent claim is included for the preparation of (A). [Image] ACTIVITY : Analgesic; Antimigraine; Antidepressant; Nootropic; Neuroprotective; Antiparkinsonian; Anticonvulsant; Antiasthmatic; Antitussive; Uropathic; Antiulcer; Antiinflammatory; Cerebroprotective; Ophthalmological; Dermatological; Antiallergic; Antipsoriatic; Antidiarrhea; Antipruritic; Osteopathic; Antiarthritic; Antirheumatic; Antialcoholic; Cardiant; Vulnerary; Tranquilizer. MECHANISM OF ACTION : (A) are ligands of the vanilloid receptors of subtype 1 (VR1/TRPV1 receptors). The compound 2-(3-fluoro-4-(methylsulfonylamino)phenyl)-N-((2-(piperidin-1-yl)-6-trifluoromethyl-pyridin-3-yl)methylpropionamide had IC50 for displacement of capsaicin from the human receptor (expressed in CHO K1 cells) of 218 nM. |
