| 摘要 |
The invention provides compounds of formula (I) wherein R1, R3, L1, L2, G1, G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.; |
| 主权项 |
1. A compound of formula (I) or a pharmaceutically acceptable salt thereof wherein: A is phenyl; each R1 is independently halogen, CN, OH, CONR5R6, NR5R6, C1-4alkyl, C2-4alkynyl, or C1-4alkoxy; said C1-4alkyl or C2-4alkynyl being optionally substituted by OH or C1-4alkyl; m is an integer that is 0, 1, or 2; each R3 is hydrogen; L1 is a direct bond, C1-3alkylene or C2-3alkenylene; L2 is a direct bond, —O—, —OCH2—, —C≡C— or —NHCONH—; G1 is phenyl; G2 is phenyl, 5- or 6-membered heteroaryl, C3-10carbocyclyl or C5-8heterocyclyl; any phenyl, heteroaryl, carbocyclyl or heterocyclyl moieties in G1 and G2 being optionally substituted by one or more substituents that are independently selected from the group consisting of halogen, OH, CN, NO2, CO2R9, C1-6alkyl, C1-6alkoxy, C1-4thioalkoxy, SO2NR10R11, NR12R13, —NHCOC(OH)(CH3)CF3, and —CH2OCH2CF2CHF2; said C1-6alkyl or C1-6alkoxy being optionally substituted by OH or by one or more F atoms; R9 is C1-6alkyl; and each R4, R5, R6, R7, R8, R10, R11, R12 and R13 is independently selected from the group consisting of H or C1-4alkyl; with the proviso that the following compounds are excluded: 2-amino-N-(2-sulfamoylphenyl)benzenesulfonamide; 3-amino-4-hydroxy-N-(2-sulfamoylphenyl)benzenesulfonamide; 4-bromo-N-(2-sulfamoylphenyl)benzenesulfonamide; 4-fluoro-N-(2-sulfamoylphenyl)benzenesulfonamide; 4-nitro-N-(2-sulfamoylphenyl)benzenesulfonamide; 2-[(phenylsulfonyl)amino]-4-(trifluoromethyl)benzenesulfonamide; 2,5-dibromo-N-(2-(N-ethylsulfamoyl)phenyl)benzenesulfonamide; and 2,3,4,5,6-pentafluoro-N-(2-sulfamoylphenyl)benzenesulfonamide. |
