http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-069919-A1
Outgoing Links
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|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0a910d33c239980f3a705e312c5bad6a |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C2601-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C2601-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C2602-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C2602-08 |
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| filingDate | 2008-12-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2010-03-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-069919-A1 |
| titleOfInvention | BIS- (SULFONYLAMINE) DERIVATIVES USEFUL FOR PAIN TREATMENT |
| abstract | Processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are microsomal prostaglandin E synthase-1 inhibitors. Claim 1: A compound of formula (1) or a pharmaceutically acceptable salt thereof wherein: A is selected from 5 or 6 membered phenyl or a heteroaryl or a 5 or 6 membered heterocyclynyl moiety; said 5 or 6-membered phenyl or heteroaryl or half or 5-membered heterocyclynyl group in group A being optionally fused to a phenyl, a 5- or 6-membered heteroaryl ring, C5-6carbocyclyl or C5-6heterocyclyl; Each R1 is independently selected from halogen, nitro, SF5, CN, NR5R6, OH, CHO, C02C1-4alkyl, CONR5R6, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C2-4alkoxy, G3, OG3 or OCHG3; said C1-4alkyl, C2-4alkenyl, C2-4alkynyl or C1-4alkoxy being optionally substituted by one or more substituents selected from OH, NR5R6, C1-4alkyl or F; m represents an integer 0, 1, 2, 3 or 4; each R3 is independently selected from hydrogen, CN and C1-4alkyl; said C1-4alkyl being optionally substituted with OH, CN, C1-4alkoxy, NR7R8, or one or more F atoms; L1 represents a direct bond, C1-4alkylene, C2-4alkenylene or C2-4aIquinylene; L2 represents a direct bond, -O-, -OCH2-, C1-2aIylene, -C ::: C- or -NHCONH-; G1 represents phenyl, 5- or 6-membered heteroaryl, C3-10carbocyclyl or C5-8heterocyclyl; G2 represents H, C1-6 alkyl, feniI, 5- or 6-membered heteroaryl, C3-10 carboxycyl or C5-8 heterocyclyl; said C1-6alkyl being optionally further substituted by one or more groups selected from OH, C1-6alkoxy and halogen; the phenyl, heteroaryl, carbocyclyl or heterocyclyl halves in G1 and G2 being optionally fused to one or more additional rings independently selected from phenyl, a 5- or 6-membered heteroaryl ring, C5-6carbocyclyl or C5-6heterocyclyl; any of the phenyl, heteroaryl, carbocyclyl or heterocyclyl halves in G1 and G2 being optionally substituted by one or more substituents independently selected from halogen, OH, CN, NO2, CO2R9, C1-6alkyl, C1-6alkoxy, C1-4thioalkoxy, SO2NR10R11, NR12R13, -NHCOC (OH) (CH3) CF3 or -CH2OCH2CF2CHF2; said C1-6alkyl or C1-6alkoxy being optionally substituted by OH or by one or more F atoms; R9 represents C1-6alkyl; G3 represents 5 or 6 membered phenyl or heteroaryl; and R4, R5, R6, R7, R8, R10, R11, R12 and R13 is independently selected from H or C1-4alkyl; with the proviso that the following compounds are excluded: 3 - [(phenylsulfonyl) amino] pyridine-2-sulfonamide; 2-amino-N- (2-sulfamoylphenyl) benzenesulfonamide; 4-tert-butyl-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-methyl-N- (2-sulfamoylphenyl) benzenesulfonamide; 4-nitro-N- (2-sulfamoylphenyl) benzenesulfonamide; 2-nitro-N- (2-sulfamoylphenyl) benzenesulfonamide; 4-amino-N- (2-sulfamoylphenyl) benzenesulfonamide; 2 - [(phenylsulfonyl) amino] -4- (trifluoromethyl) benzenesulfonamide; 2 - {[(4-methylphenyl) sulfonyl] amino} -4- (trifluoromethyl) benzenesulfonamide; N- (2- sulfamoylphenyl) quinoline-8-sulfonamide; 4-tert-butyl-N- (2- (N-ethylsulfamoyl) phenyl) -2,6-dimethylbenzenesulfonamide; 2,5-dibromo-N- (2- (N-ethylsulfamoyl) phenyl) benzenesulfonamide; methyl 4- (5-fluoro-3-methylbenzo [b] thiophene-2-sulfonamido) -3-sulfamoylbenzoate; 2,3,4,5,6-pentafluoro-N- (2-sulfamoylphenyl) benzenesulfonamide; N- (2- (N, N-dimethylsulfamoyl) phenyl) -5,7-dimethyl- [1,2,4] triazolo [1,5-a] pyrimidine-2-sulfonamide; N- (2- (N-tert-butylsulfamoyl) phenyl) -5,7-dimethyl- [1,2,4jtriazolo [1,5-a] pyrimidine-2-sulfonamide; N- (2- (N-Methoxy-N-methylsulfamoyl) phenyl) -5,7-dimethyl- [1,2,4] triazolo [1,5-a] pyrimidine-2-sulfonamide; 5,7-dimethyl-N- (2-sulfamoylphenyl) - [1,2,4] triazolo [1,5-c] pyrimidine-2-sulfonamide; 6-methy-N- (2-sulfamoylphenyl) thiazolo [3,2-b] [1,2,4] triazol-2-sulfonamide; 6-Chloro-N- (2- (N, N-dimethylsulfamoyl) phenyl) - (1,2,4] triazolo [1,5-a] pyrimidine-2-sulfonamide; 6-chloro-N- (2- ( N-ethyl-N-methylsulfamoyl) phenyl) - [1,2,4] triazolo [1,5-a] pyrimidine-2-sulfonamide; N- (2- (N, N-dimethylsulfamoyl) phenyl) -5-methyl -7,8-dihydro-6H-cyclopenta [e] [1,2,4] triazolo [1,5-a] pyrimidine-2-sulfonamide; N- (2- (N, N-dimethylsulfamoyl) -5- ( trifluoromethyl) phenyl) -5,7-dimethyl- [1,2,4] triazolo (1,5-a] pyrimidine-2-sulfonamide; N- (2- (N-ethyl-N-methylsulfamoyl) phenyl) -5 , 7-dimethyl- [1,2,4] triazolo [1,5-a] pyrimidine-2-sulfonamide; and N- (2- (N, N-dimethylsulfamoyl) phenyl) -5,7-dimethyl- [1 , 2,4] triazoIo [1,5-a] pyrimidine-2-sulfonamide. |
| priorityDate | 2007-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 85.