Tetrahydrobenzimidazole derivatives as modulators of TNF activity
AssigneeUcb Biopharma Sprl
InventorsJag Paul Heer, Victoria Elizabeth Jackson, Boris Kroeplien, Fabien Claude Lecomte, John Robert Porter
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Abstract
A series of substituted 4,5,6,7-tetrahydrobenzimidazole derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
Claims5
A compound represented by formula (IIA) or an N-oxide thereof, or a pharmaceutically acceptable salt thereof, or a glucuronide derivative thereof:
- wherein
- E represents —CH2—;
- Q represents —CH2— or —CH(OH)—;
- Z represents hydrogen, methyl, phenyl, methylsulfonylphenyl, pyridinyl, methyl sulfonylpyridinyl, oxopyrrolidinylphenyl, (hydroxy)(oxo)pyrrolidinylphenyl or (oxo)oxazolidinylphenyl;
- R11 represents hydrogen or halogen;
- R12 represents hydrogen, fluoro, chloro, trifluoro-methyl, methyl or ethoxycarbonylethyl;
- R15 represents hydrogen, halogen, C1-6 alkyl, trifluoro-methyl, C1-6 alkoxy, difluoromethoxy or trifluoromethoxy;
- and
- R16 represents hydrogen, halogen, cyano, C1-6 alkyl, trifluoromethyl, difluoromethoxy or amino.
A compound that is {1-[(2,5-Dimethylphenyl)methyl]-4,5,6,7-tetrahydrobenzimidazol-2-yl}(pyridin-4-yl)methanol.
Dependencies are inferred from the claim text.