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US 9,957,255 B2Granted
Benzotriazole derivatives as modulators of TNF activity
AssigneeUcb Biopharma Sprl
InventorsDaniel Christopher Brookings, Boris Kroeplien
Life of this patent
Estimating the term…
Abstract
A series of substituted benzotriazole derivatives, being potent modulators 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.
Claims8
A compound of formula (IIB) or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof,
- wherein
- V is C—R22 or N;
- R21 is hydroxy(C1-6)alkyl:
- or R21 is (C3-7)heterocyclo-alkyl, which group may be optionally substituted by one, two or three substituents independently selected from C1-6 alkylsulphonyl, oxo and carboxy;
- R22 is hydrogen, halogen or C1-6 alkyl;
- R23 is hydrogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy;
- E is —CH2;
- and
- R12 is hydrogen, fluoro, chloro, trifluoromethyl, methyl or ethoxycarbonylethyl;
- R15 is hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, difluoromethoxy or trifluoromethoxy;
- and
- R16 is hydrogen, halogen, cyano, C1-6 alkyl, trifluoro-methyl, difluoromethoxy or amino.
9 more elements
A compound that is,
- 4-[5-(1-{[2-(Difluoromethoxy)phenyl]methyl}benzotriazol-6-yl)pyrimidin-2-yl]-morpholine,
- 1-[5-(1-{[2-(Difluoromethoxy)phenyl]methyl}benzotriazol-6-yl)pyrimidin-2-yl]-piperidine-4-carboxylic acid,
- 4-[5-(1-{[2-(Difluoromethoxy)phenyl]methyl}benzotriazol-6-yl)pyrimidin-2-yl]-piperazin-2-one,
- 1-{[2-(Difluoromethoxy)phenyl]methyl}-6-[2-(piperazin-1-yl)pyrimidin-5-yl]-benzotriazole, or
- 1-{[2-(Difluoromethoxy)phenyl]methyl}-6-{2-[4-(methylsulfonyl)piperazin-1-yl]-pyrimidin-5-yl}benzotriazole.
2 more elements
Dependencies are inferred from the claim text.