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US 9,850,240 B2Granted
Triazolopyridine derivatives as modulators of TNF activity
AssigneeUcb Biopharma Sprl
InventorsDaniel Christopher Brookings, Victoria Elizabeth Jackson
Life of this patent
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Abstract
A series of substituted [1,2,4]triazolo[4,3-a]pyridine derivatives, being potent modulators of human TNF 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.
Claims7
A compound as represented by formula (IIB) or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof,
- wherein
- V represents C—R22 or N;
- R21 represents hydroxy(C1-6)alkyl;
- or R21 represents (C3-7)cycloalkyl or (C3-7)heterocycloalkyl, either of which groups is optionally substituted by one, two, or three substituents independently selected from halogen, halo(C1-6)alkyl, cyano, cyano-(C1-6)alkyl, nitro, nitro(C1-6)alkyl, C1-6 alkyl, trifluoro-methyl, trifluoroethyl, C2-6 alkenyl, hydroxy, hydroxy-(C1-6)alkyl, C1-6 alkoxy, difluoromethoxy, trifluoro-methoxy, trifluoroethoxy, C1-6 alkylthio, C1-6 alkylsulphinyl, C1-6 alkylsulphonyl, C1-6 alkylsulphonyl, (C1-6)alkylsulphonyl(C1-6)alkyl, oxo, amino, C1-6 alkyl-amino, di(C1-6)alkylamino, C2-6 alkylcarbonylamino, (C2-6)alkylcarbonylamino(C1-6)alkyl, C2-6 alkoxycarbonyl-amino, C1-6 alkylsulphonylamino, (C1-6)alkylsulphonyl-amino(C1-6)alkyl, formyl, C2-6 alkylcarbonyl, carboxy, carboxy(C1-6)alkyl, C2-6 alkoxycarbonyl, morpholinyl-(C1-6)alkoxycarbonyl, C2-6 alkoxycarbonyl(C1-6)alkyl, C2-6 alkoxycarbonylmethylidenyl, tetrazolyl(C1-6)alkyl, amino-carbonyl, C1-6 alkylaminocarbonyl, di(C1-6)alkylamino-carbonyl, aminosulphonyl, C1-6 alkylaminosulphonyl, di(C1-6)alkylaminosulphonyl, (C1-6)alkylsulphoximinyl, [(C1-6)alkyl][N—(C1-6)alkyl]sulphoximinyl, (C1-6)alkylsulphonylaminocarbonyl, (C2-6)alkylcarbonylamino-sulphonyl, (C1-6)alkoxyaminocarbonyl, tetrazolyl and hydroxyoxadiazolyl;
- R22 represents hydrogen, halogen or C1-6 alkyl;
- R23 represents hydrogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy;
- E represents —CH2;
- R12 represents hydrogen or halogen;
- R15 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, difluoromethoxy, or trifluoromethoxy;
- and
- R16 represents hydrogen, halogen, cyano, C1-6 alkyl, trifluoromethyl, difluoromethoxy, or amino.
8 more elements
A compound that is
- 4-[5-(3-{[2-(Difluoromethoxy)phenyl]methyl}[1,2,4]triazolo[4,3-a]pyridin-6-yl)-pyrimidin-2-yl]morpholine,
- 1-[5-(3-{[2-(Difluoromethoxy)phenyl]methyl}[1,2,4]triazolo[4,3-a]pyridin-6-yl)-pyrimidin-2-yl]piperidine-4-carboxylic acid,
- 4-[5-(3-{[2-(Difluoromethoxy)phenyl]methyl}[1,2,4]triazolo[4,3-a]pyridin-6-yl)-pyrimidin-2-yl]piperazin-2-one, or
- 3-{[2-(Difluoromethoxy)phenyl]methyl}-6-{2-[4-(methylsulfonyl)piperazin-1-yl)]-pyrimidin-5-yl}[1,2,4]triazolo[4,3-a]pyridine.
1 more element
Dependencies are inferred from the claim text.