Fused tricyclic imidazo pyrazines as modulators of TNF activity
AssigneeUcb Biopharma Sprl
InventorsVictoria Elizabeth Jackson, Jag Paul Heer, Uwe Heinelt
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Abstract
A series of substituted fused tricyclic imidazo pyrazine derivatives and analoges thereof, represented by formula (I), being potent modulators of human TNFa 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.
Claims11
A compound of formula (I) or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof, or a glucuronide derivative thereof, or a co-crystal thereof:
- wherein
- n represents an integer equal to 0 or 1;
- Y represents aryl or heteroaryl, any of which groups may be optionally substituted by one or more substituents selected from halogen, cyano, amino, C1-6 alkyl, C1-6 alkylsulphonyl, C1-6 alkoxy, trifluoromethoxy and difluoromethoxy;
- X represents oxygen, sulphur, S(O), or N(Rd), or a straight or branched C1-4 alkylene chain;
- R1 represents halogen, heteroaryl or (C3-7)heterocycloalkyl-heteroaryl any of which groups may be optionally substituted by one or more substituents selected from hydroxy, hydroxy(C1-6 alkyl) and C1-6alkoxy;
- R2 and R3 independently represent hydrogen, halogen or C1-6 alkyl;
- R4 represents hydrogen, hydroxy, halogen or trifluoromethyl;
- R5a represents hydrogen, hydroxy or —ORa;
- R5b represents hydrogen;
- and
- Ra represents C1-6 alkyl, aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted by one or more substituents selected from C1-6 alkoxy, oxo and aminocarbonyl;
- and
- Rd represents hydrogen or C1-6 alkyl.
Dependencies are inferred from the claim text.