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US 8,299,074 B2Granted
P38 MAP kinase inhibitors
AssigneeRespivert Limited
InventorsKazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Kevin Joly, Catherine Elisabeth Charron
Life of this patent
Estimating the term…
Abstract
The present disclosure relates to compounds of formula (I): which are inhibitors of p38 mitogen-activated protein kinase enzymes, particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD.
Claims17
A compound of formula (I)
- wherein R1 is C1-6 alkyl optionally substituted by a hydroxyl group;
- R2 is H or C1-6 alkyl optionally substituted by a hydroxyl group;
- R3 is H, C1-6 alkyl or C0-3 alkylC3-6 cycloalkyl;
- Ar is a naphthyl or a phenyl ring either of which may be optionally substituted by one or more (for example 1 or 2) groups independently selected from C1-6 alkyl, C1-6 alkoxy, amino, C1-4 mono or di-alkyl amino;
- X is 5 or 6 membered heteroaryl group containing at least one nitrogen atom and optionally including 1 or 2 further heteroatoms selected from O, S and N;
- Q is selected from:
- a) a saturated or unsaturated, branched or unbranched C1-10 alkyl chain, wherein at least one carbon (for example 1, 2 or 3 carbons, suitably 1 or 2, in particular 1 carbon) is replaced by a heteroatom selected from O, N, S(O)p, wherein said chain is optionally, substituted by one or more groups (for example 1, 2 or 3 groups) independently selected from oxo, halogen, an aryl group, a heteroaryl group, a heterocyclyl group or a C3-8 cycloalkyl group,
- each aryl, heteroaryl, heterocyclyl or C3-8 cycloalkyl group bearing 0 to 3 substituents selected from halogen, hydroxyl, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, amino, C1-4 mono or di-alkyl amino, C1-4 mono or di-acyl amino, S(O)qC1-6 alkyl, C0-6 alkylC(O)C1-6 alkyl or C0-6 alkylC(O)C1-6 heteroalkyl,
- with the proviso that the atom linked directly to the carbonyl in —NR3C(O)— is not an oxygen or a sulfur atom;
- and
- b) a C0-8 alkyl-heterocycle said heterocyclyl group comprising at least one heteroatom (for example 1, 2 or 3, suitably 1 or 2, in particular 1 heteroatom) selected from O, N, and S, and is optionally substituted by one, two or three groups independently selected from halogen, hydroxyl, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, amino, C1-4 mono and di-alkyl amino, C1-4 mono or di-acyl amino, S(O)qC1-6 alkyl, C0-6 alkylC(O)C1-6 alkyl or C0-6 alkylC(O)C1-6 heteroalkyl;
- and
- p is 0, 1 or 2;
- q is 0, 1 or 2
- a pharmaceutically acceptable salt or solvate thereof, including all stereoisomers, tautomers, and deuterated compounds thereof.
12 more elements
Dependencies are inferred from the claim text.