Novel compounds
AssigneeRespivert Limited
InventorsJohn King-Underwood, George Hardy, Peter John Murray, Jonathan Gareth Williams, Stuart Thomas Onions
Life of this patent
Estimating the term…
Abstract
There are provided inter alia compounds of formula (I) wherein R1, R2a, R2b, R3, R4, L, X, R5 and R6 are as defined in the description for use in the treatment of inflammatory diseases.
Claims34
1-40. (canceled)
A method of treatment of a condition selected from COPD, asthma, paediatric asthma, cystic fibrosis, sarcoidosis, idiopathic pulmonary fibrosis, allergic rhinitis, rhinitis, sinusitis, allergic conjunctivitis, conjunctivitis, allergic dermatitis, contact dermatitis, psoriasis, ulcerative colitis, inflamed joints secondary to rheumatoid arthritis or osteoarthritis, rheumatoid arthritis, pancreatitis, cachexia and growth and metastasis of tumours which comprises administering to a subject an effective amount of a compound of formula (I):
- wherein,
- R1 is H,
- phenyl, or
- a saturated or unsaturated branched or unbranched C1-10 alkylene acyclic or alicyclic chain wherein one or more carbons in the chain are optionally replaced by a heteroatom(s) independently selected from O, N and S(O)n and the chain is optionally substituted by:
- one oxo group and/or
- one or more halogen atoms;
- R2a is H, halo, saturated or unsaturated branched or unbranched C1-8 alkylene chain, wherein one or more carbons are optionally replaced by a heteroatom(s) independently selected from —O—, —N— and/or S(O)m and the chain is optionally substituted by one or more halogen atoms;
- R2b is H, halo, C1-6 alkoxy or C1-6 alkyl optionally substituted by OH;
- R3 is halo, haloalkyl, S(O)pC1-6 alkyl or cyano;
- R4 is H, halo, haloalkyl, or cyano;
- or
- R3 and R4 taken together with the carbons atoms to which they are attached form:
- a 5 to 6 membered saturated or partially unsaturated carbocyclic ring, or
- a 5 to 6 membered saturated or partially unsaturated or unsaturated heterocyclic ring containing 1 or more heteroatoms independently selected from N, O and/or S;
- L is saturated or unsaturated branched or unbranched C1-6 alkylene chain, wherein one or more carbons are optionally replaced by a heteroatom selected from —O— and/or S, and the chain is optionally substituted by one or two oxo groups;
- X is pyridine or pyrimidine optionally substituted by C1-3 alkyl, or C1-3 haloalkyl;
- R5H or C1-4 alkyl;
- R6 is selected from:
- a) a saturated or unsaturated, branched or unbranched C1-10 alkyl chain, wherein optionally at least one carbon is replaced by a heteroatom independently selected from O, N, S(O)p, wherein said chain is optionally, substituted by one or more groups independently selected from oxo, halogen, a C6-10 aryl group, a 5 or 6 membered heteroaryl group, a 5 or 6 membered heterocyclyl group or a C3-8 cycloalkyl group,
- each aryl, heteroaryl, heterocyclyl or 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 C2-8 di-alkyl amino, C1-4 mono or C2-8 di-acyl amino, S(O)qC1-6 alkyl, C0-6 alkylC(O)C1-6 alkyl or C0-6 alkylC(O)NC0-6 alkyl C0-6 alkyl, C0-6 alkylC(O)C1-6 heteroalkyl,
- with the proviso that the atom linked directly to the carbonyl in —NR5C(O)— is not an oxygen or a sulfur atom;
- and
- b) a C0-8 alkyl-heterocycle wherein the heterocyclyl group has 5 or 6 members and comprises at least one heteroatom selected from O, N, and S, and said heterocycle 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 C2-8 di-alkyl amino, C1-4 mono or C2-8 di-acyl amino, S(O)qC1-6 alkyl, C0-6 alkylC(O)C1-6 alkyl, C0-6 alkylC(O)NC0-6 alkyl C0-6 alkyl or C0-6 alkylC(O)C0-6 heteroalkyl;
- n is 0, 1 or 2;
- m is 0, 1 or 2;
- p is 0, 1 or 2;
- q is 0, 1 or 2;
- or
- a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof.
Dependencies are inferred from the claim text.