发明名称 P38 MAP kinase inhibitors
摘要 There are provided inter alia compounds of formula (I); wherein R1, Ar, L, X, R3 and Q are as defined in the specification for use in therapy, especially in the treatment of inflammatory diseases.
申请公布号 US8975285(B2) 申请公布日期 2015.03.10
申请号 US201314139982 申请日期 2013.12.24
申请人 Respivert Ltd. 发明人 Ito Kazuhiro;Strong Peter;Rapeport William Garth;Murray Peter John;King-Underwood John;Williams Jonathan Gareth;Onions Stuart Thomas;Hirst Simon Christopher;Taddei David Michel Adrien;Charron Catherine Elisabeth
分类号 A61K31/4439;C07D401/02;C07D403/12;C07D401/12;C07D401/14 主分类号 A61K31/4439
代理机构 代理人 Carey Brian C.
主权项 1. A method for the therapeutic treatment of COPD comprising administering to a subject in need thereof an effective amount of a compound of the formula 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 groups independently selected from C1-6 alkyl, C1-6 alkoxy, amino, C1-4 mono or di-alkyl amino; L is a saturated or unsaturated branched or unbranched C1-8 alkylene chain, wherein one or more carbons are optionally replaced by —O— and the chain is optionally substituted by one or more halogen atoms, 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) is replaced by a heteroatom selected from O, N, S(O)p, wherein said chain is optionally, substituted by one or more groups selected from oxo, halogen, an aryl group, a heteroaryl group or an heterocyclyl group, each aryl, heteroaryl or heterocyclyl group bearing 0 to 3 substituents selected from halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, amino, C1-4 mono or di-alkyl amino, 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 alkylC5-6 heterocyclyl said heterocyclyl group comprising at least one heteroatom selected from O, N and S, and optionally substituted by one or two or three groups independently selected from halogen C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, amino, C1-4 mono and di-alkyl amino; and p is 0, 1 or 2; or a pharmaceutically acceptable salt or solvate thereof, including all stereoisomers and tautomers thereof.
地址 High Wycombe, Buckinghamshire GB