发明名称 Fused bicyclic pyridine and pyrazine derivatives as kinase inhibitors
摘要 A series of fused bicyclic pyridine and pyrazine derivatives, substituted directly on the pyridine or pyrazine ring by a functional group attached via a sulphur-containing linkage, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
申请公布号 US8957090(B2) 申请公布日期 2015.02.17
申请号 US201013508964 申请日期 2010.11.11
申请人 UCB Pharma S.A. 发明人 Raphy Gilles;Bürli Roland;Haughan Alan Findlay
分类号 A61K31/47;C07D215/00;C07D401/12;C07D473/02;C07D487/04 主分类号 A61K31/47
代理机构 McDonnell Boehnen Hulbert & Berghoff LLP 代理人 McDonnell Boehnen Hulbert & Berghoff LLP
主权项 1. A compound of formula (I) or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof: wherein M represents the residue of an optionally substituted phenyl ring;W represents C—R1;E represents an optionally substituted straight or branched C1-4 alkylene chain;Q represents N—R2;Z represents an optionally substituted mono- or bicyclic heteroaryl group containing at least one nitrogen atom selected from pyrrolyl, pyridinyl, indolyl, quinolinyl, isoquinolinyl, imidazolyl, pyrazolyl, triazolyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, indazolyl, benzimidazolyl, furopyridinyl, thienopyridinyl, benzoxazolyl, benzothiazolyl, cinnolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, imidazopyridinyl, pyrazolopyridinyl, purinyl, pyrazolopyrimidinyl, pyrrolopyrimidinyl, triazolopyrimidinyl, pyridopyrimidinyl, pyridopyrazinyl, pyridopyridazinyl, naphthyridinyl, pteridinyl, pyrrolotriazinyl and pyrazolotriazinyl;Y represents —S—;R1 represents hydrogen, halogen, C1-6 alkyl or C1-6 alkoxy;R2 represents hydrogen or C1-6 alkyl; andRa represents trifluoromethyl; or C1-6 alkyl, C2-6 alkenyl, C3-7 cycloalkyl, C3-7 cycloalkyl(C1-6)alkyl, aryl, aryl(C1-6)alkyl, C3-7 heterocycloalkyl, C3-7 heterocycloalkyl-(C1-6)alkyl, heteroaryl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted by one or more substituents.
地址 Brussels BE