- 专利标题: Benzolactam compounds as protein kinase inhibitors
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申请号: US16541863申请日: 2019-08-15
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公开(公告)号: US11001575B1公开(公告)日: 2021-05-11
- 发明人: Valerio Berdini , Ildiko Maria Buck , James Edward Harvey Day , Charlotte Mary Griffiths-Jones , Thomas Daniel Heightman , Steven Howard , Christopher William Murray , David Norton , Marc O'Reilly , Alison Jo-Anne Woolford , Michael Liam Cooke , David Cousin , Stuart Thomas Onions , Jonathan Martin Shannon , John Paul Watts
- 申请人: OTSUKA PHARMACEUTICAL CO., LTD.
- 申请人地址: JP Tokyo
- 专利权人: OTSUKA PHARMACEUTICAL CO., LTD.
- 当前专利权人: OTSUKA PHARMACEUTICAL CO., LTD.
- 当前专利权人地址: JP Tokyo
- 代理机构: Heslin Rothenberg Farley & Mesiti P.C.
- 优先权: GB1518676.0 20151021,GB1611351.6 20160630
- 主分类号: C07D405/14
- IPC分类号: C07D405/14 ; A61K31/55 ; C07D487/04 ; A61P35/00 ; A61K31/553 ; C07D403/14 ; C07D471/08 ; C07D403/04 ; C07D413/14 ; A61K31/506 ; C07D498/22 ; A61K31/5377 ; C07D417/14 ; C07D409/14 ; C07D513/04 ; A61K31/444 ; C07D401/14 ; C07D471/04 ; C07D497/08 ; A61K31/541
摘要:
The invention provides a compound of formula (0): or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and C—F; Z is selected from C—Rz and N; R1 is selected from: -(Alk1)t-Cyc1; wherein t is 0 or 1; Optionally substituted C1-6 acyclic hydrocarbon groups R2 is selected from hydrogen; halogen; and C1-3 hydrocarbon groups optionally substituted with one or more fluorine atoms; R3 is hydrogen or a group L-R7; R4 is selected from hydrogen; methoxy; and optionally substituted C1-3 alkyl; and R4a is selected from hydrogen and a C1-3 alkyl group; wherein Rz, Alk1, Cyc1, L1 and R7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof. The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
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