基本信息:
- 专利标题： BENZOLACTAM COMPOUNDS AS PROTEIN KINASE INHIBITORS
- 申请号：US17224733 申请日：2021-04-07
- 公开(公告)号：US20230019032A1 公开(公告)日：2023-01-19
- 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
- 优先权： GB1518676.0 20151021,GB1611351.6 20160630
- 主分类号： C07D405/14
- IPC分类号： C07D405/14 ; C07D403/14 ; C07D409/14 ; C07D471/04 ; C07D413/14 ; C07D471/08 ; C07D401/14 ; C07D417/14 ; A61P35/00 ; A61K31/444 ; A61K31/506 ; A61K31/5377 ; A61K31/541 ; A61K31/55 ; A61K31/553 ; C07D403/04 ; C07D487/04 ; C07D497/08 ; C07D498/22 ; C07D513/04
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 L1-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.
公开/授权文献:
- US11939321B2 Benzolactam compounds as protein kinase inhibitors 公开/授权日：2024-03-26
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07D | 杂环化合物 |
| ------C07D405/00 | 杂环化合物，含有1个或多个以氧原子作为仅有的杂环原子的环，且含有1个或多个以氮原子作为仅有的杂环原子的环 |
| --------C07D405/14 | .含3个或更多个杂环 |