发明公开
EP3259251A1 N-PHENYL-(MORPHOLIN-4-YL OR PIPERAZINYL)ACETAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF THE WNT SIGNALLING PATHWAYS
审中-公开
N-苯基 - (吗啉-4-基或哌嗪基)乙酰胺衍生物及其作为Wnt信号通路抑制剂的用途
- 专利标题: N-PHENYL-(MORPHOLIN-4-YL OR PIPERAZINYL)ACETAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF THE WNT SIGNALLING PATHWAYS
- 专利标题(中): N-苯基 - (吗啉-4-基或哌嗪基)乙酰胺衍生物及其作为Wnt信号通路抑制剂的用途
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申请号: EP16704645.7申请日: 2016-02-16
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公开(公告)号: EP3259251A1公开(公告)日: 2017-12-27
- 发明人: THEDE, Kai , BENDER, Eckhard , SCOTT, William, J. , GIESE, Anja , ZORN, Ludwig , LIU, Ningshu , MÖNNING, Ursula , SIEGEL, Franziska , GOLZ, Stefan , HÄGEBARTH, Andrea , LIENAU, Philip , PÜEHLER, Florian , BASTING, Daniel , SCHNEIDER, Dirk , MÖWES, Manfred
- 申请人: Bayer Pharma Aktiengesellschaft
- 申请人地址: Müllerstrasse 178 13353 Berlin DE
- 专利权人: Bayer Pharma Aktiengesellschaft
- 当前专利权人: Bayer Pharma Aktiengesellschaft
- 当前专利权人地址: Müllerstrasse 178 13353 Berlin DE
- 代理机构: BIP Patents
- 优先权: EP15155884 20150220
- 国际公布: WO2016131810 20160825
- 主分类号: C07D213/73
- IPC分类号: C07D213/73 ; C07D231/12 ; C07D403/04 ; C07D239/26 ; C07D239/34 ; C07D239/42 ; C07D213/40 ; C07D213/61 ; C07D213/64 ; A61K31/496 ; A61K31/506 ; A61K31/5377 ; A61P35/00
摘要:
The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) wherein LA represents *CH2** or *Δ**; wherein indicates the point of attachment to the carbonyl group, and ** indicates the point of attachment to R1; LB represents *N(H)-C(=O)** or *C(=O)-N(H)**; wherein * indicates the point of attachment to R2, and ** indicates the point of attachment to the phenyl group; R1 represents a group selected from: (AA); wherein * indicates the point of attachment to LA, R2 represents: (BB) wherein * indicates the point of attachment to R3, and ** indicates the point of attachment to LB R3 represents a group selected from: (CC); wherein * indicates the point of attachment to R2; R4 and R5 represent a hydrogen atom; and R6 represents a halogen atom or group selected from: -CH3, -O-CH3, -O-CHF2, -O-CF3, and -O-cyclopropyl; to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular, of a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients.
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