[EN] N-PHENYL-(MORPHOLIN-4-YL OR PIPERAZINYL)ACETAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF THE WNT SIGNALLING PATHWAYS<br/>[FR] DÉRIVÉS DE N-PHÉNYL-(MORPHOLIN-4-YL OU PIPÉRAZINYL)ACÉTAMIDE ET LEUR UTILISATION COMME INHIBITEURS DES VOIES DE SIGNALISATION WNT
申请人:BAYER PHARMA AG
公开号:WO2016131810A1
公开(公告)日:2016-08-25
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.
本发明涉及抑制Wnt信号通路的抑制剂,其通用公式为(I),其中LA代表*CH2**或*Δ**;其中*表示与羰基组的连接点,**表示与R1的连接点;LB代表*N(H)-C(=O)**或*C(=O)-N(H)**;其中*表示与R2的连接点,**表示与苯基的连接点;R1代表从(AA)中选择的一个组;其中*表示与LA的连接点,R2代表:(BB)其中*表示与R3的连接点,**表示与LB的连接点;R3代表从(CC)中选择的一个组;其中*表示与R2的连接点;R4和R5代表氢原子;R6代表卤素原子或从-CH3,-O-CH3,-O-CHF2,-O-CF3和-O-环丙基中选择的一个组;涉及制备所述化合物的方法,包括所述化合物的药物组合物和组合,以及将所述化合物用于制造用于治疗或预防疾病,特别是增生紊乱的药物组合物,作为单一药剂或与其他活性成分结合使用。