[EN] PYRAZOLOPYRAZINES ACTING ON CANCERS VIA INHIBITION OF CDK12<br/>[FR] PYRAZOLOPYRAZINES AGISSANT SUR DES CANCERS PAR INHIBITION DE CDK12
申请人:BAYER AG
公开号:WO2021176049A1
公开(公告)日:2021-09-10
The present invention provides compounds of general formula (I) in which X, R1, R2 and R3 are as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of hyperproliferative disorders such as cancer disorders, as a sole agent or in combination with other active ingredients.
[EN] CYANOINDOLINE DERIVATIVES AS NIK INHIBITORS<br/>[FR] NOUVEAUX DÉRIVÉS DE CYANOINDOLINE COMME INHIBITEURS DE NIK
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2018002219A1
公开(公告)日:2018-01-04
Fused aromatic bicyclic substituted 5-(2-amino-4-pyrimidinyl)- cyanoindoline derivatives (I) useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-KB-inducing kinase (NIK - also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
Anilinotriazoles as potent gamma secretase modulators
作者:Adriana I. Velter、François P. Bischoff、Didier Berthelot、Michel De Cleyn、Daniel Oehlrich、Libuse Jaroskova、Gregor Macdonald、Garrett Minne、Serge Pieters、Frederik Rombouts、Sven Van Brandt、Yves Van Roosbroeck、Michel Surkyn、Andrés A. Trabanco、Gary Tresadern、Tongfei Wu、Herman Borghys、Marc Mercken、Chantal Masungi、Harrie Gijsen
DOI:10.1016/j.bmcl.2014.10.024
日期:2014.12
The design and synthesis of a novel series of potent gammasecretasemodulators is described. Exploration of various spacer groups between the triazole ring and the aromatic appendix in 2 has led to anilinotriazole 28, which combined high in vitro and in vivo potency with an acceptable drug-like profile.
The present invention relates to compounds of the formula
and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.