公开(公告)号：EP3623370A1

公开(公告)日：2020-03-18

申请号：EP18382659.3

申请日：2018-09-13

申请人： Fundación del Sector Público Estatal Centro Nacional de Investigaciones Oncológicas Carlos III (F.S.P. CNIO)

发明人： PASTOR FERNANDEZ, Joaquin Angel ,  BLASCO MARHUENDA, Maria Antonia ,  MARTINEZ GONZALEZ, Sonia ,  BLANCO-APARICIO, Carmen ,  GARCIA GARCIA, Ana Belen ,  VARELA BUSTO, Carmen ,  GOMEZ-CASERO ESTEBAN, Elena ,  BEJARANO BOSQUE, Leire ,  MENDEZ PERTUZ, Marinela ,  MARTINEZ RODRIGUEZ, Paula ,  GARCIA-BECCARIA, Maria

IPC分类号： C07D417/12 ,  A61P35/00 ,  A61K31/4439 ,  A61K31/506

摘要： Novel TRF1 modulators and analogues thereof.
There is provided compounds of Formula I, wherein R, R1, R2 and X have meanings written in the description. Such compounds are useful as TRF1 inhibitors and, for that reason, as medicaments, in the treatment of cancer, particularly high cancer stem cell cancer like glioblastoma and lung cancer, and can be also useful for the development of additional TRF1 inhibitors and increasing knowledge about TRF1 activity.

公开(公告)号：EP3623009A1

公开(公告)日：2020-03-18

申请号：EP18382658.5

申请日：2018-09-13

申请人： Fundación del Sector Público Estatal Centro Nacional de Investigaciones Oncológicas Carlos III (F.S.P. CNIO)

发明人： BLASCO MARHUENDA, Maria Antonia ,  PASTOR FERNANDEZ, Joaquin Angel ,  BEJARANO BOSQUE, Leire ,  MENDEZ PERTUZ, Marinela ,  MARTINEZ RODRIGUEZ, Paula ,  BLANCO-APARICIO, Carmen ,  GOMEZ-CASERO ESTEBAN, Elena ,  GARCIA-BECCARIA, Maria

IPC分类号： A61P35/00 ,  A61K31/4985 ,  A61K45/06

摘要： The invention provides TRF1 inhibitors and compositions comprising them for the treatment of a brain cancer, such as a glioblastoma, and particularly a glioblastoma multiforme (GBM). PI3K inhibitors can be among the TRF1 inhibitors used. The compositions can comprise more than one TRF1 inhibitor, being particularly advantageous that at least one of the inhibitors is a PI3K inhibitor and that at least a second possible TRF1 inhibitor present is selected from the group an RTK inhibitor, a MEK inhibitor, an ERK inhibitor, an HSP90 inhibitor, docetaxel and gemcitabine, because such compositions show a synergic effect. The invention also relates to a method for identifying compounds candidates to be used for treating glioblastoma or other cancers, which method is based on the identification of the compound as a TRF1 inhibitor.

公开(公告)号：EP3849556A1

公开(公告)日：2021-07-21

申请号：EP18773386.0

申请日：2018-09-13

申请人： Fundación del Sector Público Estatal Centro Nacional de Investigaciones Oncológicas Carlos III (F.S.P. CNIO)

发明人： BLASCO MARHUENDA, Maria Antonia ,  PASTOR FERNANDEZ, Joaquin Angel ,  BEJARANO BOSQUE, Leire ,  MENDEZ PERTUZ, Marinela ,  MARTINEZ RODRIGUEZ, Paula ,  BLANCO-APARICIO, Carmen ,  GOMEZ-CASERO ESTEBAN, Elena ,  GARCIA-BECCARIA, Maria

IPC分类号： A61K31/4985 ,  A61K45/06 ,  A61P35/00