83485-34-1Relevant articles and documents
NEW COMPOUND HAVING FGFR INHIBITORY ACTIVITY AND PREPARATION AND APPLICATION THEREOF
-
, (2019/05/30)
The present invention relates to a new compound having an FGFR inhibitory activity and preparation and application thereof. In particular, the compound according to the present invention has a structure as shown in formula I, wherein each group and substituent are as defined in the description. Also disclosed in the present invention are a preparation method for the compound and a use thereof in preparation of a drug for treating and/or preventing a tumor-related disease and/or an FGFR-related disease.
Discovery of Rogaratinib (BAY 1163877): a pan-FGFR Inhibitor
Collin, Marie-Pierre,Lobell, Mario,Hübsch, Walter,Brohm, Dirk,Schirok, Hartmut,Jautelat, Rolf,Lustig, Klemens,B?mer, Ulf,V?hringer, Verena,Héroult, Mélanie,Grünewald, Sylvia,Hess-Stumpp, Holger
, p. 437 - 445 (2018/02/21)
Rogaratinib (BAY 1163877) is a highly potent and selective small-molecule pan-fibroblast growth factor receptor (FGFR) inhibitor (FGFR1–4) for oral application currently being investigated in phase 1 clinical trials for the treatment of cancer. In this publication, we report its discovery by de novo structure-based design and medicinal chemistry optimization together with its pharmacokinetic profile.
SUBSTITUTED BENZOTHIENYL - PYRROLOTRIAZINES AND USES THEREOF IN THE TREATMENT CANCER
-
, (2013/07/05)
This invention relates to novel substituted 5-(l-benzothiophen-2-yl)pyrrolo[2,l-fJ[l,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
Disubstituted benzothienyl-pyrrolotriazines and uses thereof
-
, (2013/06/28)
This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
SUBSTITUTED BENZOTHIENYL-PYRROLOTRIAZINES AND USES THEREOF
-
, (2013/09/12)
This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
DISUBSTITUTED BENZOTHIENYL-PYRROLOTRIAZINES AND THEIR USE AS FGFR KINASE INHIBITORS
-
, (2013/07/05)
This invention relates to novel substituted 5-(1-benzothiophen-2-yl) pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives of formula (I) wherein R1 is hydrogen, chloro, methyl or methoxy, R2 is hydrogen or methoxy, with the proviso that at least one of R1 and R2 is other than hydrogen, G1 represents chloro, (C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl, 5-membered aza-heteroaryl, or the group -CH2-OR3, -CH2-NR4R5 or -C(=0)- NR4R6, and G2 represents chloro, cyano, (C1-C4)-alkyl, or the group - CR8AR8B-OH, -CH2-NR9R10, -C(=0)-NR11R12 or -CH2-OR15, having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.