1443531-60-9

Upstream product

• 38512-82-2 3-methoxy-4-nitrotoluene 
• 80041-89-0 isopropylboronic acid 
• 1388033-29-1 7-methoxy-5-methyl-1-benzothiophene 
• 7732-18-5 water 
• 1221448-80-1 methyl 7-acetoxy-1-benzothiophene-5-carboxylate 
• 314725-16-1 7-hyroxy-benzo[b]thiophene-5-carboxylic acid methyl ester 
• 1221448-81-2 7-hydroxy-1-benzothiophene-5-carboxylic acid 
• 700-38-9 2-nitro-5-methylphenol 
• 39538-68-6 2-methoxy-4-methylaniline 
• 5419-55-6 Triisopropyl borate 
• 1443531-59-6 1-[(2,2-diethoxyethyl)sulfanyl]-2-methoxy-4-methylbenzene 
• 216394-11-5 2-methoxy-4-methylbenzenesulfonyl chloride 
• 83485-34-1 2-methoxy-4-methylbenzenethiol 

Downstream Products

• 1443530-05-9 4-{[4-amino-6-(methoxymethyl)-5-(7-methoxy-5-methyl-1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-7-yl]methyl}piperazin-2-one 

Relevant academic research and scientific papers

FGFR INHIBITOR AND MEDICAL APPLICATION THEREOF

Provided is a FGFR inhibitor, designating a compound represented by formula (I) or a pharmaceutically acceptable salt thereof. Also provided is the application of a drug for treating solid tumors, such as FGFR related diseases.

NEW COMPOUND HAVING FGFR INHIBITORY ACTIVITY AND PREPARATION AND APPLICATION THEREOF

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.

PROCESS FOR PREPARING BENZOTHIOPHEN-2YL BORONATE

A process for preparing the benzothiophen-2-yl boronate of formula (VI) which serves as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of proliferative disorders, such as cancer and tumor diseases.

Discovery of Rogaratinib (BAY 1163877): a pan-FGFR Inhibitor

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

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 IN THE TREATMENT CANCER

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

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

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.