862370-77-2

Upstream product

• 770-31-0 4-amino-2-(methylthio)pyrimidine-5-carbaldehyde 
• 13388-75-5 3,5-dimethoxyphenylacetonitrile 
• 5909-24-0 4-chloro-2-methanesulfanylpyrimidine-5-carboxylic acid ethyl ester 
• 877-88-3 3,5-dimethoxybenzyl bromide 
• 588-36-3 (4-amino-2-(methylthio)pyrimidin-5-yl)methanol 
• 776-53-4 ethyl 4-amino-2-methylmercaptopyrimidine-5-carboxylate 
• 7646-69-7 sodium hydride 

Downstream Products

• 862370-83-0 N-(tert-butyl)-N'-[2-[[3-[[tert-butyl(dimethyl)silyl]oxy]propyl]amino]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]urea 
• 862370-80-7 6-(3,5-dimethoxyphenyl)-N²-[3-(4-methyl-1-piperazinyl)propyl]pyrido[2,3-d]pyrimidine-2,7-diamine 
• 862370-82-9 N²-[3-[[tert-butyl(dimethyl)silyl]oxy]propyl]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidine-2,7-diamine 
• 862370-79-4 N²-[4-(diethylamino)butyl]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidine-2,7-diamine 
• 862370-81-8 3-[[7-amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-2-yl]amino]-1-propanol 
• 862370-78-3 6-(3,5-dimethoxyphenyl)-2-(methylsulfinyl)pyrido[2,3-d]pyrimidin-7-amine 
• 1294001-68-5 C₂₁H₂₅N₅O₃S 

Relevant academic research and scientific papers

FGFR INHIBITOR AND APPLICATION THEREOF

An azatricyclic compound (as represented by formula I) which acts as an inhibitor of fibroblast growth factor receptors (FGFR), as well as a pharmaceutical composition thereof, a preparation method, and a use therefor in the treatment of FGFR-mediated diseases. The azatricyclic compound exerts an effect by means of participating in the regulation of a plurality of processes such as cell proliferation, apoptosis, migration, neovascularization, and the like. AA%%%Formula (I).

FGFR4 kinase inhibitor, preparation method and uses thereof

The present invention relates to a compound represented by a formula (I), or a pharmaceutically acceptable salt, a solvate, a polymorph or an isomer thereof, and uses in preparation of drugs for treatment of FGFR4 mediated diseases.

FGFR4 kinase inhibitor, preparation method and application thereof

The invention relates to an FGFR4 kinase inhibitor, a preparation method and application thereof, and provides a compound represented by a formula (I), or a pharmaceutically acceptable salt, a solvate, a polymorph or an isomer thereof, and use in preparation of medicaments for treatment of FGFR4 mediated diseases.

NOVEL HETEROCYCLIC DERIVATIVE COMPOUND AND USE THEREOF

The present invention relates to a novel heterocyclic derivative compound and a use thereof, and in particular, to a novel heterocyclic derivative compound having selective inhibitory activity for a fibroblast growth factor receptor (FGFR) and a pharmaceutical composition including the same preventing and treating various diseases relating to the FGFR.

HETEROARYL COMPOUNDS AND USES THEREOF

The present invention relates to compounds useful as inhibitors of protein kinases, containing a cysteine residue in the ATP binding site. The invention further provides for pharmaceutically acceptable compositions comprising therapeutically effective amounts of one or more of the protein kinase inhibitor compounds and methods of using said compositions in the treatment of cancers and carcinomas.

Synthesis and biological evaluation of a triazole-based library of pyrido[2,3-d]pyrimidines as FGFR3 tyrosine kinase inhibitors

A library of pyrido[2,3-d]pyrimidines was designed as inhibitors of FGFR3 tyrosine kinase allowing possible interactions with an unexploited region of the ATP binding-site. This library was built-up with an efficient step of click-chemistry giving easy access to triazole-based compounds bearing a large panel of substituents. Among the 27 analogues synthesized, more than half exhibited 55-89% inhibition of in vitro FGFR3 kinase activity at 2 μM and one (19g) was able to inhibit auto-phosphorylation of mutant FGFR3-K650M in transfected HEK cells.

Synthesis and structure-activity relationships of soluble 7-substituted 3-(3,5-dimethoxyphenyl)-1,6-naphthyridin-2-amines and related ureas as dual inhibitors of the fibroblast growth factor receptor-1 and vascular endothelial growth factor receptor-2 tyrosine kinases

7-Substituted 3-aryl-1,6-naphthyridine-2,7-diamines and related 2-ureas are inhibitors of fibroblast growth factor receptor-1 (FGFR-1) and vascular endothelial growth factor receptor-2 (VEGFR-2). 3-(3,5-Dimethoxyphenyl) and 3-phenyl analogues were prepared from 7-acetamido-2-teri-butylureas by alkylation with benzyl ω-iodoalkyl ethers, debenzylation, and animation, followed by selective cleavage of the 7-N-acetamide. 3-(2,6-Dichlorophenyl) analogues were prepared from the 7-fluoro-2-amine by displacement with substituted alkylamines, followed by selective acylation of the resulting substituted naphthyridine-2,7-diamines with alkyl isocyanates. The 3-(3,5-dimethoxyphenyl) derivatives were low nanomolar inhibitors of both FGFR and VEGFR and were highly selective (>100-fold) over PDGFR and c-Src. Variations in the base strength or spatial position of the 7-side chain base had only small effects on the potency (5-fold) or selectivity (20-fold). The 3-(2,6-dichlorophenyl)-2-urea derivatives were slightly less active against VEGFR and less selective, being more effective against PDGFR (ca. 10-fold) and c-Src (ca. 500-fold). The 3-(3,5-dimethoxyphenyl)-1,6-naphthyridines were generally more potent than the corresponding pyrido[2,3-d]pyrimidines against both VEGFR and FGFR (2- to 20-fold), with only slightly increased PDGFR and c-Src activity. The 3-(3,5-dimethoxyphenyl)-1,6-naphthyridine 2-ureas were also low nanomolar inhibitors of the growth of human umbilical vein endothelial cells (HUVECs) stimulated by serum, FGF, or VEGF, at concentrations that did not affect the growth of representative tumor cell lines, and were more (3- to 65-fold) potent than the corresponding pyrido[2,3-d]pyrimidines.