1184919-05-8

Basic information

• Product Name: 6-Bromo-4-hydroxy-[1,5]naphthyridine-3-carboxylic acid ethyl ester
• Synonyms: 6-Bromo-4-hydroxy-[1,5]naphthyridine-3-carboxylic acid ethyl ester;6-Bromo-1,5-naphthyridine-4-oxo-3-carboxylic acid ethyl ester;ETHYL 6-BROMO-4-HYDROXY-1,5-NAPHTHYRIDINE-3-CARBOXYLATE
• CAS NO: 1184919-05-8
• Molecular Formula: C11H9BrN2O3
• Molecular Weight: 297.10476
• Mol File: 1184919-05-8.mol
• Article Data: 7

Chemical Properties

• Appearance: /
• CAS DataBase Reference: 6-Bromo-4-hydroxy-[1,5]naphthyridine-3-carboxylic acid ethyl ester(CAS DataBase Reference)
• NIST Chemistry Reference: 6-Bromo-4-hydroxy-[1,5]naphthyridine-3-carboxylic acid ethyl ester(1184919-05-8)
• EPA Substance Registry System: 6-Bromo-4-hydroxy-[1,5]naphthyridine-3-carboxylic acid ethyl ester(1184919-05-8)

Safety Data

• Hazardous Substances Data: 1184919-05-8(Hazardous Substances Data)

Upstream product

• 4487-59-6 2-bromo-5-nitropyridine 
• 101-84-8 diphenylether 
• 1414862-25-1 C₁₁H₁₁BrN₂O₄ 
• 24362-46-7 diethyl 2-(ethoxymethylene)malonate 
• 13534-97-9 6-bromopyridine-3-amine 
• 1220700-73-1 diethyl 2-(((6-bromopyridin-3-yl)amino)methylene)malonate 

Downstream Products

• 127094-57-9 4,6-dichloro-(1,5)-naphthyridine-3-carboxylic acid ethyl ester 
• 1416000-52-6 ethyl 6-chloro-4-((3-(trifluoromethyl)phenyl)amino)-1,5-naphthyridine-3-carboxylate 
• 1415999-78-8 2-(6-methoxypyridin-3-yl)-10-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)pyrido[3,2-c][1,5] naphthyridin-9(10H)-one 
• 1416000-69-5 tert-butyl 4-(4-(2-(6-methoxypyridin-3-yl)-9-oxopyrido[3,2-c][1,5]naphthyridin-10(9H)-yl)-2-(trifluoromethyl)phenyl)piperazin-1-carboxylate 
• 1416000-70-8 ethyl 6-chloro-4-((4-(2-cyanopropan-2-yl)phenyl)amino)-1,5-naphthyridine-3-carboxylate 
• 1416000-72-0 2-(4-((6-chloro-3-(hydroxymethyl)-1,5-naphthyridin-4-yl)amino) phenyl)-2-methylpropionitrile 
• 1416000-76-4 2-(4-(2-chloro-9-oxopyrido[3,2-c][1,5]naphthyridin-10(9H)-yl)phenyl)-2-methyl propanenitrile 
• 1415999-80-2 2-methyl-2-(4-(9-oxo-2-(quinolin-3-yl)pyrido [3,2-c][1,5]naphthyridin-10(9H)-yl)phenyl) propanenitrile 
• 1416000-79-7 tert-butyl 4-(4-(2-(6-aminopyridin-3-yl)-9-oxopyrido[3,2-c][1,5]naphthyridin-10(9H)-yl)-2-(trifluoromethyl)phenyl)piperazin-1-carboxylate 
• 1415999-82-4 2-(6-aminopyridin-3-yl)-10-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)pyrido[3,2-c][1,5]naphthyridin-9(10H)-one hydrochloride 
• 1415999-84-6 2-(4-(2-(6-aminopyridin-3-yl)-9-oxopyrido [3,2-c][1,5]naphthyridin-10(9H)-yl)phenyl)-2-methylpropanenitrile 
• 1415999-86-8 2-(4-(2-(6-methoxypyridin-3-yl)-9-oxopyrido [3,2-c][1,5]naphthyridin-10(9H)-yl)phenyl)-2-methylpropanenitrile 
• 1415999-92-6 N-(5-(9-oxo-10-(3-(trifluoromethyl)phenyl)-9,10-dihydropyrido[3,2-c][1,5]naphthyridin-2-yl) pyridin-2-yl)acetamide 
• 1416000-85-5 tert-butyl 3-(9-oxo-10-(3-(trifluoromethyl)phenyl)-9,10-dihydropyrido[3,2-c][1,5]naphthyridin-2-yl)-1H-pyrrolo[2,3-b]pyridin-1-carboxylate 

Relevant articles and documents

Discovery of the highly potent PI3K/mTOR dual inhibitor PF-04979064 through structure-based drug design

PI3K, AKT, and mTOR are key kinases from PI3K signaling pathway being extensively pursued to treat a variety of cancers in oncology. To search for a structurally differentiated back-up candidate to PF-04691502, which is currently in phase I/II clinical trials for treating solid tumors, a lead optimization effort was carried out with a tricyclic imidazo[1,5]naphthyridine series. Integration of structure-based drug design and physical properties-based optimization yielded a potent and selective PI3K/mTOR dual kinase inhibitor PF-04979064. This manuscript discusses the lead optimization for the tricyclic series, which both improved the in vitro potency and addressed a number of ADMET issues including high metabolic clearance mediated by both P450 and aldehyde oxidase (AO), poor permeability, and poor solubility. An empirical scaling tool was developed to predict human clearance from in vitro human liver S9 assay data for tricyclic derivatives that were AO substrates.

THREE-RING PI3K AND/OR MTOR INHIBITOR

The present application relates to a compound as represented by general formula (I), a pharmaceutically acceptable salt, ester, solvate or stereoisomer thereof, preparation method of the compounds, a pharmaceutical composition containing the compounds, us

THREE-RING PI3K AND/OR MTOR INHIBITOR

The present application relates to a compound as represented by general formula (I), a pharmaceutically acceptable salt, ester, solvate or stereoisomer thereof, preparation method of the compounds, a pharmaceutical composition containing the compounds, uses thereof in the preparation of drugs for treating and/or preventing proliferative diseases, and a method using the compounds to treat and/or prevent proliferative diseases. R1, R2, R3, R4, R5, R6, X, A and B in the formula are as defined in the specification.