2450-08-0

Usage

Uses

Used in Pharmaceutical Research and Organic Synthesis:
PYRIMIDINE-4-CARBOXYLIC ACID METHYL ESTER is used as a key intermediate and building block in the synthesis of various pharmaceutical and agrochemical products. Its versatile chemical structure allows for the development of new materials and chemical processes, contributing to the advancement of medicinal chemistry.
Used in the Synthesis of Biologically Active Compounds:
PYRIMIDINE-4-CARBOXYLIC ACID METHYL ESTER is employed as a starting material for the synthesis of biologically active compounds, which have potential applications in the pharmaceutical industry. Its unique properties enable the creation of novel compounds with therapeutic effects.
Used in Medicinal Chemistry:
PYRIMIDINE-4-CARBOXYLIC ACID METHYL ESTER is utilized in the field of medicinal chemistry for its potential use in the development of new drugs and therapeutic agents. Its presence in the synthesis of various compounds makes it a valuable asset in the discovery and design of innovative pharmaceuticals.

InChI:InChI=1/C6H6N2O2/c1-10-6(9)5-2-3-7-4-8-5/h2-4H,1H3

Upstream product

• 31462-59-6 pyrimidine-4-carboxylic acid 
• 3438-46-8 4-Methylpyrimidine 
• 67-56-1 methanol 

Downstream Products

• 75399-06-3 3-Oxo-3-pyrimidin-4-yl-propionic acid methyl ester 
• 698395-65-2 C₁₆H₁₆ClN₃O₂ 
• 317332-24-4 1-[1-(4-fluorobenzyl)-1H-pyrrol-2-yl]-3-pyrimidin-4-yl-propan-1,3-dione 
• 39513-54-7 pyrimidine-4-carboxylic acid hydrazide 
• 33581-98-5 4-(hydroxymethyl)pyrimidine 
• 503860-53-5 2-mercapto-3-methyl-6-pyrimidin-4-yl-3H-pyrimidin-4-one 
• 503860-54-6 2-chloro-3-methyl-6-(pyrimidin-4-yl)-pyrimidine-4-one 

Relevant academic research and scientific papers

HETEROARYL-SUBSTITUTED TRIAZOLES AS APJ RECEPTOR AGONISTS

Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.

Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure

A novel class of therapeutic drug candidates for heart failure, highly potent and selective GRK2 inhibitors, exhibit potentiation of β-adrenergic signaling in vitro studies. Hydrazone derivative 5 and 1,2,4-triazole derivative 24a were identified as hit compounds by HTS. New scaffold generation and SAR studies of all parts resulted in a 4-methyl-1,2,4-triazole derivative with an N-benzylcarboxamide moiety with highly potent activity toward GRK2 and selectivity over other kinases. In terms of subtype selectivity, these compounds showed enough selectivity against GRK1, 5, 6, and 7 with almost equipotent inhibition to GRK3. Our medicinal chemistry efforts led to the discovery of 115h (GRK2 IC50 = 18 nM), which was obtained the cocrystal structure with human GRK2 and an inhibitor of GRK2 that potentiates β-adrenergic receptor (βAR)-mediated cAMP accumulation and prevents internalization of βARs in β2AR-expressing HEK293 cells treated with isoproterenol. Therefore, 115h appears to be a novel class of therapeutic for heart failure treatment.

PYRIMIDONE COMPOUNDS AS GSK-3 INHIBITORS

The invention relates to pyrimidone derivatives I having activity as GSK-3 inhibitors. The invention further relates to pharmaceutical compositions comprising such derivatives and uses thereof in treating certain disorders. Formula (I):

ARYL SULFONAMIDES

Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.