6345-43-3

Usage

Uses

Used in Pharmaceutical Industry:
DIMETHYL PYRIMIDINE-4,6-DICARBOXYLATE is used as a key intermediate in the preparation of radiolabeled selective matrix metalloproteinase 13 (MMP-13) inhibitors. These inhibitors are essential in the development of drugs targeting MMP-13, an enzyme implicated in various diseases, including arthritis and cancer. By incorporating DIMETHYL PYRIMIDINE-4,6-DICARBOXYLATE into the molecular structure of these inhibitors, researchers can enhance their selectivity and effectiveness in blocking MMP-13 activity, leading to potential therapeutic benefits for patients suffering from related conditions.

InChI:InChI=1/C8H8N2O4/c1-13-7(11)5-3-6(8(12)14-2)10-4-9-5/h3-4H,1-2H3

Upstream product

• 1558-17-4 4,6-dimethylpyrimidine 
• 67-56-1 methanol 
• 16490-02-1 pyrimidine-4,6-dicarboxylic acid 

Downstream Products

• 135002-52-7 pyrimidine-4,6-dicarbohydrazide 
• 690998-35-7 6-(4-fluoro-3-methyl-benzylcarbamoyl)-pyrimidine-4-carboxylic acid 

Relevant academic research and scientific papers

METHODS OF TREATING CANCER

The present disclosure relates to methods of treating cancer in a patient using a combination of an inhibitor of an immune checkpoint protein and an indole compound or its phosphate derivative.

INDOLE COMPOUNDS AND THEIR USE

The present disclosure relates to indole compounds and pharmaceutical compositions thereof, and their use in stimulating the immune system of patients in need thereof and in treating cancer.

Radiolabeled Selective Matrix Metalloproteinase 13 (MMP-13) Inhibitors: (Radio)Syntheses and in Vitro and First in Vivo Evaluation

The noninvasive imaging of MMP activity in vivo could have a high impact in basic research as well as in clinical applications. This approach can be established using radiolabeled MMP inhibitors (MMPIs) as tracers for the detection of activated MMPs by means of PET. However, the complexity of diseases associated with dysregulated MMP expression necessitates the imaging of distinct MMPs or MMP subgroups to distinguish their individual role in specific diseases. To this end, selective and potent MMP-13 inhibitors based on a N,N′-bis(benzyl)pyrimidine-4,6-dicarboxamide core have been synthesized and successfully radiolabeled with carbon-11, fluorine-18, and gallium-68. Selected radiolabeled candidates were evaluated in vitro and in vivo regarding their pharmacokinetic properties and metabolic stability.

HISTONE LYSINE DEMETHYLASE INHIBITORS

The invention provides a compound which is an iV-oxalylglycine derivative of formula (I): a hydroxamic acid derivative of formula (II): or a heteroaryl derivative of fomula (III): wherein n; Z1; Z2; Y1; Y2; A; p; X1; X2; m; R4; B; R5; R6; R7; R8; R9; X3; R10; R11 and R12 are as defined herein, or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of the human 2-oxoglutarate-dependant JMJD2 subfamily of histone demethylases, in particular JMJD2E. Such inhibitors are useful in changing the epigenetic state of cells resulting in the inhibition / activation of chromatin remodelling, multiple gene activation / deactivation, and in treating cancer and other conditions characterised by undesirable cellular proliferation, and psychiatric disorders including depression.

Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases

The dynamic methylation of histone lysyl residues plays an important role in biology by regulating transcription, maintaining genomic integrity, and by contributing to epigenetic effects. Here we describe a variety of inhibitor scaffolds that inhibit the human 2-oxoglutarate-dependent JMJD2 subfamily of histone demethylases. Combined with structural data, these chemical starting points will be useful to generate small-molecule probes to analyze the physiological roles of these enzymes in epigenetic signaling.

PYRIDINE-2,4-DICARBOXYLIC ACID DIAMIDES AND PYRIMIDINE-4,6-DICARBOXYLIC ACID DIAMIDES AND THE USE THEREOF FOR SELECTIVELY INHIBITING COLLAGENASES

Pyridine-2,4-dicarboxylic acid diamides and pyrimidine-4,6-dicarboxylic acid diamides of formula I. These compounds are found to possess the property of selectively inhibiting collagenase (MMP). They may therefore be useful in prophylaxis and therapy of diseases whose course involves an increased activity of matrix metalloproteinase 13.