690998-35-7

Upstream product

• 6345-43-3 pyrimidine-4,6-dicarboxylic acid dimethyl ester 
• 1558-17-4 4,6-dimethylpyrimidine 
• 16490-02-1 pyrimidine-4,6-dicarboxylic acid 
• 612088-38-7 pyrimidine-4,6-dicarboxylic acid monomethyl ester 
• 185147-08-4 4-fluoro-3-methylbenzonitrile 

Downstream Products

• 1605324-97-7 pyrimidine-4,6-dicarboxylic acid 4-{[dideutero-(4-formyl-phenyl)-methyl]-amide} 6-(4-fluoro-3-methyl-benzylamide) 
• 1605324-87-5 4-({[6-(4-fluoro-3-methyl-benzylcarbamoyl)-pyrimidine-4-carbonyl]-amino }-methyl)-benzoic acid methyl ester 

Relevant academic research and scientific papers

Development of a selective matrix metalloproteinase 13 (MMP-13) inhibitor for the treatment of Osteoarthritis

Osteoarthritis (OA) is a chronic disorder that causes damage to the cartilage and surrounding tissues and is characterized by pain, stiffness, and loss of function. Current treatments for OA primarily involve providing only relief of symptoms but does not

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.

MATRIX METALLOPROTEINASE INHIBITORS AND METHODS FOR THE TREATMENT OF PAIN AND OTHER DISEASES

The present invention relates generally to bis-amide containing MMP inhibiting compounds, and more particularly to selectively deuterated bis-amide MMP-13 inhibiting compounds that exhibit increased stability or potency in relation to currently known MMP-

Substituted bis-amide metalloprotease inhibitors

This invention relates to substituted bis-amide pyrimidine compounds of Formula (I), which are useful for the treatment of metalloprotease mediated diseases, in particular MMP-13 related diseases.

Multicyclic bis-amide MMP inhibitors

The present invention relates generally to bis-amide group containing pharmaceutical agents, and in particular, to multicyclic bis-amide MMP-13 inhibitor compounds. More particularly, the present invention provides a new class of MMP-13 inhibiting compounds, containing a pyrimidinyl bis-amide group in combination with a heterocyclic moiety, that exhibit an increased potency and solubility in relation to currently known bis-amide group containing MMP-13 inhibitors.

Selective MMP-13 inhibitors

The invention relates to a pyrimidine-4,6-dicarboxylic acid diamide compound, pharmaceutical preparation comprising it, process for preparing it and method for its pharmaceutical use. Particularly, the pyrimidine-4,6-dicarboxylic acid diamide compound is

NOVEL PYRIMIDINE-4,6-DICARBOXAMIDES FOR THE SELECTIVE INHIBITION OF COLLAGENASES

Pyrimidine-4,6-dicarboxamides of formula (I), are suitable for the selective inhibition of collagenase (MMP 13). The pyrimidine-4,6-dicarboxamides can thus be used for the treatment of degenerative joint diseases.