1246765-54-7

Basic information

• Product Name: (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid
• Synonyms: (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid
• CAS NO: 1246765-54-7
• Molecular Weight: 404.469
• Mol File: 1246765-54-7.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid(CAS DataBase Reference)
• NIST Chemistry Reference: (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid(1246765-54-7)
• EPA Substance Registry System: (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid(1246765-54-7)

Safety Data

• Hazardous Substances Data: 1246765-54-7(Hazardous Substances Data)

Upstream product

• 19841-85-1 6-acetyl-2-hydroxynicotinic acid 
• 1246765-10-5 (R)-4-(3-chloro-5-cyclopentyl-4,5-dihydro-1H-pyrazol-1-yl)-2-methylbenzonitrile 
• 19841-86-2 methyl 6-acetyl-2-methoxynicotinate 
• 19841-85-1 6-Acetyl-1,2-dihydro-2-oxo-3-pyridinecarboxylic acid 
• 65515-32-4 methyl 6-chloro-2-methoxypyridine-3-carboxylate 
• 2931-23-9 ethyl 3-cyclopentyl acrylate 
• 872-53-7 cyclopentanealdehyde 
• 38496-18-3 2,6-dichloropyridine-3-carboxylic acid 
• 1246765-51-4 methyl 6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinate 
• 1246765-04-7 4-(3-chloro-5-cyclopentyl-4,5-dihydro-1H-pyrazol-1-yl)-2-methylbenzonitrile 
• 1246765-27-4 methyl 2-methoxy-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)nicotinate 
• 1246765-08-1 4-(5-cyclopentyl-3-oxopyrazolidin-1-yl)-2-methylbenzonitrile 
• 1023649-51-5 4-hydrazinyl-2-methylbenzonitrile 
• 1246765-25-2 methyl 6-(3-cyclopentylacryloyl)-2-methoxynicotinate 

Downstream Products

• 1246766-12-0 (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxy-N-methylnicotinamide 
• 1246766-15-3 (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxy-N,N-dimethylnicotinamide 
• 1246766-25-5 (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxy-N-(methylsulfonyl)nicotinamide 
• 1246766-21-1 (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxy-N-(1H-tetrazol-5-yl)nicotinamide 

Relevant articles and documents

Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5- dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist

A novel series of nonsteroidal mineralocorticoid receptor (MR) antagonists identified as part of our strategy to follow up on the clinical candidate PF-03882845 (2) is reported. Optimization departed from the previously described pyrazoline 3a and focused on improving the selectivity for MR versus the progesterone receptor (PR) as an approach to avoid potential sex-hormone-related adverse effects and improving biopharmaceutical properties. From this effort, (R)-14c was identified as a potent nonsteroidal MR antagonist (IC50 = 4.5 nM) with higher than 500-fold selectivity versus PR and other related nuclear hormone receptors, with improved solubility as compared to 2 and pharmacokinetic properties suitable for oral administration. (R)-14c was evaluated in vivo using the increase of urinary Na+/K+ ratio in rat as a mechanism biomarker of MR antagonism. Treatment with (R)-14c by oral administration resulted in significant increases in urinary Na +/K+ ratio and demonstrated this novel compound acts as an MR antagonist.

4, 5-DIHYDRO-LH-PYRAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USES

Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.