374776-34-8

Basic information

• Product Name: 3-[[[5-(AMinocarbonyl)-1-Methyl-3-propyl-1H-pyrazol-4-yl]aMino]carbonyl]-4-propoxy-benzenesulfonyl Chloride
• Synonyms: 3-[[[5-(AMinocarbonyl)-1-Methyl-3-propyl-1H-pyrazol-4-yl]aMino]carbonyl]-4-propoxy-benzenesulfonyl Chloride
• CAS NO: 374776-34-8
• Molecular Formula: C₁₈H₂₃ClN₄O₅S
• Molecular Weight: 442.91702
• Product Categories: Aromatics, Heterocycles, Pharmaceuticals, Intermediates & Fine Chemicals
• Mol File: 374776-34-8.mol
• Article Data: 5

Chemical Properties

• Boiling Point: 573.5±50.0 °C(Predicted)
• Appearance: /
• Density: 1.42±0.1 g/cm3(Predicted)
• Storage Temp.: Refrigerator
• Solubility: Chloroform, Dichloromethane, Ethyl Acetate
• PKA: 11.77±0.70(Predicted)
• CAS DataBase Reference: 3-[[[5-(AMinocarbonyl)-1-Methyl-3-propyl-1H-pyrazol-4-yl]aMino]carbonyl]-4-propoxy-benzenesulfonyl Chloride(CAS DataBase Reference)
• NIST Chemistry Reference: 3-[[[5-(AMinocarbonyl)-1-Methyl-3-propyl-1H-pyrazol-4-yl]aMino]carbonyl]-4-propoxy-benzenesulfonyl Chloride(374776-34-8)
• EPA Substance Registry System: 3-[[[5-(AMinocarbonyl)-1-Methyl-3-propyl-1H-pyrazol-4-yl]aMino]carbonyl]-4-propoxy-benzenesulfonyl Chloride(374776-34-8)

Safety Data

• Hazardous Substances Data: 374776-34-8(Hazardous Substances Data)

Usage

Chemical Properties

Off-white Solid

Upstream product

• 139756-04-0 1-Methyl-4-(2-n-propoxybenzamido)-3-n-propylpyrazole-5-carboxamide 
• 7790-94-5 chlorosulfonic acid 

Downstream Products

• 374776-38-2 4-(5-(4-(ethoxycarbonylmethyl)piperidinylsulfonyl)-2-n-propoxybenzamido)-1-methyl-3-n-propylpyrazole-5-carboxamide 
• 374776-40-6 4-(5-(4-(2-ethoxycarbonylethyl)piperidinylsulfonyl)-2-n-propoxybenzamido)-1-methyl-3-n-propylpyrazole-5-carboxamide 
• 374776-42-8 4-(5-(4-(3-ethoxycarbonylpropyl)piperidinylsulfonyl)-2-n-propoxybenzamido)-1-methyl-3-n-propylpyrazole-5-carboxamide 
• 374776-46-2 4-(5-(4-(2-ethoxycarbonylethyl)piperazinylsulfonyl)-2-n-propoxybenzamido)-1-methyl-3-n-propylpyrazole-5-carboxamide 
• 374776-44-0 4-(5-(4-(ethoxycarbonylmethyl)piperazinylsulfonyl)-2-n-propoxybenzamido)-1-methyl-3-n-propylpyrazole-5-carboxamide 
• 712349-26-3 {1-[3-(5-carbamoyl-1-methyl-3-propyl-1H-pyrazol-4-ylcarbamoyl)-4-propoxy-benzenesulfonyl]-piperidin-4-yl}-phosphonic acid diethyl ester 
• 374776-48-4 {1-[3-(5-carbamoyl-1-methyl-3-propyl-1H-pyrazol-4-ylcarbamoyl)-4-propoxy-benzenesulfonyl]-piperidin-4-ylmethyl}-phosphonic acid diethyl ester 
• 374776-49-5 (2-{1-[3-(5-carbamoyl-1-methyl-3-propyl-1H-pyrazol-4-ylcarbamoyl)-4-propoxy-benzenesulfonyl]-piperidin-4-yl}-ethyl)-phosphonic acid diethyl ester 
• 382592-28-1 2-methyl-4-{5-[2-(1-methyl-pyrrolidin-2-yl)-ethylsulfamoyl]-2-propoxy-benzoylamino}-5-propyl-2H-pyrazole-3-carboxamide 
• 268203-93-6 5-[2-propyloxy-5-[2-(1-methyl-2-pyrrolidinyl)ethylaminosulfonyl]phenyl]-1-methyl-3-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidine-7-one 

Relevant articles and documents

PHARMACOLOGICAL COMPOSITION FOR PREVENTION AND TREATMENT OF RESPIRATORY DISEASE CONTAINING PYRAZOLOPYRIMIDINONE COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF

Disclosed herein is composition for prevention and treatment of respiratory disease containing a pyrazolopyrimidinone compound or pharmaceutically acceptable salts thereof as an active ingredient.

AGENT FOR THE PREVENTION AND TREATMENT OF LIVER DISEASES CONTAINING PYRAZOLOPYRIMIDINE DERIVATIVE

The present invention relates to the pharmaceutical compositionfor prevention and treatment of liver diseases containing pyrazolopyrimidine derivative as an active ingredient. According to the present invention, pyrazolopyrimidine derivative has an excellent effect on inhibiting collagen synthesis in hepatic stellate cellsand acts directly on the portal vein. Particularly, it may increase the diameter and the amount of blood flow of the portal vein, and finally decrease the pressure thereof. Therefore, pyrazolopyrimidine derivative can be used advantageously for prevention and treatment of hepatic fibrosis, liver cirrhosis caused by hepatic fibrosis, portal hypertension and various complications caused by portal hypertension. In addition, pyrazolopyrimidine derivative according to the present invention can reduce dosing frequency because of its long half-life, and therefore, has an advantage to improve the drug compliance of patients suffering from chronical liver diseases.

Synthesis and phosphodiesterase inhibitory activity of new sildenafil analogues containing a carboxylic acid group in the 5′-sulfonamide moiety of a phenyl ring

New sildenafil analogues possessing a carboxylic acid group in the 5′-sulfonamide of the phenyl ring, 9a-l, were prepared from the readily available starting compounds 6a-b and cyclic amines 3-5 in a three-step sequence. In the enzyme assays, it has been shown that all the target compounds 9a-l proved to be more potent in inhibiting phosphodiesterase type 5 (PDE5) than sildenafil by 4-38-fold. The effect on the IC50 values were investigated by varying the alkoxy group (R) of the phenyl ring, the sulfonamide type (X), and the length of the methylene chain linking the carboxylic acid, and the results were discussed in detail. From this study, we have clearly demonstrated that introduction of a carboxylic acid group to the 5′-sulfonamide moiety of the phenyl ring greatly enhanced PDE5 inhibitory activity, probably by mimicking the phosphate group of cGMP. The piperidinyl propionic acid derivative 9i, which showed the highest PDE5 inhibitory activity and comparable to better selectivity over PDE isozymes in comparison with sildenafil, has been selected for more detailed biological investigations.