- PHARMACOLOGICAL COMPOSITION FOR PREVENTION AND TREATMENT OF RESPIRATORY DISEASE CONTAINING PYRAZOLOPYRIMIDINONE COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
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Disclosed herein is composition for prevention and treatment of respiratory disease containing a pyrazolopyrimidinone compound or pharmaceutically acceptable salts thereof as an active ingredient.
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Page/Page column 5 - 6
(2010/04/03)
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- HIGHLY SELECTIVE and LONG-ACTING PDE5 MODULATORS
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Disclosed herein are substituted phosphodiesterase type 5 enzyme modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
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Page/Page column 58
(2008/12/07)
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- AGENT FOR THE PREVENTION AND TREATMENT OF LIVER DISEASES CONTAINING PYRAZOLOPYRIMIDINE DERIVATIVE
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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.
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Page/Page column 7
(2008/06/13)
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- Preparing pyrazolopyrimidinone derivatives for the treatment of impotence
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The present invention relates to the method for preparing pyrazolopyrimidinone derivatives and their pharmaceutically acceptable salts having efficacy on the treatment of impotence, one of male sexual dysfunctions. The method according to the present invention comprises the steps of chlorosufonation the pyrazolamide, followed by amination with amine and intramolecular cyclization. The method provides the pyrazolopyrimidinone derivatives and their pharmaceutically acceptable salts with high yield and in an economic manner.
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- Synthesis and phosphodiesterase inhibitory activity of new sildenafil analogues containing a carboxylic acid group in the 5′-sulfonamide moiety of a phenyl ring
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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.
- Kim,Lee,Lee,Ryu,Kim,Lee,Choi,Ryu,Kim,Im,Choi,Kim
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p. 3013 - 3021
(2007/10/03)
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