Salts of pyrrolopyrimidinone derivatives and process for...

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01)

Patent

CA 2666696

The present invention relates to salts of a pyrrolopyrimidinone derivative having superior PDE-5 inhibition activity and a process for preparing the same. More particularly, the present invention relates to a crystalline acid addition salt prepared by reacting a pyrrolopyrimidinone derivative with an acid selected from gentisic acid, maleic acid, citric acid, fumaric acid and tartaric acid. With no hygroscopic property and superior long-term storage stability, photostability and thermal stability, the salts of the pyrrolopyrimidinone derivative are appropriate to be prepared into medications and, with superior PDE-5 inhibition activity, are useful for the treatment and prevention of erectile dysfunction, pulmonary arterial hypertension, chronic obstructive pulmonary disease, benign prostatic hypertrophy and lower urinary tract diseases.

Sels d'un dérivé de pyrrolopyrimidinone présentant une activité supérieure d'inhibition de PDE-5 et leur méthode d'obtention. L'invention concerne plus particulièrement un sel d'addition d'acide cristallin obtenu par réaction d'un dérivé de pyrrolopyrimidinone avec un acide pris dans le groupe suivant: acide gentisique, acide maléique, acide citrique, acide fumarique et acide tartarique. Exempts de propriété hygroscopique, mais supérieurs en terme de capacité de stockage à long terme, de photostabilité et de stabilité thermique, les sels de dérivés de pyrrolopyrimidinone peuvent êtres utilisés dans des préparations médicales et, compte tenu de leur activité inhibitrice supérieure de PDE-5, conviennent pour le traitement et la prévention du dysfonctionnement érectile, de l'hypertension artérielle, de la maladie pulmonaire obstructive chronique, de l'hypertrophie bénigne de la prostate et des affections des voies urinaires inférieures.

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