公开(公告)号：US20100069632A1

公开(公告)日：2010-03-18

申请号：US12307144

申请日：2007-07-03

申请人： Nam Ho Kim ,  Jin-Young Lee ,  Jae-Sun Kim ,  Nam Kyu Lee ,  Woo Jae Jang ,  Joo Gyo Oh ,  Yoon-Jung Lee ,  Won-No Youn ,  Jin-Heung Sung ,  Key An Um

发明人： Nam Ho Kim ,  Jin-Young Lee ,  Jae-Sun Kim ,  Nam Kyu Lee ,  Woo Jae Jang ,  Joo Gyo Oh ,  Yoon-Jung Lee ,  Won-No Youn ,  Jin-Heung Sung ,  Key An Um

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： 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.

摘要翻译： 本发明涉及具有优异的PDE-5抑制活性的吡咯并嘧啶酮衍生物的盐及其制备方法。 更具体地，本发明涉及通过使吡咯并嘧啶酮衍生物与选自龙胆酸，马来酸，柠檬酸，富马酸和酒石酸的酸反应制备的结晶酸加成盐。 无吸湿性和优异的长期储存稳定性，光稳定性和热稳定性，吡咯并嘧啶酮衍生物的盐适于制备成药物，并且具有优异的PDE-5抑制活性，可用于治疗和预防勃起功能障碍 肺动脉高压，慢性阻塞性肺疾病，良性前列腺肥大和下尿路疾病。