SALTS OF PYRROLOPYRIMIDINONE DERIVATIVES AND PROCESS FOR PREPARING THE SAME
    2.
    发明申请
    SALTS OF PYRROLOPYRIMIDINONE DERIVATIVES AND PROCESS FOR PREPARING THE SAME 审中-公开
    吡咯烷酮衍生物的制备方法及其制备方法

    公开(公告)号:US20100069632A1

    公开(公告)日:2010-03-18

    申请号:US12307144

    申请日:2007-07-03

    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。

    LYOPHILIZED PHARMACEUTICAL COMPOSITION WITH IMPROVED RECONSTITUTION TIME CONTAINING TAXANE DERIVATIVES AND METHOD OF MANUFACTURING THE SAME
    8.
    发明申请
    LYOPHILIZED PHARMACEUTICAL COMPOSITION WITH IMPROVED RECONSTITUTION TIME CONTAINING TAXANE DERIVATIVES AND METHOD OF MANUFACTURING THE SAME 审中-公开
    具有改进的包含TAXANE衍生物的重新构建时间的LYOPHILIZED药物组合物及其制备方法

    公开(公告)号:US20100267817A1

    公开(公告)日:2010-10-21

    申请号:US12744151

    申请日:2008-11-21

    IPC分类号: A61K31/337 A61P43/00

    CPC分类号: A61K9/19 A61K47/26 A61K47/32

    摘要: The present invention relates to a lyophilized composition with an improved reconstitution time comprising a taxoid and a method thereof. More specifically, the present invention relates to a lyophilized composition with an improved reconstitution time prepared by mixing and dissolving a taxoid; cyclodextrin (CD); a hydrophilic polymer selected from the group consisting of hydroxypropylmethyl CeIIuIoSe (HPMC), polyethylene glycol (PEG), and polyvinylpyrrolidone (PVP); and a bulking agent of saccharides in water for injection; and lyophilizing the mixture, and a method thereof.

    摘要翻译: 本发明涉及具有改进的重构时间的冻干组合物,其包含紫杉烷及其方法。 更具体地,本发明涉及通过混合和溶解紫杉烷制备的具有改进的重构时间的冻干组合物; 环糊精(CD); 选自羟丙基甲基CeIIuIoSe(HPMC),聚乙二醇(PEG)和聚乙烯吡咯烷酮(PVP)的亲水性聚合物; 和糖类在注射用水中的填充剂; 并将混合物冻干,及其方法。