会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 8. 发明申请
    • ORAL FORMULATION OF KINASE INHIBITORS
    • 激素抑制剂口服制剂
    • WO2012006081A1
    • 2012-01-12
    • PCT/US2011/042162
    • 2011-06-28
    • PONIARD PHARMACEUTICALS, INC.CHEN, Andrew XianTSAI, Yali J.
    • CHEN, Andrew XianTSAI, Yali J.
    • A61K9/00
    • A61K9/107A61K31/435A61K31/5377C07D213/74
    • The invention is directed to formulations of bioactive compounds of limited water solubility, inhibitors of focal adhesion kinase (FAK) of the 2,4-diaminopyridine class, adapted for oral administration to patients. The formulations are self-emulsifying in the gastrointestinal tract of the patients, providing enhanced absorption and bioavailability of the bioactive compounds as dispersions or emulsions in an oil base. For example, esters of PEG-ylated glycerol can be used as the oil, in conjunction with surfactants such as lecithin and TEPG succinate and solubilizers such as PEG 400 to provide useful oral formulations for administration to patients having a malcondition wherein inhibition of FAK is medically indicated, such as cancer or arthritis.
    • 本发明涉及适于口服给患者的2,4-二氨基吡啶类的局限性水溶性生物活性化合物的制剂,2,4-二氨基吡啶类的粘着斑激酶(FAK)抑制剂。 制剂在患者的胃肠道中自乳化,提供生物活性化合物作为油基中的分散体或乳液的增强的吸收和生物利用度。 例如,可以使用PEG-取代的甘油的酯作为油,与表面活性剂如卵磷脂和TEPG琥珀酸酯以及增溶剂如PEG 400一起使用,以提供用于给予具有恶化条件的患者的有用的口服制剂,其中FAK的抑制是医学上 表明,如癌症或关节炎。