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    • 5. 发明申请
    • GUGGULPHOSPHOLIPID METHODS AND COMPOSITIONS
    • GUGGPHPHPHPHIPIPI方法和组合物
    • WO2008058156A2
    • 2008-05-15
    • PCT/US2007083832
    • 2007-11-06
    • JINA PHARMACEUTICALS INCAHMAD MOGHIS UALI SHOUKATH MAHMAD ATEEQSHEIKH SAIFUDDINAHMAD IMRAN
    • AHMAD MOGHIS UALI SHOUKATH MAHMAD ATEEQSHEIKH SAIFUDDINAHMAD IMRAN
    • A01N65/00
    • C07J13/007A61K31/337A61K47/554A61K47/6907A61K47/6911C07J7/0005C07J31/006C07J41/0005C07J41/0088C07J51/00C12N15/85
    • The present invention relates to the methods for preparing synthetic guggulphospholipids, their fatty acid analogues and other bioactive molecules. The present invention relates to E-guggulsterone and Z-guggulsterone or mixture of E- and Z-guggulsterones; and E-guggulsterol and Z-guggulsterol or mixture of E- and Z-guggulsterols synthetically modified to guggulphospholipids and analogues and salts thereof, fatty acid analogues of guggulsterols, guggulsulfate and salts thereof, guggulphosphate and salts thereof; and guggulsterols conjugated with drugs for use as prodrugs. Also the present invention provides a novel method for the preparation of E-guggulsterol and Z-guggulsterol or mixture of E-and Z-guggulsterols from a mixture of E- and Z-guggulsterones. The present invention further relates to guggulphospholipids and other bioactive molecules incorporated into complexes such as liposomes, complexes, emulsions, vesicles, micelles, and mixed micelles, which can include other active agents, such as hydrophobic or hydrophilic drugs for use, e.g., in treatment of human and animal diseases.
    • 本发明涉及制备合成瓜瓜磷脂,其脂肪酸类似物和其它生物活性分子的方法。 本发明涉及戊二酮和Z-鬼臼酮或E-和Z-格鲁酮的混合物; 合成修饰成瓜瓜尔斯醇和Z-guggulsterol或者合成修饰成瓜瓜尔斯醇及其类似物及其盐的瓜尔豆甾醇和Z-瓜格尔斯醇的混合物,瓜焦糖醇,巨硫酸盐及其盐的脂肪酸类似物,磷酸瓜瓜酯及其盐; 和与药物缀合的糖苷醇用作前药。 本发明还提供了一种从E-和Z-格鲁酮的混合物制备E-guggulsterol和Z-guggulsterol或E-和Z-苦瓜甾醇的混合物的新方法。 本发明还涉及结合到诸如脂质体,复合物,乳液,囊泡,胶束和混合胶束的复合物中的瓜瓜磷脂和其它生物活性分子,其可以包括其它活性剂,例如用于治疗的疏水或亲水药物 的人类和动物疾病。