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    DISODIUM SALTS, MONOHYDRATES, AND ETHANOL SOLVATES
    3.
    发明公开
    DISODIUM SALTS, MONOHYDRATES, AND ETHANOL SOLVATES 有权
    乙醇钠，乙醇钠，乙醇溶液

    公开(公告)号：EP1175390A4

    公开(公告)日：2002-09-04

    申请号：EP00921909

    申请日：2000-04-05

    申请人： EMISPHERE TECH INC

    发明人： BAY WILLIAM E ,  AGARWAL RAJESH K ,  CHAUDHARY KIRAN ,  MAJURU SHINGAI ,  GOLDBERG MICHAEL M ,  RUSSO JOANNE P

    IPC分类号： A61K47/16 ,  A61K9/08 ,  A61K9/20 ,  A61K9/48 ,  A61K38/22 ,  A61K47/12 ,  A61K47/18 ,  A61P3/14 ,  C07C231/00 ,  C07C231/12 ,  C07C235/58 ,  C07C235/60 ,  C07D265/26 ,  C07C229/00

    CPC分类号： C07C231/00 ,  A61K9/2013 ,  A61K47/183 ,  C07C235/60 ,  C07D265/26 ,  C07C235/58

    摘要： The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have formula (I) wherein R?1, R2, R3, and R4¿ are indepedently hydrogen, halogen, C¿1?-C4 alkyl, or C1-C4 alkoxy; and R?5¿ is a substituted or unsubstituted C¿2?-C16 alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of formula (I) above. Preferred delivery agents include, but are not limited to, N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC),N-(10-[2-hydroxybenzoyl]amino)decanoic acid (SNAD), and sodium N-(8-[2-hydroxybenzoyl]amino)caprylate (SNAC). The invention also provides methods of preparing the disodium salt, ethanol solvate, and hydrate and compositions containing the disodium salt, ethanol solvate, and/or hydrate.

    摘要翻译： 发明人已经发现，某些递送剂的二钠盐比相应的单钠盐具有令人惊奇的更大的递送活性剂的功效。 此外，本发明人已经发现，这些递送剂的二钠盐与乙醇形成溶剂合物并与水合。 递送剂具有下式：其中R 1，R 2，R 3和R 4独立地为氢，卤素，C 1 -C 4烷基或C 1 -C 4烷氧基; 取代或未取代的C 2 -C 16亚烯基，取代或未取代的C 1 -C 12烷基（亚芳基）或取代或未取代的芳基（C 1 -C 12亚烷基）。 本发明的水合物和溶剂合物对于递送活性剂（例如肝素和降钙素）比其相应的单钠盐和游离酸具有惊人的更大功效。 本发明提供一种醇溶剂合物，如乙醇溶剂化物，其具有上式的递送剂的二钠盐。 本发明还提供了上式的递送剂的二钠盐的水合物。 优选的递送剂包括但不限于N-（5-氯水杨酰基）-8-氨基辛酸（5-CNAC），N-（10- [2-羟基苯甲酰基]氨基）癸酸（SNAD）和N - （8- [2-羟基苯甲酰基]氨基）辛酸酯（SNAC）。 本发明还提供了制备二钠盐，乙醇溶剂化物和水合物的方法以及含有二钠盐，乙醇溶剂化物和/或水合物的组合物。