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    • 3. 发明申请
    • CAMPHANYLIDENE AND PHENYLALKYL INOSITOL POLYPHOSPHATE COMPOUNDS, COMPOSITIONS, AND METHODS OF THEIR USE
    • 邻苯二甲酸和苯乙烯磺酰胺多磷酸酯化合物,组合物及其使用方法
    • WO2004087721A1
    • 2004-10-14
    • PCT/US2004/009088
    • 2004-03-25
    • INOLOGIC, INC.TRAYNOR-KAPLAN, Alexis, E.
    • TRAYNOR-KAPLAN, Alexis, E.
    • C07F9/117
    • C07F9/093A61K31/6615C07F9/117C07F9/65517
    • This invention relates to new camphanylidene and phenyl alkyl inositol polyphosphate derivatives that inhibit the absorption of sodium ions in epithelial cells and regulate inducible nitric oxide synthase (iNOS) in macrophages. The invention provides methods for inhibiting sodium ion absorption by epithelial cells and/or regulating inducible nitric oxide synthase (iNOS) in macrophages, by treating epithelial cells or administering to a patient in need of such treatment a therapeutically effective amount of camphanylidene and/or phenyl alkyl inositol polyphosphate compound. Representative camphanylidene and phenyl alkyl inositol polyphosphate compounds include, for example, 1,2-camphanylidene- myo -inositol 3,4,5,6-tetrakisphosphate octakis (propionoxymethyl) ester (INO-4996), 2,3-camphanylidene- myo -inositol 1,4,5,6­-tetrakisphosphate octakis (propionoxymethyl) ester (INO-4984) and 2- O -butyryl-1- O -(3-­phenylpropyl)- myo -inositol 3,4,5,6-tetrakisphosphate octakis (propionoxymethyl) ester (INO-4997).
    • 本发明涉及抑制上皮细胞中钠离子吸收并调节巨噬细胞诱导型一氧化氮合酶(iNOS)的新型亚烷基和苯基烷基肌醇多磷酸酯衍生物。 本发明提供了抑制上皮细胞的钠离子吸收和/或调节巨噬细胞中的诱导型一氧化氮合酶(iNOS)的方法,通过治疗上皮细胞或向需要这种治疗的患者施用治疗有效量的亚芳基和/或苯基 烷基肌醇多磷酸盐化合物。 代表性的亚正辛基和苯基烷基肌醇多磷酸酯化合物包括例如,1,2-亚辛基 - 肌醇3,4,5,6-四磷酸八辛酯(丙酰氧基甲基)酯(INO-4996),2,3-月桂酰基肌醇 肌醇1,4,5,6-四磷酸八钠(丙酰氧甲基)酯(INO-4984)和2-O-丁酰基-1-O-(3-苯基丙基) - 肌醇3,4,5,6-四磷酸八钠 (丙酰氧基甲基)酯(INO-4997)。