[EN] CAMPHANYLIDENE AND PHENYLALKYL INOSITOL POLYPHOSPHATE COMPOUNDS, COMPOSITIONS, AND METHODS OF THEIR USE<br/>[FR] COMPOSES DE CAMPHANYLIDENE ET POLYPHOSPHATES D'INOSITOL PHENYLALKYLE, COMPOSITIONS ET LEURS PROCEDES D'UTILISATION
申请人:INOLOGIC INC
公开号:WO2004087721A1
公开(公告)日:2004-10-14
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).
这项发明涉及新的松节醇亚烯基和苯基烷基肌醇多磷酸衍生物,能够抑制上皮细胞中钠离子的吸收并调节巨噬细胞中的诱导型一氧化氮合酶(iNOS)。该发明提供了通过治疗上皮细胞或向需要此类治疗的患者施用松节醇亚烯基和/或苯基烷基肌醇多磷酸化合物的治疗方法,以抑制上皮细胞中的钠离子吸收和/或调节巨噬细胞中的诱导型一氧化氮合酶(iNOS)。代表性的松节醇亚烯基和苯基烷基肌醇多磷酸化合物包括,例如,1,2-松节醇亚烯基-肌醇3,4,5,6-四磷酸八(丙酰氧甲基)酯(INO-4996)、2,3-松节醇亚烯基-肌醇1,4,5,6-四磷酸八(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(丙酰氧甲基)酯(INO-4997)。