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    • 6. 发明授权
    • Dietary and pharmaceutical compositions containing tricyclic diterpenes and their derivates and their uses
    • 含三环二萜及其衍生物及其用途的膳食和药物组合物
    • US08552055B2
    • 2013-10-08
    • US12654596
    • 2009-12-23
    • Antoine De SaizieuAnn FowlerRegina GoralczykClaus KilpertGoede SchuelerChristof Wehrli
    • Antoine De SaizieuAnn FowlerRegina GoralczykClaus KilpertGoede SchuelerChristof Wehrli
    • A01N43/02A01N37/10A61K31/235A61K31/19
    • A61K31/192A23K20/105A23K50/40A23L33/10A23L33/105A23V2002/00A61K31/085A61K31/122A61K31/19A61K31/365A23V2200/322A23V2250/21
    • The present invention refers to tricyclic diterpenes and their derivatives of the formulae (I) and (II), wherein R1 is hydrogen or C1-6-alkyl; R2 is hydroxy, C3-5-acyloxy, hydroxymethyl, 1,3-dihydroxypropyl or C1-6-alkyl; R3 and R4 independently from each other are hydrogen, hydroxy, hydroxymethyl, C1-5-acyloxy or C1-6-alkoxy; R5 is C1-6-alkyl, hydroxymethyl carboxy or methoxycarbonyl; R9 is hydrogen, hydroxymethyl, methoxy, oxo or C1-5-acyloxy; R10 is hydrogen, or R5 and R9 taken together are —CH2—O— or —O—CH2—; or R5 and R10 taken together are —CO—O—, —O—CO—, —CH2—O— or —O—CH2—; R6 is hydrogen, or R5 and R6 together form a bond; R7 and R8 independently from each other are C1-6-alkyl, carboxy, x-hydroxy-Cx-alkyl (with x being an integer from 1 to 6), or C1-6-alkoxycarbonyl with the proviso that at least one of R7 and R8 is C1-6-alkyl; R11 and R12 are both hydrogen or R11 and R12 together are oxo, with the further proviso for formula (I) that if R2 is hydroxy R1 is C1-6-alkyl, for use as medicaments for the treatment of a disorder connected to impaired neurotransmission, as well as to dietary and pharmaceutical compositions and their uses.
    • 本发明涉及式(I)和(II)的三环二萜及其衍生物,其中R 1是氢或C 1-6 - 烷基; R2是羟基,C3-5-酰氧基,羟甲基,1,3-二羟基丙基或C1-6烷基; R 3和R 4彼此独立地是氢,羟基,羟甲基,C 1-5 - 酰氧基或C 1-6 - 烷氧基; R5是C1-6烷基,羟甲基羧基或甲氧基羰基; R9是氢,羟甲基,甲氧基,氧代或C1-5-酰氧基; R 10是氢,或者R 5和R 9一起是-CH 2 -O-或-O-CH 2 - ; 或R 5和R 10一起是-CO-O-,-O-CO-,-CH2-O-或-O-CH2-; R6是氢,或R5和R6一起形成键; R 7和R 8彼此独立地是C 1-6 - 烷基,羧基,x-羟基-C 1-6 - 烷基(x是1至6的整数)或C 1-6 - 烷氧基羰基,条件是R 7 并且R 8是C 1-6 - 烷基; R 11和R 12都是氢或R 11和R 12一起是氧代,进一步的条件是式(I),如果R 2是羟基,则R 1是C 1-6 - 烷基,用作治疗与神经传递受损有关的病症的药物 ,以及饮食和药物组合物及其用途。