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    Dietary and pharmaceutical compositions containing tricyclic diterpenes and their derivatives and their uses
    1.
    发明授权
    Dietary and pharmaceutical compositions containing tricyclic diterpenes and their derivatives and their uses 失效
    包含三环二萜及其衍生物及其用途的膳食和药物组合物

    公开(公告)号：US08748491B2

    公开(公告)日：2014-06-10

    申请号：US14016265

    申请日：2013-09-03

    Applicant: DSM IP Assets B.V.

    Inventor： Antione De Saizieu ,  Ann Fowler ,  Regina Goralczyk ,  Claus Kilpert ,  Goede Schueler ,  Christof Wehrli

    IPC: A61K31/19 ,  A61K31/335 ,  A01N43/02 ,  A01N37/10 ,  A61K31/192

    CPC classification number: A61K31/192 ,  A23K20/105 ,  A23K50/40 ,  A23L33/10 ,  A23L33/105 ,  A23V2002/00 ,  A61K31/085 ,  A61K31/122 ,  A61K31/19 ,  A61K31/365 ,  A23V2200/322 ,  A23V2250/21

    Abstract: 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 to 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.

    Abstract translation: 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。

    DIETARY AND PHARMACEUTICAL COMPOSITIONS CONTAINING TRICYCLIC DITERPENES AND THEIR DERIVATIVES AND THEIR USES
    6.
    发明申请
    DIETARY AND PHARMACEUTICAL COMPOSITIONS CONTAINING TRICYCLIC DITERPENES AND THEIR DERIVATIVES AND THEIR USES 失效
    含有三聚磷酸酯及其衍生物及其用途的膳食和药物组合物

    公开(公告)号：US20140005270A1

    公开(公告)日：2014-01-02

    申请号：US14016265

    申请日：2013-09-03

    Applicant: DSM IP ASSETS B.V.

    Inventor： Antoine DE SAIZIEU ,  Ann Fowler ,  Regina Goralczyk ,  Claus Kilpert ,  Goede Schueler ,  Christof Wehrli

    IPC: A61K31/192 ,  A23L1/30

    CPC classification number: A61K31/192 ,  A23K20/105 ,  A23K50/40 ,  A23L33/10 ,  A23L33/105 ,  A23V2002/00 ,  A61K31/085 ,  A61K31/122 ,  A61K31/19 ,  A61K31/365 ,  A23V2200/322 ,  A23V2250/21

    Abstract: 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 to 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.

    Abstract translation: 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。

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