Camptothecin-skeleton compounds isolated from Mappia foetida and the use
thereof as syntones for novel medicaments as well as therapeutical
agents
    2.
    发明授权
    Camptothecin-skeleton compounds isolated from Mappia foetida and the use thereof as syntones for novel medicaments as well as therapeutical agents 失效
    从益母草中分离的喜树碱骨架化合物及其作为新药物的合成物以及治疗剂

    公开(公告)号:US6121277A

    公开(公告)日:2000-09-19

    申请号:US155960

    申请日:1998-10-06

    CPC分类号: C07D471/14

    摘要: The present invention relates to camptothecin-skeleton alkaloids isolated from Mappia foetida or obtained by semi-synthesis from said alkaloids.Mappia foetida, a plant growing in the Indian subcontinent, is known to contain in its various parts, mainly in the seeds, camptothecin, mappicine and foetidine I and II (EP-A-685481).The alkaloids of the invention have the following general formula: ##STR1## in which R is a hydrogen atom or a methoxy group; R.sub.1 is hydroxy, an OM group wherein M is an alkali cation, preferably sodium or potassium, a C.sub.1 -C.sub.6 alkoxy group, an optionally substituted phenoxy group, an amino, C.sub.1 -C.sub.6 monoalkylamino or C.sub.2 -C.sub.12 dialkylamino group in which the alkyl moiety is optionally substituted by amino groups, an arylamino group; R.sub.2 is a C.sub.1 -C.sub.6 alkyl group or a group of formula COR.sub.3 wherein R.sub.3 is alkyl C.sub.1 -C.sub.6 or optionally substituted phenyl or benzyl.

    摘要翻译: PCT No.PCT / EP97 / 02244 Sec。 371 1998年10月6日第 102(e)日期1998年10月6日PCT提交1997年5月2日PCT公布。 公开号WO97 / 43290 日期:1997年11月20日本发明涉及从益生菌中分离得到的喜树碱骨架生物碱,或通过从所述生物碱半合成得到的生物碱。 已知在印度次大陆生长的植物豌豆,其各个部分主要含有种子,喜树碱,地西泮和氟替丁I和II(EP-A-685481)。 本发明的生物碱具有以下通式:其中R为氢原子或甲氧基; R1是羟基,其中M是碱金属阳离子,优选钠或钾,一个C 1 -C 6烷氧基,任意取代的苯氧基,氨基,C 1 -C 6单烷基氨基或C 2 -C 12二烷基氨基的OM基团,其中烷基部分 任选被氨基取代,芳基氨基; R2是C1-C6烷基或式COR3的基团,其中R3是烷基C1-C6或任选取代的苯基或苄基。

    Process for the preparation of N-10 alpha-methoxyl-lumilysergol and
esters, thereof, and intermediates for their preparation
    3.
    发明授权
    Process for the preparation of N-10 alpha-methoxyl-lumilysergol and esters, thereof, and intermediates for their preparation 失效
    制备N-10α-甲氧基 - 亮片糊精及其酯及其制备方法

    公开(公告)号:US4980475A

    公开(公告)日:1990-12-25

    申请号:US716501

    申请日:1985-03-26

    IPC分类号: C07D457/02

    CPC分类号: C07D457/02

    摘要: Processes for the preparation of esters of N.sub.1 -methyl-10.alpha.-methoxylumilysergol are described, in which lysergol esters are subjected to N-methylation and subsequently to photochemical reaction with methanol/H.sub.2 SO.sub.4. The esters of N.sub.1 -methyl-10-methoxylumilysergol obtained in this way can then be saponified or converted directly into other esters.

    摘要翻译: 描述了制备N1-甲基-10α-甲氧基甘露醇的酯的方法,其中将莱赛尔酯进行N-甲基化,随后用甲醇/ H 2 SO 4进行光化学反应。 然后可以将以这种方式得到的N1-甲基-10-甲氧基甘露醇的酯类皂化或直接转化成其他酯。

    Extracts of Ginkgo biloba and their methods of preparation
    8.
    发明授权
    Extracts of Ginkgo biloba and their methods of preparation 失效
    银杏提取物及其制备方法

    公开(公告)号:US5637302A

    公开(公告)日:1997-06-10

    申请号:US445916

    申请日:1995-05-22

    CPC分类号: A61K36/16 A61K31/70

    摘要: A process is provided for producing a purified extract from Ginkgo biloba leaves by solvent extraction with selected solvents. In the process, a crude or partially purified extract is subjected to solvent extraction with a solvent comprising toluene and n-butanol. Pharmaceutical. compositions comprising dimeric flavones and/or polyphenols are also described.

    摘要翻译: 提供了通过溶剂萃取用选择的溶剂从银杏生产纯化提取物的方法。 在此过程中,将粗制或部分纯化的提取物用包含甲苯和正丁醇的溶剂进行溶剂萃取。 制药。 还描述了包含二聚黄酮和/或多酚的组合物。

    Bilobalide derivatives, their applications and formulations containing
them
    9.
    发明授权
    Bilobalide derivatives, their applications and formulations containing them 失效
    BILOBALIDE衍生物,其应用和包含它们的制剂

    公开(公告)号:US5202313A

    公开(公告)日:1993-04-13

    申请号:US651598

    申请日:1991-02-06

    摘要: Complexes between natural or synthetic phospholipids and bilobalide, a sesquiterpene extracted from the leaves of Gingko biloba, are disclosed, as well as the preparation thereof and their therapeutic application as antiinflammatory agents and as agents for the treatment of disorders associated with inflammatory or traumatic neuritic processes. These new compounds, which exhibit a different bioavailability compared with free bilobalide, are suitable for incorporation into pharmaceutical formulations for systemic and topical administration: the latter route has been found to be particularly useful for the treatment of common peripheral disorders associated with inflammatory or neurodystrophic alterations.

    摘要翻译: 公开了天然的或合成的磷脂和碧花苜蓿之间的复合物,从银杏叶提取的倍半萜,以及其制备方法及其作为抗炎剂的治疗应用以及用于治疗与炎性或创伤性神经突过程相关的病症 。 这些新的化合物与游离的碧绿苷相比表现出不同的生物利用度,适合于并入用于全身和局部给药的药物制剂中:后一种途径特别可用于治疗与炎性或神经营养不良变化相关的常见周围疾病 。