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    ANTIPSYCHOTIC AGENTS AND STANDARDIZED ANTIPSYCHOTIC FRACTIONS FROM RAUWOLFIA TETRAPHYLLA AND PROCESS OF THEIR ISOLATION
    13.
    发明申请
    ANTIPSYCHOTIC AGENTS AND STANDARDIZED ANTIPSYCHOTIC FRACTIONS FROM RAUWOLFIA TETRAPHYLLA AND PROCESS OF THEIR ISOLATION 有权
    来自RAUWOLFIA TETRAPHYLLA的抗菌药物和标准化抗肿瘤药物及其分离方法

    公开(公告)号：US20120184576A1

    公开(公告)日：2012-07-19

    申请号：US13262040

    申请日：2010-03-31

    申请人： Santosh Kumar Srivastava ,  Ashok Kumar Agrawal ,  Subhash Chandra Singh ,  Vinay Kumar Khanna ,  Janardan Singh ,  Chandeshwar Nath ,  Madan Mohan Gupta ,  Shikha Gupta ,  Ram Kishor Verma ,  Anirban Pal ,  Duyaneshwar Umrao Bawankule ,  Dharmendra Saikia ,  Anil Kumar Gupta ,  Anupam Maurya ,  Suman Preet Singh Khanuja

    发明人： Santosh Kumar Srivastava ,  Ashok Kumar Agrawal ,  Subhash Chandra Singh ,  Vinay Kumar Khanna ,  Janardan Singh ,  Chandeshwar Nath ,  Madan Mohan Gupta ,  Shikha Gupta ,  Ram Kishor Verma ,  Anirban Pal ,  Duyaneshwar Umrao Bawankule ,  Dharmendra Saikia ,  Anil Kumar Gupta ,  Anupam Maurya ,  Suman Preet Singh Khanuja

    IPC分类号： A61K31/4375 ,  C07D455/00 ,  A61P25/18 ,  A61K31/475

    CPC分类号： A61K36/24

    摘要： The present invention relates to bioactive extracts its fractions and isolation of compound from Rauwolfia tetraphylla. The extracts and fractions are useful for the treatment of psychosis based on in-vivo validation on animal model and proportional binding affinities for dopaminergic-D2, Cholinergic (muscarinic) and Serotonergic (5HT2A) receptors for antipsychotic activity. The present invention relates to novel antipsychotic activity in the leaf alkaloids of Formula 1 and 2 named tetrahydroalstonine, 10-methoxytetrahydroalstonine, isoreserpiline, 10-derαethoxyreserpiline, 11-demethoxyreserpiline, reserpiline and α-yohimbine. The present invention also relates to processes for obtaining antipsychotic extracts as well as for the isolation of alkabids of formula 1 and 2 from the leaves of Rauwolfia tetraphylla. The present invention particularly relates to significant antipsychotic activity in the MeOH extract, ethylacetate and chloroform fractions of R. tetraphylla and in the isolated compounds α-yohimbine, reserpiline and in a mixture 10-demethoxyreserpiline and 11-demethoxyreserpiline in 1:1.5 ratios for treating psychosis without any extra pyramidal symptoms (EPS). 1. R1=R2=OMe R3=β-H (Isoreserpiline) 2. R1=R2=OMe R3=β-H (Reserpiline) ″3. R1=OMe R2=HR3=β-H (11-Demethoxy reserpiline) ″4.R1=H R2=OMe R3=β-H (10-Demethoxy reserpiline) ″5. R1=R2=H R3=α-H (Tetrahydroalstonine) *7. R1=OMe R2=H R3=α-H (10-Methoxytetrahudroalstonine).

    摘要翻译： 本发明涉及生物活性提取物，其部分和化合物从萝卜（Rauwolfia tetraphylla）分离。 基于动物模型的体内验证和针对抗精神病活性的多巴胺能D2，胆碱能（毒蕈碱）和血清素能（5HT2A）受体的比例结合亲和力，提取物和级分可用于治疗精神病。 本发明涉及式1和2的叶生物碱中的新型抗精神病活性，命名为四氢奥斯汀，10-甲氧基四氢奥斯汀，异丙基苯胺，10-脱乙氧基去甲苯胺，11-去甲氧基甲苯吡胺，储存蛋白和α-育亨宾。 本发明还涉及获得抗精神病药提取物以及分离来自罗非草（Rauwolfia tetraphylla）的叶子的式1和2的烷烃的方法。 本发明特别涉及在四氢叶酸甲酯的MeOH提取物，乙酸乙酯和氯仿级分中以及在分离的化合物α-育亨宾，储存器中和以1:1.5比例混合的10-脱甲氧基对苯二胺和11-脱甲氧基苯甲苯胺中的显着的抗精神病活性，用于治疗 精神病没有任何额外的锥体症状（EPS）。 R1 = R2 = OMe R3 =＆bgr; -H（Isoreserpiline）2.R1 = R2 = OMe R3 =＆bgr; -H（Reserpiline）“3。 R1 = OMe R2 = HR3 =＆bgr; -H（11-甲氧基乙酰胺）“4.R1 = H R2 = OMe R3 =＆bgr; -H（10-甲氧基乙胺） R1 = R2 = H R3 =α-H（四氢奥斯汀）* 7。 R1 = OMe R2 = H R3 =α-H（10-甲氧基四胡司汀）。

    Process for the isolation of compound scopoletin useful as nitric oxide synthesis inhibitor
    17.
    发明授权
    Process for the isolation of compound scopoletin useful as nitric oxide synthesis inhibitor 失效
    用于分离化合物scopoletin的方法可用作一氧化氮合成抑制剂

    公开(公告)号：US06337095B1

    公开(公告)日：2002-01-08

    申请号：US09538893

    申请日：2000-03-30

    申请人： Dharam Chand Jain ,  Neerja Pant ,  Madan Mohan Gupta ,  Rajendra Singh Bhakuni ,  Ram Kishor Verma ,  Sudeep Tandon ,  Shiv Kumar Gupta ,  Amit Tewari ,  Atul Prakash Kahol ,  Sushil Kumar

    发明人： Dharam Chand Jain ,  Neerja Pant ,  Madan Mohan Gupta ,  Rajendra Singh Bhakuni ,  Ram Kishor Verma ,  Sudeep Tandon ,  Shiv Kumar Gupta ,  Amit Tewari ,  Atul Prakash Kahol ,  Sushil Kumar

    IPC分类号： A01N6500

    CPC分类号： C07D311/16

    摘要： The invention relates to a process for the isolation of compound scopoletin which is used as nitric oxide synthesis inhibitor from Artemisia annua and other plant families, said process comprising extraction of dried powdered material of different plant parts with an aqueous acetonitrite solvent in the ratio of 1:5 for 6 to 8 hrs., concentration of the extracted solvent upto 30% of its original extract under vacuum, partitioning the concentrated extract with halogenated solvent to transfer scopoletin in the non-polar halogenated solvent, drying halogenated solvent over anhydrous sodium sulphate and evaporating the solvent, crystallizing the residues in methanol and filtering the crystals, concentrating the filtrate and chromatographed on silica gel, eluting scopoletin in chloroform methanol mixture; and crystallization of the fractions containing the scopoletin to get the pure scopoletin compound.

    摘要翻译： 本发明涉及一种用于分离化合物番茄酱的方法，其用作来自青蒿和其他植物家族的一氧化氮合成抑制剂，所述方法包括用比例为1的丙酮酸溶剂萃取不同植物部分的干燥粉末材料 5℃6〜8小时，真空浓缩提取溶剂至30％原始萃取液，用卤代溶剂分配浓缩萃取液，在非极性卤代溶剂中转移香料，用无水硫酸钠干燥卤代溶剂， 蒸发溶剂，结晶甲醇残余物并过滤晶体，浓缩滤液并在硅胶上进行色谱分离，用氯仿甲醇混合物洗脱; 并将含有scopoletin的级分结晶，得到纯的scopoletin化合物。

    Process for the preparation of a extract rich in bacosides from the herb Bacopa monniera
    18.
    发明授权
    Process for the preparation of a extract rich in bacosides from the herb Bacopa monniera 失效
    从草药Bacopa monniera制备富含芽孢杆菌的提取物的方法

    公开(公告)号：US06833143B1

    公开(公告)日：2004-12-21

    申请号：US10400192

    申请日：2003-03-26

    申请人： Atul Prakash Kahol ,  Tarun Singh ,  Sudeep Tandon ,  Madan Mohan Gupta ,  Suman Preet Singh Khanuja

    发明人： Atul Prakash Kahol ,  Tarun Singh ,  Sudeep Tandon ,  Madan Mohan Gupta ,  Suman Preet Singh Khanuja

    IPC分类号： A61K3578

    CPC分类号： A61K36/80

    摘要： The present invention provides a novel process for the preparation of bacosides enriched fraction in a non-hygroscopic form the extract of Bacopa monniera, the said process comprising the steps of drying freshly harvested herb in a hot air oven at 37-42° C., powdering and sieving the dried herb to obtain powder of 30-40 mesh size, defatting the powdered herb with hexane in a modified soxhlet extractor, extracting the defatted powdered herb with acetone, again extracting the same herb with methanol to obtain an extract containing bacosides, concentrating the extract to one twentieth of its original volume under reduced pressure, gradually adding the concentrated extract to acetone for precipitating the bacosides, filtering the bacosides in a Nutsche type vacuum filter, dissolving the crude bacoside mass into 2-10 parts water, extracting the bacoside solution with n-butanol to selectively transfer the bacosides to the solvent phase, separating and concentrating the solvent phase under vacuum to obtain semi-dry mass, dissolving the semi dried mass into 2-10 parts water, adding and stirring 1-5% of &bgr;-cyclodextrin to stabilize the bacosides, spray drying the stabilized bacoside solution by maintaining hot air temperature at 90-110° C., to obtain a stable free flowing fraction of Bacopa monniera rich in bacosides.

    摘要翻译： 本发明提供了一种用于制备以非吸湿形式的Bacopa monniera提取物富集杆菌的部分的新方法，所述方法包括以下步骤：在37-42℃的热空气烘箱中干燥新鲜收获的草本植物， 粉碎和筛分干草，得到30-40目尺寸的粉末，用改性索氏提取器用己烷脱脂粉末，用丙酮提取脱脂粉末草药，再次用甲醇提取相同的草本，得到含有药剂的提取物， 将提取物在减压下浓缩至其原始体积的二十分之一，逐渐将浓缩提取物加入到丙酮中沉淀芽孢杆菌，过滤Nutsche型真空过滤器中的芽孢杆菌，将粗制药物块溶解在2-10份水中， 使用正丁醇选择性转移杆菌苷至溶剂相，分离和浓缩溶剂相 获得半干质量，将半干质量溶解在2-10份水中，加入并搅拌1-5％的β-环糊精以稳定芽孢杆菌，通过将热空气温度保持在90℃喷雾干燥稳定的bacoside溶液， 110℃，以获得富含芽孢杆菌的Bacopa monniera的稳定的自由流动分数。