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    METHOD FOR PREDICTING AND MODELING ANTI-PSYCHOTIC ACTIVITY USING VIRTUAL SCREENING MODEL
    1.
    发明申请
    METHOD FOR PREDICTING AND MODELING ANTI-PSYCHOTIC ACTIVITY USING VIRTUAL SCREENING MODEL 审中-公开
    使用虚拟筛选模型预测和建模抗心理活动的方法

    公开(公告)号：US20130184462A1

    公开(公告)日：2013-07-18

    申请号：US13876658

    申请日：2011-09-30

    申请人： Santosh Kumar Srivastava ,  Feroz Khan ,  Shikha Gupta ,  Dharmendra K. Yadav ,  Vinay Kumar Khanna

    发明人： Santosh Kumar Srivastava ,  Feroz Khan ,  Shikha Gupta ,  Dharmendra K. Yadav ,  Vinay Kumar Khanna

    IPC分类号： G06F19/00

    CPC分类号： C07D459/00 ,  G16C20/30 ,  G16C20/50

    摘要： The present invention relates to the development of a virtual screening model for predicting antipsychotic activity using quantitative structure activity relationship (QSAR), molecular docking, oral bioavailability, ADME and Toxicity studies. The present invention also relates to the development of QSAR model using forward stepwise method of multiple linear regression with leave-one-out validation approach. QSAR model showed activity-descriptors relationship correlating measure (r2) 0.87 (87%) and predictive accuracy of 81% (rCV2=0.81). The present invention specifically showed strong binding affinity of the untested (unknown) novel compounds against anti-psychotic targets viz., Dopamine D2 and Serotonin (5HT2A) receptors through molecular docking approach. Theoretical results were in accord with the in vitro and in vivo experimental data. The present invention further showed compliance of Lipinski's rule of five for oral bioavailability and toxicity risk assessment for all the active Yohimbine derivatives. Therefore, use of developed virtual screening model will definitely facilitate the screening of more effective antipsychotic leads/drugs with improved antipsychotic activity and also reduced the drug discovery cost and duration.

    摘要翻译： 本发明涉及使用定量结构活性关系（QSAR），分子对接，口服生物利用度，ADME和毒性研究来预测抗精神病活性的虚拟筛选模型。 本发明还涉及使用多元线性回归的前向逐步方法与离开一个验证方法开发QSAR模型。 QSAR模型显示活动描述符关系相关度（r2）0.87（87％）和预测精度81％（rCV2 = 0.81）。 本发明通过分子对接方法具体显示未测试（未知）新化合物对抗精神病性靶标即多巴胺D2和5-羟色胺（5HT2A）受体的强结合亲和力。 理论结果符合体外和体内实验数据。 本发明进一步显示了所有活跃的育亨宾衍生物的Lipinski的五条规则符合口服生物利用度和毒性风险评估。 因此，使用开发的虚拟筛选模型肯定会有助于筛选更有效的抗精神病药物，抗精神病药物活性更好，降低药物发现成本和持续时间。

    ANTIPSYCHOTIC AGENTS AND STANDARDIZED ANTIPSYCHOTIC FRACTIONS FROM RAUWOLFIA TETRAPHYLLA AND PROCESS OF THEIR ISOLATION
    3.
    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）。

    Automated downloading from mainframe to local area network
    5.
    发明授权
    Automated downloading from mainframe to local area network 有权
    从主机自动下载到局域网

    公开(公告)号：US07797334B2

    公开(公告)日：2010-09-14

    申请号：US11614072

    申请日：2006-12-20

    申请人： Santosh Kumar Srivastava ,  Sathish Babu Namasivayam ,  Mahipal Pukhraj Jain

    发明人： Santosh Kumar Srivastava ,  Sathish Babu Namasivayam ,  Mahipal Pukhraj Jain

    IPC分类号： G06F17/30 ,  G06F7/00

    CPC分类号： H04L67/06 ,  Y10S707/959 ,  Y10S707/966

    摘要： A tool can automate the process of downloading from a mainframe to a local area network (LAN). A back-end tool and a front-end tool can cooperate to accomplish the downloading process. Both tools can simplify the download process, avoiding complications and common errors. A user interface can provide features for simplifying the download process. Files can be downloaded from separate sub-areas on the mainframe to respective separate sub-areas on the LAN. Download settings can be saved and later retrieved via a name. Downloading for multiple software projects can be supported.

    摘要翻译： 一个工具可以自动执行从大型机到局域网（LAN）的下载过程。 后端工具和前端工具可以协作完成下载过程。 这两种工具都可以简化下载过程，避免并发症和常见错误。 用户界面可以提供简化下载过程的功能。 文件可以从主机上的单独子区域下载到LAN上的各个子区域。 下载设置可以保存，稍后通过名称进行检索。 可以支持多个软件项目的下载。

    Process for isolation of hepatoprotective agent “oleanolic acid” from Lantana camera
    9.
    发明授权
    Process for isolation of hepatoprotective agent “oleanolic acid” from Lantana camera 失效
    从Lantana相机中分离肝保护剂“齐墩果酸”的方法

    公开(公告)号：US06884908B2

    公开(公告)日：2005-04-26

    申请号：US10815095

    申请日：2004-03-30

    申请人： Santosh Kumar Srivastava ,  Merajuddin Khan ,  Suman Preet Singh Khanuja

    发明人： Santosh Kumar Srivastava ,  Merajuddin Khan ,  Suman Preet Singh Khanuja

    IPC分类号： C11B1/04 ,  C11B1/10 ,  C11B3/00 ,  C11B7/00 ,  C07C61/12

    CPC分类号： C11B3/006 ,  C11B1/04 ,  C11B1/10 ,  C11B7/0025 ,  C11B7/0075

    摘要： Accordingly the present invention provides an improved and economical process for the isolation of oleanolic acid from the roots of Lantana camara, which comprises of drying, grinding and defattening of Lantana camara roots with light petroleum followed by over night extractions at room temperature (30-40° C.) three times with a single solvent selected from CH2Cl2, CHCl3, EtOAc, ether, acetone, MeOH, EtOH etc., removal of solvent under vacuum at 35-45° C., precipitation of crude extract and repeated partial crystallization of precipitate with a single solvent selected from CH2Cl2, CHCl3, EtOAc, ether, acetone, MeOH, EtOH, H2O and others resulting in the isolation of oleanolic acid with 1% yield.

    摘要翻译： 因此，本发明提供了一种用于从马齿苋根中分离齐墩果酸的改进和经济的方法，其包括用轻质石油干燥，研磨和降解马缨丹的根，然后在室温下过夜（30-40℃） ℃，使用选自CH 2 Cl 2，CHCl 3 3，EtOAc，乙醚，丙酮，MeOH，EtOH的单一溶剂三次 等等，在35-45℃下真空除去溶剂，沉淀粗提取物并用选自CH 2 Cl 2的单一溶剂重结晶沉淀物， CHCl 3 3，EtOAc，乙醚，丙酮，MeOH，EtOH，H 2 O 2等，其结果以1％产率分离齐墩果酸。