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1. 发明申请

WO2010113180A8 ANTIPSYCHOTIC AGENTS AND STANDARDIZED ANTIPSYCHOTIC FRACTIONS FROM RAUWOLFIA TETRAPHYLLA AND PROCESS OF THEIR ISOLATION 审中-公开
标题翻译：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：WO2010113180A8
公开(公告)日：2011-06-30
申请号：PCT/IN2010000208
申请日：2010-03-31
申请人： COUNCIL SCIENT IND RES , SRIVASTAVA SANTOSH KUMAR , AGRAWAL ASHOK KUMAR , SINGH SUBHASH CHANDRA , KHANNA VINAY KUMAR , SINGH JANARDAN , NATH CHANDESHWAR , GUPTA MADAN MOHAN , GUPTA SHIKHA , VERMA RAM KISHOR , PAL ANIRBAN , BAWANKULE DNYANESHWAR UMRAO , SAIKIA DHARMENDRA , GUPTA ANIL KUMAR , MAURYA ANUPAM , KHANUJA SUMAN PREET SINGH
发明人： SRIVASTAVA SANTOSH KUMAR , AGRAWAL ASHOK KUMAR , SINGH SUBHASH CHANDRA , KHANNA VINAY KUMAR , SINGH JANARDAN , NATH CHANDESHWAR , GUPTA MADAN MOHAN , GUPTA SHIKHA , VERMA RAM KISHOR , PAL ANIRBAN , BAWANKULE DNYANESHWAR UMRAO , SAIKIA DHARMENDRA , GUPTA ANIL KUMAR , MAURYA ANUPAM , KHANUJA SUMAN PREET SINGH
IPC分类号： A61K36/24 , A61P25/18
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- deraethoxyreserpiline, 11-demethoxyreserpiline, reserpiline and a -yohimbine. The present invention also relates to processes for obtaining antipsychotic extracts as well as for the isolation of alkaloids 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 a -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 = a-H (Isoreserpiline) ? 2. R1=R2 = OMe R3 = ß-H (Reserpiline) "3. R1 = OMe R2 = HR3 = ß-H (11-Demethoxy reserpiline) "4. R1 = H R2 = OMe R3 = ß-H (10-Demethoxy reserpiline) "5. R1 = R2 = H R3 = a -H (Tetrahydroalstonine) * 7. R1 = OMe R2 = H R3 = a -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，其命名为四氢奥斯汀，10-甲氧基四氢al嗪，异孢子甲苯胺，10-脱乙氧基去甲苯胺，11-脱甲氧基苯甲苯胺，保留剂和a-育宁。本发明还涉及获得抗精神病药提取物以及分离来自萝卜（Rauwolfia tetraphylla）的叶子的式1和2的生物碱的方法。本发明特别涉及在四氢叶酸的MeOH提取物，乙酸乙酯和氯仿级分中以及在分离的化合物a -yohimbine，储存器和以1:1.5比例混合的10-脱乙氧基去甲苯胺和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 = a-H（异间苯二胺） 2. R1 = R2 = OMe R3 =ß-H（Reserpiline）“3.R1 = OMe R2 = HR3 =ß-H（11-Demethoxy Reserpiline）”4。 R1 = H R2 = OMe R3 =ß-H（10-脱甲氧基甲苯胺）“5.R1 = R2 = H R3 = a-H（四氢奥斯汀）* 7.R1 = OMe R2 = H R3 = Methoxytetrahudroalstonine）。

2. 发明申请

WO2012042541A3 METHOD FOR PREDICTING AND MODELING ANTI-PSYCHOTIC ACTIVITY USING VIRTUAL SCREENING MODEL 审中-公开
标题翻译：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：WO2012042541A3
公开(公告)日：2012-11-29
申请号：PCT/IN2011000681
申请日：2011-09-30
申请人： COUNCIL SCIENT IND RES , SRIVASTAVA SANTOSH KUMAR , KHANNA VINAY KUMAR , GUPTA SHIKHA , KHAN FEROZ , YADAV DHARMENDRA K
发明人： SRIVASTAVA SANTOSH KUMAR , KHANNA VINAY KUMAR , GUPTA SHIKHA , KHAN FEROZ , YADAV DHARMENDRA K
IPC分类号： C07D459/00 , G06F19/00
CPC分类号： G06F19/704 , C07D459/00 , G06F19/706
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。

3. 发明专利

CA2757311A1 ANTIPSYCHOTIC AGENTS AND STANDARDIZED ANTIPSYCHOTIC FRACTIONS FROM RAUWOLFIA TETRAPHYLLA AND PROCESS OF THEIR ISOLATION 未知
公开(公告)号：CA2757311A1
公开(公告)日：2010-10-07
申请号：CA2757311
申请日：2010-03-31
申请人： COUNCIL SCIENT IND RES
发明人： SRIVASTAVA SANTOSH KUMAR , AGRAWAL ASHOK KUMAR , SINGH SUBHASH CHANDRA , KHANNA VINAY KUMAR , SINGH JANARDAN , NATH CHANDESHWAR , GUPTA MADAN MOHAN , GUPTA SHIKHA , VERMA RAM KISHOR , PAL ANIRBAN , BAWANKULE DNYANESHWAR UMRAO , SAIKIA DHARMENDRA , GUPTA ANIL KUMAR , MAURYA ANUPAM , KHANUJA SUMAN PREET SINGH , SRIVASTAVA SANTSH KUMAR
IPC分类号： A61K36/24 , A61P25/18
摘要： The present invention relates to bioactive extracts its fractions and isolation of compound from RauwolSa 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- deraethoxyreserpiline, 11-demethoxyreserpiline, reserpiline and a -yohimbine. The present invention also relates to processes for obtaining antipsychotic extracts as well as for the isolation of alkaloids 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 a -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 = a-H (Isoreserpiline) ? 2. R1=R2 = OMe R3 = ß-H (Reserpiline) "3. R1 = OMe R2 = HR3 = ß-H (11-Demethoxy reserpiline) "4. R1 = H R2 = OMe R3 = ß-H (10-Demethoxy reserpiline) "5. R1 = R2 = H R3 = a -H (Tetrahydroalstonine) * 7. R1 = OMe R2 = H R3 = a -H (10-Methoxytetrahudroalstonine)

4. 发明专利

AU2010231489B2 Antipsychotic agents and standardized antipsychotic fractions from Rauwolfia tetraphylla and process of their isolation 未知
$Antipsychotic agents and standardized antipsychotic fractions from Rauwolfia tetraphylla and process of their isolation$
公开(公告)号：AU2010231489B2
公开(公告)日：2014-01-16
申请号：AU2010231489
申请日：2010-03-31
申请人： COUNCIL SCIENT IND RES
发明人： SRIVASTAVA SANTOSH KUMAR , AGRAWAL ASHOK KUMAR , SINGH SUBHASH CHANDRA , KHANNA VINAY KUMAR , SINGH JANARDAN , NATH CHANDESHWAR , GUPTA MADAN MOHAN , GUPTA SHIKHA , VERMA RAM KISHOR , PAL ANIRBAN , BAWANKULE DNYANESHWAR UMRAO , SAIKIA DHARMENDRA , GUPTA ANIL KUMAR , MAURYA ANUPAM , KHANUJA SUMAN PREET SINGH
IPC分类号： A61K36/24 , A61P25/18
摘要： The present invention relates to bioactive extracts its fractions and isolation of compound from RauwolSa 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 - D

6. 发明专利

ES2225777T3 COMPOSICION FARMACEUTICA ANTIBIOTICA CON LISERGOL COMO POTENCIADOR BIOACTIVO Y METODO DE TRATAMIENTO. 未知
公开(公告)号：ES2225777T3
公开(公告)日：2005-03-16
申请号：ES02716990
申请日：2002-03-25
申请人： COUNCIL SCIENT IND RES
发明人： KHANUJA SUMAN PREET , ARYA JAI SHANKAR , SRIVASTAVA SANTOSH KUMAR , SHASANY AJIT KUMAR , KUMAR TIRUPPADIRIPULIYUR , DAROKAR MAHENDRA PANDURANG CEN
IPC分类号： A61K31/43 , A61K31/48 , A61K31/495 , A61K31/65 , A61P31/04
摘要： Una composición farmacéutica antibiótica sinérgica que tiene bioactividad potenciada en sujetos, comprendiendo la citada composición: (a) un compuesto antibiótico; (b) una cantidad eficaz de lisergol, 1-10 µg/ml; y (c) aditivos farmacéuticamente aceptables opcionales.

8. 发明专利

DE60324608D1 未知
公开(公告)号：DE60324608D1
公开(公告)日：2008-12-18
申请号：DE60324608
申请日：2003-03-31
申请人： COUNCIL SCIENT IND RES
发明人： KHANUJA SUMAN PREET SINGH , ARYA JAI SHANKER , TIRUPPADIRIPULIYUR RANGANATHAN , SAIKIA DHARMENDRA , KAUR HARPREET , SINGH MONIKA , GUPTA SUBHASH CHANDRA , SHASANY AJIT KUMAR , DAROKAR MAHENDRA PANDURANG , SRIVASTAVA SANTOSH KUMAR , GUPTA MADAN MOHAN , VERMA SUBASH CHANDRA , PAL ANIRBAN
IPC分类号： C07H15/00

9. 发明专利

GB2438552A Ethanolic extracts of Everniastrum Cirrhatum for use in the treatment of fungal infections 未知
公开(公告)号：GB2438552A
公开(公告)日：2007-11-28
申请号：GB0716892
申请日：2003-03-31
申请人： COUNCIL SCIENT IND RES
发明人： KHANUJA SUMAN PREET SINGH , TIRUPPADIRIPULIYUR RANGANATHAN , GUPTA VIVEK KUMAR , CHAND PREETI , GARG ANKUR , SRIVASTAVA SANTOSH KUMAR , VERMA SUBASH CHANDRA , SAIKIA DHARMENDRA , DAROKAR MAHENDRA PANDURANG , SHASANY AJIT KUMAR , PAL ANIRBAN
IPC分类号： A61K36/09 , A61K31/235 , A61P31/10
摘要： Ethanolic extracts of Everniastrum Cirrhatum comprising methyl-I-orcinol carboxylate of formula (1) may be useful for treating pathogenic fungal infections (in humans) that are resistant to polyene and azole antibiotics such as amphotericin B, nystatin, clotrimazole etc. The methyl-B-orcinol is optionally present in a concentration in a range of 10 to 400 pg/ml. The ethanolic extract may subsequently be extracted using hexane and ethyl acetate with the use of these extract for treating pathogenic fungal infections.

10. 发明专利

DE60201022T2 未知
公开(公告)号：DE60201022T2
公开(公告)日：2005-08-18
申请号：DE60201022
申请日：2002-03-25
申请人： COUNCIL SCIENT IND RES
发明人： KHANUJA SUMAN PREET SINGH , ARYA JAI SHANKAR , SRIVASTAVA SANTOSH KUMAR , SHASANY AJIT KUMAR , KUMAR TIRUPPADIRIPULIYUR R , DAROKAR MAHENDRA PANDURANG , KUMAR SUSHIL
IPC分类号： A61K31/43 , A61K31/48 , A61K31/495 , A61K31/65 , A61P31/04

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