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    METHOD FOR IN-VIVO BINDING OF CHROMATIN FRAGMENTS
    4.
    发明申请
    METHOD FOR IN-VIVO BINDING OF CHROMATIN FRAGMENTS 有权
    色氨酸片段的体内结合方法

    公开(公告)号：US20120301487A1

    公开(公告)日：2012-11-29

    申请号：US13575756

    申请日：2011-01-24

    申请人： Indraneel Mittra ,  Rekha Mannemcherril Ramesan ,  Chandra Prakash Sharma ,  Gopichettipalayam Subbaratnam Vaneshwar ,  Kavita Anirban Pal

    发明人： Indraneel Mittra ,  Rekha Mannemcherril Ramesan ,  Chandra Prakash Sharma ,  Gopichettipalayam Subbaratnam Vaneshwar ,  Kavita Anirban Pal

    IPC分类号： A61K39/395 ,  C07K16/18 ,  A61P29/00 ,  B82Y5/00

    CPC分类号： C07K16/18 ,  A61K47/61 ,  A61K47/6939 ,  A61K2039/505 ,  C07K16/08 ,  Y10T428/2982

    摘要： A process for substantially reducing levels of circulating chromatin fragments (CCFs) from a medium using binding agents such as antibodies or antibodies complexed with haemocompatible natural polymer substrates like as alginates, chitosan and pullulan to form complexed antibody-substrate nano-particulates (CNP) to bind and/or inactivate CCFs is disclosed. The amount of antibody bound to the polymer varies from 30% to 100% of activated sites in the polymer. Elevated levels of CCFs can be substantially reduced following administration of tissue damaging agents that generate apoptotic chromatin fragments by the concomitant administration of CNPs or concomitant administration of H4 antibody alone. A method of treatment is disclosed wherein therapeutic dose of CNPs, or H4 antibody alone, are administered systematically, or orally, in a delivery system to curb pathological conditions that are associated with increased burden of circulating chromatin fragments.

    摘要翻译： 使用结合剂（例如抗体或抗体与诸如藻酸盐，壳聚糖和支链淀粉等血液相容性天然聚合物底物复合的抗体）从培养基中显着降低循环染色质片段（CCF）的水平的方法，以形成复合的抗体 - 底物纳米颗粒（CNP） 公开了结合和/或灭活CCF。 与聚合物结合的抗体的量在聚合物中的活化位点的30％至100％不等。 在施用组合损伤剂后，CCF的升高水平可以显着降低，所述组织损伤剂通过伴随施用CNP或单独施用H4抗体产生凋亡染色质片段。 公开了一种治疗方法，其中治疗剂量的CNP或单独的H4抗体在递送系统中系统地或口服地施用以遏制与循环染色质片段的负担增加相关的病理状况。

    ANTIPSYCHOTIC AGENTS AND STANDARDIZED ANTIPSYCHOTIC FRACTIONS FROM RAUWOLFIA TETRAPHYLLA AND PROCESS OF THEIR ISOLATION
    5.
    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）。

    Method for in-vivo binding of chromatin fragments
    10.
    发明授权
    Method for in-vivo binding of chromatin fragments 有权
    染色质片段的体内结合方法

    公开(公告)号：US09096655B2

    公开(公告)日：2015-08-04

    申请号：US13575756

    申请日：2011-01-24

    申请人： Indraneel Mittra ,  Rekha Mannemcherril Ramesan ,  Chandra Prakash Sharma ,  Gopichettipalayam Subbaratnam Bhuvaneshwar ,  Kavita Anirban Pal

    发明人： Indraneel Mittra ,  Rekha Mannemcherril Ramesan ,  Chandra Prakash Sharma ,  Gopichettipalayam Subbaratnam Bhuvaneshwar ,  Kavita Anirban Pal

    IPC分类号： A61K47/28 ,  A61K39/44 ,  C07K16/08 ,  A61K47/48 ,  A61K39/00

    CPC分类号： C07K16/18 ,  A61K47/61 ,  A61K47/6939 ,  A61K2039/505 ,  C07K16/08 ,  Y10T428/2982

    摘要： A process for substantially reducing levels of circulating chromatin fragments (CCFs) from a medium using binding agents such as antibodies or antibodies complexed with haemocompatible natural polymer substrates like as alginates, chitosan and pullulan to form complexed antibody-substrate nano-particulates (CNP) to bind and/or inactivate CCFs is disclosed. The amount of antibody bound to the polymer varies from 30% to 100% of activated sites in the polymer. Elevated levels of CCFs can be substantially reduced following administration of tissue damaging agents that generate apoptotic chromatin fragments by the concomitant administration of CNPs or concomitant administration of H4 antibody alone. A method of treatment is disclosed wherein therapeutic dose of CNPs, or H4 antibody alone, are administered systematically, or orally, in a delivery system to curb pathological conditions that are associated with increased burden of circulating chromatin fragments.

    摘要翻译： 使用结合剂（例如抗体或抗体与诸如藻酸盐，壳聚糖和支链淀粉等血液相容性天然聚合物底物复合的抗体）从培养基中显着降低循环染色质片段（CCF）的水平的方法，以形成复合的抗体 - 底物纳米颗粒（CNP） 公开了结合和/或灭活CCF。 与聚合物结合的抗体的量在聚合物中的活化位点的30％至100％不等。 在施用组合损伤剂后，CCF的升高水平可以显着降低，所述组织损伤剂通过伴随施用CNP或单独施用H4抗体产生凋亡染色质片段。 公开了一种治疗方法，其中治疗剂量的CNP或单独的H4抗体在递送系统中系统地或口服地施用以遏制与循环染色质片段的负担增加相关的病理状况。