公开(公告)号：US08846721B2

公开(公告)日：2014-09-30

申请号：US13574886

申请日：2011-01-22

申请人： Venkateswarlu Akella ,  Uday Saxena ,  Anji Reddy Kallam

发明人： Venkateswarlu Akella ,  Uday Saxena ,  Anji Reddy Kallam

IPC分类号： C07D401/06 ,  C07D213/56 ,  A61K31/44 ,  C07D213/82 ,  C07D213/80 ,  C07D401/12

CPC分类号： C07D213/82 ,  C07D213/56 ,  C07D213/80 ,  C07D401/06 ,  C07D401/12

摘要： Novel small molecule compounds for reduction of Aβ 42 production and for treatment of Alzheimer′s Disease and other neurodegenerative disorders, methods of making them and pharmaceutical compositions containing them are described.

摘要翻译： 用于还原A和Bgr的新型小分子化合物 描述了生产和治疗阿尔茨海默病和其他神经变性疾病，制备它们的方法和含有它们的药物组合物。

公开(公告)号：US20100063083A1

公开(公告)日：2010-03-11

申请号：US12577399

申请日：2009-10-12

申请人： Venkateswarlu Akella ,  Shanavas Alikunju ,  Ajaya Kumar Reka ,  Ramesh Mullangi ,  Raju Sirisilla ,  Subrahmanyam Duvvuri ,  Sriram Rajagopal

发明人： Venkateswarlu Akella ,  Shanavas Alikunju ,  Ajaya Kumar Reka ,  Ramesh Mullangi ,  Raju Sirisilla ,  Subrahmanyam Duvvuri ,  Sriram Rajagopal

IPC分类号： A61K31/4375 ,  C07D491/22 ,  A61P35/00

CPC分类号： C07D491/22 ,  C07D519/00

摘要： A 5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin diasterisomer is described which is a better inhibitor of topoisomerase I than either the diastereoisomeric mixture 5(RS)-(2′-hydroxyethoxy)-20(S)-camptothecin, or the 5(R)-(2′-hydroxyethoxy)-20(S)-camptothecin diastereoisomer. Pharmaceutical compositions of the 5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin diastereoisomer are also described as are methods of using the compound for the inhibition of topoisomerase I and for the treatment of cancer.

摘要翻译： 描述了5（S） - （2'-羟基乙氧基）-20（S） - 喜树碱非对映异构体，其是非对映异构体混合物5（RS） - （2'-羟基乙氧基）-20（S ） - 喜树碱或5（R） - （2'-羟基乙氧基）-20（S） - 喜树碱非对映异构体。 还描述了5（S） - （2'-羟基乙氧基）-20（S） - 喜树碱非对映异构体的药物组合物是使用该化合物抑制拓扑异构酶I和治疗癌症的方法。

公开(公告)号：US07601732B2

公开(公告)日：2009-10-13

申请号：US11753392

申请日：2007-05-24

申请人： Venkateswarlu Akella ,  Shanavas Alikunju ,  Ajaya Kumar Reka ,  Ramesh Mullangi ,  Raju Sirisilla ,  Subrahmanyam Duvvuri ,  Sriram Rajagopal

发明人： Venkateswarlu Akella ,  Shanavas Alikunju ,  Ajaya Kumar Reka ,  Ramesh Mullangi ,  Raju Sirisilla ,  Subrahmanyam Duvvuri ,  Sriram Rajagopal

IPC分类号： A61K31/4745 ,  C07D491/22

CPC分类号： C07D491/22 ,  C07D519/00

摘要： A crystalline form of 5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin diastereoisomer of 5(RS)-(2′-hydroxyethoxy)-20(S)-camptothecin is described that is characterized by having an X-ray powder diffraction pattern comprising one or more peak intensities expressed in degrees 2θ that are selected from the group consisting of 7.2±0.1, 9.4±0.1, 11.02±0.1, 12.00±0.1, 14.54±0.1, 15.2±0.1, 18.92±0.1, 21.86±0.1, 22.74±0.1 and 26.42±0.1. Methods of making and using the compound are also described.

摘要翻译： 描述了5（S） - （2'-羟基乙氧基）-20（S） - 喜树碱5（RS） - （2'-羟基乙氧基）-20（S） - 喜树碱的非对映异构体的结晶形式，其特征在于具有 X射线粉末衍射图，其包含以度2θ表示的一个或多个峰强度，其选自7.2±0.1,9.4±0.1,11.02±0.1,12.00±0.1,14.54±0.1,15.2±0.1,18.92± 0.1，21.86±0.1,22.74±0.1和26.42±0.1。 还描述了制备和使用该化合物的方法。

公开(公告)号：US20080076790A1

公开(公告)日：2008-03-27

申请号：US11753392

申请日：2007-05-24

申请人： Venkateswarlu Akella ,  Shanavas Alikunju ,  Ajaya Reka ,  Ramesh Mullangi ,  Raju Sirisilla ,  Subrahmanyam Duvvuri ,  Sriram Rajagopal

发明人： Venkateswarlu Akella ,  Shanavas Alikunju ,  Ajaya Reka ,  Ramesh Mullangi ,  Raju Sirisilla ,  Subrahmanyam Duvvuri ,  Sriram Rajagopal

IPC分类号： A61K31/436 ,  A61P35/00 ,  C07D491/22

CPC分类号： C07D491/22 ,  C07D519/00

摘要： A crystalline form of 5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin diastereoisomer of 5(RS)-(2′-hydroxyethoxy)-20(S)-camptothecin is described that is characterized by having an X-ray powder diffraction pattern comprising one or more peak intensities expressed in degrees 2θ that are selected from the group consisting of 7.2±0.1, 9.4±0.1, 11.02±0.1, 12.00±0.1, 14.54±0.1, 15.2±0.1, 18.92±0.1, 21.86±0.1, 22.74±0.1 and 26.42±0.1. Methods of making and using the compound are also described.

摘要翻译： 描述了5（S） - （2'-羟基乙氧基）-20（S） - 喜树碱5（RS） - （2'-羟基乙氧基）-20（S） - 喜树碱的非对映异构体的结晶形式，其特征在于具有 X射线粉末衍射图，其包含以度2θ表示的一个或多个峰强度，其选自7.2±0.1,9.4±0.1,11.02±0.1,12.00±0.1,14.54±0.1,15.2±0.1,18.92± 0.1，21.86±0.1,22.74±0.1和26.42±0.1。 还描述了制备和使用该化合物的方法。

公开(公告)号：US20060089500A1

公开(公告)日：2006-04-27

申请号：US11296749

申请日：2005-12-07

申请人： Ranga Gurram ,  Venkateswarlu Akella ,  Rajagopalan Ramanujam ,  Ranjan Chakrabarti ,  Parimal Misra ,  Vidya Lohray ,  Braj Lohray ,  Rao Paraselli

发明人： Ranga Gurram ,  Venkateswarlu Akella ,  Rajagopalan Ramanujam ,  Ranjan Chakrabarti ,  Parimal Misra ,  Vidya Lohray ,  Braj Lohray ,  Rao Paraselli

IPC分类号： A61K31/513 ,  C07D239/02

CPC分类号： C07D239/36 ,  C07C217/22 ,  C07C237/32 ,  C07C247/04 ,  C07D239/90

摘要： The present invention relates to novel antiobesity and hypocholesterolemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel β-aryl-α-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. The present invention also relates to a process for the preparation of the above said novel compounds, their analogs, their derivatives, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them. The present invention also relates to novel intermediates, processes for their preparation and their use in the preparation of compounds of formula (I).

公开(公告)号：US07601733B2

公开(公告)日：2009-10-13

申请号：US11753432

申请日：2007-05-24

申请人： Venkateswarlu Akella ,  Shanavas Alikunju ,  Ajaya Kumar Reka ,  Ramesh Mullangi ,  Raju Sirisilla ,  Subrahmanyam Duvvuri ,  Sriram Rajagopal

发明人： Venkateswarlu Akella ,  Shanavas Alikunju ,  Ajaya Kumar Reka ,  Ramesh Mullangi ,  Raju Sirisilla ,  Subrahmanyam Duvvuri ,  Sriram Rajagopal

IPC分类号： A61K31/4745 ,  C07D491/22

CPC分类号： C07D491/22 ,  C07D519/00

摘要： A 5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin diasterisomer is described which is a better inhibitor of topoisomerase I than either the diastereoisomeric mixture 5(RS)-(2′-hydroxyethoxy)-20(S)-camptothecin, or the 5(R)-(2′-hydroxyethoxy)-20(S)-camptothecin diastereoisomer. Pharmaceutical compositions of the 5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin diastereoisomer are also described as are methods of using the compound for the inhibition of topoisomerase I and for the treatment of cancer.

摘要翻译： 描述了5（S） - （2'-羟基乙氧基）-20（S） - 喜树碱非对映异构体，其是非对映异构体混合物5（RS） - （2'-羟基乙氧基）-20（S ） - 喜树碱或5（R） - （2'-羟基乙氧基）-20（S） - 喜树碱非对映异构体。 还描述了5（S） - （2'-羟基乙氧基）-20（S） - 喜树碱非对映异构体的药物组合物是使用该化合物抑制拓扑异构酶I和治疗癌症的方法。

公开(公告)号：US06177439B1

公开(公告)日：2001-01-23

申请号：US08771391

申请日：1996-12-19

申请人： Subrahmanyam Duvvuri ,  Venkateswarlu Akella ,  Sharma Manohara Vedula ,  Sastry V. R. S. Thungathurthi ,  Vamsee Krishna Chintakunta ,  Shobha Madabhushi

发明人： Subrahmanyam Duvvuri ,  Venkateswarlu Akella ,  Sharma Manohara Vedula ,  Sastry V. R. S. Thungathurthi ,  Vamsee Krishna Chintakunta ,  Shobha Madabhushi

IPC分类号： A61K34745

CPC分类号： C07D491/22

摘要： Novel water soluble C-ring analogues of 20(S)-camptothecin having the general formula 1, All the compounds of the formula 1 are prepared from the compounds of the general formula 2 having 20(S)-chiral carbon where R1 to R5 have the meaning given above. The compounds of the formula 1 possess potent anti-cancer and anti-viral properties. The invention also provides an alternate process for the preparation of known C-5 substituted compounds of the formula 1,

摘要翻译： 具有通式1的20（S） - 喜树碱的新型水溶性C-环类似物，所有式1化合物均由具有20（S） - 手性碳的通式2的化合物制备，其中R 1至R 5具有 上面给出的含义。 式1的化合物具有有效的抗癌和抗病毒性质。本发明还提供制备式1的已知C-5取代的化合物的替代方法，

公开(公告)号：US07157581B2

公开(公告)日：2007-01-02

申请号：US11296749

申请日：2005-12-07

申请人： Ranga Madhavan Gurram ,  Venkateswarlu Akella ,  Rajagopalan Ramanujam ,  Ranjan Chakrabarti ,  Parimal Misra ,  Vidya Bhushan Lohray ,  Braj Bhushan Lohray ,  Rao Bheema Paraselli

发明人： Ranga Madhavan Gurram ,  Venkateswarlu Akella ,  Rajagopalan Ramanujam ,  Ranjan Chakrabarti ,  Parimal Misra ,  Vidya Bhushan Lohray ,  Braj Bhushan Lohray ,  Rao Bheema Paraselli

IPC分类号： C07D239/02

CPC分类号： C07D239/36 ,  C07C217/22 ,  C07C237/32 ,  C07C247/04 ,  C07D239/90

摘要： The present invention relates to novel antiobesity and hypocholesterolemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel β-aryl-α-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. The present invention also relates to a process for the preparation of the above said novel compounds, their analogs, their derivatives, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them. The present invention also relates to novel intermediates, processes for their preparation and their use in the preparation of compounds of formula (I).

摘要翻译： 本发明涉及新型抗肥胖和低胆固醇血症化合物，其衍生物，其类似物，其互变异构形式，其立体异构体，其多晶型物，其药学上可接受的盐，其药学上可接受的溶剂合物和含有它们的药学上可接受的组合物。 更具体地，本发明涉及通式（I）的新型β-芳基-α-氧代取代的烷基羧酸，其衍生物，它们的类似物，其互变异构形式，它们的立体异构体，它们的多晶型物，其药学上可接受的盐，它们的药学上可接受的 溶剂合物和含有它们的药学上可接受的组合物。 本发明还涉及制备上述新化合物，其类似物，其衍生物，其互变异构形式，其立体异构体，其多晶型物，其药学上可接受的盐，药学上可接受的溶剂化物和含有它们的药物组合物的方法。 本发明还涉及新型中间体，其制备方法及其在制备式（I）化合物中的用途。

公开(公告)号：US06486196B2

公开(公告)日：2002-11-26

申请号：US09849586

申请日：2001-05-04

申请人： Srinivas Nanduri ,  Sairam Pothukuchi ,  Sriram Rajagopal ,  Venkateswarlu Akella ,  Sunilkumar Bhadramma Kochunarayana Pillai ,  Ranjan Chakrabarti

发明人： Srinivas Nanduri ,  Sairam Pothukuchi ,  Sriram Rajagopal ,  Venkateswarlu Akella ,  Sunilkumar Bhadramma Kochunarayana Pillai ,  Ranjan Chakrabarti

IPC分类号： A61K31335

CPC分类号： C07D407/06 ,  C07D307/34

摘要： The present invention relates to novel anticancer agents, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The present invention more particularly relates to novel derivatives of andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The novel derivatives of andrographolide have the general formula (I).

摘要翻译： 本发明涉及新型抗癌剂，其立体异构体，其多晶型物，其药学上可接受的盐及其药学上可接受的溶剂合物。 本发明更具体地涉及穿心莲内酯的新型衍生物，其立体异构体，其多晶型物，其药学上可接受的盐及其药学上可接受的溶剂合物。 穿心莲内酯的新衍生物具有通式（I）。

公开(公告)号：US06214836B1

公开(公告)日：2001-04-10

申请号：US08772071

申请日：1996-12-19

申请人： Subrahmanyam Duvvuri ,  Venkateswarlu Akella ,  Sharma Manohara Vedula ,  Rao Venkateswara Kalla ,  Srinivas S.S.V. Akella

发明人： Subrahmanyam Duvvuri ,  Venkateswarlu Akella ,  Sharma Manohara Vedula ,  Rao Venkateswara Kalla ,  Srinivas S.S.V. Akella

IPC分类号： A61K314745

CPC分类号： C07D491/22

摘要： Novel water soluble C-ring analogues of 20(S)-camptothecin having the general formula 1. All the compounds of the formula 1 are prepared from the compounds of the general formula 2 having 20(S)-chiral carbon. The compounds of the formula 1 possess potent anti-cancer and anti-viral properties. The invention also provides an alternate process for the preparation of known C-5 substituted compounds of the formula 1.

摘要翻译： 具有通式1的20（S） - 喜树碱的新型水溶性C-环类似物。所有式1化合物由具有20（S） - 手性碳的通式2的化合物制备。 式1的化合物具有有效的抗癌和抗病毒性质。 本发明还提供了制备式1的已知C-5取代的化合物的替代方法。