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1. 发明申请

US20120322831A1 COMPOSITIONS FOR REDUCING AB 42 PRODUCTION AND THEIR USE IN TREATING ALZHEIMER'S DISEASE (AD) 有权
标题翻译：用于减少AB 42生产的组合物及其在治疗阿尔茨海默病（AD）中的应用
公开(公告)号：US20120322831A1
公开(公告)日：2012-12-20
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： A61K31/4406 , A61P25/16 , A61K31/4439 , A61P25/28 , C07D213/56 , 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。

2. 发明授权

US08846721B2 Compositions for reducing aβ 42 production and their use in treating alzheimer's disease (AD) 有权
标题翻译：降低成本的组合 42生产及其在治疗阿尔茨海默病（AD）中的应用
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。

3. 发明申请

US20130338199A1 Novel Niacin Compositions for Reduction of Amyloid Beta Peptide 42 (AB42) Production and for Treatment of Alzheimer's Disease 审中-公开
标题翻译：用于还原淀粉样β肽42（AB42）的新型烟酸组合物生产和治疗阿尔茨海默病
公开(公告)号：US20130338199A1
公开(公告)日：2013-12-19
申请号：US13971151
申请日：2013-08-20
申请人： Uday Saxena , Venkateswarlu Akella
发明人： Uday Saxena , Venkateswarlu Akella
IPC分类号： C07D213/80
CPC分类号： C07D213/80 , A61K31/085 , A61K31/12 , A61K31/192 , A61K31/196 , A61K31/455 , A61K2300/00
摘要： The present invention discloses (1) phenolic ester hybrids of niacin with m-methoxy-p-hydroxy phenyl compounds like eugenol, vanillin, apocynin, ferulic acid, isoferulic acid and eugenol epoxide and (2) cocrystals of hybrids as above, particularly cocrystal of niacin-eugenol hybrid with cocrystal former like eugenol and oxalic acid (3) novel pharmaceutical compositions comprising a combination of niacin and one or more small molecule/potentiating agent like eugenol, curcumin, cinnamic acid, meclofenamic acid, and their use in the treatment of a disorder or a disease caused by excess production of amyloid beta peptide-42 (Aβ42), its deposition, accumulation, and plaque formation including Alzheimer's Disease, dementia and mild cognitive impairment as well as other neurodegenerative diseases such as Parkinson's Disease, Huntington's disease, multiple sclerosis, amytrophic lateral sclerosis and ischemic stroke.
摘要翻译：本发明公开了（1）烟酸与α-甲氧基对羟基苯基化合物如丁子香酚，香草醛，阿朴替林，阿魏酸，异钌酸和丁子香酚环氧化物的酚酯混合物和（2）上述杂合体的共晶体，特别是共晶体烟酸 - 丁子香酚与共晶体如丁子香酚和草酸的混合物（3）包含烟酸和一种或多种小分子/增效剂如丁子香酚，姜黄素，肉桂酸，甲氯芬那酸的组合的新型药物组合物及其在治疗由淀粉样β肽-42（Abeta42）的过量产生引起的疾病或疾病，其沉积，积累和斑块形成，包括阿尔茨海默氏病，痴呆和轻度认知障碍以及其他神经变性疾病如帕金森病，亨廷顿舞蹈病，多发性硬化，肌萎缩性侧索硬化和缺血性卒中。

4. 发明授权

US07601733B2 5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin and its preparation and use for the treatment of cancer 失效
标题翻译： 5（S） - （2'-羟基乙氧基）-20（S） - 喜树碱及其制备及用于治疗癌症
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。

5. 发明授权

US06177439B1 Water soluble analogues of 20(S)-camptothecin 失效
标题翻译： 20（S） - 喜树碱的水溶性类似物
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，

6. 发明授权

US07053217B2 Monocyclic compounds and their use in medicine: process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：单环化合物及其在药物中的应用：其制备方法和含有它们的药物组合物
公开(公告)号：US07053217B2
公开(公告)日：2006-05-30
申请号：US10041384
申请日：2002-01-08
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： C07D239/22
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。

7. 发明授权

US06576662B2 Compounds having anticancer activity : process for their preparation and pharmaceutical compositions containing them 失效
公开(公告)号：US06576662B2
公开(公告)日：2003-06-10
申请号：US09849584
申请日：2001-05-04
申请人： Srinivas Nanduri , Sriram Rajagopal , Venkateswarlu Akella
发明人： Srinivas Nanduri , Sriram Rajagopal , Venkateswarlu Akella
IPC分类号： A61K3134
CPC分类号： C07D405/06 , C07D307/58 , C07D405/08 , C07D405/12 , C07D417/12
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).

8. 发明申请

US20100063083A1 5(S)-(2'-HYDROXYETHOXY)-20(S)-CAMPTOTHECIN AND ITS PREPARATION AND USE FOR THE TREATMENT OF CANCER 失效
标题翻译： 5（S） - （2'-羟基乙酰氧基）-20（S）-CAMPTOTHECIN及其制备和用于治疗癌症
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。

9. 发明授权

US07601732B2 Crystalline form of 5(S)-(2-hydroxyethoxy)-20(S)-camptothecin 失效
标题翻译： 5（S） - （2'-羟基乙氧基）-20（S）-CAMPTOTHECIN的晶体形式
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。

10. 发明申请

US20080076790A1 CRYSTALLINE FORM OF 5(S)-(2-HYDROXYETHOXY)-20(S)-CAMPTOTHECIN 失效
标题翻译： 5（S） - （2'-羟基乙氧基）-20（S）-CAMPTOTHECIN的晶体形式
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。

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