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    Novel Niacin Compositions for Reduction of Amyloid Beta Peptide 42 (AB42) Production and for Treatment of Alzheimer's Disease
    12.
    发明申请
    Novel Niacin Compositions for Reduction of Amyloid Beta Peptide 42 (AB42) Production and for Treatment of Alzheimer's Disease 审中-公开
    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。

    Fused 7-oxo-pyrimidinyl compounds, preparation, composition and use thereof
    15.
    发明授权
    Fused 7-oxo-pyrimidinyl compounds, preparation, composition and use thereof 失效
    融合的7-氧代 - 嘧啶基化合物，其制备，组成和用途

    公开(公告)号：US06444816B1

    公开(公告)日：2002-09-03

    申请号：US09507373

    申请日：2000-02-18

    申请人： Saibal Kumar Das ,  Papi Reddy Purma ,  Venkateswarlu Akella ,  Rajagopalan Ramanujam ,  Ranjan Chakrabarti ,  Vidya Bhushan Lohray ,  Braj Bhushan Lohray ,  Rao Bheema Paraselli

    发明人： Saibal Kumar Das ,  Papi Reddy Purma ,  Venkateswarlu Akella ,  Rajagopalan Ramanujam ,  Ranjan Chakrabarti ,  Vidya Bhushan Lohray ,  Braj Bhushan Lohray ,  Rao Bheema Paraselli

    IPC分类号： C07D23902

    CPC分类号： C07C217/22 ,  C07C237/32 ,  C07C247/04 ,  C07D239/36 ,  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 &bgr;-aryl-&agr;-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。

    Monocyclic compounds and their use in medicine: process for their preparation and pharmaceutical compositions containing them
    16.
    发明授权
    Monocyclic compounds and their use in medicine: process for their preparation and pharmaceutical compositions containing them 失效
    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：US06369067B1

    公开(公告)日：2002-04-09

    申请号：US09507371

    申请日：2000-02-18

    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： A01N4354

    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 &bgr;-aryl-&agr;-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。

    Monocyclic compounds and their use in medicine: process for their preparation and pharmaceutical compositions containing them
    19.
    发明授权
    Monocyclic compounds and their use in medicine: process for their preparation and pharmaceutical compositions containing them 失效
    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。