2-amino-2- [8-(dimethyl carbamoyl)- 8-aza- bicyclo [3.2.1] oct-3-yl]-exo- ethanoyl derivatives as potent DPP-IV inhibitors
    2.
    发明授权
    2-amino-2- [8-(dimethyl carbamoyl)- 8-aza- bicyclo [3.2.1] oct-3-yl]-exo- ethanoyl derivatives as potent DPP-IV inhibitors 失效
    2-氨基-2- [8-(二甲基氨基甲酰基)-8-氮杂 - 双环[3.2.1]辛-3-基] - 异 - 乙酰基衍生物作为有效的DPP-IV抑制剂

    公开(公告)号:US08748457B2

    公开(公告)日:2014-06-10

    申请号:US13378941

    申请日:2009-09-01

    IPC分类号: C07D451/02 A61K31/46

    CPC分类号: A61K31/46 C07D451/02

    摘要: The present invention is related to novel 2-Amino-2-[8-(dimethyl carbamoyl)-8-aza-bicyclo[3.2.1]oct-3-yl]-exo-ethanoyl derivatives of the general formula (A), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods of making of the above compounds, and their use as Dipeptidyl Peptidase-IV (DPP-IV) Inhibitors, which are useful in the treatment or prevention of diseases particularly Type II diabetes, other complications related to diabetes and other pathogenic conditions in which DPP IV enzyme is involved.

    摘要翻译: 本发明涉及通式(A)的新型2-氨基-2- [8-(二甲基氨基甲酰基)-8-氮杂 - 双环[3.2.1]辛-3-基] - 异 - 乙酰基衍生物, 它们的互变异构形式,其立体异构体,其药学上可接受的盐,含有它们的药物组合物,制备上述化合物的方法,以及它们作为二肽基肽酶-IV(DPP-IV)抑制剂的用途,其可用于治疗或预防疾病 特别是II型糖尿病,与糖尿病有关的其他并发症和涉及DPP IV酶的其他致病条件。

    Herbal extract comprising a mixture of saponins obtained from sapindus trifoliatus for anticonvulsant activity
    5.
    发明申请
    Herbal extract comprising a mixture of saponins obtained from sapindus trifoliatus for anticonvulsant activity 审中-公开
    草药提取物包含从三叶皂甙获得的皂苷混合物,用于抗惊厥活性

    公开(公告)号:US20050249831A1

    公开(公告)日:2005-11-10

    申请号:US10525992

    申请日:2003-08-27

    CPC分类号: A61K36/77

    摘要: A pharmaceutical composition comprising a herbal extract, comprising a mixture of saponins prepared from the pericarp of Sapindus trifoliatus, with binding affinities for the receptor sites viz. GABA-A agonist site, Glutamate-AMPA site, Glutamate-Kainate site, Glutamate-NMDA agonistic site, Glutamate-NMDA glycine (strychnine insensitive) site and Sodium channel (site 2), having major mediatory role in anticonvulsant activity. A process for preparation of the herbal extract; isolation of six pure compounds from the mixture of saponins in the aqueous extract; and a pharmaceutical composition comprising the said extract in combination with pharmaceutically acceptable additives. A method of prophylactic treatment of migraine through anticonvulsant activity of the composition by its administration through intranasal route.

    摘要翻译: 包含草药提取物的药物组合物,其包含由Sapindus trifoliatus的果皮制备的皂苷的混合物,对受体位点的结合亲和力。 GABA-A激动剂位点,谷氨酸 - AMPA位点,谷氨酸 - 红藻酸酯位点,谷氨酸-N NMDA激动位点,谷氨酸-N NMDA甘氨酸(士的宁不敏感)位点和钠通道(位点2),在抗惊厥活性中具有主要的介导作用。 制备草药提取物的方法 在水提取物中从皂甙混合物中分离出六种纯化合物; 以及包含所述提取物与药学上可接受的添加剂组合的药物组合物。 一种通过鼻内途径施用组合物的抗惊厥活性来预防性治疗偏头痛的方法。