OPTICALLY ACTIVE QUATERNARY AMMONIUM SALT HAVING AXIAL ASYMMETRY, AND METHOD FOR PRODUCING ALPHA-AMINO ACID AND DERIVATIVE THEREOF BY USING THE SAME
    92.
    发明申请
    OPTICALLY ACTIVE QUATERNARY AMMONIUM SALT HAVING AXIAL ASYMMETRY, AND METHOD FOR PRODUCING ALPHA-AMINO ACID AND DERIVATIVE THEREOF BY USING THE SAME 审中-公开
    具有轴向不对称性的光学活性季铵盐,以及通过使用它们生产α-氨基酸及其衍生物的方法

    公开(公告)号:US20120101309A1

    公开(公告)日:2012-04-26

    申请号:US13338301

    申请日:2011-12-28

    Abstract: The present invention discloses an optically active quanternary ammonium salt having axial asymmetry and a method for producing an α-amino acid and a derivative thereof using the same. The optically active quanternary ammonium salt having axial asymmetry of the present invention is a chiral phase-transfer catalyst that has a simple structure and that can be produced in a smaller number of process steps. The compound of the present invention is very useful as a phase-transfer catalyst in the synthesis of an α-alkyl-α-amino acid and a derivative thereof as well as an α,α-dialkyl-α-amino acid and a derivative thereof. Therefore, the compound of the present invention can be used in the development of novel foods and pharmaceuticals.

    Abstract translation: 本发明公开了具有轴向不对称性的光学活性季铵盐和使用其制备α-氨基酸及其衍生物的方法。 具有本发明的轴向不对称性的光学活性季铵盐是手性相转移催化剂,其具有简单的结构,并且可以以较少数量的工艺步骤生产。 本发明的化合物在α-烷基-α-氨基酸及其衍生物以及α,α-二烷基-α-氨基酸及其衍生物的合成中作为相转移催化剂是非常有用的 。 因此,本发明的化合物可用于开发新型食品和药物。

    SUBSTITUTED LACTAMS AS INHIBITORS OF A BETA PROTEIN PRODUCTION
    93.
    发明申请
    SUBSTITUTED LACTAMS AS INHIBITORS OF A BETA PROTEIN PRODUCTION 审中-公开
    作为蛋白质生产的抑制剂的替代的LACTAMS

    公开(公告)号:US20100069373A1

    公开(公告)日:2010-03-18

    申请号:US12615799

    申请日:2009-11-10

    Abstract: This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

    Abstract translation: 本发明涉及式(I)的新型内酰胺:具有药物和生物影响性质,其药物组合物和使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工,更具体地,抑制Aβ的生成,从而起到防止淀粉样蛋白的神经沉积的形成的作用。 更具体地说,本发明涉及与阿尔茨海默病和唐氏综合征等淀粉样蛋白生成相关的神经障碍的治疗。

    SUBSTITUTED LACTAMS AS INHIBITORS OF ABETA PROTEIN PRODUCTION
    95.
    发明申请
    SUBSTITUTED LACTAMS AS INHIBITORS OF ABETA PROTEIN PRODUCTION 审中-公开
    作为ABETA蛋白质生产的抑制剂的替代的LACTAMS

    公开(公告)号:US20100009966A1

    公开(公告)日:2010-01-14

    申请号:US12560213

    申请日:2009-09-15

    Abstract: This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

    Abstract translation: 本发明涉及式(I)的新型内酰胺:具有药物和生物影响性质,其药物组合物和使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工,更具体地,抑制Aβ肽的产生,从而起到防止淀粉样蛋白质神经沉积的形成的作用。 更具体地,本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病,例如阿尔茨海默病和唐氏综合征。

    Malonamide derivatives
    99.
    发明申请
    Malonamide derivatives 有权
    丙二酰胺衍生物

    公开(公告)号:US20070225273A1

    公开(公告)日:2007-09-27

    申请号:US11726639

    申请日:2007-03-22

    CPC classification number: C07D223/18

    Abstract: The invention relates to malonamide derivatives of formula wherein A1, A2, R1, R2, R3, and R4 are as defined herein and to pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof for the treatment of Alzheimer's disease.

    Abstract translation: 本发明涉及下式的丙二酰胺衍生物:其中A 1,S 2,R 1,R 2,R 2,R 2, R 4和R 4如本文所定义,以及用于治疗阿尔茨海默病的药学上可接受的酸加成盐,光学纯对映异构体,外消旋物或非对映体混合物。

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