Composition for beneficially influencing Alzheimer's disease and/or for Alzheimer's prophylaxis
    4.
    发明申请
    Composition for beneficially influencing Alzheimer's disease and/or for Alzheimer's prophylaxis 审中-公开
    用于有益地影响阿尔茨海默氏病和/或阿尔茨海默病预防的组合物

    公开(公告)号:US20070225367A1

    公开(公告)日:2007-09-27

    申请号:US11725674

    申请日:2007-03-20

    IPC分类号: A61K31/22

    摘要: The invention relates to a composition for Alzheimer's prophylaxis and/or for therapeutic treatment of pre-existing symptoms of the type of Alzheimer's disease comprising a mixture of VLCFA3, in particular based on montan waxes and/or derivatives thereof or Guerbet acids or the corresponding components of carnauba wax, shellac or policosanols or VLCFA3 from natural waxes, where appropriate in combination with physiologically tolerated copper salts such as copper orotate and in combination with DMAE. The composition can be administered orally according to the invention as food additive or as beverage.

    摘要翻译: 本发明涉及用于阿尔茨海默病预防和/或治疗性治疗阿尔茨海默病类型的先前存在的症状的组合物,其包括VLCFA3的混合物,特别是基于褐泥蜡和/或其衍生物或格瑞贝特酸或相应组分 巴西棕榈蜡,虫胶或聚山梨糖醇或天然蜡中的VLCFA3,其中适当地与生理上耐受的铜盐如硫酸铜和DMAE组合。 组合物可以根据本发明口服给药作为食品添加剂或作为饮料。

    Process for the preparation of racemic and optically active
1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid and its precursors

    公开(公告)号:US5252738A

    公开(公告)日:1993-10-12

    申请号:US822930

    申请日:1992-01-21

    IPC分类号: C07D217/26

    CPC分类号: C07D217/26

    摘要: A process for the preparation of racemic and optically active 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is described, in which dihalo-o-xylylenes are cyclized to dicarboxylic acid esters in basic medium using dialkyl N-acylamidomalonates of the formula (CO.sub.2 R.sup.1).sub.2 CHNHCOR.sup.2, in which R.sup.1 is (C.sub.1 -C.sub.4)-alkyl and R.sup.2 is H, (C.sub.1 -C.sub.4)-alkyl or (C.sub.6 -C.sub.12)-aryl, decarboxylated by basic hydrolysis and subsequent acid work-up and then reacted in acid medium to give (D,L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, or dihalo-o-xylylenes are cyclized in basic medium to give the dicarboxylic acid esters and these are reacted directly without isolation in a one-pot process to give (D,L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, if desired the racemic 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is reacted with (-)menthol and p-toluenesulfonic acid to give (-)menthyl (D)- or (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate, then the diastereomers are separated by column chromatography and subjected to basic hydrolysis to give (D)- or (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, or (D,L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is esterified by means of benzyl alcohol and p-toluenesulfonic acid, reacted with D(-)mandelic acid to give benzyl (D)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (D)-mandelate and benzyl (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (D)-mandelate or with L(+)mandelic acid to give benzyl (D)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (L)-mandelate and benzyl (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (L)-mandelate and then the compounds obtained are separated into the optical antipodes by fractional crystallization in an inert solvent and the enantiomers (D)- or (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid are liberated by basic hydrolysis, the chiral auxiliary reagent being recovered.

    Process for the preparation of racemic and optically active
1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid and its precursors

    公开(公告)号:US5359074A

    公开(公告)日:1994-10-25

    申请号:US76772

    申请日:1993-06-15

    CPC分类号: C07D217/26

    摘要: A process for the preparation of racemic and optically active 1,2.3,4-tetrahydroisoquinoline-3-carboxylic acid is described, in which dihalo-o-xylylenes are cyclized to dicarboxylic acid esters in basic medium using dialkyl N-acylamidomalonates of the formula (CO.sub.2 R.sup.1).sub.2 CHNHCOR.sup.2, in which R.sup.1 is (C.sub.1 -C.sub.4)-alkyl and R.sup.2 is H, (C.sub.1 -C.sub.4)-alkyl or (C.sub.6 -C.sub.12)-aryl, decarboxylated by basic hydrolysis and subsequent acid work-up and then reacted in acid medium to give (D,L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, or dihalo-o-xylylenes are cyclized in basic medium to give the dicarboxylic acid esters and these are reacted directly without isolation in a one-pot process to give (D,L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, if desired the racemic 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is reacted with (-)menthol and p-toluenesulfonic acid to give (-)menthyl (D)- or (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate, then the diastereomers are separated by column chromatography and subjected to basic hydrolysis to give (D)-or (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, or (D,L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is esterified by means of benzyl alcohol and p-toluenesulfonic acid, reacted with D(-)mandelic acid to give benzyl (D)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (D)-mandelate and benzyl (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (D)-mandelate or with L(+)mandelic acid to give benzyl (D)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (L)-mandelate and benzyl (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (L)-mandelate and then the compounds obtained are separated into the optical antipodes by fractional crystallization in an inert solvent and the enantiomers (D)- or (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid are liberated by basic hydrolysis, the chiral auxiliary reagent being recovered.