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    6-phenoxymethyl-4-hydroxytetrahydropyran-2-ones and 6-thiphenoxymethyl-4-hydroxytetrahydropyran-2-ones and the corresponding dihydroxycarboxylic acid derivatives, salts and esters, and in treating hypercholesterolemia
    2.
    发明授权
    6-phenoxymethyl-4-hydroxytetrahydropyran-2-ones and 6-thiphenoxymethyl-4-hydroxytetrahydropyran-2-ones and the corresponding dihydroxycarboxylic acid derivatives, salts and esters, and in treating hypercholesterolemia 失效
    6-苯氧基甲基-4-羟基四氢吡喃-2-酮和6-硫代氧甲基-4-羟基四氢吡喃-2-酮及相应的二羟基羧酸衍生物，盐和酯，以及治疗高胆固醇血症

    公开(公告)号：US5166171A

    公开(公告)日：1992-11-24

    申请号：US680613

    申请日：1991-04-02

    申请人： Heiner Jendralla ,  Gunther Wess ,  Wilhelm Bartmann ,  Gerhard Beck

    发明人： Heiner Jendralla ,  Gunther Wess ,  Wilhelm Bartmann ,  Gerhard Beck

    IPC分类号： C07C59/68 ,  C07C323/09 ,  C07D309/30

    CPC分类号： C07C59/68 ,  C07C323/09 ,  C07D309/30 ,  Y10S514/824

    摘要： 6-Phenoxymethyl-4-hydroxytetrahydropyran-2-ones and 6-thiophenoxymethyl-4-hydroxytetrahydropyran-2-ones and the corresponding dihydroxycarboxylic acid derivatives, salts and esters, processes for the preparation of these compounds, their use as pharmaceuticals, pharmaceutical preparations and novel phenols and thiophenols Compounds of the general formula I ##STR1## and the corresponding open-chain dihydroxycarboxylic acids of the formula II ##STR2## in which X, Y and Z have the meanings given, and pharmacologically tolerated salts thereof with bases and pharmacologically tolerated esters thereof, processes for the preparation of these compounds, their use as pharmaceuticals and pharmaceutical preparations are described. Novel phenols and thiophenols of the formula III ##STR3## in which X, Y and Z have the meanings given, are also described.

    摘要翻译： 6-苯氧基甲基-4-羟基四氢吡喃-2-酮和6-噻吩氧基甲基-4-羟基四氢吡喃-2-酮以及相应的二羟基羧酸衍生物，盐和酯，用于制备这些化合物的方法，它们作为药物，药物制剂和 新型酚类和噻吩类化合物通式Ⅰ的化合物及其相应的式Ⅱ的开环二羟基羧酸，其中X，Y和Z具有给定的含义，其药理学上可容许的盐与碱和 描述了其药理学耐受的酯，制备这些化合物的方法，它们作为药物和药物制剂的用途。 还描述了其中X，Y和Z具有给定的含义的式III“III”的新型酚类和噻吩类。

    Process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides
    4.
    发明授权
    Process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides 有权
    制备乙酰基 - 脒基苯丙氨酰 - 环己基甘氨酰 - 吡啶并氨酰胺的方法

    公开(公告)号：US07084250B2

    公开(公告)日：2006-08-01

    申请号：US10869076

    申请日：2004-06-17

    申请人： Gerhard Breipohl ,  Wolfgang Holla ,  Heiner Jendralla ,  Gerhard Beck

    发明人： Gerhard Breipohl ,  Wolfgang Holla ,  Heiner Jendralla ,  Gerhard Beck

    IPC分类号： C07K5/08

    CPC分类号： C07K5/0821 ,  C07K5/06139

    摘要： The present invention relates to a process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides of the formula I, in which the anions X are physiologically acceptable anions, and their analogs, which are effective inhibitors of the blood coagulation factor Xa and which can be used, for example, for preventing thromboses. The process according to the invention comprises the coupling of 2-[2-acetylamino-3-(4-amidinophenyl)propionylamino]-2-cyclohexylacetic acid, which is obtained from 2-[2-acetylamino-3-(4-cyanophenyl)acryloylamino]-2-cyclohexylacetic acid by asymmetric hydrogenation and conversion of the cyano group into the amidine, or a salt thereof, with a 3-(2-amino-2-carbamoylethyl)-1-methylpyridinium salt or a salt thereof. The invention furthermore provides starting materials and intermediates for this process, processes for their preparation and acetyl-(S)-4-amidiniophenylalanyl-(S)-cyclohexylglycyl-(S)-(1-methyl-3-pyridinio)alaninamide as ditosylate salt.

    摘要翻译： 本发明涉及一种制备式I的乙酰基 - 脒基苯脒基 - 环己基甘氨酰 - 吡啶并吡喃酰胺的方法，其中阴离子X是生理上可接受的阴离子，以及它们的类似物，它们是凝血因子Xa的有效抑制剂， 可用于例如用于预防血栓形成。 根据本发明的方法包括2- [2-乙酰氨基-3-（4-脒基苯基）丙酰基氨基] -2-环己基乙酸的偶联，其由2- [2-乙酰氨基-3-（4-氰基苯基） 丙烯酰氨基] -2-环己基乙酸，通过不对称氢化，并将氰基转化为脒或其盐与3-（2-氨基-2-氨基甲酰基乙基）-1-甲基吡啶鎓盐或其盐。 本发明还提供了该方法的起始原料和中间体，其制备方法和乙酰基 - （S）-4-脒基苯基丙氨酰 - （S） - 环己基甘氨酰 - （S） - （1-甲基-3-吡啶鎓）丙烯酰胺作为二甲苯磺酸盐 。

    Process for the enantioselective synthesis of 2(R)-benzylsuccinic acid monoamide derivatives
    7.
    发明授权
    Process for the enantioselective synthesis of 2(R)-benzylsuccinic acid monoamide derivatives 失效
    2（R） - 苄基琥珀酸单酰胺衍生物的对映选择性合成方法

    公开(公告)号：US5321139A

    公开(公告)日：1994-06-14

    申请号：US22887

    申请日：1993-02-16

    申请人： Ulrich Lerch ,  Heiner Jendralla ,  Bernhard Seuring ,  Rainer Henning

    发明人： Ulrich Lerch ,  Heiner Jendralla ,  Bernhard Seuring ,  Rainer Henning

    IPC分类号： B01J31/24 ,  C07B61/00 ,  C07C231/02 ,  C07C231/18 ,  C07C233/14 ,  C07C233/22 ,  C07C233/40 ,  C07D211/44 ,  C07D211/58 ,  C07D241/04 ,  C07F9/572 ,  C07F15/00 ,  C07D211/06

    CPC分类号： C07F15/0013 ,  C07C231/18 ,  C07D211/58 ,  C07F15/008 ,  C07F9/5726

    摘要： Two processes are described for the preparation of the optically pure compounds of formula 1: ##STR1## in which R.sup.1 and R.sup.2 are e.g. alkyl, R.sup.3 and R.sup.4 are e.g. hydrogen and R.sup.5 is e.g. hydrogen. Both processes include, as key steps, the enantioselective hydrogenation of a C.dbd.C double bond and the regioselective formation of a dicarboxylic acid monoamide derivative. In one process a phenylitaconic acid derivative is asymmetrically hydrogenated to give an optically active (R)-benzylsuccinic acid which is then converted to a diester, said diester being converted to the monoamide compound of formula 1. In the second process, a phenylitaconic acid derivative is converted to its anhydride, and the anhydride is then converted to a monoamide which is then asymmetrically hydrogenated to give the compound of formula 1.

    摘要翻译： 描述了制备光学纯的式1化合物的两种方法：其中R 1和R 2是例如： 烷基，R 3和R 4是例如。 氢和R 5是例如。 氢。 作为关键步骤，两种方法都包括C = C双键的对映选择性氢化和二羧酸单酰胺衍生物的区域选择性形成。 在一个过程中，苯基衣康酸衍生物被不对称氢化，得到光学活性（R） - 苄基琥珀酸，然后将其转化为二酯，所述二酯转化成式1的单酰胺化合物。在第二种方法中，苯基衣康酸衍生物 转化成其酐，然后将酸酐转化为单酰胺，然后将其不对称氢化，得到式1的化合物。

    Optically active β-aminoketones, optically active 1,3-amino alcohols and processes for preparing them
    10.
    发明授权
    Optically active β-aminoketones, optically active 1,3-amino alcohols and processes for preparing them 有权
    光学活性β-氨基酮，旋光性1,3-氨基醇及其制备方法

    公开(公告)号：US07161008B2

    公开(公告)日：2007-01-09

    申请号：US10430023

    申请日：2003-05-05

    申请人： Heiner Jendralla ,  Wilfried Schwab ,  Thomas Stuedemann

    发明人： Heiner Jendralla ,  Wilfried Schwab ,  Thomas Stuedemann

    IPC分类号： C07D213/36 ,  C07C211/00

    CPC分类号： C07D213/74

    摘要： The invention relates to chiral Mannich bases of formula (I), chiral 1,3-amino alcohols of formula (II) derived therefrom, wherein R1, R2, R3, R4 and R5 are as defined herein, and to processes for preparing Mannich salts of formula (III) containing a chiral anion Y*− and compounds of formulae (I) and (II), wherein R1, R2, R3, R4, R5 and Y*− are as defined herein.

    摘要翻译： 本发明涉及式（I）的手性曼尼希碱，由其衍生的式（II）的手性1,3-氨基醇，其中R 1，R 2，R 2， R 4和R 5如本文所定义，并且涉及制备含有手性阴离子Y的式（III）的曼尼希盐的方法， 和式（I）和（II）的化合物，其中R 1，R 2，R 3，...， >，R 4，R 5和Y * - 如本文所定义。