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    Organic nitrates, processes for their preparation and their use in the treatment of cardiovascular diseases
    1.
    发明授权
    Organic nitrates, processes for their preparation and their use in the treatment of cardiovascular diseases 失效
    有机硝酸盐，其制备方法及其在治疗心血管疾病中的应用

    公开(公告)号：US5591758A

    公开(公告)日：1997-01-07

    申请号：US971812

    申请日：1993-05-04

    申请人： Jean-Pierre Nallet ,  Jacques Dreux ,  Alain Berdeaux ,  Vincent Richard ,  Piero Martorana ,  Helmut Bohn

    发明人： Jean-Pierre Nallet ,  Jacques Dreux ,  Alain Berdeaux ,  Vincent Richard ,  Piero Martorana ,  Helmut Bohn

    IPC分类号： A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61K31/54 ,  A61K38/00 ,  A61P9/08 ,  A61P9/10 ,  C07C323/23 ,  C07D213/62 ,  C07D277/06 ,  C07D279/04 ,  C07D493/04 ,  C07K9/00 ,  A01K31/425

    CPC分类号： C07D493/04 ,  C07D277/06 ,  C07K9/001 ,  A61K38/00

    摘要： Organic nitrates, processes for their preparation and their use in the treatment of vascular diseases and in particular in the treatment of angina.The said nitrates correspond to the following formula I:R--CO--(A).sub.n --Y--B (I)in which:R represents, in particular, a sulphur-containing radical and a sulphur-containing amino acid residue; A represents, in particular, a CH.sub.2 group or a substituted amino acid; n is 0 or 1 or greater than 1; Y represents an oxygen atom or an NH group and B represents, in particular, a 1,4:3,6-dianhydro hexitol mononitrate radical, an itol nitrate radical or an inositol radical.The said organic nitrates are prepared by reacting:I. either a thio acid of the type R--COOH, in which R has the same meaning as above, with a derivative of formula II: (A).sub.n --Y--B, in which A, Y, B and n have the same meaning as above,II. or a derivative of formula III: R--CO--(A).sub.n, in which R, A and n have the same meaning as above, with a derivative of formula Y--B, in which Y and B have the same meaning as above, in an appropriate solvent and under non-epimerising conditions.

    摘要翻译： PCT No.PCT / EP92 / 01746 Sec。 371日期：1993年5月4日 102（e）日期1993年5月4日PCT提交1992年8月1日PCT公布。 出版物WO93 / 03037 日期：1993年2月18日有机硝酸盐，其制备方法及其在治疗血管疾病中的用途，特别是治疗心绞痛。 所述硝酸盐对应于下式I：R-CO-（A）n -Y-B（I）其中：R表示特别是含硫基团和含硫氨基酸残基; A特别表示CH 2基团或取代的氨基酸; n为0或1或大于1; Y表示氧原子或NH基团，B表示特别是1,4：3,6-二脱水己糖醇单硝酸根基团，硝酸盐基团或肌醇基团。 所述有机硝酸盐通过以下方法制备：I。R-COOH型硫代酸，其中R具有与上述相同的含义，与式II的衍生物：（A）nYB反应，其中A，Y， B和n与上述相同，II。 或式III的衍生物：其中R，A和n具有与上述相同的含义，与式YB的衍生物（其中Y和B具有与上述相同的含义），R-CO-（A） 适当的溶剂和在非差向异构条件下。

    Halogen derivatives of 8-hydroxycarboxylic acids; the processes for their preparation and medicaments in which they are present
    2.
    发明授权
    Halogen derivatives of 8-hydroxycarboxylic acids; the processes for their preparation and medicaments in which they are present 失效
    8-羟基羧酸的卤素衍生物; 其制备过程及其存在的药物

    公开(公告)号：US4287206A

    公开(公告)日：1981-09-01

    申请号：US72411

    申请日：1979-09-04

    申请人： Pierre Simon ,  Jacques Dreux

    发明人： Pierre Simon ,  Jacques Dreux

    IPC分类号： C07C59/56 ,  C07C59/84 ,  C07C255/56 ,  C07D309/10 ,  C07D309/30 ,  A61K31/335 ,  C07C59/11

    CPC分类号： C07C255/00 ,  C07C59/56 ,  C07C59/84 ,  C07D309/30

    摘要： Halogen derivatives of 8-hydroxycarboxylic acids, which correspond to the formula ##STR1## (open form, in a basic medium) or to the formula ##STR2## (cyclized form, in an acid medium) in which formulae: X.sub.1 and X.sub.2 are halogen atoms, n.sub.1 and n.sub.2 are integers between 0 and 5, but, if n.sub.1 =0, n.sub.2 is different from 0, and vice versa, R is a hydrogen atom or an alkyl or aryl group, and Cation represents an ion originating from a base, or a metal ion, which is pharmaceutically compatible are suitable as antidepressants having a psychostimulant action.

    摘要翻译： 8-羟基羧酸的卤素衍生物，其对应于下式（图1a）（开放形式，在碱性介质中）或式（IMAGR）（环状化合物，在酸性介质中），式中X 1和X 2为卤素 原子，n1和n2是0和5之间的整数，但如果n1 = 0，n2不为0，反之亦然，R为氢原子或烷基或芳基，阳离子表示源自碱的离子 或药学上相容的金属离子适合作为具有精神兴奋作用的抗抑郁药。