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    Substituted 3-aminosyndone imines, a process for their preparation and their use
    5.
    发明授权
    Substituted 3-aminosyndone imines, a process for their preparation and their use 失效
    取代的3-氨基壬烯亚胺，其制备方法及其用途

    公开(公告)号：US5120732A

    公开(公告)日：1992-06-09

    申请号：US575388

    申请日：1990-08-29

    Applicant: Karl Schonafinger ,  Rudi Beyerle ,  Helmut Bohn ,  Melitta Just

    Inventor： Karl Schonafinger ,  Rudi Beyerle ,  Helmut Bohn ,  Melitta Just

    IPC: C07D271/04

    CPC classification number: C07D271/04

    Abstract: Substituted 3-aminosydnone imines of the formula I ##STR1## and their pharmacologically acceptable acid addition salts, in which A denotes, for example, --CH.sub.2 --,R.sup.1 denotes hydrogen or the radical --COR.sup.5,R.sup.2, R.sup.3 denote alkyl having 1 to 4 C atoms,R.sup.5 denotes, for example, an aliphatic radical having 1 to 4 C atoms,and methods for preparing such compounds by cyclization of a compound of the formula II ##STR2## and if desired subsequent acylation. The invention also includes formulations containing effective amounts of such compounds, and methods for administering same to patients for the control and prophylaxis of cardiovascular disorders.

    Abstract translation: 式I（I）的取代的3-氨基茚三酮及其药理学上可接受的酸加成盐，其中A表示例如-CH 2 - ，R 1表示氢或基团-COR 5，R 2，R 3表示具有 1至4个C原子，R5表示例如具有1至4个C原子的脂族基团，以及通过使式II化合物（II）环化并如果需要，随后酰化制备此类化合物的方法。 本发明还包括含有有效量的这种化合物的制剂，以及将其给予患者以控制和预防心血管疾病的方法。

    Optically active, substituted 1,4-dihydropyridines and their use as medicaments
    9.
    发明授权
    Optically active, substituted 1,4-dihydropyridines and their use as medicaments 失效
    光学活性的取代的1,4-二氢吡啶类及其用作药物

    公开(公告)号：US4760147A

    公开(公告)日：1988-07-26

    申请号：US941176

    申请日：1986-12-12

    Applicant: Karl Schonafinger ,  Helmut Bohn ,  Piero Martorana ,  Rolf-Eberhard Nitz

    Inventor： Karl Schonafinger ,  Helmut Bohn ,  Piero Martorana ,  Rolf-Eberhard Nitz

    IPC: A61K31/44 ,  A61P3/00 ,  A61P3/14 ,  A61P9/00 ,  C07D211/90 ,  C07D413/04 ,  C07D493/04

    CPC classification number: C07D413/04 ,  C07D211/90 ,  C07D493/04

    Abstract: Optically active substituted 1,4-dihydropyridines of the formula I having calcium antogonistic properties: ##STR1## wherein R denotes alkyl with 1 to 5 C atoms, alkoxy-alkyl with 1 to 4 C atoms, in the alkoxy part and 2 to 4 C atoms in the alkyl part, dialkylaminioalkyl with a total of 3 to 6 C atoms each of the alkyl groups as substituents on the amino group having 1 to 3 C atoms, or --CH(CH.sub.3)CO.sub.2 R.sup.5 in the optically active (R)-forms,R.sup.1 denotes phenyl which is monosubstituted by cyano, nitro or chlorine or is disubstituted by chlorine, R.sup.2 denotes oxadiazolyl, or an oxadiaxolyl which is substituted by methyl, ethyl, i-propyl, tert.-butyl, benzyl, methylthio, i-propylthio, aminocarbonylthio or methoxymethyl,R.sup.5 denotes alkyl with 1 to 4 C atoms, and acid-addition salts thereof, and acid addition salts thereof.

    Abstract translation: 式I的光学活性取代的1,4-二氢吡啶具有钙非共轭性：其中R表示具有1至5个C原子的烷基，烷氧基 - 烷基，具有1至4个C原子，烷氧基部分和2 至烷基部分中的4个C原子，具有3至6个C原子的二烷基氨基烷基，每个烷基作为在具有1至3个C原子的氨基上的取代基，或光学活性的R（CH 3）CO 2 R 5 ）形式，R 1表示被氰基，硝基或氯单取代或被氯二取代的苯基，R 2表示恶二唑基，或被甲基，乙基，异丙基，叔丁基，苄基，甲硫基取代的恶二唑基， 异丙硫基，氨基羰硫基或甲氧基甲基，R5表示具有1-4个C原子的烷基，及其酸加成盐及其酸加成盐。

    Organic nitrates, processes for their preparation and their use in the treatment of cardiovascular diseases
    10.
    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

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

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

    IPC: 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 classification number: C07D493/04 ,  C07D277/06 ,  C07K9/001 ,  A61K38/00

    Abstract: 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.

    Abstract translation: 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。

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