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    Amino-substituted benzoylguanidines, process for their preparation, their use as a medicament and medicament containing them
    8.
    发明授权
    Amino-substituted benzoylguanidines, process for their preparation, their use as a medicament and medicament containing them 失效
    氨基取代的苯甲酰胍，其制备方法，它们作为药物的用途和含有它们的药物

    公开(公告)号：US5364868A

    公开(公告)日：1994-11-15

    申请号：US16535

    申请日：1993-02-11

    申请人： Heinrich Englert ,  Dieter Mania ,  Hans-Jochen Lang ,  Wolfgang Scholz ,  Wolfgang Linz ,  Udo Albus

    发明人： Heinrich Englert ,  Dieter Mania ,  Hans-Jochen Lang ,  Wolfgang Scholz ,  Wolfgang Linz ,  Udo Albus

    IPC分类号： A61K31/155 ,  A61K31/165 ,  A61K31/445 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  C07C279/22 ,  C07D213/65 ,  C07D295/14 ,  C07D295/155 ,  C07C279/10 ,  C07D207/06 ,  C07D211/28

    CPC分类号： C07D295/155 ,  C07C279/22 ,  C07D213/65

    摘要： Amino-substituted benzoylguanidines, process for their preparation, their use as a medicament and medicament containing themBenzoylguanidines of the formula I ##STR1## are described in which R(1) or R(2) is an amino group --NR(3)R(4), where R(3) and R(4) are H or (cyclo)alkyl or R(3) is phenyl-(CH.sub.2).sub.p -- where p=0, 1, 2, 3 or 4, or phenyl, or R(3) and R(4) can also together be a methylene chain, and in which the other substituent R(1) or R(2) in each case is H, F, Cl, alkyl, alkoxy, CF.sub.3, C.sub.m F.sub.2m+1 --CH.sub.2 --, benzyl or phenoxy, and their pharmaceutically tolerable salts.The compounds according to the invention have very good antiarrhythmic properties, as occur, for example, in the case of oxygen deficiency symptoms. The compounds are used as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and infarct treatment as well as for the treatment of angina pectoris, where they also preventively inhibit or greatly decrease the pathophysiological processes in the formation of ischemically induced damage, in particular in the production of ischemically induced cardiac arrhythmias.

    摘要翻译： 氨基取代的苯甲酰胍，其制备方法，它们作为药物的用途和含有它们的药物描述了其中R（1）或R（2）是氨基-NR（ 3）R（4）其中R（3）和R（4）是H或（环）烷基或R（3）是苯基 - （CH 2）p - ，其中p = 0,1,2,3或4， 或苯基或R（3）和R（4）也可以一起为亚甲基链，其中每种情况下其它取代基R（1）或R（2）为H，F，Cl，烷基，烷氧基， CF3，CmF2m + 1-CH2-，苄基或苯氧基，及其药学上可耐受的盐。 根据本发明的化合物具有非常好的抗心律失常性质，例如在缺氧症状的情况下发生。 该化合物被用作具有用于梗塞预防和梗塞治疗的心脏保护组分以及用于治疗心绞痛的抗心律失常药物，其中它们也预防性地抑制或大大降低缺血诱导的损伤形成中的病理生理过程，特别是在 产生缺血诱导的心律失常。