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    3,5-Substituted benzoylguanidines, process for their preparation, their use as a medicament of diagnostic and medicament containing them
    52.
    发明授权
    3,5-Substituted benzoylguanidines, process for their preparation, their use as a medicament of diagnostic and medicament containing them 失效
    3,5-取代的苯甲酰胍，其制备方法，它们作为含有它们的诊断药物和药物的用途

    公开(公告)号：US5373024A

    公开(公告)日：1994-12-13

    申请号：US15926

    申请日：1993-02-10

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

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

    IPC分类号： A61K31/155 ,  A61K31/18 ,  A61K31/275 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P35/04 ,  C07C217/44 ,  C07C311/16 ,  C07C311/37 ,  C07C311/39 ,  C07C311/47 ,  C07C317/42 ,  C07C317/44 ,  C07C323/65 ,  C07C279/22

    CPC分类号： C07C217/44 ,  C07C311/16 ,  Y10S514/821

    摘要： Benzoylguanidines of the formula I ##STR1## are described where R(1) is R(4)--SO.sub.m or R(5)R(6)N--SO.sub.z --, where R(4) and R(5) are alk(en)yl or --C.sub.n H.sub.2n --R(7), and where R(7) is a cycloalkyl or phenyl, where R(5) also has the meaning of H, and R(6) is H or C.sub.1 -C.sub.4 -alkyl, R(2) is hydrogen, halogen, alkyl, O--(CH.sub.2).sub.m C.sub.p F.sub.2p+1, --X--R(10), where X is O, S or NR(11), R(10) is H, (cyclo)alkyl(methyl) or --C.sub.n H.sub.2n --R(12) where R(12) is phenyl, and R(3) is defined, inter alia, as R(1), and their pharmaceutically tolerable salts.The compounds I are obtained by reaction of compounds of the formula II ##STR2## with guanidine, in which L is a leaving group which can be easily nucleophilically substituted.Compounds I are outstandingly suitable as antiarrythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and infarct treatment and for the treatment of angina pectoris, where they also preventively inhibit or greatly reduce the pathophysiological processes during the formation of ischemically induced damage. They are moreover distinguished by strong inhibitory action on the proliferation of cells. They can therefore be used as antiatherosclerotics, agents against late-onset diabetic complications, cancers, and fibrotic diseases such as pulmonary fibrosis, fibrosis of the liver or fibrosis of the kidneys.They are effective inhibitors of the cellular sodium/proton antiporter (Na.sup.+ /H.sup.+ exchanger).

    摘要翻译： 其中R（1）为R（4）-SOm或R（5）R（6）N-SOz-，其中R（4）和R（5）为 烷基（烯）或-C n H 2n-R（7），其中R（7）为环烷基或苯基，其中R（5）也为H，R（6）为H或C 1 -C 4 - 烷基，R（2）为氢，卤素，烷基，O-（CH2）mCpF2p + 1，-XR（10）其中X为O，S或NR（11），R（10）为H，（环） 烷基（甲基）或-CnH2n-R（12）其中R（12）为苯基，R（3）特别定义为R（1）及其药学上可耐受的盐。 化合物I通过式II化合物（II）与胍反应而获得，其中L是可容易地亲核取代的离去基团。 化合物I非常适合作为具有用于梗死预防和梗塞治疗的心脏保护组分和用于治疗心绞痛的抗焦虑药物，其中它们还预防性地抑制或大大降低在缺血诱导的损伤形成期间的病理生理过程。 此外，它们通过对细胞增殖的强抑制作用而不同。 因此，它们可以用作抗动脉粥样硬化，抗晚发性糖尿病并发症，癌症和纤维化疾病如肺纤维化，肝纤维化或肾纤维化的药物。 它们是细胞钠/质子反转录酶（Na + / H +交换剂）的有效抑制剂。

    Triaza- and tetraaza-anthracenedione derivatives, their preparation and their use as pharmaceuticals
    58.
    发明授权
    Triaza- and tetraaza-anthracenedione derivatives, their preparation and their use as pharmaceuticals 有权
    三氮杂和四氮杂蒽醌二酮衍生物，其制备及其作为药物的用途

    公开(公告)号：US07132536B2

    公开(公告)日：2006-11-07

    申请号：US10829064

    申请日：2004-04-21

    申请人： Andreas Weichert ,  Hartmut Strobel ,  Paulus Wohlfart ,  Marcel Patek ,  Martin Smrcina ,  Aleksandra Weichsel

    发明人： Andreas Weichert ,  Hartmut Strobel ,  Paulus Wohlfart ,  Marcel Patek ,  Martin Smrcina ,  Aleksandra Weichsel

    IPC分类号： C07D471/14

    CPC分类号： C07D471/14 ,  C07D487/04

    摘要： The present invention relates to triaza- and tetraaza-anthracenedione derivatives of the formula I, wherein A, B and R1 to R5 are as defined herein. The compounds of formula I are valuable pharmacologically active compounds. They are useful in the treatment of various disease states including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency. They upregulate the expression of the enzyme endothelial nitric oxide (NO) synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

    摘要翻译： 本发明涉及式I的三氮杂和四氮杂蒽并二酮衍生物，其中A，B和R 1至R 5如本文所定义。 式I的化合物是有价值的药理活性化合物。 它们可用于治疗各种疾病状态，包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全。 它们上调酶内皮一氧化氮（NO）合酶的表达，并且可以在需要所述酶的增加的表达或增加的NO水平或降低的NO水平的归一化的条件下应用。 本发明还涉及式I化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。