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    3,5-Substituted benzoylguanidines, process for their preparation, their use as a medicament of diagnostic and medicament containing them
    17.
    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。

    Arylcarbonylaminoalkyl-dihydro-oxo-pyridines, their production and their use
    18.
    发明授权
    Arylcarbonylaminoalkyl-dihydro-oxo-pyridines, their production and their use 失效
    芳基羰基氨基烷基 - 二氢 - 氧代 - 吡啶，其生产及其用途

    公开(公告)号：US5360808A

    公开(公告)日：1994-11-01

    申请号：US19296

    申请日：1993-02-18

    申请人： Heinrich Englert ,  Dieter Mania ,  David Wettlaufer ,  Erik Klaus

    发明人： Heinrich Englert ,  Dieter Mania ,  David Wettlaufer ,  Erik Klaus

    IPC分类号： A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4425 ,  A61P9/00 ,  A61P21/00 ,  C07D213/64 ,  C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D213/89 ,  C07D401/12

    CPC分类号： C07D213/80 ,  C07D213/81 ,  C07D401/12

    摘要： Arylcarbonylaminoalkyl-dihydro-oxo-pyridines of Formula I ##STR1## are disclosed wherein aryl is an aromatic or heteroaromatic system, n is zero through 5; R and R(1), are hydrogen, or loweralkyl; W is hydrogen, (hetero)-(aryl)-loweralkyl; Z is hydrogen, CH.sub.2 OR(2.sub.), CHO, (CO)OR(2), (CO)NR(2).sub.2.Processes for the preparation of compound I are also disclosed.Compounds I are suitable for the treatment of disorders of the cardiovascular system, for example of hypertension, of cardiac insufficiency or of disturbances of blood flow in the coronary systems such as, for example, angina. Disturbances of cerebral and peripheral blood flow are likewise influenced beneficially. Furthermore, compounds I are able to influence smooth-muscle organs such as uterus, bronchi, intestines and biliary system, the urinary tract (ureter, bladder and urethra) in the sense of spasmolysis. They are therefore also suitable for the treatment of diseases associated with spasms of these organs, for example for the treatment of premature labor in pregnancy, of ureteral or biliary colic, of obstructive airway diseases such as asthma, of disturbances of intestinal motility such as, for example, of irritable colon or of bladder incontinence. Additionally, compounds of formula 1 can serve as anticonvulsants in the treatment of epilepsy.

    摘要翻译： 公开了式I的芳基羰基氨基烷基 - 二氢 - 氧代 - 吡啶，其中芳基是芳族或杂芳族体系，n为0至5; R和R（1）是氢或低级烷基; W是氢，（杂） - （芳基） - 低级烷基; Z是氢，CH2OR（2），CHO，（CO）OR（2），（CO）NR（2）2。 还公开了制备化合物I的方法。 化合物I适用于治疗冠状动脉系统（例如心绞痛）的心脏功能不全或血液流动紊乱的心血管系统疾病，例如高血压。 脑和周围血流紊乱同样受到有利影响。 此外，化合物I能够影响平滑肌器官如子宫，支气管，肠和胆汁系统，尿道（输尿管，膀胱和尿道）在解剖意义上。 因此，它们也适用于治疗与这些器官的痉挛有关的疾病，例如用于治疗怀孕期间的输尿管或胆道绞痛，阻塞性气道疾病如哮喘，肠蠕动紊乱， 例如，肠易激综合症或膀胱失禁。 此外，式1的化合物可用作治疗癫痫的抗惊厥药。

    Amino-substituted benzoylguanidines, process for their preparation, their use as a medicament and medicament containing them
    19.
    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。