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101.发明授权Substituted anthranilic acids, their use as a medicament or diagnostic, and medicament comprising them, and a pharmaceutical combination preparation containing a sodium/hydrogen exchange (NHE) blocker 失效取代的邻氨基苯甲酸，它们作为药物或诊断剂的用途，以及包含它们的药物和含有钠/氢交换（NHE）阻断剂的药物组合制剂公开(公告)号：US06593352B2
公开(公告)日：2003-07-15
申请号：US10003282
申请日：2001-12-06
申请人： Andreas Weichert , Hans-Willi Jansen , Heinz-Werner Kleemann , Hans-Jochen Lang , Hartmut Rütten
发明人： Andreas Weichert , Hans-Willi Jansen , Heinz-Werner Kleemann , Hans-Jochen Lang , Hartmut Rütten
IPC分类号： C07C31139
CPC分类号： C07D213/42 , C07C311/39 , C07D307/52 , C07D333/20
摘要： Substituted anthranilic acids of the formula I their use as a medicament or diagnostic, and medicament comprising them, and a pharmaceutical combination preparation containing a sodium/hydrogen exchange (NHE) blocker.
摘要翻译： 式Itheir的取代的邻氨基苯甲酸用作药物或诊断剂，以及包含它们的药物，以及含有钠/氢交换（NHE）阻断剂的药物组合制剂。
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102.发明授权Five-membered heterocycles having biphenylsulfonyl substitution, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them 失效具有联苯磺酰基取代的五元杂环，其制备方法，它们作为药物或诊断剂的用途，以及包含它们的药物公开(公告)号：US06486189B2
公开(公告)日：2002-11-26
申请号：US09984469
申请日：2001-10-30
申请人： Heinz-Werner Kleemann , Hans Jochen Lang , Jan-Robert Schwark , Andreas Weichert , Sabine Faber , Hans-Willi Jansen
发明人： Heinz-Werner Kleemann , Hans Jochen Lang , Jan-Robert Schwark , Andreas Weichert , Sabine Faber , Hans-Willi Jansen
IPC分类号： A61K314164
CPC分类号： C07D233/64 , A01N1/02 , A01N1/0205 , C07D233/68 , C07D233/70 , C07D233/84 , C07D233/90
摘要： Five-membered heterocycles having biphenylsulfonyl substitution, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them. Compounds of the formula I in which the symbols have the meanings indicated in the claims, have outstanding antiarrhythmic properties and exhibit a cardioprotective component. They can preventively inhibit or greatly decrease the pathophysiological processes in the formation of ischemically induced damage, in particular in the elicitation of ischemically induced cardiac arrhythmias. Moreover, they have a potent inhibitory action on the proliferation of cells.
摘要翻译： 具有联苯磺酰基取代的五元杂环，其制备方法，它们作为药物或诊断剂的用途，以及包含它们的药物。 符号具有权利要求书中所示含义的式Iin化合物具有突出的抗心律不齐特性并显示心脏保护成分。 它们可以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，特别是引发缺血诱导的心律失常。 此外，它们对细胞增殖具有有效的抑制作用。
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103.发明授权Diacyl-substituted guanidines, a process for their preparation, their use as medicine or diagnostic aid, and medicine containing them 失效二酰基取代的胍胺，它们的制备方法，它们作为药物或诊断助剂的用途以及含有它们的药物公开(公告)号：US06436999B1
公开(公告)日：2002-08-20
申请号：US08837460
申请日：1997-04-18
申请人： Heinz-Werner Kleemann , Hans-Jochen Lang , Andreas Weichert , Peter Crause , Wolfgang Scholz , Udo Albus , Jan-Robert Schwark
发明人： Heinz-Werner Kleemann , Hans-Jochen Lang , Andreas Weichert , Peter Crause , Wolfgang Scholz , Udo Albus , Jan-Robert Schwark
IPC分类号： A01N3252
CPC分类号： C07D295/155 , C07C279/22 , C07C317/44 , C07C2601/04 , C07C2601/08 , C07D215/54 , C07D231/12 , C07D233/56 , C07D249/08
摘要： Diacyl-substituted guanidines of the formula I are described where X(1) and X(2) are as defined herein. The compounds are suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventitive manner the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias.
摘要翻译： 在本文定义的X（1）和X（2）区域中描述的式I的二酰基取代的胍。 该化合物适合用作抗心律失常药物，其具有用于预防和治疗梗死的心脏保护成分，并用于治疗心绞痛，并与之抑制或强烈地减少，以预防方式与发生相关的病理生理过程 缺血诱导的损伤，特别是与缺血诱发的心律失常的引发有关。
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104.发明授权Biphenylsulfonyl cyanamides, method for the production thereof and their utilization as a medicament 有权联苯磺酰氰胺，其制备方法及其作为药物的利用公开(公告)号：US06369069B1
公开(公告)日：2002-04-09
申请号：US09601630
申请日：2000-08-04
申请人： Heinz-Werner Kleemann , Hans-Jochen Lang , Jan-Robert Schwark , Andreas Weichert , Sabine Faber , Hans-Willi Jansen , Stefan Petry
发明人： Heinz-Werner Kleemann , Hans-Jochen Lang , Jan-Robert Schwark , Andreas Weichert , Sabine Faber , Hans-Willi Jansen , Stefan Petry
IPC分类号： A61K31435
CPC分类号： C07C311/47 , C07C311/37 , C07C311/46 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10
摘要： The invention relates to compounds of the formula (I), in which the symbols have the following meaning: R(1) is 1. alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms; 2. alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, in which one to all hydrogen atoms are replaced by fluorine; 3. alkenyl having 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12 carbon atoms; or 4. —CnH2n−nn—Y, nn is zero or 2; and n is zero, 1, 2, 3 or 4; where n is unequal to zero or 1 if nn is equal to 2; 5. —CnH2n−nn—Y, nn is zero or 2; and n is 1, 2, 3 or 4; where n is unequal to 1 if nn is equal to 2.
摘要翻译： 本发明涉及式（I）化合物，其中符号具有以下含义：R（1）是1。 具有1,2,3,4,5,6,7或8个碳原子的烷基; 2。 具有1,2,3,4,5,6,7或8个碳原子的烷基，其中全部氢原子被氟取代; 3。 具有2个，3个，4个，5个，6个，7个，8个，9个，10个，11个或12个碳原子的链烯基; or4。 -CnH 2 n -nn-Y，nn为0或2; andn为零，1,2,3或4; 其中n不等于零，如果nn等于2，则为1; 5。 -CnH 2 n -nn-Y，nn为0或2; andn是1,2,3或4; 如果n n等于2，则n不等于1。
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105.发明授权Substituted 4-benzylaminoquinolines and their hetero analogs, process for their preparation, pharmaceuticals containing these compounds and use thereof 有权取代的4-苄基氨基喹啉及其杂类似物，其制备方法，含有这些化合物的药物及其用途公开(公告)号：US06339077B1
公开(公告)日：2002-01-15
申请号：US09667668
申请日：2000-09-22
IPC分类号： A61K3158
CPC分类号： C07J43/003 , C07J9/005 , C07J41/0055 , C07J41/0061
摘要： The invention relates to substituted 4-benzylaminoquinolines and their hetero analogs, and to the pharmaceutically acceptable salts and physiologically functional derivatives thereof. Compounds of formula I in which the radicals are defined in the specification, and their physiologically tolerated salts, physiologically functional derivatives and processes for their preparation are described. The compounds are suitable, for example, as medicines for the prophylaxis or treatment of gallstones.
摘要翻译： 本发明涉及取代的4-苄基氨基喹啉及其杂类似物，以及其药学上可接受的盐和生理功能衍生物。 描述了本说明书中定义的基团的式Iin化合物及其生理上耐受的盐，生理功能衍生物及其制备方法。 该化合物例如可用作预防或治疗胆结石的药物。
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106.发明授权Five-membered heterocycles having biphenylsulfonyl substitution, with sulfonylcyanamide side chain, compositions containing them, and methods of using them 失效具有联苯基磺酰基取代的五元杂环，含磺酰胺酰胺侧链，含有它们的组合物及其使用方法公开(公告)号：US06335451B1
公开(公告)日：2002-01-01
申请号：US09010181
申请日：1998-01-21
申请人： Heinz-Werner Kleemann , Hans Jochen Lang , Jan-Robert Schwark , Andreas Weichert , Sabine Faber , Hans-Willi Jansen
发明人： Heinz-Werner Kleemann , Hans Jochen Lang , Jan-Robert Schwark , Andreas Weichert , Sabine Faber , Hans-Willi Jansen
IPC分类号： C07D23364
CPC分类号： C07D233/64 , A01N1/02 , A01N1/0205 , C07D233/68 , C07D233/70 , C07D233/84 , C07D233/90
摘要： Five-membered heterocycles having biphenylsulfonyl substitution, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them. Compounds of the formula I in which the symbols have the meanings indicated in the claims, have outstanding antiarrhythmic properties and exhibit a cardioprotective component. They can preventively inhibit or greatly decrease the pathophysiological processes in the formation of ischemically induced damage, in particular in the elicitation of ischemically induced cardiac arrhythmias. Moreover, they have a potent inhibitory action on the proliferation of cells.
摘要翻译： 具有联苯磺酰基取代的五元杂环，其制备方法，它们作为药物或诊断剂的用途，以及包含它们的药物。 符号具有权利要求书中所示含义的式Iin化合物具有突出的抗心律不齐特性并显示心脏保护成分。 它们可以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，特别是引发缺血诱导的心律失常。 此外，它们对细胞增殖具有有效的抑制作用。
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107.发明授权4-fluoroalkyl-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing them 失效4-氟烷基取代的苯甲酰基胍，其制备方法，它们作为药物或诊断剂的用途，以及含有它们的药物
公开(公告)号：US6156800A
公开(公告)日：2000-12-05
申请号：US108126
申请日：1998-06-22
申请人： Andreas Weichert , Joachim Brendel , Heinz-Werner Kleemann , Hans Jochen Lang , Jan-Robert Schwark , Wolfgang Scholz , Udo Albus
发明人： Andreas Weichert , Joachim Brendel , Heinz-Werner Kleemann , Hans Jochen Lang , Jan-Robert Schwark , Wolfgang Scholz , Udo Albus
IPC分类号： A61K49/00 , A01N1/02 , A61K31/155 , A61K31/165 , A61K31/18 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P41/00 , C07C303/40 , C07C311/16 , C07C315/04 , C07C317/44 , C07C279/22
CPC分类号： C07C317/44
摘要： There are described benzoylguanidines of the formula I ##STR1## where R(1) is R(4)--SO.sub.m, R(5)R(6)N--SO.sub.2 --; O.sub.p --(CH.sub.2).sub.q --(CF.sub.2).sub.r --CF.sub.3 ; --SR(10), --OR(10) or --CR(10)R(11)R(12); R(2) is --(CH.sub.2).sub.u --(CF.sub.2).sub.t --CF.sub.3 ; R(3) is hydrogen or independently defined as R(1); and their pharmaceutically tolerable salts. They are obtained by reaction of a compound of the formula II ##STR2## with guanidine. They are compounds of outstanding activity on the cardiovascular system.
摘要翻译： 描述式I的苯甲酰基胍，其中R（1）是R（4）-SOm，R（5）R（6）N-SO 2 - ; （CH2）q-（CF2）r-CF3; -SR（10），-OR（10）或-CR（10）R（11）R（12）; R（2）为 - （CH 2）u - （CF 2）t -CF 3; R（3）为氢或独立地定义为R（1）; 及其药学上可耐受的盐。 它们通过式II的化合物与胍的反应获得。 它们是心血管系统突出活性的化合物。
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108.发明授权Basically-substituted benzoylguanidines, a process for preparing them, their use as a medicament or diagnostic agent, and a medicament containing them 失效基本取代的苯甲酰胍，其制备方法，它们作为药物或诊断剂的用途，以及含有它们的药物
公开(公告)号：US6057322A
公开(公告)日：2000-05-02
申请号：US903438
申请日：1997-07-30
申请人： Heinz-Werner Kleemann , Hans-Jochen Lang , Jan-Robert Schwark , Andreas Weichert , Wolfgang Scholz , Udo Albus
发明人： Heinz-Werner Kleemann , Hans-Jochen Lang , Jan-Robert Schwark , Andreas Weichert , Wolfgang Scholz , Udo Albus
IPC分类号： C07C311/29 , C07C311/64 , C07C317/28 , C07C317/46 , C07C323/16 , C07C335/32 , C07C381/10 , C07D207/09 , C07D213/40 , C07D213/70 , C07D215/36 , C07D233/54 , C07D233/84 , C07D235/28 , C07D521/00 , A61K31/18 , A61K31/165 , A61K31/445 , A61K31/47
CPC分类号： C07D213/40 , C07C311/29 , C07C311/64 , C07C317/28 , C07C317/46 , C07C323/16 , C07C335/32 , C07C381/10 , C07D207/09 , C07D213/70 , C07D215/36 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/84 , C07D235/28 , C07D249/08 , Y10S514/821 , Y10S514/866 , Y10S514/921
摘要： Compounds of the formula I ##STR1## and the pharmaceutically tolerated salts thereof, are described. A process for their preparation and their use as medicaments in cardiovascular diseases are also described.
摘要翻译： 描述式I化合物及其药学上可耐受的盐。 还描述了其制备方法及其作为心血管疾病药物的用途。
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109.发明授权Phenyl.-substituted alkenylcarboguanidides carrying perfluoroalkyl groups, a process for their preparation, their use as a medicament or diagnostic agent, and also a medicament containing them 失效携带全氟烷基的苯基取代的烯基羧基胍，其制备方法，它们作为药物或诊断剂的用途，以及含有它们的药物
公开(公告)号：US6025349A
公开(公告)日：2000-02-15
申请号：US118914
申请日：1998-07-20
申请人： Jan-Robert Schwark , Heinz-Werner Kleemann , Hans-Jochen Lang , Andreas Weichert , Wolfgang Scholz , Udo Albus
发明人： Jan-Robert Schwark , Heinz-Werner Kleemann , Hans-Jochen Lang , Andreas Weichert , Wolfgang Scholz , Udo Albus
IPC分类号： A61K31/165 , A01N1/02 , A61K31/16 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P31/04 , A61P35/00 , A61P37/08 , C07C277/08 , C07C279/22 , C07C233/64
CPC分类号： C07C279/22 , Y10S514/821 , Y10S514/921
摘要： Phenyl-substituted alkenylcarboguanidides carrying perfluoroalkyl groups, a process for their preparation, their use as a medicament or diagnostic agent, and also a medicament containing them.Phenyl-substituted alkenylcarboguanidides carrying perfluoroalkyl groups, of the formula I ##STR1## in which the substituents have the meanings stated in the description, and their pharmaceutically suitable salts, are described. They are obtained by reacting a compound II ##STR2## with guanidine, in which R(1) to R(5) and R(A), R(B), R(C) and R(D) have the stated meaning, and L is a leaving group which easily undergoes nucleophilic substitution. Compounds I are excellent cardiovascular therapeutic agents.
摘要翻译： 带有全氟烷基的苯基取代的烯基羧基胍，其制备方法，它们作为药物或诊断剂的用途，以及含有它们的药物。 描述了具有其中取代基具有说明书中所述含义的式I的具有全氟烷基的苯基取代的烯基羧酰基苷及其药学上合适的盐。 其中R（1）至R（5）和R（A），R（B），R（C）和R（D）具有所定义的化合物II与胍反应得到，L为 一个容易进行亲核取代的离去基团。 化合物I是优异的心血管治疗剂。
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110.发明授权Substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing them 失效取代的苯甲酰胍，其制备方法，它们作为药物或诊断用途以及含有它们的药物
公开(公告)号：US5880156A
公开(公告)日：1999-03-09
申请号：US898889
申请日：1996-01-30
IPC分类号： A61K31/165 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , C07C277/08 , C07C279/22 , C07C311/15 , C07C317/44 , C07C317/46 , C07C323/62 , C07D241/28 , C07C233/77 , C07C321/24
CPC分类号： C07C279/22 , C07C317/46
摘要： Substituted benzoylguanidines, process for their preparation, their use as a pharmaceutical or diagnostic, and pharmaceutical containing them Benzoylguanidines of the formula I ##STR1## are described in which: R(1), R(2), R(3), R(4) are as defined in the specification, and pharmaceutically tolerated salts thereof.
摘要翻译： 描述了其中：R（1），R（2），R（3），R（3），（R） 4）如说明书中所定义，及其药学上可耐受的盐。
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