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1.发明公开N-((3-OXO-2,3-DIHYDRO-1H-ISOINDOL-1-YL)ACETYL)GUANIDINE DERIVATIVES AS NHE1-INHIBITORS FOR THE TREATMENT OF INFARCTION AND ANGINA PECTORIS 有权N - （（3-氧代-2,3-二氢-1H-异吲哚-1-基）乙酰基）胍衍生物作为NHE1抑制剂用于治疗心绞痛的梗塞的治疗和
公开(公告)号：EP1528923A1
公开(公告)日：2005-05-11
申请号：EP03730076.1
申请日：2003-05-20
发明人： KLEEMANN, Heinz-Werner , HOFMEISTER, Armin , CARRY, Jean-Christophe , MIGNANI, Serge , BIGOT, AntonyCentre de recherche de Paris , RONAN, Baptiste
IPC分类号： A61K31/4035 , A61K31/155 , C07D209/46 , C07C279/20 , C07C277/08
CPC分类号： C07D209/46
摘要： Isoindolone derivatives, preparation process and intermediates of this process, their use as medicaments, and pharmaceutical compositions comprising them. The present invention relates to the novel isoindolone derivatives of the Formula (I), in which R1 to R6 have the meanings stated in the claims. The inventive compounds are suitable as antiarrhythmic medicaments with a cardioprotective component for infarction prophylaxis and infarction treatment and for the treatment of angina pectoris. They also inhibit in a preventive manner the pathophysiological processes associated with the development of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias and of heart failure.
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2.发明授权ARYLIERTE FURAN- UND THIOPHENCARBONSAUREAMIDE MIT KALIUM KANAL BLOCKIERENDER WIRKUNG 有权芳基化呋喃和THIOPHENCARBONSAUREAMIDE钾通道阻断作用
公开(公告)号：EP1349846B1
公开(公告)日：2005-02-09
申请号：EP01985832.3
申请日：2001-11-29
IPC分类号： C07D307/68 , C07D333/38 , A61K31/38 , A61K31/34 , A61P9/06
CPC分类号： C07D333/38 , A61K31/34 , A61K31/38 , C07D307/68 , A61K2300/00
摘要： The invention relates to arylated furane and thiophene carboxylic acid amides, a method for the production thereof, the use thereof as medicaments, in addition to pharmaceutical preparations containing the compounds of formula (Ia) and (Ib) wherein X, R(1), R(2), R(3), R(4), R(5), R(6), R(7), R(30) and R(31) have the same meaning as cited in the claims. According to the invention, the compounds are particularly suitable as novel anti-arrhythmic active ingredients, particularly for the treatment and prophylaxis of atrial arrhythmia for example, atrial fibrillation, AF, or atrial flutter.
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3.发明公开MERCAPTOACETYLAMIDE DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND THEIR USE 有权MERCAPTOACETYLAMID衍生物，以制作工艺及其用途
公开(公告)号：EP1381605A1
公开(公告)日：2004-01-21
申请号：EP02732549.7
申请日：2002-04-03
发明人： FLYNN, Gary, A. , MEHDI, Shujaath , KOEHL, Jack, Roger , ANDERSON, Barbara, Ann , GERKEN, Manfred , JABLONKA, Bernd , KLEEMANN, Heinz-Werner , LINZ, Wolfgang , SEIZ, Werner , SEURING, Bernhard
IPC分类号： C07D471/04 , A61K31/55 , A61P9/04
CPC分类号： C07D471/04
摘要： This invention discloses and claims a series of mercaptoacetylamide derivatives of formula (I). Also disclosed and claimed are pharmaceutical compositions incorporating these compounds and processes for preparing said compounds. The use of said compounds for inhibition of the enzymes angiotensin converting enzyme and neutral endopeptidase, and for the treatment of hypertension and congestive heart failure are also disclosed and claimed.
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4.发明公开IMIDAZOLDERIVATE MIT BIPHENYLSULFONYLSUBSTITUTION, VERFAHREN ZU IHRER HERSTELLUNG, IHRE VERWENDUNG ALS MEDIKAMENT ODER DIAGNOSTIKUM 有权有BIPHENYLSULFONYLSUBSTITUTION，PROCESS FOR THEIR咪唑衍生物，它们作为药物或诊断
公开(公告)号：EP1097141A1
公开(公告)日：2001-05-09
申请号：EP99938222.9
申请日：1999-07-10
发明人： KLEEMANN, Heinz-Werner , LANG, Hans, Jochen , SCHWARK, Jan-Robert , PETRY, Stefan , WEICHERT, Andreas
IPC分类号： C07D233/70 , C07D233/88 , A61K31/4164
CPC分类号： C07D233/70 , C07D233/88
摘要： The invention relates to compounds of formula (I), wherein the symbols have the meanings indicated in the specification. The inventive compounds exhibit dramatic antiarrhythmic proprieties and contain a cardioprotective compound. They can preventively inhibit or strongly reduce pathophysiologic processes upon occurrence of ischemic injuries, especially ischemic cardiac arrhythmia. Said compounds also exhibit a strong inhibiting effect on cellular proliferation.
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5.发明授权ORTHO-SUBSTITUIERTE STICKSTOFFHALTIGE BISARYLVERBINDUNGEN ZUR VERWENDUNG ALS KALIUM-KANAL-INHIBITOREN 有权邻位取代的含氮BISARYLVERBINDUNGEN用作钾通道阻断剂
公开(公告)号：EP1341764B1
公开(公告)日：2005-06-15
申请号：EP01999558.8
申请日：2001-11-24
IPC分类号： C07D213/81 , C07D213/82 , C07D241/24 , C07D213/56 , C07D401/12 , C07D413/12 , A61K31/497 , A61P9/06
CPC分类号： C07D213/81 , C07D213/56 , C07D213/82 , C07D241/24 , C07D401/12 , C07D413/12
摘要： Compounds of formula (I) wherein A1 - A8, R(1), R(2), R(3), R(4), R(30) and R(31) have the meanings cited in the claims. Said compounds are particularly suitable for use as novel antiarrythmic substances, especially in the treatment and prophylaxis of atrial arrhythmia, for example, atrial fibrillation (AF) or atrial flutter.
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6.发明公开ANTHRANILSÄUREAMIDE, VERFAHREN ZU IHRER HERSTELLUNG, IHRE VERWENDUNG ALS ANTIARRHYTHMIKA SOWIE PHARMAZEUTISCHE ZUBEREITUNGEN DAVON 有权邻氨基，PROCESS FOR THEIR，它们的使用抗心律不齐药物及其制备物
公开(公告)号：EP1385820A1
公开(公告)日：2004-02-04
申请号：EP02742898.6
申请日：2002-04-13
发明人： BRENDEL, Joachim , PIRARD, Bernard , PEUKERT, Stefan , KLEEMANN, Heinz-Werner , HEMMERLE, Horst
IPC分类号： C07C311/21 , C07C311/29 , C07D213/56 , C07C311/08 , C07D233/64 , C07D235/16 , C07D307/54 , C07D277/30 , C07D215/14 , C07D231/12 , A61K31/18
CPC分类号： C07D207/335 , C07C311/08 , C07C311/21 , C07C311/29 , C07C311/44 , C07C2601/02 , C07C2601/14 , C07D213/40 , C07D213/64 , C07D215/12 , C07D231/12 , C07D231/16 , C07D233/56 , C07D233/64 , C07D235/14 , C07D249/08 , C07D277/28 , C07D307/14 , C07D307/52 , C07D405/12
摘要： The invention relates to anthranilic acid amides, to a method for the production thereof, to their use as a medicament, and to pharmaceutical preparations containing these anthranilic acid amides. The anthranilic acid amides consist of compounds of formula (I) in which R(1) to (R7) have the meanings as cited in the claims, act upon the Kv1.5 potassium channel, and inhibit a potassium stream described as an 'ultra-rapidly activating delayed rectifier' in the human cardiac atrium. The compounds are therefore especially suited as novel antiarrhythmic active substances, particularly for treating and preventing atrial arrhythmias, e.g. atrial fibrillation AF or atrial flutter.
摘要翻译： 本发明涉及式I的邻氨基苯甲酰胺，其中R（1）〜R（7）的含义为在中，其制备方法，它们作为药物的用途以及含有它们的药物制剂。 这些化合物作用于对Kv1.5钾通道和抑制钾电流的所有其通过被称为在人类心脏的心房超快速激活延迟整流。 的化合物是适于用作用于治疗THEREFORE新颖抗心律不齐剂和房性心律失常的预防（例如，心房纤维性颤动（AF）或心房扑动）。
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7.发明公开SUBSTITUIERTE BENZOYLGUANIDINE, VERFAHREN ZU IHRER HERSTELLUNG, IHRE VERWENDUNG ALS MEDIKAMENT ODER DIAGNOSTIKUM SOWIE SIE ENTHALTENDES MEDIKAMENT 有权替补benzoylguanidines，工艺所周之，及其作为药物或诊断和药物含
公开(公告)号：EP1259481A1
公开(公告)日：2002-11-27
申请号：EP01900139.5
申请日：2001-01-08
发明人： WEICHERT, Andreas , ALBUS, Udo , JANSEN, Hans-Willi , KLEEMANN, Heinz-Werner , LANG, Hans-Jochen
IPC分类号： C07C279/22 , C07D233/64 , C07D249/02 , A61K31/41 , A61P9/10
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： The invention relates to benzoylguanidines of formula (I), wherein R2 stands for -Y-p-(C6H4)-R11, -Y-m-(C6-H4)-R11 or -Y-o-(C6H4)-R11; R11 represents (C1-C9)-heteroaryl, which is bonded by C or N and is substituted or unsubstituted with 1 to 3 substituents selected from the group consisting of F, Cl, CF3, CH3, methoxy, hydroxy, amino, methylamino, dimethylamino and benzyl; Y represents oxygen, -S- or NR12; R12 represents H or (C1-C4)-alkyl; R4 F, Cl, Br, I or C1-C4-alkyl; R1 and R3 are defined as per the claims. Said benzoylguanidines are suitable for use as anti-arrhythmic medicaments containing cardioprotective components for the prophylaxis and treatment of infarcts and for the treatment of angina pectoris. They also preventively inhibit the pathophysiological processes associated with the origination of defects caused by ischaemia, in particular during the triggering of ischaemically induced cardiac arrhythmia.
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8.发明公开HETEROCYCLISCH SUBSTITUIERTE BENZOYLGUANIDINE UND IHRE VERWENDUNG ALS NHE-INHIBITOREN 审中-公开杂环取代benzoylguanidines及其作为NHE抑制剂
公开(公告)号：EP1226124A1
公开(公告)日：2002-07-31
申请号：EP00966135.6
申请日：2000-10-07
发明人： WEICHERT, Andreas , ALBUS, Udo , JANSEN, Hans-Willi , KLEEMANN, Heinz-Werner , LANG, Hans-Jochen
IPC分类号： C07D233/54 , C07D235/06 , A61K31/4164 , A61P9/00
CPC分类号： C07D235/06 , C07D231/12 , C07D233/56 , C07D249/08
摘要： The invention relates to heterocyclically substituted benzoylguanidine of formula (I), wherein the substituents R(1) to R(4) have the meanings given in the claims. These compounds (I) are suitable for use as anti-arrhythmic medicaments containing a cardio-protective component for infarct prophylaxis and infarct treatment and for the treatment of angina pectoris. The benyozlguanadines also preventively inhibit the pathophysiological processes arising from ischaemically induced traumas, in particular during the triggering of ischaemically induced cardiac arrhythmia.
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9.发明公开SUBSTITUIERTE SULFONYLCYANAMIDE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS MEDIKAMENT 有权取代SULFONYLCYANAMIDE，用于生产及其作为药物
公开(公告)号：EP1076651A1
公开(公告)日：2001-02-21
申请号：EP99948554.3
申请日：1999-04-30
发明人： WEICHERT, Andreas , LANG, Hans, Jochen , PETRY, Stefan , SCHWARK, Jan-Robert , KLEEMANN, Heinz-Werner , FABER, Sabine , JANSEN, Hans-Willi
IPC分类号： C07D233/90 , C07D233/68 , A61K31/415
CPC分类号： C07D233/90 , C07C311/16 , C07D233/68
摘要： The invention relates to compounds of formula (I) in which the symbols have the meanings given in the claims. Said compounds are inhibitors of the sodium-dependent bicarbonate/chloride ion exchanger which can be used as medicines for the prophylaxis or treatment of a wide range of diseases, for example the treatment and/or prophylaxis of myocardial infarction, angina pectoris, diseases caused by ischaemia, impaired respiration, cardiac ischaemia, ischaemia of the peripheral and central nervous system and stroke, ischaemia of the peripheral organs and limbs and diseases in which cell proliferation is a primary or secondary cause, in the treatment of shock, during surgical interventions and organ transplants or for preserving and storing transplants to be used in surgical interventions.
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10.发明公开BIPHENYLSULFONYLCYANAMIDE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS MEDIKAMENT 有权BIPHENYLSULFONYLCYANAMIDE，生产方法及其作为药物
公开(公告)号：EP1053224A1
公开(公告)日：2000-11-22
申请号：EP99913138.6
申请日：1999-02-04
发明人： KLEEMANN, Heinz-Werner , LANG, Hans-Jochen , SCHWARK, Jan-Robert , WEICHERT, Andreas , FABER, Sabine , JANSEN, Hans-Willi , PETRY, Stefan
IPC分类号： C07C311/46 , C07C311/37 , C07D333/24 , C07D333/60 , C07D209/18 , A61K31/18
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 formula (I) in which the symbols have the meanings given in the description. The compounds have excellent antiarrhythmic properties and comprise a cardioprotective component. The inventive compounds can preventively inhibit or strongly reduce the pathophysiological processes when ischaemic induced damages arise, especially during the onset of ischaemic induced cardiac arrhythmias. In addition, the inventive compounds have a strong inhibiting effect on the proliferation of cells.
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