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91. 发明授权

US5602127A (Alkanesultam-1-yl)-benzimidazol-1-yl)-1yl)-methyl-biphenyls useful as angiotensin-II antagonists 失效
标题翻译：（烷基磺酰基-1-基） - 苯并咪唑-1-基）-1-基） - 甲基 - 联苯作为血管紧张素II拮抗剂
公开(公告)号：US5602127A
公开(公告)日：1997-02-11
申请号：US456978
申请日：1995-06-01
申请人： Norbert Hauel , Berthold Narr, deceased , Uwe Ries , Jacobus C. A. van Meel , Wolfgang Wienen , Michael Entzeroth
发明人： Norbert Hauel , Berthold Narr, deceased , Uwe Ries , Jacobus C. A. van Meel , Wolfgang Wienen , Michael Entzeroth
IPC分类号： A61K31/415 , A61K31/42 , C07D235/08 , C07D235/24 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04 , C07D521/00 , A61K31/54 , C07D279/02
CPC分类号： A61K31/415 , A61K31/42 , C07D231/12 , C07D233/56 , C07D235/08 , C07D235/24 , C07D249/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： Angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo [1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An exemplary compound is: 4'-[(2-n-propyl-4-methyl-6-(butanesultam-1-yl)benzimidazol-1-yl)-methyl]-biphenyl-2-carboxylic acid.
摘要翻译：其中R1不是氢，尤其是卤素，低级烷基或环烷基;式 R2尤其是任选取代的苯并咪唑-2-基，5,6,7,8-四氢 - 咪唑并[1,2-a]吡啶-2-基，丁磺酰-1-基，咪唑-4-基，和四氢苯并咪唑-2-基; R3尤其是低级烷基; R4是酸性基团，例如羧基或四唑基。示例性的化合物是4' - [（2-正丙基-4-甲基-6-（丁内酰胺-1-基）苯并咪唑-1-基） - 甲基] - 联苯-2-羧酸。

92. 发明授权

US5587393A Benzimidazoles, pharmaceutical compositions containing these compounds and processes for preparing them 失效
公开(公告)号：US5587393A
公开(公告)日：1996-12-24
申请号：US299693
申请日：1994-09-01
申请人： Berthold Narr , Norbert Hauel , Jacques Van Meel , Wolfgang Wienen , Michael Entzeroth , Uwe Ries
发明人： Berthold Narr , Norbert Hauel , Jacques Van Meel , Wolfgang Wienen , Michael Entzeroth , Uwe Ries
IPC分类号： C07D235/08 , C07D403/04 , C07D403/10 , C07D403/14 , A61K31/42 , C07D235/06 , C07D257/04
CPC分类号： C07D403/04 , C07D235/08 , C07D403/10 , C07D403/14
摘要： The invention relates to benzimidazoles of general formula ##STR1## wherein R.sub.1 to R.sub.4 are as defined herein, the 1-, 3-isomer mixtures thereof and the addition salts thereof. The new compounds are useful, in particular, as angiotensin antagonists.

93. 发明授权

US4716169A Imidazo[1,2a]pyridines and their use as cardiotonic agents 失效
标题翻译：咪唑并[1,2a]吡啶并用作强心剂
公开(公告)号：US4716169A
公开(公告)日：1987-12-29
申请号：US810008
申请日：1985-12-17
申请人： Joachim Heider , Norbert Hauel , Volkhard Austel , Klaus Noll , Andreas Bomhard , Jacques van Meel , Willi Diederen
发明人： Joachim Heider , Norbert Hauel , Volkhard Austel , Klaus Noll , Andreas Bomhard , Jacques van Meel , Willi Diederen
IPC分类号： A61K31/435 , A61K31/495 , A61P7/02 , A61P9/04 , C07D471/04 , C07D487/04 , A61K31/41
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to new imidazo derivatives of the formula ##STR1## wherein "A-D and R.sup.1 -R.sup.3 are as defined in the specification". The new compounds have valuable pharmacological properties, particularly antithrombotic and cardiovascular properties such as a cardiotonic activity and/or an effect on blood pressure, and can be prepared using methods known per se.
摘要翻译：本发明涉及式（I）的新的咪唑衍生物，其中“A-D和R 1 -R 3如说明书中所定义”。新化合物具有有价值的药理学性质，特别是抗血栓形成和心血管性质，例如强心剂活性和/或对血压的作用，并且可以使用本身已知的方法制备。

94. 发明授权

US4656171A 2-phenyl-imidazo-pyrazines, useful as cardiotonics 失效
标题翻译： 2-苯基 - 咪唑并吡嗪，可用作强心剂
公开(公告)号：US4656171A
公开(公告)日：1987-04-07
申请号：US675299
申请日：1984-11-27
申请人： Volkhard Austel , Norbert Hauel , Joachim Heider , Manfred Reiffen , Jacobus C. A. Van Meel , Willi Diederen
发明人： Volkhard Austel , Norbert Hauel , Joachim Heider , Manfred Reiffen , Jacobus C. A. Van Meel , Willi Diederen
IPC分类号： A61K31/50 , A61K31/53 , A61P9/02 , A61P9/04 , C07D487/04 , A61K31/495 , C07D471/02
CPC分类号： C07D487/04
摘要： Compounds of the formula ##STR1## wherein A, B, C and D are each independently --N.dbd. or --CH.dbd., provided, however, that at least two of them must be --N.dbd., and when A and C are both --N.dbd., at least one or both of B and D must be --N.dbd.; andR.sub.1, R.sub.2 and R.sub.3 are substituents of diverse types;tautomers thereof; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds are useful as cardiotonics.
摘要翻译：其中A，B，C和D各自独立地为-N =或-CH =，但条件是其中至少两个必须为-N =，并且当A和C均为 - N =，B和D中的至少一个或两个必须为-N =; 并且R1，R2和R3是不同类型的取代基; 互变异构体和无毒的，药学上可接受的酸加成盐。这些化合物可用作强心剂。

95. 发明授权

US4616018A Benzotriazolyl-4,5-dihydro-3(2H)-pyridazinones 失效
标题翻译：苯并三唑基-4,5-二氢-3（2H） - 哒嗪酮
公开(公告)号：US4616018A
公开(公告)日：1986-10-07
申请号：US749580
申请日：1985-06-27
申请人： Norbert Hauel , Volkhard Austel , Joachim Heider , Manfred Reiffen , Willi Diederen , Walter Haarman
发明人： Norbert Hauel , Volkhard Austel , Joachim Heider , Manfred Reiffen , Willi Diederen , Walter Haarman
IPC分类号： A61K31/50 , A61K31/501 , A61P7/02 , A61P9/12 , C07D237/04 , C07D249/18 , C07D401/14 , C07D403/04 , C07D403/02
CPC分类号： C07D401/14 , C07D237/04 , C07D249/18 , C07D403/04 , Y10S514/822
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen; alkyl of 1 to 7 carbon atoms; cycloalkyl of 3 to 7 carbon atoms; monosubstituted alkyl of 1 to 3 carbon atoms, where the substituent is pyridyl, methylpyridyl, phenyl, mono-, di- or trisubstituted phenyl, where the substituents on the phenyl ring, which may be identical to or different from each other, are selected from the group consisting of one amino, one dimethylamino, one to two hydroxyls, one to three methoxys and one to three halogens; .omega.-monosubstituted alkyl of 2 to 4 carbon atoms, where the substituent is hydroxyl or di(alkyl of 1 to 3 carbon atoms)amino; phenyl; monohalo-phenyl; unsubstituted or monosubstituted straight or branched alkanoyl of 1 to 6 carbon atoms, where the substituent is phenyl, methoxyphenyl or cycloalkyl of 3 to 7 carbon atoms; or unsubstituted or monosubstituted phenylsulfonyl, where the substituent is methyl or methoxy; and,R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as cardiotonics, hypotensives and antithrombotics.
摘要翻译：其中R 1是氢的式IMAMA的化合物; 1至7个碳原子的烷基; 3至7个碳原子的环烷基; 其中取代基是吡啶基，甲基吡啶基，苯基，单 - ，二 - 或三取代的苯基，其中可以相同或不同的苯环上的取代基选自由一个氨基，一个二甲基氨基，一至两个羟基，一至三个甲氧基和一至三个卤素组成的组; 2至4个碳原子的ω-单取代的烷基，其中取代基是羟基或二（1至3个碳原子的烷基）氨基; 苯基; 单卤代苯基; 未取代的或单取代的1至6个碳原子的直链或支链烷酰基，其中取代基是苯基，甲氧基苯基或3-7个碳原子的环烷基; 或未取代或单取代的苯基磺酰基，其中取代基是甲基或甲氧基; R2为氢或1〜3个碳原子的烷基; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作强心剂，低血糖剂和抗血栓药物。

96. 发明申请

US20140038977A1 PYRIDAZIN DERIVATIVES AS ANTAGONISTS OF THE BRADYKININ B1 RECEPTOR 有权
标题翻译：作为BRADYKININ B1受体拮抗剂的吡啶衍生物
公开(公告)号：US20140038977A1
公开(公告)日：2014-02-06
申请号：US13816303
申请日：2011-08-19
申请人： Norbert Hauel , Raimund Kuelzer
发明人： Norbert Hauel , Raimund Kuelzer
IPC分类号： C07D405/14
CPC分类号： C07D405/14
摘要： The present invention relates to the compounds of general formula I wherein R1 and R2 are defined as described hereinafter, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the medicaments containing the pharmacologically effective compounds, the preparation thereof and the use thereof.
摘要翻译：本发明涉及通式I的化合物，其中R 1和R 2如下所述定义，其对映异构体，非对映异构体，混合物及其盐，特别是其与有机或无机酸或碱的生理上可接受的盐，其具有有价值的性质，其制备，含有药理学有效化合物的药物，其制备及其用途。

97. 发明授权

US08486398B2 Anticoagulant antidotes comprising antibodies that bind dabigatran and/or related compounds 有权
标题翻译：抗凝血剂解毒剂，其包含结合达比加群和/或相关化合物的抗体
公开(公告)号：US08486398B2
公开(公告)日：2013-07-16
申请号：US13010403
申请日：2011-01-20
申请人： Joanne Van Ryn , John Edward Park , Norbert Hauel , Ulrich Kunz , Tobias Litzenburger , Keith Canada , Sanjaya Singh , Alisa Waterman
发明人： Joanne Van Ryn , John Edward Park , Norbert Hauel , Ulrich Kunz , Tobias Litzenburger , Keith Canada , Sanjaya Singh , Alisa Waterman
IPC分类号： A61K39/395
CPC分类号： C07K16/44 , A61K31/4439 , A61K39/39583 , C07K2317/24 , C07K2317/54 , C07K2317/55 , C07K2317/565 , C07K2317/569 , C07K2317/622 , C07K2317/626 , C07K2317/76 , G01N33/86 , G01N2500/02 , G01N2500/10
摘要： The present invention relates to antibody molecules against anticoagulants, in particular dabigatran, and their use as antidotes of such anticoagulants.
摘要翻译：本发明涉及针对抗凝剂，特别是达比加群的抗体分子，以及它们作为这种抗凝剂的解毒剂的用途。

98. 发明申请

US20120027780A1 ANTICOAGULANT ANTIDOTES 有权
标题翻译：抗生素抗体
公开(公告)号：US20120027780A1
公开(公告)日：2012-02-02
申请号：US13010403
申请日：2011-01-20
申请人： Joanne Van Ryn , John Edward Park , Norbert Hauel , Ulrich Kunz , Tobias Litzenburger , Keith Canada , Sanjaya Singh , Alisa Waterman
发明人： Joanne Van Ryn , John Edward Park , Norbert Hauel , Ulrich Kunz , Tobias Litzenburger , Keith Canada , Sanjaya Singh , Alisa Waterman
IPC分类号： A61K39/395 , A61P7/04 , C12P21/00 , C07K16/00
CPC分类号： C07K16/44 , A61K31/4439 , A61K39/39583 , C07K2317/24 , C07K2317/54 , C07K2317/55 , C07K2317/565 , C07K2317/569 , C07K2317/622 , C07K2317/626 , C07K2317/76 , G01N33/86 , G01N2500/02 , G01N2500/10
摘要： The present invention relates to antibody molecules against anticoagulants, in particular dabigatran, and their use as antidotes of such anticoagulants.
摘要翻译：本发明涉及针对抗凝剂的抗体分子，特别是达比加群，以及它们作为这种抗凝剂的解毒剂的用途。

99. 发明申请

US20060183779A1 ADMINISTRATION FORM FOR THE ORAL APPLICATION OF 3-[(2-{[4-(HEXYLOXYCARBONYLAMINO-IMINO-METHYL)-PHENYLAMINO]-METHYL}-1-METHYL-1H-BENZIMIDAZOL-5-CARBONYL)-PYRIDIN-2-YL-AMINO]-PROPIONIC ACID ETHYL ESTER AND THE SALTS THEREOF 有权
标题翻译： 3 - [（2 - {[4-（十二碳烯酰氨基）亚氨基 - 甲基） - 苯甲酰胺] - 甲基} -1-甲基-1H-苯并咪唑-5-羰基） - 吡啶-2-基] - 苯胺的口服应用的管理形式氨基]丙酸乙酯及其盐
公开(公告)号：US20060183779A1
公开(公告)日：2006-08-17
申请号：US11381890
申请日：2006-05-05
申请人： Ulrich Brauns , Norbert Hauel
发明人： Ulrich Brauns , Norbert Hauel
IPC分类号： A61K31/4439 , A61K31/19
CPC分类号： A61K31/4439 , C07D401/12
摘要： The invention relates to a new administration form for the oral application of the active substance ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-propionate and the pharmacologically acceptable salts thereof.
摘要翻译：本发明涉及用于口服应用活性物质的3 - [（2 - {[4-（己氧基羰基氨基 - 亚氨基 - 甲基） - 苯基氨基] - 甲基} -1-甲基-1H-苯并咪唑-5 - 羰基） - 吡啶-2-基 - 氨基] - 丙酸酯及其药理学上可接受的盐。

100. 发明申请

US20050234235A1 2-Amino-imidazo[4,5-d]pyridazin-4-ones, their preparation and their use as pharmaceutical compositions 有权
标题翻译： 2-氨基 - 咪唑并[4,5-d]哒嗪-4-酮，它们的制备及其作为药物组合物的用途
公开(公告)号：US20050234235A1
公开(公告)日：2005-10-20
申请号：US11102048
申请日：2005-04-08
申请人： Matthias Eckhardt , Frank Himmelsbach , Elke Langkopf , Norbert Hauel , Mohammad Tadayyon , Leo Thomas
发明人： Matthias Eckhardt , Frank Himmelsbach , Elke Langkopf , Norbert Hauel , Mohammad Tadayyon , Leo Thomas
IPC分类号： A61K31/503 , C07D487/02
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention relates to 2-amino-imidazo[4,5-d]pyridazin-4-ones and 2-amino-imidazo[4,5-c]pyridin-4-ones of general formula wherein R1 to R4 and X are defined as in claims 1 to 6, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译：本发明涉及以下通式的2-氨基 - 咪唑并[4,5-d]哒嗪-4-酮和2-氨基 - 咪唑并[4,5-c]吡啶-4-酮，其中R 1， R 4和X如权利要求1至6中所定义，其互变异构体，对映异构体，非对映异构体，其混合物及其盐具有有价值的药理学性质，特别是抑制对二肽基肽酶-IV（DPP-IV）酶活性的影响。

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