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71. 发明授权

US06451805B1 Substituted pyrazole derivatives for the treatment of cardiocirculatory diseases 失效
标题翻译：用于治疗心脏循环疾病的取代的吡唑衍生物
公开(公告)号：US06451805B1
公开(公告)日：2002-09-17
申请号：US09297121
申请日：1999-04-23
申请人： Alexander Straub , Chantal Fürstner , Thomas Jaetsch , Achim Feurer , Raimund Kast , Johannes-Peter Stasch , Elisabeth Perzborn , Joachim Hütter , Klaus Dembowsky
发明人： Alexander Straub , Chantal Fürstner , Thomas Jaetsch , Achim Feurer , Raimund Kast , Johannes-Peter Stasch , Elisabeth Perzborn , Joachim Hütter , Klaus Dembowsky
IPC分类号： A61K31506
CPC分类号： C07D405/04 , C07D471/04 , C07D487/04
摘要： The present invention relates to new substituted pyrazole derivatives, processes for their preparation and their use as medicaments, in particular as medicaments for the treatment of cardiovascular disorders.
摘要翻译：本发明涉及新的取代的吡唑衍生物，其制备方法及其作为药物的用途，特别是用于治疗心血管疾病的药物。

72. 发明授权

US06387940B1 Heterocyclylmethyl-substituted pyrazole derivatives 失效
公开(公告)号：US06387940B1
公开(公告)日：2002-05-14
申请号：US09644179
申请日：2000-08-23
申请人： Alexander Straub , Chantal Fürstner , Ulrich Niewöhner , Thomas Jaetsch , Achim Feurer , Raimund Kast , Johannes-Peter Stasch , Elisabeth Perzborn , Joachim Hütter , Klaus Dembowsky , Dieter Arlt
发明人： Alexander Straub , Chantal Fürstner , Ulrich Niewöhner , Thomas Jaetsch , Achim Feurer , Raimund Kast , Johannes-Peter Stasch , Elisabeth Perzborn , Joachim Hütter , Klaus Dembowsky , Dieter Arlt
IPC分类号： A61K314155
CPC分类号： C07D401/04 , C07D263/32 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04
摘要： The present invention relates to new heterocyclylmethyl-substituted pyrazole derivatives, processes for their preparation and their use as medicaments, in particular as medicaments for treatment of cardiovascular diseases.

73. 发明授权

US5093340A Substituted phenylsulphonamides 失效
标题翻译：取代的苯基磺酰胺
公开(公告)号：US5093340A
公开(公告)日：1992-03-03
申请号：US587594
申请日：1990-09-24
申请人： Klaus Mohrs , Elisabeth Perzborn , Friedel Seuter , Romanis Fruchtmann , Christian Kohlsdorfer
发明人： Klaus Mohrs , Elisabeth Perzborn , Friedel Seuter , Romanis Fruchtmann , Christian Kohlsdorfer
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/47 , A61K31/472 , A61P3/00 , A61P7/02 , A61P9/08 , A61P9/10 , A61P29/00 , A61P37/08 , C07D213/38 , C07D213/74 , C07D215/12 , C07D215/14 , C07D215/20 , C07D215/22 , C07D215/227 , C07D215/26 , C07D215/38 , C07D217/02 , C07D217/14 , C07D217/22
CPC分类号： C07D213/74 , C07D213/38 , C07D215/14 , C07D215/20 , C07D215/227 , C07D215/26
摘要： New phenylsulphonamides of the formula in which ##STR1## R.sup.1 represents a pyridyl, quinolyl or isoquinolyl radical which is unsubstituted or substituted by halogen, alkyl, cycloalkyl, alkoxy, cyano, nitro, halogenoalkyl, halogenoalkoxy, alkoxycarbonyl or alkylsulphonyl,R.sup.2 represents hydrogen, cyano, nitro, halogen, alkyl, alkoxy, halogenoalkyl, halogenoalkoxy or alkoxycarbonyl,R.sup.3 represents an aryl radical which is unsubstituted or monosubstituted, disubstituted or trisubstituted by halogen, halogenoalkyl, halogenoalkoxy, alkyl, alkoxy, alkylthio, alkylsulphonyl, cyano, nitro or alkoxycarbonyl, the substitutents being identical or different, or represents pentafluorophenyl or represents a straight-chain, branched or cyclic alkyl which is unsubstituted or substituted by halogen, aryl, aryloxy, cyano, alkoxycarbonyl, alkoxy, alkylthio or trifluoromethyl, andX represents an --O--, --A--B-- or --B--A-- group, whereA denotes --O--, ##STR2## B denotes --O--; ##STR3## where R.sup.1 does not represent a pyridyl radical when X represents an --O-- group, and salts thereof are prepared by reacting appropriate amines with sulphonyl halides. The substituted phenylsulphonamides can be employed as active compounds for inhibiting enzymatic reactions and for inhibiting thrombocyte aggregations.

74. 发明授权

US5015657A 2-halogen-substituted N-indolylethyl-sulphonamides and inhibiting platelet aggregation and antagonizing thromboxane A.sub.2 therewith 失效
标题翻译： 2-卤素取代的N-吲哚基乙基磺酰胺，并且抑制血小板聚集并拮抗血栓素A2
公开(公告)号：US5015657A
公开(公告)日：1991-05-14
申请号：US436858
申请日：1989-11-15
申请人： Horst Boshagen , Elisabeth Perzborn , Volker-Bernd Fiedler
发明人： Horst Boshagen , Elisabeth Perzborn , Volker-Bernd Fiedler
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P7/02 , C07D209/30
CPC分类号： C07D209/30
摘要： Inhibiting platelet aggregation and antagonizing thromboxane A.sub.2 with new 2-halogen-substituted N-indolyethyl-sulphonamides of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, trifluoromethyl, carboxyl or alkoxycarbonyl having up to 8 carbon atoms, orrepresents straight-chain or branched alkyl having up to 8 carbon atoms, or represents cycloalkyl having 3 to 8 carbon atoms, which is optionally substituted by carboxyl, halogen, alkoxy or alkoxycarbonyl having in each case up to 8 carbon atoms, cyano or hydroxyl, orrepresents a group of the formula --S(O).sub.n --R.sup.5,--NR.sup.6 R.sup.7 or --OR.sup.8represents straight-chain or branched alkyl having up to 10 carbon atoms, which is optionally substituted by halogen, phenyl, hydroxyl or cyano, orrepresents aryl having 6 to 10 carbon atoms, which is optionally substituted by up to 5 identical or different substituents from the group comprising halogen, cyano, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, alkyl, alkoxy, alkoxycarbonyl or alkylthio having in each case up to 8 carbon atoms, hydroxyl, carboxyl, phenyl, phenoxy, benzyloxy and benzylthio, or by a group of the formula --NR.sup.6 R.sup.7,R.sup.3 represents halogen,R.sup.4 represents hydrogen or straight-chain or branched alkyl having up to 8 carbon atoms, or represents phenylandm represents one of the numbers 2, 3 or 4, and salts thereof.
摘要翻译：抑制血小板聚集和拮抗血栓素A2与新的2-卤素取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N- 具有至多8个碳原子的直链或支链烷基，或代表具有3-8个碳原子的环烷基，其任选被羧基，卤素，烷氧基或烷氧基羰基所取代，每种情况下最多具有8个碳原子，氰基或羟基，或表示式-S（O）n -R 5，-NR 6 R 7或-OR 8表示具有至多10个碳原子的直链或支链烷基，其任选被卤素，苯基，羟基或氰基取代，或表示芳基具有6至10个碳原子，其任选被至多5个相同或不同的取代基取代，所述取代基包括卤素，氰基，三氟甲基，三氟甲氧基，三氟甲硫基，烷基，烷氧基，烷氧基羰基或具有至多8个碳原子的烷硫基，羟基，羧基，苯基，苯氧基，苄氧基和苄硫基，或由-NR 6 R 7基团，R 3表示卤素，R 4表示氢或具有直链或支链烷基的直链或支链烷基 8个碳原子，或表示苯基，m表示数2，3或4中的一个，及其盐。

75. 发明授权

US4970215A Substituted 4-(quinolin-2-yl-methoxy)phenyl-acetic acid derivatives and anti-allergic use thereof 失效
标题翻译：取代的4-（喹啉-2-基 - 甲氧基）苯基 - 乙酸衍生物及其抗过敏应用
公开(公告)号：US4970215A
公开(公告)日：1990-11-13
申请号：US354536
申请日：1989-05-19
申请人： Klaus Mohrs , Siegfried Raddatz , Elisabeth Perzborn , Romanis Fruchtmann , Christian Kohlsdorfer , Reiner Muller-Peddinghaus , Pia Theisen
发明人： Klaus Mohrs , Siegfried Raddatz , Elisabeth Perzborn , Romanis Fruchtmann , Christian Kohlsdorfer , Reiner Muller-Peddinghaus , Pia Theisen
IPC分类号： A61K31/47 , A61K31/4709 , A61P7/02 , A61P9/00 , A61P11/00 , A61P11/06 , A61P29/00 , A61P37/08 , A61P43/00 , C07D215/14 , C07D215/18 , C07D405/12
CPC分类号： C07D215/14 , C07D215/18
摘要： Leucotriene synthesis inhibiting substituted 4-(quinolin-2-yl-methoxy)phenyl-acetic acid derivatives of the formula ##STR1## R.sup.1 --represents a group of the formula ##STR2## wherein Y--represents a group of the formula ##STR3## Z--represents norbornyl, or represents a group of the formula ##STR4## and A and B are identical or different and denote hydrogen, lower alkyl or halogen, and salts thereof.
摘要翻译：抑制下式（I）的取代的4-（喹啉-2-基 - 甲氧基）苯基 - 乙酸衍生物的亮氨酸三烯合成R1代表式IMA的基团，其中Y代表式 IMAGE> Z-代降冰片基，或代表式IMA的基团，A和B相同或不同，表示氢，低级烷基或卤素，及其盐。

76. 发明授权

US08334284B2 Aminoacyl prodrug derivatives and medicaments for the treatment of thromboembolitic disorders 有权
标题翻译：用于治疗血栓栓塞性疾病的氨基酰基前药衍生物和药物
公开(公告)号：US08334284B2
公开(公告)日：2012-12-18
申请号：US13328532
申请日：2011-12-16
申请人： Hans-Georg Lerchen , Ursula Krenz , Karl-Heinz Schlemmer , Elisabeth Perzborn , Joerg Keldenich
发明人： Hans-Georg Lerchen , Ursula Krenz , Karl-Heinz Schlemmer , Elisabeth Perzborn , Joerg Keldenich
IPC分类号： A61K31/5375
CPC分类号： C07D413/14
摘要： The present application relates to prodrug derivatives of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of thromboembolic disorders.
摘要翻译：本申请涉及5-氯-N - （{（5S）-2-氧代-3- [4-（3-氧代吗啉-4-基）苯基] -1,3-恶唑烷-5-基的前药衍生物）甲基）噻吩-2-甲酰胺，其制备方法，它们用于治疗和/或预防疾病的用途，以及它们用于制备用于治疗和/或预防疾病，特别是血栓栓塞性疾病的药物的用途。

77. 发明授权

US08101601B2 Aminoacyl prodrug derivatives and medicaments for the treatment of thromboembolitic disorders 有权
标题翻译：用于治疗血栓栓塞性疾病的氨基酰基前药衍生物和药物
公开(公告)号：US08101601B2
公开(公告)日：2012-01-24
申请号：US12224007
申请日：2007-02-06
申请人： Hans-Georg Lerchen , Ursula Krenz , Karl-Heinz Schlemmer , Elisabeth Perzborn , Joerg Keldenich
发明人： Hans-Georg Lerchen , Ursula Krenz , Karl-Heinz Schlemmer , Elisabeth Perzborn , Joerg Keldenich
IPC分类号： A61K31/5377 , C07D413/14 , A61P7/02
CPC分类号： C07D413/14
摘要： The present application relates to prodrug derivatives of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-morpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of thromboembolic disorders.
摘要翻译：本申请涉及5-氯-N - （{（5S）-2-氧代-3- [4-（3-氧代 - 吗啉-4-基）苯基] -1,3-恶唑烷-5-酮 - 基}甲基）噻吩-2-甲酰胺，其制备方法，其用于治疗和/或预防疾病的用途及其用于制备用于治疗和/或预防疾病，特别是血栓栓塞性疾病的药物的用途。

78. 发明申请

US20110034467A1 DIHYDRO-PYRROLOPYRIDINE-, DIHYDRO-PYRROLOPYRIDAZINE- AND DIHYDRO-PYRROLOPYRIMIDINE-DERIVATIVES AND USE THEREOF 审中-公开
标题翻译：二羟基吡咯烷酮，二氢吡咯烷酮和二氢吡咯并吡啶衍生物及其用途
公开(公告)号：US20110034467A1
公开(公告)日：2011-02-10
申请号：US12302286
申请日：2007-05-25
申请人： Susanne Röhrig , Mario Jeske , Elisabeth Perzborn , Mark Jean Gnoth
发明人： Susanne Röhrig , Mario Jeske , Elisabeth Perzborn , Mark Jean Gnoth
IPC分类号： A61K31/5025 , C07D471/04 , C07D487/04 , A61K31/437 , A61K31/519 , A61P7/02
CPC分类号： C07D487/04 , C07D471/04
摘要： The invention relates to novel dihydro-pyrrolopyridine, dihydro-pyrrolopyridazine and dihydro-pyrrolopyrimidine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.
摘要翻译：本发明涉及新的二氢吡咯并吡啶，二氢吡咯并哒嗪和二氢吡咯并嘧啶衍生物，其制备方法，其用于治疗和/或预防疾病及其用于制备用于治疗和/或预防的药物的用途的疾病，特别是血栓栓塞性疾病。

79. 发明申请

US20100273789A1 AMINOACYL PRODRUGS 审中-公开
公开(公告)号：US20100273789A1
公开(公告)日：2010-10-28
申请号：US12668619
申请日：2008-06-28
申请人： Hans-Georg Lerchen , Ursula Krenz , Michael Härter , Mark Jean Gnoth , Georges Von Degenfeld , Elke Dittrich-Wengenroth , Anja Buchmüller , Susanne Röhrig , Swen Allerheiligen , Elisabeth Perzborn , Christoph Gerdes , Karl-Heinz Schlemmer , Metin Akbaba
发明人： Hans-Georg Lerchen , Ursula Krenz , Michael Härter , Mark Jean Gnoth , Georges Von Degenfeld , Elke Dittrich-Wengenroth , Anja Buchmüller , Susanne Röhrig , Swen Allerheiligen , Elisabeth Perzborn , Christoph Gerdes , Karl-Heinz Schlemmer , Metin Akbaba
IPC分类号： A61K31/5377 , C07D413/14 , A61P7/02
CPC分类号： C07D413/14
摘要： The present application relates to prodrug derivatives of 5-chloro-N-({(5S)-2-oxo-3-[2-fluoro-4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of thromboembolic disorders.
摘要翻译：本申请涉及5-氯-N - （{（5S）-2-氧代-3- [2-氟-4-（3-氧代吗啉-4-基）苯基] -1,3-恶唑烷的前药衍生物 -5-基}甲基）噻吩-2-甲酰胺，其制备方法，其用于治疗和/或预防疾病的用途及其用于制备用于治疗和/或预防疾病的药物的用途，特别是血栓栓塞性疾病

80. 发明授权

US07767702B2 Substituted oxazolidinones for combinational therapy 有权
标题翻译：用于组合治疗的取代恶唑烷酮
公开(公告)号：US07767702B2
公开(公告)日：2010-08-03
申请号：US10481297
申请日：2002-06-07
申请人： Alexander Straub , Thomas Lampe , Josef Pernerstorfer , Elisabeth Perzborn , Jens Pohlmann , Susanne Röhrig , Karl-Heinz Schlemmer
发明人： Alexander Straub , Thomas Lampe , Josef Pernerstorfer , Elisabeth Perzborn , Jens Pohlmann , Susanne Röhrig , Karl-Heinz Schlemmer
IPC分类号： A61K31/421
CPC分类号： A61K31/422 , A61K31/421 , A61K31/5377 , A61K45/06 , A61K2300/00
摘要： The invention relates to combinations of A) oxazolidinones of formula (I) and B) other active ingredients, to a method for producing said combinations and to the use thereof as medicaments, in particular for the treatment and/or prophylaxis of thrombo-embolic diseases.
摘要翻译：本发明涉及式（I）的A）恶唑烷酮和B）其它活性成分的组合，用于制备所述组合的方法及其作为药物的用途，特别是用于治疗和/或预防血栓栓塞性疾病。

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