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41. 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。

42. 发明授权

US4988820A Cycloalkano(1,2-B) indole-sulponamides 失效
标题翻译：环咯烷（1,2-B）吲哚磺胺
公开(公告)号：US4988820A
公开(公告)日：1991-01-29
申请号：US556592
申请日：1990-07-20
申请人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Friedel Seuter , Elisabeth Perzborn , Volker-Bernd Fiedler
发明人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Friedel Seuter , Elisabeth Perzborn , Volker-Bernd Fiedler
IPC分类号： C07D209/80 , C07D209/86 , C07D209/88 , C07D491/10
CPC分类号： C07D209/80 , C07D209/86 , C07D209/88 , C07D491/10
摘要： Cycloalkano[1,2-b]indole-sulphonamides of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, trifluoromethyl, carboxyl or alkoxycarbonyl, represents a group of the formula --S(O).sub.m R.sup.3, in which R.sup.3 denotes alkyl or aryl, and m denotes one of the numbers 0, 1 or 2, represents a group of the formula ##STR2## in which R.sup.4 and R.sup.5 are identical or different and represent hydrogen, alkyl, aryl, aralkyl or acetyl, represents a group of the formula --OR.sup.6, in which R.sup.6 denotes hydrogen, alkyl, aryl, aralkyl, alkyl-SO.sub.2 --, aryl--SO.sub.2 --, aralkyl--SO.sub.2 -- or trifluoromethyl, or represents alkyl, alkenyl or cycloalkyl, each of which is optionally substituted by carboxyl, alkoxycarbonyl, halogen, hydroxyl, alkoxy, alkylthio or cyano, R.sup.2 represents aryl which is optionally substituted up to 5 times by halogen, cyano, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, alkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxy, alkylthio, hydroxyl, carboxyl, alkoxycarbonyl, phenyl, phenoxy, benzyloxy, benzylthio or a group of the formula ##STR3## in which R.sup.4 and R.sup.5 have the abovementioned meaning, x represents the number 1, 2 or 3, and y represents the number 0 or 1, where appropriate in an isomeric form, and their salts are disclosed. These compounds are useful to inhibit platelet aggregation and to antagonize thromboxane A.sub.2.
摘要翻译：其中R 1表示氢，卤素，三氟甲基，羧基或烷氧基羰基的式[IMAGE]的环烷基[1,2-b]吲哚磺酰胺代表式-S（O）m R 3的基团，其中R 3表示烷基或芳基，m表示数字0,1或2中的一个，表示其中R 4和R 5相同或不同并且表示氢，烷基，芳基，芳烷基或乙酰基的式“IMAGE”的基团，表示其中R 6表示氢，烷基，芳基，芳烷基，烷基-SO 2 - ，芳基-SO 2 - ，芳烷基-SO 2 - 或三氟甲基，或表示烷基，烯基或环烷基，其各自任选被羧基，氰基，三氟甲基，三氟甲氧基，三氟甲硫基，烷基，羧基烷基，烷氧基羰基烷基，烷氧基，烷硫基，羟基，羧基，烷氧基羰基，烷氧基羰基，烷硫基，苯基，苯氧基，苄氧基，苄硫基或其中R 4和R 5具有上述含义的式“IMAGE”的基团，x表示数字1,2或3，并且y代表数字0或1，其中适当的是异构体形式，并且其公开的盐。这些化合物可用于抑制血小板聚集和拮抗血栓素A2。

43. 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。

44. 发明授权

US4843091A Indolylpropionic acids, compositions of, and use thereof to inhibit thrombocyte aggregation 失效
标题翻译：吲哚丙酸，其组合物及其用途，用于抑制血小板聚集
公开(公告)号：US4843091A
公开(公告)日：1989-06-27
申请号：US58489
申请日：1987-06-05
申请人： Ulrich Rosentreter , Horst Boshagen , Folker Lieb , Hermann Oediger , Volker-Bernd Fiedler , Elisabeth Perzborn , Friedel Seuter
发明人： Ulrich Rosentreter , Horst Boshagen , Folker Lieb , Hermann Oediger , Volker-Bernd Fiedler , Elisabeth Perzborn , Friedel Seuter
IPC分类号： A61K31/403 , A61K31/404 , A61K31/405 , A61P7/02 , C07D209/08 , C07D209/18 , C07D209/24 , C07D401/04 , C07D405/04 , C07D409/04
CPC分类号： C07D401/04 , C07D209/08 , C07D209/24 , C07D405/04 , C07D409/04
摘要： An N-sulphonamidoethyl-indole of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl, alkoxy, alkylthio, halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, difluoromethoxy, aryl, arylthio, aralkyl, aralkoxy, aralkylthio, acyl or a group of the formula ##STR2## in which R.sup.5 and R.sup.6 are identical or different and denote hydrogen, alkyl, aryl, aralkyl or acyl, andR.sup.3 represents hydrogen, alkyl, aryl, pyridyl, thienyl or furyl, andR.sup.4 represents hydrogen, alkyl, alkoxy, alkylthio, halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, aryl, aryloxy, arylthio, aralkyl, aralkoxy, aralkylthio, acl or a group of the formula ##STR3## in which R.sup.7 and R.sup.8 are identical or different and denote hydrogen, alkyl, aryl, aralkyl or acyl,R.sup.5 represents hydrogen, ##STR4## or a pharmacologically acceptable salt of ##STR5## and R.sup.2 represents hydrogen, alkyl or aryl.The compounds were R.sup.5 is ##STR6## or a salt thereof inhibit the aggregation of thrombocytes.
摘要翻译：其中R 1表示氢，烷基，烷氧基，烷硫基，卤素，三氟甲基，三氟甲氧基，三氟甲硫基，二氟甲氧基，芳基，芳硫基，芳烷基，芳烷氧基，芳烷硫基，酰基或一组基团的N-磺酰氨基乙基 - 吲哚式中，R 5和R 6相同或不同，表示氢，烷基，芳基，芳烷基或酰基，R 3表示氢，烷基，芳基，吡啶基，噻吩基或呋喃基，R 4表示氢，烷基，烷氧基，烷硫基卤素，三氟甲基，三氟甲氧基，三氟甲硫基，芳基，芳氧基，芳硫基，芳烷基，芳烷氧基，芳烷硫基，acl或其中R 7和R 8相同或不同并表示氢，烷基，芳基，芳烷基或酰基，R 5表示氢，或者是IMA IMA的药理学上可接受的盐，R 2表示氢，烷基或芳基。化合物是R5是抑制凝血细胞聚集的盐或其盐。

45. 发明授权

US4827032A Cycloalkyl-one-containing benzenesulphonamides 失效
标题翻译：含环烷基一的苯磺酰胺
公开(公告)号：US4827032A
公开(公告)日：1989-05-02
申请号：US212840
申请日：1988-06-29
申请人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Friedel Seuter , Elisabeth Perzborn , Volker-Bernd Fiedler
发明人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Friedel Seuter , Elisabeth Perzborn , Volker-Bernd Fiedler
IPC分类号： A61K31/40 , A61K31/403 , A61P7/02 , A61P11/00 , A61P37/08 , C07D209/80 , C07D209/86 , C07D209/88 , C07D209/94 , C07D491/10 , C07C143/78
CPC分类号： C07D209/80 , C07D209/86 , C07D209/88 , C07D491/10
摘要： Cycloalkanol[1,2-b]indole-sulphonamides of the formula ##STR1## where appropriate in an isomeric form, and their salts are disclosed. These compounds are useful to inhibit platelet aggregation and to antagonize thromboxane A.sub.2.
摘要翻译：公开了具有异构体形式的合适的式“IMAGE”的环烷醇[1,2-b]吲哚磺酰胺及其盐。这些化合物可用于抑制血小板聚集和拮抗血栓素A2。

46. 发明授权

US4806551A N-dihydroindolylethyl-sulphonamides 失效
标题翻译： N-二氢吲哚基乙基磺酰胺
公开(公告)号：US4806551A
公开(公告)日：1989-02-21
申请号：US39395
申请日：1987-04-16
申请人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Volker-Bernd Fiedler , Elisabeth Perzborn , Friedel Seuter
发明人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Volker-Bernd Fiedler , Elisabeth Perzborn , Friedel Seuter
IPC分类号： C07D209/14 , A61K31/40 , A61K31/403 , A61K31/404 , A61P7/02 , C07D209/16 , C07D209/34
CPC分类号： C07D209/16
摘要： New N-dihydroindolylethyl-sulphonamides are prepared from the corresponding N-indolylethyl-sulphonamides by oxidation or hydrogenation and are useful as active compounds in medicaments. These compounds exhibit a platelet aggregation-inhibiting and thromboxan A.sub.2 -antagonistic action.The N-dihydroindolylethyl-sulphonamides have the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, trifluoromethyl, carboxyl or alkoxycarbonyl, or represents a group of the formula --S(O).sub.m R.sup.5,whereinR.sup.5 denotes alkyl or aryl andm denotes one of the numbers 0, 1 or 2, orR.sup.1 represents a group of the formula ##STR2## or R.sup.1 represents a group of the formula --OR.sup.8, orR.sup.1 represents optionally substituted alkyl, alkenyl or cycloalkyl,R.sup.2 represents aryl, which is optionally substituted by up to 5 substituents,R.sup.3 represents hydrogenor alkyl andR.sup.4 represents hydrogen, orR.sup.3 and R.sup.4 together bond a carbonyl oxygen.
摘要翻译：通过氧化或氢化由相应的N-吲哚基乙基磺酰胺制备新的N-二氢吲哚基乙基磺酰胺，并且可用作药物中的活性化合物。这些化合物表现出血小板聚集抑制和血栓素A2拮抗作用。 N-二氢吲哚基乙基磺酰胺具有式“IMAGE”，其中R 1表示氢，卤素，三氟甲基，羧基或烷氧基羰基，或表示式-S（O）m R 5的基团，其中R 5表示烷基或芳基，m表示一个数字0,1或2，或者R1表示式“IMAGE”或R1表示式-OR8的基团，或R1表示任选取代的烷基，烯基或环烷基，R 2表示芳基，其任选被取代最多5个取代基，R 3表示氢或烷基，R 4表示氢，或者R 3和R 4一起键合羰基氧。

47. 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。

48. 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。

49. 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。

50. 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

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