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公开(公告)号：US20120122820A1
公开(公告)日：2012-05-17
申请号：US12671681
申请日：2008-07-23
申请人： Nicole Diedrichs , Thomas Krahn , Ursula Krenz , Jörg Keldenich , Hanna Tinel , Claudia Hirth-Dietrich , Hans-Georg Lerchen
发明人： Nicole Diedrichs , Thomas Krahn , Ursula Krenz , Jörg Keldenich , Hanna Tinel , Claudia Hirth-Dietrich , Hans-Georg Lerchen
IPC分类号： A61K31/675 , A61P9/00 , C07D417/14 , A61K31/4439 , C07F9/6539 , C07D417/12
CPC分类号： C07D417/12 , C07D417/14 , C07F9/65583
摘要： The present application relates to prodrug derivatives of 2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitrile, 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 cardiovascular disorders.
摘要翻译： 本申请涉及2-氨基-6 - （{[2-（4-氯苯基）-1,3-噻唑-4-基]甲基}硫基）-4- [4-（2-羟基乙氧基） 苯基]吡啶-3,5-二腈，其制备方法，它们用于治疗和/或预防疾病的用途，及其用于制备用于治疗和/或预防疾病，特别是心血管疾病的药物的用途。
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公开(公告)号：US08703696B2
公开(公告)日：2014-04-22
申请号：US12671694
申请日：2008-07-23
申请人： Hans-Georg Lerchen , Ursula Krenz , Joerg Keldenich , Nicole Diedrichs , Thomas Krahn , Claudia Hirth-Dietrich , Barbara Albrecht-Küpper
发明人： Hans-Georg Lerchen , Ursula Krenz , Joerg Keldenich , Nicole Diedrichs , Thomas Krahn , Claudia Hirth-Dietrich , Barbara Albrecht-Küpper
IPC分类号： A61K38/00 , A61K31/44 , C07D417/00
CPC分类号： A61K47/48246 , A61K31/4439 , A61K47/542 , A61K47/64 , C07D417/12 , C07K5/06086
摘要： The present application relates to prodrug derivatives of 2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitrile, 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 cardiovascular disorders.
摘要翻译： 本申请涉及2-氨基-6 - （{[2-（4-氯苯基）-1,3-噻唑-4-基]甲基}硫代）-4- [4-（2-羟基乙氧基） 苯基]吡啶-3,5-二腈，其制备方法，它们用于治疗和/或预防疾病的用途，及其用于制备用于治疗和/或预防疾病，特别是心血管疾病的药物的用途。
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公开(公告)号：US20110294718A1
公开(公告)日：2011-12-01
申请号：US12671694
申请日：2008-07-23
申请人： Hans-Georg Lerchen , Ursula Krenz , Joerg Keldenich , Nicole Diedrichs , Thomas Krahn , Claudia Hirth-Dietrich , Barbara Albrecht-Küpper
发明人： Hans-Georg Lerchen , Ursula Krenz , Joerg Keldenich , Nicole Diedrichs , Thomas Krahn , Claudia Hirth-Dietrich , Barbara Albrecht-Küpper
IPC分类号： A61K38/05 , A61P9/00 , C07D417/14 , C07D417/12 , A61K31/4439
CPC分类号： A61K47/48246 , A61K31/4439 , A61K47/542 , A61K47/64 , C07D417/12 , C07K5/06086
摘要： The present application relates to prodrug derivatives of 2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitrile, 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 cardiovascular disorders.
摘要翻译： 本申请涉及2-氨基-6 - （{[2-（4-氯苯基）-1,3-噻唑-4-基]甲基}硫基）-4- [4-（2-羟基乙氧基） 苯基]吡啶-3,5-二腈，其制备方法，它们用于治疗和/或预防疾病的用途，及其用于制备用于治疗和/或预防疾病，特别是心血管疾病的药物的用途。
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4.发明授权公开(公告)号：US08420825B2
公开(公告)日：2013-04-16
申请号：US12697000
申请日：2010-01-29
申请人： Alexandros Vakalopoulos , Daniel Meibom , Barbara Albrecht-Küpper , Katja Zimmermann , Jörg Keldenich , Hans-Georg Lerchen , Peter Nell , Frank Süssmeier , Ursula Krenz
发明人： Alexandros Vakalopoulos , Daniel Meibom , Barbara Albrecht-Küpper , Katja Zimmermann , Jörg Keldenich , Hans-Georg Lerchen , Peter Nell , Frank Süssmeier , Ursula Krenz
IPC分类号： A61K31/44 , C07D409/00
CPC分类号： C07D417/14 , A61K47/64 , C07D417/12 , C07K5/0202 , C07K5/06026 , C07K5/06034 , C07K5/06086 , C07K5/06147 , C07K5/06165
摘要： The present application relates to novel 6-alkylamino-substituted dicyanopyridines, to their amino acid ester prodrugs, 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, preferably for the treatment and/or prevention of cardiovascular disorders.
摘要翻译： 本申请涉及新的6-烷基氨基取代的二氰基吡啶，其氨基酸酯前药，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，优选用于治疗和/或预防心血管疾病。
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5.发明申请公开(公告)号：US20120088761A1
公开(公告)日：2012-04-12
申请号：US13328532
申请日：2011-12-16
IPC分类号： A61K31/5375 , 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-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。
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公开(公告)号：US20110237629A1
公开(公告)日：2011-09-29
申请号：US13132989
申请日：2009-12-03
申请人： Daniel Meibom , Hans-Georg Lerchen , Alexandros Vakalopoulos , Barbara Albrech-Küpper , Peter Nell , Jörg Keldenich , Katja Zimmermann , Ursula Krenz
发明人： Daniel Meibom , Hans-Georg Lerchen , Alexandros Vakalopoulos , Barbara Albrech-Küpper , Peter Nell , Jörg Keldenich , Katja Zimmermann , Ursula Krenz
IPC分类号： A61K31/4439 , C07D413/12 , A61P9/00 , A61P9/04 , A61P9/12 , A61P9/10
CPC分类号： C07D413/12 , A61K31/4439
摘要： The present application relates to amino acid ester prodrug derivatives of 2-amino-6-({[2-(4-chlorophenyl)-1,3-oxazol-4-yl]methyl}sulfanyl)-4-(4-{[2,3-dihydroxypropyl]oxy}phenyl)pyridine-3,5-dicarbonitriles, 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 cardiovascular disorders.
摘要翻译： 本申请涉及2-氨基-6 - （{[2-（4-氯苯基）-1,3-恶唑-4-基]甲基}硫烷基）-4-（4 - {[ 2,3-二羟基丙基]氧基}苯基）吡啶-3,5-二腈，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/或预防的药物的用途 的疾病，特别是心血管疾病。
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7.发明授权Aminoacyl prodrug derivatives and medicaments for treatment of thromboembolic disorders 有权氨基酰基前药衍生物和治疗血栓栓塞障碍的药物公开(公告)号：US08362015B2
公开(公告)日：2013-01-29
申请号：US12438097
申请日：2007-08-23
IPC分类号： A61K31/535 , C07D413/14
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。
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8.发明申请AMINOACYL PRODRUGS AS AN ACTIVE PHARMACEUTICAL INGREDIENT FOR THROMBOEMBOLIC DISORDERS 审中-公开作为血栓性疾病的活性药物成分的氨基酸制剂公开(公告)号：US20110172232A1
公开(公告)日：2011-07-14
申请号：US12668590
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)-3-[2-fluoro-4-(3-oxomorpholin-4-yl)phenyl]-2-oxo-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）-3- [2-氟-4-（3-氧代吗啉-4-基）苯基] -2-氧代-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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9.发明申请BENZOFURAN AND BENZOTHIOPHENE DERIVATIVES USEFUL IN THE TREATMENT OF CANCERS OF THE CENTRAL NERVOUS SYSTEM 审中-公开用于治疗中枢神经系统癌症的苯唑呋喃和苯并噻吩衍生物公开(公告)号：US20100125073A1
公开(公告)日：2010-05-20
申请号：US12439062
申请日：2007-08-28
申请人： Olaf Weber , Verena Voehringer , Hans-Georg Lerchen , Frank-Thorsten Hafner , Joerg Keldenich , Karl-Heinz Schlemmer , Ursula Krenz , Bernd Riedl
发明人： Olaf Weber , Verena Voehringer , Hans-Georg Lerchen , Frank-Thorsten Hafner , Joerg Keldenich , Karl-Heinz Schlemmer , Ursula Krenz , Bernd Riedl
IPC分类号： A61K31/5377 , C07D307/82 , A61K31/343 , C07D413/10 , A61K31/422 , A61K31/427 , C07D417/10 , C07D405/10 , A61K31/443 , C07D413/12 , A61P35/00
CPC分类号： A61K31/343 , C07D307/82
摘要： The present invention relates to benzofuran and benzothiophene derivatives and compositions containing such compounds for the production of medicaments for the treatment of cancers of the central nervous system as monotherapy or combination with other agents.
摘要翻译： 本发明涉及苯并呋喃和苯并噻吩衍生物和含有这些化合物的组合物，用于制备用于治疗中枢神经系统癌症的药物作为单一疗法或与其它药剂组合。
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公开(公告)号：US08987209B2
公开(公告)日：2015-03-24
申请号：US13876777
申请日：2011-09-26
申请人： Hans-Georg Lerchen , Sherif El Sheikh , Beatrix Stelte-Ludwig , Sven Golfier , Joachim Schuhmacher , Jean Mark Gnoth , Ursula Krenz
发明人： Hans-Georg Lerchen , Sherif El Sheikh , Beatrix Stelte-Ludwig , Sven Golfier , Joachim Schuhmacher , Jean Mark Gnoth , Ursula Krenz
CPC分类号： C07K5/1021 , A61K38/00 , A61K38/07 , A61K38/08 , A61K45/06 , C07K1/1077 , C07K5/0205 , C07K7/02
摘要： The present application relates to new derivatives of monomethylauristatin F, substituted on the N terminus by a carboxyalkyl group, processes for preparing these derivatives, their use for the treatment and/or prevention of diseases and to produce medication for the treatment and/or prevention of diseases, particularly hyperproliferative and/or angiogenic disorders such as cancer disorders, for example. Such treatments can occur as monotherapies or in combination with other medication or further therapeutic measures.
摘要翻译： 本申请涉及通过羧基烷基在N末端被取代的单甲基海洛定蛋白F的新衍生物，用于制备这些衍生物的方法，其用于治疗和/或预防疾病以及产生用于治疗和/或预防 疾病，特别是过度增生和/或血管发生疾病，例如癌症。 这种治疗可以作为单一疗法发生，或与其他药物或其他治疗措施组合发生。
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