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公开(公告)号：US09000029B2
公开(公告)日：2015-04-07
申请号：US14530532
申请日：2014-10-31
申请人： Christoph Boss , Christine Brotschi , John Gatfield , Markus Gude , Bibia Heidmann , Thierry Sifferlen , Jodi T. Williams
发明人： Christoph Boss , Christine Brotschi , John Gatfield , Markus Gude , Bibia Heidmann , Thierry Sifferlen , Jodi T. Williams
IPC分类号： A61K31/40 , C07D207/48
CPC分类号： A61K31/401 , A61K31/40 , A61K31/4025 , C07D207/48 , C07D409/12
摘要： The present invention relates to (S)-proline sulfonamide compounds of formula (I) wherein R1 and R2 are as described in the description, or pharmaceutically acceptable salts thereof, for use in the prevention or treatment of diseases or disorders related to the orexin system. The present invention also relates to the use of (S)-proline sulfonamide compounds of formula (II) as pharmaceuticals, to pharmaceutical compositions comprising compounds of formula (II), and especially their use in the prevention or treatment of diseases or disorders related to the orexin system.
摘要翻译： 本发明涉及式（I）的（S） - 脯氨酸磺酰胺化合物，其中R 1和R 2如描述中所述或其药学上可接受的盐，用于预防或治疗与食欲素系统相关的疾病或病症 。 本发明还涉及式（II）的（S）脯氨酸磺酰胺化合物作为药物在包含式（II）化合物的药物组合物中的应用，特别是其用于预防或治疗与 食欲素系统。
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公开(公告)号：US08895606B2
公开(公告)日：2014-11-25
申请号：US13818647
申请日：2011-08-23
申请人： Christoph Boss , Christine Brotschi , John Gatfield , Markus Gude , Bibia Heidmann , Thierry Sifferlen , Jodi T. Williams
发明人： Christoph Boss , Christine Brotschi , John Gatfield , Markus Gude , Bibia Heidmann , Thierry Sifferlen , Jodi T. Williams
IPC分类号： A61K31/40 , C07D207/48 , A61K31/4025 , C07D409/12
CPC分类号： A61K31/401 , A61K31/40 , A61K31/4025 , C07D207/48 , C07D409/12
摘要： The present invention relates to (S)-proline sulfonamide compounds of formula (I) wherein R1 and R2 are as described in the description, or pharmaceutically acceptable salts thereof, for use in the prevention or treatment of diseases or disorders related to the orexin system. The present invention also relates to the use of (S)-proline sulfonamide compounds of formula (II) as pharmaceuticals, to pharmaceutical compositions comprising compounds of formula (II), and especially their use in the prevention or treatment of diseases or disorders related to the orexin system.
摘要翻译： 本发明涉及式（I）的（S） - 脯氨酸磺酰胺化合物，其中R 1和R 2如描述中所述或其药学上可接受的盐，用于预防或治疗与食欲素系统相关的疾病或病症 。 本发明还涉及式（II）的（S）脯氨酸磺酰胺化合物作为药物在包含式（II）化合物的药物组合物中的应用，特别是其用于预防或治疗与 食欲素系统。
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公开(公告)号：US08889688B2
公开(公告)日：2014-11-18
申请号：US13519938
申请日：2011-01-04
IPC分类号： A61K31/497 , C07D403/12 , A61K31/496
CPC分类号： A61K31/496 , C07D213/56 , C07D295/192 , C07D403/12 , Y02A50/411
摘要： The invention relates to novel piperazine derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria.
摘要翻译： 本发明涉及新型哌嗪衍生物及其在制备药物组合物中作为活性成分的用途。 本发明还涉及包括含有一种或多种这些化合物的药物组合物及其作为用于治疗或预防原生动物感染的药物的用途的相关方面，例如特别是疟疾。
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74.发明授权1-phenyl-substituted heterocyclyl derivatives and their use as prostaglandin D2 receptor modulators 有权1-苯基取代的杂环基衍生物及其作为前列腺素D2受体调节剂的用途公开(公告)号：US08575158B2
公开(公告)日：2013-11-05
申请号：US13808857
申请日：2011-07-04
申请人： Hamed Aissaoui , Christoph Boss , Heinz Fretz , Julien Pothier , Sylvia Richard-Bildstein , Philippe Risch , Romain Siegrist
发明人： Hamed Aissaoui , Christoph Boss , Heinz Fretz , Julien Pothier , Sylvia Richard-Bildstein , Philippe Risch , Romain Siegrist
IPC分类号： C07D265/36 , C07D221/04
CPC分类号： C07D487/04 , A61K31/4035 , A61K31/472 , C07D209/44 , C07D217/16 , C07D217/26 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/04 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D417/12 , C07D471/04
摘要： The present invention relates to 1-phenyl-substituted heterocyclyl derivatives of the formula (I), wherein X, Y, Z, n, R1, R2, R3, R4, R5, R6, R7 and R10 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.
摘要翻译： 本发明涉及式（I）的1-苯基取代的杂环基衍生物，其中X，Y，Z，n，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 10如说明书和 其用作前列腺素受体调节剂，最特别地作为前列腺素D2受体调节剂用于治疗各种前列腺素介导的疾病和病症，含有这些化合物的药物组合物及其制备方法。
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![2-aza-bicyclo[3.1.0]hexane derivatives as orexin receptor antagonists](/abs-image/US/2012/10/16/US08288435B2/abs.jpg.150x150.jpg)
75.发明授权2-aza-bicyclo[3.1.0]hexane derivatives as orexin receptor antagonists 失效2-氮杂 - 双环[3.1.0]己烷衍生物作为食欲素受体拮抗剂公开(公告)号：US08288435B2
公开(公告)日：2012-10-16
申请号：US12521453
申请日：2007-12-28
申请人： Hamed Aissaoui , Christoph Boss , Markus Gude , Ralf Koberstein , Thierry Sifferlen , Daniel Trachsel
发明人： Hamed Aissaoui , Christoph Boss , Markus Gude , Ralf Koberstein , Thierry Sifferlen , Daniel Trachsel
IPC分类号： A61K31/403 , C07D209/12
CPC分类号： C07D513/04 , C07D405/12 , C07D405/14 , C07D417/14
摘要： The invention relates to novel 2-aza-bicyclo[3.1.0]hexane derivatives of Formula (I) wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
摘要翻译： 本发明涉及式（I）的新的2-氮杂 - 双环[3.1.0]己烷衍生物，其中A，B，n和R 1如描述中所述，以及这些化合物或其药学上可接受的盐 的这些化合物，作为药物，特别是作为食欲素受体拮抗剂。
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![2-aza-bicyclo[3.3.0]octane derivatives](/abs-image/US/2012/10/16/US08288429B2/abs.jpg.150x150.jpg)
公开(公告)号：US08288429B2
公开(公告)日：2012-10-16
申请号：US12670823
申请日：2008-07-25
申请人： Hamed Aissaoui , Christoph Boss , Markus Gude , Ralf Koberstein , Thierry Sifferlen , Daniel Trachsel
发明人： Hamed Aissaoui , Christoph Boss , Markus Gude , Ralf Koberstein , Thierry Sifferlen , Daniel Trachsel
IPC分类号： A61K31/403 , C07D209/52
CPC分类号： C07D413/12 , C07D209/02 , C07D405/12 , C07D417/14 , C07D513/04
摘要： The invention relates to 2-aza-bicyclo[3.3.0]octane derivatives of Formula (I) wherein A, B, and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
摘要翻译： 本发明涉及式（I）的2-氮杂 - 双环[3.3.0]辛烷衍生物，其中A，B和R1如说明书中所述，以及这些化合物或其药学上可接受的盐的用途 化合物，作为药物，特别是作为食欲素受体拮抗剂。
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![2-AZA-BICYCLO[3.3.0]OCTANE DERIVATIVES](/abs-image/US/2011/01/13/US20110009461A1/abs.jpg.150x150.jpg)
公开(公告)号：US20110009461A1
公开(公告)日：2011-01-13
申请号：US12670823
申请日：2008-07-25
申请人： Hamed Aissaoui , Christoph Boss , Markus Gude , Ralf Koberstein , Thierry Sifferlen , Daniel Trachsel
发明人： Hamed Aissaoui , Christoph Boss , Markus Gude , Ralf Koberstein , Thierry Sifferlen , Daniel Trachsel
IPC分类号： A61K31/429 , C07D513/04 , C07D417/14 , A61K31/427 , A61P25/00
CPC分类号： C07D413/12 , C07D209/02 , C07D405/12 , C07D417/14 , C07D513/04
摘要： The invention relates to 2-aza-bicyclo[3.3.0]octane derivatives of Formula (I) wherein A, B, and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
摘要翻译： 本发明涉及式（I）的2-氮杂 - 双环[3.3.0]辛烷衍生物，其中A，B和R1如说明书中所述，以及这些化合物或其药学上可接受的盐的用途 化合物，作为药物，特别是作为食欲素受体拮抗剂。
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公开(公告)号：US20100324052A1
公开(公告)日：2010-12-23
申请号：US12855016
申请日：2010-08-12
申请人： Olivier Bezencon , Christoph Boss , Daniel Bur , Austin Chih-Yu Chen , Olivier Corminboeuf , Daniel Dube , Walter Fischli , Corinna Grisostomi , Lubos Remen , Sylvia Richard-Bildstein , Thierry Sifferlen , Michel Therien , Thomas Weller
发明人： Olivier Bezencon , Christoph Boss , Daniel Bur , Austin Chih-Yu Chen , Olivier Corminboeuf , Daniel Dube , Walter Fischli , Corinna Grisostomi , Lubos Remen , Sylvia Richard-Bildstein , Thierry Sifferlen , Michel Therien , Thomas Weller
IPC分类号： A61K31/504 , C07D471/08 , A61P9/00 , A61P13/12 , C07D211/60 , A61K31/451 , C07D213/81 , A61K31/444
CPC分类号： C07D471/08 , C07D211/78 , C07D401/10 , C07D401/12
摘要： The invention relates to novel piperidine carboxylic acid amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of these novel compounds, pharmaceutical compositions comprising such compounds and especially the use of such compounds as inhibitors of renin.
摘要翻译： 本发明涉及新型的哌啶羧酸酰胺衍生物及其在制备药物组合物中作为活性成分的用途。 本发明还涉及包括制备这些新化合物的方法，包含这些化合物的药物组合物，特别是使用这些化合物作为肾素抑制剂的相关方面。
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公开(公告)号：US20100113531A1
公开(公告)日：2010-05-06
申请号：US12593095
申请日：2008-03-25
IPC分类号： A61K31/4439 , A61K31/427 , C07D417/12 , C07D277/04 , A61P25/18 , A61P25/24 , A61P15/00 , A61P25/28 , A61P23/00 , A61P19/02 , A61P37/00 , A61P35/00
CPC分类号： C07D417/14 , C07D277/04 , C07D277/24 , C07D277/56 , C07D417/06 , C07D417/12 , C07D513/04
摘要： The invention relates to novel thiazolidine derivatives of the formula (I) wherein A and R1 are as described in the description and their use as medicaments, especially as orexin receptor antagonists.
摘要翻译： 本发明涉及式（I）的新型噻唑烷衍生物，其中A和R 1如描述中所述及其作为药物的用途，特别是作为食欲素受体拮抗剂。
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80.发明申请公开(公告)号：US20090099228A1
公开(公告)日：2009-04-16
申请号：US12298369
申请日：2007-04-25
IPC分类号： A61K31/437 , C07D471/04 , A61P25/00
CPC分类号： C07D471/04
摘要： The invention relates to novel pyrazolo-tetrahydropyridines compounds and their use as orexin receptor antagonists.
摘要翻译： 本发明涉及新型吡唑并四氢吡啶类化合物及其作为食欲素受体拮抗剂的用途。
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