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公开(公告)号：US08067419B2
公开(公告)日：2011-11-29
申请号：US12090816
申请日：2006-10-20
IPC分类号： A61K31/4965 , C07D487/00
CPC分类号： C07D295/185 , C07D209/04 , C07D209/16 , C07D213/26 , C07D213/38 , C07D213/40 , C07D213/60 , C07D213/74 , C07D217/04 , C07D217/14 , C07D233/64 , C07D239/42 , C07D277/28 , C07D307/14 , C07D317/58 , C07D333/20 , C07D333/28 , C07D333/58
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, 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用作治疗或预防原生动物感染，特别是疟疾的药物的相关方面。
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公开(公告)号：US20080234272A1
公开(公告)日：2008-09-25
申请号：US12090816
申请日：2006-10-20
IPC分类号： A61K31/5377 , C07D241/04 , C07D295/00 , A61P33/06 , A61K31/495 , A61K31/496
CPC分类号： C07D295/185 , C07D209/04 , C07D209/16 , C07D213/26 , C07D213/38 , C07D213/40 , C07D213/60 , C07D213/74 , C07D217/04 , C07D217/14 , C07D233/64 , C07D239/42 , C07D277/28 , C07D307/14 , C07D317/58 , C07D333/20 , C07D333/28 , C07D333/58
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, 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用作治疗或预防原生动物感染，特别是疟疾的药物的相关方面。
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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：US07799805B2
公开(公告)日：2010-09-21
申请号：US11915594
申请日：2006-05-23
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： A01N43/40 , A61K31/445 , C07D211/68 , C07D211/80 , C07D213/02
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：US08138340B2
公开(公告)日：2012-03-20
申请号：US11660987
申请日：2005-08-22
申请人： Olivier Bezencon , Christoph Boss , Daniel Bur , Olivier Corminboeuf , Walter Fiśchli , Corinna Grisostomi , Lubos Remen , Sylvia Richard-Bildstein , Thierry Sifferlen , Thomas Weller
发明人： Olivier Bezencon , Christoph Boss , Daniel Bur , Olivier Corminboeuf , Walter Fiśchli , Corinna Grisostomi , Lubos Remen , Sylvia Richard-Bildstein , Thierry Sifferlen , Thomas Weller
IPC分类号： C07D241/36
CPC分类号： C07D471/08 , C07D513/08
摘要： The invention relates to novel bicyclononene derivatives of Formula (I); and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.
摘要翻译： 本发明涉及式（I）的新型双环壬烯衍生物; 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化合物的方法，含有一种或多种这些化合物的药物组合物，特别是其作为肾素抑制剂的用途的相关方面。
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公开(公告)号：US20110224210A1
公开(公告)日：2011-09-15
申请号：US13130151
申请日：2009-11-18
申请人： Hamed Aissaoui , Christoph Boss , Olivier Corminboeuf , Marie-Celine Frantz , Corinna Grisostomi
发明人： Hamed Aissaoui , Christoph Boss , Olivier Corminboeuf , Marie-Celine Frantz , Corinna Grisostomi
IPC分类号： A61K31/5377 , A61K31/497 , A61K31/501 , A61K31/4545 , A61K31/4439 , A61K31/4418 , C07D401/14 , C07D413/12 , C07D401/12 , C07D211/70 , A61P33/06 , A61P33/02
CPC分类号： C07C237/22 , C07D211/16 , C07D401/12 , C07D403/12 , C07D413/12
摘要： The invention relates to novel bis-amide 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： 本发明涉及新颖的双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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公开(公告)号：US20090306123A1
公开(公告)日：2009-12-10
申请号：US11660987
申请日：2005-08-22
申请人： Olivier Bezencon , Christoph Boss , Daniel Bur , Olivier Corminboeuf , Walter Fischli , Corinna Grisostomi , Lubos Remen , Sylvia Richard-Bildstein , Thierry Sifferlen , Thomas Weller
发明人： Olivier Bezencon , Christoph Boss , Daniel Bur , Olivier Corminboeuf , Walter Fischli , Corinna Grisostomi , Lubos Remen , Sylvia Richard-Bildstein , Thierry Sifferlen , Thomas Weller
IPC分类号： A61K31/4995 , C07D487/08
CPC分类号： C07D471/08 , C07D513/08
摘要： The invention relates to novel bicyclononene derivatives of Formula (I); and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.
摘要翻译： 本发明涉及式（I）的新型双环壬烯衍生物; 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化合物的方法，含有一种或多种这些化合物的药物组合物，特别是其作为肾素抑制剂的用途的相关方面。
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公开(公告)号：US20080214598A1
公开(公告)日：2008-09-04
申请号：US11915594
申请日：2006-05-23
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： A61K31/4375 , C07D471/02 , A61P9/10 , A61P9/12 , A61P13/12
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：US20080076762A1
公开(公告)日：2008-03-27
申请号：US11720181
申请日：2005-11-21
申请人： Christoph Boss , Daniel Bur , Olivier Corminboeuf , Corinna Grisostomi , Lars Prade , Thomas Weller
发明人： Christoph Boss , Daniel Bur , Olivier Corminboeuf , Corinna Grisostomi , Lars Prade , Thomas Weller
IPC分类号： A61K31/541 , A61K31/4468 , A61K31/4523 , A61P33/06 , C07D241/04 , C07D295/00 , C07D221/00 , A61K31/496 , A61K31/5377
CPC分类号： C07D409/14 , C07D211/58 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14
摘要： Novel substituted 4-aminopiperidine derivatives of the formula I: wherein n, R1, Y, and are as defined in claim 1, and optically pure enantiomers, mixtures of enantiomers, racemates, diastereomers, mixtures of diastereomers, diastereomeric racemates, mixtures of diastereomeric racemates and meso-forms, as well as salts and solvent complexes of such compounds, and morphological forms, that exhibit useful parasite aspartic proteases inhibiting properties and can thus be used in the form of pharmaceutical compositions as antimalarial medicines.
摘要翻译： 式I的新型取代的4-氨基哌啶衍生物：其中n，R 1，Y和如权利要求1中所定义，和光学纯对映异构体，对映异构体的混合物，外消旋体，非对映异构体，非对映异构体的混合物 ，非对映异构体外消旋体，非对映体外消旋体和内消旋体的混合物，以及这些化合物的盐和溶剂配合物，以及形态形式，其表现出有用的寄生虫天冬氨酸蛋白酶抑制性质，因此可以以药物组合物的形式用作抗疟药物 。
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公开(公告)号：US08580831B2
公开(公告)日：2013-11-12
申请号：US13376966
申请日：2010-06-07
申请人： Daniel Bur , Olivier Corminboeuf , Sylvaine Cren , Corinna Grisostomi , Xavier Leroy , Sylvia Richard-Bildstein
发明人： Daniel Bur , Olivier Corminboeuf , Sylvaine Cren , Corinna Grisostomi , Xavier Leroy , Sylvia Richard-Bildstein
IPC分类号： A61K31/422 , A61K31/427 , C07D413/14 , C07D417/14
CPC分类号： C07D413/14 , C07D417/14
摘要： The invention relates to fluorinated aminotriazole derivatives of formula (I), wherein A, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
摘要翻译： 本发明涉及式（I）的氟化氨基三唑衍生物，其中A，R 1和R 2如说明书中所定义，其制备及其作为药物活性化合物的用途。
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