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1. 发明授权

US07868036B2 Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US07868036B2
公开(公告)日：2011-01-11
申请号：US10593461
申请日：2005-03-17
申请人： Peter Herold , Stefan Stutz , Robert Mah , Vincenzo Tschinke , Aleksandar Stojanovic , Nathalie Jotterand , Michael Quirmbach , Dirk Behnke , Christiane Marti
发明人： Peter Herold , Stefan Stutz , Robert Mah , Vincenzo Tschinke , Aleksandar Stojanovic , Nathalie Jotterand , Michael Quirmbach , Dirk Behnke , Christiane Marti
IPC分类号： A61K31/405 , C07D209/04
CPC分类号： C07D209/12 , C07D401/06
摘要： The invention relates to novel amino alcohols of the general formula (I) where X, R1, R2, R3, R4, R5 and R6 are each as defined in detail in the description, to a process for their preparation and to the use of these compounds as medicines, in particular as renin inhibitors.
摘要翻译：本发明涉及通式（I）的新型氨基醇，其中X，R 1，R 2，R 3，R 4，R 5和R 6各自如说明书中详细定义，其制备方法和使用这些化合物作为药物，特别是作为肾素抑制剂。

2. 发明授权

US07687495B2 Substituted piperidines 失效
标题翻译：取代的哌啶
公开(公告)号：US07687495B2
公开(公告)日：2010-03-30
申请号：US12076221
申请日：2008-03-14
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christiane Marti , Stefan Stutz , Stjepan Jelakovic , Zenon D. Konteatis , Jennifer L. Ludington , Michael Quirmbach , Aleksandar Stojanovic , Dirk Behnke , Frank Hollinger
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christiane Marti , Stefan Stutz , Stjepan Jelakovic , Zenon D. Konteatis , Jennifer L. Ludington , Michael Quirmbach , Aleksandar Stojanovic , Dirk Behnke , Frank Hollinger
IPC分类号： C07D401/02 , A61K31/50 , A61K31/4965
CPC分类号： C07D413/12 , C07D413/14
摘要： Substituted piperidines of formulae (I) and (II) with the substituent definitions as explained in the specification. The compounds are suitable in particular as renin inhibitors and are highly potent.
摘要翻译：式（I）和（II）的取代的哌啶与说明书中所述的取代基定义相同。该化合物特别适合作为肾素抑制剂，并且是非常有效的。

3. 发明申请

US20090118512A1 Process for Preparing 6,7-Dihydro-5H-Imidazo[1,5-A]Pyridin-8-One 审中-公开
标题翻译： 6,7-二氢-5H-咪唑并[1,5-a]吡啶-8-酮的制备方法
公开(公告)号：US20090118512A1
公开(公告)日：2009-05-07
申请号：US12225813
申请日：2007-03-30
申请人： Pierre Martin , Andreas Boudier , Michael Quirmbach , Robert Mah , Nathalie Jotterand
发明人： Pierre Martin , Andreas Boudier , Michael Quirmbach , Robert Mah , Nathalie Jotterand
IPC分类号： C07D471/04 , C07D211/74 , C07F7/10 , C07D233/64
CPC分类号： C07D233/22 , C07D213/65 , C07D471/04 , C07F7/0814
摘要： 6,7-Dihydro-5H-imidazo[1,5-a]pyridin-8-one (I), is obtainable in high yields by: 1) a process which proceeds from a suitably protected C-(3-hydroxypyridin-2-yl)methylamine whose amine is converted to the formamide which is then cyclized to the imidazo[1,5-a]pyridine and hydrogenated to the 6,7-dihydro-5H-imidazo[1,5-a]pyridin-8-one, and suitably protected C-(3-hydroxypyridin-2-yl)methylamines can be prepared either in 2 steps proceeding from commercially available 3-hydroxy-2-cyanopyridine [932-35-4] or in 3 steps proceeding from commercially available 2-hydroxymethylpyridin-3-ol [14173-30-9]; 2) a process for preparing 4-hydroxy-1-(1H-imidazol-4-yl)butan-1-one, an intermediate from the synthesis of 6,7-dihydro-5H-imidazo[1,5-a]pyridin-8-one (formula I), as described in WO 2002/040484, proceeding from N,N-dimethyl-2-(trialkylsilanyl)imidazole-1-sulphonamide by lithiation and subsequent reaction with a suitably protected 4-hydroxybutyraldehyde, followed by oxidation of the secondary alcohol, acid-induced deprotection of the imidazole and deprotection of the alcohol functionality; 3) a process which proceeds from 5,6,7,8-tetrahydroimidazo[1,5-a]pyridine [38666-30-7], which is oxidized.
摘要翻译： 6,7-二氢-5H-咪唑并[1,5-a]吡啶-8-酮（I）可以通过以下方式获得：1）从适当保护的C-（3-羟基吡啶-2 - 基）甲胺，其胺转化成甲酰胺，然后将其环化为咪唑并[1,5-a]吡啶，并氢化成6,7-二氢-5H-咪唑并[1,5-a] 一个和适当保护的C-（3-羟基吡啶-2-基）甲胺可以从市售的3-羟基-2-氰基吡啶[932-35-4]或以商业上可获得的3个步骤 2-羟甲基吡啶-3-醇[14173-30-9]; 2）制备4-羟基-1-（1H-咪唑-4-基）丁-1-酮，合成6,7-二氢-5H-咪唑并[1,5-a]吡啶的中间体 -8-（异构体I），如WO 2002/040484中所述，通过锂化从N，N-二甲基-2-（三烷基硅烷基）咪唑-1-磺酰胺进行，随后与适当保护的4-羟基丁醛反应，然后仲醇的氧化，酸诱导的咪唑脱保护和醇官能团的脱保护; 3）从被氧化的5,6,7,8-四氢咪唑并[1,5-a]吡啶[38666-30-7]进行的方法。

4. 发明申请

US20080076784A1 Bicyclic, Nitrogen-Containing Heterocycles and Aromatase Inhibitors 审中-公开
标题翻译：双环，含氮杂环和芳香酶抑制剂
公开(公告)号：US20080076784A1
公开(公告)日：2008-03-27
申请号：US11597585
申请日：2005-05-27
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christoph Schumacher , Michael Quirmbach
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christoph Schumacher , Michael Quirmbach
IPC分类号： A61K31/435 , A61K31/437 , A61K31/517 , A61P43/00 , C07D221/04 , C07D239/70 , C07D471/04
CPC分类号： C07D221/04 , C07D217/02 , C07D239/74 , C07D471/04
摘要： The application relates to novel heterocyclic compounds of the general formula (I) (I*) in which R, R1, R2, X, Y, Z and n have the meanings defined in the description, to a process for their preparation and to the use of these compounds as medicaments, in particular as aromatase inhibitors.
摘要翻译：本申请涉及通式（I）（I *）的新型杂环化合物，其中R 1，R 2，R 2，X，Y，Z和n具有描述中定义的含义，其制备方法和这些化合物作为药物的用途，特别是芳香酶抑制剂。

5. 发明申请

US20070066582A1 Diaminoalcohols as therapeutic compounds 审中-公开
标题翻译：二氨基醇作为治疗化合物
公开(公告)号：US20070066582A1
公开(公告)日：2007-03-22
申请号：US11522316
申请日：2006-09-18
申请人： Peter Herold , Robert Mah , Stefan Stutz , Vincenzo Tschinke , Aleksandar Stojanovic , Christiane Marti , Dirk Behnke , Nathalie Jotterand , Michael Quirmbach , Christoph Schumacher
发明人： Peter Herold , Robert Mah , Stefan Stutz , Vincenzo Tschinke , Aleksandar Stojanovic , Christiane Marti , Dirk Behnke , Nathalie Jotterand , Michael Quirmbach , Christoph Schumacher
IPC分类号： A61K31/55 , A61K31/54 , A61K31/5375 , A61K31/538 , A61K31/496 , A61K31/497 , A61K31/495 , A61K31/50 , A61K31/505
CPC分类号： A61K31/404 , Y02A50/411
摘要： Use of compounds of the general formula (I) wherein R1, R2, R3, R4, R5, R6 and X have the definitions elucidated in more detail in the description, as beta-secretase, cathepsin D, plasmepsin II and/or HIV protease inhibitors.
摘要翻译：通式（I）的化合物其中R 1，R 2，R 3，R 4，R 4， R 5，R 6和X的定义在说明书中更详细地描述为β-分泌酶，组织蛋白酶D，浆细胞素II和/或HIV蛋白酶抑制剂。

6. 发明授权

US08008334B2 Bis-heterocyclic imidazolyl compounds 有权
标题翻译：双杂环咪唑基化合物
公开(公告)号：US08008334B2
公开(公告)日：2011-08-30
申请号：US12086193
申请日：2006-12-08
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Michael Quirmbach , Christiane Marti , Aleksandar Stojanovic , Stefan Stutz
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Michael Quirmbach , Christiane Marti , Aleksandar Stojanovic , Stefan Stutz
IPC分类号： C07D235/02 , C07D403/00 , A01N43/52 , A61K31/415
CPC分类号： C07D471/04
摘要： The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R1, R2, R3, R4 and n have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.
摘要翻译：该专利申请涉及通式（I）的新的杂环化合物，其中R，R 1，R 2，R 3，R 4和n具有在说明书中更详细阐述的定义，其制备方法和使用这些化合物作为药物，特别是作为醛固酮合酶抑制剂。

7. 发明授权

US07767690B2 Amino alcohol derivatives and their use as renin inhibitor 失效
标题翻译：氨基醇衍生物及其作为肾素抑制剂的用途
公开(公告)号：US07767690B2
公开(公告)日：2010-08-03
申请号：US10587046
申请日：2005-01-21
申请人： Peter Herold , Stefan Stutz , Aleksandar Stojanovic , Vincenzo Tschinke , Christiane Marti , Michael Quirmbach
发明人： Peter Herold , Stefan Stutz , Aleksandar Stojanovic , Vincenzo Tschinke , Christiane Marti , Michael Quirmbach
IPC分类号： A61K31/435 , C07D221/04
CPC分类号： C07D215/38 , C07D401/06 , C07D401/12 , C07D405/12 , C07D471/08 , C07D471/10
摘要： The application relates to novel amino alcohols of the general formula (I) where R, R1, R2, R3, R4, R5 and R6 each have the definitions illustrated in detail in the description, to a process for their preparation and to the use of these compounds as medicines, in particular as renin inhibitors.
摘要翻译：本申请涉及通式（I）的新型氨基醇，其中R，R 1，R 2，R 3，R 4，R 5和R 6各自具有在说明书中详细说明的定义，其制备方法和使用这些化合物作为药物，特别是作为肾素抑制剂。

8. 发明申请

US20100029694A1 Heterocyclic compounds and their use as aldosterone synthase inhibitors 审中-公开
标题翻译：杂环化合物及其作为醛固酮合酶抑制剂的用途
公开(公告)号：US20100029694A1
公开(公告)日：2010-02-04
申请号：US12585584
申请日：2009-09-18
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christoph Schumacher , Michael Quirmbach
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christoph Schumacher , Michael Quirmbach
IPC分类号： A61K31/517 , A61K31/437 , A61P5/40
CPC分类号： C07D471/04 , C07D417/04
摘要： Heterocyclic compounds of the general formula (I) in which R, R1, R2, W, X, Y, Z and n have the meanings defined in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.
摘要翻译： R 1，R 2，W，X，Y，Z和n具有本说明书中定义的含义的通式（I）的杂环化合物，其制备方法和这些化合物作为药物的用途，特别是作为醛固酮合酶抑制剂。

9. 发明申请

US20090306064A1 Substituted Piperidines as Renin Inhibitors 失效
标题翻译：取代哌啶酮作为肾素抑制剂
公开(公告)号：US20090306064A1
公开(公告)日：2009-12-10
申请号：US11887355
申请日：2006-03-30
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Dirk Behnke , Christiane Marti , Nathalie Jotterand , Stefan Stutz , Michael Quirmbach
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Dirk Behnke , Christiane Marti , Nathalie Jotterand , Stefan Stutz , Michael Quirmbach
IPC分类号： A61K31/538 , C07D413/12 , A61P9/12 , A61P9/00
CPC分类号： C07D413/12 , C07D413/14
摘要： Compounds of the general formula (I) in which the meanings of the substituents R1, R2, R3, R4, X, Z and n as stated in claim 1 have renin-inhibiting properties and can be used as medicines.
摘要翻译：具有权利要求1所述的取代基R 1，R 2，R 3，R 4，X，Z和n的含义的通式（I）的化合物具有肾素抑制性质并可用作药物。

10. 发明申请

US20090306062A1 2,5-Disubstituted Piperidines 审中-公开
标题翻译： 2,5-二取代哌啶子
公开(公告)号：US20090306062A1
公开(公告)日：2009-12-10
申请号：US12308117
申请日：2007-06-07
申请人： Peter Herold , Robert Mah , Stefan Stutz , Vincenzo Tschinke , Isabelle Lyothier , Stjepan Jelakovic , Michael Quirmbach , Christiane Marti
发明人： Peter Herold , Robert Mah , Stefan Stutz , Vincenzo Tschinke , Isabelle Lyothier , Stjepan Jelakovic , Michael Quirmbach , Christiane Marti
IPC分类号： A61K31/5386 , C07D413/14 , A61K31/538 , C07D498/10
CPC分类号： C07D413/12 , C07D405/12 , C07D405/14 , C07D413/14
摘要： The application relates to 2,5-disubstituted piperidines, their preparation and use as medicines, especially as renin inhibitors, of the general formula (I) in which R, R1 and X are each as defined in detail in the description, and pharmaceutical preparations comprising these compounds.
摘要翻译：本申请涉及2,5-二取代的哌啶，它们的制备和用途作为通式（I）的药物，特别是作为肾素抑制剂，其中R，R 1和X X各自如说明书中详细定义，药物制剂包括这些化合物。

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