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1. 发明申请

WO2009053452A1 4,4-DISUBSTITUTED PIPERIDINES 审中-公开
标题翻译： 4,4-取代的哌啶
公开(公告)号：WO2009053452A1
公开(公告)日：2009-04-30
申请号：PCT/EP2008/064417
申请日：2008-10-24
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , BEHNKE, Dirk , JELAKOVIC, Stjepan , JOTTERAND, Nathalie , STUTZ, Stefan , LYOTHIER, Isabelle
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , BEHNKE, Dirk , JELAKOVIC, Stjepan , JOTTERAND, Nathalie , STUTZ, Stefan , LYOTHIER, Isabelle
IPC分类号： C07D413/14 , C07D413/12 , A61K31/538 , A61P9/12
CPC分类号： C07D413/12 , C07D413/14
摘要： The application relates to 4,4-disubstituted piperidines of the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R 2 , has the meanings explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.
摘要翻译：本申请涉及通式（I）的4,4-二取代哌啶及其盐，优选其药学上可接受的盐，其中R2具有说明书中所述的含义，其制备方法和这些化合物的用途作为药物，特别是作为肾素抑制剂。

2. 发明申请

WO2008031811A1 NITRATE ESTERS OF AMINOALCOHOLS 审中-公开
标题翻译：硝酸酯的硝酸酯
公开(公告)号：WO2008031811A1
公开(公告)日：2008-03-20
申请号：PCT/EP2007/059504
申请日：2007-09-11
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , MARTI, Christiane , JOTTERAND, Nathalie
发明人： HEROLD, Peter , MAH, Robert , MARTI, Christiane , JOTTERAND, Nathalie
IPC分类号： C07C233/13 , C07D209/08 , C07D213/64 , C07D231/56 , C07D265/36 , C07D307/80 , A61K31/404 , A61K31/343 , A61K31/44 , A61K31/416 , A61P9/10 , A61P9/12
CPC分类号： C07C237/20 , C07C2601/14 , C07D209/12 , C07D211/16 , C07D211/30 , C07D213/56 , C07D213/64 , C07D215/54 , C07D231/56 , C07D265/36 , C07D307/80 , C07D401/12 , C07D405/12 , C07D413/12
摘要： The application relates to novel nitrate ester derivatives of substituted aminoalcohols of the general formula (I), wherein R 1 , R 2 , R 3 , V, X, Y and Z 0 have the meanings explained in more detail in the description, to a process for their preparation and to the use of these compounds as therapeutics in cardiovascular diseases, in particular in high blood pressure and vascular and organ damage accompanying high blood pressure.
摘要翻译：本申请涉及通式（I）的取代氨基醇的新型硝酸酯衍生物，其中R 1，R 2，R 3， V，X，Y和Z 0具有在描述中更详细解释的含义，其制备方法和这些化合物作为心血管疾病，特别是高血液中的治疗剂压力和血管和器官损伤伴随高血压。

3. 发明申请

WO2007113235A1 PROCESS FOR PREPARING 6,7-DIHYDRO-5H-IMIDAZO[1,5-A]PYRIDIN-8-ONE 审中-公开
标题翻译：制备6,7-二氢-5H-咪唑并[1,5-a]吡啶-8-酮的方法
公开(公告)号：WO2007113235A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053078
申请日：2007-03-30
申请人： Speedel Experimenta AG , MARTIN, Pierre , BOUDIER, Andreas , QUIRMBACH, Michael , MAH, Robert , JOTTERAND, Nathalie
发明人： MARTIN, Pierre , BOUDIER, Andreas , QUIRMBACH, Michael , MAH, Robert , JOTTERAND, Nathalie
IPC分类号： C07D213/65 , C07D233/22 , C07D471/04 , C07F7/08 , C07F7/18
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，其胺转化为甲酰胺，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] 一种适当保护的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-酮的方法，由6,7-二氢-5H-咪唑并[1,5-a]吡啶 -8-（咪唑-1-基）磺酰胺的N，N-二甲基-2-（三烷基硅烷基）咪唑-1-磺酰胺进行的步骤（WO 2002/040484中所述），然后与适当保护的4-羟基丁醛反应，随后与仲醇的氧化，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

WO2008017685A1 NITRATE ESTERS OF PIPERIDINES 审中-公开
标题翻译：硝酸酯系列
公开(公告)号：WO2008017685A1
公开(公告)日：2008-02-14
申请号：PCT/EP2007/058207
申请日：2007-08-07
申请人： Speedel Experimenta AG , HEROLD, Peter , MAH, Robert , STUTZ, Stefan , TSCHINKE, Vincenzo , LYOTHIER, Isabelle , SCHUMACHER, Christoph , MARTI, Christiane , JOTTERAND, Nathalie
发明人： HEROLD, Peter , MAH, Robert , STUTZ, Stefan , TSCHINKE, Vincenzo , LYOTHIER, Isabelle , SCHUMACHER, Christoph , MARTI, Christiane , JOTTERAND, Nathalie
IPC分类号： C07D401/04 , C07D405/04 , C07D405/12 , C07D413/04 , A61K31/445 , A61P9/00
CPC分类号： C07D413/04 , C07D211/52 , C07D401/04 , C07D405/04 , C07D405/12
摘要： The application relates to novel nitrate ester derivatives of substituted piperidines of the general formula (I), wherein R 1 , R 2 , R 3 , X, Y and Z 0 , and m, n, p and q have the meanings explained in more detail in the description, a process for their preparation and the use of these compounds as a curative agent in cardiovascular diseases, in particular in high blood pressure and vascular and organ damage accompanying high blood pressure.
摘要翻译：本申请涉及通式（I）的取代哌啶的新型硝酸酯衍生物，其中R 1，R 2，R 3， X，Y和Z 0，m，n，p和q具有在说明书中更详细解释的含义，其制备方法和这些化合物作为心血管中的治疗剂的用途疾病，特别是伴有高血压的高血压和血管和器官损伤。

5. 发明申请

WO2006128853A1 HETEROCYCLIC SPIRO-COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS 审中-公开
标题翻译：杂环化合物作为醛固酮合成酶抑制剂
公开(公告)号：WO2006128853A1
公开(公告)日：2006-12-07
申请号：PCT/EP2006/062696
申请日：2006-05-30
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , MARTI, Christiane , JOTTERAND, Nathalie , SCHUMACHER, Christoph , QUIRMBACH, Michael
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , MARTI, Christiane , JOTTERAND, Nathalie , SCHUMACHER, Christoph , QUIRMBACH, Michael
IPC分类号： C07D471/20 , A61K31/35 , A61P9/00
CPC分类号： C07D471/20
摘要： The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R 1 , R 2 , W, X, Y, Z 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 1，R 2，R 2，W，X，Y，Z和n具有在本说明书中更详细地描述了其定义，制备方法以及这些化合物作为药物，特别是醛固酮合酶抑制剂的用途。

6. 发明申请

WO2006128851A1 FUSED IMIDAZOLE DERIVATIVES AND USE THEREOF AS ALDOSTERONE SYNTHASE INHIBITORS 审中-公开
标题翻译：熔融咪唑衍生物及其作为阿糖胞苷合成酶抑制剂的用途
公开(公告)号：WO2006128851A1
公开(公告)日：2006-12-07
申请号：PCT/EP2006/062694
申请日：2006-05-30
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , MARTI, Christiane , JOTTERAND, Nathalie , SCHUMACHER, Christoph , QUIRMBACH, Michael
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , MARTI, Christiane , JOTTERAND, Nathalie , SCHUMACHER, Christoph , QUIRMBACH, Michael
IPC分类号： A61K31/438 , C07D471/04 , C07D491/20 , C07D471/20 , A61P5/02
CPC分类号： C07D471/04
摘要： The patent application relates to new heterocyclic compounds of the general formula (I) in which A, R, R 1 , R 2 , X, Y, Z, n and p 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A，R，R 1，R 2，X，Y，Z，n和p 在描述中更详细地定义了这些定义，其制备方法以及这些化合物作为药物，特别是作为醛固酮合酶抑制剂的用途。

7. 发明申请

WO2006005741A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2006005741A2
公开(公告)日：2006-01-19
申请号：PCT/EP2005053306
申请日：2005-07-11
申请人： SPEEDEL EXPERIMENTA AG , HEROLD PETER , MAH ROBERT , STUTZ STEFAN , STOJANOVIC ALEKSANDAR , TSCHINKE VINCENZO , JOTTERAND NATHALIE , BEHNKE DIRK
发明人： HEROLD PETER , MAH ROBERT , STUTZ STEFAN , STOJANOVIC ALEKSANDAR , TSCHINKE VINCENZO , JOTTERAND NATHALIE , BEHNKE DIRK
IPC分类号： C07D413/14 , A61K31/538 , C07D413/12
CPC分类号： C07D413/12 , C07D413/14
摘要： The application relates to novel substituted piperidines of the general formula (I) in which R 1 , R 2 , R 3 , R 4 , W, X, Z, m and n 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：本申请涉及通式（I）的新的取代的哌啶，其中R 1，R 2，R 3，R 3， 4，W，X，Z，m和n各自在说明书中详细描述，其制备方法和这些化合物作为药物，特别是作为肾素抑制剂的用途。

8. 发明申请

WO2009074674A3 TRISUBSTITUTED PIPERIDINES AS RENIN INHIBITORS 审中-公开
标题翻译：作为RININ抑制剂的TRISUBSTITUTED PIPERIDINES
公开(公告)号：WO2009074674A3
公开(公告)日：2009-07-30
申请号：PCT/EP2008067407
申请日：2008-12-12
申请人： NOVARTIS AG , HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , JELAKOVIC STJEPAN , STUTZ STEFAN , BEHNKE DIRK , JOTTERAND NATHALIE
发明人： HEROLD PETER , MAH ROBERT , TSCHINKE VINCENZO , JELAKOVIC STJEPAN , STUTZ STEFAN , BEHNKE DIRK , JOTTERAND NATHALIE
IPC分类号： C07D491/113 , A61K31/435 , A61P9/00 , A61P13/00 , C07D491/107
CPC分类号： C07D491/107 , C07D491/113
摘要： The application relates to trisubstituted piperidines of the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R1, R2', X, U, W, m and n have the meanings explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.
摘要翻译：本申请涉及通式（I）的三取代哌啶及其盐，优选其药学上可接受的盐，其中R 1，R 2'，X，U，W，m和n具有说明书中所述的含义，它们的制备和这些化合物作为药物的使用，特别是作为肾素抑制剂。

9. 发明申请

WO2008119744A1 HETEROCYCLIC SPIRO-COMPOUNDS 审中-公开
标题翻译：杂环螺旋化合物
公开(公告)号：WO2008119744A1
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053671
申请日：2008-03-27
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , STUTZ, Stefan , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , JOTTERAND, Nathalie , BENNACER, Bibia
发明人： HEROLD, Peter , MAH, Robert , STUTZ, Stefan , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , JOTTERAND, Nathalie , BENNACER, Bibia
IPC分类号： C07D491/20 , A61P5/00 , A61P9/00 , A61K31/4188
CPC分类号： C07D491/20
摘要： The patent application relates to new heterocyclic compounds of the general formula (I), in which R, R 1 , R 2 , Q, T, n and p 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）的新杂环化合物，其中R 1，R 2，R 2，Q，T，n和p具有定义在描述中更详细地阐明，制备它们的方法以及这些化合物作为药物，特别是作为醛固酮合酶抑制剂的用途。

10. 发明申请

WO2007082907A1 SUBSTITUTED 4-PHENYLPIPERIDINES 审中-公开
标题翻译：取代的4-苯基哌啶
公开(公告)号：WO2007082907A1
公开(公告)日：2007-07-26
申请号：PCT/EP2007/050481
申请日：2007-01-18
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , BEHNKE, Dirk , JOTTERAND, Nathalie , STOJANOVIC, Aleksandar , STUTZ, Stefan , JELAKOVIC, Stjepan , QUIRMBACH, Michael
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , BEHNKE, Dirk , JOTTERAND, Nathalie , STOJANOVIC, Aleksandar , STUTZ, Stefan , JELAKOVIC, Stjepan , QUIRMBACH, Michael
IPC分类号： C07D413/12 , C07D413/14 , A61P9/12 , A61K31/538
CPC分类号： C07D401/12 , C07D413/12 , C07D413/14
摘要： The application relates to substituted 4-phenylpiperidines of the general formula and their salts, preferably their pharmaceutically acceptable salts, in which R 2 , R 3 , W and X have the meanings explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.
摘要翻译：本申请涉及通式的取代的4-苯基哌啶及其盐，优选其药学上可接受的盐，其中R 2，R 3，W和X具有如下含义：在说明书中解释，其制备方法和这些化合物作为药物的使用，特别是作为肾素抑制剂。

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