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11. 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。

12. 发明申请

WO2006061426A1 ω-PHENYLOCTANAMIDES 审中-公开
标题翻译：？-PHENYLOCTANAMIDES
公开(公告)号：WO2006061426A1
公开(公告)日：2006-06-15
申请号：PCT/EP2005/056622
申请日：2005-12-09
申请人： Speedel Experimenta AG , HEROLD, Peter , STUTZ, Stefan , MAH, Robert , TSCHINKE, Vincenzo , MARTI, Christiane
发明人： HEROLD, Peter , STUTZ, Stefan , MAH, Robert , TSCHINKE, Vincenzo , MARTI, Christiane
IPC分类号： C07C237/20 , A61K31/165
CPC分类号： C07C255/59 , C07C237/20 , C07D317/58 , C07D319/18
摘要： Compounds of the general formula (I) in which the substituents R, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are each as defined in Claim 1 have renin-inhibiting properties and can be used as medicaments.
摘要翻译：通式（I）的化合物，其中取代基R 1，R 1，R 2，R 3，R 4， R 5，R 6和R 6各自如权利要求1中所定义，具有肾素抑制性质，可用作药物。

13. 发明申请

WO2005070870A3 AMINO ALCOHOL DERIVATIVES AND THEIR USE AS RENIN INHIBITORS 审中-公开
公开(公告)号：WO2005070870A3
公开(公告)日：2005-08-04
申请号：PCT/EP2005/050273
申请日：2005-01-21
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , STUTZ, Stefan , STOJANOVIC, Aleksandar , TSCHINKE, Vincenzo , MARTI, Christiane , QUIRMBACH, Michael
发明人： HEROLD, Peter , STUTZ, Stefan , STOJANOVIC, Aleksandar , TSCHINKE, Vincenzo , MARTI, Christiane , QUIRMBACH, Michael
IPC分类号： C07C213/08
摘要： The application relates to novel amino alcohols of the general formula (I) where R, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 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.

14. 发明申请

WO2007085651A1 PROCESS FOR THE PREPARATION OF ORGANIC COMPOUNDS 审中-公开
标题翻译：制备有机化合物的方法
公开(公告)号：WO2007085651A1
公开(公告)日：2007-08-02
申请号：PCT/EP2007/050816
申请日：2007-01-29
申请人： Speedel Experimenta AG , HEROLD, Peter , STUTZ, Stefan , MAH, Robert , STOJANOVIC, Aleksandar , LYOTHIER, Isabelle , BEHNKE, Dirk , SPINDLER, Felix , BAPPERT, Erhard
发明人： HEROLD, Peter , STUTZ, Stefan , MAH, Robert , STOJANOVIC, Aleksandar , LYOTHIER, Isabelle , BEHNKE, Dirk , SPINDLER, Felix , BAPPERT, Erhard
IPC分类号： C07D231/56 , C07D471/04
CPC分类号： C07D471/04 , C07D231/56
摘要： Compounds of the formula I, in which R' 1 and R' 2 represent, independently of one another, H, C 1 -C 8 -alkyl, halogen, polyhalo-C 1 -C 8 -alkoxy, polyhalo-C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -alkoxy-C 1 -C 8 -alkyl or C 1 -C 8 -alkoxy-C 1 -C 8 -alkoxy, R' 1 and R' 2 not simultaneously representing H, and R' 3 represents C 1 -C 8 -alkyl and in which the carbon atom to which the R' 3 radical is bonded exhibits either the (R) or (S) configuration, the (R) configuration being preferred, can be obtained in high yields by a stereoselective addition of R' 3 -substituted propionates to RV and R' 2 -substituted unsaturated bicyclic heterocyclyl aldehydes of the formula R-CHO to give corresponding 3-R-3-hydroxy-2-R' 3 -propionates. Conversion of the OH group to a leaving group, subsequently a regioselective elimination to give 3-R-2-R' 3 -propenoates, followed by 1 ) the saponification to give the corresponding 3-R-2-R' 3 -propenoic acids, the enantioselective hydrogenation thereof to give corresponding chiral 3-R-2-R' 3 -propanoic acids and the reduction thereof, or 2) the saponification to give the corresponding 3-R-2-R' 3 -propenoic acids, the reduction thereof to give corresponding 3-R-2-R' 3 -allyl alcohols and the enantioselective hydrogenation thereof, or 3) the reduction to give corresponding 3-R-2-R' 3 -allyl alcohols and the enantioselective hydrogenation thereof, R being
摘要翻译：其中R 1'和R“2'的式I化合物彼此独立地表示H，C 1 -C 3烷基，烷基，卤素，多卤代-C 1 -C 8 - 烷氧基，多卤代-C 1 -C 1 - C 1 -C 8 - 烷氧基，C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基，C 1 -C 8 - - 烷氧基-C 1 -C 8 - 烷基或C 1 -C 8 - 烷氧基-C R 1'和R“2不同时表示H，R' N 3表示C 1 -C 8 - 烷基，并且其中R'3个基团的碳原子是（R）或（S）构型可以以高收率通过立体选择性添加R'3 - 取代丙酸酯至RV和R' 式R-CHO的2-取代的不饱和双环杂环基醛，得到相应的3-R-3-羟基-2R'3 - 丙酸酯。将OH基转化为离去基团，随后进行区域选择性消除，得到3-R-2-R“3 - 丙烯酸酯，然后1）皂化，得到相应的3-R-2 -R'3'-丙烯酸，其对映选择性氢化反应，得到相应的手性3-R-2-R'3'-丙酸及其还原剂，或2）皂化，得到相应的3-R-2-R“3 - 丙烯酸，将其还原，得到相应的3-R-2-R”3 - 烯丙基醇和其对映体选择性氢化，或3）还原反应得到相应的3-R-2-R“3 - 烯丙醇及其对映选择性氢化，R为

15. 发明申请

WO2006095020A1 HETEROCYCLIC-SUBSTITUTED ALKANAMIDES USEFUL AS RENIN INHIBITORS 审中-公开
标题翻译：作为RININ抑制剂有用的杂环取代的烷烃
公开(公告)号：WO2006095020A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/060625
申请日：2006-03-10
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STUTZ, Stefan , BEHNKE, Dirk , STOJANOVIC, Aleksandar , JELAKOVIC, Stjepan , MARTI, Christiane
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , STUTZ, Stefan , BEHNKE, Dirk , STOJANOVIC, Aleksandar , JELAKOVIC, Stjepan , MARTI, Christiane
IPC分类号： C07C237/20 , C07D307/14 , C07D321/08 , C07D211/58 , C07D307/52 , C07D307/93 , C07D207/14 , C07D205/04 , C07D319/12 , C07D493/08 , C07D309/04 , C07D311/96 , C07D309/14 , C07D303/36 , C07D311/94
CPC分类号： C07D309/06 , C07C237/20 , C07D207/14 , C07D211/58 , C07D303/36 , C07D307/00 , C07D307/14 , C07D307/20 , C07D307/52 , C07D307/93 , C07D309/08 , C07D309/10 , C07D311/00 , C07D311/94 , C07D311/96 , C07D313/14 , C07D319/12 , C07D319/14 , C07D321/08 , C07D493/08
摘要： Compounds of the general formula (I) in which the meanings of the substituents R 1 and R 2 are as stated in claim 1, have renin-inhibiting properties and can be used as medicines.
摘要翻译：其中取代基R 1和R 2的含义如权利要求1所述的通式（I）的化合物具有肾素抑制性质并且可以使用作为药物

16. 发明申请

WO2006005741A3 PIPERDINE DERIVATIVES AS RENIN INHIBITORS 审中-公开
公开(公告)号：WO2006005741A3
公开(公告)日：2006-01-19
申请号：PCT/EP2005/053306
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 , C07D413/12 , A61K31/538
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.

17. 发明申请

WO2005090304A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2005090304A1
公开(公告)日：2005-09-29
申请号：PCT/EP2005/051241
申请日：2005-03-17
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , STUTZ, Stefan , MAH, Robert , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , JOTTERAND, Nathalie , QUIRMBACH, Michael , BEHNKE, Dirk , MARTI, Christiane
发明人： HEROLD, Peter , STUTZ, Stefan , MAH, Robert , TSCHINKE, Vincenzo , STOJANOVIC, Aleksandar , JOTTERAND, Nathalie , QUIRMBACH, Michael , BEHNKE, Dirk , MARTI, Christiane
IPC分类号： C07D209/12
CPC分类号： C07D209/12 , C07D401/06
摘要： The invention relates to novel amino alcohols of the general formula (I) where X, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 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各自如上所定义在描述中详细描述了它们的制备方法和这些化合物作为药物的用途，特别是作为肾素抑制剂。

18. 发明申请

WO2005061457A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2005061457A1
公开(公告)日：2005-07-07
申请号：PCT/EP2004/052389
申请日：2004-09-30
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , STUTZ, Stefan , STOJANOVIC, Aleksandar , TSCHINKE, Vincenzo , JOTTERAND, Nathalie
发明人： HEROLD, Peter , MAH, Robert , STUTZ, Stefan , STOJANOVIC, Aleksandar , TSCHINKE, Vincenzo , JOTTERAND, Nathalie
IPC分类号： C07D211/42
CPC分类号： C07D211/42 , C07D401/12 , C07D413/12
摘要： Novel substituted piperidines of the general formulae (I) and (II) with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent.
摘要翻译：描述通式（I）和（II）的新颖取代的哌啶与具有如在说明书中详细说明的取代基定义。该化合物特别适合作为肾素抑制剂，并且是非常有效的。

19. 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。

20. 发明申请

WO2008055941A1 PROCESS FOR PREPARING OF 2-ALKYL 3-ARYL PROP-2-2ENE-1-OLS 审中-公开
标题翻译：制备2-烷基-3-芳基丙-2-烯-1-醇的方法
公开(公告)号：WO2008055941A1
公开(公告)日：2008-05-15
申请号：PCT/EP2007/062024
申请日：2007-11-08
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , STUTZ, Stefan , STOJANOVIC, Aleksandar , LYOTHIER, Isabelle , BEHNKE, Dirk
发明人： HEROLD, Peter , MAH, Robert , STUTZ, Stefan , STOJANOVIC, Aleksandar , LYOTHIER, Isabelle , BEHNKE, Dirk
IPC分类号： C07C29/36 , C07C29/44 , C07C41/18 , C07C41/30 , C07C43/23
CPC分类号： C07C41/20 , C07B2200/07 , C07C41/22 , C07C41/30 , C07C231/12 , C07C235/34 , C07C43/23 , C07C43/225
摘要： Process for preparing a compound of the formula (I) in which R 1 and R 2 are each independently H, C 1 -C 8 -alkyl, halogen, polyhalo-C 1 -C 8 -alkoxy, polyhalo-C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -alkoxy-C 1 -C 8 -alkyl, or C 1 -C 8 -alkoxy-C 1 -C 8 -alkoxy, where R 1 and R 2 are not both H, and R 3 is C 1 -C 8 -alkyl, which is characterized in that a) a compound of the formula (II) in which R 1 and R 2 are each as defined above and X is Br, I, triflate, toyslate or mesylate is reacted with prop-2-yn-1-ol to give the compound of the formula (III), b) the compound of the formula (III) is reacted with an alkyl-metal compound in which "alkyl" is as defined above for R 3 to give a compound of the formula (I).
摘要翻译：制备式（I）化合物的方法，其中R 1和R 2各自独立地为H，C 1 -C 3 烷基，卤素，多卤代-C 1 -C 8 - 烷氧基，多卤代-C 1 -C 3 C 1 -C 8烷基，C 1 -C 8 - 烷氧基，C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基，C 1 -C 8 - - 烷氧基-C 1 -C 8 - 烷基或C 1 -C 8 - 烷氧基-C 其中R 1和R 2都不是H，R 1和R 2都不是H， 3是C 1 -C 8 - 烷基，其特征在于a）式（II）的化合物，其中R 1 R 2和R 2各自如上所定义，X是Br，I，三氟甲磺酸酯，玩具和甲磺酸酯与丙-2-炔-1-醇反应，得到式（III）的化合物，b）式（III）化合物与烷基金属化合物反应，其中“烷基”如上述R 3所定义，得到式（I ）。

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