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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

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。

3. 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.

4. 发明申请

WO2012175487A1 CYCLOHEXYL ISOQUINOLINONE COMPOUNDS 审中-公开
标题翻译：环辛基异喹啉化合物
公开(公告)号：WO2012175487A1
公开(公告)日：2012-12-27
申请号：PCT/EP2012/061691
申请日：2012-06-19
申请人： NOVARTIS AG , HOLZER, Philipp , MASUYA, Keiichi , GUAGNANO, Vito , FURET, Pascal , KALLEN, Joerg , STUTZ, Stefan
发明人： HOLZER, Philipp , MASUYA, Keiichi , GUAGNANO, Vito , FURET, Pascal , KALLEN, Joerg , STUTZ, Stefan
IPC分类号： C07D217/04 , C07D405/08 , A61K31/47 , A61P35/00
CPC分类号： C07D217/24 , A61K31/472 , A61K31/4725 , C07D217/04 , C07D401/08 , C07D405/08
摘要： The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
摘要翻译：本发明涉及式（I）化合物：如申请中所定义。这些化合物适用于治疗由MDM2和/或MDM4或其变体的活性介导的病症或疾病。

5. 发明申请

WO2011076786A1 SUBSTITUTED ISOQUINOLINONES AND QUINAZOLINONES 审中-公开
标题翻译：取代的异喹啉和喹唑啉酮
公开(公告)号：WO2011076786A1
公开(公告)日：2011-06-30
申请号：PCT/EP2010/070364
申请日：2010-12-21
申请人： NOVARTIS AG , BERGHAUSEN, Joerg , BUSCHMANN, Nicole , FURET, Pascal , GESSIER, François , HERGOVICH LISZTWAN, Joanna , HOLZER, Philipp , JACOBY, Edgar , KALLEN, Joerg , MASUYA, Keiichi , PISSOT SOLDERMANN, Carole , REN, Haixia , STUTZ, Stefan
发明人： BERGHAUSEN, Joerg , BUSCHMANN, Nicole , FURET, Pascal , GESSIER, François , HERGOVICH LISZTWAN, Joanna , HOLZER, Philipp , JACOBY, Edgar , KALLEN, Joerg , MASUYA, Keiichi , PISSOT SOLDERMANN, Carole , REN, Haixia , STUTZ, Stefan
IPC分类号： A61P35/00 , A61K31/495 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D405/14 , C07D413/14 , C07D217/24
CPC分类号： C07D239/82 , C07D217/24 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The invention relates to substituted nitrogen containing bicyclic heterocycles of the formula (I): wherein Z is CH 2 or N-R 4 and X, R 1 , R 2 , R 4 , R 6 , R 7 and n are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
摘要翻译：本发明涉及式（I）的取代的含氮双环杂环：其中Z是CH 2或N-R 4，X，R 1，R 2，R 4，R 6，R 7和n如说明书中所定义。这些化合物适用于治疗由MDM2和/或MDM4或其变体的活性介导的病症或疾病。

6. 发明申请

WO2009106599A3 SUBSTITUTED PIPERIDINES AS THERAPEUTIC COMPOUNDS 审中-公开
标题翻译：替代的哌啶类作为治疗化合物
公开(公告)号：WO2009106599A3
公开(公告)日：2009-12-03
申请号：PCT/EP2009052335
申请日：2009-02-27
申请人： NOVARTIS AG , HEROLD PETER , MAH ROBERT , STUTZ STEFAN , TSCHINKE VINCENZO , LYOTHIER ISABELLE , JELAKOVIC STJEPAN
发明人： HEROLD PETER , MAH ROBERT , STUTZ STEFAN , TSCHINKE VINCENZO , LYOTHIER ISABELLE , JELAKOVIC STJEPAN
IPC分类号： C07D405/12 , A61K31/445 , A61K31/4523 , A61K31/538 , A61K31/5386 , C07D405/14 , C07D413/12 , C07D413/14
CPC分类号： C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14
摘要： Use of compounds of the general formula (I) and pharmaceutically acceptable salt thereof, in which R, R1 and X have the definitions illustrated in detail in the description, as beta-secretase, cathepsin D, plasmepsin Il and/or HIV protease inhibitors.
摘要翻译：其中R，R 1和X具有描述中详细说明的定义的通式（I）化合物及其药学上可接受的盐作为β-分泌酶，组织蛋白酶D，浆细胞蛋白酶II和/或HIV蛋白酶抑制剂。

7. 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

8. 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

9. 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.

10. 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。

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