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1. 发明申请

US20120115859A1 3,4,5-SUBSTITUTED PIPERIDINES AS RENIN INHIBITORS 审中-公开
标题翻译：作为RENIN抑制剂的3,4,5-取代的哌啶
公开(公告)号：US20120115859A1
公开(公告)日：2012-05-10
申请号：US13349869
申请日：2012-01-13
申请人： Peter HEROLD , Robert Mah , Vincenzo Tschinke , Nathalie Jotterand , Dirk Behnke , Aleksandar Stojanovic , Stefan Stutz , Michael Quirmbach , Stjepan Jelakovic
发明人： Peter HEROLD , Robert Mah , Vincenzo Tschinke , Nathalie Jotterand , Dirk Behnke , Aleksandar Stojanovic , Stefan Stutz , Michael Quirmbach , Stjepan Jelakovic
IPC分类号： A61K31/538 , C07D413/14 , C07D405/12 , A61K31/453 , A61P9/00 , A61P9/04 , A61P27/06 , A61P9/10 , A61P13/12 , C07D413/12 , A61P9/12
CPC分类号： C07D413/14 , C07D413/12
摘要： The application relates to novel substituted piperidines of the general formula (II) in which R1′, R2′, R2″, R4′, X, Z, m and n have the meanings defined in the description, to a process for the preparation thereof and to the use of these compounds as medicines, especially as renin inhibitors.
摘要翻译：本申请涉及通式（II）的新的取代的哌啶，其中R1'，R2'，R2“，R4'，X，Z，m和n具有本说明书中定义的含义与制备方法以及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

US07625893B2 Substituted 4-phenyl piperidines for use as renin inhibitors 失效
标题翻译：取代的4-苯基哌啶用作肾素抑制剂
公开(公告)号：US07625893B2
公开(公告)日：2009-12-01
申请号：US12224440
申请日：2007-10-03
申请人： Peter Herold , Robert Mah , Stefan Stutz , Vincenzo Tschinke , Aleksandar Stojanovic , Dirk Behnke , Nathalie Jotterand , Stjepan Jelakovic
发明人： Peter Herold , Robert Mah , Stefan Stutz , Vincenzo Tschinke , Aleksandar Stojanovic , Dirk Behnke , Nathalie Jotterand , Stjepan Jelakovic
IPC分类号： C07D413/12 , A61K31/538
CPC分类号： C07D413/12
摘要： Compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which R1 is straight-chain C1-8-alkanoyloxy, straight-chain C1-8-alkoxy, straight-chain C1-8-alkoxy-straight-chain-C1-8-alkoxy, straight-chain C1-8-alkoxycarbonylamino, straight-chain C0-8-alkylcarbonylamino, optionally N-mono- or N,N-di-C1-8-alkylated amino or hydroxy or straight-chain omega-hydroxy-C1-8-alkyl.
摘要翻译：通式（I）的化合物及其盐，优选其药学上可接受的盐; 其中R 1为直链C 1-8 - 烷酰氧基，直链C 1-8 - 烷氧基，直链C 1-8 - 烷氧基 - 直链-C 1-8 - 烷氧基，直链C 1-8烷氧基羰基氨基，直链C0-8-烷基羰基氨基，任选N-单或N，N-二-C 1-8 - 烷基化氨基或羟基或直链ω-羟基-C 1-8 - 烷基。

3. 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。

4. 发明授权

US07842688B2 Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US07842688B2
公开(公告)日：2010-11-30
申请号：US12068443
申请日：2008-02-06
申请人： Peter Herold , Robert Mah , Stefan Stutz , Aleksandar Stojanovic , Vincenzo Tschinke , Nathalie Jotterand
发明人： Peter Herold , Robert Mah , Stefan Stutz , Aleksandar Stojanovic , Vincenzo Tschinke , Nathalie Jotterand
IPC分类号： C07D401/12 , A61K31/4427
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。

5. 发明申请

US20090088426A1 Substituted 4-Phenyl Piperidines for Use as Renin Inhibitors 失效
标题翻译：用作肾素抑制剂的取代的4-苯基哌啶子
公开(公告)号：US20090088426A1
公开(公告)日：2009-04-02
申请号：US12224440
申请日：2007-10-03
申请人： Peter Herold , Robert Mah , Stefan Stutz , Vincenzo Tschinke , Aleksandar Stojanovic , Dirk Behnke , Nathalie Jotterand , Stjepan Jelakovic
发明人： Peter Herold , Robert Mah , Stefan Stutz , Vincenzo Tschinke , Aleksandar Stojanovic , Dirk Behnke , Nathalie Jotterand , Stjepan Jelakovic
IPC分类号： A61K31/538 , C07D265/36 , A61P9/00 , A61P13/12
CPC分类号： C07D413/12
摘要： Compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which R1 is straight-chain C1-8-alkanoyloxy, straight-chain C1-8-alkoxy, straight-chain C1-8-alkoxy-straight-chain-C1-8-alkoxy, straight-chain C1-8-alkoxycarbonylamino, straight-chain C0-8-alkylcarbonylamino, optionally N-mono- or N,N-di-C1-8-alkylated amino or hydroxy or straight-chain omega-hydroxy-C1-8-alkyl.
摘要翻译：通式（I）的化合物及其盐，优选其药学上可接受的盐; 其中R 1为直链C 1-8 - 烷酰氧基，直链C 1-8 - 烷氧基，直链C 1-8 - 烷氧基 - 直链-C 1-8 - 烷氧基，直链C 1-8烷氧基羰基氨基，直链C0-8-烷基羰基氨基，任选N-单或N，N-二-C 1-8 - 烷基化氨基或羟基或直链ω-羟基-C 1-8 - 烷基。

6. 发明申请

US20090012055A1 Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US20090012055A1
公开(公告)日：2009-01-08
申请号：US12068443
申请日：2008-02-06
申请人： Peter Herold , Robert Mah , Stefan Stutz , Aleksandar Stojanovic , Vincenzo Tschinke , Nathalie Jotterand
发明人： Peter Herold , Robert Mah , Stefan Stutz , Aleksandar Stojanovic , Vincenzo Tschinke , Nathalie Jotterand
IPC分类号： A61K31/397 , C07D211/40 , A61K31/445 , C07D265/36 , A61K31/538 , C07D413/02 , A61K31/454 , A61K31/4525 , A61K31/5415 , A61P13/12 , A61P9/00 , C07D279/16 , C07D401/02 , C07D215/00 , A61K31/4709 , A61K31/5377 , C07D239/24 , A61K31/506
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。

7. 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。

8. 发明申请

US20070010511A1 Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US20070010511A1
公开(公告)日：2007-01-11
申请号：US10574108
申请日：2004-09-30
申请人： Peter Herold , Robert Mah , Stefan Stutz , Aleksandar Stojanovic , Vincenzo Tschinke , Nathalie Jotterand
发明人： Peter Herold , Robert Mah , Stefan Stutz , Aleksandar Stojanovic , Vincenzo Tschinke , Nathalie Jotterand
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/46 , C07D453/02
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。

9. 发明申请

US20070167433A1 3,4,5-Substituted piperidines as therapeutic compounds 审中-公开
标题翻译： 3,4,5-取代的哌啶作为治疗化合物
公开(公告)号：US20070167433A1
公开(公告)日：2007-07-19
申请号：US11655108
申请日：2007-01-19
申请人： Peter Herold , Robert Mah , Stefan Stutz , Vincenzo Tschinke , Christoph Schumacher , Aleksandar Stojanovic , Nathalie Jotterand , Dirk Behnke
发明人： Peter Herold , Robert Mah , Stefan Stutz , Vincenzo Tschinke , Christoph Schumacher , Aleksandar Stojanovic , Nathalie Jotterand , Dirk Behnke
IPC分类号： A61K31/551 , A61K31/55 , A61K31/542 , A61K31/5383 , A61K31/517 , A61K31/445
CPC分类号： C07D413/14 , A61K31/452 , A61K31/453 , A61K31/4545 , C07D405/12 , C07D413/12 , Y02A50/411
摘要： Use of compounds of the general formula (I) and pharmaceutically acceptable salt thereof, in which R1, R2, R3, R4, W, X and Z, n and m have the definitions illustrated in detail in the description, as beta-secretase, cathepsin D, plasmepsin II and/or HIV protease inhibitors.
摘要翻译：使用通式（I）的化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 3， SEQ ID NO：4，W，X和Z，n和m具有在说明书中详细说明的定义，如β-分泌酶，组织蛋白酶D，浆细胞素II和/或HIV蛋白酶抑制剂。

10. 发明授权

US07851634B2 5-amino 4-hydroxy-7-(1H-indolmethyl)-8-methylnonamide derivatives as renin inhibitors for the treatment of hypertension 失效
标题翻译： 5-氨基-4-羟基-7-（1H-吲哚甲基）-8-甲基壬酰胺衍生物作为治疗高血压的肾素抑制剂
公开(公告)号：US07851634B2
公开(公告)日：2010-12-14
申请号：US10593460
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： C07D405/02 , A61K31/44
CPC分类号： C07C237/06 , C07C237/22 , C07D209/12 , C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The application relates to novel alkanamides of the general formula (I) where X is —CH2— or >CH—OH; (A) R1 is e.g. an optionally substituted heterocyclyl radical or an optionally substituted polycyclic, unsaturated hydrocarbon radical where X is hydroxymethylene; R2 is C1-C6-alkyl or C3-C6-cydoalkyl; R3 are each independently H, C1-C6-alkyl, C1-6-alkoxycarbonyl or C1-C6-alkanoyl; R4 is C1-C6-alkyl, C3-C6-cycloalkyl, C2-C6-alkenyl or unsubstituted or substituted arylC1-C6-alkyl; R5 is C1-C6-alkyl, C1-C6-hydroxyalkyl, C1-C6-alkoxy-C1-C6-alkyl, C1-C6-alkanoyloxy C1-C6-alkyl, C1-C6-aminoalkyl, C1-C6-alkylamino-C1-C6-alkyl, C1-C6-dialkylamino-C1-C6-alkyl, C1-C6-alkanoylamido-C1-C6-alkyl, HO(O)C—C1-C6-alkyl, C1-C6-alkyl-O—(O)C—C1-C6-alkyl, H2N—C(O)—C1-C6-alkyl, C1-C6-alkyl-HN—C(O)—C1-C6-alkyl, (C1,-C6-alkyl)2N—C(O)—C1-C6-alkyl, C2-C8-alkenyl, C2-C8-alkynyl, cyano-C1-C6-alkyl, halo-C1-C6-alkyl, optionally substituted aryl-Co-C6-alkyl, optionally substituted C3-C8-cycloalkyl-Co-C6-alkyl or optionally substituted heterocydyl-Co-C6-alkyl; to a process for their preparation and to the use of these compounds as medicines, especially as renin inhibitors for the treatment of hypertension.
摘要翻译：本申请涉及通式（I）的新型烷酰胺，其中X为-CH 2 - 或> CH-OH; （A）R1是例如任选取代的杂环基或任选取代的多环不饱和烃基，其中X是羟基亚甲基; R2是C1-C6-烷基或C3-C6-环烷基; R 3各自独立地为H，C 1 -C 6 - 烷基，C 1-6 - 烷氧基羰基或C 1 -C 6 - 烷酰基; R4是C1-C6-烷基，C3-C6-环烷基，C2-C6-烯基或未取代或取代的芳基C1-C6-烷基; R5是C1-C6-烷基，C1-C6-羟基烷基，C1-C6-烷氧基-C1-C6-烷基，C1-C6-烷酰氧基C1-C6-烷基，C1-C6-氨基烷基，C1-C6烷基氨基-C1 C 1 -C 6 - 烷基，C 1 -C 6 - 二烷基氨基-C 1 -C 6 - 烷基，C 1 -C 6 - 烷酰基氨基-C 1 -C 6烷基，HO（O）C 1 -C 6 - 烷基，C 1 -C 6烷基-O-（ O）-C 1 -C 6烷基，H 2 N-C（O）-C 1 -C 6 - 烷基，C 1 -C 6烷基-NH-C（O）-C 1 -C 6 - 烷基，（C 1 -C 6 - 烷基） C 1 -C 6 - 烷基，C 2 -C 8 - 烯基，C 2 -C 8炔基，氰基-C 1 -C 6烷基，卤代-C 1 -C 6烷基，任选取代的芳基-C 0 -C 6 - 烷基，任选取代的C 3 -C 8 - 环烷基-C 0 -C 6 - 烷基或任选取代的杂环-Co-C 6 - 烷基; 其制备方法和这些化合物作为药物的使用，特别是用作治疗高血压的肾素抑制剂。

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