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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。

4. 发明申请

US20090029981A1 SUBSTITUTED 4-PHENYLPIPERIDINES 审中-公开
标题翻译：取代的4-苯基哌啶
公开(公告)号：US20090029981A1
公开(公告)日：2009-01-29
申请号：US12087904
申请日：2007-01-18
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Dirk Behnke , Nathalie Jotterand , Aleksandar Stojanovic , Stefan Stutz , Stjepan Jelakovic , Michael Quirmbach
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Dirk Behnke , Nathalie Jotterand , Aleksandar Stojanovic , Stefan Stutz , Stjepan Jelakovic , Michael Quirmbach
IPC分类号： A61K31/538 , A61P9/00 , C07D413/12 , C07D413/14
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 R2, R3, 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。

5. 发明申请

US20110009399A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：US20110009399A1
公开(公告)日：2011-01-13
申请号：US12745960
申请日：2008-12-12
申请人： Peter Herold , Stjepan Jelakovic , Robert Mah , Dirk Behnke , Stefan Stutz , Vincenzo Tschinke , Nathalie Jotterand
发明人： Peter Herold , Stjepan Jelakovic , Robert Mah , Dirk Behnke , Stefan Stutz , Vincenzo Tschinke , Nathalie Jotterand
IPC分类号： A61K31/538 , C07D491/107 , A61K31/438 , A61P27/06 , A61P9/10 , A61P13/12 , A61P9/00 , A61P9/12
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。

6. 发明申请

US20110212950A1 4,4-DISUBSTITUTED PIPERIDINES 审中-公开
标题翻译： 4,4-取代的哌啶
公开(公告)号：US20110212950A1
公开(公告)日：2011-09-01
申请号：US12734321
申请日：2008-10-24
申请人： Dirk Behnke , Peter Herold , Stjepan Jelakovic , Nathalie Jotterand , Isabelle Lyothier , Robert Mah , Stefan Stutz , Vincenzo Tschinke
发明人： Dirk Behnke , Peter Herold , Stjepan Jelakovic , Nathalie Jotterand , Isabelle Lyothier , Robert Mah , Stefan Stutz , Vincenzo Tschinke
IPC分类号： A61K31/538 , C07D413/12 , C07D413/14 , A61P9/00
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 R2, 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。

7. 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。

8. 发明申请

US20100029628A1 2,4,5-Substituted Piperidines as Renin Inhibitors 审中-公开
标题翻译： 2,4,5-取代哌啶酮作为肾素抑制剂
公开(公告)号：US20100029628A1
公开(公告)日：2010-02-04
申请号：US11887227
申请日：2006-03-30
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： A61K31/538 , C07D413/02 , A61P9/00 , A61P13/00
CPC分类号： C07D413/12 , C07D413/14
摘要： SP-P2140 ATE-132—Abstract Novel substituted piperidines of the general formula (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： SP-P2140ATE-132-摘要描述了通式（I）和（II）的具有取代基定义的新颖取代的哌啶，如在说明书中详细说明的。该化合物特别适合作为肾素抑制剂，并且是非常有效的。

9. 发明授权

US08071651B2 5-amino-4-hydroxy-7-(imidazo [1,2-A] pyridin-6-ylmethyl)-8-methyl-nonamide derivatives and related compounds as renin inhibitors for the treatment of hypertension 失效
标题翻译： 5-氨基-4-羟基-7-（咪唑并[1,2-A]吡啶-6-基甲基）-8-甲基 - 非酰胺衍生物和相关化合物作为治疗高血压的肾素抑制剂
公开(公告)号：US08071651B2
公开(公告)日：2011-12-06
申请号：US11992132
申请日：2006-09-14
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Stefan Stutz , Aleksandar Stojanovic , Christiane Marti , Dirk Behnke , Stjepan Jelakovic
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Stefan Stutz , Aleksandar Stojanovic , Christiane Marti , Dirk Behnke , Stjepan Jelakovic
IPC分类号： A01N43/42 , A01N43/40 , A01N43/58 , A01N43/00 , A01N43/64 , A01N37/18 , A01N35/00 , A01N33/18 , A01N33/24 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00 , A61K31/16 , A61K31/12
CPC分类号： C07D405/12 , C07D471/04
摘要： Compounds of the general formula (I) or its salt or a compound in which one or more atoms are replaced by their stable, nonradio-active isotopes, in particular its pharmaceutically acceptable salt; in which X is —CH2—; R is a mono- to tetra-substituted, mono- or bicyclic, unsaturated heterocyclic radical having 1 to 4 nitrogen atoms, R2 is C1-6alkyl or C3-6cycloalkyl; R3 is independently of one another H, C1-6alkyl, C1-6alkoxycarbonyl or C1-6alkanoyl; R4 is C2-6alkenyl, C1-6alkyl, unsubstituted or substituted aryl-C1-6alkyl or C3-8cycloalkyl; R5 is -Lm-R6; L is C1-6alkylene which is optionally substituted by 1-4 halogen, or a linker: formula (II) n=0, 1 or 2; m=0 or 1; R6 is a radical composed of 2 cyclic systems selected from bicyclo[x.y.z]alkyl, spiro[o.p]alkyl, mono- or bioxabicyclo[x.y.z]alkyl or mono- or bioxaspiro[o.p]alkyl, all of which may be substituted by 1-3 substituents selected from C1-6alkyl, C1-6alkoxy, cyano, halogen, C1-6alkoxy-C1-6alkyl, hydroxy-C1-6alkyl or dialkylamino, or if m=0: is also saturated C3-8heterocyclyl which comprises 1-2 oxygen atoms, substituted by 1-3 substituents selected from C1-6alkyl, C1-6alkoxy, cyano, halogen, C1-6alkoxy-C1-6alkyl, hydroxy-C1-6alkyl or dialkylamino, or if m=1: is also saturated C3-8heterocyclyl which comprises 1-2 oxygen atoms, optionally substituted by 1-3 substituents selected from C1-6alkyl, C1-6alkoxy, cyano, halogen, C1-6-alkoxy-C1-6alkyl, hydroxy-C1-6alkyl or dialkylamino; have renin-inhibiting properties and can be used as medicines for the treatment of hypertension.
摘要翻译：通式（I）的化合物或其盐或其中一个或多个原子被其稳定的非放射性活性同位素替代的化合物，特别是其药学上可接受的盐; 其中X是-CH 2 - ; R是具有1至4个氮原子的单 - 四取代的单 - 或双环不饱和杂环基，R 2是C 1-6烷基或C 3-6环烷基; R 3彼此独立地为H，C 1-6烷基，C 1-6烷氧基羰基或C 1-6烷酰基; R 4是C 2-6烯基，C 1-6烷基，未取代或取代的芳基-C 1-6烷基或C 3-8环烷基; R5是-Lm-R6; L是任选被1-4个卤素取代的C 1-6亚烷基或连接基：式（II）n = 0,1或2; m = 0或1; R6是由选自双环[xyz]烷基，螺[op]烷基，单或生双环[xyz]烷基或单 - 或生物密封[op]烷基的2个环状体组成的基团，所有这些可以被1- 选自C 1-6烷基，C 1-6烷氧基，氰基，卤素，C 1-6烷氧基-C 1-6烷基，羟基-C 1-6烷基或二烷基氨基的3个取代基，或者如果m = 0：也是饱和的C 3-8杂环基，其包含1-2个氧原子被1-3个选自C 1-6烷基，C 1-6烷氧基，氰基，卤素，C 1-6烷氧基-C 1-6烷基，羟基-C 1-6烷基或二烷基氨基取代的取代基取代，或者如果m = 1：也是饱和的C 3-8杂环基其包含1-2个氧原子，任选被1-3个选自C 1-6烷基，C 1-6烷氧基，氰基，卤素，C 1-6 - 烷氧基-C 1-6烷基，羟基-C 1-6烷基或二烷基氨基的取代基取代; 具有肾素抑制性质，可用作治疗高血压的药物。

10. 发明申请

US20080176947A1 Heterocyclic-Substituted Alkanamides Useful as Renin Inhibitors 审中-公开
标题翻译：用作肾素抑制剂的杂环取代的烷酰胺
公开(公告)号：US20080176947A1
公开(公告)日：2008-07-24
申请号：US11885967
申请日：2006-03-10
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Stefan Stutz , Dirk Behnke , Aleksandar Stojanovic , Stjepan Jelakovic , Christiane Marti
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Stefan Stutz , Dirk Behnke , Aleksandar Stojanovic , Stjepan Jelakovic , Christiane Marti
IPC分类号： A61K31/165 , C07C237/20 , A61P9/00
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 R1 and R2 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

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