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21. 发明申请

US20090325947A1 NITRATE ESTERS OF PIPERIDINES 审中-公开
标题翻译：硝酸酯系列
公开(公告)号：US20090325947A1
公开(公告)日：2009-12-31
申请号：US12310022
申请日：2007-08-07
申请人： Peter Herold , Robert Mah , Stefan Stutz , Vincenzo Tschinke , Isabelle Lyothier , Christoph Schumacher , Christiane Marti , Nathalie Jotterand
发明人： Peter Herold , Robert Mah , Stefan Stutz , Vincenzo Tschinke , Isabelle Lyothier , Christoph Schumacher , Christiane Marti , Nathalie Jotterand
IPC分类号： A61K31/5377 , C07D211/06 , A61K31/445 , C07D413/02
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 R1, R2, R3, X, Y and Z0, 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R1，R2，R3，X，Y和Z0以及m，n，p和q具有在说明书中更详细解释的含义，其制备方法以及这些化合物作为心血管疾病中的治疗剂的用途，特别是伴有高血压的高血压和血管和器官损伤。

22. 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。

23. 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

24. 发明授权

US08008334B2 Bis-heterocyclic imidazolyl compounds 有权
标题翻译：双杂环咪唑基化合物
公开(公告)号：US08008334B2
公开(公告)日：2011-08-30
申请号：US12086193
申请日：2006-12-08
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Michael Quirmbach , Christiane Marti , Aleksandar Stojanovic , Stefan Stutz
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Michael Quirmbach , Christiane Marti , Aleksandar Stojanovic , Stefan Stutz
IPC分类号： C07D235/02 , C07D403/00 , A01N43/52 , A61K31/415
CPC分类号： C07D471/04
摘要： The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R1, R2, R3, R4 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，R 1，R 2，R 3，R 4和n具有在说明书中更详细阐述的定义，其制备方法和使用这些化合物作为药物，特别是作为醛固酮合酶抑制剂。

25. 发明申请

US20110028512A1 BIS-HETEROCYCLIC IMIDAZOLYL COMPOUNDS 失效
标题翻译：双相异构体咪唑啉化合物
公开(公告)号：US20110028512A1
公开(公告)日：2011-02-03
申请号：US12900779
申请日：2010-10-08
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Michael Quirmbach , Christiane Marti , Aleksandar Stojanovic , Stefan Stutz
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Michael Quirmbach , Christiane Marti , Aleksandar Stojanovic , Stefan Stutz
IPC分类号： A61K31/437 , C07D487/04 , C07D471/04 , A61K31/4188 , A61P9/12 , A61P3/06 , A61P3/00 , A61P9/04
CPC分类号： C07D471/04
摘要： Heterocyclic compounds of the general formula (I) are provided in which R, R1, R2, R3, R4 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 aldostereone synthase inhibitors,
摘要翻译：提供通式（I）的杂环化合物，其中R，R 1，R 2，R 3，R 4和n具有在说明书中更详细阐述的定义，其制备方法和这些化合物作为药物的用途，特别是作为醛固酮合成酶抑制剂，

26. 发明申请

US20090197909A1 Bis-Heterocyclic Imidazolyl Compounds 有权
标题翻译：双杂环咪唑基化合物
公开(公告)号：US20090197909A1
公开(公告)日：2009-08-06
申请号：US12086193
申请日：2006-12-08
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Michael Quirmbach , Christiane Marti , Aleksandar Stojanovic , Stefan Stutz
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Michael Quirmbach , Christiane Marti , Aleksandar Stojanovic , Stefan Stutz
IPC分类号： A61K31/437 , C07D487/04 , C07D471/04 , A61K31/4188 , A61P5/42
CPC分类号： C07D471/04
摘要： The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R1, R2, R3, R4 and n have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these C 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，R 1，R 2，R 3，R 4和n具有在说明书中更详细阐述的定义，其制备方法和使用这些C化合物作为药物，特别是作为醛固酮合酶抑制剂。

27. 发明申请

US20090192145A1 Spiro-Imidazo Compounds 失效
标题翻译：螺咪唑化合物
公开(公告)号：US20090192145A1
公开(公告)日：2009-07-30
申请号：US12226215
申请日：2007-04-12
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Aleksandar Stojanovic , Christiane Marti , Christiane Marti , Stjepan Jelakovic , Bibia Bennacer , Stefan Stutz
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Aleksandar Stojanovic , Christiane Marti , Christiane Marti , Stjepan Jelakovic , Bibia Bennacer , Stefan Stutz
IPC分类号： A61K31/547 , A61K31/5386 , C07D498/10 , C07D513/10 , A61P5/40
CPC分类号： C07D498/04 , C07D513/04
摘要： Novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R1, R1′, Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.
摘要翻译：通式（I）的新型杂环化合物及其盐，优选其药学上可接受的盐，其中R，R 1，R 1'，Q，m和n具有在说明书中详细说明的含义，其制备方法和使用这些化合物作为药物，特别是作为醛固酮合成酶抑制剂。

28. 发明授权

US07767690B2 Amino alcohol derivatives and their use as renin inhibitor 失效
标题翻译：氨基醇衍生物及其作为肾素抑制剂的用途
公开(公告)号：US07767690B2
公开(公告)日：2010-08-03
申请号：US10587046
申请日：2005-01-21
申请人： Peter Herold , Stefan Stutz , Aleksandar Stojanovic , Vincenzo Tschinke , Christiane Marti , Michael Quirmbach
发明人： Peter Herold , Stefan Stutz , Aleksandar Stojanovic , Vincenzo Tschinke , Christiane Marti , Michael Quirmbach
IPC分类号： A61K31/435 , C07D221/04
CPC分类号： C07D215/38 , C07D401/06 , C07D401/12 , C07D405/12 , C07D471/08 , C07D471/10
摘要： The application relates to novel amino alcohols of the general formula (I) where R, R1, R2, R3, R4, R5 and R6 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.
摘要翻译：本申请涉及通式（I）的新型氨基醇，其中R，R 1，R 2，R 3，R 4，R 5和R 6各自具有在说明书中详细说明的定义，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。

29. 发明申请

US20090118281A1 Amino Alcohol Derivatives And Their Use As Renin Inhibitor 失效
标题翻译：氨基醇衍生物及其作为肾素抑制剂的用途
公开(公告)号：US20090118281A1
公开(公告)日：2009-05-07
申请号：US10587046
申请日：2005-01-21
申请人： Peter Herold , Stefan Stutz , Aleksandar Stojanovic , Vincenzo Tschinke , Christiane Marti , Michael Quirmbach
发明人： Peter Herold , Stefan Stutz , Aleksandar Stojanovic , Vincenzo Tschinke , Christiane Marti , Michael Quirmbach
IPC分类号： A61K31/5377 , C07D215/38 , A61K31/47 , C07D401/14 , A61P13/12 , A61P9/12 , A61K31/438 , C07D413/02
CPC分类号： C07D215/38 , C07D401/06 , C07D401/12 , C07D405/12 , C07D471/08 , C07D471/10
摘要： The application relates to novel amino alcohols of the general formula (I) where R, R1, R2, R3, R4, R5 and R6 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.
摘要翻译：本申请涉及通式（I）的新型氨基醇，其中R 1，R 2，R 3，R 4，R 5和R 6各自具有在说明书中详细说明的定义，其制备方法和使用方法这些化合物作为药物，特别是作为肾素抑制剂。

30. 发明申请

US20070155743A1 Amino alcohol derivatives and their activity as renin inhibitors 失效
标题翻译：氨基醇衍生物及其作为肾素抑制剂的活性
公开(公告)号：US20070155743A1
公开(公告)日：2007-07-05
申请号：US10587150
申请日：2005-01-21
申请人： Peter Herold , Stefan Stutz , Aleksandar Stojanovic , Vincenzo Tschinke , Christiane Marti , Michael Quirmbach
发明人： Peter Herold , Stefan Stutz , Aleksandar Stojanovic , Vincenzo Tschinke , Christiane Marti , Michael Quirmbach
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/5375 , A61K31/495 , A61K31/4545 , C07D413/02 , C07D403/02 , C07D401/02
CPC分类号： C07D471/10 , C07C235/60 , C07C237/06 , C07C237/10 , C07C237/22 , C07C237/24 , C07C243/28 , C07C275/14 , C07C311/05 , C07C311/10 , C07C311/13 , C07C311/14 , C07C311/18 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/06 , C07C2602/22 , C07C2603/74 , C07D211/76 , C07D295/13 , C07D311/00
摘要： The application relates to novel amino alcohols of general formula (I) where R, R1, R2, R3, R4, R5,X1 and X2 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.
摘要翻译：本申请涉及通式（I）的新型氨基醇，其中R 1，R 2，R 2，R 3，R 3， 4，R 5，X 1和X 2各自具有在说明书中详细说明的定义，涉及一种它们的制备和使用这些化合物作为药物，特别是作为肾素抑制剂。

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