公开(公告)号：US08263615B2

公开(公告)日：2012-09-11

申请号：US12900779

申请日：2010-10-08

Applicant: Peter Herold ,  Robert Mah ,  Vincenzo Tschinke ,  Michael Quirmbach ,  Christiane Marti ,  Aleksandar Stojanovic ,  Stefan Stutz

Inventor： Peter Herold ,  Robert Mah ,  Vincenzo Tschinke ,  Michael Quirmbach ,  Christiane Marti ,  Aleksandar Stojanovic ,  Stefan Stutz

IPC: A61K31/437 ,  C07D487/04 ,  C07D471/04 ,  A61K31/4188 ,  A61P9/12 ,  A61P3/06 ,  A61P3/00 ,  A61P9/04

CPC classification number: C07D471/04

Abstract: 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,

Abstract translation: 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，

公开(公告)号：US20120115859A1

公开(公告)日：2012-05-10

申请号：US13349869

申请日：2012-01-13

Applicant: Peter HEROLD ,  Robert Mah ,  Vincenzo Tschinke ,  Nathalie Jotterand ,  Dirk Behnke ,  Aleksandar Stojanovic ,  Stefan Stutz ,  Michael Quirmbach ,  Stjepan Jelakovic

Inventor： Peter HEROLD ,  Robert Mah ,  Vincenzo Tschinke ,  Nathalie Jotterand ,  Dirk Behnke ,  Aleksandar Stojanovic ,  Stefan Stutz ,  Michael Quirmbach ,  Stjepan Jelakovic

IPC: A61K31/538 ,  C07D413/14 ,  C07D405/12 ,  A61K31/453 ,  A61P9/00 ,  A61P9/04 ,  A61P27/06 ,  A61P9/10 ,  A61P13/12 ,  C07D413/12 ,  A61P9/12

CPC classification number: C07D413/14 ,  C07D413/12

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08138176B2

公开(公告)日：2012-03-20

申请号：US12975949

申请日：2010-12-22

Applicant: Peter Herold ,  Robert Mah ,  Vincenzo Tschinke ,  Aleksandar Stojanovic ,  Christiane Marti ,  Stjepan Jelakovic ,  Stefan Stutz

Inventor： Peter Herold ,  Robert Mah ,  Vincenzo Tschinke ,  Aleksandar Stojanovic ,  Christiane Marti ,  Stjepan Jelakovic ,  Stefan Stutz

IPC: C07D513/04 ,  A61K31/542

CPC classification number: C07D513/04 ,  C07D498/04

Abstract: Heterocyclic compounds of the formula (I) and salts, preferably pharmaceutically acceptable salts thereof, are provided in which R, R1, R2, Q, m and n have the meanings explained in detail in the description. Also provided are a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.

Abstract translation: 提供式（I）的杂环化合物和其盐，优选其药学上可接受的盐，其中R，R 1，R 2，Q，m和n具有在说明书中详细解释的含义。 还提供了它们制备和使用这些化合物作为药物的方法，特别是作为醛固酮合酶抑制剂。

公开(公告)号：US20100305110A1

公开(公告)日：2010-12-02

申请号：US12857032

申请日：2010-08-16

Applicant: Peter HEROLD ,  Robert Mah ,  Vincenzo Tschinke ,  Aleksandar Stojanovic ,  Christiane Marti ,  Stefan Stutz ,  Bibia Bennacer

Inventor： Peter HEROLD ,  Robert Mah ,  Vincenzo Tschinke ,  Aleksandar Stojanovic ,  Christiane Marti ,  Stefan Stutz ,  Bibia Bennacer

IPC: A61K31/542 ,  C07D498/04 ,  A61K31/5383 ,  C07D513/04 ,  A61P3/06 ,  A61P9/12

CPC classification number: C07D513/04

Abstract: The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferable pharmaceutically acceptable salts, thereof, in which R, R1, R2, R3, 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.

Abstract translation: 本申请涉及通式（I）的新型杂环化合物及其盐，优选的药学上可接受的盐，其中R，R 1，R 2，R 3，Q，m和n具有在说明书中详细说明的含义， 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酶抑制剂。

公开(公告)号：US20100168145A1

公开(公告)日：2010-07-01

申请号：US11921313

申请日：2006-05-30

Applicant: Peter Herold ,  Robert Mah ,  Vincenzo Tschinke ,  Aleksandar Stojanovic ,  Christiane Marti ,  Nathalie Jotterand ,  Christoph Schumacher ,  Michael Quirmbach

Inventor： Peter Herold ,  Robert Mah ,  Vincenzo Tschinke ,  Aleksandar Stojanovic ,  Christiane Marti ,  Nathalie Jotterand ,  Christoph Schumacher ,  Michael Quirmbach

IPC: A61K31/438 ,  C07D471/10 ,  C07D471/20 ,  A61P5/42

CPC classification number: C07D471/04

Abstract: The patent application relates to new heterocyclic compounds of the general formula (I) in which A, R, R1, R2, X, Y, Z, 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.

Abstract translation: 该专利申请涉及通式（I）的新的杂环化合物，其中A，R，R 1，R 2，X，Y，Z，n和p具有在说明书中更详细阐述的定义涉及制备方法 它们以及这些化合物作为药物的使用，特别是作为醛固酮合酶抑制剂。

公开(公告)号：US07625893B2

公开(公告)日：2009-12-01

申请号：US12224440

申请日：2007-10-03

Applicant: Peter Herold ,  Robert Mah ,  Stefan Stutz ,  Vincenzo Tschinke ,  Aleksandar Stojanovic ,  Dirk Behnke ,  Nathalie Jotterand ,  Stjepan Jelakovic

Inventor： Peter Herold ,  Robert Mah ,  Stefan Stutz ,  Vincenzo Tschinke ,  Aleksandar Stojanovic ,  Dirk Behnke ,  Nathalie Jotterand ,  Stjepan Jelakovic

IPC: C07D413/12 ,  A61K31/538

CPC classification number: C07D413/12

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20090192145A1

公开(公告)日：2009-07-30

申请号：US12226215

申请日：2007-04-12

Applicant: Peter Herold ,  Robert Mah ,  Vincenzo Tschinke ,  Aleksandar Stojanovic ,  Christiane Marti ,  Christiane Marti ,  Stjepan Jelakovic ,  Bibia Bennacer ,  Stefan Stutz

Inventor： Peter Herold ,  Robert Mah ,  Vincenzo Tschinke ,  Aleksandar Stojanovic ,  Christiane Marti ,  Christiane Marti ,  Stjepan Jelakovic ,  Bibia Bennacer ,  Stefan Stutz

IPC: A61K31/547 ,  A61K31/5386 ,  C07D498/10 ,  C07D513/10 ,  A61P5/40

CPC classification number: C07D498/04 ,  C07D513/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20090105503A1

公开(公告)日：2009-04-23

申请号：US12224418

申请日：2007-11-08

Applicant: Peter Herold ,  Robert Mah ,  Stefan Stutz ,  Aleksandar Stojanovic ,  Isabelle Lyothier ,  Dirk Behnke

Inventor： Peter Herold ,  Robert Mah ,  Stefan Stutz ,  Aleksandar Stojanovic ,  Isabelle Lyothier ,  Dirk Behnke

IPC: C07C231/12 ,  C07C41/08 ,  C07C43/23

CPC classification number: C07C41/20 ,  C07B2200/07 ,  C07C41/22 ,  C07C41/30 ,  C07C231/12 ,  C07C235/34 ,  C07C43/23 ,  C07C43/225

Abstract: Process for preparing a compound of the formula (I) in which R1 and R2 are each independently H, C1-C8-alkyl, halogen, polyhalo-C1-C8-alkoxy, polyhalo-C1-C8-alkyl, C1-C8-alkoxy, C1-C8-alkoxy-C1-C8-alkyl, or C1-C8-alkoxy-C1-C8-alkoxy, where R1 and R2 are not both H, and R3 is C1-C8-alkyl, which is characterized in that a) a compound of the formula (II) in which R1 and R2 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 R3 to give a compound of the formula (I).

Abstract translation: 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 8 - 烷基，卤素，多卤代-C 1 -C 8 - 烷氧基，多卤代-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 1 -C 8 - 烷氧基，其中R 1和R 2不都是H，且R 3是C 1 -C 8 - 烷基，其特征在于 ）其中R 1和R 2各自如上定义并且X是Br，I，三氟甲磺酸酯，玩具或甲磺酸酯的式（II）化合物与丙-2-炔-1-醇反应，得到式 （III）中，b）式（III）化合物与烷基金属化合物反应，其中“烷基”如上述R3所定义，得到式（I）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

Applicant: Peter Herold ,  Stefan Stutz ,  Robert Mah ,  Vincenzo Tschinke ,  Aleksandar Stojanovic ,  Nathalie Jotterand ,  Michael Quirmbach ,  Dirk Behnke ,  Christiane Marti

Inventor： Peter Herold ,  Stefan Stutz ,  Robert Mah ,  Vincenzo Tschinke ,  Aleksandar Stojanovic ,  Nathalie Jotterand ,  Michael Quirmbach ,  Dirk Behnke ,  Christiane Marti

IPC: A61K31/405 ,  C07D209/04

CPC classification number: C07D209/12 ,  C07D401/06

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07842688B2

公开(公告)日：2010-11-30

申请号：US12068443

申请日：2008-02-06

Applicant: Peter Herold ,  Robert Mah ,  Stefan Stutz ,  Aleksandar Stojanovic ,  Vincenzo Tschinke ,  Nathalie Jotterand

Inventor： Peter Herold ,  Robert Mah ,  Stefan Stutz ,  Aleksandar Stojanovic ,  Vincenzo Tschinke ,  Nathalie Jotterand

IPC: C07D401/12 ,  A61K31/4427

CPC classification number: C07D211/42 ,  C07D401/12 ,  C07D413/12

Abstract: 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.

Abstract translation: 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。