公开(公告)号：US07718675B2

公开(公告)日：2010-05-18

申请号：US10586814

申请日：2005-01-21

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

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

IPC: A61K31/445 ,  C07D211/06

CPC classification number: C07D207/27 ,  C07C233/36 ,  C07C233/78 ,  C07C311/05 ,  C07D205/04 ,  C07D207/12 ,  C07D207/273 ,  C07D209/18 ,  C07D211/34 ,  C07D211/76 ,  C07D213/56 ,  C07D223/10 ,  C07D239/10 ,  C07D277/42 ,  C07D295/13 ,  C07D295/15 ,  C07D303/48 ,  C07D309/04 ,  C07D333/34 ,  C07D413/06 ,  C07D471/10

Abstract: 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.

Abstract translation: 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，其制备方法和用途 的这些化合物作为药物，特别是作为肾素抑制剂。

公开(公告)号：US20090192144A1

公开(公告)日：2009-07-30

申请号：US12226214

申请日：2007-04-12

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: A61K31/542 ,  C07D498/04 ,  C07D495/04 ,  A61K31/5383 ,  A61P9/12

CPC classification number: C07D513/04 ,  C07D498/04

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

公开(公告)号：US20080318978A2

公开(公告)日：2008-12-25

申请号：US11597620

申请日：2006-11-27

Applicant: Peter HEROLD ,  Robert MAH ,  Vincenzo TSCHINKE ,  Christoph SCHUMACHER ,  Michael QUIRMBACH

Inventor： Peter HEROLD ,  Robert MAH ,  Vincenzo TSCHINKE ,  Christoph SCHUMACHER ,  Michael QUIRMBACH

IPC: A61K31/495 ,  C07D471/02

CPC classification number: C07D471/04 ,  C07D417/04

Abstract: The application relates to novel heterocyclic compounds of the general formula (I) in which R, R1, R2, W, X, Y, Z and n have the meanings defined in the description, to a process for their preparation and to 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，其中R，R 1，R 2，W，X，Y，Z和n具有本说明书中定义的含义，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酶抑制剂。

公开(公告)号：US07687495B2

公开(公告)日：2010-03-30

申请号：US12076221

申请日：2008-03-14

Applicant: 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

Inventor： 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: C07D401/02 ,  A61K31/50 ,  A61K31/4965

CPC classification number: C07D413/12 ,  C07D413/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20090192149A1

公开(公告)日：2009-07-30

申请号：US12226212

申请日：2007-04-12

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: A61K31/5383 ,  C07D498/04 ,  A61P35/00

CPC classification number: C07D513/04 ,  C07D498/04

Abstract: The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R1, R2, Q, m and n have the meanings explained in detail in the description and * designates an asymmetric carbon atom, a process for their preparation and the use of these compounds as medicaments, in particular as aromatase inhibitors.

Abstract translation: 本申请涉及通式（I）的新型杂环化合物和其盐，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说明的含义，*表示 不对称碳原子，其制备方法和这些化合物作为药物的用途，特别是芳香酶抑制剂。

公开(公告)号：US20090088426A1

公开(公告)日：2009-04-02

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: A61K31/538 ,  C07D265/36 ,  A61P9/00 ,  A61P13/12

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：US20090048241A1

公开(公告)日：2009-02-19

申请号：US12226209

申请日：2007-04-12

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

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

IPC: C07D498/04 ,  A61K31/5365

CPC classification number: C07D513/04

Abstract: The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R1, R2, R3, Q, m and n have the meanings explained in detail in the description, and * designates an asymmetric carbon atom, a process for their preparation and the use of these compounds as medicaments, in particular as aromatase inhibitors.

Abstract translation: 本申请涉及通式（I）的新型杂环化合物及其盐，优选药学上可接受的盐，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， *表示不对称碳原子，其制备方法和这些化合物作为药物的用途，特别是芳香酶抑制剂。

公开(公告)号：US20090318432A1

公开(公告)日：2009-12-24

申请号：US12310881

申请日：2007-09-11

Applicant: Peter Herold ,  Robert Mah ,  Christiane Marti ,  Nathalie Jotterand

Inventor： Peter Herold ,  Robert Mah ,  Christiane Marti ,  Nathalie Jotterand

IPC: A61K31/538 ,  C07C229/02 ,  A61K31/195 ,  A61K31/445 ,  C07D211/60 ,  C07D265/36

CPC classification number: C07C237/20 ,  C07C2601/14 ,  C07D209/12 ,  C07D211/16 ,  C07D211/30 ,  C07D213/56 ,  C07D213/64 ,  C07D215/54 ,  C07D231/56 ,  C07D265/36 ,  C07D307/80 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12

Abstract: The application relates to novel nitrate ester derivatives of substituted aminoalcohols of the general formula (I), wherein R1, R2, R3, V, X, Y and Z0 have the meanings explained in more detail in the description, to a process for their preparation and to the use of these compounds as therapeutics in cardiovascular diseases, in particular in high blood pressure and vascular and organ damage age accompanying high blood pressure.

Abstract translation: 本申请涉及通式（I）的取代氨基醇的新型硝酸酯衍生物，其中R1，R2，R3，V，X，Y和Z0具有在说明书中更详细解释的含义及其制备方法 以及这些化合物在心血管疾病中的应用，特别是伴随高血压的高血压和血管和器官损伤年龄的使用。

公开(公告)号：US20090275651A1

公开(公告)日：2009-11-05

申请号：US11992127

申请日：2006-09-14

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

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

IPC: A61K31/351 ,  C07D315/00 ,  A61P9/10 ,  A61P9/04 ,  C07D307/14 ,  A61K31/341

CPC classification number: A61K31/335

Abstract: Compounds of the general formula (formula I) in which the meanings of the substituents R1 to R6 are as indicated in claim 1, have renin-inhibiting properties and can be used as medicines.

Abstract translation: 取代基R 1〜R 6的含义如权利要求1所示的通式（式I）的化合物具有肾素抑制性质，可用作药物。

公开(公告)号：US20070161622A1

公开(公告)日：2007-07-12

申请号：US10586814

申请日：2005-01-21

Applicant: Peter Herold ,  Stefan Stutz ,  Aleksandar Stojanovic ,  Vincenzo Tschinke ,  Christiane Martin ,  Michael Quirmbach

Inventor： Peter Herold ,  Stefan Stutz ,  Aleksandar Stojanovic ,  Vincenzo Tschinke ,  Christiane Martin ,  Michael Quirmbach

IPC: A61K31/55 ,  A61K31/5415 ,  A61K31/54 ,  A61K31/5375 ,  A61K31/495

CPC classification number: C07D207/27 ,  C07C233/36 ,  C07C233/78 ,  C07C311/05 ,  C07D205/04 ,  C07D207/12 ,  C07D207/273 ,  C07D209/18 ,  C07D211/34 ,  C07D211/76 ,  C07D213/56 ,  C07D223/10 ,  C07D239/10 ,  C07D277/42 ,  C07D295/13 ,  C07D295/15 ,  C07D303/48 ,  C07D309/04 ,  C07D333/34 ,  C07D413/06 ,  C07D471/10

Abstract: 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.

Abstract translation: 本申请涉及通式（I）的新型氨基醇，其中R 1，R 1，R 2，R 3，R 3， R 5，R 5和R 6各自具有在说明书中详细说明的定义，其制备方法以及这些的使用 化合物作为药物，特别是作为肾素抑制剂。