公开(公告)号：US07799780B2

公开(公告)日：2010-09-21

申请号：US12223789

申请日：2007-04-12

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: 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, 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，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：US07723550B2

公开(公告)日：2010-05-25

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: C07C29/36 ,  C07C29/44 ,  C07C41/18 ,  C07C41/30 ,  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：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：US20090088576A1

公开(公告)日：2009-04-02

申请号：US12223338

申请日：2007-01-29

Applicant: Peter Herold ,  Stefan Stutz ,  Robert Mah ,  Aleksandar Stojanovic ,  Isabelle Lyothier ,  Dirk Behnke ,  Felix Spindler ,  Erhard Bappert

Inventor： Peter Herold ,  Stefan Stutz ,  Robert Mah ,  Aleksandar Stojanovic ,  Isabelle Lyothier ,  Dirk Behnke ,  Felix Spindler ,  Erhard Bappert

IPC: C07D231/56

CPC classification number: C07D471/04 ,  C07D231/56

Abstract: A process for the synthesis of an alcohol of formula (I), using as intermediate a compound of formula (V).

Abstract translation: 用于合成式（I）的醇的方法，使用式（V）化合物作为中间体。

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：US20090012068A1

公开(公告)日：2009-01-08

申请号：US12223789

申请日：2007-04-12

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

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

IPC: A61K31/542 ,  C07D498/04 ,  A61K31/5383 ,  A61P5/00 ,  C07D513/04

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, 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，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：US20090012055A1

公开(公告)日：2009-01-08

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: 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 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。

公开(公告)号：US20070066582A1

公开(公告)日：2007-03-22

申请号：US11522316

申请日：2006-09-18

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

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

IPC: A61K31/55 ,  A61K31/54 ,  A61K31/5375 ,  A61K31/538 ,  A61K31/496 ,  A61K31/497 ,  A61K31/495 ,  A61K31/50 ,  A61K31/505

CPC classification number: A61K31/404 ,  Y02A50/411

Abstract: 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.

Abstract translation: 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。