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：US20100063087A1

公开(公告)日：2010-03-11

申请号：US11992132

申请日：2006-09-14

Applicant: Peter HEROLD

Inventor： Peter HEROLD

IPC: A61K31/437 ,  C07D471/02 ,  C07D405/12 ,  C07D209/54 ,  A61K31/4433 ,  A61K31/403 ,  A61P9/10 ,  A61P9/12

CPC classification number: C07D405/12 ,  C07D471/04

Abstract: 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-R ; 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.

Abstract translation: 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-R; 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- 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，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。

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：US07615664B2

公开(公告)日：2009-11-10

申请号：US11792673

申请日：2005-12-09

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

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

IPC: C07C233/05 ,  A61K31/65

CPC classification number: C07C255/59 ,  C07C237/20 ,  C07D317/58 ,  C07D319/18

Abstract: Compounds of the general formula (I) in which the substituents R, R1, R2, R3, R4, R5 and R6 are each as defined in claim 1 have renin-inhibiting properties and can be used as medicaments.

Abstract translation: 其中取代基R 1，R 2，R 3，R 4，R 5和R 6各自如权利要求1中所定义的通式（I）的化合物具有肾素抑制性质，可用作药物。

公开(公告)号：US07612088B2

公开(公告)日：2009-11-03

申请号：US11597620

申请日：2005-05-27

Applicant: Peter Herold ,  Robert Mah ,  Vincenzo Tschinke ,  Christoph Schumacher ,  Michael Quirmbach

Inventor： Peter Herold ,  Robert Mah ,  Vincenzo Tschinke ,  Christoph Schumacher ,  Michael Quirmbach

IPC: A61K31/437

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：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。