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：US20080280895A1

公开(公告)日：2008-11-13

申请号：US10593460

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: A61K31/538 ,  A61P9/00 ,  C07D209/18 ,  C07D401/02 ,  C07D471/04 ,  A61K31/437 ,  A61K31/4412 ,  A61K31/519 ,  C07D265/36 ,  C07D487/04 ,  C07D213/63

CPC classification number: C07C237/06 ,  C07C237/22 ,  C07D209/12 ,  C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

Abstract: The application relates to novel alkanamides of the general formula (I) where X is —CH2— or >CH—OH; (A) R1 is e.g. an optionally substituted heterocyclyl radical or an optionally substituted polycyclic, unsaturated hydrocarbon radical where X is hydroxymethylene; R2 is C1-C6-alkyl or C3-C6-cydoalkyl; R3 are each independently H, C1-C6-alkyl, C1-6-alkoxycarbonyl or C1-C6-alkanoyl; R4 is C1-C6-alkyl, C3-C6-cycloalkyl, C2-C6-alkenyl or unsubstituted or substituted arylC1-C6-alkyl; R5 is C1-C6-alkyl, C1-C6-hydroxyalkyl, C1-C6-alkoxy-C1-C6-alkyl, C1-C6-alkanoyloxy C1-C6-alkyl, C1-C6-aminoalkyl, C1-C6-alkylamino-C1-C6-alkyl, C1-C6-dialkylamino-C1-C6-alkyl, C1-C6-alkanoylamido-C1-C6-alkyl, HO(O)C—C1-C6-alkyl, C1-C6-alkyl-O—(O)C—C1-C6-alkyl, H2N—C(O)—C1-C6-alkyl, C1-C6-alkyl-HN—C(O)—C1-C6-alkyl, (C1, —C6-alkyl)2N—C(O)—C1-C6-alkyl, C2-C8-alkenyl, C2-C8-alkynyl, cyano-C1-C6-alkyl, halo-C1-C6-alkyl, optionally substituted aryl-Co-C6-alkyl, optionally substituted C3-C8-cycloalkyl-Co-C6-alkyl or optionally substituted heterocydyl-Co-C6-alkyl; to a process for their preparation and to the use of these compounds as medicines, especially as renin inhibitors for the treatment of hypertension.

公开(公告)号：US20080076766A1

公开(公告)日：2008-03-27

申请号：US11631777

申请日：2005-07-11

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

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

IPC: A61K31/5365 ,  A61P13/12 ,  A61P27/06 ,  A61P9/10 ,  A61P9/12 ,  C07D265/36

CPC classification number: C07D413/12 ,  C07D413/14

Abstract: The application relates to novel substituted piperidines of the general formula (I) in which R1, R2, R3, R4, W, X, Z, m and n 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: 本申请涉及通式（I）的新的取代的哌啶，其中R 1，R 2，R 3，R 3， 4，W，X，Z，m和n各自在说明书中详细描述，其制备方法和这些化合物作为药物，特别是作为肾素抑制剂的用途。

公开(公告)号：US20080058320A1

公开(公告)日：2008-03-06

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: A61K31/454 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/54 ,  A61P9/04 ,  A61P9/12 ,  C07D401/02 ,  C07D413/02 ,  C07D417/02 ,  C07D407/02 ,  C07D211/06 ,  A61P9/10 ,  A61P13/12 ,  A61K31/5375 ,  A61K31/4525

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 2， R 4，R 5和R 6各自如说明书中详细定义，其制备方法和这些化合物的用途为 药物，特别是作为肾素抑制剂。

公开(公告)号：US20070021413A1

公开(公告)日：2007-01-25

申请号：US11488854

申请日：2006-07-19

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

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

IPC: A61K31/54 ,  A61K31/5375 ,  A61K31/495 ,  A61K31/445 ,  A61K31/44 ,  A61K31/426 ,  A61K31/4164 ,  A61K31/138

CPC classification number: A61K31/137 ,  A61K31/16 ,  A61K31/18 ,  A61K31/351 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/405 ,  A61K31/426 ,  A61K31/4406 ,  A61K31/445 ,  A61K31/45 ,  A61K31/454 ,  A61K31/505 ,  A61K31/5375 ,  A61K31/55 ,  Y02A50/411

Abstract: Use of compounds of the general formula (I) in which R, R1, R2, R3, R4, R5, and R6 have the definitions illustrated in detail in the description, as beta-secretase, cathepsin D, plasmepsin II and/or HIV protease inhibitors.

Abstract translation: 使用通式（I）的化合物，其中R 1，R 2，R 2，R 3，R 4， R 5，R 5和R 6具有在说明书中详细说明的定义，作为β-分泌酶，组织蛋白酶D，浆细胞素II和/或HIV蛋白酶抑制剂 。

公开(公告)号：US09840498B2

公开(公告)日：2017-12-12

申请号：US14907225

申请日：2014-07-24

Applicant: NOVARTIS AG ,  Zhenxing Du ,  Samuel Hintermann ,  Konstanze Hurth ,  Sebastien Jacquier ,  Hansjoerg Lehmann ,  Henrik Moebitz ,  Nicolas Soldermann ,  Aleksandar Stojanovic

Inventor： Zhenxing Du ,  Samuel Hintermann ,  Konstanze Hurth ,  Sébastien Jacquier ,  Hansjoerg Lehmann ,  Henrik Moebitz ,  Nicolas Soldermann ,  Aleksandar Stojanovic

IPC: C07D403/14 ,  C07D401/14 ,  C07D417/14 ,  C07D473/16 ,  A61K31/517 ,  A61K31/52

CPC classification number: C07D403/14 ,  A61K31/517 ,  A61K31/52 ,  C07D401/14 ,  C07D417/14 ,  C07D473/16

Abstract: Provided are substituted quinazolin-4-one compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein R1, R2, R3, R5, R6 and L are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the class I PI3K kinases.

公开(公告)号：US08138179B2

公开(公告)日：2012-03-20

申请号：US12226215

申请日：2007-04-12

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

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

IPC: A61K31/535 ,  C07D265/00

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：US08071651B2

公开(公告)日：2011-12-06

申请号：US11992132

申请日：2006-09-14

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

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

IPC: 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 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-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.

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-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。

公开(公告)号：US08058307B2

公开(公告)日：2011-11-15

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: A61K31/38 ,  A61K31/355 ,  A61K31/35 ,  C07D335/06 ,  C07D311/00 ,  C07D315/00 ,  C07D215/00

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：US08008334B2

公开(公告)日：2011-08-30

申请号：US12086193

申请日：2006-12-08

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: C07D235/02 ,  C07D403/00 ,  A01N43/52 ,  A61K31/415

CPC classification number: C07D471/04

Abstract: 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.

Abstract translation: 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。