公开(公告)号：WO2013007712A1

公开(公告)日：2013-01-17

申请号：PCT/EP2012/063455

申请日：2012-07-10

Applicant: F. HOFFMANN-LA ROCHE AG ,  BIRRER, Beat ,  CLARKE, Leo ,  DEICHTMANN, Walter ,  HAYES, John ,  JEISY, Julius ,  LAUTZ, Christian ,  MARTIN, Rainer E. ,  MEADE, Michael ,  PINTAO, Joaquim ,  SCALONE, Michelangelo ,  SCHAEFER, Juergen ,  SMITH, Dennis ,  STAEMPFLI, Andreas ,  VEITS, Joachim ,  WALCH, Christian ,  WALSH, Andrew ,  ZOGG, Andreas

Inventor： BIRRER, Beat ,  CLARKE, Leo ,  DEICHTMANN, Walter ,  HAYES, John ,  JEISY, Julius ,  LAUTZ, Christian ,  MARTIN, Rainer E. ,  MEADE, Michael ,  PINTAO, Joaquim ,  SCALONE, Michelangelo ,  SCHAEFER, Juergen ,  SMITH, Dennis ,  STAEMPFLI, Andreas ,  VEITS, Joachim ,  WALCH, Christian ,  WALSH, Andrew ,  ZOGG, Andreas

IPC: C07C327/30 ,  C07C51/06 ,  C07C51/08 ,  C07C61/08 ,  C07C319/06 ,  C07C319/20

CPC classification number: C07C319/20 ,  C07C51/02 ,  C07C51/06 ,  C07C51/08 ,  C07C319/06 ,  C07C327/30 ,  C07C2601/14 ,  C07C323/40 ,  C07C61/08

Abstract: A process for the preparation of a compound of formula (I): which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.

Abstract translation: 制备式（I）化合物的方法：其可用作制备中间体。 药物活性化合物。

公开(公告)号：WO2011089099A1

公开(公告)日：2011-07-28

申请号：PCT/EP2011/050558

申请日：2011-01-18

Applicant: F. HOFFMANN-LA ROCHE AG ,  BISSANTZ, Caterina ,  DEHMLOW, Henrietta ,  ERICKSON, Shawn, David ,  KIM, Kyungjin ,  MARTIN, Rainer, E. ,  OBST SANDER, Ulrike ,  PIETRANICO-COLE, Sherrie, Lynn ,  RICHTER, Hans ,  ULLMER, Christoph

Inventor： BISSANTZ, Caterina ,  DEHMLOW, Henrietta ,  ERICKSON, Shawn, David ,  KIM, Kyungjin ,  MARTIN, Rainer, E. ,  OBST SANDER, Ulrike ,  PIETRANICO-COLE, Sherrie, Lynn ,  RICHTER, Hans ,  ULLMER, Christoph

IPC: C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/506 ,  A61P3/00

CPC classification number: C07D417/14 ,  C07D213/82 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D417/12

Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula (I), wherein A 1 , A 2 , B 1 , B 2 and R 1 to R 11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.

Abstract translation: 本发明涉及式（I）的新型苯基酰胺或吡啶基酰胺衍生物，其中A1，A2，B1，B2和R1至R11如说明书和权利要求书中所定义，以及其药学上可接受的盐。 这些化合物是GPBAR1激动剂，可用作治疗II型糖尿病等疾病的药物。

公开(公告)号：WO2011039130A1

公开(公告)日：2011-04-07

申请号：PCT/EP2010/064217

申请日：2010-09-27

Applicant: F. HOFFMANN-LA ROCHE AG ,  BENSON, Gregory Martin ,  BLEICHER, Konrad ,  FENG, Song ,  GRETHER, Uwe ,  KUHN, Bernd ,  MARTIN, Rainer E. ,  PLANCHER, Jean-Marc ,  RICHTER, Hans ,  RUDOLPH, Markus ,  TAYLOR, Sven

Inventor： BENSON, Gregory Martin ,  BLEICHER, Konrad ,  FENG, Song ,  GRETHER, Uwe ,  KUHN, Bernd ,  MARTIN, Rainer E. ,  PLANCHER, Jean-Marc ,  RICHTER, Hans ,  RUDOLPH, Markus ,  TAYLOR, Sven

IPC: C07D235/18 ,  C07D401/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/14 ,  C07D417/14 ,  A61K31/4184 ,  A61K31/4439

CPC classification number: C07D401/04 ,  C07D235/18 ,  C07D403/10 ,  C07D403/12 ,  C07D405/14 ,  C07D417/14

Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A, B, R 1 , R 2 , R 3 , R 4 , R 5 , n, m and p have the significance given in claim 1.

Abstract translation: 式（I）化合物及其药学上可接受的盐可以以药物组合物的形式使用，其中A，B，R 1，R 2，R 3，R 4，R 5，n，m和p具有权利要求1中给出的含义 。

公开(公告)号：WO2009080555A2

公开(公告)日：2009-07-02

申请号：PCT/EP2008067399

申请日：2008-12-12

Applicant: HOFFMANN LA ROCHE ,  BENSON GREGORY MARTIN ,  BLEICHER KONRAD ,  GRETHER UWE ,  KUHN BERND ,  MARTIN RAINER E ,  PLANCHER JEAN-MARC ,  RICHTER HANS ,  TAYLOR SVEN ,  YANG MINMIN

Inventor： BENSON GREGORY MARTIN ,  BLEICHER KONRAD ,  GRETHER UWE ,  KUHN BERND ,  MARTIN RAINER E ,  PLANCHER JEAN-MARC ,  RICHTER HANS ,  TAYLOR SVEN ,  YANG MINMIN

IPC: C07D401/04

CPC classification number: C07D401/04 ,  C07D235/12 ,  C07D401/12 ,  C07D401/14

Abstract: This invention relates to novel carboxyl- or hydroxylsubstituted benzimidazole derivatives of formula (I) wherein R1 to R6 are as defined in the description and in the claims, as well as 5 physiologically acceptable salts and esters thereof. These compounds bind to FXR and can be used as medicaments.

Abstract translation: 本发明涉及式（I）的新型羧基或羟基取代的苯并咪唑衍生物，其中R 1至R 6如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。 这些化合物与FXR结合，可用作药物。

公开(公告)号：WO2009062874A2

公开(公告)日：2009-05-22

申请号：PCT/EP2008/065012

申请日：2008-11-05

Applicant: F. HOFFMANN-LA ROCHE AG ,  BENSON, Gregory Martin ,  BLEICHER, Konrad ,  GRETHER, Uwe ,  MARTIN, Rainer E. ,  PLANCHER, Jean-Marc ,  RICHTER, Hans ,  TAYLOR, Sven ,  YANG, Minmin

Inventor： BENSON, Gregory Martin ,  BLEICHER, Konrad ,  GRETHER, Uwe ,  MARTIN, Rainer E. ,  PLANCHER, Jean-Marc ,  RICHTER, Hans ,  TAYLOR, Sven ,  YANG, Minmin

IPC: C07D235/06 ,  C07D405/12 ,  C07D409/12 ,  A61K31/4184 ,  A61P3/00

CPC classification number: C07D235/06 ,  C07D405/12 ,  C07D409/12

Abstract: The invention is concerned with novel substituted benzimidazole derivatives of formula (I) wherein R 1 to R 10 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds can be used as medicaments.

Abstract translation: 本发明涉及式（I）的新型取代的苯并咪唑衍生物，其中R 1至R 10如说明书和权利要求书中所定义，以及其生理学上可接受的盐和酯。 这些化合物可以用作药物。

公开(公告)号：WO2013072265A1

公开(公告)日：2013-05-23

申请号：PCT/EP2012/072348

申请日：2012-11-12

Applicant: F. HOFFMANN-LA ROCHE AG ,  DEHMLOW, Henrietta ,  MARTIN, Rainer E. ,  MATTEI, Patrizio ,  OBST SANDER, Ulrike ,  RICHTER, Hans

Inventor： DEHMLOW, Henrietta ,  MARTIN, Rainer E. ,  MATTEI, Patrizio ,  OBST SANDER, Ulrike ,  RICHTER, Hans

IPC: C07D237/08 ,  A61K31/50 ,  A61P3/10

CPC classification number: C07D237/08 ,  C07D237/14 ,  C07D401/10

Abstract: This invention relates to 1-pyridazinyl-hydroxyimino-3-phenyl-propanes of the formula (I) wherein R 1 to R 7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.

Abstract translation: 本发明涉及式（I）的1-哒嗪基 - 肟基-3-苯基 - 丙烷，其中R 1至R 7如说明书和权利要求书中所定义，以及其药学上可接受的盐。 这些化合物是GPBAR1激动剂，因此可用作治疗诸如II型糖尿病的疾病的药物。

公开(公告)号：WO2010049302A1

公开(公告)日：2010-05-06

申请号：PCT/EP2009/063649

申请日：2009-10-19

Applicant: F. HOFFMANN-LA ROCHE AG ,  BISSANTZ, Caterina ,  DEHMLOW, Henrietta ,  MARTIN, Rainer E. ,  OBST SANDER, Ulrike ,  RICHTER, Hans ,  ULLMER, Christoph

Inventor： BISSANTZ, Caterina ,  DEHMLOW, Henrietta ,  MARTIN, Rainer E. ,  OBST SANDER, Ulrike ,  RICHTER, Hans ,  ULLMER, Christoph

IPC: C07D213/81 ,  C07D213/82 ,  A61K31/455 ,  C07D209/08 ,  C07D215/08 ,  C07D215/18 ,  C07D241/42 ,  C07D265/36 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/06 ,  C07D417/06 ,  C07D471/04

CPC classification number: C07D209/08 ,  C07C235/64 ,  C07D213/81 ,  C07D213/82 ,  C07D215/08 ,  C07D215/18 ,  C07D241/42 ,  C07D265/36 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/06 ,  C07D417/06 ,  C07D471/04 ,  C07D487/04

Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula (I) wherein A 1 , A 2 , B 1 , B 2 and R 1 to R 11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.

Abstract translation: 本发明涉及式（I）的新型苯基酰胺或吡啶基酰胺衍生物，其中A1，A2，B1，B2和R1至R11如说明书和权利要求书中所定义，以及其药学上可接受的盐。 这些化合物是GPBAR1激动剂，可用作治疗II型糖尿病等疾病的药物。

公开(公告)号：WO2008148710A2

公开(公告)日：2008-12-11

申请号：PCT/EP2008/056674

申请日：2008-05-30

Applicant: F. HOFFMANN-LA ROCHE AG ,  CHRIST, Andreas D. ,  MARTIN, Rainer E. ,  MOHR, Peter

Inventor： CHRIST, Andreas D. ,  MARTIN, Rainer E. ,  MOHR, Peter

IPC: C07D401/12 ,  C07D413/12 ,  A61K31/4468 ,  A61P3/10

CPC classification number: C07D413/12 ,  C07D401/12

Abstract: This invention relates to compounds of the formula (I) wherein X is O or NR 8 , Y is CR 7 or N, and R 1 to R 8 are as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

Abstract translation: 本发明涉及式（I）的化合物，其中X为O或NR8，Y为CR7或N，R1至R8如说明书中所定义，及其药学上可接受的盐。 本发明还涉及含有这些化合物的药物组合物，其制备方法及其用于治疗和/或预防与调节SST受体亚型5相关的疾病的用途。

公开(公告)号：WO2008000692A3

公开(公告)日：2008-02-28

申请号：PCT/EP2007056226

申请日：2007-06-22

Applicant: HOFFMANN LA ROCHE ,  CHRIST ANDREAS D ,  MARTIN RAINER E

Inventor： CHRIST ANDREAS D ,  MARTIN RAINER E

IPC: C07D401/12 ,  A61K31/506 ,  A61P3/10 ,  C07D473/16 ,  C07D487/04

CPC classification number: C07D473/16 ,  C07D401/12 ,  C07D487/04

Abstract: This invention is concerned with compounds of the formula (I) wherein A, R 1 to R 5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

Abstract translation: 本发明涉及式（I）的化合物，其中A，R 1至R 5和G如说明书和权利要求中所定义，及其药学上可接受的盐 。 本发明还涉及含有这些化合物的药物组合物，其制备方法及其用于治疗和/或预防与调节SST受体亚型5相关的疾病的用途。

公开(公告)号：WO2008000692A2

公开(公告)日：2008-01-03

申请号：PCT/EP2007/056226

申请日：2007-06-22

Applicant: F. HOFFMANN-LA ROCHE AG ,  CHRIST, Andreas D. ,  MARTIN, Rainer E.

Inventor： CHRIST, Andreas D. ,  MARTIN, Rainer E.

IPC: C07D401/12 ,  C07D473/16 ,  C07D487/04 ,  A61K31/506 ,  A61P3/10

CPC classification number: C07D473/16 ,  C07D401/12 ,  C07D487/04

Abstract: This invention is concerned with compounds of the formula ( l ) wherein A, R 1 to R 5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

Abstract translation: 本发明涉及式（I）的化合物，其中A，R 1至R 5和G如说明书和权利要求书中所定义，以及其药学上可接受的盐 。 本发明还涉及含有这些化合物的药物组合物，其制备方法及其用于治疗和/或预防与调节SST受体亚型5相关的疾病的用途。