公开(公告)号：WO2012080144A1

公开(公告)日：2012-06-21

申请号：PCT/EP2011/072392

申请日：2011-12-12

Applicant: F. HOFFMANN-LA ROCHE AG ,  HEBEISEN, Paul ,  ROEVER, Stephan

Inventor： HEBEISEN, Paul ,  ROEVER, Stephan

IPC: C07D213/63 ,  C07D213/74 ,  C07D241/24 ,  A61K31/465 ,  A61K31/4965 ,  A61P9/00

CPC classification number: C07D213/63 ,  A61K31/465 ,  A61K31/4965 ,  C07D213/74 ,  C07D241/24

Abstract: The present invention relates to compounds of the formula (I) wherein A 1 to A 3 and R 1 to R 9 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.

Abstract translation: 本发明涉及式（I）化合物，其中A1至A3和R1至R9在说明书中定义，及其药学上可接受的盐，其制备方法，含有它们的药物组合物及其用作治疗和/ 或预防可用HDL-胆固醇升高剂如特别是血脂异常，动脉粥样硬化和心血管疾病治疗的疾病。

公开(公告)号：WO2012032018A1

公开(公告)日：2012-03-15

申请号：PCT/EP2011/065341

申请日：2011-09-06

Applicant: F. HOFFMANN-LA ROCHE AG ,  HEBEISEN, Paul ,  ZOFFMANN JENSEN, Sannah ,  MATILE, Hugues ,  ROEVER, Stephan ,  WRIGHT, Matthew

Inventor： HEBEISEN, Paul ,  ZOFFMANN JENSEN, Sannah ,  MATILE, Hugues ,  ROEVER, Stephan ,  WRIGHT, Matthew

IPC: A61K31/4427 ,  A61K31/455 ,  A61K31/506 ,  C07D213/16 ,  C07D401/06 ,  C07D413/08 ,  G01N33/92

CPC classification number: C07D417/12 ,  C07D213/82 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14

Abstract: The present invention relates to compounds of the formula I wherein A 1 , A 2 , A 3 and R 1 to R 8 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.

Abstract translation: 本发明涉及式I化合物，其中A1，A2，A3和R1至R8在说明书中定义，及其药学上可接受的盐，其制备方法，含有它们的药物组合物及其用作治疗和/ 或预防可用HDL-胆固醇升高剂如特别是血脂异常，动脉粥样硬化和心血管疾病治疗的疾病。

公开(公告)号：WO2008040649A3

公开(公告)日：2008-05-29

申请号：PCT/EP2007060090

申请日：2007-09-24

Applicant: HOFFMANN LA ROCHE ,  DIETZ MICHEL ,  GRUENER SABINE ,  HEBEISEN PAUL ,  MEYER REIGNER SYLVIE C ,  NETTEKOVEN MATTHIAS ,  PUELLMANN BERND ,  ROEVER STEPHAN ,  ULLMER CHRISTOPH

Inventor： DIETZ MICHEL ,  GRUENER SABINE ,  HEBEISEN PAUL ,  MEYER REIGNER SYLVIE C ,  NETTEKOVEN MATTHIAS ,  PUELLMANN BERND ,  ROEVER STEPHAN ,  ULLMER CHRISTOPH

IPC: C07D241/26 ,  A61K31/4965 ,  A61K31/497 ,  A61P9/00 ,  A61P9/10 ,  A61P11/06 ,  A61P29/00 ,  A61P37/00 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

CPC classification number: C07D241/26 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

Abstract: The present invention relates to compounds of the formula (I) wherein R 1 to R 4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB 2 receptors.

Abstract translation: 本发明涉及式（I）的化合物，其中R 1至R 4如在说明书和权利要求书中所定义，及其药学上可接受的盐。 该化合物可用于治疗和/或预防与调节CB 2受体相关的疾病。

公开(公告)号：WO2006077025A2

公开(公告)日：2006-07-27

申请号：PCT/EP2006/000126

申请日：2006-01-10

Applicant: F. HOFFMANN-LA ROCHE AG ,  VERNALIS RESEARCH LIMITED ,  BENTLEY, Jonathan, Mark ,  DAWSON, Claire, Elizabeth ,  GUBA, Wolfgang ,  HEBEISEN, Paul ,  MONCK, Nathaniel ,  PRATT, Robert, Mark ,  RICHTER, Hans ,  ROEVER, Stephan ,  RUSTON, Vicki

Inventor： BENTLEY, Jonathan, Mark ,  DAWSON, Claire, Elizabeth ,  GUBA, Wolfgang ,  HEBEISEN, Paul ,  MONCK, Nathaniel ,  PRATT, Robert, Mark ,  RICHTER, Hans ,  ROEVER, Stephan ,  RUSTON, Vicki

IPC: C07D265/30 ,  A61K31/5375 ,  A61P3/04 ,  A61P3/10

CPC classification number: C07D265/30

Abstract: The present invention refers to chemical compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R 1 to R 5 have the significance given in claim 1. These compounds can be used for the preparation of medicaments.

Abstract translation: 本发明涉及式（I）化合物及其药学上可接受的盐和酯，其中R 1至R 5具有权利要求1中给出的含义。 这些化合物可用于制备药物。

公开(公告)号：WO2012031817A1

公开(公告)日：2012-03-15

申请号：PCT/EP2011/062548

申请日：2011-07-21

Applicant: F. HOFFMANN-LA ROCHE AG ,  WRIGHT, Matthew ,  ZOFFMANN JENSEN, Sannah ,  MATILE, Hugues ,  HEBEISEN, Paul ,  ROEVER, Stephan

Inventor： WRIGHT, Matthew ,  ZOFFMANN JENSEN, Sannah ,  MATILE, Hugues ,  HEBEISEN, Paul ,  ROEVER, Stephan

IPC: G01N33/68 ,  G01N33/92

CPC classification number: C07D417/12 ,  C07D213/82 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14

Abstract: The present invention refers to an assay method for determining the ability of compounds to modulate the level of ABCA1 protein in cells and its use in drug discovery and screening. The method is characterized by the use of apolipoprotein A-I labeled with a fluorophore for the detection of ABCA1 protein levels in cells and can be used for the detection of compounds being useful as HDL-cholesterol raising agents.

Abstract translation: 本发明涉及测定化合物调节细胞中ABCA1蛋白水平的能力的测定方法及其在药物发现和筛选中的用途。 该方法的特征在于使用用荧光团标记的载脂蛋白A-1用于检测细胞中的ABCA1蛋白水平，并且可用于检测用作HDL-胆固醇升高剂的化合物。

公开(公告)号：WO2009121741A1

公开(公告)日：2009-10-08

申请号：PCT/EP2009/053344

申请日：2009-03-23

Applicant: F. HOFFMANN-LA ROCHE AG ,  HEBEISEN, Paul ,  PANOUSIS, Constantinos, G. ,  ROEVER, Stephan ,  WRIGHT, Matthew

Inventor： HEBEISEN, Paul ,  PANOUSIS, Constantinos, G. ,  ROEVER, Stephan ,  WRIGHT, Matthew

IPC: C07D241/28 ,  C07D401/12 ,  A61P3/04 ,  A61K31/4965

CPC classification number: C07D241/28 ,  C07D401/12

Abstract: The present invention relates to pyrazine derivatives of the formula (I) wherein R 1 to R 8 are as defined in the description and claims, for the preparation of medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as preferably dyslipidemia.

Abstract translation: 本发明涉及式（I）的吡嗪衍生物，其中R1至R8如说明书和权利要求中所定义，用于制备用于治疗和/或预防可用HDL-胆固醇升高剂治疗的疾病的药物 ，例如优选血脂异常。

公开(公告)号：WO2008037628A1

公开(公告)日：2008-04-03

申请号：PCT/EP2007/059842

申请日：2007-09-18

Applicant: F. HOFFMANN-LA ROCHE AG ,  HAAP, Wolfgang ,  HEBEISEN, Paul ,  KITAS, Eric, A. ,  KOHLER, Philipp Christoph ,  KUEHNE, Holger ,  RUF, Armin

Inventor： HAAP, Wolfgang ,  HEBEISEN, Paul ,  KITAS, Eric, A. ,  KOHLER, Philipp Christoph ,  KUEHNE, Holger ,  RUF, Armin

IPC: C07C311/37 ,  C07C303/38 ,  A61K31/18 ,  C07D307/12 ,  C07D333/10 ,  C07D333/12 ,  C07D333/16

CPC classification number: C07C311/58 ,  C07D307/64 ,  C07D317/62 ,  C07D333/34 ,  C07D333/38

Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein L, R 1 , R 2 , m and n have the meaning given in claim 1 and which can be used in the form of pharmaceutical compositions.

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

公开(公告)号：WO2008031734A1

公开(公告)日：2008-03-20

申请号：PCT/EP2007/059167

申请日：2007-09-03

Applicant: F. HOFFMANN-LA ROCHE AG ,  HEBEISEN, Paul ,  ROEVER, Stephan

Inventor： HEBEISEN, Paul ,  ROEVER, Stephan

IPC: C07D213/82 ,  C07D401/06 ,  C07D417/06 ,  A61K31/455 ,  A61K31/425 ,  A61P5/48 ,  A61P25/32 ,  A61K31/34

CPC classification number: C07D213/82 ,  C07D401/06 ,  C07D417/06

Abstract: The present invention relates to compounds of the formula (I) wherein R 1 to R 8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors.

Abstract translation: 本发明涉及式（I）化合物，其中R 1至R 8如在说明书和权利要求书中所定义，及其药学上可接受的盐。 该化合物可用于治疗和/或预防与调节CB1受体相关的疾病。

公开(公告)号：WO2013037703A1

公开(公告)日：2013-03-21

申请号：PCT/EP2012/067469

申请日：2012-09-07

Applicant: F. HOFFMANN-LA ROCHE AG ,  GRETHER, Uwe ,  HEBEISEN, Paul ,  MOHR, Peter ,  RICKLIN, Fabienne ,  ROEVER, Stephan

Inventor： GRETHER, Uwe ,  HEBEISEN, Paul ,  MOHR, Peter ,  RICKLIN, Fabienne ,  ROEVER, Stephan

IPC: C07D213/87 ,  C07D401/06 ,  C07D405/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444

CPC classification number: C07D213/87 ,  C07D401/06 ,  C07D405/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: The present invention relates to compounds of the formula wherein R 1 to R 5 are defined in the description and claims, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.

Abstract translation: 本发明涉及下式的化合物，其中R 1至R 5在说明书和权利要求书中定义，及其药学上可接受的盐，其制备方法，含有它们的药物组合物及其用作治疗和/或预防疾病的药物的用途 可以用HDL-胆固醇升高剂治疗，如特别是血脂异常，动脉粥样硬化和心血管疾病。

公开(公告)号：WO2012049190A1

公开(公告)日：2012-04-19

申请号：PCT/EP2011/067753

申请日：2011-10-12

Applicant: F. HOFFMANN-LA ROCHE AG ,  GRETHER, Uwe ,  HEBEISEN, Paul ,  HOFFMANN, Torsten ,  ROEVER, Stephan

Inventor： GRETHER, Uwe ,  HEBEISEN, Paul ,  HOFFMANN, Torsten ,  ROEVER, Stephan

IPC: C07D213/75 ,  C07D401/12 ,  C07D403/12 ,  C07D407/12 ,  C07D413/12 ,  C07D417/12 ,  C07D498/04 ,  A61K31/444 ,  A61K31/4965 ,  A61P9/00

CPC classification number: C07D213/75 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D413/12 ,  C07D417/12 ,  C07D498/04

Abstract: The present invention relates to compounds of the formula I wherein A, R 1 to R 7 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.

Abstract translation: 本发明涉及式I化合物，其中A，R 1至R 7在说明书中定义，及其药学上可接受的盐，其制备方法，含有它们的药物组合物及其作为用于治疗和/或预防疾病的药物的用途 其可以用HDL-胆固醇升高剂治疗，例如特别是血脂异常，动脉粥样硬化和心血管疾病。