公开(公告)号：EP1639129A2

公开(公告)日：2006-03-29

申请号：EP04732966.9

申请日：2004-05-14

申请人： F. HOFFMANN-LA ROCHE AG

发明人： WRIGHT, Matthew, Blake

IPC分类号： C12Q1/68 ,  C12N15/10 ,  C07H21/00

CPC分类号： C12Q1/6883 ,  C07H21/00 ,  C12Q2600/156

摘要： The present invention relates to surrogate markers for LXR activation, and methods of diagnosing a disease linked to LXR activation, methods of monitoring the treatment of patients suffering from a disease linked to LXR activation, and methods of identifying compounds which modulate LXR activity.

公开(公告)号：EP1682508A1

公开(公告)日：2006-07-26

申请号：EP04790987.4

申请日：2004-10-28

申请人： F. HOFFMANN-LA ROCHE AG

发明人： ACKERMANN, Jean ,  AEBI, Johannes ,  BINGGELI, Alfred ,  GRETHER, Uwe ,  HIRTH, Georges ,  KUHN, Bernd ,  MAERKI, Hans-Peter ,  MEYER, Markus ,  MOHR, Peter ,  WRIGHT, Matthew, Blake

IPC分类号： C07D213/38 ,  C07D213/30 ,  C07D213/32 ,  C07D239/26 ,  C07D213/56 ,  C07D241/12 ,  C07D237/08 ,  C07D213/82 ,  C07D239/28 ,  A61K31/435 ,  A61K31/505 ,  A61P3/10

CPC分类号： C07D213/30 ,  C07D213/32 ,  C07D213/38 ,  C07D213/56 ,  C07D213/82 ,  C07D237/08 ,  C07D239/26 ,  C07D239/28 ,  C07D241/12

摘要： This invention relates to compounds of the formula wherein one of R 5 , R 6 and R 7 is and X 1 , X 2 , Y 1 to Y 4 , R 1 to R 13 and m and n are as defined in the description, and to all enantiomers and pharmaceutically acceptable salts and/or esters 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 modulated by PPAR´ and/or PPAR± agonists.

公开(公告)号：EP1636198A1

公开(公告)日：2006-03-22

申请号：EP04739479.6

申请日：2004-06-01

申请人： F. HOFFMANN-LA ROCHE AG

发明人： ACKERMANN, Jean ,  AEBI, Johannes ,  BINGGELI, Alfred ,  GRETHER, Uwe ,  HIRTH, Georges ,  KUHN, Bernd ,  MAERKI, Hans-Peter ,  MEYER, Markus ,  MOHR, Peter ,  WRIGHT, Matthew, Blake

IPC分类号： C07D263/32 ,  C07D277/28 ,  A61K31/421 ,  A61K31/426 ,  A61P3/00 ,  A61P9/00 ,  A61P35/00

CPC分类号： C07D277/28 ,  C07D263/32

摘要： This invention relates to compounds of the formula (I); wherein X, Y, R1 to R11 and n are as defined in the description, and all enantiomers; and pharmaceutically acceptable salts and/or esters 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 modulated by PPARδ and/or PPARα agonists. Examples of such diseases are diabetes, particularly non-insulin dependent diabetes mellitus, increased lipid and cholesterol levels, particularly low HDL-cholesterol; high LDL- cholesterol, or high triglyceride levels, atherosclerotic diseases, metabolic syndrome (syndrome X), elevated blood pressure, endothelial dysfunction, procoagulant state, dyslipidemia, polycystic ovary syndrome, inflammatory diseases such as rheumatoid arthritis, osteoarthritis, psoriasis and other skin disorder, and proliferative diseases.

摘要翻译： 本发明涉及式（I）的化合物; 其中X，Y，R 1至R 11和n如说明书中所定义，并且所有对映异构体; 及其药学上可接受的盐和/或酯。 本发明进一步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/或预防由PPARδ和/或PPARα激动剂调节的疾病的用途。 这些疾病的例子是糖尿病，特别是非胰​​岛素依赖型糖尿病，脂质和胆固醇水平升高，特别是低HDL-胆固醇; 高LDL-胆固醇或高甘油三酯水平，动脉粥样硬化疾病，代谢综合征（X综合征），血压升高，内皮功能障碍，促凝血状态，血脂异常，多囊卵巢综合征，炎症性疾病如类风湿性关节炎，骨关节炎，牛皮癣和其他皮肤病 和增殖性疾病。

公开(公告)号：EP1802566B1

公开(公告)日：2008-11-26

申请号：EP05786065.2

申请日：2005-09-22

申请人： F. Hoffmann-La Roche AG

发明人： DEHMLOW, Henrietta ,  KUHN, Bernd ,  PANDAY, Narendra ,  RATNI, Hasane ,  WRIGHT, Matthew, Blake

IPC分类号： C07C69/92 ,  C07D263/32 ,  C07C43/23 ,  C07C69/734 ,  C07C59/68 ,  C07C65/24 ,  C07D261/20 ,  C07D275/04 ,  A61K31/085 ,  A61K31/192 ,  A61K31/216 ,  A61K31/235 ,  A61K31/421 ,  A61K31/423 ,  A61K31/428

CPC分类号： C07D275/04 ,  C07C43/23 ,  C07C59/68 ,  C07C65/24 ,  C07C69/734 ,  C07C69/92 ,  C07D249/06 ,  C07D261/08 ,  C07D261/20 ,  C07D263/32

摘要： The invention is concerned with hexafluoroisopropanol substituted ether derivatives of formula (I), wherein Rl to R3 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.

摘要翻译： 本发明涉及式（I）的六氟异丙醇取代的醚衍生物，其中R1至R3如说明书和权利要求中所定义，以及其生理上可接受的盐和酯。 这些化合物与LXRα和LXRβ结合，可用作药物。

公开(公告)号：EP1682535A1

公开(公告)日：2006-07-26

申请号：EP04790967.6

申请日：2004-10-28

申请人： F. HOFFMANN-LA ROCHE AG

发明人： ACKERMANN, Jean ,  AEBI, Johannes ,  BINGGELI, Alfred ,  GRETHER, Uwe ,  HIRTH, Georges ,  KUHN, Bernd ,  MAERKI, Hans-Peter ,  MEYER, Markus ,  MOHR, Peter ,  WRIGHT, Matthew, Blake

IPC分类号： C07D403/12 ,  C07D401/12 ,  A61K31/4439 ,  A61K31/506 ,  A61P3/10

CPC分类号： C04B35/632 ,  C07D401/12 ,  C07D403/12

摘要： This invention relates to compounds of formula (I), wherein one of R6, R7 and R8 is formula (II) and X, Y1 to Y4 , R1 to R 14 and n are as defined in the description, and to all enantiomers and pharmaceutically acceptable salts and/or esters 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 modulated by PPARδ and/or PPARα agonists.

公开(公告)号：EP1682507A1

公开(公告)日：2006-07-26

申请号：EP04790969.2

申请日：2004-10-28

申请人： F. HOFFMANN-LA ROCHE AG

发明人： ACKERMANN, Jean ,  AEBI, Johannes ,  BINGGELI, Alfred ,  GRETHER, Uwe ,  HIRTH, Georges ,  KUHN, Bernd ,  MAERKI, Hans-Peter ,  MEYER, Markus ,  MOHR, Peter ,  WRIGHT, Matthew, Blake

IPC分类号： C07D213/38 ,  C07D213/30 ,  C07D239/26 ,  A61K31/345 ,  A61K31/505 ,  A61P3/10

CPC分类号： C07D213/30 ,  C07D213/38 ,  C07D239/26

摘要： This invention relates to compounds of the formula (I) wherein R6 and R7 is formula (II) R4 and R5 or R5 and R6 together with the carbon atoms to which they are attached, form a ring as defined in the description and X1, X2, Y1 to Y4, R1 to R13 and n are as specified in the description, and to all enantiomers and pharmaceutically acceptable salts and/or esters 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 modulated by PPARδ and/or- PPARα agonists.

公开(公告)号：EP1644368A1

公开(公告)日：2006-04-12

申请号：EP04740332.4

申请日：2004-06-25

申请人： F. HOFFMANN-LA ROCHE AG

发明人： ACKERMANN, Jean ,  AEBI, Johannes ,  BINGGELI, Alfred ,  GRETHER, Uwe ,  HIRTH, Georges ,  KUHN, Bernd ,  MAERKI, Hans-Peter ,  MEYER, Markus ,  MOHR, Peter ,  WRIGHT, Matthew, Blake

IPC分类号： C07D417/12 ,  A61K31/426 ,  A61P3/10 ,  A61P3/04

CPC分类号： C07D417/12

摘要： This invention relates to compounds of the formula (I) wherein one of R6, R7 or R8 is and X, Y, R1 to R13 and n are as defined in the description, and all enantiomers and pharmaceutically acceptable salts and/or esters 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 modulated by PPARδ and/or PPARα agonists.

公开(公告)号：EP1644368B1

公开(公告)日：2008-08-27

申请号：EP04740332.4

申请日：2004-06-25

申请人： F. Hoffmann-La Roche AG

发明人： ACKERMANN, Jean ,  AEBI, Johannes ,  BINGGELI, Alfred ,  GRETHER, Uwe ,  HIRTH, Georges ,  KUHN, Bernd ,  MAERKI, Hans-Peter ,  MEYER, Markus ,  MOHR, Peter ,  WRIGHT, Matthew, Blake

IPC分类号： C07D417/12 ,  A61K31/426 ,  A61P3/10 ,  A61P3/04

CPC分类号： C07D417/12

摘要： This invention relates to compounds of the formula (I) wherein one of R6, R7 or R8 is and X, Y, R1 to R13 and n are as defined in the description, and all enantiomers and pharmaceutically acceptable salts and/or esters 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 modulated by PPARδ and/or PPARα agonists.