公开(公告)号：EP1781608B1

公开(公告)日：2009-10-21

申请号：EP05772210.0

申请日：2005-08-08

申请人： F.HOFFMANN-LA ROCHE AG

发明人： ACKERMANN, Jean ,  AEBI, Johannes ,  BINGGELI, Alfred ,  GRETHER, Uwe ,  KUHN, Bernd ,  MAERKI, Hans-Peter ,  MEYER, Markus

IPC分类号： C07D209/08 ,  A61K31/405 ,  A61P3/10 ,  A61P3/06

CPC分类号： C07D209/08

摘要： This invention is concerned with compounds of the formula (I), wherein one of R6, R7, R8 and R9 is formula (II), and X, R1 to R12, m, n and o are as defined in the description, 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：EP2102215A1

公开(公告)日：2009-09-23

申请号：EP07857234.4

申请日：2007-11-28

申请人： F. Hoffmann-La Roche AG

发明人： CHEN, Li ,  LAI, Wayne Wen ,  NETTEKOVEN, Matthias ,  ROCHE, Olivier ,  ZHENG, Deye

IPC分类号： C07D495/04 ,  A61K31/4365 ,  A61P3/04 ,  A61P3/10

CPC分类号： C07D495/04

摘要： The present invention relates to compounds of formula (I), wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

公开(公告)号：EP2079721A2

公开(公告)日：2009-07-22

申请号：EP07822030.8

申请日：2007-10-30

申请人： F. Hoffmann-La Roche AG

发明人： ZUTTER, Ulrich

IPC分类号： C07D307/32 ,  C07D471/04

CPC分类号： C07D307/32 ,  C07D471/04

摘要： The present invention relates to a process of the preparation of (S)-4-fluoromethyl-dihydro-furan-2-one of the formula (I) by employing a dialkylmalonate of the formula (V) wherein R1b is lower alkyl, and the use of this process for the manufacture of DPP-IV inhibitors that are useful for the treatment and/or prophylaxis of diseases such as diabetes.

摘要翻译： 本发明涉及通过使用式（V）的二烷基丙二酸酯（其中R 1b是低级烷基）制备式（I）的（S）-4-氟甲基 - 二氢呋喃-2-酮的方法， 该方法用于制造可用于治疗和/或预防诸如糖尿病的疾病的DPP-IV抑制剂。

公开(公告)号：EP2079447A1

公开(公告)日：2009-07-22

申请号：EP07820919.4

申请日：2007-10-04

申请人： F.HOFFMANN-LA ROCHE AG

发明人： ALBANO, Antonio A. ,  PHUAPRADIT, Wantanee ,  SHAH, Navnit Hargovindas ,  YU, Zhongshui ,  ZHANG, Lin

IPC分类号： A61K9/16 ,  A61K9/19 ,  A61K45/06 ,  A61K47/34

CPC分类号： A61K9/1676 ,  A61K47/32

摘要： The present invention provides novel pharmaceutical solid dosage forms for oral administration comprising a therapeutically effective amount of an unstable crystalline form or an amorphous form of a therapeutically effective compound micro-embedded into an ionic water-insoluble polymer. The therapeutically effective compounds, which have a tendency to gel, are micro-embedded into an ionic water-insoluble polymer matrix to provide a dosage form having rapid, reproducible, and complete dissolution profiles. These novel solid pharmaceutical dosage forms are useful in the treatment or control of a number of diseases.

公开(公告)号：EP2074096A1

公开(公告)日：2009-07-01

申请号：EP07820501.0

申请日：2007-09-24

申请人： F.HOFFMANN-LA ROCHE AG

发明人： ANDJELKOVIC, Mirjana ,  BÉNARDEAU, Agnès ,  CHAPUT, Evelyne ,  HEBEISEN, Paul ,  NETTEKOVEN, Matthias ,  OBST SANDER, Ulrike ,  PANOUSIS, Constantinos G. ,  ROEVER, Stephan

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

CPC分类号： C07D213/82 ,  C07D213/74 ,  C07D241/24

摘要： The present invention relates to the use of compounds of the formula wherein A, G, R1 to R8 and R17 are as defined in the description, for the preparation of medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as peripheral vascular disease, dyslipidemia, hyperbetalipoproteinemia, hypoalphalipoproteinemia, hypercholesterolemia, hypertriglyceridemia, familial hypercholesterolemia, cardiovascular disorders, angina, ischemia, cardiac ischemia, stroke, myocardial infarction, reperfusion injury, angioplastic restenosis, hypertension, and vascular complications of diabetes, obesity or endotoxemia.

公开(公告)号：EP2069343A2

公开(公告)日：2009-06-17

申请号：EP07803229.9

申请日：2007-09-05

申请人： F. Hoffmann-La Roche AG

发明人： ABRECHT, Stefan ,  SCALONE, Michelangelo ,  SCHMID, Rudolf

IPC分类号： C07D471/04

CPC分类号： C07D455/06 ,  B01J31/2295 ,  B01J2231/641 ,  B01J2531/822 ,  C07D471/04 ,  Y02P20/55

摘要： The invention relates to a process for the preparation of pyrido[2, 1-a] isoquinoline derivatives of the formula (I), weherein R2, R3 and R4 are as defined in the specification, comprising the steps of: a) catalytic asymmetric hydrogenation of an enamine of the formula (II), wherein R1 is lower alkyl, in the presence of a transition metal catalyst containing a chiral diphosphane ligand, b) introduction of an amino protecting group Prot and c) amidation of the ester to form an amide of formula (V), wherein R2, R3, R4 and Prot are as defined in the specification.

公开(公告)号：EP1945635B1

公开(公告)日：2009-05-06

申请号：EP06792744.2

申请日：2006-08-09

申请人： F.HOFFMANN-LA ROCHE AG

发明人： NETTEKOVEN, Matthias Heinrich ,  ROCHE, Olivier

IPC分类号： C07D417/04 ,  C07D417/14 ,  A61K31/427 ,  A61K31/426 ,  A61K31/4436 ,  A61K31/455 ,  A61P3/04 ,  A61P25/00

CPC分类号： C07D417/04 ,  C07D417/14

摘要： The present invention relates to compounds of formula (I) wherein R1, R2 and R3 are as defined in the description and claims. It further relates to pharmaceutically acceptable salts thereof as well as to pharmaceutical compositions comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

公开(公告)号：EP1725546B1

公开(公告)日：2008-10-08

申请号：EP05715587.1

申请日：2005-02-28

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 ,  A61K31/4155 ,  A61P9/00

CPC分类号： C07D403/12

摘要： This invention is concerned with compounds of the formula (I), wherein one of R6, R7 and R8 is (II), and R1 to R15 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.

摘要翻译： 本发明涉及式（I）化合物，其中R 6，R 7和R 8中的一个是（II），并且R 1至R 15和n如说明书中所定义，且所有对映异构体和药学上可接受的盐和/或酯 它们。 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。

公开(公告)号：EP1583762B1

公开(公告)日：2008-07-09

申请号：EP03789381.5

申请日：2003-12-22

申请人： F. Hoffmann-La Roche AG

发明人： GUBA, Wolfgang ,  HAAP, Wolfgang ,  MARTY, Hans, Peter ,  NARQUIZIAN, Robert

IPC分类号： C07D417/04 ,  C07D417/14 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  A61P3/04

CPC分类号： C07D417/14 ,  C07D417/04

摘要： The present invention relates to compounds of formula (1) wherein R1, R2, R3, R4, R5, R6 and R7 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 CBI receptors.

公开(公告)号：EP1761519B1

公开(公告)日：2008-05-07

申请号：EP05756581.4

申请日：2005-06-13

申请人： F.HOFFMANN-LA ROCHE AG

发明人： GATTI MCARTHUR, Silvia ,  HERTEL, Cornelia ,  NETTEKOVEN, Matthias, Heinrich ,  RAAB, Susanne ,  ROCHE, Olivier ,  RODRIGUEZ-SARMIENTO, Rosa, Maria ,  SCHULER, Franz ,  PLANCHER, Jean-Marc

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D209/42 ,  A61K31/4439 ,  A61P3/04

CPC分类号： C07D405/14 ,  C07D209/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14

摘要： The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.