公开(公告)号：EP2220055A2

公开(公告)日：2010-08-25

申请号：EP08785999.7

申请日：2008-07-09

申请人： F. Hoffmann-La Roche AG

发明人： AEBI, Johannes ,  BINGGELI, Alfred ,  GREEN, Luke ,  HARTMANN, Guido ,  MAERKI, Hans P. ,  MATTEI, Patrizio ,  RICKLIN, Fabienne ,  ADAM, Jean-Michel ,  IDING, Hans ,  SCHMID, Rudolf ,  WIRZ, Beat

IPC分类号： C07D241/08 ,  C07D285/18 ,  C07D401/06 ,  C07D403/06 ,  A61K31/495 ,  A61K31/496 ,  A61P9/10

CPC分类号： C07D241/08 ,  C07D285/18 ,  C07D401/06 ,  C07D403/06

摘要： The invention is concerned with novel heterocyclyl compounds of formula (I), wherein A, X, Y, R3, R4, R5, R6, R7, R8, R9, R10, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.

公开(公告)号：EP1868999B1

公开(公告)日：2009-07-01

申请号：EP06725329.4

申请日：2006-03-27

申请人： F. Hoffmann-La Roche AG

发明人： HEBEISEN, Paul ,  IDING, Hans ,  NETTEKOVEN, Matthias Heinrich ,  OBST, Ulrike ,  ROEVER, Stephan ,  WIRZ, Beat

IPC分类号： C07D213/64 ,  C07D213/74 ,  A61P25/34 ,  A61P3/00 ,  A61K31/465

CPC分类号： C07D213/64 ,  C07D213/74 ,  C07D213/82 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to compounds of the formula (I) wherein X and R1 to R8 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, such as obesity.

公开(公告)号：EP1664323A1

公开(公告)日：2006-06-07

申请号：EP04765204.5

申请日：2004-09-15

申请人： F. HOFFMANN-LA ROCHE AG

发明人： IDING, Hans ,  KRUMMENACHER, Daniela ,  WIRZ, Beat ,  WOSTL, Wolfgang

IPC分类号： C12P41/00 ,  C07D207/26 ,  C12R1/72

CPC分类号： C07D207/26 ,  C07D207/277 ,  C12P17/10 ,  C12P41/005

摘要： The present invention relates to a process for the preparation of enantiopure intermediates useful in the synthesis of valuable pharmaceutically active compounds, e.g. MAOB inhibitors, and to novel intermediates of formulae (I) and (II) wherein R21, R22, R23 and R24 are as defined in the description and claims.

公开(公告)号：EP1434870A1

公开(公告)日：2004-07-07

申请号：EP02779375.1

申请日：2002-09-19

申请人： F. HOFFMANN-LA ROCHE AG

发明人： BLEICHER, Konrad ,  BORTHWICK, Scott ,  IDING, Hans ,  ROGERS-EVANS, Mark ,  SCHMID, Stefan ,  TONG, Han, Min ,  WIRZ, Beat

IPC分类号： C12P13/04 ,  C12P11/00 ,  C07C323/63

CPC分类号： C12P13/04 ,  C07C323/59 ,  C07C323/63 ,  C07D285/36 ,  C12P11/00 ,  C12P41/005

摘要： The compounds of formula (I) are useful for the preparation of 1,5-benzothiazepines which are useful as enzyme inhibitors, such as protease, interleukin-1β-converting enzyme, elastase or angiotensin enzyme, GPCR antagonists (cholecystokinin, angiotensin II receptor). The present invention relates to a new process for the preparation compounds of formula (I), wherein R?1, R2, R3¿ and n are as described in the description which process comprises reacting compounds of formula (II), wherein R?1, R2, R3¿, n and R4 are as described in the description, with a protease in an aqueous system containing an organic co-solvent.

公开(公告)号：EP1542969B1

公开(公告)日：2010-03-03

申请号：EP03748052.2

申请日：2003-09-18

申请人： F. Hoffmann-La Roche AG

发明人： IDING, Hans ,  JOLIDON, Synese ,  KRUMMENACHER, Daniela ,  RODRIGUEZ SARMIENTO, Rosa, Maria ,  THOMAS, Andrew, William ,  WIRZ, Beat ,  WOSTL, Wolfgang ,  WYLER, Rene

IPC分类号： C07D207/26 ,  C07D401/04 ,  A61K31/4015 ,  A61P25/16 ,  A61P25/28

CPC分类号： C07D207/273 ,  C07D207/277

摘要： Racemic enantiomerically pure 4- pyrrolidino derivatives of formula (I), processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, in particular which is mediated by monoamine oxidase B inhibitors, in particular Alzheimer’s disease or senile dementia.

公开(公告)号：EP2035394A1

公开(公告)日：2009-03-18

申请号：EP07765355.8

申请日：2007-06-11

申请人： F. Hoffmann-La Roche AG

发明人： HEBEISEN, Paul ,  IDING, Hans ,  NETTEKOVEN, Matthias Heinrich ,  OBST SANDER, Ulrike ,  ROEVER, Stephan ,  WEISS, Urs ,  WIRZ, Beat

IPC分类号： C07D241/24 ,  C07D241/26 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  A61K31/497 ,  A61P25/32

CPC分类号： C07D241/26 ,  C07D241/24 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

摘要： The present invention relates to compounds of the formula (I) wherein R1 to R8 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, such as obesity.

公开(公告)号：EP1542969A1

公开(公告)日：2005-06-22

申请号：EP03748052.2

申请日：2003-09-18

申请人： F. Hoffmann-La Roche AG

发明人： IDING, Hans ,  JOLIDON, Synese ,  KRUMMENACHER, Daniela ,  RODRIGUEZ SARMIENTO, Rosa, Maria ,  THOMAS, Andrew, William ,  WIRZ, Beat ,  WOSTL, Wolfgang ,  WYLER, Rene

IPC分类号： C07D207/26 ,  C07D401/04 ,  A61K31/4015 ,  A61P25/16 ,  A61P25/28

CPC分类号： C07D207/273 ,  C07D207/277

摘要： Racemic enantiomerically pure 4- pyrrolidino derivatives of formula (I), processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, in particular which is mediated by monoamine oxidase B inhibitors, in particular Alzheimer’s disease or senile dementia.

摘要翻译： 式（I）的外消旋对映体纯的4-吡咯烷基衍生物，其制备方法，包含所述衍生物的药物组合物及其在预防和治疗疾病中的用途，特别是由单胺氧化酶B抑制剂，特别是阿尔茨海默病 或老年痴呆症。

公开(公告)号：EP1539746A1

公开(公告)日：2005-06-15

申请号：EP03747962.3

申请日：2003-09-04

申请人： F. Hoffmann-La Roche AG

发明人： BINGGELI, Alfred ,  GRETHER, Uwe ,  HILPERT, Hans ,  HUMM, Roland ,  IDING, Hans ,  KUHN, Bernd ,  MAERKI, Hans-Peter ,  MEYER, Markus ,  MOHR, Peter ,  WIRZ, Beat

IPC分类号： C07D413/06 ,  A61K31/405 ,  C07D413/14 ,  C07D417/06 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10

CPC分类号： C07D413/06 ,  C07D417/06

摘要： Compounds of formula (I), as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R8, A, A1 and n have the significance given in claim 1 can be used in the form of pharmaceutical preparations.

公开(公告)号：EP3197875B1

公开(公告)日：2019-08-14

申请号：EP15782120.8

申请日：2015-09-25

申请人： F. Hoffmann-La Roche AG ,  Genentech, Inc.

发明人： GOSSELIN, Francis ,  HAN, Chong ,  IDING, Hans ,  REENTS, Reinhard ,  SAVAGE, Scott ,  WIRZ, Beat

IPC分类号： C07D239/70

公开(公告)号：EP3197875A1

公开(公告)日：2017-08-02

申请号：EP15782120.8

申请日：2015-09-25

申请人： F. Hoffmann-La Roche AG ,  Genentech, Inc.

发明人： GOSSELIN, Francis ,  HAN, Chong ,  IDING, Hans ,  REENTS, Reinhard ,  SAVAGE, Scott ,  WIRZ, Beat

IPC分类号： C07D239/70

CPC分类号： C07D239/70 ,  C07B57/00 ,  C07B2200/07 ,  C07C253/30 ,  C07C253/34 ,  C07C255/22 ,  C07D239/42 ,  C07D239/54 ,  C12N9/78 ,  C12P41/00 ,  C12Y305/05001

摘要： The present disclosure relates to processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds, and more particularly relates to processes for preparing (R)-4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d] pyrimidin-4-yl)piperazine and N-protected derivatives thereof, which may be used as an intermediate in the synthesis of Ipatasertib (i.e., (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)-propan-1-one). The present disclosure additionally relates to various compounds that are intermediates employed in these processes.

摘要翻译： 本发明涉及制备（环戊基[d]嘧啶-4-基）哌嗪化合物的方法，更具体地涉及制备（R）-4-（5-甲基-7-氧代-6,7-二氢 -5H-环戊并[d]嘧啶-4-基）哌嗪和其N-保护的衍生物，其可以用作合成Ipatasertib（即（S）-2-（4-氯苯基）-1- （4 - （（5R，7R）-7-羟基-5-甲基-6,7-二氢-5H-环戊二烯并[d]嘧啶-4-基）哌嗪-1-基）-3-（异丙基氨基） - 丙 -1-酮）。 本公开另外涉及作为在这些方法中使用的中间体的各种化合物。