公开(公告)号：EP2958893A1

公开(公告)日：2015-12-30

申请号：EP14706519.7

申请日：2014-02-18

申请人： F.Hoffmann-La Roche AG

发明人： FISHLOCK, Daniel ,  GU, Chen ,  SHU, Lianhe ,  REGE, Pankaj, Devdatta ,  SARMA, Keshab

IPC分类号： C07D207/16

CPC分类号： C07D207/16

摘要： The present invention provides an improved method for the large scale production of the compound 4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid.

公开(公告)号：EP2841418A1

公开(公告)日：2015-03-04

申请号：EP13718188.9

申请日：2013-04-23

申请人： F.Hoffmann-La Roche AG

发明人： ADAM, Jean-Michel ,  DVORAK, Charles Alois ,  FISHLOCK, Daniel ,  HUMPHREYS, Eric R. ,  IDING, Hans ,  PFLEGER, Christophe ,  REGE, Pankaj D. ,  SHI, Xianqing ,  VITALE, Justin ,  WANG, Shaoning ,  ZAJAC, Marian

IPC分类号： C07D207/08 ,  A61K31/40 ,  A61P25/22 ,  A61P25/24

CPC分类号： C07D207/08

摘要： The present invention is concerned with a novel process for the preparation of a compound of formula I and its hydrates, as well as with a crystall polymorph thereof. The compounds of formula (I) and the corresponding hydrates are pharmaceutically active substances.

摘要翻译： 式I化合物和相应的水合物是药物活性物质。

公开(公告)号：EP2825528A1

公开(公告)日：2015-01-21

申请号：EP13708466.1

申请日：2013-03-12

申请人： F.Hoffmann-La Roche AG

发明人： FISHLOCK, Daniel ,  BARTKOVITZ, David Joseph ,  CHU, Xin-Jie ,  VU, Binh Thanh ,  ZHAO, Chunlin

IPC分类号： C07D207/16 ,  C07D405/12 ,  C07D493/04 ,  C07F9/572 ,  A61K31/40 ,  A61K31/4035 ,  A61P35/00

CPC分类号： C07D403/12 ,  C07D207/16 ,  C07D405/12 ,  C07D493/04 ,  C07F9/572 ,  C07F9/5727 ,  C07H15/26

摘要： There are provided compounds of formula (I) wherein X, Y, Z, R
1 , R
2 , R
3 and R
4 are as described herein, and enantiomers and pharmaceutically acceptable salts and esters thereof; as well as methods for making such compounds, pharmaceutical compositions comprising said compounds, and their use in the treatment of cancer.