公开(公告)号：EP2509963A1

公开(公告)日：2012-10-17

申请号：EP10788479.3

申请日：2010-12-06

申请人： Novartis AG

发明人： BERGHAUSEN, Joerg ,  KAPA, Prasad, Koteswara ,  MCKENNA, Joseph ,  SLADE, Joel ,  WU, Raeann ,  DU, Zhengming ,  STOWASSER, Frank

IPC分类号： C07D239/48 ,  A61K31/506 ,  A61P35/00

CPC分类号： C07D239/48

摘要： The present technology provides novel anhydrous and hydrated crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea, amorphous and anhydrous crystalline polymorphs of its monophosphoric acid salt, and the hydrochloride salt, including its dihydrate. The present technology further provides methods for preparing the various forms, compositions containing them, and methods of treatment employing them.

公开(公告)号：EP2640467B1

公开(公告)日：2014-12-17

申请号：EP11790916.8

申请日：2011-11-17

申请人： Novartis AG

发明人： BERGHAUSEN, Joerg ,  REN, Haixia

IPC分类号： A61P35/00 ,  A61K31/495 ,  C07D401/12

CPC分类号： C07D401/12

公开(公告)号：EP2516009A1

公开(公告)日：2012-10-31

申请号：EP10792944.0

申请日：2010-12-21

申请人： Novartis AG

发明人： BERGHAUSEN, Joerg ,  BUSCHMANN, Nicole ,  FURET, Pascal ,  GESSIER, François ,  HERGOVICH LISZTWAN, Joanna ,  HOLZER, Philipp ,  JACOBY, Edgar ,  KALLEN, Joerg ,  MASUYA, Keiichi ,  PISSOT SOLDERMANN, Carole ,  REN, Haixia ,  STUTZ, Stefan

IPC分类号： A61P35/00 ,  A61K31/495 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12 ,  C07D405/14 ,  C07D413/14 ,  C07D217/24

CPC分类号： C07D239/82 ,  C07D217/24 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： The invention relates to substituted nitrogen containing bicyclic heterocycles of the formula (I): wherein Z is CH
2 or N-R
4 and X, R
1 , R
2 , R
4 , R
6 , R
7 and n are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.

公开(公告)号：EP2509963B1

公开(公告)日：2015-11-25

申请号：EP10788479.3

申请日：2010-12-06

申请人： Novartis AG

发明人： BERGHAUSEN, Joerg ,  KAPA, Prasad, Koteswara ,  MCKENNA, Joseph ,  SLADE, Joel ,  WU, Raeann ,  DU, Zhengming ,  STOWASSER, Frank

IPC分类号： C07D239/48 ,  A61K31/506 ,  A61P35/00

CPC分类号： C07D239/48

公开(公告)号：EP2451458A2

公开(公告)日：2012-05-16

申请号：EP10734715.5

申请日：2010-07-05

申请人： Novartis AG

发明人： BERGHAUSEN, Joerg ,  HAUG, Claire ,  HERBIG, Michael ,  HU, Bin ,  JONAT, Stéphane ,  LELETI, Rajender ,  MEINGASSNER, Josef Gottfried ,  MONNIER, Stéphanie ,  NAPP, Matthias ,  PRASHAD, Mahavir ,  STUETZ, Anton ,  THAKUR, Ranjit

IPC分类号： A61K31/505 ,  A61K47/10 ,  A61K9/00 ,  A61P17/00

CPC分类号： A61K31/505 ,  A61K9/0014 ,  A61K47/06 ,  A61K47/10 ,  A61K47/14 ,  C07D239/34

摘要： The present invention relates to pharmaceutical compositions of 6-(6-hydroxymethyl- pyrimidin-4-yloxy)-naphthalene-1-carboxyfic acid (3-trifluoromethyl-phenyl)-amide, to the use of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthatene-1-carboxylic acid (3-trifluoromethyI- phenyl)-amide and compositions of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1- carboxylic acid (3-trifluoromethyi-phenyi)-amide in therapeutic applications, especially indications with a dysregulation/overexpression of VEFG, (neo)-vascularisation and VEGF driven angiogenesis and to methods for manufacturing such compositions, the invention further relates to specific forms of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-πaphthalene-1- carboxyiic acid (3-trifluαromethyl-phenyl)-amide and to the manufacturing and use of such forms. The present invention also relates to a new process to produce 6-{6-hydroxymethyl- pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide.

公开(公告)号：EP2516009B1

公开(公告)日：2014-09-24

申请号：EP10792944.0

申请日：2010-12-21

申请人： Novartis AG

发明人： BERGHAUSEN, Joerg ,  BUSCHMANN, Nicole ,  FURET, Pascal ,  GESSIER, François ,  HERGOVICH LISZTWAN, Joanna ,  HOLZER, Philipp ,  JACOBY, Edgar ,  KALLEN, Joerg ,  MASUYA, Keiichi ,  PISSOT SOLDERMANN, Carole ,  REN, Haixia ,  STUTZ, Stefan

IPC分类号： A61P35/00 ,  A61K31/495 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12 ,  C07D405/14 ,  C07D413/14 ,  C07D217/24

CPC分类号： C07D239/82 ,  C07D217/24 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

公开(公告)号：EP2640467A1

公开(公告)日：2013-09-25

申请号：EP11790916.8

申请日：2011-11-17

申请人： Novartis AG

发明人： BERGHAUSEN, Joerg ,  REN, Haixia

IPC分类号： A61P35/00 ,  A61K31/495 ,  C07D401/12

CPC分类号： C07D401/12

摘要： A crystalline form of (S)-1-(4-Chloro-phenyl)-7-isopropoxy-6-methoxy-2-(4-{methyl-[4-(4- methyl-3-oxo-piperazin-1-yl)-trans-cyclohexylmethyl]-amino}-phenyl)-1,4dihydro-2H- isoquinolin-3-one, which is useful in the treatment of a disease or disorder associated with the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively, (I).