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.