公开(公告)号：EP2044051B1

公开(公告)日：2010-01-27

申请号：EP07786791.9

申请日：2007-06-21

申请人： BIOVITRUM AB (publ)

发明人： JENMALM JENSEN, Annika ,  RINGOM, Rune ,  MEDINA, Carmen ,  SHILVOCK, John ,  WIIK, Marie ,  KOOLMEISTER, Tobias ,  ANGBRANT, Johan ,  SUTIN, Lori ,  HENRIKSSON, Martin ,  SANDVALL, Teresa ,  JOHANSSON, Lars ,  NILSSON, Björn

IPC分类号： C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D471/04

CPC分类号： C07D401/12 ,  C07D401/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D471/04

摘要： The present invention relates to compounds of the general formula (I) wherein X, Y, Z, A, Ar, R1, R2, R3, and R4 are as defined herein, which compounds are inhibitors of MNK2 and MNK1. The invention also relates to the use of the compounds in therapy, pharmaceutical compositions comprising the compounds, and the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of disorders related to undesired activity of MNK1 and/or MNK2 kinases.

公开(公告)号：EP2059517A1

公开(公告)日：2009-05-20

申请号：EP07819987.4

申请日：2007-08-29

申请人： Biovitrum AB (publ)

发明人： BRANDT, Peter ,  JOHANSSON, Gary ,  JOHANSSON, Lars ,  KOOLMEISTER, Tobias ,  NILSSON, Björn M ,  SANDVALL, Teresa ,  WEBER, Michael

IPC分类号： C07D401/12 ,  A61K31/506 ,  A61P3/00 ,  C07D401/14

CPC分类号： A61K31/4545 ,  A61K31/496 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  A61K2300/00

摘要： The present invention relates to compounds of Formula (1a) and pharmaceutically acceptable salts, hydrates, geometrical isomers, racemates, tautomers, optical isomers and N-oxides thereof, wherein W1 and W3 are N and W and W4 are CR12, or W1 and W3 are CR12 and W2 and W4 are N. The invention also relates to pharmaceutical compositions comprising these compounds, and to the use of these compounds for the prophylaxis and treatment of medical conditions relating to disorders of the G-protein-coupled receptor GPR119, such as diabetes and obesity.

公开(公告)号：EP2059516A1

公开(公告)日：2009-05-20

申请号：EP07803008.7

申请日：2007-08-29

申请人： BIOVITRUM AB (publ)

发明人： BRANDT, Peter ,  EMOND, Rikard ,  JOHANSSON, Gary ,  JOHANSSON, Lars ,  KOOLMEISTER, Tobias ,  NILSSON, Björn, M. ,  SANDVALL, Teresa ,  WEBER, Michael

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  A61K31/4545 ,  A61K31/496 ,  A61P3/00

CPC分类号： A61K31/4545 ,  A61K31/496 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  A61K2300/00

摘要： The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, hydrates, geometrical isomers, racemates, tautomers, optical isomers and N-oxides thereof, wherein one of W1 and W2 is N and the other is CR12. The invention also relates to pharmaceutical compositions comprising these compounds, and to the use of these compounds for the prophylaxis and treatment of medical conditions relating to disorders of the G-protein-coupled receptor GPRl 19, such as diabetes and obesity.

公开(公告)号：EP2044051A1

公开(公告)日：2009-04-08

申请号：EP07786791.9

申请日：2007-06-21

申请人： BIOVITRUM AB (publ)

发明人： JENMALM JENSEN, Annika ,  RINGOM, Rune ,  MEDINA, Carmen ,  SHILVOCK, John ,  WIIK, Marie ,  KOOLMEISTER, Tobias ,  ANGBRANT, Johan ,  SUTIN, Lori ,  HENRIKSSON, Martin ,  SANDVALL, Teresa ,  JOHANSSON, Lars ,  NILSSON, Björn

IPC分类号： C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D471/04

CPC分类号： C07D401/12 ,  C07D401/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D471/04

摘要： The present invention relates to compounds of the general formula (I) wherein X, Y, Z, A, Ar, R1, R2, R3, and R4 are as defined herein, which compounds are inhibitors of MNK2 and MNK1. The invention also relates to the use of the compounds in therapy, pharmaceutical compositions comprising the compounds, and the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of disorders related to undesired activity of MNK1 and/or MNK2 kinases.