公开(公告)号：EP2358684B8

公开(公告)日：2014-10-22

申请号：EP08876356.0

申请日：2008-10-20

申请人： The Government of the United States of America as represented by the Secretary of the Department of Health and Human Services ,  Forschungsverbund Berlin e.V.

发明人： GERSHENGORN, Marvin, C. ,  NEUMANN, Susanne ,  RAAKA, Bruce, M. ,  THOMAS, Craig, J. ,  INGLESE, James ,  SOUTHALL, Noel, T. ,  TITUS, Steven ,  ZHENG, Wei ,  HUANG, Wenwei ,  KRAUSE, Gerd ,  KLEINAU, Gunnar

IPC分类号： C07D401/06 ,  C07D405/06 ,  C07D239/91 ,  C07D487/04

CPC分类号： C07D405/06 ,  A61K31/517 ,  A61K49/0004 ,  A61K51/00 ,  C07D239/91 ,  C07D401/06 ,  C07D405/14 ,  C07D487/04

公开(公告)号：EP2018384A2

公开(公告)日：2009-01-28

申请号：EP07777162.4

申请日：2007-05-17

申请人： The Government of the United States of America as represented by the Secretary of the Department of Health and Human Services ,  Forschungsverbund Berlin E.V.

发明人： GERSHENGORN, Marvin, C. ,  NEUMANN, Susanne ,  THOMAS, Craig ,  JAESCHKE, Holger ,  MOORE, Susanna ,  KRAUSE, Gerd ,  RAAKA, Bruce ,  PASCHKE, Ralf ,  KLEINAU, Gunnar

IPC分类号： C07D495/04 ,  A61K31/519 ,  A61P5/06 ,  A61P5/08

CPC分类号： A61K31/519 ,  C07D495/04

摘要： Disclosed herein are small molecule modulators hormone receptors, including agonists and antagonists of luteinizing hormone/choriogonadotropin, follicle stimulating hormone and thyroid stimulating hormone receptors. Exemplary disclosed compounds include those of the formula wherein X is -S(O)nR5; n is 0, 1 or 2; Y is -OR6 or -NR7R8 R1 and R2 independently are selected from optionally substituted lower aliphatic, alkoxy, aralkyl, halogen, H and -OR5, wherein R5 is selected from lower alkyl, H, aralkyl, acyl, alkoxycarbonyl and aminocarbonyl; R3 and R4 independently are selected from acyl, alkoxycarbonyl, aminocarbonyl, aralkyl, H, lower alkyl and cycloalkyl; R5 is selected from lower alkyl, aralkyl, cycloalkyl and haloalkyl; R6 is selected from H, lower alkyl and aralkyl; R7 and R8 independently are selected from H, lower alkyl, aralkyl and cycloalkyl.

公开(公告)号：EP2358684A1

公开(公告)日：2011-08-24

申请号：EP08876356.0

申请日：2008-10-20

申请人： The Government of the United States of America as represented by the Secretary of the Department of Health and Human Services

发明人： GERSHENGORN, Marvin, C. ,  NEUMANN, Susanne ,  RAAKA, Bruce, M. ,  THOMAS, Craig, J. ,  INGLESE, James ,  SOUTHALL, Noel, T. ,  TITUS, Steven ,  ZHENG, Wei ,  HUANG, Wenwei ,  KRAUSE, Gerd ,  KLEINAU, Gunnar

IPC分类号： C07D235/18 ,  A61K31/4184

CPC分类号： C07D405/06 ,  A61K31/517 ,  A61K49/0004 ,  A61K51/00 ,  C07D239/91 ,  C07D401/06 ,  C07D405/14 ,  C07D487/04

摘要： Disclosed are oxo-hydroquinazolines that are useful as selective TSHR agonists. The compounds may be used for detecting or treating thyroid cancer, or treating a bone degenerative disorder.

公开(公告)号：EP2358684B1

公开(公告)日：2014-08-06

申请号：EP08876356.0

申请日：2008-10-20

申请人： The Government of the United States of America as represented by the Secretary of the Department of Health and Human Services

发明人： GERSHENGORN, Marvin, C. ,  NEUMANN, Susanne ,  RAAKA, Bruce, M. ,  THOMAS, Craig, J. ,  INGLESE, James ,  SOUTHALL, Noel, T. ,  TITUS, Steven ,  ZHENG, Wei ,  HUANG, Wenwei ,  KRAUSE, Gerd ,  KLEINAU, Gunnar

IPC分类号： C07D401/06 ,  C07D405/06 ,  C07D239/91 ,  C07D487/04

CPC分类号： C07D405/06 ,  A61K31/517 ,  A61K49/0004 ,  A61K51/00 ,  C07D239/91 ,  C07D401/06 ,  C07D405/14 ,  C07D487/04