公开(公告)号：EP2563777A2

公开(公告)日：2013-03-06

申请号：EP11766807.9

申请日：2011-04-08

申请人： The U.S.A. as represented by the Secretary, Department of Health and Human Services

发明人： GERSHENGORN, Marvin ,  NEUMANN, Susanne ,  HUANG, Wenwei ,  THOMAS, Craig, J.

IPC分类号： C07D405/06 ,  C07D401/06 ,  C07D239/91 ,  A61K31/517 ,  A61P35/00

CPC分类号： C07D401/06 ,  A61K31/517 ,  C07D239/91 ,  C07D405/06

摘要： TSHR inverse agonists and neutral antagonists that are useful for treating Graves' orbitopathy, Graves' hyperthyroidism and/or thyroid cancer.

公开(公告)号：EP2563761A1

公开(公告)日：2013-03-06

申请号：EP11730473.3

申请日：2011-04-26

申请人： The U.S.A. as represented by the Secretary, Department of Health and Human Services

发明人： BOXER, Matthew, B. ,  SHEN, Min ,  AULD, Douglas, S. ,  THOMAS, Craig, J. ,  WALSH, Martin, J.

IPC分类号： C07D209/30 ,  C07D215/36 ,  C07D223/16 ,  C07D265/36 ,  A61K31/404 ,  A61K31/4704 ,  A61K31/538 ,  A61K31/55 ,  A61P35/00

CPC分类号： C07D215/227 ,  C07D209/12 ,  C07D209/30 ,  C07D209/34 ,  C07D215/36 ,  C07D223/16 ,  C07D235/26 ,  C07D265/36

摘要： Disclosed are pyruvate kinase M2 activators which are compounds of Formula (I), including those of Formula (II), wherein A1, A2, L, R, R1 to R3, X1 to X3, k, n, and m are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer. A1-NR-L-A2 (I).

公开(公告)号：EP2310378A2

公开(公告)日：2011-04-20

申请号：EP09791490.7

申请日：2009-08-13

申请人： The U.S.A. As Represented By The Secretary, Department Of Health And Human Services ,  Illinois State University

发明人： THOMAS, Craig, J. ,  MALONEY, David, J. ,  BANTUKALLU, Ganesha, Rai ,  SAYED, Ahmed, A. ,  SIMEONOV, Anton ,  WILLIAMS, David, L.

IPC分类号： C07D271/08 ,  C07D413/04 ,  A61K31/4245 ,  A61P33/12

CPC分类号： C07D271/08 ,  C07D413/04

摘要： The invention provides 1,2,5-oxadiazole-containing compounds of Formula (I), wherein R
1 , A, and R
2 are as defined herein, that are useful in treating schistosomiasis. The invention also provides a composition comprising a pharmaceutically suitable carrier and at least one compound of the invention, and a method of of treating schistosomiasis in a mammal.

公开(公告)号：EP2231669A1

公开(公告)日：2010-09-29

申请号：EP09701318.9

申请日：2009-01-08

申请人： The U.S.A. As Represented By The Secretary, Department Of Health And Human Services

发明人： THOMAS, Craig, J. ,  XIA, Menghang ,  SKOUMBOURDIS, Amanda, P. ,  LECLAIRE, Christopher, A. ,  WALSH, Marty ,  HUANG, Ruili

IPC分类号： C07D487/04 ,  C07D513/04 ,  A61K31/549 ,  A61P11/06

CPC分类号： C07D513/04 ,  C07D487/04

摘要： The invention relates to compounds of formula I useful for inhibiting phosphodiesterase-4.