公开(公告)号：EP3240785A2

公开(公告)日：2017-11-08

申请号：EP15839113.6

申请日：2015-12-29

申请人： The United States of America, as represented by The Secretary, Department of Health and Human Services ,  Vanderbilt University ,  The Trustees of The University of Pennsylvania ,  The UAB Research Foundation

发明人： MALONEY, David J. ,  JADHAV, Ajit ,  BANTUKALLU, Ganesha Rai ,  BRIMACOMBE, Kyle Ryan ,  MOTT, Bryan T. ,  YANG, Shyh Ming ,  URBAN, Daniel Jason ,  HU, Xin ,  SIMEONOV, Anton ,  KOUZNETSOVA, Jennifer L. ,  WATERSON, Alex Gregory ,  SULIKOWSKI, Gary Allen ,  KIM, Kwangho ,  CHRISTOV, Plamen ,  JANA, Somnath ,  DARLEY-USMAR, Victor M. ,  NECKERS, Leonard M. ,  MOORE, William J. ,  DANG, Chi V.

IPC分类号： C07D417/04 ,  C07D403/04 ,  C07D417/14 ,  A61K31/427 ,  A61K31/4427 ,  A61P35/00

CPC分类号： C07D417/04 ,  C07D403/04 ,  C07D417/14

摘要： Provided is a compound of formula (I)[Formula (I) should be inserted here], in which Ar
1 , R
1 , U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/ or lactate dehydrogenase B (LDHB) activity in a cell.

公开(公告)号：EP3954685A1

公开(公告)日：2022-02-16

申请号：EP21181777.0

申请日：2015-12-29

申请人： The United States Of America, As Represented By The Secretary, Department Of Health And Human Services ,  Vanderbilt University ,  The Trustees of The University of Pennsylvania ,  The UAB Research Foundation

发明人： MALONEY, David J. ,  JADHAV, Ajit ,  BANTUKALLU, Ganesha Rai ,  BRIMACOMBE, Kyle Ryan ,  MOTT, Bryan T. ,  YANG, Shyh Ming ,  URBAN, Daniel Jason ,  HU, Xin ,  SIMEONOV, Anton ,  KOUZNETSOVA, Jennifer L. ,  WATERSON, Alex Gregory ,  SULIKOWSKI, Gary Allen ,  KIM, Kwangho ,  CHRISTOV, Plamen ,  JANA, Somnath ,  DARLEY-USMAR, Victor M. ,  NECKERS, Leonard M. ,  MOORE, William J. ,  DANG, Chi V.

IPC分类号： C07D417/04 ,  C07D403/04 ,  C07D417/14 ,  A61K31/427 ,  A61K31/4427 ,  A61P35/00

摘要： Provided is a compound of formula (I)

in which Ar 1 , R 1 , U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/ or lactate dehydrogenase B (LDHB) activity in a cell.

公开(公告)号：EP3237385A1

公开(公告)日：2017-11-01

申请号：EP15823901.2

申请日：2015-12-22

申请人： The United States of America, as represented by The Secretary, Department of Health and Human Services ,  The University of North Carolina at Chapel Hill

发明人： BOXER, Matthew Brian ,  ROHDE, Jason Matthew ,  PRAGANI, Rajan ,  LIU, Li ,  DAVIS, Mindy Irene Emily ,  BRIMACOMBE, Kyle Ryan ,  SHEN, Min ,  SIMEONOV, Anton ,  KARAVADHI, Surendra ,  URBAN, Daniel Jason ,  JADHAV, Ajit ,  WANG, Xiaodong ,  MCIVER, Andrew Louis

IPC分类号： C07D215/22 ,  C07D401/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  A61K31/4545 ,  A61K31/4436 ,  A61K31/4704 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/55 ,  A61P35/00

CPC分类号： C07D471/04 ,  C07D215/22 ,  C07D215/54 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/14 ,  C07D487/08 ,  C07D487/10 ,  C07D491/052 ,  C07D491/107

摘要： Compounds of Formula I and Formula II and the pharmaceutically acceptable salts thereof are disclosed The variables A, B, Y, Z, X
1 , X
2 , R
1-4 and R
13-18 are disclosed herein. The compounds are useful for treating cancer disorders, especially those involving mutant IDH1 enzymes. Pharmaceutical compositions containing compounds of Formula I or Formula II and methods of treatment comprising administering compounds of Formula I and Formula II are also disclosed.

摘要翻译： 式I和式II化合物及其药学上可接受的盐公开于此。变量A，B，Y，Z，X 1，X 2，R 1-4和R 13-18在本文中公开。 这些化合物可用于治疗癌症疾病，尤其是那些涉及突变IDH1酶的疾病。 还公开了含有式I或式II化合物的药物组合物和包含给予式I和式II化合物的治疗方法。

公开(公告)号：EP3478677A1

公开(公告)日：2019-05-08

申请号：EP17737708.2

申请日：2017-06-29

申请人： The U.S.A. as represented by the Secretary, Department of Health and Human Services ,  Vanderbilt University ,  The UAB Research Foundation ,  The Trustees of The University of Pennsylvania

发明人： MALONEY, David J. ,  WATERSON, Alex Gregory ,  BANTUKALLU, Ganesha Rai ,  BRIMACOMBE, Kyle Ryan ,  CHRISTOV, Plamen ,  DANG, Chi V. ,  DARLEY-USMAR, Victor M. ,  HALL, Matthew ,  HU, Xin ,  JADHAV, Ajit ,  JANA, Somnath ,  KIM, Kwangho ,  MOORE, William J. ,  MOTT, Brian T. ,  NECKERS, Leonard M. ,  SIMEONOV, Anton ,  SULIKOWSKI, Gary Allen ,  URBAN, Daniel Jason ,  YANG, Shyh Ming

IPC分类号： C07D417/04 ,  C07D417/14 ,  A61K31/427 ,  A61P35/00 ,  A61P11/00