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

公开(公告)号：EP3074001A1

公开(公告)日：2016-10-05

申请号：EP14809235.6

申请日：2014-11-20

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

发明人： LIANG, Tsanyang Jake ,  FERRER, Marc ,  HE, Shanshan ,  HU, Xin ,  HU, Zongyi ,  MARUGAN, Juan Jose ,  SOUTHALL, Noel Terrence ,  XIAO, Jingbo ,  ZHENG, Wei

IPC分类号： A61K31/12 ,  A61K35/00 ,  A61K31/4468 ,  A61K31/4465 ,  A61K31/445 ,  A61K31/4995 ,  C07D243/08 ,  C07D295/073 ,  C07D295/088 ,  C07D295/096 ,  C07D295/185 ,  C07D209/48 ,  A61P31/12 ,  A61P35/00

CPC分类号： C07D405/10 ,  A61K31/4409 ,  A61K31/4465 ,  A61K31/4468 ,  A61K31/453 ,  A61K31/495 ,  A61K31/496 ,  A61K31/55 ,  A61K45/06 ,  C07D209/48 ,  C07D211/12 ,  C07D211/14 ,  C07D211/58 ,  C07D213/16 ,  C07D243/08 ,  C07D295/03 ,  C07D295/073 ,  C07D295/088 ,  C07D295/096 ,  C07D295/185 ,  C07D403/12

摘要： Disclosed are compounds of formula (I) (formula I),as antiviral agents, antineoplastic agents, pharmaceutical compositions comprising such compounds, and a method of use of these compounds, wherein X and Y are independently CH or N, o is 0, 1 or 2, and E is absent or is (CR
13 R
14 )m, NH, or S, F is absent or is (CR
15 R
16 )n, C=O, or -SO
2 -, G is absent or is (CR
17 CR
18 )r, H is absent or is C=O, or -SO
2 - and R
1 , Ar
1 , Ar
2 are as defined in the specification. These compounds are antiviral agents and are contemplated in the treatment of viral infections, for example, hepatitis C, or are antineoplastic agents.

摘要翻译： 本发明公开了式（I）（式I），作为抗病毒剂，抗肿瘤剂，药物组合物，包含检查化合物，和使用合成的化合物的方法，worin X和Y独立地是CH或N，o为0，1的化合物 或2，e是不存在或（CR 13 R 14）米，NH或S，R不存在或为（CR 15 R 16）N，C = O，或-SO 2 - ，G是不存在或为（CR17 CR18）R H是不存在或为C = O，-SO 2或 - 且R 1中，Ar 1中，Ar 2是如说明书中所定义。 这些化合物的抗病毒剂和病毒感染的治疗被预期，例如，丙型肝炎，或是抗肿瘤剂。

公开(公告)号：EP3154966A1

公开(公告)日：2017-04-19

申请号：EP15730666.3

申请日：2015-06-12

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

发明人： LIANG,Tsanyang ,  HU, Zongyi ,  MARUGAN, Juan Jose ,  SOUTHALL, Noel Terrence ,  HE, Shanshan ,  HU, Xin ,  XIAO, Jingbo ,  FERRER, Marc ,  ZHENG, Wei ,  FRANKOWSKI, Kevin J. ,  SCHOENEN, Frank J. ,  LI, Kelin

IPC分类号： C07D413/14 ,  C07D471/08 ,  A61K31/553 ,  A61P31/14

CPC分类号： C07D413/06 ,  A61K31/4178 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/7056 ,  A61K31/7068 ,  A61K38/07 ,  A61K38/13 ,  A61K38/212 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  Y02A50/385

摘要： Disclosed are compounds of formula (I), formula (II), and formula (III): wherein Ar, R1, A, and X are as defined in the specification. These compounds are antiviral agents and are contemplated for use in the treatment of viral infections, for example, hepatitis C. These compounds are also contemplated for use in treating or preventing cancers.

摘要翻译： 公开了式（I），式（II）和式（III）的化合物：其中Ar，R 1，A和X如说明书中所定义。 这些化合物是抗病毒剂，并且被考虑用于治疗病毒感染，例如丙型肝炎。这些化合物也被考虑用于治疗或预防癌症。

公开(公告)号：EP3154966B1

公开(公告)日：2019-05-08

申请号：EP15730666.3

申请日：2015-06-12

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

发明人： LIANG,Tsanyang ,  HU, Zongyi ,  MARUGAN, Juan Jose ,  SOUTHALL, Noel Terrence ,  HE, Shanshan ,  HU, Xin ,  XIAO, Jingbo ,  FERRER, Marc ,  ZHENG, Wei ,  FRANKOWSKI, Kevin J. ,  SCHOENEN, Frank J. ,  LI, Kelin

IPC分类号： C07D413/14 ,  C07D471/08 ,  A61K31/553 ,  A61P31/14

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：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.