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公开(公告)号：EP3331878A1
公开(公告)日：2018-06-13
申请号：EP16751125.2
申请日：2016-08-05
申请人： Arnér, Elias, Set Jenö , The United States of America, as represented by The Secretary, Department of Health and Human Services
发明人： STAFFORD, William, Chester , COUSSENS, Nathan, Patrick , LUCI, Diane, Karen , MALONEY, David, Joseph , SIMEONOV, Anton , JADHAV, Ajit , DEXHEIMER, Thomas, S. , ARNÉR, Elias, Set Jenö
IPC分类号： C07D413/06 , A61K31/501 , A61P35/00
CPC分类号： C07D413/06
摘要： There is provided compounds of formula (I) or pharmaceutically-acceptable salts thereof, wherein W, X, Y, Z, R1, R2 and R3 have meanings provided in the description, which compounds are useful in the treatment of cancers.
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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.-
3.发明公开SMALL MOLECULE INHIBITORS OF LACTATE DEHYDROGENASE AND METHODS OF USE THEREOF 审中-公开乳酸脱氢酶的小分子抑制剂及其使用方法
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：EP4453236A1
公开(公告)日：2024-10-30
申请号：EP22854698.2
申请日：2022-12-21
发明人： RONZETTI, Michael H. , HENDERSON, Mark J. , SANCHEZ, Tino W. , MICHAEL, Samuel G. , VOSS, Ty C. , BALJINNYAM, Bolormaa , SIMEONOV, Anton
IPC分类号： C12Q1/66 , G01N33/58 , G01N33/68 , G01N33/542
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公开(公告)号：EP4192976A1
公开(公告)日：2023-06-14
申请号：EP21773171.0
申请日：2021-08-09
发明人： J. HENDERSON, Mark , RONZETTI, Michael H. , BALJINNYAM, Bolormaa , SANCHEZ, Tino W. , MICHAEL, Samuel G. , OWENS, Ashley E. , SIMEONOV, Anton
IPC分类号： C12Q1/66 , G01N33/542 , G01N33/58 , G01N33/68
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6.发明公开
公开(公告)号：EP4402165A1
公开(公告)日：2024-07-24
申请号：EP22782640.1
申请日：2022-09-09
发明人： FU, Ying , FLEMING, Bryan, D. , RENN, Alex , HALL, Matthew, D. , SIMEONOV, Anton
IPC分类号： C07K16/10
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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。
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公开(公告)号：EP3331858A1
公开(公告)日：2018-06-13
申请号：EP16759907.5
申请日：2016-08-05
申请人： Arnér, Elias, Set Jenö , The U.S.A. as represented by the Secretary, Department of Health and Human Services
发明人： STAFFORD, William, Chester , COUSSENS, Nathan, Patrick , LUCI, Diane, Karen , MALONEY, David, Joseph , SIMEONOV, Anton , JADHAV, Ajit , DEXHEIMER, Thomas, S. , ARNÉR, Elias Set Jenö
IPC分类号： C07D213/71 , A61P35/00 , A61K31/435
CPC分类号： C07D213/71
摘要： There is provided compounds of formula (I) or pharmaceutically-acceptable salts thereof, wherein L, R1, R2, R3, R4 and n have meanings provided in the description, which compounds are useful in the treatment of cancers.
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公开(公告)号：EP3331883A1
公开(公告)日：2018-06-13
申请号：EP16751126.0
申请日：2016-08-05
申请人： Arnér, Elias, Set Jenö , The U.S.A. as represented by the Secretary, Department of Health and Human Services
发明人： STAFFORD, William, Chester , COUSSENS, Nathan, Patrick , LUCI, Diane, Karen , MALONEY, David, Joseph , SIMEONOV, Anton , JADHAV, Ajit , DEXHEIMER, Thomas, S. , ARNÉR, Elias, Set Jenö
IPC分类号： C07D471/18 , A61K31/407 , A61P35/00
CPC分类号： C07D471/18
摘要： There is provided compounds of formula (I), or pharmaceutically-acceptable salts thereof, wherein X, Y, Z, R1 and R2 have meanings provided in the description, which compounds are useful in the treatment of cancers.
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