公开(公告)号：US20160199370A1

公开(公告)日：2016-07-14

申请号：US15076258

申请日：2016-03-21

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

发明人： Craig J. Thomas ,  Douglas S. Auld ,  James Inglese ,  Amanda P. Skoumbourdis ,  Jian-Kang Jiang ,  Matthew B. Boxer

IPC分类号： A61K31/496 ,  A61K31/445 ,  A61K31/495

CPC分类号： A61K31/496 ,  A61K31/445 ,  A61K31/495 ,  A61K31/5025 ,  C07D295/26 ,  C07D319/18 ,  C07D495/14

摘要： Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia,

摘要翻译： 公开了丙酮酸激酶M2活化剂，其为式（I）的双磺酰胺哌嗪基化合物和2,4-二取代的4H-噻吩并[3,2-b]吡咯-2-（取代的苄基）哒嗪-3（2H） 式（II）的化合物，其中L和R 1至R 16如本文所定义，其可用于治疗可通过PKM2的活化治疗的许多疾病，例如癌症和贫血，

公开(公告)号：US20150183744A1

公开(公告)日：2015-07-02

申请号：US14643107

申请日：2015-03-10

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

发明人： Matthew B. Boxer ,  Min Shen ,  Douglas S. Auld ,  Craig J. Thomas ,  Martin J. Walsh

IPC分类号： C07D215/227

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)

摘要翻译： 公开了作为式（I）化合物的丙酮酸激酶M2活化剂，包括式（II）的化合物，其中A1，A2，L，R，R1至R3，X1至X3，k，n和m如本文所定义 ，其可用于治疗可通过激活PKM2（例如癌症）治疗的许多疾病。 A1-NR-L-A2（I）

公开(公告)号：US20150105395A1

公开(公告)日：2015-04-16

申请号：US14576333

申请日：2014-12-19

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

发明人： Craig J. Thomas ,  Douglas S. Auld ,  James Inglese ,  Amanda P. Skoumbourdis ,  Jian-Kang Jiang ,  Matthew B. Boxer

IPC分类号： C07D495/14

CPC分类号： A61K31/496 ,  A61K31/445 ,  A61K31/495 ,  A61K31/5025 ,  C07D295/26 ,  C07D319/18 ,  C07D495/14

摘要： Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia, Formulas (I); (II).

摘要翻译： 公开了丙酮酸激酶M2活化剂，其为式（I）的双磺酰胺哌嗪基化合物和2,4-二取代的4H-噻吩并[3,2-b]吡咯-2-（取代的苄基）哒嗪-3（2H） 式（II）的化合物，其中L和R 1至R 16如本文所定义，其可用于治疗可通过PKM2的活化治疗的许多疾病，例如癌症和贫血，式（I）; （二）。