公开(公告)号：US20150374697A1

公开(公告)日：2015-12-31

申请号：US14730707

申请日：2015-06-04

申请人： The United States of America, as Represented by the Secretary, Department of Health and Human Serv ,  The Rockefeller University ,  Icahn School of Medicine at Mount Sinai

发明人： Barry S. Coller ,  Craig Thomas ,  Marta Filizola ,  Joshua McCoy ,  Wenwei Huang ,  Min Shen

IPC分类号： A61K31/519 ,  A61K45/06

CPC分类号： A61K31/519 ,  A61K31/497 ,  A61K45/06 ,  C07D487/04 ,  C07D513/04 ,  A61K2300/00

摘要： The present invention relates to compounds and compositions useful for inhibiting and/or reducing platelet deposition, adhesion and/or aggregation. The present invention further relates to methods for the treatment or prophylaxis of thrombotic disorders, including stroke, myocardial infarction, unstable angina, peripheral vascular disease, abrupt closure following angioplasty or stent placement and thrombosis as a result of vascular surgery.

摘要翻译： 本发明涉及可用于抑制和/或减少血小板沉积，粘附和/或聚集的化合物和组合物。 本发明还涉及用于治疗或预防血栓形成障碍的方法，包括中风，心肌梗死，不稳定型心绞痛，外周血管疾病，血管成形术或支架放置后的突然闭合以及血管手术导致的血栓形成。

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：US09532989B2

公开(公告)日：2017-01-03

申请号：US14730707

申请日：2015-06-04

申请人： The United States of America, as Represented by the Secretary, Department of Health and Human Services ,  The Rockefeller University ,  Icahn School of Medicine at Mount Sinai

发明人： Barry S. Coller ,  Craig Thomas ,  Marta Filizola ,  Joshua McCoy ,  Wenwei Huang ,  Min Shen

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/04 ,  A61K31/497 ,  A61K45/06 ,  C07D513/04

CPC分类号： A61K31/519 ,  A61K31/497 ,  A61K45/06 ,  C07D487/04 ,  C07D513/04 ,  A61K2300/00

摘要： The present invention relates to compounds of Formula P-I where the variables (e.g. R1, Y, A, R1, Ra, Ra′, Rb, Rb′, Rc, Rc′, Rd, Rd′, Re, or Re′) and compositions useful for inhibiting and/or reducing platelet deposition, adhesion and/or aggregation. The present invention further relates to methods for the treatment or prophylaxis of thrombotic disorders, including stroke, myocardial infarction, unstable angina, peripheral vascular disease, abrupt closure following angioplasty or stent placement and thrombosis as a result of vascular surgery.

摘要翻译： 本发明涉及可用于抑制和/或减少血小板沉积，粘附和/或聚集的化合物和组合物。 本发明还涉及用于治疗或预防血栓形成障碍的方法，包括中风，心肌梗死，不稳定型心绞痛，外周血管疾病，血管成形术或支架放置后的突然闭合以及血管手术导致的血栓形成。

公开(公告)号：US09303044B2

公开(公告)日：2016-04-05

申请号：US14372488

申请日：2013-01-16

申请人： The Rockefeller University ,  The United States of America, as Represented by the Secretary, Department of Health and Human Services ,  Mount Sinai School of Medicine, Office of Technology and Business Development

发明人： Barry S. Coller ,  Craig Thomas ,  Marta Filizola ,  Joshua McCoy ,  Wenwei Huang ,  Min Shen ,  Jian-Kang Jiang

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00 ,  C07D513/04 ,  A61K45/06 ,  A61K31/436 ,  A61K31/337 ,  A61K31/4353 ,  A61K31/727 ,  A61L31/02 ,  A61L31/10 ,  A61L31/16

CPC分类号： C07D513/04 ,  A61K31/337 ,  A61K31/4353 ,  A61K31/436 ,  A61K31/519 ,  A61K31/727 ,  A61K45/06 ,  A61L31/022 ,  A61L31/10 ,  A61L31/16 ,  A61L2300/416 ,  A61L2300/42 ,  A61L2300/45 ,  A61K2300/00

摘要： The present invention relates to compounds and compositions of Formula P useful for inhibiting and/or reducing platelet deposition, adhesion and/or aggregation. The definitions of variables A, B, R2, R3, R4, Ra, Ra′, Rb, Rb′, Rc, Rd, Rd′, Re, and Re′ are provided in the disclosure. The present invention further relates to methods for the treatment or prophylaxis of thrombotic disorders, including stroke, myocardial infarction, unstable angina, peripheral vascular disease, abrupt closure following angioplasty or stent placement and thrombosis as a result of vascular surgery.

摘要翻译： 本发明涉及用于抑制和/或减少血小板沉积，粘附和/或聚集的式P化合物和组合物。 在本公开中提供了变量A，B，R2，R3，R4，Ra，Ra'，Rb，Rb'，Rc，Rd，Rd'，Re和Re'的定义。 本发明还涉及用于治疗或预防血栓形成障碍的方法，包括中风，心肌梗死，不稳定型心绞痛，外周血管疾病，血管成形术或支架放置后的突然闭合以及血管手术导致的血栓形成。

公开(公告)号：US20150050325A1

公开(公告)日：2015-02-19

申请号：US14372488

申请日：2013-01-16

申请人： The Rockefeller University ,  The United States, as Represented by the Secretary Department of Health and Human Services ,  Mount Sinai School of Medicine, Office of Technology and Business Development

发明人： Barry S. Coller ,  Craig Thomas ,  Marta Filizola ,  Joshua McCoy ,  Wenwei Huang ,  Min Shen ,  Jian-Kang Jiang

IPC分类号： C07D513/04 ,  A61K31/727 ,  A61L31/10 ,  A61L31/16 ,  A61L31/02 ,  A61K31/519 ,  A61K45/06

CPC分类号： C07D513/04 ,  A61K31/337 ,  A61K31/4353 ,  A61K31/436 ,  A61K31/519 ,  A61K31/727 ,  A61K45/06 ,  A61L31/022 ,  A61L31/10 ,  A61L31/16 ,  A61L2300/416 ,  A61L2300/42 ,  A61L2300/45 ,  A61K2300/00

摘要： The present invention relates to compounds and compositions useful for inhibiting and/or reducing platelet deposition, adhesion and/or aggregation. The present invention further relates to a drug-eluting stent comprising said compounds and methods for the treatment or prophylaxis of thrombotic disorders, including stroke, myocardial infarction, unstable angina, peripheral vascular disease, abrupt closure following angioplasty or stent placement and thrombosis as a result of vascular surgery.

摘要翻译： 本发明涉及可用于抑制和/或减少血小板沉积，粘附和/或聚集的化合物和组合物。 本发明还涉及包含所述化合物的药物洗脱支架和用于治疗或预防血栓形成障碍的方法，包括中风，心肌梗塞，不稳定型心绞痛，外周血管疾病，血管成形术或支架置入后突然闭合以及血栓形成 的血管手术。