公开(公告)号：EP2970311A2

公开(公告)日：2016-01-20

申请号：EP14775808.0

申请日：2014-03-13

申请人： The Brigham and Women's Hospital, Inc. ,  The U.S.A. as represented by the Secretary, Department of Health and Human Services

发明人： ALIMARDANOV, Asaf ,  CUNY, Gregory, D. ,  GREWAL, Gurmit, Singh ,  LEE, Arthur ,  MCKEW, John, C. ,  MOHEDAS, Agustin, H. ,  SHEN, Min ,  XU, Xin ,  YU, Paul, B.

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61P9/10 ,  A61P35/00 ,  A61P31/10 ,  A61P27/00 ,  A61P29/00 ,  A61P33/00 ,  A61P31/04 ,  A61P31/12 ,  A61P5/30

CPC分类号： C07D487/04 ,  C07D519/00

摘要： The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds may also be used to reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.

摘要翻译： 本发明提供了BMP信号传导的小分子抑制剂。 这些化合物可用于调节细胞生长，分化，增殖和凋亡，因此可用于治疗与BMP信号传导相关的疾病或病症，包括炎症，心血管疾病，血液病，癌症和骨疾病，以及 用于调节细胞分化和/或增殖。 这些化合物还可用于降低ApoB-100或LDL的循环水平，并治疗或预防获得性或先天性高胆固醇血症或高脂蛋白血症; 与脂质吸收或代谢缺陷相关的疾病，病症或综合征; 或由高脂血症引起的疾病，病症或综合征。

公开(公告)号：EP2451779A2

公开(公告)日：2012-05-16

申请号：EP10797846.2

申请日：2010-07-08

申请人： The General Hospital Corporation ,  The Brigham and Women's Hospital, Inc.

发明人： RAINES, Douglas E. ,  FORMAN, Stuart, A. ,  MILLER, Keith, W. ,  HUSAIN, Syed, S. ,  CUNY, Gregory, D. ,  COTTON, Joseph F.

IPC分类号： C07D207/333 ,  C07D233/64 ,  A61K31/4164 ,  A61P5/38 ,  A61P25/00

CPC分类号： C07D207/34 ,  A61K31/40

摘要： The invention is directed to compounds according to formula (I): where R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0 to 5; each R3 is independently halogen or R2; R4 and R5 are independently H, halogen, CN or CF3; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene; and T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.

公开(公告)号：EP3154547A1

公开(公告)日：2017-04-19

申请号：EP15806816.3

申请日：2015-06-15

申请人： Yuma Therapeutics, Inc. ,  The Brigham and Women's Hospital, Inc.

发明人： CUNY, Gregory, D. ,  GLICKSMAN, Marcie, A. ,  HODGETTS, Kevin, J. ,  MATHIEU, Steven, L. ,  PERRELLA, Yukari, Y. ,  DARMENCY, Vincent ,  LUSIC, Hrvoje

IPC分类号： A61K31/505

CPC分类号： C07D495/04 ,  C07D239/42 ,  C07D239/70 ,  C07D239/84 ,  C07D251/16 ,  C07D251/22 ,  C07D405/04 ,  C07D405/10 ,  C07D471/04 ,  C07D487/04

摘要： The present invention relates to 2-amino-4-arylpyrimidine and 2-amino-4-aryltriazine compounds as inhibitors of heat shock protein 90 family of chaperone proteins. The invention also features pharmaceutical compositions and kits that include the compounds and compositions of the invention. The invention further relates to the medical use of these compounds and compositions for the treatment of a disorder in a subject. For example, the disorder is a neurodegenerative disease.

摘要翻译： 本发明涉及2-氨基-4-芳基嘧啶和2-氨基-4-芳基三嗪化合物作为伴侣蛋白的热休克蛋白90家族的抑制剂。 本发明还包括药物组合物和试剂盒，其包括本发明的化合物和组合物。 本发明还涉及这些化合物和组合物用于治疗受试者中的病症的医学用途。 例如，该疾病是神经变性疾病。

公开(公告)号：EP3034494A1

公开(公告)日：2016-06-22

申请号：EP15002668.0

申请日：2008-08-15

申请人： President and Fellows of Harvard College ,  The Brigham and Women's Hospital, Inc. ,  Trustees of Boston University ,  TUFTS UNIVERSITY

发明人： CUNY, Gregory, D. ,  TENG, Xin ,  YUAN, Junying ,  DEGTEREV, Alexei ,  PORCO, John, A., Jr.,

IPC分类号： C07D207/34 ,  A61K31/41 ,  A61P25/28

CPC分类号： C07D417/12 ,  C07D207/34 ,  C07D231/14 ,  C07D241/24 ,  C07D263/34 ,  C07D277/56 ,  C07D285/06 ,  C07D307/68 ,  C07D307/84 ,  C07D333/38

摘要： The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-α) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-α induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.

摘要翻译： 本发明特征在于一系列抑制肿瘤坏死因子α（TNF-α）诱导的人工坏死的杂环衍生物。 本发明的杂环化合物由式（I）和（Ia） - （Ie）描述，并且显示出抑制人Jurkat T细胞的FADD缺陷型变体中的TNF-诱导的人工死亡。 本发明还涉及以本发明化合物为特征的药物组合物。 本发明的化合物和组合物还可以用于治疗其中棘球菌根可能发挥重要作用的病症。

公开(公告)号：EP2964651A1

公开(公告)日：2016-01-13

申请号：EP14760191.8

申请日：2014-03-04

申请人： The Brigham and Women's Hospital, Inc. ,  The General Hospital Corporation

发明人： YU, Paul, B. ,  CUNY, Gregory, D. ,  MOHEDAS, Agustin, H. ,  BLOCH, Kenneth, D. ,  PETERSON, Randall, T.

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P9/00

CPC分类号： C07D487/04

摘要： The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds may also be used to reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.

公开(公告)号：EP2265603B1

公开(公告)日：2014-05-07

申请号：EP09720039.8

申请日：2009-03-13

申请人： The General Hospital Corporation ,  The Brigham and Women's Hospital, Inc.

发明人： YU, Paul, B. ,  CUNY, Gregory, D. ,  BLOCH, Kenneth, D. ,  PETERSON, Randall, T. ,  HONG, Charles, C.

IPC分类号： C07D403/04 ,  C07D403/02 ,  C07D487/04 ,  C07D487/02

CPC分类号： C07D487/04 ,  A61K31/519

公开(公告)号：EP2265603A1

公开(公告)日：2010-12-29

申请号：EP09720039.8

申请日：2009-03-13

申请人： The General Hospital Corporation ,  The Brigham and Women's Hospital, Inc.

发明人： YU, Paul, B. ,  CUNY, Gregory, D. ,  BLOCH, Kenneth, D. ,  PETERSON, Randall, T. ,  HONG, Charles, C.

IPC分类号： C07D403/04 ,  C07D403/02 ,  C07D487/04 ,  C07D487/02

CPC分类号： C07D487/04 ,  A61K31/519

摘要： The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation.

公开(公告)号：EP1968583A2

公开(公告)日：2008-09-17

申请号：EP06847822.1

申请日：2006-12-20

申请人： President and Fellows of Harvard College ,  The Brigham and Women's Hospital, Inc.

发明人： YUAN, Junying ,  DEGTEREV, Alexei ,  HITOMI, Junichi ,  CUNY, Gregory, D. ,  JAGTAP, Prakash

IPC分类号： A61K31/4178

CPC分类号： C07D231/54 ,  A61K31/4178 ,  C07D403/06 ,  C07D491/052 ,  C07D495/04 ,  Y02A50/475

摘要： The present invention features compounds, pharmaceutical compositions, and methods for treating trauma, ischemia, stroke, degenerative diseases associated with cellular necrosis, and other conditions. Screening assays for identifying compounds useful for treating these conditions are also described.

公开(公告)号：EP3122355A1

公开(公告)日：2017-02-01

申请号：EP15768638.7

申请日：2015-03-25

申请人： The Brigham and Women's Hospital, Inc.

发明人： YU, Paul, B. ,  CUNY, Gregory, D. ,  MOHEDAS, Agustin, H.

IPC分类号： A61K31/43 ,  A61K31/44 ,  A61P1/00 ,  A61P17/00 ,  A61P19/00 ,  C07D213/73 ,  C07D401/04 ,  C07D401/10 ,  C07D413/10 ,  C07D417/14 ,  C07D495/04

CPC分类号： C07D487/04 ,  C07D213/38 ,  C07D213/61 ,  C07D213/64 ,  C07D213/73 ,  C07D213/74 ,  C07D401/04 ,  C07D405/04

摘要： The present invention provides small molecule inhibitors of BMP signaling and compositions and methods for inhibiting BMP signaling. These compounds and compositions may be used to modulate cell growth, di.fferentia.tion, proliferation, and apoptosis, and thus may be useful tor treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds and compositions may also be used to reduce circulating levels of ApoB- 100 or LDL and treat or prevent acquired or congenital, hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.

摘要翻译： 本发明提供了BMP信号的小分子抑制剂以及用于抑制BMP信号传导的组合物和方法。 这些化合物和组合物可用于调节细胞生长，异常，增殖和凋亡，因此可用于治疗与BMP信号相关的疾病或病症，包括炎症，心血管疾病，血液病，癌症和 骨骼疾病，以及调节细胞分化和/或增殖。 这些化合物和组合物也可用于降低ApoB-100或LDL的循环水平并治疗或预防获得性或先天性高胆固醇血症或高脂蛋白血症; 与脂质吸收或代谢缺陷相关的疾病，病症或综合征; 或由高脂血症引起的疾病，病症或综合征。

公开(公告)号：EP2451779B1

公开(公告)日：2014-09-03

申请号：EP10797846.2

申请日：2010-07-08

申请人： The General Hospital Corporation ,  The Brigham and Women's Hospital, Inc.

发明人： RAINES, Douglas E. ,  FORMAN, Stuart, A. ,  MILLER, Keith, W. ,  HUSAIN, Syed, S. ,  CUNY, Gregory, D. ,  COTTON, Joseph F.

IPC分类号： C07D207/34 ,  A61K31/40 ,  A61P25/00 ,  A61P5/38

CPC分类号： C07D207/34 ,  A61K31/40