公开(公告)号：EP3458052A1

公开(公告)日：2019-03-27

申请号：EP17726573.3

申请日：2017-05-17

申请人： Scandion Oncology A/S

发明人： BRÜNNER, Nils, Aage ,  CHRISTOPHERSEN, Palle ,  STENVANG, Jan ,  LICHTENBERG, Jens ,  THOUGAARD, Annemette

IPC分类号： A61K31/4245 ,  C07D271/07 ,  A61P35/00

摘要： The present invention relates to treatment of cancer, in particular to methods of sensitising cancer cells to an anti-cancer therapy by administering an effective amount of a modulator of Volume Regulated Anion Channels, i.e. a VRAC modulator.

公开(公告)号：EP3153498A1

公开(公告)日：2017-04-12

申请号：EP15803170.8

申请日：2015-01-06

申请人： ABA Chemicals Corporation

发明人： LIN, Zhigang ,  LIU, Yanqin ,  XU, Jun ,  JIANG, Yueheng ,  CAI, Tong

IPC分类号： C07C255/58 ,  C07C253/30 ,  C07D271/07

CPC分类号： C07C253/30 ,  C07C255/58 ,  C07D271/07

摘要： Disclosed is an N-substituted phenyl glycine (dabigatran etexilate intermediate) preparation method unreported in any document, the method comprising: utilizing cheap and easily available substituted aniline (1) as raw material to condense with glyoxylic acid to form an imine, while conducting hydrogenation reduction to obtain N-(substituted phenyl) glycine. The synthetic route is not reported in any document, and the raw material is cheap and easily available; in addition, the present invention has simple unit operation and low device requirement, and is suitable for large-scale industrial production.

摘要翻译： 公开了任何文献中没有报道的N-取代苯基甘氨酸（达比加群酯中间体）的制备方法，该方法包括：使用便宜且容易获得的取代苯胺（1）作为原料与乙醛酸缩合形成亚胺，同时进行氢化 还原得到N-（取代苯基）甘氨酸。 合成路线不在任何文件中报道，原材料便宜且易于获得; 另外本发明的单元操作简单，装置要求低，适用于大规模的工业化生产。

公开(公告)号：EP3119774A1

公开(公告)日：2017-01-25

申请号：EP15711117.0

申请日：2015-03-17

申请人： reMYND NV

发明人： GRIFFIOEN, Gerard ,  DE TAEYE, Bart ,  PRINCEN, Katrien ,  DE WITTE, Koen ,  BLANCHE, Emilie ,  RATNI, Hasane ,  NETTEKOVEN, Matthias ,  ROGERS-EVANS, Mark

IPC分类号： C07D413/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D271/07 ,  A61K31/496 ,  A61K31/438 ,  A61P25/00 ,  A61P3/00 ,  A61P9/00

CPC分类号： C07D271/07 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D471/10

摘要： The present invention relates to a compound of formula (I) or (II) or a stereoisomer, enantiomer, racemic, or tautomer thereof, (I) (II) wherein R
1 ,R
2 ,R
3 ,L
1 ,L
2 ,L
3 ,L
4 ,L
5 and n, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of metabolic disorders and/or neurodegenerative diseases, and/or protein misfolding disorders.

摘要翻译： 本发明涉及式（I）或（II）化合物或其立体异构体，对映体，外消旋或互变异构体，（I）（II）其中R1，R2，R3，L1，L2，L3，L4，L5 和n具有与权利要求和说明书中所定义的相同的含义。 本发明还涉及包含这些化合物的组合物，特别是药物，以及这些化合物和组合物用于预防和/或治疗代谢紊乱和/或神经变性疾病和/或蛋白质错误折叠障碍的用途。

公开(公告)号：EP3083572A1

公开(公告)日：2016-10-26

申请号：EP14821571.8

申请日：2014-12-16

申请人： Novassay SA

发明人： MEGHANI, Premji ,  KRICEK, Franz

IPC分类号： C07D257/04 ,  C07D271/07 ,  C07C255/07 ,  C07C205/02 ,  A61K31/4245 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  A61P25/22

CPC分类号： A61K31/41 ,  A61K31/4245 ,  C07B2200/07 ,  C07C205/50 ,  C07C233/10 ,  C07C255/31 ,  C07C259/14 ,  C07C2602/20 ,  C07D257/04 ,  C07D271/07

摘要： Processes to prepare said compounds and novel intermediates are also claimed. Such compound finds utility in treating neuropathic pain and disorders of the central nervous system.

摘要翻译： 还要求保护所述化合物和新型中间体的方法。 这种化合物可用于治疗神经性疼痛和中枢神经系统疾病。

公开(公告)号：EP2694470B1

公开(公告)日：2016-06-01

申请号：EP12723970.5

申请日：2012-04-04

申请人： The Medical College of Wisconsin, Inc. ,  The Board of Regents of The University of Texas System

发明人： IMIG, John, David ,  CAMPBELL, William, B. ,  FALCK, John, Russell

IPC分类号： C07C309/15 ,  C07C311/18 ,  C07D271/06 ,  C07D271/07 ,  C07D277/34 ,  C07D277/82 ,  C07D285/08 ,  C07D291/04 ,  C07D257/04

CPC分类号： C07F9/40 ,  C07C233/46 ,  C07C233/47 ,  C07C233/56 ,  C07C237/22 ,  C07C275/20 ,  C07C309/15 ,  C07C311/18 ,  C07C311/19 ,  C07C311/51 ,  C07C317/28 ,  C07C323/44 ,  C07D249/12 ,  C07D257/04 ,  C07D271/06 ,  C07D271/07 ,  C07D277/34 ,  C07D277/593 ,  C07D277/82 ,  C07D285/08 ,  C07D291/04

公开(公告)号：EP1622613A4

公开(公告)日：2008-04-02

申请号：EP04775981

申请日：2004-05-12

申请人： CYTOKINETICS INC

发明人： QIAN XIANGPING ,  ZHOU HAN-JIE ,  BERGNES GUSTAVE

IPC分类号： C07D271/06 ,  A61K20060101 ,  A61K31/4245 ,  C07D271/07

CPC分类号： C07D271/07

公开(公告)号：EP1817305A2

公开(公告)日：2007-08-15

申请号：EP05850799.7

申请日：2005-11-16

申请人： Neurochem (International) Limited

发明人： KONG, Xianqi ,  WU, Xinfu ,  VALADE, Isabelle ,  GERVAIS, Francine

IPC分类号： C07D401/12 ,  C07D233/42 ,  C07D215/12 ,  C07D233/54 ,  C07D235/04 ,  C07D257/04 ,  C07D263/30 ,  C07D271/07 ,  C07D295/04 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D413/12 ,  C07D487/04

CPC分类号： C07D401/12 ,  C07D233/84 ,  C07D239/47 ,  C07D239/56 ,  C07D249/12 ,  C07D257/04 ,  C07D271/113 ,  C07D401/04 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04

摘要： Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing CNS and amyloid associated disease. Also described are methods, compounds, pharmaceutical compositions and kits for detecting, diagnosing, monitoring and treating or preventing CNS and amyloid associated disease Pn particular, modified blood bram barrier (BBB) vectors such as phenylalanine derivatives are described as to provide parameters to select CNS drug candidates designated to penetrate the bram using a specific active transporter.

公开(公告)号：EP1603890A1

公开(公告)日：2005-12-14

申请号：EP04713604.9

申请日：2004-02-23

申请人： Warner-Lambert Company LLC

发明人： BARTA, Nancy Sue,Pfizer Global Res.and Dev. ,  COLBRY, Norman Lloyd,Pfizer Global Res.and Dev. ,  HUDACK, Raymond Andrew Jr.,Pfizer Global Res.&Dev ,  LIN, Kristin Knapp,Pfizer Global Res.and Dev. ,  .SCHWARZ, Jacob Bradley,Pfizer Global Res.andDev. ,  THORPE, Andrew John,Pfizer Global Res.and Dev. ,  WUSTROW, David Juergen,Pfizer Global Res.and Dev. ,  ZHU, Zhijian,Pfizer Global Res.and Development

IPC分类号： C07D271/07 ,  C07D257/04 ,  A61K31/4245 ,  A61K31/41

CPC分类号： C07D257/04 ,  C07D271/07

摘要： This invention relates to novel tetrazole and oxadiazalone β-amino acids derivatives of the formula (I, II), wherein G is (III, IV) wherein R1 through R4 are defined as in the specification, pharmaceutical compositions containing them and their use for the treatment of various central nervous system and other disorders. The cyclopropyl β-amino acids derivatives of this invention exhibit activity as alpha2delta ligands (α2δ ligands). Such compounds have affinity for the α2δ subunit of a calcium channel.

公开(公告)号：EP1377559A4

公开(公告)日：2005-09-28

申请号：EP02723389

申请日：2002-03-08

申请人： INCYTE SAN DIEGO INC

发明人： PFAHL MAGNUS ,  TACHDJIAN CATHERINE ,  AL-SHAMMA HUSSIEN A ,  FANJUL ANDREA ,  PLEYNET DAVID P M ,  SPRUCE LYLE W ,  FINE RICHARD ,  ZAPF JAMES W ,  GUO JIANHUA ,  JAKUBOWICZ-JAILLARDON KARINE

IPC分类号： A61K31/4245 ,  A61K31/426 ,  A61K31/454 ,  A61K45/00 ,  A61P1/00 ,  A61P3/06 ,  A61P3/10 ,  A61P7/12 ,  A61P9/10 ,  A61P11/00 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  C07D271/06 ,  C07D271/07 ,  C07D277/20 ,  C07D277/34 ,  C07D277/36 ,  C07D417/10 ,  A61K31/4166

CPC分类号： C07D271/07 ,  C07D277/20 ,  C07D417/10

公开(公告)号：EP1565429A2

公开(公告)日：2005-08-24

申请号：EP03770917.7

申请日：2003-11-10

申请人： NEUROSEARCH A/S

发明人： VALGEIRSSON, Jon ,  NIELSEN, Elsebet Ostergaard,c/o Neurosearch A/S ,  PETERS, Dan,c/o Neurosearch A/S

IPC分类号： C07C275/42 ,  C07C309/46 ,  C07D209/40 ,  C07D213/72 ,  C07D231/56 ,  C07D257/04 ,  C07D271/07 ,  C07D333/36 ,  A61K31/17 ,  A61K31/19 ,  A61K31/381 ,  A61K31/416 ,  A61K31/4245 ,  A61K31/44

CPC分类号： C07D213/75 ,  C07C275/42 ,  C07C309/51 ,  C07C2603/18 ,  C07D209/40 ,  C07D231/56 ,  C07D257/04 ,  C07D271/07 ,  C07D317/66 ,  C07D333/36

摘要： This invention relates to novel aryl ureido benzoic acid derivatives useful as selective and non-competitive antagonists of the ionotropic GluR5 receptor. Due to their biological activity, the aryl ureido derivatives of the invention are considered useful for treating diseases that are responsive to modulation of an aspartate or a glutamate receptor. Moreover the invention provides chemical compounds for use according to the invention, as well as pharmaceutical compositions comprising the chemical compounds, and methods of treating diseases or disorders or conditions responsive to modulation of an aspartate or a glutamate receptor.