公开(公告)号：EP2791113A1

公开(公告)日：2014-10-22

申请号：EP12813630.6

申请日：2012-12-13

申请人： GE Healthcare Limited

发明人： JONES, Clare ,  GLASER, Matthias Eberhard ,  WYNN, Duncan ,  NAIRNE, James ,  MOKKAPATI, Umamaheshwar P. ,  NEWINGTON, Ian, Martin ,  RANGASWAMY, Chitralekha ,  JOSE, Jinto ,  JOHANSSON, Saga

IPC分类号： C07D213/74 ,  C07D237/24 ,  C07D495/04 ,  C07C243/22 ,  A61K31/5025 ,  A61P25/00

CPC分类号： A61K51/0459 ,  A61K49/0052 ,  C07B59/002 ,  C07D213/74 ,  C07D237/24 ,  C07D495/04 ,  G01N33/6896 ,  G01N2800/2821

摘要： Pyridazinone compounds of Formula I: (I) wherein: R' is alkyl or Ar, optionally substituted with at least one alkyl, halo¬ gen, hydroxyl, alkoxy, haloalkoxy, acid, ester, amino, nitro, amide, or alkoxyhalo; 2 R is independently alkyi, alkynyl, ester, amino, amide, acid, aryl, heteroaryl, aminoalkyl, -C(=0)alkyl, -C(=0)aryl, -C(=0)heteroaryl, -C(=0)heterocycloalkyl, - C(=0)heterocycloalkylAr, -C(=0)(CH
2 )
n halo, -C(=0)(CH
2 )nheterocyclyl, or -SC^Ar, optionally substituted with at least one alkyi, alkylhalo, halogen, nitro, aryl, heteroaryl, or heteroaryl(CH
2 )nhalo; R
3 and R
4 are independently hydrogen, alkyi, alkenyl, alkynyl, aryl, heteroaryl; Ar is an aryl, heteroaryl, cycloalkyl, heterocycloalkyl group; n is an integer from 0-10; or a radiolabeled derivative thereof. The compounds are useful as imaging probes of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.

公开(公告)号：EP3036209B1

公开(公告)日：2018-08-01

申请号：EP14758263.9

申请日：2014-08-21

申请人： GE Healthcare Limited

发明人： LUTHRA, Sajinder ,  GLASER, Matthias Eberhard ,  NAIRNE, James ,  BROWN, Jane

IPC分类号： C07B59/00 ,  B01J19/24 ,  C07C303/22 ,  C07C303/30 ,  C07C303/44

CPC分类号： C07C303/22 ,  B01J19/24 ,  B01J2219/24 ,  C07B59/001 ,  C07B2200/05 ,  C07C303/30 ,  C07C303/44 ,  C07C309/73

摘要： [18F]-fluoralkyl tosylates are useful building block for the radiosynthesis of a number of small molecules. A method of purifying [18F]-fluoroalkyl tosylates using an automated radiosynthesis apparatus (e.g. FASTlab module) is described. A method of purifying [18F]-fluoroalky tosylates using a FASTlab module that includes a solid phase extraction (SPE) purification system is described.

公开(公告)号：EP3036209A1

公开(公告)日：2016-06-29

申请号：EP14758263.9

申请日：2014-08-21

申请人： GE Healthcare Limited

发明人： LUTHRA, Sajinder ,  GLASER, Matthias Eberhard ,  NAIRNE, James ,  BROWN, Jane

IPC分类号： C07B59/00

CPC分类号： C07C303/22 ,  B01J19/24 ,  B01J2219/24 ,  C07B59/001 ,  C07B2200/05 ,  C07C303/30 ,  C07C303/44 ,  C07C309/73

摘要： [18F]-fluoralkyl tosylates are useful building block for the radiosynthesis of a number of small molecules. A method of purifying [18F]-fluoroalkyl tosylates using an automated radiosynthesis apparatus (e.g. FASTlab module) is described. A method of purifying [18F]-fluoroalky tosylates using a FASTlab module that includes a solid phase extraction (SPE) purification system is described.

摘要翻译： [18 F] - 甲苯磺酸烷基酯可用于许多小分子的放射合成。 描述了使用自动放射合成装置（例如FASTlab模块）纯化[18 F] - 氟烷基甲苯磺酸酯的方法。 描述了使用包含固相萃取（SPE）纯化系统的FASTlab模块来纯化[18 F] - 氟烷基甲苯磺酸酯的方法。

公开(公告)号：EP2640427A1

公开(公告)日：2013-09-25

申请号：EP11841188.3

申请日：2011-11-15

申请人： GE Healthcare Limited

发明人： JONES, Clare ,  NAIRNE, James

IPC分类号： A61K51/00 ,  A61K31/428

CPC分类号： C07D417/06 ,  A61K31/428 ,  A61K51/0465

摘要： Radiolabeled compounds useful as diagnostic imaging agents of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.

公开(公告)号：EP2155747B1

公开(公告)日：2012-10-24

申请号：EP08769433.7

申请日：2008-05-09

申请人： GE Healthcare Limited

发明人： OLSSON, Roger ,  BURSTEIN, Ethan ,  KNAPP, Anne, Eeg ,  ESKILDSEN, Jorgen ,  CASTILLO, Joel ,  NAIRNE, James ,  IVESON, Veronique, Morisson ,  ROBINS, Edward ,  GIBSON, Alex

IPC分类号： C07D471/04 ,  C07D487/04 ,  A61P29/00 ,  A61P25/00 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/519

CPC分类号： C07D471/04 ,  C07D487/04