公开(公告)号：EP2776382B1

公开(公告)日：2018-09-19

申请号：EP12748492.1

申请日：2012-08-21

申请人： Merck & Cie

发明人： SCHIBLI, Roger ,  MOSER, Rudolf ,  MÜLLER, Cristina Magdalena ,  AMETAMEY, Simon Mensah ,  FISCHER, Cindy Ramona ,  GROEHN, Viola

IPC分类号： A61K51/04 ,  G01N33/60 ,  C07B59/00

CPC分类号： A61K51/0491 ,  C07B59/005 ,  G01N33/60

摘要： The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein the 18F isotope is linked via a prosthetic group, more specifically via a prosthetic group having a saccharide group, such as a cyclic mono- or oligosaccharide, preferably based on a pyranoside or furanoside, which is covalently linked to the glutamate portion of a folate or derivative thereof, a method of their preparation, as well as their use in diagnosis and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.

公开(公告)号：EP2346870B1

公开(公告)日：2015-08-05

申请号：EP09783938.5

申请日：2009-10-12

申请人： Merck & Cie

发明人： SCHIBLI, Roger ,  MOSER, Rudolf ,  MÜLLER, Cristina, Magdalena ,  AMETAMEY, Simon, Mensah ,  ROSS, Tobias, Ludwig ,  GROEHN, Viola

IPC分类号： C07D475/04 ,  A61K31/519

CPC分类号： C07D475/04

摘要： The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein fluorine-18 is covalently linked to the glutamate portion of a folate or derivative thereof, a method of their preparation, as well as their use in diagnosis and monitoring of therapy of cancer and inflammatory and autoimmune diseases.

公开(公告)号：EP2864329A1

公开(公告)日：2015-04-29

申请号：EP13721738.6

申请日：2013-05-08

申请人： Merck & Cie

发明人： SCHIBLI, Roger ,  MOSER, Rudolf ,  MÜLLER, Cristina Magdalena ,  AMETAMEY, Simon Mensah ,  BETZEL, Thomas ,  GROEHN, Viola

IPC分类号： C07D475/04 ,  C07B59/00 ,  A61K31/522 ,  A61K51/04

CPC分类号： A61K51/0459 ,  C07B59/002 ,  C07D475/04 ,  G01N33/60 ,  G01N2333/705

摘要： The present invention is directed towards new 18F-folate/antifolate analogue radiopharmaceuticals, wherein the phenyl group within folate structures has been replaced by an 18F-heterocycle, their precursors, a method of their preparation, as well as their use in diagnosis of a cell or population of cells expressing a folate-receptor and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.

公开(公告)号：EP2346870A1

公开(公告)日：2011-07-27

申请号：EP09783938.5

申请日：2009-10-12

申请人： Merck & Cie

发明人： SCHIBLI, Roger ,  MOSER, Rudolf ,  MÜLLER, Cristina, Magdalena ,  AMETAMEY, Simon, Mensah ,  ROSS, Tobias, Ludwig ,  GROEHN, Viola

IPC分类号： C07D475/04 ,  A61K31/519

CPC分类号： C07D475/04

摘要： The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein fluorine-18 is covalently linked to the glutamate portion of a folate or derivative thereof, a method of their preparation, as well as their use in diagnosis and monitoring of therapy of cancer and inflammatory and autoimmune diseases.

公开(公告)号：EP2766364A1

公开(公告)日：2014-08-20

申请号：EP12746091.3

申请日：2012-08-10

申请人： Merck & Cie

发明人： SCHIBLI, Roger ,  MOSER, Rudolf ,  MÜLLER, Cristina Magdalena ,  STRUTHERS, Harriet ,  GROEHN, Viola ,  AMETAMEY, Simon Mensah ,  FISCHER, Cindy Ramona

IPC分类号： C07D475/04 ,  A61K31/519 ,  A61P35/00 ,  C07K5/02

CPC分类号： A61K51/0497 ,  A61K47/48107 ,  A61K47/551 ,  A61K51/0472 ,  A61K51/0491 ,  C07B59/002 ,  C07D475/04 ,  G01N33/56966

摘要： The present invention is directed towards new trifunctional folate-conjugates comprising a folate, an albumin binder and a radionuclide-based therapeutic or diagnostic moiety as well as pharmaceutical compositions thereof, their method of production and their use in diagnostic and therapeutic medical applications, such as diagnostic nuclear imaging and radionuclide therapy.

摘要翻译： 本发明涉及包含叶酸，白蛋白粘合剂和基于放射性核素的治疗或诊断部分的新的三官能叶酸盐缀合物，以及其药物组合物，其生产方法及其在诊断和治疗医学应用中的用途，例如 诊断性核成像和放射性核素治疗。

公开(公告)号：EP2864329B1

公开(公告)日：2018-09-26

申请号：EP13721738.6

申请日：2013-05-08

申请人： Merck & Cie

发明人： SCHIBLI, Roger ,  MOSER, Rudolf ,  MÜLLER, Cristina Magdalena ,  AMETAMEY, Simon Mensah ,  BETZEL, Thomas ,  GROEHN, Viola

IPC分类号： C07D475/04 ,  C07B59/00 ,  A61K31/522 ,  A61K51/04

CPC分类号： A61K51/0459 ,  C07B59/002 ,  C07D475/04 ,  G01N33/60 ,  G01N2333/705

摘要： The present invention is directed towards new 18F-folate/antifolate analogue radiopharmaceuticals, wherein the phenyl group within folate structures has been replaced by an 18F-heterocycle, their precursors, a method of their preparation, as well as their use in diagnosis of a cell or population of cells expressing a folate-receptor and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.

公开(公告)号：EP2776382A1

公开(公告)日：2014-09-17

申请号：EP12748492.1

申请日：2012-08-21

申请人： Merck & Cie

发明人： SCHIBLI, Roger ,  MOSER, Rudolf ,  MÜLLER, Cristina Magdalena ,  AMETAMEY, Simon Mensah ,  FISCHER, Cindy Ramona ,  GROEHN, Viola

IPC分类号： C07B59/00 ,  C07H3/02

CPC分类号： A61K51/0491 ,  C07B59/005 ,  G01N33/60

摘要： The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein the 18F isotope is linked via a prosthetic group, more specifically via a prosthetic group having a saccharide group, such as a cyclic mono- or oligosaccharide, preferably based on a pyranoside or furanoside, which is covalently linked to the glutamate portion of a folate or derivative thereof, a method of their preparation, as well as their use in diagnosis and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.

摘要翻译： 本发明涉及新的18F-叶酸放射性药物，其中18F同位素通过假体基团更具体地经由具有糖基团的假基团连接，例如环状单糖或寡糖，优选基于吡喃糖苷或呋喃糖苷 ，其与叶酸或其衍生物的谷氨酸部分共价连接，其制备方法，以及它们在诊断和监测癌症和炎症和自身免疫性疾病及其治疗中的用途。