公开(公告)号：US20150315189A1

公开(公告)日：2015-11-05

申请号：US14797640

申请日：2015-07-13

Applicant: MERCK & CIE

Inventor： Simon Mensah AMETAMEY ,  Rudolf MOSER ,  Tobias Ludwig ROSS ,  Phoebe LAM ,  Viola GROEHN

IPC: C07D475/04 ,  C07B59/00

CPC classification number: C07D475/04 ,  A61K51/0459 ,  A61K51/0497 ,  C07B59/002

Abstract: The present invention is directed towards a new method of synthesis of 18F-folate radiopharmaceuticals, wherein fluorine-18 is attached to a pteroate (or folate) or derivative thereof, through direct radiolabeling with 18[F]fluoride, as well as 18F-folate radiopharmaceuticals obtained by such method of synthesis and their use in diagnosis and monitoring of cancer therapy and therapy of inflammatory and autoimmune diseases.

Abstract translation: 本发明涉及一种合成18 F-叶酸放射性药物的新方法，其中氟-18通过与氟化氟[18 F]直接放射性标记以及18F-叶酸连接在叶酸（或叶酸）或其衍生物上 通过这种合成方法获得的放射性药物及其在诊断和监测癌症治疗和治疗炎性和自身免疫疾病中的用途。

公开(公告)号：US20180072734A1

公开(公告)日：2018-03-15

申请号：US15711316

申请日：2017-09-21

Applicant: MERCK & CIE

Inventor： Roger SCHIBLI ,  Rudolf MOSER ,  Cristina Magdalena MULLER ,  Simon Mensah AMETAMEY ,  Tobias Ludwig ROSS ,  Viola GROEHN

IPC: C07D475/04

CPC classification number: C07D475/04

Abstract: 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：US20190255200A1

公开(公告)日：2019-08-22

申请号：US16400736

申请日：2019-05-01

Applicant: MERCK & CIE

Inventor： Roger SCHIBLI ,  Rudolf MOSER ,  Christina Magdalena MULLER ,  Simon Mensah AMETAMEY ,  Cindy Ramona FISCHER ,  Viola GROEHN

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

Abstract: 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：US20160159802A1

公开(公告)日：2016-06-09

申请号：US15042657

申请日：2016-02-12

Applicant: MERCK & CIE

Inventor： Simon Mensah AMETAMEY ,  Rudolf MOSER ,  Tobais Ludwig ROSS ,  Viola GROEHN

IPC: C07D475/08 ,  G01N33/60 ,  G01N33/82 ,  A61K51/04 ,  G01N33/574

CPC classification number: C07D475/08 ,  A61K51/0459 ,  A61K51/0497 ,  C07B2200/05 ,  C07D475/04 ,  G01N33/57492 ,  G01N33/60 ,  G01N33/82 ,  G01N2333/705

Abstract: The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein the fluorine-18 is covalently linked to the aminobenzoyl moiety, which connects the condensed pyrimidine heterocycle to the amino acid portion within folate structures, as well as their precursors and their non-radioactive references, 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.

Abstract translation: 本发明涉及新的18F-叶酸类放射性药物，其中氟-18共价连接到氨基苯甲酰部分，其将稠合的嘧啶杂环连接到叶酸结构内的氨基酸部分，以及它们的前体及其非放射性 参考文献，其制备方法以及它们在诊断表达叶酸受体的细胞或细胞群以及监测癌症和炎性和自身免疫性疾病及其治疗方面的用途。