公开(公告)号：EP2951171A1

公开(公告)日：2015-12-09

申请号：EP14701569.7

申请日：2014-01-28

Applicant: Boehringer Ingelheim International GmbH ,  Stichting VU-VUmc

Inventor： SLOBBE, Paul ,  POOT, Alex Johannes ,  VAN DONGEN, Augustinus Antonius Maria Silvester ,  NIESSEN, Heiko ,  WINDHORST, Albert Dirk

IPC: C07D405/12 ,  A61K51/04

CPC classification number: C07D405/12 ,  A61K51/0459 ,  C07B2200/05

Abstract: Novel radiotracer for positron emission tomography (PET) or single photon emission computed tomography (SPECT) imaging are described. Specifically, the invention relates to
18 F-labeled afatinib suitable as a PET or SPECT tracer for imaging epidermal growth factor receptor (EGFR, erbB1) and human epidermal growth factor receptor 2 (Her2, erbB2), to a precursor compound for use in its synthesis, to methods for the preparation
18 F-iabeled afatinib, as well as to the use thereof in in vivo diagnosis, tumor imaging or patient stratification on the basis of mutational status of EGFR (erbB1) and Her2 (erbB2).

公开(公告)号：WO2015194954A1

公开(公告)日：2015-12-23

申请号：PCT/NL2015/050447

申请日：2015-06-18

Applicant: STICHTING VOOR DE TECHNISCHE WETENSCHAPPEN ,  STICHTING VU-VUMC ,  RIJKSUNIVERSITEIT GRONINGEN ,  ACADEMISCH ZIEKENHUIS GRONINGEN ,  BIOFORDRUG SRL, SPIN-OFF DELL'UNIVERSITA DEGLI STUDI DI BARI

Inventor： LUURTSEMA, Gert ,  WINDHORST, Albert Dirk ,  COLABUFO, Nicola Antonio ,  CANTORE, Mariangela ,  SAVOLAINEN, Heli

IPC: C07D217/04 ,  A61K49/00 ,  A61K51/04 ,  A61K31/472 ,  G01N33/58 ,  G01N33/60 ,  G21H5/02 ,  A61P25/28

CPC classification number: C07D217/04 ,  A61K51/0455 ,  G21H5/02

Abstract: The present invention relates to a 6,7-dioxyalkyltetrahydroisoquinoline compound, or a salt or solvate thereof according to formula I: (formula I), (I) wherein R represents hydrogen or a fluorinated alkyl group, and R 2 and R 3 independently represents hydrogen or an alkyl group.

Abstract translation: 本发明涉及式I的6,7-二氧烷基四氢异喹啉化合物或其盐或溶剂合物：（Ⅰ）式（Ⅰ）其中R代表氢或氟化烷基，R2和R3独立地代表氢或 烷基。

公开(公告)号：WO2014118197A1

公开(公告)日：2014-08-07

申请号：PCT/EP2014/051659

申请日：2014-01-28

Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH ,  STICHTING VU-VUMC

Inventor： SLOBBE, Paul ,  POOT, Alex Johannes ,  VAN DONGEN, Augustinus Antonius Maria Silvester ,  NIESSEN, Heiko ,  WINDHORST, Albert Dirk

IPC: C07D405/12 ,  A61K51/04

CPC classification number: C07D405/12 ,  A61K51/0459 ,  C07B2200/05

Abstract: Novel radiotracer for positron emission tomography (PET) or single photon emission computed tomography (SPECT) imaging are described. Specifically, the invention relates to 18 F-labeled afatinib suitable as a PET or SPECT tracer for imaging epidermal growth factor receptor (EGFR, erbB1) and human epidermal growth factor receptor 2 (Her2, erbB2), to a precursor compound for use in its synthesis, to methods for the preparation 18 F-iabeled afatinib, as well as to the use thereof in in vivo diagnosis, tumor imaging or patient stratification on the basis of mutational status of EGFR (erbB1) and Her2 (erbB2).

Abstract translation: 描述了用于正电子发射断层扫描（PET）或单光子发射计算机断层摄影（SPECT）成像的新型放射性示踪剂。 具体地说，本发明涉及适用于成像表皮生长因子受体（EGFR，erbB1）和人表皮生长因子受体2（Her2，erbB2）的PET或SPECT示踪剂的18F-标记的阿片碱，用于其合成中的前体化合物 ，依据EGFR（erbB1）和Her2（erbB2）的突变状态制备18F-标记的阿伐替尼的方法，以及其在体内诊断，肿瘤成像或患者分层中的应用。

公开(公告)号：WO2014098593A9

公开(公告)日：2014-06-26

申请号：PCT/NL2013/050925

申请日：2013-12-19

Applicant: STICHTING VOOR DE TECHNISCHE WETENSCHAPPEN ,  STICHTING VU-VUMC ,  RIJKSUNIVERSITEIT GRONINGEN ,  ACADEMISCH ZIEKENHUIS GRONINGEN

Inventor： RAAPHORST, Renske ,  LUURTSEMA, Gert ,  WINDHORST, Albert Dirk ,  LAMMERTSMA, Adriaan

IPC: A61K51/04 ,  A61K31/277 ,  C07B59/00

Abstract: The invention is directed to a compound, a salt or a solvate thereof according to (I) wherein R 1 is an optionally branched fluoroalkyl group or [ 18 F]fluoroalkyl group, R 2 , R 3 , R 4 and R 5 are eacn independently a methyl, [ 3 H]methyl, fluoroalkyl or [ 18 F]fluoroalkyl group, and R 6 is a ( R )-cyano group or a ( S )-cyano group; or wherein R 1 is a methyl group, and R 3 is a R 3 is a fluoroalkyl group or a [ 18 F]fluoroalkyl group, R 2 , R 4 and R 5 are each independently a methyl, [ 3 H]methyl, fluoroalkyl or [ 18 F]fluoroalkyl group, and R 6 is a (R)-cyano group or a (S)-cyano group; or wherein if R 1 is hydrogen, at least one of R 2 , R 3 , R 4 is an optionally branched fluoroalkyl group or [ 18 F]fluoroalkyl group.

公开(公告)号：WO2014007629A1

公开(公告)日：2014-01-09

申请号：PCT/NL2013/050497

申请日：2013-07-04

Applicant: STICHTING VU-VUMC

Inventor： CHRISTIAANS, Johannes Antonius Maria ,  WINDHORST, Albert Dirk ,  METAXAS, Athanasios ,  KLEIN, Pieter Jacob ,  KOOIJMAN, Esther Johanna Maria ,  VAN BERCKEL, Bart Nicolaas Maria

IPC: C07C217/56 ,  C07D213/24

CPC classification number: C07D213/74 ,  C07C213/02 ,  C07C2601/02 ,  C07C2601/08 ,  C07D213/24 ,  C07D213/38 ,  C07C215/74

Abstract: The invention is directed to a compound according to formula (1) wherein R 2 is fluorine, X is nitrogen or carbon and R 3 is an organic group. The invention is also directed to the use of this compound as a precursor for the preparation of a 11 C or 18 F-radio labelled compound. The radio labelled compound may be used in an in vivo diagnostic or imaging method.

Abstract translation: 本发明涉及式（1）的化合物，其中R 2是氟，X是氮或碳，R 3是有机基团。 本发明还涉及该化合物作为制备11C或18F-无线电标记化合物的前体的用途。 放射性标记的化合物可以用于体内诊断或成像方法。

公开(公告)号：WO2012165956A1

公开(公告)日：2012-12-06

申请号：PCT/NL2012/050377

申请日：2012-05-30

Applicant: VERENIGING VOOR CHRISTELIJK HOGER ONDERWIJS, WETENSCHAPPELIJK ONDERZOEK EN PATIENTENZORG ,  STICHTING VU-VUMC ,  KLEIN, Pieter Jacob ,  METAXAS, Athansios ,  WINDHORST, Albert Dirk ,  CHRISTIAANS, Johannes Antonius Maria ,  VAN BERCKEL, Bart Nicolaas Maria

Inventor： KLEIN, Pieter Jacob ,  METAXAS, Athansios ,  WINDHORST, Albert Dirk ,  CHRISTIAANS, Johannes Antonius Maria ,  VAN BERCKEL, Bart Nicolaas Maria

IPC: C07C279/18 ,  C07B59/00 ,  A61K31/155

CPC classification number: C07C279/18 ,  A61K31/155 ,  A61K51/04 ,  C07B59/001 ,  C07B2200/05 ,  C07C277/08 ,  C07C319/20 ,  C07C323/44

Abstract: The invention is directed to a N, N-substituted guanidine compound or a salt or solvate thereof according to formula (1), R 1 RNC(NH)NR 2 R 3 , wherein R 1 is methyl and R 2 is hydrogen. R 3 is a organic group comprising a halogen and thiomethyl substituted phenyl group. R is an organic group comprising a substituted aryl group Z wherein the substituent group is -Y-R 4 , wherein Y is a heteroatom chosen from the group consisting of O, S and N and R 4 is a fluorinated organic group.

Abstract translation: 本发明涉及根据式（1）的R1，R2，R2是氢的N，N-取代的胍化合物或其盐或溶剂合物，R1RNC（NH）NR2R3。 R3是包含卤素和硫代甲基取代的苯基的有机基团。 R是包含取代的芳基Z的有机基团，其中取代基是-Y-R 4，其中Y是选自O，S和N的杂原子，R4是氟化有机基团。

公开(公告)号：EP2867200A1

公开(公告)日：2015-05-06

申请号：EP13739857.4

申请日：2013-07-04

Applicant: Stichting VU-VUmc

Inventor： CHRISTIAANS, Johannes Antonius Maria ,  WINDHORST, Albert Dirk ,  METAXAS, Athanasios ,  KLEIN, Pieter Jacob ,  KOOIJMAN, Esther Johanna Maria ,  VAN BERCKEL, Bart Nicolaas Maria

IPC: C07C217/56 ,  C07D213/24

CPC classification number: C07D213/74 ,  C07C213/02 ,  C07C2601/02 ,  C07C2601/08 ,  C07D213/24 ,  C07D213/38 ,  C07C215/74

Abstract: The invention is directed to a compound according to formula (1) wherein R
2 is fluorine, X is nitrogen or carbon and R
3 is an organic group. The invention is also directed to the use of this compound as a precursor for the preparation of a
11 C or
18 F-radio labelled compound. The radio labelled compound may be used in an in vivo diagnostic or imaging method.

Abstract translation: 本发明涉及式（1）的化合物，其中R 2是氟，X是氮或碳，R 3是有机基团。 本发明还涉及该化合物作为制备11C或18F-无线电标记化合物的前体的用途。 放射性标记的化合物可以用于体内诊断或成像方法。