公开(公告)号：EP2252605B1

公开(公告)日：2018-06-13

申请号：EP09705728.5

申请日：2009-01-28

申请人： Institut National de la Santé et de la Recherche Médicale (INSERM) ,  Commissariat à l'Énergie Atomique et aux Énergies Alternatives ,  Université Clermont Auvergne ,  Laboratoires Cyclopharma

发明人： CHEZAL, Jean-Michel ,  DOLLE, Frédéric ,  MADELMONT, Jean-Claude ,  MAISONIAL, Aurélie ,  MIOT-NOIRAULT, Elisabeth ,  MOINS, Nicole ,  PAPON, Janine ,  KUHNAST, Bertand ,  TAVITIAN, Bertrand ,  BOISGARD, Raphaël

IPC分类号： C07D401/12 ,  C07D241/44 ,  C07D215/54 ,  C07D215/48 ,  C07D215/50 ,  A61K31/498 ,  A61K31/47 ,  A61P35/00

CPC分类号： A61K49/0002 ,  C07D213/65 ,  C07D213/76 ,  C07D215/54 ,  C07D241/44 ,  C07D401/12 ,  C07D487/04

摘要： The present invention relates to the compound of formula (I): in which R 1 represents a hydrogen atom, an optionally labelled halogen atom, a radionuclide or a Sn[(C 1 -C 4 )alkyl] 3 group, Ar represents an aryl group or a heteroaryl group, R 9 represents a hydrogen atom, a (C 1 -C 4 )alkyl group or forms together with the group R 1 -Ar a ring fused with the Ar group, A represents a group of formula (²) or (´): €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ -(CH 2 ) t -€ƒ€ƒ€ƒ€ƒ€ƒ(²) R 3 and R 4 independently represent a hydrogen atom, a (C 1 -C 6 )alkyl group, a (C 1 -C 6 )alkenyl group or a group of formula (y): €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ -Y-Z-W-R 11 €ƒ€ƒ€ƒ€ƒ€ƒ(³) wherein R 11 represents an optionally labelled halogen atom, a radionuclide, an aryl or heteroaryl group optionally substituted by an optionally labelled halogen atom, a radionuclide, a -NO 2 group, a -NR 5 R 6 group, a -N + R 5 R 6 R 7 X - group, or a -OSO 2 R 12 group, and their addition salts with pharmaceutically acceptable acids. The present invention also relates to pharmaceutical compositions comprising them and to their use in diagnosis, in particular with SPECT, PET and in therapy.

公开(公告)号：EP2252605A2

公开(公告)日：2010-11-24

申请号：EP09705728.5

申请日：2009-01-28

申请人： Institut National de la Santé et de la Recherche Médicale (INSERM) ,  Commissariat à l'Énergie Atomique et aux Énergies Alternatives ,  Université d'Auvergne Clermont 1 ,  Laboratoires Cyclopharma

发明人： CHEZAL, Jean-Michel ,  DOLLE, Frédéric ,  MADELMONT, Jean-Claude ,  MAISONIAL, Aurélie ,  MIOT-NOIRAULT, Elisabeth ,  MOINS, Nicole ,  PAPON, Janine ,  KUHNAST, Bertand ,  TAVITIAN, Bertrand ,  BOISGARD, Raphaël

IPC分类号： C07D401/12 ,  C07D241/44 ,  C07D215/54 ,  C07D215/48 ,  C07D215/50 ,  A61K31/498 ,  A61K31/47 ,  A61P35/00

CPC分类号： A61K49/0002 ,  C07D213/65 ,  C07D213/76 ,  C07D215/54 ,  C07D241/44 ,  C07D401/12 ,  C07D487/04

摘要： The present invention relates to the compound of formula (I): in which R 1 represents a hydrogen atom, an optionally labelled halogen atom, a radionuclide or a Sn[(C 1 -C 4 )alkyl] 3 group, Ar represents an aryl group or a heteroaryl group, R 9 represents a hydrogen atom, a (C 1 -C 4 )alkyl group or forms together with the group R 1 -Ar a ring fused with the Ar group, A represents a group of formula (²) or (´): €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ -(CH 2 ) t -€ƒ€ƒ€ƒ€ƒ€ƒ(²) R 3 and R 4 independently represent a hydrogen atom, a (C 1 -C 6 )alkyl group, a (C 1 -C 6 )alkenyl group or a group of formula (y): €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ -Y-Z-W-R 11 €ƒ€ƒ€ƒ€ƒ€ƒ(³) wherein R 11 represents an optionally labelled halogen atom, a radionuclide, an aryl or heteroaryl group optionally substituted by an optionally labelled halogen atom, a radionuclide, a -NO 2 group, a -NR 5 R 6 group, a -N + R 5 R 6 R 7 X - group, or a -OSO 2 R 12 group, and their addition salts with pharmaceutically acceptable acids. The present invention also relates to pharmaceutical compositions comprising them and to their use in diagnosis, in particular with SPECT, PET and in therapy.

摘要翻译： 本发明涉及式（I）化合物：其中R 1表示氢原子，任选标记的卤素原子，放射性核素或Sn [（C 1 -C 4）烷基] 3基团，Ar表示芳基 基团或杂芳基，R 9表示氢原子，（C 1 -C 4）烷基或与Ar基团稠合的基团R 1 -Ar a形成，A表示式（²）的基团， 或（'）：€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ - （CH 2）t - €ƒ€ƒ€ƒ（²）R 3和R 4独立地表示氢 原子，（C 1 -C 6）烷基，（C 1 -C 6）烯基或式（y）的基团：ƒ€ƒ€ƒ€ƒ€ƒ€ƒ-YZWR 11ƒ€ƒ€ƒ€ƒ（³）其中R 11表示任选标记的卤素原子，任选被任意标记的卤素原子取代的放射性核素，芳基或杂芳基，放射性核素，-NO 2基， -NR 5 R 6基团，-N + R 5 R 6 R 7 X基团或-OSO 2 R 12基团，以及它们的 与药学上可接受的酸的盐。 本发明还涉及包含它们的药物组合物及其在诊断中的用途，特别是在SPECT，PET和治疗中的用途。

公开(公告)号：EP2841402A1

公开(公告)日：2015-03-04

申请号：EP13725814.1

申请日：2013-04-19

申请人： Institut National de la Santé et de la Recherche Médicale (INSERM) ,  Laboratoires Cyclopharma ,  Universite d'Auvergne Clermont I

发明人： CHEZAL, Jean-Michel ,  RBAH-VIDAL, Latifa ,  BILLAUD, Emilie ,  AUZELOUX, Philippe ,  MADELMONT, Jean-Claude ,  VIDAL, Aurélien ,  MIOT-NOIRAULT, Elisabeth ,  PAPON, Janine ,  MAISONIAL, Aurélie

IPC分类号： C07B59/00 ,  C07D241/44 ,  C07D403/12 ,  C07F7/22

CPC分类号： A61K51/0459 ,  C07B59/002 ,  C07D241/44 ,  C07D403/12 ,  C07F7/2212

摘要： The present invention relates to the compound of formula (I), in which R1 represents Sn(R)
3 , B(OH)
2 , B(OR)
2 , a halogen atom, NO
2 , a radionuclide or a -N
+ (R)
3 group, where R is a (C
1 -C
6 ) alkyl group, R2 represents a hydrogen atom or a (C
1 -C
6 )alkyl group, R3 represents: - a -(CH
2 CH
2 O)
n2 -(CH
2 )
n3 -X group, or - a –(CH
2 CH
2 O)
n4 -(CH
2 )n
5 -Y group with Y representing a -C=C-H, a -N
3 or a -Ar-(CH
2 )
n6 -(OCH
2 CH
2 )
n7 -X group, and X represents a halogen atom, a radionuclide or a -OSO
2 R' group, where R' is a CF
3 , CH
3 ,
t -Bu, Ph,
p -NO
2 Ph,
p -BrPh or
p -CH
3 Ph group, and their addition salts with pharmaceutically acceptable acids, The present invention also relates to pharmaceutical compositions comprising them and to their use in diagnosis, in particular with SPECT or PET imaging and in therapy of melanoma, via targeted radionuclide therapy.

公开(公告)号：EP3177598A1

公开(公告)日：2017-06-14

申请号：EP15750269.1

申请日：2015-07-28

申请人： Institut National de la Santé et de la Recherche Médicale (INSERM) ,  Universite d'Auvergne Clermont I

发明人： DENIS, Claire ,  GAUMET, Vincent ,  VIDAL, Aurélien ,  AUZELOUX, Philippe ,  MADELMONT, Jean-Claude ,  MIOT-NOIRAULT, Elisabeth ,  CHEZAL, Jean-Michel

IPC分类号： C07D257/02 ,  C07D487/08 ,  C07F1/08 ,  A61P19/00

CPC分类号： C07D257/02 ,  C07D487/08 ,  C07F1/08

摘要： The present invention concerns compounds of formula (I):their process of preparation and compositions thereof. The present invention also concerns their use as diagnostic agent in PET imaging.

摘要翻译： 本发明涉及式（I）的化合物：它们的制备和它们的组合物的过程。 因此，本发明涉及它们作为在PET成像诊断剂的用途。

公开(公告)号：EP3177598B1

公开(公告)日：2019-08-28

申请号：EP15750269.1

申请日：2015-07-28

申请人： Institut National de la Santé et de la Recherche Médicale (INSERM) ,  Universite d'Auvergne Clermont I

发明人： DENIS, Claire ,  GAUMET, Vincent ,  VIDAL, Aurélien ,  AUZELOUX, Philippe ,  MADELMONT, Jean-Claude ,  MIOT-NOIRAULT, Elisabeth ,  CHEZAL, Jean-Michel

IPC分类号： C07D257/02 ,  C07D487/08 ,  C07F1/08 ,  A61P19/00

公开(公告)号：EP2841402B1

公开(公告)日：2016-11-30

申请号：EP13725814.1

申请日：2013-04-19

申请人： Institut National de la Santé et de la Recherche Médicale ,  Laboratoires Cyclopharma ,  Universite d'Auvergne Clermont I

发明人： CHEZAL, Jean-Michel ,  RBAH-VIDAL, Latifa ,  BILLAUD, Emilie ,  AUZELOUX, Philippe ,  MADELMONT, Jean-Claude ,  VIDAL, Aurélien ,  MIOT-NOIRAULT, Elisabeth ,  PAPON, Janine ,  MAISONIAL, Aurélie

IPC分类号： C07B59/00 ,  C07D241/44 ,  C07D403/12 ,  C07F7/22

CPC分类号： A61K51/0459 ,  C07B59/002 ,  C07D241/44 ,  C07D403/12 ,  C07F7/2212