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1. 发明公开

EP2790732A1 CLICKED SOMATOSTATIN CONJUGATED ANALOGS FOR BIOLOGICAL APPLICATIONS 有权
标题翻译：点击后，SOMATOSTATINKONJUGIERTE类似物生物应用
公开(公告)号：EP2790732A1
公开(公告)日：2014-10-22
申请号：EP12818617.8
申请日：2012-12-14
申请人： Centre National de la Recherche Scientifique (CNRS) , Université de Bourgogne Dijon , Université de Cergy-Pontoise
发明人： D'ADDONA, Debora , BERNHARD, Claire , ROVERO, Anna Maria , DENAT, Franck , CHOREV, Michael
IPC分类号： A61K47/48 , C07K7/06 , C07K7/56 , A61K49/00 , A61K51/08 , A61K38/08
CPC分类号： A61K51/083 , A61K38/00 , A61K47/547 , A61K47/64 , A61K49/0056 , A61K49/108 , A61K49/14 , A61K51/0482 , A61K51/085 , A61K51/088 , C07K14/655
摘要： The invention relate to the new conjugated somatostatin analogs of formula (I), wherein A- is H or TAG-B-, wherein -B- is 0 or a spacer, wherein TAG is a chelating agent (e.g. DOTA), a fluorescent dye, (e.g. Bodipy-B derivative, a Rho- damine-B derivative, a Fluorescein-B derivative, a Cyanine-B derivative, a Porphyrin-B derivative), a bimodal agent, or a cytotoxic agent (e.g. a doxorubicin derivative) wherein Rl is CI- C4 alkynyl radical when R2 is CI- C4 azido radical and viceversa and methods for preparing same, pharmaceutical compositions comprising them and their use in imaging and the treatment of cancer.

2. 发明授权

EP2790732B1 CLICKED SOMATOSTATIN CONJUGATED ANALOGS FOR BIOLOGICAL APPLICATIONS 有权
标题翻译：点击后，SOMATOSTATINKONJUGIERTE类似物生物应用
公开(公告)号：EP2790732B1
公开(公告)日：2016-03-09
申请号：EP12818617.8
申请日：2012-12-14
申请人： Centre National de la Recherche Scientifique (CNRS) , Université de Bourgogne Dijon , Université de Cergy-Pontoise
发明人： D'ADDONA, Debora , BERNHARD, Claire , ROVERO, Anna Maria , DENAT, Franck , CHOREV, Michael
IPC分类号： A61K47/48 , C07K7/06 , C07K7/56 , A61K49/00 , A61K51/08 , A61K38/08
CPC分类号： A61K51/083 , A61K38/00 , A61K47/547 , A61K47/64 , A61K49/0056 , A61K49/108 , A61K49/14 , A61K51/0482 , A61K51/085 , A61K51/088 , C07K14/655

3. 发明授权

EP1644344B1 PROCEDE DE PREPARATION DU CIS-8B-METHYLDECAHYDRO-2A,4A,6A,8A-TETRAAZACYCLOPENTA[FG] ACENAPHTHYLENE, DU CIS-DECAHYDRO-2A,4 A,6A,8A-TETRAAZACYCLOPENTA[FG] ACENAPHTHYLENE, DU CYCLENE, ET DE CYCLENES FONCTIONNALISES 有权
标题翻译：用于生产CIS-8B-METHYLDECAHYDRO-2A，4A，6A，8A-四氮杂[FG]苊，CIS-十氢2A，4A，6A，8A-四氮杂[FG]苊，CYCLEN和官能cyclens
公开(公告)号：EP1644344B1
公开(公告)日：2011-09-14
申请号：EP04785719.8
申请日：2004-06-04
申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
发明人： BOSCHETTI, Frédéric , CHAUX, Fanny , DENAT, Franck , GUILARD, Roger , LEDON, Henry
IPC分类号： C07D257/02 , C07D487/22 , C07D487/18 , C07D487/08
CPC分类号： C07D487/08 , C07D257/02
摘要： The invention relates to a method of preparing cyclene having formula (I) from triethylenetetraamine having formula (VIII) or ethylenediamine having formula (VIII'). The inventive method is characterised in that it comprises one of the following series of successive steps. The first series of steps (I) comprises a step A involving the one-pot preparation of the compound having formula (IIa) from the compound having formula (VIII) as defined above, followed by a step B involving the transformation of the compound having formula (IIa) into cyclene having formula (I). The second series of steps (II) comprises a step C involving the preparation of the compound having formula (IIb) from the compound having formula (VIII) as defined above, followed by a step D involving the transformation of the compound having formula (IIb) into cylcene having formula (I). Finally, the third series of steps (III) comprises a step E involving the one-pot preparation of the compound having formula (IIa), as defined above, from the compound having formula (VIII) as defined above, followed by a step B involving the transformation of the compound having formula (IIa) into cyclene having formula (I).

4. 发明公开

EP2922830A1 SYNTHESIS OF IMIDAZO[1,2-a]PYRAZIN-4-IUM SALTS FOR THE SYNTHESIS OF 1,4,7-TRIAZACYCLONONANE (TACN) AND N- AND/OR C-FUNCTIONALIZED DERIVATIVES THEREOF 有权
标题翻译：咪唑并[1,2-a]吡嗪-4-鎓SLAZEN为1,4,7-三氮杂环的合成（TACN），和Nb和/或C-官能衍生物
公开(公告)号：EP2922830A1
公开(公告)日：2015-09-30
申请号：EP13794915.2
申请日：2013-11-21
申请人： Université de Bourgogne , Centre National de la Recherche Scientifique (CNRS)
发明人： DENAT, Franck , BERNHARD, Claire , BOSCHETTI, Frédéric , DESOGERE, Pauline , ROUSSELIN, Yoann
IPC分类号： C07D255/02 , A61K51/00 , B01D43/00 , B01J23/00 , C07D487/04 , C07D301/02 , G01N24/00 , C07D401/06 , C07F9/32
CPC分类号： C07D487/04 , A61K49/0002 , A61K49/0021 , A61K49/0052 , A61K49/106 , A61K51/0482 , B01J31/182 , B01J2231/72 , C07D255/02 , C07D301/02 , C07D401/06 , C07D401/14 , C07F9/6515
摘要： The present invention embodiments relate to a compound with formula (V′) The invention also relates in certain embodiments to the synthesis method for compound (V′) and its use for the preparation of 1,4,7-triazacyclononane (tacn) and N- and/or C-functionalized derivatives thereof, particularly compounds with formula (I) The invention also relates in certain embodiments to metallic complexes comprising a ligand with formula (I) and a metal and their use for imaging.
摘要翻译：本发明实施例涉及具有式（V“）本发明因此涉及到的合成方法的某些实施例为化合物（V”）和它的对的1,4,7- triazacyclononanes（TACN）和N的制备中使用的化合物 - 和/或C-官能衍生物，与式（I）化合物尤其因此，本发明涉及的某些实施例为金属配合物包含具有式（I）的配体和金属及其用于成像的用途。

5. 发明公开

EP1644344A1 PROCEDE DE PREPARATION DU CIS-8B-METHYLDECAHYDRO-2A,4A,6A,8A-TETRAAZACYCLOPENTA[FG] ACENAPHTHYLENE, DU CIS-DECAHYDRO-2A,4 A,6A,8A-TETRAAZACYCLOPENTA[FG] ACENAPHTHYLENE, DU CYCLENE, ET DE CYCLENES FONCTIONNALISES 有权
标题翻译：制备方法步骤2 CIS-8B-METHYLDECAHYDRO-2A，4A，6A，8A-四氮杂环戊烷[FG]邻苯二亚甲基二亚乙基二胺-2A，4A，6A，8A-四氮杂环戊烷[FG]邻苯二亚甲基，DU CYCLENE，ET DE CYCLENES FONCTIONNALISES
公开(公告)号：EP1644344A1
公开(公告)日：2006-04-12
申请号：EP04785719.8
申请日：2004-06-04
申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
发明人： BOSCHETTI, Frédéric , CHAUX, Fanny , DENAT, Franck , GUILARD, Roger , LEDON, Henry
IPC分类号： C07D257/02 , C07D487/22 , C07D487/18 , C07D487/08
CPC分类号： C07D487/08 , C07D257/02
摘要： The invention relates to a method of preparing cyclene having formula (I) from triethylenetetraamine having formula (VIII) or ethylenediamine having formula (VIII'). The inventive method is characterised in that it comprises one of the following series of successive steps. The first series of steps (I) comprises a step A involving the one-pot preparation of the compound having formula (IIa) from the compound having formula (VIII) as defined above, followed by a step B involving the transformation of the compound having formula (IIa) into cyclene having formula (I). The second series of steps (II) comprises a step C involving the preparation of the compound having formula (IIb) from the compound having formula (VIII) as defined above, followed by a step D involving the transformation of the compound having formula (IIb) into cylcene having formula (I). Finally, the third series of steps (III) comprises a step E involving the one-pot preparation of the compound having formula (IIa), as defined above, from the compound having formula (VIII) as defined above, followed by a step B involving the transformation of the compound having formula (IIa) into cyclene having formula (I).
摘要翻译：本发明涉及从具有式（VIII）的三亚乙基四胺或具有式（VIII'）的乙二胺制备具有式（I）的环炔的方法。本发明的方法的特征在于它包括以下一系列连续步骤中的一个。第一系列步骤（I）包括步骤A，涉及由上述定义的具有式（VIII）的化合物一锅制备式（IIa）化合物，接着步骤B包括转化具有式式（IIa）代入式（I）的环辛烯。第二系列步骤（II）包括步骤C，涉及由上述定义的具有式（VIII）的化合物制备具有式（IIb）的化合物，接着步骤D包括将具有式（IIb）的化合物）转化成式（I）的环庚烯。最后，第三系列步骤（III）包括步骤E，涉及如上所定义的具有式（IIa）的化合物由上述定义的式（VIII）化合物一锅法制备，接着步骤B 涉及将具有式（IIa）的化合物转化成具有式（I）的环辛烯。

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