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1. 发明申请

WO2011151348A1 HETEROCYCLIC AMINO ACIDS 审中-公开
标题翻译：杂环氨基酸
公开(公告)号：WO2011151348A1
公开(公告)日：2011-12-08
申请号：PCT/EP2011/058991
申请日：2011-05-31
申请人： BAYER PHARMA AKTIENGESELLSCHAFT , BÖHNKE, Niels , BRUMBY, Thomas , LESCHE, Ralf , GRAHAM, Keith
发明人： BÖHNKE, Niels , BRUMBY, Thomas , LESCHE, Ralf , GRAHAM, Keith
IPC分类号： C07D307/24 , C07D309/14 , C07D515/04 , A61K51/04
CPC分类号： C07D307/24 , A61K51/0419 , A61K51/0421 , C07D309/14 , C07D515/04
摘要： This invention relates to heterocyclic amino acid derivatives suitable for labeling or already labeled with 18 F or 19 F , methods of preparing such compounds, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for imaging proliferative diseases.
摘要翻译：本发明涉及适用于标记或已经用18F或19F标记的杂环氨基酸衍生物，制备此类化合物的方法，包含这些化合物的组合物，包含这些化合物或组合物的试剂盒和用于成像增殖性疾病的这些化合物，组合物或试剂盒的用途。

2. 发明申请

WO2011073286A1 PROSTATE SPECIFIC MEMBRANE ANTIGEN INHIBITORS 审中-公开
标题翻译： PROSTATE特异性膜抗原抑制剂
公开(公告)号：WO2011073286A1
公开(公告)日：2011-06-23
申请号：PCT/EP2010/069827
申请日：2010-12-16
申请人： Bayer Schering Pharma Aktiengesellschaft , GRAHAM, Keith , KETTSCHAU, Georg , LESCHE, Ralf , GROMOV, Alexey , BÖHNKE, Niels , HAßFELD, Jorma
发明人： GRAHAM, Keith , KETTSCHAU, Georg , LESCHE, Ralf , GROMOV, Alexey , BÖHNKE, Niels , HAßFELD, Jorma
IPC分类号： C07F7/18 , C07F9/38 , C07F9/40 , C07F9/655 , A61K31/662 , A61K31/665 , A61P25/00 , A61P35/00 , C07B59/00 , A61K51/04
CPC分类号： C07F7/1844 , A61K51/0489 , C07B59/004 , C07F9/3808 , C07F9/4006 , C07F9/65515 , C07F9/6552
摘要： This invention relates to novel compounds suitable for labelling by 18 F and the corresponding 18 F labelled compounds themselves, 19 F-fluorinated analogues thereof and their use as reference standards, methods of preparing such compounds, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).
摘要翻译：本发明涉及适用于通过18F和相应的18F标记的化合物本身，相应的18F-氟化的类似物及其作为参考标准物的用途，制备这些化合物的方法，包含这些化合物的组合物，包含这些化合物或组合物的试剂的这种化合物，用于通过正电子发射断层摄影（PET）进行诊断成像的组合物或试剂盒。

3. 发明申请

WO2012150220A1 RADIOLABELED AMINO ACIDS FOR DIAGNOSTIC IMAGING 审中-公开
标题翻译：放射性氨基酸用于诊断成像
公开(公告)号：WO2012150220A1
公开(公告)日：2012-11-08
申请号：PCT/EP2012/057925
申请日：2012-04-30
申请人： BAYER PHARMA AKTIENGESELLSCHAFT , BERNDT, Mathias , MÜLLER, Andre , SCHMITT-WILLICH, Heribert , STELLFELD, Timo , KETTSCHAU, Georg , BRUMBY, Thomas , GRAHAM, Keith , LEHMANN, Lutz , HAßFELD, Jorma , KRÜGER, Martin
发明人： BERNDT, Mathias , MÜLLER, Andre , SCHMITT-WILLICH, Heribert , STELLFELD, Timo , KETTSCHAU, Georg , BRUMBY, Thomas , GRAHAM, Keith , LEHMANN, Lutz , HAßFELD, Jorma , KRÜGER, Martin
IPC分类号： C07B59/00 , A61K31/195 , A61K49/10 , A61K51/04 , C07C229/36 , A61P35/00 , C07C229/42 , C07C271/22 , C07C309/73 , C07D213/55 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/89 , C07D249/04 , C07D317/22
CPC分类号： C07D249/06 , A61K51/0406 , C07B59/00 , C07B2200/05 , C07C229/24 , C07C229/36 , C07C229/42 , C07C271/22 , C07C309/73 , C07C2601/04 , C07D213/55 , C07D213/61 , C07D213/65 , C07D213/69 , C07D319/06
摘要： This invention relates to novel compounds suitable for labeling by 18 F and to the corresponding 18 F labeled compounds themselves, 19 F-fluorinated analogues thereof and their use as reference standards, methods of preparing such compounds, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by Positron Emission Tomography (PET).
摘要翻译：本发明涉及适用于通过18F和相应的18F标记的化合物本身或其相应的18F-氟化的类似物进行标记的新化合物及其作为参考标准物的用途，制备此类化合物的方法，包含这些化合物的组合物，包含这些化合物或组合物的试剂盒，以及这些化合物，组合物或试剂盒用于通过正电子发射断层扫描（PET）进行诊断成像的用途。

4. 发明申请

WO2012025464A1 FLUORODEUTERIOMETHYL TYROSINE DERIVATIVES 审中-公开
标题翻译：氟代二甲基吡啶衍生物
公开(公告)号：WO2012025464A1
公开(公告)日：2012-03-01
申请号：PCT/EP2011/064311
申请日：2011-08-19
申请人： BAYER PHARMA AKTIENGESELLSCHAFT , GRAHAM, Keith , ZITZMANN-KOLBE, Sabine , BRUMBY, Thomas
发明人： GRAHAM, Keith , ZITZMANN-KOLBE, Sabine , BRUMBY, Thomas
IPC分类号： C07B59/00 , C07C229/36 , A61K51/04
CPC分类号： C07B59/001 , A61K51/0402 , C07B2200/07 , C07C229/36
摘要： This invention relates to deuterated tyrosine derivatives labeled with 18 F or 19 F, methods of preparing such compounds, compositions comprising such compounds, kits thereof and uses of such compounds, compositions or kits for imaging proliferative diseases.
摘要翻译：本发明涉及用18F或19F标记的氘代酪氨酸衍生物，制备此类化合物的方法，包含这些化合物的组合物，其试剂盒和用于成像增殖性疾病的这些化合物，组合物或试剂盒的用途。

5. 发明申请

WO2011060887A3 METHOD FOR PRODUCTION OF F-18 LABELED GLUTAMIC ACID DERIVATIVES 审中-公开
公开(公告)号：WO2011060887A3
公开(公告)日：2011-05-26
申请号：PCT/EP2010/006766
申请日：2010-11-06
申请人： BAYER PHARMA AKTIENGESELLSCHAFT , BERNDT, Mathias , SCHMIITT-WILLICH, Heribert , FRIEBE, Matthias , GRAHAM, Keith , BRUMBY, Thomas , HULTSCH, Christina , WESTER, Hans-Jürgen , WAGNER, Franziska
发明人： BERNDT, Mathias , SCHMIITT-WILLICH, Heribert , FRIEBE, Matthias , GRAHAM, Keith , BRUMBY, Thomas , HULTSCH, Christina , WESTER, Hans-Jürgen , WAGNER, Franziska
IPC分类号： C07B59/00 , C07C227/20 , C07C229/24 , C07C271/22 , C07C309/66 , C07C309/73 , A61K31/198 , A61K51/04
摘要： This invention relates to methods, which provide access to F-18 labeled glutamic acid derivatives.

6. 发明申请

WO2008083729A1 RADIOLABELLING VIA FLUORINATION OF AZIRIDINES 审中-公开
标题翻译：通过氟化钠的放射性辐射
公开(公告)号：WO2008083729A1
公开(公告)日：2008-07-17
申请号：PCT/EP2007/007968
申请日：2007-09-07
申请人： BAYER SCHERING PHARMA AKTIENGESELLSCHAFT , SRINIVASAN, Ananth , BRUMBY, Thomas , STELLFELD, Timo , GRAHAM, Keith , VOIGTMANN, Ulrike , BECAUD, Jessica , MU, Linjing
发明人： SRINIVASAN, Ananth , BRUMBY, Thomas , STELLFELD, Timo , GRAHAM, Keith , VOIGTMANN, Ulrike , BECAUD, Jessica , MU, Linjing
IPC分类号： C07C311/19 , C07D203/08 , C07D203/24 , C07D207/14 , C07D403/12 , C07D405/04 , C07D405/14 , C07D487/04 , C07D487/22 , C07D491/04 , C07K7/02
CPC分类号： C07C311/19 , C07B59/001 , C07B2200/05 , C07D203/08 , C07D203/24 , C07D207/14 , C07D403/12 , C07D405/04 , C07D405/14 , C07D487/04 , C07D487/22 , C07D491/04 , C07K5/06191 , C07K7/02
摘要： The present invention relates to novel compounds suitable for or already radiolabeled with 18 F, methods of making such compounds and use of such compounds for diagnostic imaging.
摘要翻译：本发明涉及适用于或已经用<！ - SIPO - >已经放射性标记的新化合物，制备这些化合物的方法和用于诊断成像的这些化合物的用途。

7. 发明申请

WO2013001088A1 DIRECT SYNTHESIS OF 18F-FLUOROMETHOXY COMPOUNDS FOR PET IMAGING AND THE PROVISION OF NEW PRECURSORS FOR DIRECT RADIOSYNTHESIS OF PROTECTED DERIVATIVES OF O-([18F]FLUOROMETHYL) TYROSINE 审中-公开
标题翻译：用于PET成像的18F-荧光素化合物的直接合成以及用于O - （[18F]氟甲基）酪氨酸受体衍生物的直接放射化的新前体的提供
公开(公告)号：WO2013001088A1
公开(公告)日：2013-01-03
申请号：PCT/EP2012/062786
申请日：2012-06-29
申请人： PIRAMAL IMAGING SA , BRUMBY, Thomas , GRAHAM, Keith , KRÜGER, Martin
发明人： BRUMBY, Thomas , GRAHAM, Keith , KRÜGER, Martin
IPC分类号： C07D249/04 , C07D249/18 , C07D471/04
CPC分类号： A61K51/0453 , A61K51/0455 , C07C227/16 , C07C229/36 , C07C269/06 , C07C271/22 , C07D249/04 , C07D249/18 , C07D471/04
摘要： The invention describes novel direct synthesis methods for converting a precursor into a PET-tracer with a 18 F-fluoromethoxy-group. The invention is also directed to novel and stable precursors for the direct radiosynthesis of protected derivatives of O- ([ 18 F]Fluoromethyl) tyrosines.
摘要翻译：本发明描述了用18F-氟甲氧基将前体转化成PET示踪剂的新型直接合成方法。本发明还涉及用于直接放射合成O-（[18 F]氟甲基）酪氨酸的受保护衍生物的新型和稳定的前体。

8. 发明申请

WO2008028688A2 COMPOUNDS AND METHODS FOR 18F LABELED AGENTS 审中-公开
标题翻译： 18F标签代理的化合物和方法
公开(公告)号：WO2008028688A2
公开(公告)日：2008-03-13
申请号：PCT/EP2007/008042
申请日：2007-09-07
申请人： BAYER SCHERING PHARMA AKTIENGESELLSCHAFT , LEHMANN, Lutz , SRINIVASAN, Ananth , BRUMBY, Thomas , SÜLZLE, Detlef , STELLFELD, Timo , GRAHAM, Keith , KARRAMKAM, Mylène , AMETAMEY, Simon
发明人： LEHMANN, Lutz , SRINIVASAN, Ananth , BRUMBY, Thomas , SÜLZLE, Detlef , STELLFELD, Timo , GRAHAM, Keith , KARRAMKAM, Mylène , AMETAMEY, Simon
IPC分类号： A61K51/08 , C07K7/06 , A61K51/04 , C07C255/58
CPC分类号： C07K14/6555 , A61K51/088 , C07K14/57545
摘要： The present invention relates to novel compounds suitable for or already radiolabeled with 18 F, methods of making such compounds and use of such compounds for diagnostic imaging. Such labeled compounds are characterized by Formula II, wherein the substituents G, Q, L, Y and U have the meaning as defined in the specification and claims.
摘要翻译：本发明涉及适用于或已经用<！ - SIPO - >已经放射性标记的新化合物，制备这些化合物的方法和用于诊断成像的这些化合物的用途。这些标记的化合物由式II表征，其中取代基G，Q，L，Y和U具有如说明书和权利要求书中所定义的含义。

9. 发明申请

WO2012104225A1 DERIVATIZATION OF RADIOPHARMACEUTICALS 审中-公开
标题翻译：放射线衍生物的衍生物
公开(公告)号：WO2012104225A1
公开(公告)日：2012-08-09
申请号：PCT/EP2012/051368
申请日：2012-01-27
申请人： BAYER PHARMA AKTIENGESELLSCHAFT , GRAHAM, Keith , SELAHATTIN, Ede
发明人： GRAHAM, Keith , SELAHATTIN, Ede
IPC分类号： C07F9/38 , C07F9/40 , C07B59/00
CPC分类号： C07F9/3808 , C07B59/004 , C07F9/4006
摘要： This invention relates to methods for analyzing radiopharmaceuticals wherein the radiopharmaceutical is derivatized beforehand. This method is suitable for compounds labeled with radioisotope or with cold counterpart e.g. 18 F or 19 F, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for analyzing radiopharmaceuticals. wherein R 1 is C(=0)OR6; R 2 is C(=0)OR 7 ; R 3 is, 19 F or 18 F R 4 is hydrogen, Methyl, Ethyl, Propyl. Butyl, t-Butyl or Benzyl; R 5 is hydrogen. Methyl, Ethyl, Propyl. Butyl, t-Butyl or Benzyl; R 6 is hydrogen, Methyl, Ethyl, Propyl, Butyl, t-Butyl or Benzyl; R 7 is hydrogen, Methyl, Ethyl, Propyl. Butyl, t-Butyl or Benzyl; with the proviso that at least one of R 4 , R 5 , R 6 , and R 7 is hydrogen
摘要翻译：本发明涉及放射性药物分析方法，其中放射性药物是预先衍生的。该方法适用于用放射性同位素标记的化合物，或适用于冷对照物的化合物。 18F或19F，包含这些化合物的组合物，包含这样的化合物或组合物的试剂盒和用于分析放射性药物的这些化合物，组合物或试剂盒的用途。其中R1是C（= O）OR6; R2为C（= O）OR7; R3是，19F或18F R4是氢，甲基，乙基，丙基。丁基，叔丁基或苄基; R5是氢。甲基，乙基，丙基。丁基，叔丁基或苄基; R6是氢，甲基，乙基，丙基，丁基，叔丁基或苄基; R7是氢，甲基，乙基，丙基。丁基，叔丁基或苄基; 条件是R4，R5，R6和R7中的至少一个是氢

10. 发明申请

WO2020048831A1 5-ARYL-3,9-DIAZASPIRO[5.5]UNDECAN-2-ONE COMPOUNDS 审中-公开
公开(公告)号：WO2020048831A1
公开(公告)日：2020-03-12
申请号：PCT/EP2019/072880
申请日：2019-08-27
申请人： BAYER AKTIENGESELLSCHAFT , BAYER PHARMA AKTIENGESELLSCHAFT
发明人： GRAHAM, Keith , BUCHGRABER, Philipp , AIGUABELLA FONT, Nuria , WITTROCK, Sven , HEINRICH, Tobias , BRÄUER, Nico , KUHNKE, Lara, Patricia , LANGE, Martin , BADER, Benjamin , PRECHTL, Stefan , LIENAU, Philip , KOPITZ, Charlotte, Christine , NOWAK-REPPEL, Katrin , POTZE, Lisette , STEUBER, Holger
IPC分类号： C07D471/10 , A61K31/438 , A61P35/00
摘要： The present invention covers 5-aryl-3,9-diazaspiro[5.5]undecan-2-one compounds of general formula (I) and general formula (I-a): (I) and (I-a), in which R 1 , R 2 , R 3 and R 4 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

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