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1. 发明申请

WO2022255915A1 PET RADIOTRACERS 审中-公开
公开(公告)号：WO2022255915A1
公开(公告)日：2022-12-08
申请号：PCT/SE2022/050413
申请日：2022-04-28
申请人： NORDBERG, Agneta , LÅNGSTRÖM, Bengt , ÅGREN, Hans , HALLDIN, Christer
发明人： NORDBERG, Agneta , LÅNGSTRÖM, Bengt , ÅGREN, Hans , HALLDIN, Christer
IPC分类号： C07D471/08 , A61K51/04 , A61P25/16 , A61P25/18 , G01N33/60
摘要： The compounds of the invention are ASEM analogs with different ortho- and para-substitutions that can be labelled with 3H and/or 11C to be used as PET radiotracers capable of binding to α7-nAChR both in vitro and in vivo in a subject body. The PET radiotracers thereby enable visualization and quantification of α7-nAChR in various target tissues, including monitoring the distribution of α7-nAChRs in such a target tissue. The compounds exhibit of high binding affinity and specificity towards α7-nAChR and are able to pass the blood-brain barrier (BBB).

2. 发明申请

WO2014111838A1 USE OF ALPHA 7 NICOTINIC ACETYLCHOLINE RECEPTOR AGONISTS 审中-公开
标题翻译：使用ALPHA 7 NICOTINIC乙酰胆碱受体激动剂
公开(公告)号：WO2014111838A1
公开(公告)日：2014-07-24
申请号：PCT/IB2014/058225
申请日：2014-01-13
申请人： NOVARTIS AG , FENDT, Markus , FEUERBACH, Dominik , FINNEMA, Sjoerd Johannes , HALLDIN, Christer , JOHNS, Donald , LOPEZ-LOPEZ, Cristina , MCALLISTER, Kevin Hall , SOVAGO, Judit , WEISS, Markus
发明人： FENDT, Markus , FEUERBACH, Dominik , FINNEMA, Sjoerd Johannes , HALLDIN, Christer , JOHNS, Donald , LOPEZ-LOPEZ, Cristina , MCALLISTER, Kevin Hall , SOVAGO, Judit , WEISS, Markus
IPC分类号： A61K31/501 , A61K31/506 , A61K31/55 , A61K31/4545 , A61P43/00
CPC分类号： A61K31/4545 , A61K31/501 , A61K31/506 , A61K31/55
摘要： The invention concerns the use of certain alpha 7 nicotinic acetylcholine receptor agonist for the facilitation of emergence from general anesthesia.
摘要翻译：本发明涉及某些α7烟碱乙酰胆碱受体激动剂用于促进全身麻醉的出现。

3. 发明申请

WO2012052409A1 COMPOUNDS FOR USE IN IMAGING, DIAGNOSING AND/OR TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM 审中-公开
标题翻译：用于成像，诊断和/或治疗中枢神经系统疾病的化合物
公开(公告)号：WO2012052409A1
公开(公告)日：2012-04-26
申请号：PCT/EP2011/068124
申请日：2011-10-17
申请人： Bayer Pharma Aktiengesellschaft , THIELE, Andrea , KETTSCHAU, Georg , HEINRICH, Tobias , LEHMANN, Lutz , HALLDIN, Christer , NAG, Sangram , VARRONE, Andrea , GULYAS, Balazs
发明人： THIELE, Andrea , KETTSCHAU, Georg , HEINRICH, Tobias , LEHMANN, Lutz , HALLDIN, Christer , NAG, Sangram , VARRONE, Andrea , GULYAS, Balazs
IPC分类号： C07B59/00 , C07C209/16 , C07C211/29
CPC分类号： A61K51/04 , C07B59/001 , C07C211/29
摘要： This invention relates to novel compounds suitable as precursors for the preparation of certain 18 F labelled positron emission tomography (PET) tracers. Furthermore, the invention relates to the preparation of such precursor molecules and to the preparation of PET tracers by 18 F labelling of such precursors.
摘要翻译：本发明涉及适用于制备某些18F标记的正电子发射断层扫描（PET）示踪剂的前体的新化合物。此外，本发明涉及这种前体分子的制备和通过18F标记这些前体制备PET示踪剂。

4. 发明申请

WO2013027845A1 RADIOLABELED COMPOUNDS AND THEIR USE AS RADIOTRACERS FOR QUANTITATIVE IMAGING OF PHOSPHODIESTERASE (PDE10A) IN MAMMALS 审中-公开
标题翻译：无机化合物及其作为放射性分子的用途，用于定量成像磷脂酰胆碱（PDE10A）
公开(公告)号：WO2013027845A1
公开(公告)日：2013-02-28
申请号：PCT/JP2012/071523
申请日：2012-08-21
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , TANIGUCHI, Takahiko , MIURA, Shotaro , HASUI, Tomoaki , HALLDIN, Christer , STEPANOV, Vladimir , TAKANO, Akihiro
发明人： TANIGUCHI, Takahiko , MIURA, Shotaro , HASUI, Tomoaki , HALLDIN, Christer , STEPANOV, Vladimir , TAKANO, Akihiro
IPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D498/08 , A61K31/501 , A61K51/04
CPC分类号： A61K51/0459 , A61K51/0463 , A61K51/0468 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D498/08
摘要： The present invention provides radiolabeled compounds useful as radiotracers for quantitative imaging of PDE10A in mammals. The compound of the present invention is represented by the formula (I): wherein each symbols are as defined in the specification.
摘要翻译：本发明提供了用作放射性示踪剂的放射性标记化合物，用于哺乳动物中PDE10A的定量成像。本发明的化合物由式（I）表示：其中每个符号如说明书中所定义。

5. 发明申请

WO2012126913A1 COMPOUNDS FOR USE IN IMAGING, DIAGNOSING AND/OR TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM 审中-公开
标题翻译：用于成像，诊断和/或治疗中枢神经系统疾病的化合物
公开(公告)号：WO2012126913A1
公开(公告)日：2012-09-27
申请号：PCT/EP2012/054917
申请日：2012-03-20
申请人： PIRAMAL IMAGING SA , THIELE, Andrea , KETTSCHAU, Georg , HEINRICH, Tobias , LEHMANN, Lutz , HALLDIN, Christer , NAG, Sangram , VARRONE, Andrea , GULYÁS, Balazs
发明人： THIELE, Andrea , KETTSCHAU, Georg , HEINRICH, Tobias , LEHMANN, Lutz , HALLDIN, Christer , NAG, Sangram , VARRONE, Andrea , GULYÁS, Balazs
IPC分类号： C07C211/41 , C07C209/68
CPC分类号： A61K49/0004 , A61K51/04 , A61K51/0406 , C07B2200/05 , C07C211/41 , C07C211/42 , C07C307/02 , C07C2602/08 , C07D291/08
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扫描（PET）进行诊断成像的组合物或试剂盒。

6. 发明申请

WO2009140210A2 RADIOTRACERS FOR IMAGING CANNABINOID SUB-TYPE1 (CB1) RECEPTOR 审中-公开
标题翻译：用于成像CANNABINOID亚型1（CB1）受体的放射线吸收剂
公开(公告)号：WO2009140210A2
公开(公告)日：2009-11-19
申请号：PCT/US2009/043491
申请日：2009-05-11
申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY OF THE DEPARTMENT OF HEALTH AND HUMAN SERVICES , PIKE, Victor, W. , DONOHUE, Sean, R. , HALLDIN, Christer
发明人： PIKE, Victor, W. , DONOHUE, Sean, R. , HALLDIN, Christer
IPC分类号： A61K51/04
CPC分类号： A61K51/0455 , A61K51/0453
摘要： Imaging of cannabinoid subtype-1 (CB 1 ) receptors in vivo is important for understanding their role in neuropsychiatric disorders and for drug development. Radioligands for imaging with PET or SPECT are required for this purpose. The present invention provides new ligands, including (-)-3-(4-chlorophenyl)-N'-[(4-cyanophenyl)sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamidine) and 1-(2-iodophenyl)-4-cyano-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxylate, which were found to have high affinity and selectivity for binding to CB1 receptors. These compounds were labeled and evaluated as a PET and SPECT radioligands for use in mammals. After injection of [ 11 C] (-)-3-(4-chlorophenyl)-N'-[(4-cyanophenyl)sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamidine) into mammals, high uptake and retention of radioactivity across brain according to the rank order of CB 1 receptor densities was observed. Likewise 125 I-labeled 1-(2-iodophenyl)-4-cyano-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxylate showed a distinct regional distribution of radioactivity in brain tissue according to the known CB 1 receptor densities. Ligands of the present invention are useful for in vivo imaging CB 1 receptor function in mammals.
摘要翻译：在体内成像大麻素亚型1（CB1）受体对于了解其在神经精神障碍和药物开发中的作用是重要的。为此，需要使用PET或SPECT进行成像的放射性配体。本发明提供了新的配体，包括（ - ） - 3-（4-氯苯基）-N' - [（4-氰基苯基）磺酰基] -4-苯基-4,5-二氢-1H-吡唑-1-甲脒）和1-（2-碘苯基）-4-氰基-5-（4-甲氧基苯基）-N-（哌啶-1-基）-1H-吡唑-3-羧酸甲酯，发现它们具有高的结合亲和力和选择性到CB1受体。这些化合物被标记和评估为用于哺乳动物的PET和SPECT放射性配体。将[11C]（ - ） - 3-（4-氯苯基）-N' - [（4-氰基苯基）磺酰基] -4-苯基-4,5-二氢-1H-吡唑-1-甲脒注射入哺乳动物观察到根据CB1受体密度的等级顺序，大脑中放射性的摄取和保留率高。同样地，125 I-标记的1-（2-碘苯基）-4-氰基-5-（4-甲氧基苯基）-N-（哌啶-1-基）-1H-吡唑-3-羧酸乙酯显示在脑中放射性的区别分布根据已知的CB1受体密度组织。本发明的配体可用于哺乳动物体内成像CB1受体功能。

7. 发明申请

WO2009052970A3 COMPOUNDS FOR USE IN IMAGING, DIAGNOSING, AND/OR TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM OR OF TUMORS 审中-公开
公开(公告)号：WO2009052970A3
公开(公告)日：2009-04-30
申请号：PCT/EP2008/008668
申请日：2008-10-14
申请人： BAYER SCHERING PHARMA AKTIENGESELLSCHAFT , LEHMANN, Lutz , THIELE, Andrea , HEINRICH, Tobias , BRUMBY, Thomas , HALLDIN, Christer , GULYAS, Balazs , NAG, Sangram
发明人： LEHMANN, Lutz , THIELE, Andrea , HEINRICH, Tobias , BRUMBY, Thomas , HALLDIN, Christer , GULYAS, Balazs , NAG, Sangram
IPC分类号： C07B59/00 , C07D307/52 , A61K31/135 , A61P43/00 , C07C309/66
摘要： This invention relates to novel compounds suitable for labelling or already labelled by 18 F, methods of preparing such a compound, 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).

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