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公开(公告)号：US6060038A
公开(公告)日：2000-05-09
申请号：US74346
申请日：1998-05-07
申请人： Hugh D. Burns , Wai-Si Eng , Raymond E. Gibson
发明人： Hugh D. Burns , Wai-Si Eng , Raymond E. Gibson
IPC分类号： C07D403/06 , A61K31/496 , A61K51/00 , A61K51/04 , C07D233/56 , C12Q1/48 , C07D241/00
CPC分类号： C12Q1/48 , A61K51/0459 , C07D403/06 , A61K2123/00
摘要： The present invention is directed toward radiolabeled farnesyl-protein transferase inhibitor compounds which are useful to label FPTase in assays, whether cell-based, tissue-based or in whole animal. The tracers can also be used in competitive binding assays to obtain information on the interaction of unlabeled FTIs with FPTase.
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公开(公告)号：US07354935B2
公开(公告)日：2008-04-08
申请号：US10528888
申请日：2003-09-19
IPC分类号： A61K31/445 , C07D401/12
CPC分类号： C07D401/12
摘要： The present invention is directed to radiolabeled neurokinin-1 receptor antagonists which are useful for the labeling and diagnostic imaging of neurokinin-1 receptors in mammals.
摘要翻译： 本发明涉及放射性标记的神经激肽-1受体拮抗剂，其可用于哺乳动物中神经激肽-1受体的标记和诊断成像。
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公开(公告)号：US06458935B1
公开(公告)日：2002-10-01
申请号：US09668637
申请日：2000-06-12
IPC分类号： C07D40304
CPC分类号： C12Q1/48 , A61K51/0459 , C07D233/64
摘要： The present invention is directed toward radiolabeled farnesyl-protein transferase inhibitor compounds which are useful to label FPTase in assays, whether cell-based, tissue-based or in whole animal. The tracers can also be used in competitive binding assays to obtain information on the interaction of unlabeled FTIs with FPTase.
摘要翻译： 本发明涉及放射性标记的法呢基 - 蛋白转移酶抑制剂化合物，其用于在测定中标记FPTase，无论是基于细胞的，基于组织的还是在整个动物中。 示踪剂也可用于竞争性结合测定中以获得关于未标记的FTI与FPTase的相互作用的信息。
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公开(公告)号：US4994258A
公开(公告)日：1991-02-19
申请号：US488192
申请日：1990-03-05
IPC分类号： A61K51/00 , A61K51/04 , C07D243/16 , C07D243/18 , C07D243/24 , C07D403/12
CPC分类号： C07D243/24 , A61K51/047
摘要： Novel radiolabeled cholecystokinin-A (CCK-A) antagonists have been developed which, after intravenous injection, localize in the pancreas as a result of specific binding to CCK-A receptors. These tracers, when labeled with appropriate radiohalogens, are useful as commercial diagnostic imaging radiopharmaceuticals and radiotherapeutic drugs.
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5.发明授权3-quinuclidinol esters, useful as antagonists of muscarinic acetylcholine receptors 失效3-奎宁环酯，可用作毒蕈碱乙酰胆碱受体的拮抗剂
公开(公告)号：US4644003A
公开(公告)日：1987-02-17
申请号：US719405
申请日：1985-04-03
IPC分类号： C07D453/02 , A61K31/435
CPC分类号： C07D453/02
摘要： The present invention relates to antagonists of muscarinic acetylcholine receptors. More specifically, this invention contemplates highly selective antimuscarinic agents which are characterized as esters of 3-quinuclidinol and unsymmetrical alpha-disubstituted glycolic acids.These highly selective antimuscarinic agents permit efficacy at particular sites designated m.sub.1 -AChR without affecting the muscarinic acetylcholine receptors of other tissues characterized by sites designated m.sub.2 -AChR. Such efficacy requires lower quantities of the antagonist thereby lowering toxicity and other undesirable side effects.
摘要翻译： 本发明涉及毒蕈碱性乙酰胆碱受体的拮抗剂。 更具体地，本发明考虑了高选择性抗毒蕈碱剂，其特征为3-奎宁环醇和不对称的α-二取代的乙醇酸的酯。 这些高度选择性的抗毒蕈碱剂允许在指定为m1-AChR的特定位点的功效，而不影响特征为m2-AChR的位点的其他组织的毒蕈碱性乙酰胆碱受体。 这种功效需要较少量的拮抗剂，从而降低毒性和其它不期望的副作用。
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公开(公告)号：US07754188B2
公开(公告)日：2010-07-13
申请号：US10559228
申请日：2004-06-25
申请人： H. Donald Burns , Alex M. Chen , Raymond E. Gibson , Mark T. Goulet , William K. Hagmann , Terence G. Hamill , James P. Jewell , Linus S. Lin , Ping Liu , Andrey V. Peresypkin
发明人： H. Donald Burns , Alex M. Chen , Raymond E. Gibson , Mark T. Goulet , William K. Hagmann , Terence G. Hamill , James P. Jewell , Linus S. Lin , Ping Liu , Andrey V. Peresypkin
CPC分类号： C07D213/64 , A61K51/0406 , A61K51/0455 , A61K51/0459 , C07D239/34
摘要： The present invention relates to particular radiolabeled Cannabinoid-1 (CB1) receptor modulators, and methods of using these modulators for labeling and diagnostic imaging of Cannabinoid-1 receptors in mammals, particularly humans. In addition, intermediates useful for the synthesis of the radiolabeled Cannabinoid-1 receptor modulators are also disclosed, as well as the processes for synthesizing the radiolabeled Cannabinoid-1 receptor modulators. Still further, formulations of the radiolabeled Cannabinoid-1 receptor compounds are described.
摘要翻译： 本发明涉及特定的放射性标记的大麻素-1（CB1）受体调节剂，以及使用这些调节剂用于哺乳动物，特别是人类中大麻素-1受体的标记和诊断成像的方法。 此外，还公开了可用于合成放射性标记的大麻素-1受体调节剂的中间体，以及合成放射性标记的大麻素-1受体调节剂的方法。 此外，描述了放射性标记的大麻素-1受体化合物的制剂。
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7.发明授权Gamma-emitting receptor-binding 3-quinuclidinyl glycolates; methods of preparation thereof and imaging and assay methods utilizing same 失效发光受体结合3-奎宁环酸乙二醇酯; 其制备方法和利用其的成像和测定方法
公开(公告)号：US4431627A
公开(公告)日：1984-02-14
申请号：US336340
申请日：1981-12-31
IPC分类号： A61K51/00 , A61K51/04 , C07D453/00 , C07D453/02 , G01N33/60 , A61K49/00 , A61K43/00 , G01N33/54
CPC分类号： C07D453/02 , A61K51/0455 , A61K51/0497 , G01N33/60 , A61K2123/00
摘要： Compounds of the formula: ##STR1## wherein R is aryl, alkyl, cycloalkyl, phenyl, cyclopentyl, cyclohexyl, a ligand containing Tc-99m in chelated form or a ligand capable of chelating Tc-99m;R.sub.1 is H or lower alkyl;X is in the ortho-, meta or para- position, and is selected from the group consisting of .sup.125 I, .sup.123 I, .sup.127 I, I, .sup.18 F, .sup.75 Br, .sup.77 Br, NH.sub.2, and ##STR2## wherein R.sub.2 is in the 2,3, or 4 position and is selected from the group consisting of H and lower alkyl, provided that when R is a ligand capable of chelating Tc-99m or containing Tc-99m in chelated form, X is not a radioisotope and may also be H or lower alkyl;Z.sup..crclbar. is an anion; or the free amine thereof; anddenotes an asymmetric carbon atom.
摘要翻译： 其中R为芳基，烷基，环烷基，苯基，环戊基，环己基，含有螯合形式的Tc-99m或能够螯合Tc-99m的配体的配体; R1是H或低级烷基; X是在邻位，间位或对位，并且选自125I，123I，127I，I，18F，75Br，77Br，NH2和其中R2在2,3， 或4位，并且选自H和低级烷基，条件是当R是能够螯合Tc-99m或含有螯合形式的Tc-99m的配体时，X不是放射性同位素，也可以是H或更低 烷基; Z（ - ）为阴离子; 或其游离胺; 并表示不对称碳原子。
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公开(公告)号：US06939966B2
公开(公告)日：2005-09-06
申请号：US10484551
申请日：2002-07-19
IPC分类号： G01T1/161 , A61K51/00 , A61K51/04 , C07D491/04 , C07D491/107 , C07D491/10 , A61K49/00
CPC分类号： C07D491/04 , A61K51/0459 , C07B2200/05
摘要： The present invention is directed to radiolabeled neuropeptide Y Y5 receptor antagonists which are useful for the labeling and diagnostic imaging of neuropeptide Y Y5 receptors in mammals.
摘要翻译： 本发明涉及放射性标记的神经肽Y Y5受体拮抗剂，其可用于哺乳动物中神经肽Y Y5受体的标记和诊断成像。
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公开(公告)号：US06241964B1
公开(公告)日：2001-06-05
申请号：US09407822
申请日：1999-09-28
IPC分类号： A61K5100
CPC分类号： C07D401/12 , A61K51/0455 , C07B59/002 , C07B2200/05 , Y10S436/804
摘要： The present invention is directed to radiolabeled neurokinin-1 receptor antagonists which are useful for the labeling and diagnostic imaging of neurokinin-1 receptors in mammals.
摘要翻译： 本发明涉及放射性标记的神经激肽-1受体拮抗剂，其可用于哺乳动物中神经激肽-1受体的标记和诊断成像。
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