公开(公告)号：US4913891A

公开(公告)日：1990-04-03

申请号：US52921

申请日：1987-05-22

申请人： Joanna S. Fowler ,  Robert R. MacGregor ,  Alfred P. Wolf ,  Bengt Langstrom

发明人： Joanna S. Fowler ,  Robert R. MacGregor ,  Alfred P. Wolf ,  Bengt Langstrom

IPC分类号： A61K51/04

CPC分类号： A61K51/0406 ,  A61K2123/00

摘要： This invention involves a new strategy for imaging and mapping enzyme activity in the living human and animal body using positron emitter-labeled suicide enzyme inactivators or inhibitors which become covalently bound to the enzyme as a result of enzymatic catalysis. Two such suicide inactivators for monoamine oxidase have been labeled with carbon-11 and used to map the enzyme subtypes in the living human and animal body using PET. By using positron emission tomography to image the distribution of radioactivity produced by the body penetrating radiation emitted by carbon-11, a map of functionally active monoamine oxidase activity is obtained. Clorgyline and L-deprenyl are suicide enzyme inhibitors and irreversibly inhibit monoamine oxidase. When these inhibitors are labeled with carbon-11 they provide selective probes for monoamine oxidase localization and reactivity in vivo using positron emission tomography.

摘要翻译： 本发明涉及使用正电子发射体标记的自杀酶灭活剂或由于酶促催化而与酶共价结合的抑制剂在活的人和动物体中成像和测定酶活性的新策略。 已经用碳-11标记了两种用于单胺氧化酶的这种自杀灭活剂，并且用于使用PET对活的人和动物体中的酶亚型进行映射。 通过使用正电子发射断层扫描来对由碳-11发射的身体穿透辐射产生的放射性分布进行成像，获得功能活性单胺氧化酶活性的图谱。 Clorgyline和L-去肾上腺素是自杀性酶抑制剂，并且不可逆地抑制单胺氧化酶。 当这些抑制剂用碳-11标记时，它们使用正电子发射断层扫描为体内单胺氧化酶定位和反应性提供选择性探针。

公开(公告)号：US4617386A

公开(公告)日：1986-10-14

申请号：US488311

申请日：1983-04-25

申请人： David R. Elmaleh ,  Shlomo Levy ,  Chyng-Yann Shiue ,  Alfred P. Wolf

发明人： David R. Elmaleh ,  Shlomo Levy ,  Chyng-Yann Shiue ,  Alfred P. Wolf

IPC分类号： C07H5/02 ,  C07H15/04 ,  C07H1/00

CPC分类号： C07H5/02 ,  C07H15/04

摘要： Process for the production of 2-deoxy-2-fluoro-D-glucose and the corresponding .sup.18 F-compound in which methyl 4,6-O-benzylidine-3-O-methyl-2-O-trifluoromethanesulfonyl-.beta.-D-mannopyranoside is reacted with a triflating reagent, the resulting compound reacted with CsHF.sub.2, RbF or the corresponding .sup.18 F-compounds, and thereafter the alkyl groups removed by hydrolysis.

摘要翻译： 制备2-脱氧-2-氟-D-葡萄糖的方法和相应的18F-化合物，其中甲基4,6-O-亚苄基-3-O-甲基-2-O-三氟甲磺酰基-β-D-吡喃甘露糖苷 与三氟甲烷试剂反应，所得化合物与CsHF 2，RbF或相应的18 F化合物反应，然后通过水解除去烷基。

公开(公告)号：USH74H

公开(公告)日：1986-06-03

申请号：US469597

申请日：1983-02-24

申请人： Chyng-Yann Shiue ,  Piero A. Salvadori ,  Alfred P. Wolf ,  Joanna S. Fowler ,  Robert R. MacGregor

发明人： Chyng-Yann Shiue ,  Piero A. Salvadori ,  Alfred P. Wolf ,  Joanna S. Fowler ,  Robert R. MacGregor

IPC分类号： C07H5/02

CPC分类号： C07H5/02

摘要： Process for the production of 2-deoxy-2-fluoro-D-glucose and the corresponding .sup.18 F-compound by the reaction of acetyl hypofluorite or the corresponding .sup.18 F-compound with 3,4,6-tri-O-acetyl-D-glucal followed by hydrolysis. Process includes the production of the hypofluorite compound at ambient temperature.

公开(公告)号：US4436717A

公开(公告)日：1984-03-13

申请号：US268422

申请日：1981-05-29

申请人： Chyng-Yann Shiue ,  Alfred P. Wolf

发明人： Chyng-Yann Shiue ,  Alfred P. Wolf

IPC分类号： A61K51/04 ,  A61K43/00 ,  A61K49/00

CPC分类号： A61K51/0453 ,  A61K2123/00

摘要： The novel radioactive compound .sup.18 F-4-fluoroantipyrine having high specific activity which can be used in nuclear medicine in diagnostic applications, prepared by the direct fluorination of antipyrine in acetic acid with radioactive fluorine at room temperature and purifying said radioactive compound by means of gel chromatography with ethyl acetate as eluent is disclosed. The non-radioactive 4-fluoroantipyrine can also be prepared by the direct fluorination of antipyrine in acetic acid with molecular fluorine at room temperature and purified by means of gel chromotography with ethyl acetate eluent.

摘要翻译： 在诊断应用中可用于核医学中的具有高比活性的新型放射性化合物18F-4-氟替平吡啶，其通过在室温下用放射性氟在乙酸中直接氟化安替比林并通过凝胶色谱法纯化所述放射性化合物 公开了乙酸乙酯作为洗脱剂。 非放射性4-氟替苯胺也可以通过在室温下用分配氟在乙酸中直接氟化安替比林并通过乙酸乙酯洗脱液的凝胶色谱法纯化来制备。

公开(公告)号：US4011307A

公开(公告)日：1977-03-08

申请号：US692625

申请日：1976-06-03

申请人： Richard M. Lambrecht ,  Samuel Packer ,  Jerald C. Merrill ,  Harold L. Atkins ,  Alfred P. Wolf ,  Patrick R. Bradley-Moore

发明人： Richard M. Lambrecht ,  Samuel Packer ,  Jerald C. Merrill ,  Harold L. Atkins ,  Alfred P. Wolf ,  Patrick R. Bradley-Moore

IPC分类号： A61K51/04 ,  G21G1/10 ,  G21H5/02 ,  A61K29/00 ,  A61K43/00 ,  G01T1/161

CPC分类号： G21H5/02 ,  A61K51/0478 ,  G21G1/10 ,  A61K2123/00

摘要： .sup.203 Pb-tris complex injected for use in the detection and localization of tumors. The lead-203 is produced from the deuteron bombardment of a thallium target and chemically separated from the thallium. The tris is added which complexes with the lead-203.

公开(公告)号：US4252668A

公开(公告)日：1981-02-24

申请号：US14179

申请日：1979-02-22

申请人： Richard M. Lambrecht ,  Alfred P. Wolf

发明人： Richard M. Lambrecht ,  Alfred P. Wolf

IPC分类号： A61K51/02 ,  A61K51/12 ,  G21G1/10

CPC分类号： G21G1/10 ,  A61K51/02 ,  A61K51/121 ,  A61K51/1282 ,  A61K2123/00 ,  F16D2001/062

摘要： A solution of potassium-38 suitable for use as a radiopharmaceutical and a method for its production. Argon is irradiated with protons having energies above the threshold for the .sup.40 Ar(p,3n).sup.38 K reaction. The resulting potassium-38 is dissolved in a sterile water and any contaminating chlorine-38 is removed.

摘要翻译： 适合用作放射性药物的一种钾38的溶液及其生产方法。 用能量超过40Ar（p，3n）38K反应阈值的质子照射氩。 将所得的钾38溶于无菌水中，并除去任何污染的氯-38。

公开(公告)号：US5254726A

公开(公告)日：1993-10-19

申请号：US711684

申请日：1991-06-07

申请人： Yu-Shin Ding ,  Joanna S. Fowler ,  Alfred P. Wolf

发明人： Yu-Shin Ding ,  Joanna S. Fowler ,  Alfred P. Wolf

IPC分类号： C07C215/28 ,  C07C229/36 ,  C07D317/62 ,  C07C229/42 ,  C07C47/52 ,  C07C213/08

CPC分类号： C07C229/36 ,  C07C215/28 ,  C07D317/62

摘要： A method for synthesizing no-carrier-added (NCA) aryl [.sup.18 F] fluoride substituted aromatic aldehyde compositions bearing an electron donating group is described. The method of the present invention includes the step of reacting aromatic nitro aldehydes having a suitably protected hydroxyl substitutent on an electron rich ring. The reaction isThe U.S. Government has rights in this invention pursuant to Contract Number DE-AC02-76CH00016, between the U.S. Department of Energy and Associated Universities Inc.

摘要翻译： 描述了一种合成具有给电子基团的无载体添加（NCA）芳基[18 F]氟取代的芳族醛组合物的方法。 本发明的方法包括使具有适当保护的羟基取代基的芳族硝基醛与富电子环反应的步骤。 该反应通过亲核芳族取代通过无载体添加（NCA）[18F]氟离子进行。 本发明的方法可用于合成各种无载体添加的芳基[18 F]氟化物组合物，包括6- [18 F]氟-L-多巴，2- [18 F]氟酪氨酸，6- [18 F]氟去甲肾上腺素， 和6- [18F]氟代多巴胺。 在通过本发明产生对映异构体的外消旋混合物的情况下，例如在6- [18 F]氟去甲肾上腺素的合成中，优选的方法还包括在手性HPLC柱上拆分外消旋混合物。 该方法导致高产率的对映体纯的[18 F]标记的异构体，例如[ - ] - 6- [18 F]氟去甲肾上腺素和[+] - 6- [18F]氟去甲肾上腺素。

公开(公告)号：USH1209H

公开(公告)日：1993-07-06

申请号：US784149

申请日：1985-10-04

申请人： Chyng-Yann Shiue ,  Joanna S. Fowler ,  Alfred P. Wolf

发明人： Chyng-Yann Shiue ,  Joanna S. Fowler ,  Alfred P. Wolf

IPC分类号： A61K51/04

CPC分类号： A61K51/0455 ,  A61K2123/00

摘要： There is disclosed a radioligand labeled with a positron emitting radionuclide suitable for dynamic study in living humans with positron emission transaxial tomography. [.sup.18 F]-N-methylspiroperidol, exhibiting extremely high affinity for the dopamine receptors, provides enhanced uptake and retention in the brain concomitant with reduced radiation burden. These characteristics all combine to provide [.sup.18 F]-N-methylspiroperidol as a radioligand superior to known radioligands for mapping dopamine receptors in normal and disease states in the living brain. Additionally, a new synthetic procedure for this material is disclosed.

公开(公告)号：US4874600A

公开(公告)日：1989-10-17

申请号：US853105

申请日：1986-04-17

申请人： Daniel W. McPherson ,  Joanna S. Fowler ,  Alfred P. Wolf

发明人： Daniel W. McPherson ,  Joanna S. Fowler ,  Alfred P. Wolf

IPC分类号： A61K51/04

CPC分类号： A61K51/0406 ,  A61K2123/00

摘要： The invention relates to a new radiolabeled imaging agent, no-carrier-added [1-.sup.11 C]putrescine, and to the use of this very pure material as a radiotracer with positron emission tomography for imaging brain tumors. The invention further relates to the synthesis of no-carrier-added [1-.sup.11 C]putrescine based on the Michael addition of potassium .sup.11 C-labeled cyanide to acrylonitrile followed by reduction of the .sup.11 C-labeled dinitrile. The new method is rapid and efficient and provides radiotracer with a specific activity greater than 1.4 curies per millimol and in a purity greater than 95%.

摘要翻译： 本发明涉及一种新的放射性标记成像剂，无载体添加的[1-11C]腐胺，以及使用这种非常纯的材料作为放射性示踪剂，具有用于成像脑肿瘤的正电子发射断层扫描。 本发明还涉及基于将11C标记的氰化钾向丙烯腈中迈克尔加成，然后还原11C-标记的二腈，合成无载体添加的[1-11C]腐胺。 新方法快速有效，并提供具有大于1.4百分点/毫摩尔的比活性的放射性示踪剂，纯度大于95％。

公开(公告)号：US4871527A

公开(公告)日：1989-10-03

申请号：US43824

申请日：1987-04-29

申请人： Chyng-Yann Shiue ,  Alfred P. Wolf ,  Lan-Qin Bai ,  Ren-Tui Teng

发明人： Chyng-Yann Shiue ,  Alfred P. Wolf ,  Lan-Qin Bai ,  Ren-Tui Teng

IPC分类号： A61K51/04

CPC分类号： C07B59/002 ,  A61K51/0455 ,  A61K2123/00

摘要： There is disclosed radioligands labeled with the position emitting radionuclide [.sup.18 F] suitable for dynamic study in living humans with position emission transaxial tomography. These new [.sup.18 F]-N-fluoroalkylspiroperidols, wherein the alkyl group contains from 2-6 carbon atoms, exhibit extremely high affinity for the dopamine receptors and provide enhanced uptake and retention in the brain concomitant with reduced radiation burden. These characteristics all combine to make these new radioligands useful for mapping dopamine receptors in normal and disease states in the living brain. Additionally, a new synthetic procedure for these radioligands as well as a new procedure for preparing the radiolabeled alkyl halide alkylating reagents are also disclosed.

摘要翻译： 公开了放射性核素标记的放射性核素[18F]的位置，适用于活体位置发射横轴断层扫描的动态研究。 这些新的[18 F] -N-氟烷基螺环脂醇，其中烷基含有2-6个碳原子，对多巴胺受体表现出非常高的亲和力，并且随着减少的辐射负担而提供增强的大脑摄取和保留。 这些特征都结合起来，使这些新的放射性配体可用于在活体大脑的正常和疾病状态下测定多巴胺受体。 此外，还公开了这些放射性配体的新合成方法以及制备放射性标记的烷基卤烷基化试剂的新方法。