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    • 5. 发明申请
    • Imaging Agents
    • 成像剂
    • US20070082879A1
    • 2007-04-12
    • US11425078
    • 2006-06-19
    • Mark Goodman
    • Mark Goodman
    • A61K31/397A61K31/337A61K31/38A61K31/335
    • C07C229/48A61K51/0402A61K51/0406C07B59/001C07C2601/04C07D291/04C07D345/00C07F13/005
    • The present invention provides novel amino acid compounds useful in detecting and evaluating brain and body tumors. These compounds have the advantageous properties of rapid uptake and prolonged retention in tumors and can be labeled with halogen isotopes such as fluorine-18, iodine-123, iodine-124, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77, bromine-82, astatine-210, astatine-211, and other astatine isotopes. These compounds can also be labeled with technetium and rhenium isotopes using known chelation complexes. The compounds disclosed herein bind tumor tissues in vivo with high specificity and selectivity when administered to a subject. Preferred compounds show a target to non-target ratio of at least 2:1, are stable in vivo and substantially localized to target within 1 hour after administration. Preferred compounds include 1-amino-2-[18F]fluorocyclobutyl-1-carboxylic acid (2-[18F]FACBC) and 1-amino-2-[18F]fluoromethylcyclobutyl-1-carboxylic acid (2-[18F]FMACBC). The labeled amino acid compounds of the invention are useful as imaging agents in detecting and/or monitoring tumors in a subject by PET or SPECT.
    • 本发明提供了可用于检测和评估脑和体肿瘤的新型氨基酸化合物。 这些化合物具有在肿瘤中快速吸收和延长保留的有利特性,并可用卤素同位素如氟-18,碘-123,碘-124,碘-125,碘-131,溴-75,溴-76 ,溴-77,溴-82,ast ine -21,ast ine -211和其他ast同位素。 这些化合物也可以使用已知的螯合络合物用锝和铼同位素标记。 当给予受试者时,本文所公开的化合物以高特异性和选择性在体内结合肿瘤组织。 优选的化合物显示至少2:1的目标与非目标比例,在给药后1小时内在体内是稳定的并且基本上定位于靶标上。 优选的化合物包括1-氨基-2 - [[18 F]氟代环丁基-1-羧酸(2 - [(18 F)FACBC))和1-氨基-2- [ F]氟甲基环丁基-1-羧酸(2- [叔丁基] FMACBC))。 本发明的标记氨基酸化合物可用作通过PET或SPECT检测和/或监测受试者的肿瘤的成像剂。
    • 6. 发明授权
    • Ultrasonic leak detecting apparatus
    • 超声波检漏仪
    • US5955670A
    • 1999-09-21
    • US749910
    • 1996-11-15
    • Mark GoodmanJohn R. Zeno, deceasedLinda Mabbs, executrix
    • Mark GoodmanJohn R. Zeno, deceasedLinda Mabbs, executrix
    • G01N29/04F16C17/24F16N3/12F16N21/00F16N29/02G01H1/08G01M3/24G01N29/032G01N29/14G01N29/36H04B1/26G01H17/00G01N29/12
    • F16C33/6625F16N29/02G01H1/08G01N29/032G01N29/14G01N29/36G01N2291/015G01N2291/0226H04B1/26
    • An ultrasonic leak detector with a wide dynamic bandwidth and repeatable fixed attenuation reference points includes a transducer which receives ultrasonic energy and converts it into an electrical output signal related in intensity and frequency to the received ultrasonic energy. A high gain charge preamplifier is connected to the transducer and generates an amplified version of the transducer's electrical output signal. The amplified signal is then passed through a multi-level logarithmic attenuator having at least one fixed attenuation reference point to create an attenuated version of the detected and amplified ultrasonic signal. The output of the logarithmic attenuator is connected to a frequency shift circuit which converts the ultrasonic frequency signal into an audio frequency signal related in magnitude and frequency to the attenuated signal. The audio frequency signal is then amplified by an audio amplifier and used to drive a signal level indicator which provides an indication of the magnitude of the amplified output signal. The detector may be used with a lubrication tool to determine the amount of lubrication applied to a sealed mechanical device, such as a bearing, by detecting the decrease in received ultrasonic energy as the lubrication reaches the device. The detector may also be used to detect the increase in ultrasonic energy associated with pending mechanical failure.
    • 具有宽动态带宽和可重复的固定衰减参考点的超声波泄漏检测器包括接收超声能量并将其转换为与所接收的超声波能量相关的电输出信号的换能器。 高增益电荷前置放大器连接到换能器,并产生传感器的电气输出信号的放大版本。 放大的信号然后通过具有至少一个固定衰减参考点的多电平对数衰减器,以产生检测和放大的超声波信号的衰减版本。 对数衰减器的输出连接到频移电路,该频移电路将超声波频率信号转换成与衰减信号相关的音频和频率的音频信号。 音频信号然后被音频放大器放大,并用于驱动提供放大的输出信号幅度的指示的信号电平指示器。 检测器可以与润滑工具一起使用,以通过检测在润滑到达设备时接收到的超声能量的减少来确定施加到密封的机械装置(例如轴承)上的润滑量。 检测器也可用于检测与待机械故障相关联的超声能量的增加。
    • 10. 发明申请
    • Tumor imaging compounds
    • 肿瘤成像化合物
    • US20050192458A1
    • 2005-09-01
    • US10507221
    • 2003-04-24
    • Mark GoodmanJonathan McConathy
    • Mark GoodmanJonathan McConathy
    • G01T1/161A61K51/00A61K51/04C07C229/20C07C229/22C07F13/00C07C61/00C07C61/08
    • C07F13/005A61K51/04A61K51/0478A61K51/0487C07B2200/05C07C229/20C07C229/22
    • The invention provides novel amino acid compounds of use in detecting and evaluating brain and body tumors. These compounds combine the advantageous properties of α-aminoisobutyric acid (AIB) analogs namely, their rapid uptake and prolonged retention in tumors with the properties of halogen sustituents, including certain useful halogen isotopes such as fluorine-18, iodine-123, iodine-124, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77, bromine-82, astatine-210, astatine-211, and other astatine isotopes. In addition the compounds can be labeled with technetium and rhenium isotopes using known chelation complexes. The amino acid compounds disclosed herein have a high specificity for target sites when administered to a subject in vivo. Preferred amino acid compounds include [18F] FAMP, ([18F]5a) and [18F]N-MeFAMP, ([18F]5b). The invention further features pharmaceutical compositions comprised of an α-amino acid moiety attached to eiher a four, five or a six member carbon-chain ring. The labeled amino acid compounds are useful as imaging agents in detecting and/or monitoring tumors in a subject by Positron Emission Tomography (PET) and Single Photon Emission Computer Tomography (SPECT).
    • 本发明提供了用于检测和评价脑和体肿瘤的新型氨基酸化合物。 这些化合物结合了α-氨基异丁酸(AIB)类似物的有利性质,即它们在肿瘤中的快速摄取和延长的保留性,其具有卤素支持物质的性质,包括某些有用的卤素同位素如氟-18,碘-123,碘-124 ,碘-125,碘-131,溴-75,溴-76,溴-77,溴-82,ast ine -21,ast ine -211和其他ast同位素。 此外,化合物可以使用已知的螯合络合物用锝和铼同位素标记。 当在体内施用于受试者时,本文公开的氨基酸化合物对靶位点具有高特异性。 优选的氨基酸化合物包括[[SUP] 18F] FAMP,([[18 F] 5a)和[ - 18 F] N-MeFAMP,([ F)5b)。 本发明进一步包括由连接四个,五个或六个碳链环的更多的α-氨基酸部分组成的药物组合物。 标记的氨基酸化合物可用作通过正电子发射断层扫描(PET)和单光子发射计算机断层扫描(SPECT)检测和/或监测受试者的肿瘤的成像剂。