Hetero-biaryl-pyridoquinazolinone derivatives as anti-cancer agents
    2.
    发明授权
    Hetero-biaryl-pyridoquinazolinone derivatives as anti-cancer agents 失效
    杂环芳基吡啶并喹唑啉酮衍生物作为抗癌剂

    公开(公告)号:US5908840A

    公开(公告)日:1999-06-01

    申请号:US965217

    申请日:1997-11-06

    CPC分类号: C07D471/04

    摘要: This invention provides a compound having the formula: ##STR1## wherein: (A) n=2-4;(B) R.sub.1 and R.sub.2 are the same or different and selected from the group consisting of H, (C.sub.1 -C.sub.3) alkyl, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 NH.sub.2, and --CH.sub.2 CH.sub.2 N(CH.sub.3).sub.2 or R.sub.1 and R.sub.2 are alkyl moieties which are taken together to form a 4- to 7- membered ring;(C) R.sub.3 is selected from the group consisting of H, --CH.sub.3, --CH.sub.2 CH.sub.3, and --CH.sub.2 CH.sub.2 NH.sub.2 ;(D) Y is a heterocyclic radical having 5-14 atoms, located at the 2- or 3- position of the pyridoquinazolinone nucleus, in which 1-3 of the heterocyclic ring atoms are independently nitrogen, oxygen, or sulfur; wherein Y may be optionally mono-, di-, or tri- substituted with --OR.sub.4, --NR.sub.5 R.sub.6, --CO.sub.2 H, --CO.sub.2 R.sub.4, or phenyl;R.sub.4 is H or (C.sub.1 -C.sub. 4) straight-chain alkyl;R.sub.5 and R.sub.6 are the same or different and are selected from the group consisting of H, (C.sub.1 -C.sub.4) straight-chain alkyl, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 NH.sub.2, and --CH.sub.2 CH.sub.2 N(CH.sub.3).sub.2 or R.sub.5 and R.sub.6 are alkyl moieties which are taken together to form a 4-7 membered ring;or a pharmaceutically acceptable salt thereof which is useful as an antineoplastic agent.

    摘要翻译: 本发明提供具有下式的化合物:其中:(A)n = 2-4; (B)R 1和R 2相同或不同,选自H,(C 1 -C 3)烷基,-CH 2 CH 2 OH,-CH 2 CH 2 NH 2和-CH 2 CH 2 N(CH 3)2或R 1和R 2为被取代的烷基部分 一起形成4-至7-元环; (C)R 3选自H,-CH 3,-CH 2 CH 3和-CH 2 CH 2 NH 2; (D)Y是位于吡啶并喹啉酮核的2-或3-位的具有5-14个原子的杂环基,其中1-3个杂环环原子独立地是氮,氧或硫; 其中Y可任选被-OR 4,-NR 5 R 6,-CO 2 H,-CO 2 R 4或苯基单,二或三取代; R4是H或(C1-C4)直链烷基; R5和R6相同或不同,选自H,(C1-C4)直链烷基,-CH2CH2OH,-CH2CH2NH2和-CH2CH2N(CH3)2或R5和R6是烷基部分,它们是 一起形成4-7元环; 或其药学上可接受的盐,其可用作抗肿瘤剂。

    Biaryl-pyridoquinazolinone derivatives as anti-cancer agents
    3.
    发明授权
    Biaryl-pyridoquinazolinone derivatives as anti-cancer agents 失效
    二芳基吡啶并喹唑啉酮衍生物作为抗癌剂

    公开(公告)号:US5914327A

    公开(公告)日:1999-06-22

    申请号:US965552

    申请日:1997-11-06

    CPC分类号: C07D471/04

    摘要: This invention provides a compound having the formula: ##STR1## wherein: (A) n=2-4;(B) R.sub.1 and R.sub.2 are the same or different and selected from the group consisting of H, (C.sub.1 -C.sub.3)alkyl, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 NH.sub.2, and --CH.sub.2 CH.sub.2 N(CH.sub.3).sub.2 or R.sub.1 and R.sub.2 are alkyl moieties which may taken together to form a 4- to 7-membered ring;(C) R.sub.3 is selected from H, --CH.sub.3, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 NH.sub.2 ;(D) X is located at the 2-, or 3-position and is selected from the group consisting of 2-naphthyl, 1-naphthyl, 1-phenanthrenyl, 2-phenanthrenyl, 3-phenanthrenyl, 4-phenanthrenyl, 9-phenanthrenyl, phenyl, and mono- or polysubstituted phenyl wherein the substituents are selected from the group consisting of --OR.sub.4, --NR.sub.5 R.sub.6, (C.sub.1 -C.sub.3) alkyl, --CF.sub.3, F, Cl, Br, I, --NO.sub.2, --CN, --SO.sub.3 H, --SO.sub.2 NR.sub.5 R.sub.6, --CO.sub.2 H, --CO.sub.2 R.sub.4, and phenyl;R.sub.4 is H or (C.sub.1 -C.sub.4)alkyl;R.sub.5 and R.sub.6 are the same or different and are selected from H, or (C.sub.1 -C.sub.4)alkyl, or R.sub.5 and R.sub.6 are alkyl groups which may be taken together to form a 4-7 membered ring;(E) W is selected from H, --OR.sub.4, --NR.sub.5 R.sub.6, (C.sub.1 -C.sub.3)alkyl, --CF.sub.3, F, Cl, Br, I, --NO.sub.2, --CN, --SO.sub.2 NR.sub.5 R.sub.6, --CO.sub.2 R.sub.4 ; or a pharmacologically acceptable salt thereof which is useful as an antineoplastic agent.

    摘要翻译: 本发明提供具有下式的化合物:其中:(A)n = 2-4; (B)R 1和R 2相同或不同,选自H,(C 1 -C 3)烷基,-CH 2 CH 2 OH,-CH 2 CH 2 NH 2和-CH 2 CH 2 N(CH 3)2或R 1和R 2是可以被取代的烷基部分 一起形成4-至7-元环; (C)R 3选自H,-CH 3,-CH 2 CH 3,-CH 2 CH 2 NH 2; (D)X位于2-或3-位,并且选自2-萘基,1-萘基,1-菲基,2-菲基,3-菲基,4-菲基,9-菲基 ,苯基和单取代或多取代的苯基,其中取代基选自-OR4,-NR5R6,(C1-C3)烷基,-CF3,F,Cl,Br,I,-NO2,-CN, SO 3 H,-SO 2 NR 5 R 6,-CO 2 H,-CO 2 R 4和苯基; R4是H或(C1-C4)烷基; R5和R6相同或不同并且选自H或(C1-C4)烷基,或R5和R6是可以一起形成4-7元环的烷基; (E)W选自H,-OR4,-NR5R6,(C1-C3)烷基,-CF3,F,Cl,Br,I,-NO2,-CN,-SO2NR5R6,-CO2R4; 或其药理学上可接受的盐,其可用作抗肿瘤剂。

    Systems and methods for calibrating a silicon photomultiplier-based positron emission tomography system
    5.
    发明授权
    Systems and methods for calibrating a silicon photomultiplier-based positron emission tomography system 有权
    用于校准基于硅光电倍增管的正电子发射断层扫描系统的系统和方法

    公开(公告)号:US09588230B2

    公开(公告)日:2017-03-07

    申请号:US12560054

    申请日:2009-09-15

    摘要: A representative positron emission tomography (PET) system includes a positron emission tomography detector having one or more silicon photomultipliers that output silicon photomultipliers signals. The PET system further includes a calibration system that is electrically coupled to the silicon photomultipliers. The calibration system determines a single photoelectron response of the silicon photomultipliers signals and adjusts a gain of the silicon photomultipliers based on the single photoelectron response.

    摘要翻译: 代表性的正电子发射断层摄影(PET)系统包括正电子发射断层摄影检测器,其具有输出硅光电倍增管信号的一个或多个硅光电倍增管。 PET系统还包括电耦合到硅光电倍增管的校准系统。 校准系统确定硅光电倍增管信号的单个光电子响应,并且基于单个光电子响应调整硅光电倍增管的增益。

    Just-in-time analytics on large file systems
    6.
    发明授权
    Just-in-time analytics on large file systems 有权
    大型文件系统的即时分析

    公开(公告)号:US09244975B2

    公开(公告)日:2016-01-26

    申请号:US13328810

    申请日:2011-12-16

    IPC分类号: G06F17/30

    CPC分类号: G06F17/30442

    摘要: As file systems reach the petabytes scale, users and administrators are increasingly interested in acquiring high-level analytical information for file management and analysis. Two particularly important tasks are the processing of aggregate and top-k queries which, unfortunately, cannot be quickly answered by hierarchical file systems such as ext3 and NTFS. Existing pre-processing based solutions, e.g., file system crawling and index building, consume a significant amount of time and space (for generating and maintaining the indexes) which in many cases cannot be justified by the infrequent usage of such solutions. User interests can often be sufficiently satisfied by approximate (i.e., statistically accurate) answers. A just-in-time sampling-based system can, after consuming a small number of disk accesses, produce extremely accurate answers for a broad class of aggregate and top-k queries over a file system without the requirement of any prior knowledge. The system is efficient, accurate and scalable.

    摘要翻译: 随着文件系统达到PB级,用户和管理员越来越有兴趣获取用于文件管理和分析的高级分析信息。 两个特别重要的任务是处理聚合和top-k查询,不幸的是不能通过分层文件系统(如ext3和NTFS)快速回答。 现有的基于预处理的解决方案,例如文件系统爬行和索引构建,消耗了大量的时间和空间(用于生成和维护索引),这在许多情况下不能被这种解决方案的频繁使用所证明。 用户兴趣通常可以通过近似(即统计准确的)答案来充分满足。 基于时间抽样的系统可以在消耗少量磁盘访问后,通过文件系统为广泛的聚合和顶级查询提供非常准确的答案,而无需任何先前的知识。 该系统是高效,准确和可扩展的。

    Concurrent DC-coupled anode and dynode readout scheme for PET block detectors
    7.
    发明授权
    Concurrent DC-coupled anode and dynode readout scheme for PET block detectors 有权
    并联DC耦合阳极和用于PET块检测器的倍增电极读出方案

    公开(公告)号:US09086492B2

    公开(公告)日:2015-07-21

    申请号:US11753067

    申请日:2007-05-24

    IPC分类号: G01T1/00 G01T1/164

    CPC分类号: G01T1/1642 G01T1/208

    摘要: A scintillation detector including one or more photomultiplier tubes, a scintillation block optically attached to the photomultiplier tubes, and a DC-coupled bleeder circuit combining outputs of dynodes of the photomultipliers to provide a DC-coupled dynode output together with a DC-coupled anode output of the photomultiplier tubes. The DC-coupled bleeder circuit includes a RF transformer. A positive high voltage supply also can be used together with a DC-coupled bleeder circuit for the anode outputs.

    摘要翻译: 闪烁检测器,包括一个或多个光电倍增管,与光电倍增管光学连接的闪烁块,以及组合光电倍增管的倍增电极输出的DC耦合泄放电路,以提供DC耦合的倍增电极输出以及直流耦合的阳极输出 的光电倍增管。 直流耦合放电电路包括RF变压器。 阳极高压电源也可以与阳极输出的直流耦合泄放电路一起使用。

    Energy correction for one-to-one coupled radiation detectors having non-linear sensors
    8.
    发明授权
    Energy correction for one-to-one coupled radiation detectors having non-linear sensors 有权
    具有非线性传感器的一对一耦合辐射探测器的能量校正

    公开(公告)号:US08884213B2

    公开(公告)日:2014-11-11

    申请号:US13539931

    申请日:2012-07-02

    IPC分类号: G01T1/202 G01T1/24

    CPC分类号: G01T1/248 G01T1/202

    摘要: Systems and methods for correcting output signals from non-linear photosensors, specifically silicon photomultipliers (SiPMs). SiPMs are used in a PET detector to readout light emissions from LSO scintillator crystals. The non-linear output of the SiPM can distort and compress the energy spectrum which is crucial in PET imaging. The non-linearity effect for inter-crystal scattered events can place an energy event outside of the PET detector energy window, resulting in a rejected event. Systems and methods to correct the SiPM non-linearity for inter-crystal scattered events, so as to be able to obtain the proper energy event and produce an accurate medical image, are disclosed.

    摘要翻译: 用于校正非线性光电传感器,特别是硅光电倍增管(SiPM)的输出信号的系统和方法。 SiPM用于PET检测器以读出LSO闪烁体晶体的光发射。 SiPM的非线性输出可以扭曲和压缩在PET成像中至关重要的能谱。 晶体间散射事件的非线性效应可以将能量事件置于PET检测器能量窗口之外,导致被拒绝的事件。 公开了用于校正晶间散射事件的SiPM非线性的系统和方法,以便能够获得适当的能量事件并产生精确的医学图像。

    Compound for inhibiting type 5 phosphodiesterase and preparation method thereof
    9.
    发明授权
    Compound for inhibiting type 5 phosphodiesterase and preparation method thereof 有权
    抑制5型磷酸二酯酶的化合物及其制备方法

    公开(公告)号:US08859565B2

    公开(公告)日:2014-10-14

    申请号:US13512524

    申请日:2010-07-30

    申请人: Nan Zhang Rong Zhong

    发明人: Nan Zhang Rong Zhong

    摘要: The present invention discloses a compound of formula (I) and citrate thereof as type 5 phosphodiesterase inhibitor, a preparation method thereof, and a pharmaceutical composition including the compound of formula (I) and citrate thereof. The experimental results of the present invention prove that the compound of formula (I) and citrate thereof can inhibit activity of type 5 phosphodiesterase, and can be used for treating erectile dysfunction, inhibiting platelet aggregation and treating thrombosis, decreasing pulmonary hypertension and treating cardiovascular diseases, treating asthma and treating diabetes gastroparesis.

    摘要翻译: 本发明公开了式(I)化合物及其柠檬酸盐作为5型磷酸二酯酶抑制剂及其制备方法,以及含有式(I)化合物及其柠檬酸盐的药物组合物。 本发明的实验结果证明,式(I)化合物及其柠檬酸盐可抑制5型磷酸二酯酶的活性,可用于治疗勃起功能障碍,抑制血小板聚集和治疗血栓形成,降低肺动脉高压和治疗心血管疾病 治疗哮喘和治疗糖尿病胃轻瘫。

    Positron Emission Tomography Block Detector Interconnect
    10.
    发明申请
    Positron Emission Tomography Block Detector Interconnect 有权
    正电子发射断层扫描检测器互连

    公开(公告)号:US20130062525A1

    公开(公告)日:2013-03-14

    申请号:US13229797

    申请日:2011-09-12

    IPC分类号: G01T1/20 G01T1/164

    CPC分类号: G01T1/1648

    摘要: Using standard or “off the shelf” cable to interconnect between the PET block detector and the detector circuit may save substantial costs given the number of PMTs in a PET system. Given space constraints, simple maintenance with reduced risk of disturbing cabling is desired, making ongoing use of standard cabling without adding further cabling desired. To implement digital gain control, a further communication is provided between the PET detector block and the detector circuit. Since the standard cable may not have additional wires for such communications and to reduce timing degradation, the PMT signals are combined, such as generating position and energy signals at the PET detector block. The four PMT signals are reduced to three signals without reduction in function, allowing a fourth twisted pair of wires in a CAT5 cable to be used for digital gain control.

    摘要翻译: 使用标准或现货电缆在PET块检测器和检测器电路之间进行互连可以节省大量成本,因为PET系统中PMT的数量。 鉴于空间限制,需要简单的维护,减少干扰布线的风险,不断增加布线需求,不断使用标准布线。 为了实现数字增益控制,在PET检测器块和检测器电路之间提供进一步的通信。 由于标准电缆可能没有用于这种通信的附加电线并且减少定时劣化,所以组合PMT信号,例如在PET检测器块处产生位置和能量信号。 四个PMT信号减少到三个信号,而不会降低功能,允许CAT5电缆中的第四根双绞线用于数字增益控制。