METHODS FOR PRODUCING PHENYLALANINE DERIVATIVES HAVING A QUINAZOLINEDIONE SKELETON AND INTERMEDIATES FOR PRODUCTION THEREOF
    1.
    发明申请
    METHODS FOR PRODUCING PHENYLALANINE DERIVATIVES HAVING A QUINAZOLINEDIONE SKELETON AND INTERMEDIATES FOR PRODUCTION THEREOF 有权
    用于生产具有四氮唑烷酮的苯乙烯胺衍生物的方法及其生产中间体

    公开(公告)号:US20100204505A1

    公开(公告)日:2010-08-12

    申请号:US12766178

    申请日:2010-04-23

    IPC分类号: C07C229/52

    CPC分类号: C07D239/96 C07C233/87

    摘要: The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising of reacting an acylphenylalanine derivative(s) of formula (1) with a carbonyl group-introducing reagent(s) and a derivative(s) of anthranilic acid to form an asymmetric urea intermediate(s); making the asymmetric urea intermediate(s) into a quinazolinedione compound(s) of formula (4) in the presence of a base(s); and N-alkylating quinazolinedione ring amide of the obtained quinazolinedione compounds with N-alkylation agents. This production method is an industrially applicable method for producing phenylalanine derivatives having a quinazolinedione skeleton, which are compounds highly useful as drugs having α 4 integrin inhibiting activity. In the formulae (1) and (5), R1 represents a phenyl group having a substituent(s) and the like, R2 represents an alkyl group and the like, R3 represents a dialkylamino group and the like, and R4 represents an alkyl group and the like.

    摘要翻译: 本发明提供了具有式(5)喹唑啉二酮环的苯丙氨酸衍生物的制备方法,包括使式(1)的酰基苯丙氨酸衍生物与羰基引入试剂反应的步骤, 和邻氨基苯甲酸的衍生物以形成不对称脲中间体; 在碱的存在下使不对称脲中间体转化为式(4)的喹唑啉二酮化合物; 和得到的喹唑啉二酮化合物的N-烷基化喹唑啉二酮环酰胺与N-烷基化剂。 该制造方法是用于生产具有喹唑啉二酮骨架的苯丙氨酸衍生物的工业上适用的方法,其是作为具有α4整联蛋白抑制活性的药物高度有用的化合物。 在式(1)和(5)中,R 1表示具有取代基等的苯基,R 2表示烷基等,R 3表示二烷基氨基等,R 4表示烷基 等等。

    Methods for producing phenylalanine derivatives having a quinazolinedione skeleton and intermediates for production thereof
    2.
    发明授权
    Methods for producing phenylalanine derivatives having a quinazolinedione skeleton and intermediates for production thereof 有权
    具有喹唑啉二酮骨架的苯丙氨酸衍生物的制造方法及其制造用中间体

    公开(公告)号:US08318975B2

    公开(公告)日:2012-11-27

    申请号:US12766178

    申请日:2010-04-23

    IPC分类号: C07C63/04

    CPC分类号: C07D239/96 C07C233/87

    摘要: The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising of reacting an acylphenylalanine derivative(s) of formula (1) with a carbonyl group-introducing reagent(s) and a derivative(s) of anthranilic acid to form an asymmetric urea intermediate(s); making the asymmetric urea intermediate(s) into a quinazolinedione compound(s) of formula (4) in the presence of a base(s); and N-alkylating quinazolinedione ring amide of the obtained quinazolinedione compounds with N-alkylation agents. This production method is an industrially applicable method for producing phenylalanine derivatives having a quinazolinedione skeleton, which are compounds highly useful as drugs having α 4 integrin inhibiting activity. In the formulae (1) and (5), R1 represents a phenyl group having a substituent(s) and the like, R2 represents an alkyl group and the like, R3 represents a dialkylamino group and the like, and R4 represents an alkyl group and the like.

    摘要翻译: 本发明提供了具有式(5)喹唑啉二酮环的苯丙氨酸衍生物的制备方法,包括使式(1)的酰基苯丙氨酸衍生物与羰基引入试剂反应的步骤, 和邻氨基苯甲酸的衍生物以形成不对称脲中间体; 在碱的存在下使不对称脲中间体转化为式(4)的喹唑啉二酮化合物; 和得到的喹唑啉二酮化合物的N-烷基化喹唑啉二酮环酰胺与N-烷基化剂。 该制造方法是用于生产具有喹唑啉二酮骨架的苯丙氨酸衍生物的工业上适用的方法,其是作为具有α4整联蛋白抑制活性的药物高度有用的化合物。 在式(1)和(5)中,R 1表示具有取代基等的苯基,R 2表示烷基等,R 3表示二烷基氨基等,R 4表示烷基 等等。

    Methods for producing phenylalanine derivatives having a quinazolinedione skeleton and intermediates for production thereof
    3.
    发明授权
    Methods for producing phenylalanine derivatives having a quinazolinedione skeleton and intermediates for production thereof 有权
    具有喹唑啉二酮骨架的苯丙氨酸衍生物的制造方法及其制造用中间体

    公开(公告)号:US07737274B2

    公开(公告)日:2010-06-15

    申请号:US11207751

    申请日:2005-08-22

    CPC分类号: C07D239/96 C07C233/87

    摘要: The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising of reacting an acylphenylalanine derivative(s) of formula (1) with a carbonyl group-introducing reagent(s) and a derivative(s) of anthranilic acid to form an asymmetric urea intermediate(s); making the asymmetric urea intermediate(s) into a quinazolinedione compound(s) of formula (4) in the presence of a base(s); and N-alkylating quinazolinedione ring amide of the obtained quinazolinedione compounds with N-alkylation agents. This production method is an industrially applicable method for producing phenylalanine derivatives having a quinazolinedione skeleton, which are compounds highly useful as drugs having α 4 integrin inhibiting activity. In the formulae (1) and (5), R1 represents a phenyl group having a substituent(s) and the like, R2 represents an alkyl group and the like, R3 represents a dialkylamino group and the like, and R4 represents an alkyl group and the like.

    摘要翻译: 本发明提供了具有式(5)喹唑啉二酮环的苯丙氨酸衍生物的制备方法,包括使式(1)的酰基苯丙氨酸衍生物与羰基引入试剂反应的步骤, 和邻氨基苯甲酸的衍生物以形成不对称脲中间体; 在碱的存在下使不对称脲中间体转化为式(4)的喹唑啉二酮化合物; 和得到的喹唑啉二酮化合物的N-烷基化喹唑啉二酮环酰胺与N-烷基化剂。 该制造方法是用于生产具有喹唑啉二酮骨架的苯丙氨酸衍生物的工业上适用的方法,其是作为具有α4整联蛋白抑制活性的药物高度有用的化合物。 在式(1)和(5)中,R 1表示具有取代基等的苯基,R 2表示烷基等,R 3表示二烷基氨基等,R 4表示烷基 等等。

    Methods for producing phenylalanine derivatives having a quinazolinedione skeleton and intermediates for production thereof
    4.
    发明申请
    Methods for producing phenylalanine derivatives having a quinazolinedione skeleton and intermediates for production thereof 有权
    具有喹唑啉二酮骨架的苯丙氨酸衍生物的制造方法及其制造用中间体

    公开(公告)号:US20060009476A1

    公开(公告)日:2006-01-12

    申请号:US11207751

    申请日:2005-08-22

    IPC分类号: A61K31/517 C07D239/91

    CPC分类号: C07D239/96 C07C233/87

    摘要: The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising of reacting an acylphenylalanine derivative(s) of formula (1) with a carbonyl group-introducing reagent(s) and a derivative(s) of anthranilic acid to form an asymmetric urea intermediate(s); making the asymmetric urea intermediate(s) into a quinazolinedione compound(s) of formula (4) in the presence of a base(s); and N-alkylating quinazolinedione ring amide of the obtained quinazolinedione compounds with N-alkylation agents. This production method is an industrially applicable method for producing phenylalanine derivatives having a quinazolinedione skeleton, which are compounds highly useful as drugs having α 4 integrin inhibiting activity. In the formulae (1) and (5), R1 represents a phenyl group having a substituent(s) and the like, R2 represents an alkyl group and the like, R3 represents a dialkylamino group and the like, and R4 represents an alkyl group and the like.

    摘要翻译: 本发明提供了具有式(5)喹唑啉二酮环的苯丙氨酸衍生物的制备方法,包括使式(1)的酰基苯丙氨酸衍生物与羰基引入试剂反应的步骤, 和邻氨基苯甲酸的衍生物以形成不对称脲中间体; 在碱的存在下使不对称脲中间体转化为式(4)的喹唑啉二酮化合物; 和得到的喹唑啉二酮化合物的N-烷基化喹唑啉二酮环酰胺与N-烷基化剂。 该制造方法是用于生产具有喹唑啉二酮骨架的苯丙氨酸衍生物的工业上适用的方法,其是作为具有α4整联蛋白抑制活性的药物高度有用的化合物。 在式(1)和(5)中,R 1表示具有取代基等的苯基,R 2表示烷基等,R 3表示二烷基氨基等,R 4表示烷基 等等。

    Liquid crystal spatial light modulator for edge detection employing
diffusion in the photoconductive layer to enlarge image
    5.
    发明授权
    Liquid crystal spatial light modulator for edge detection employing diffusion in the photoconductive layer to enlarge image 失效
    用于边缘检测的液晶空间光调制器,其利用光电导层中的扩散来放大图像

    公开(公告)号:US5420709A

    公开(公告)日:1995-05-30

    申请号:US905280

    申请日:1992-06-26

    CPC分类号: G06K9/58 G02F1/135 G02F1/141

    摘要: An edge image extraction light modulator forms an edge portion image corresponding to a boundary between two optically equalized portions of a liquid crystal layer. Each portion has a different bistable state and an edge portion optically distinct from the two optically equalized portions. An optical image is written onto the light valve while applying a voltage between two transparent electrode layers of the light valve to effect switching between a first stable optical axis and a second stable optical axis. The light valve is illuminated and the edge portion of the written image is read. A first and a second polarizer are in crossed-Nicols position so that the two optically equalized portions comprise a portion having the written image except for the edge portion thereof and a non-written portion. The edge portion is not optically equal to the two optically equal portions and can thus be detected. A method of driving the edge image extraction light modulator includes writing an optical image onto the light valve by irradiating a photoconductive layer with light. A first pulse voltage is applied to erase and reset the light valve, and a second pulse voltage is applied, having a polarity opposite that of the first pulse voltage, to generate carriers diffusing in the photoconductive film to impart an electric field to the liquid crystal layer and form an enlarged image of the optical image in the light valve. A third pulse voltage, having the same polarity as that of the first pulse voltage, erases a part of the enlarged image except for an edge portion thereof to form an edge enhanced image in the light valve.

    摘要翻译: 边缘图像提取光调制器形成与液晶层的两个光学均衡部分之间的边界对应的边缘部分图像。 每个部分具有不同的双稳态和与两个光学均衡部分光学不同的边缘部分。 在光阀的两个透明电极层之间施加电压以在第一稳定光轴和第二稳定光轴之间进行切换,将光学图像写入光阀。 点亮光阀,读取写入图像的边缘部分。 第一和第二偏振器处于十字尼科耳尔位置,使得两个光学均衡部分包括除了其边缘部分之外的具有写入图像的部分和非写入部分。 边缘部分不是光学上等于两个光学相等的部分,因此可以被检测。 驱动边缘图像提取光调制器的方法包括通过用光照射光电导层将光学图像写入光阀。 施加第一脉冲电压以擦除和复位光阀,施加具有与第一脉冲电压相反的极性的第二脉冲电压,以产生在光电导膜中扩散的载流子以向液晶施加电场 并在光阀中形成光学图像的放大图像。 具有与第一脉冲电压相同极性的第三脉冲电压擦除除了其边缘部分之外的放大图像的一部分,以在光阀中形成边缘增强图像。

    Method of manufacturing a semiconductor detector for detecting light and
radiation
    6.
    发明授权
    Method of manufacturing a semiconductor detector for detecting light and radiation 失效
    制造用于检测光和辐射的半导体检测器的方法

    公开(公告)号:US6001667A

    公开(公告)日:1999-12-14

    申请号:US553565

    申请日:1996-06-03

    CPC分类号: H01L27/1443 H01L27/14658

    摘要: A method of manufacturing a semiconductor detector for detecting light and radiation comprises the steps of providing a first semiconductor substrate of a first conductivity type, attaching a second substrate to the first semiconductor substrate through an insulating film, grinding the first semiconductor substrate from a surface thereof to a predetermined thickness, forming a MOS transistor on the ground surface of the first semiconductor substrate, removing the second substrate, and forming electrodes on the first semiconductor substrate for forming a depletion layer.

    摘要翻译: PCT No.PCT / JP95 / 00559 Sec。 371日期:1996年6月3日 102(e)1996年6月3日PCT 1995年3月27日PCT PCT。 公开号WO95 / 26573 日期1995年10月5日制造用于检测光和辐射的半导体检测器的方法包括以下步骤:提供第一导电类型的第一半导体衬底,通过绝缘膜将第二衬底附接到第一半导体衬底,研磨第一半导体 从其表面到预定厚度,在第一半导体衬底的接地表面上形成MOS晶体管,去除第二衬底,以及在第一半导体衬底上形成用于形成耗尽层的电极。

    Avalanche photodiode for light detection
    7.
    发明授权
    Avalanche photodiode for light detection 失效
    用于光检测的雪崩光电二极管

    公开(公告)号:US5763903A

    公开(公告)日:1998-06-09

    申请号:US516234

    申请日:1995-08-17

    摘要: An avalanche photodiode for detecting x-rays and other radiation comprises a first substrate having a portion removed therefrom, a first insulating film formed on the first substrate, a second substrate comprising a floating zone silicon semiconductor substrate disposed on the first insulating film, an impurity region selectively formed in the second substrate at a surface corresponding to the removed portion, a PN junction formed on the second substrate, a glass substrate mounted to the second substrate, a first electrode formed on the first substrate for applying a voltage to the impurity region, a second electrode formed on the second substrate for applying a voltage to the second substrate, a third electrode formed on the glass substrate and electrically connected to the second electrode, and an integrated circuit package having a lead pin connected to the third electrode. Accordingly, a shallow depletion layer may be provided on a floating zone SOI substrate. The substrates may be joined to the glass substrate using a eutectic bonding process.

    摘要翻译: 用于检测X射线和其它辐射的雪崩光电二极管包括:第一衬底,其具有从其中去除的部分;第一绝缘膜,形成在第一衬底上;第二衬底,包括布置在第一绝缘膜上的浮动区硅半导体衬底, 在与第二基板对应的表面上选择性地形成在第二基板上的区域,形成在第二基板上的PN结,安装到第二基板的玻璃基板,形成在第一基板上的用于向杂质区域施加电压的第一电极 形成在第二基板上的用于向第二基板施加电压的第二电极,形成在玻璃基板上并电连接到第二电极的第三电极,以及具有连接到第三电极的引脚的集成电路封装。 因此,可以在浮动区域SOI衬底上提供浅耗尽层。 可以使用共晶接合工艺将基板连接到玻璃基板。

    Charge pump rush current limiting circuit
    8.
    发明授权
    Charge pump rush current limiting circuit 有权
    电荷泵冲击电流限流电路

    公开(公告)号:US06738272B2

    公开(公告)日:2004-05-18

    申请号:US10124354

    申请日:2002-04-16

    IPC分类号: H02M318

    CPC分类号: H02M3/07 Y10S323/908

    摘要: In a charge pump circuit, a constant current circuit is disposed between an input power supply and an output capacitor, when a power supply is started to turn on, the operation of the charge pump circuit is stopped, and the output capacitor is charged up to a given voltage by the constant current circuit, and thereafter the normal operation of the charge pump is started to limit the rush current. When the power supply is started, the operation is conducted by an oscillator circuit having a small duty ratio, and thereafter the control is replaced by the PFM control having the normal duty ratio, to thereby reduce the rush current as compared with that of the conventional PFM control. When the power supply is started, a pre-driver including a current limiting element is used to drive a driver, resulting in such an advantage that the rush current is reduced as compared with that driven by the conventional pre-driver.

    摘要翻译: 在电荷泵电路中,在输入电源和输出电容器之间设置恒流电路,当电源开始接通时,电荷泵电路的动作停止,输出电容充电至 通过恒流电路的给定电压,然后开始电荷泵的正常操作以限制冲击电流。 当电源启动时,通过占空比小的振荡电路进行动作,之后用具有正常占空比的PFM控制代替控制,从而与现有技术相比减小了冲击电流 PFM控制。 当电源启动时,使用包括限流元件的预驱动器来驱动驱动器,从而产生与传统的前驱动器驱动相比冲击电流降低的优点。

    Photoelectric conversion semiconductor device with insulation film
    9.
    发明授权
    Photoelectric conversion semiconductor device with insulation film 失效
    具有绝缘膜的光电转换半导体器件

    公开(公告)号:US5719414A

    公开(公告)日:1998-02-17

    申请号:US213952

    申请日:1994-03-16

    摘要: A photoelectric conversion semiconductor device is characterized in that a second conductivity type impurity region is formed in a first conductivity type semiconductor substrate, the second conductivity type impurity region having a depth of 0.1 .mu.m or less and a peak density of 1.times.10.sup.19 atoms/cm.sup.3 or more. A method of manufacturing a photoelectric conversion semiconductor device is characterized by a step of ion-injecting boron or boron fluoride with a dose amount of 1.times.10.sup.16 to 5.times.10.sup.16 atoms/cm.sup.2 into a semiconductor substrate as an impurity.

    摘要翻译: 光电转换半导体器件的特征在于,在第一导电型半导体衬底中形成第二导电类型杂质区,第二导电类型杂质区的深度为0.1μm或更小,峰密度为1×1019原子/ cm3或 更多。 制造光电转换半导体器件的方法的特征在于将作为杂质的半导体衬底中的剂量为1×10 16至5×10 16原子/ cm 2的硼或氟化硼离子注入的步骤。