公开(公告)号：US20110257376A1

公开(公告)日：2011-10-20

申请号：US13053192

申请日：2011-03-21

申请人： Chi-Huey Wong ,  Tsui-Ling Hsu ,  Sarah R. Hanson ,  Masaaki Sawa

发明人： Chi-Huey Wong ,  Tsui-Ling Hsu ,  Sarah R. Hanson ,  Masaaki Sawa

IPC分类号： C07K14/47 ,  C07H19/207

CPC分类号： G01N33/582 ,  G01N1/30 ,  G01N2400/00

摘要： Methods are provided for labeling cellular glycans bearing azide groups via fluorescent labeling comprising Cu(I)-catalyzed [3+2] cycloaddition of a probe comprising alkynyl group. Generation of fluorescent probes from a nonfluorescent precursor, 4-ethynyl-N-ethyl-1,8-naphthalimide, by Cu(I)-catalyzed [3+2] cycloaddition of the alkyne group of the probe to an azido-modified sugar are provided. Incorporation of azido-containing fucose analog into glycoconjugates via the fucose salvage pathway are disclosed. Fluorescent visualization of fucosylated cells by flow cytometry of cells treated with 6-azidofucose labeled with click-activated fluorogenic probe or biotinylated alkyne is disclosed. Visualization of intracellular location of fucosylated glycoconjugates by fluorescence microscopy are disclosed.

摘要翻译： 提供了通过含有包含炔基的探针的Cu（I）催化的[3 + 2]环加成的荧光标记来标记携带叠氮基的细胞聚糖的方法。 通过Cu（I）催化的[3 + 2]环加成的探针的炔基与叠氮改性的糖，从非荧光前体4-乙炔基-N-乙基-1,8-萘二甲酰亚胺生成荧光探针是 提供。 公开了通过岩藻糖补救途径将叠氮基岩藻糖类似物掺入糖缀合物。 公开了通过用用点击激活的荧光探针或生物素化的炔标记的6-叠氮基聚糖处理的细胞的流式细胞术的岩藻糖基化细胞的荧光可视化。 公开了通过荧光显微镜观察岩藻糖基化糖缀合物的细胞内位置。

公开(公告)号：US20110190299A1

公开(公告)日：2011-08-04

申请号：US13002147

申请日：2010-04-19

申请人： Takayuki Irie ,  Masaaki Sawa ,  Sayuri Ito ,  Chika Tanaka ,  Seong Gu Ro ,  Choul Hong Park

发明人： Takayuki Irie ,  Masaaki Sawa ,  Sayuri Ito ,  Chika Tanaka ,  Seong Gu Ro ,  Choul Hong Park

IPC分类号： A61K31/5377 ,  C07D417/06 ,  C07D417/14 ,  A61K31/427 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/454

CPC分类号： C07D277/20 ,  A61K31/427 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  C07D277/54 ,  C07D417/14

摘要： An object of the present invention is to provide thiazolidinone derivatives. More specifically, an object of the present invention is to provide novel compounds having a CDC7 inhibitory action.The present invention provides thiazolidinone derivatives represented by the formula (I) The compounds of the present invention inhibit the CDC7 protein kinase activity, and suppress cell proliferation.

摘要翻译： 本发明的目的是提供噻唑烷酮衍生物。 更具体地，本发明的目的是提供具有CDC7抑制作用的新化合物。 本发明提供式（I）表示的噻唑烷酮衍生物本发明化合物抑制CDC7蛋白激酶活性，抑制细胞增殖。

公开(公告)号：US07960139B2

公开(公告)日：2011-06-14

申请号：US12079226

申请日：2008-03-24

申请人： Masaaki Sawa ,  Chi-Huey Wong ,  Tsui-Ling Hsu ,  Sarah Hanson

发明人： Masaaki Sawa ,  Chi-Huey Wong ,  Tsui-Ling Hsu ,  Sarah Hanson

IPC分类号： G01N33/53

CPC分类号： G01N33/5005 ,  G01N33/5008 ,  G01N33/533 ,  G01N2400/00

摘要： The present disclosure relates to a method for metabolic oligosaccharide engineering that incorporates derivatized alkyne-bearing sugar analogs as “tags” into cellular glycoconjugates. The disclosed method incorporates alkynyl derivatized Fuc and alkynyl derivatized ManNAc sugars into a cellular glycoconjugate. A chemical probe comprising an azide group and a visual probe or a fluorogenic probe is used to label the alkyne-derivatized sugar-tagged glycoconjugate. In one aspect, the chemical probe binds covalently to the alkynyl group by Cu(I)-catalyzed [3+2] azide-alkyne cycloaddition and is visualized at the cell surface, intracellularly, or in a cellular extract. The labeled glycoconjugate is capable of detection by flow cytometry, SDS-PAGE, Western blot, ELISA or confocal microscopy, and mass spectrometry.

摘要翻译： 本公开内容涉及将衍生的含炔烃类似物作为“标签”掺入细胞糖缀合物的代谢寡糖工程方法。 所公开的方法将炔基衍生化的Fuc和炔基衍生的ManNAc糖引入细胞糖缀合物中。 使用包含叠氮化物基团和视觉探针或荧光探针的化学探针来标记炔衍生的糖标记的糖缀合物。 在一个方面，化学探针通过Cu（I）催化的[3 + 2]叠氮炔环加成共价结合到炔基上，并且在细胞表面，细胞内或细胞提取物中可视化。 标记的糖缀合物能够通过流式细胞术，SDS-PAGE，Western印迹，ELISA或共聚焦显微镜和质谱检测。

公开(公告)号：US07910319B2

公开(公告)日：2011-03-22

申请号：US12079228

申请日：2008-03-24

申请人： Chi-Huey Wong ,  Tsui-Ling Hsu ,  Sarah R Hanson ,  Masaaki Sawa

发明人： Chi-Huey Wong ,  Tsui-Ling Hsu ,  Sarah R Hanson ,  Masaaki Sawa

IPC分类号： G01N33/53

CPC分类号： G01N33/582 ,  G01N1/30 ,  G01N2400/00

摘要： The disclosure provides a method of labeling of cellular glycans bearing azide groups via a fluorescent labeling technique based on Cu(I)-catalyzed [3+2]cycloaddition (click activation) of a probe comprising an alkynyl group. The method entails generating a fluorescent probe from a nonfluorescent precursor, 4-ethynyl-N-ethyl-1,8-naphthalimide, by Cu(I)-catalyzed [3+2]cycloaddition of the alkyne group of the probe with an azido-modified sugar. The disclosure further provides a method of incorporating an azido-containing fucose analog into glycoconjugates via the fucose salvage pathway. The disclosure provides a method of fluorescent visualization of fucosylated cells by flow cytometry when cells treated with 6-azidofucose are labeled with the click-activated fluorogenic probe or biotinylated alkyne. A method of visualizing the intracellular localization of fucosylated glycoconjugates by fluorescence microscopy is also disclosed.

摘要翻译： 本公开提供了通过基于包含炔基的探针的Cu（I）催化的[3 + 2]环加成（点击活化）的荧光标记技术来标记携带叠氮基的细胞聚糖的方法。 该方法需要通过Cu（I）催化的[3 + 2]环加成的探针的炔基与非荧光前体4-乙炔基-N-乙基-1,8-萘酰亚胺的生成荧光探针， 改性糖。 本公开进一步提供了通过岩藻糖补救途径将含叠氮基岩藻糖类似物掺入糖缀合物的方法。 本公开内容提供了当用6-叠氮基聚糖处理的细胞用点击激活的荧光探针或生物素化的炔被标记时，流式细胞仪荧光显示岩藻糖基化细胞的方法。 还公开了通过荧光显微镜观察岩藻糖基化糖缀合物的细胞内定位的方法。

公开(公告)号：US20100311965A1

公开(公告)日：2010-12-09

申请号：US12810386

申请日：2008-12-26

申请人： Masaaki Sawa ,  Koichi Yokota ,  Hideki Moriyama ,  Myoungyoup Shin ,  Seonggu Ro ,  Joong Myung Cho

发明人： Masaaki Sawa ,  Koichi Yokota ,  Hideki Moriyama ,  Myoungyoup Shin ,  Seonggu Ro ,  Joong Myung Cho

IPC分类号： C07D413/12 ,  C07D403/12 ,  C07D239/84 ,  C07D405/12 ,  C07D411/14 ,  C07D403/14

CPC分类号： C07D239/84 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： An object of the present invention is to provide compounds which are useful as protein kinase inhibitors.Disclosed is a 2-aminoquinazoline derivative represented by the following formula (I): wherein R1 represents a lower alkyl group which may be substituted with a halogen atom, or a halogen atom; R2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a halogen atom, a hydroxyl group, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, a substituted or unsubstituted acylamino group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, or a substituted or unsubstituted lower alkylureido group; and X, Y and Z each independently represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a halogen atom, a hydroxyl group, a carboxyl group, a lower alkoxycarbonyl group, a cyano group, a carbamoyl group, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, a substituted or unsubstituted lower alkoxycarbonylamino group, a substituted or unsubstituted lower alkylaminocarbonyl group, a lower alkylsulfonylamino group, a substituted or unsubstituted lower alkylureido group, or a substituted or unsubstituted acylamino group, or X and Y may be combined to form a 5- to 6-membered ring forming a bicyclic fused ring, wherein the 5- to 6-membered ring may optionally have a substituent, provided that when X and Y are not combined to form a fused ring, R2 represents a hydrogen atom and, when X and Y are combined to form a fused ring, a saturated or unsaturated, bicyclic alicyclic or heterocyclic fused ring can be formed.

摘要翻译： 本发明的目的是提供可用作蛋白激酶抑制剂的化合物。 公开了由下式（I）表示的2-氨基喹唑啉衍生物：其中R1表示可被卤素原子或卤素原子取代的低级烷基; R 2表示氢原子，取代或未取代的低级烷基，卤素原子，羟基，取代或未取代的低级烷氧基，取代或未取代的氨基，取代或未取代的酰氨基，羧基，低级 烷氧基羰基，氨基甲酰基或取代或未取代的低级烷基脲基; X，Y和Z各自独立地表示氢原子，取代或未取代的低级烷基，卤素原子，羟基，羧基，低级烷氧基羰基，氰基，氨基甲酰基，取代或未取代的 取代或未取代的低级烷氧基羰基氨基，取代或未取代的低级烷基氨基羰基，低级烷基磺酰基氨基，取代或未取代的低级烷基脲基，或取代或未取代的酰基氨基，或X 并且Y可以组合形成一个形成双环稠合环的5至6元环，其中5至6元环可以任选地具有取代基，条件是当X和Y不组合形成稠环时 R2表示氢原子，当X和Y组合形成稠环时，可以形成饱和或不饱和的双环脂环或杂环稠合环。

公开(公告)号：US5583433A

公开(公告)日：1996-12-10

申请号：US193290

申请日：1994-02-08

申请人： Masaaki Sawa

发明人： Masaaki Sawa

IPC分类号： G01B17/00 ,  G01D5/48 ,  G01B7/14 ,  G01B7/26 ,  G01F23/30

CPC分类号： G01B17/00 ,  G01D5/485

摘要： A length measuring apparatus that uses an ultrasonic magnetostrictive delay line can detect a position with high accuracy by utilizing a reflected wave positively. In a measuring apparatus using an ultrasonic magnetostrictive delay line in which a wave transmitter (4) is disposed at one end of an ultrasonic magnetostrictive delay line (1), and the other end of the ultrasonic magnetostrictive delay line (1) is made an open end, a detecting coil (3) is wound around the outer periphery of the ultrasonic magnetostrictive delay line (1) over the whole area of the measuring range, a magnet piece (2) is disposed so as to become slidable along the ultrasonic magnetostrictive delay line (1) an a position of the magnet piece (2) is measured on the basis of a delay time of a detection pulse (B) produced in the detection coil (3) relative to a drive pulse (A) applied to the wave transmitter (4), a period (T.sub.1) of the drive pulse (A) applied to the wave transmitter (4) is matched with a time in which a reflected wave (C) is generated at the ultrasonic magnetostrictive delay line (1) at its one end in which the wave transmitter (4) is disposed.

摘要翻译： 使用超声磁致伸缩延迟线的长度测量装置可以通过利用反射波来高精度地检测位置。 在使用超声波磁致伸缩延迟线的测量装置中，超声磁致伸缩延迟线（1）的一端设置有波发射器（4），超声磁致伸缩延迟线（1）的另一端为开路 在超声波磁致伸缩延迟线（1）的外周围绕测量范围的整个区域缠绕检测线圈（3），磁体片（2）设置成沿超声磁致伸缩延迟滑动 线（1）根据检测线圈（3）中产生的检测脉冲（B）相对于施加到波的驱动脉冲（A）的延迟时间来测量磁片（2）的位置 发射器（4），施加到波发射器（4）的驱动脉冲（A）的周期（T1）与在超声磁致伸缩延迟线（1）处产生反射波（C）的时间匹配 其一端设置有波发射器（4）。