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1. 发明授权

US08329413B2 Glycoproteomic probes for fluorescent imaging of fucosylated glycans in vivo 有权
标题翻译：用于体内岩藻糖基化聚糖荧光成像的糖蛋白质组学探针
公开(公告)号：US08329413B2
公开(公告)日：2012-12-11
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： G01N33/53
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。

2. 发明授权

US08119812B2 Thiazolidinone derivative 失效
标题翻译：噻唑烷酮衍生物
公开(公告)号：US08119812B2
公开(公告)日：2012-02-21
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： A61K31/427 , C07D417/06 , C07D417/14
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。

3. 发明申请

US20100137386A1 TNIK INHIBITOR AND THE USE 审中-公开
标题翻译： TNIK抑制剂及其用途
公开(公告)号：US20100137386A1
公开(公告)日：2010-06-03
申请号：US12503374
申请日：2009-07-15
申请人： Tesshi YAMADA , Miki SHITASHIGE , Koichi YOKOTA , Masaaki SAWA , Hideki MORIYAMA
发明人： Tesshi YAMADA , Miki SHITASHIGE , Koichi YOKOTA , Masaaki SAWA , Hideki MORIYAMA
IPC分类号： A61K31/426 , C07D277/56 , A61P35/00
CPC分类号： C07D277/56 , A61K9/1652 , A61K9/2054 , A61K9/4858
摘要： The present invention relates to compositions and methods for the treatment of cancer patients with Traf2- and Nck-interacting kinase (TNIK) inhibitors. More particularly, the present invention relates to pharmaceutical compositions comprising TNIK inhibitor and a pharmaceutically acceptable carrier, and to methods for treating the TNIK inhibitor administered to cancer patients, especially to solid cancer patients such as colorectal cancer, pancreatic cancer, non-small cell lung cancer, prostate cancer or breast cancer.And the present invention relates to a novel aminothiazole derivatives.
摘要翻译：本发明涉及用于治疗患有Traf2-和Nck相互作用激酶（TNIK）抑制剂的癌症患者的组合物和方法。更具体地，本发明涉及包含TNIK抑制剂和药学上可接受的载体的药物组合物，以及用于治疗施用于癌症患者的TNIK抑制剂的方法，特别是涉及固体癌症患者如结肠直肠癌，胰腺癌，非小细胞肺癌症，前列腺癌或乳腺癌。本发明涉及一种新的氨基噻唑衍生物。

4. 发明申请

US20130317218A1 NOVEL BICYCLIC THIAZOLE COMPOUNDS 审中-公开
公开(公告)号：US20130317218A1
公开(公告)日：2013-11-28
申请号：US13479396
申请日：2012-05-24
申请人： Masaaki Sawa , Hideki Moriyama , Tesshi Yamada , Miki Shitashige , Yusuke Kawase , Yuko Uno
发明人： Masaaki Sawa , Hideki Moriyama , Tesshi Yamada , Miki Shitashige , Yusuke Kawase , Yuko Uno
IPC分类号： C07D417/12 , C07D417/14 , C07D495/04 , C07D277/56
CPC分类号： C07D277/56 , C07D417/12 , C07D417/14
摘要： The present invention relates to novel bicyclic thiazole compounds that inhibit Traf2- and Nck-interacting kinase (TNIK), and as such are useful as TNIK inhibitors administered to cancer patients, especially to solid cancer patients such as colorectal cancer, pancreatic cancer, non-small cell lung cancer, prostate cancer or breast cancer. The bicyclic thiazole compounds are showed by a next formula (I). (wherein R1, R2, R3 and Q are as defined in the specification), or a pharmaceutically acceptable salt thereof.

5. 发明申请

US20080241856A1 Glycoproteomic probes for fluorescent imaging of fucosylated glycans in vivo 有权
标题翻译：用于体内岩藻糖基化聚糖荧光成像的糖蛋白质组学探针
公开(公告)号：US20080241856A1
公开(公告)日：2008-10-02
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 , C12P19/44 , C12Q1/00
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。

6. 发明申请

US20140018533A1 NOVEL FURANONE DERIVATIVE 有权
标题翻译：新鲜的呋喃酮衍生物
公开(公告)号：US20140018533A1
公开(公告)日：2014-01-16
申请号：US14008488
申请日：2012-03-30
申请人： Takayuki Irie , Ayako Sawa , Masaaki Sawa , Tokiko Asami , Yoko Funakoshi , Chika Tanaka
发明人： Takayuki Irie , Ayako Sawa , Masaaki Sawa , Tokiko Asami , Yoko Funakoshi , Chika Tanaka
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4375 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5355 , A61K31/541 , C07D519/00
摘要： To provide a novel furanone derivative, and a medicine including the same. The furanone derivative is represented by the formula (I): wherein A represents —COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocycle; R2 and R3 are the same or different and each independently represent a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocycle, an optionally substituted heterocyclic fused ring, or an optionally substituted amino group; or alternatively, R2 and R3, taken together with the nitrogen atom to which they are attached, may form an optionally substituted heterocycle or an optionally substituted heterocyclic fused ring; and R4 represents a hydrogen atom or a halogen atom; with the proviso that when A represents —COOR1, R2 and R3 are not optionally substituted amino groups at the same time, and when A represents a hydrogen atom, R3 represents a hydrogen atom.
摘要翻译：提供一种新颖的呋喃酮衍生物，以及包含该呋喃酮衍生物的药物。呋喃酮衍生物由式（I）表示：其中A表示-COOR 1或氢原子; R1表示氢原子，任选取代的烃基或任选取代的杂环; R2和R3相同或不同，并且各自独立地表示氢原子，任选取代的烃基，任选取代的苯基，任选取代的杂环，任选取代的杂环稠合环或任选取代的氨基; 或者R2和R3与它们所连接的氮原子一起可以形成任选取代的杂环或任选取代的杂环稠环; R4代表氢原子或卤原子; 条件是当A表示-COOR 1时，R2和R3不同时为任选取代的氨基，当A表示氢原子时，R 3表示氢原子。

7. 发明申请

US20120149887A1 ALKYNYL SUGAR ANALOGS FOR LABELING AND VISUALIZATION OF GLYCOCONJUGATES IN CELLS 审中-公开
标题翻译：用于在细胞中标记和观察甘油三酯的ALKYNYL糖模拟物
公开(公告)号：US20120149887A1
公开(公告)日：2012-06-14
申请号：US13159339
申请日：2011-06-13
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： C07H15/04 , C07H19/10
CPC分类号： G01N33/5005 , G01N33/5008 , G01N33/533 , G01N2400/00
摘要： Methods for metabolic oligosaccharide engineering that incorporates derivatized alkyne-bearing sugar analogs as “tags” into cellular glycoconjugates are disclosed. Alkynyl derivatized Fuc and alkynyl derivatized ManNAc sugars are incorporated into cellular glycoconjugates. Chemical probes comprising an azide group and a visual or fluorogenic probe and used to label alkyne-derivatized sugar-tagged glycoconjugates are disclosed. Chemical probes bind covalently to the alkynyl group by Cu(I)-catalyzed [3+2] azide-alkyne cycloaddition and are 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, confocal microscopy, and mass spectrometry.
摘要翻译：公开了将衍生的含炔烃类似物作为细胞糖缀合物的“标签”的代谢寡糖工程方法。将炔基衍生的Fuc和炔基衍生的ManNAc糖掺入细胞糖缀合物中。公开了包含叠氮基和视觉或荧光探针并用于标记炔衍生的糖标记的糖缀合物的化学探针。化学探针通过Cu（I）催化的[3 + 2]叠氮炔环加成与炔基共价结合，并在细胞表面，细胞内或细胞提取物中显现。标记的糖缀合物能够通过流式细胞术，SDS-PAGE，Western印迹，ELISA，共聚焦显微镜和质谱检测。

8. 发明申请

US20100216795A1 TNIK INHIBITOR AND THE USE 审中-公开
标题翻译： TNIK抑制剂及其用途
公开(公告)号：US20100216795A1
公开(公告)日：2010-08-26
申请号：US12766513
申请日：2010-04-23
申请人： Tesshi Yamada , Miki Shitashige , Koichi Yokota , Masaaki Sawa , Hideki Moriyama
发明人： Tesshi Yamada , Miki Shitashige , Koichi Yokota , Masaaki Sawa , Hideki Moriyama
IPC分类号： A61K31/5377 , C07D277/42 , A61K31/425 , C07D413/12 , A61K31/496 , C07D417/12 , A61P35/00
CPC分类号： C07D277/56 , A61K9/1652 , A61K9/2018 , A61K9/2054 , A61K9/2059 , A61K9/4858 , A61K31/425 , A61K31/426 , A61K31/496 , A61K31/5377
摘要： The present invention relates to Traf2- and Nck-interacting kinase (TNIK) inhibitors, pharmaceutical compositions, and methods for the treatment of cancer patients with TNIK inhibitors.And the present invention relates to a novel aminothiazole derivatives.The TNIK inhibitors are showed by a next formula (I). Wherein R1, R2, R3, R4, R5 and R6 represent independently a hydrogen atom or a substituent group.
摘要翻译：本发明涉及用于治疗TNIK抑制剂的癌症患者的Traf2-和Nck相互作用激酶（TNIK）抑制剂，药物组合物和方法。本发明涉及一种新的氨基噻唑衍生物。 TNIK抑制剂由下式（I）表示。其中R1，R2，R3，R4，R5和R6独立地表示氢原子或取代基。

9. 发明授权

US09816981B2 Alkynyl sugar analogs for labeling and visualization of glycoconjugates in cells 有权
公开(公告)号：US09816981B2
公开(公告)日：2017-11-14
申请号：US13159339
申请日：2011-06-13
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： C07H15/04 , C07H19/10 , G01N33/50 , G01N33/533
CPC分类号： G01N33/5005 , G01N33/5008 , G01N33/533 , G01N2400/00
摘要： Methods for metabolic oligosaccharide engineering that incorporates derivatized alkyne-bearing sugar analogs as “tags” into cellular glycoconjugates are disclosed. Alkynyl derivatized Fuc and alkynyl derivatized ManNAc sugars are incorporated into cellular glycoconjugates. Chemical probes comprising an azide group and a visual or fluorogenic probe and used to label alkyne-derivatized sugar-tagged glycoconjugates are disclosed. Chemical probes bind covalently to the alkynyl group by Cu(I)-catalyzed [3+2] azide-alkyne cycloaddition and are 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, confocal microscopy, and mass spectrometry.

10. 发明授权

US08742113B2 Furanone derivative 有权
标题翻译：呋喃酮衍生物
公开(公告)号：US08742113B2
公开(公告)日：2014-06-03
申请号：US14008488
申请日：2012-03-30
申请人： Takayuki Irie , Ayako Sawa , Masaaki Sawa , Tokiko Asami , Yoko Funakoshi , Chika Tanaka
发明人： Takayuki Irie , Ayako Sawa , Masaaki Sawa , Tokiko Asami , Yoko Funakoshi , Chika Tanaka
IPC分类号： C07D471/02 , C07D491/02 , C07D498/02 , C07D513/02 , C07D515/02
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4375 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5355 , A61K31/541 , C07D519/00
摘要： To provide a novel furanone derivative, and a medicine including the same. The furanone derivative is represented by the formula (I): wherein A represents —COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocycle; R2 and R3 are the same or different and each independently represent a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocycle, an optionally substituted heterocyclic fused ring, or an optionally substituted amino group; or alternatively, R2 and R3, taken together with the nitrogen atom to which they are attached, may form an optionally substituted heterocycle or an optionally substituted heterocyclic fused ring; and R4 represents a hydrogen atom or a halogen atom; with the proviso that when A represents —COOR1, R2 and R3 are not optionally substituted amino groups at the same time, and when A represents a hydrogen atom, R3 represents a hydrogen atom.
摘要翻译：提供一种新颖的呋喃酮衍生物，以及包含该呋喃酮衍生物的药物。呋喃酮衍生物由式（I）表示：其中A表示-COOR 1或氢原子; R1表示氢原子，任选取代的烃基或任选取代的杂环; R2和R3相同或不同，并且各自独立地表示氢原子，任选取代的烃基，任选取代的苯基，任选取代的杂环，任选取代的杂环稠合环或任选取代的氨基; 或者R2和R3与它们所连接的氮原子一起可以形成任选取代的杂环或任选取代的杂环稠环; R4代表氢原子或卤原子; 条件是当A表示-COOR 1时，R2和R3不同时为任选取代的氨基，当A表示氢原子时，R 3表示氢原子。

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