公开(公告)号：US20140142044A1

公开(公告)日：2014-05-22

申请号：US14111540

申请日：2012-04-12

申请人： Terrence R. Burke, JR. ,  Wenjian Qian ,  Fa Liu ,  Kyung S. Lee ,  Jung-Eun Park

发明人： Terrence R. Burke, JR. ,  Wenjian Qian ,  Fa Liu ,  Kyung S. Lee ,  Jung-Eun Park

IPC分类号： C07K7/06

CPC分类号： C07K7/06 ,  A61K38/00 ,  A61K47/60 ,  C07K1/006 ,  C07K5/0827 ,  C12N9/12 ,  C12Y207/11021

摘要： Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds. The compounds of the invention have potential therapeutic activity in view of their binding and inhibitory activities towards Plk1. They are based on the amino acid sequence PLHSpT (phosphorylated Thr). The PEG moiety, when present, is covalently attached at the N-terminus. The invention also encompasses derivatives having substituents on the Pro and/or the His side chains, substituents on the phosphate group, the replacement of His with Gln, the replacement of Pro with a N-substituted Gly, the replacement of Ser with Ala, as well as HS-pT fragments with N-terminal alkoxycarbonyl group and PLHS fragments with a C-terminal glyco-imino-alkylxyalkylamide group.

摘要翻译： 提供了通过polo-box结构域结合polo样激酶的新型化合物。 在某些实施方案中，新化合物是PEG化肽。 根据本发明的聚乙二醇化肽表现出高PBD结合亲和力。 在某些实施方案中，聚乙二醇化肽还在整个细胞系统中获得活性。 本发明还提供通过马球结构域结合polo样激酶并具有减少的阴离子电荷的化合物。 还提供了聚乙二醇化肽的设计和/或合成方法及其使用方法。 本发明提供了化合物的使用方法和化合物的合成方法。 考虑到它们对Plk1的结合和抑制活性，本发明的化合物具有潜在的治疗活性。 它们基于氨基酸序列PLHSpT（磷酸化的Thr）。 存在时，PEG部分在N末端共价连接。 本发明还包括在Pro和/或His侧链上具有取代基的衍生物，磷酸基团上的取代基，用Gln取代His，用N-取代的Gly取代Pro，用Ala取代Ser，作为 以及具有N-末端烷氧基羰基的HS-pT片段和具有C-末端糖 - 亚氨基 - 烷基烷基酰胺基团的PLHS片段。

公开(公告)号：US09175038B2

公开(公告)日：2015-11-03

申请号：US13320726

申请日：2010-05-17

申请人： Terrence R. Burke, Jr. ,  Fa Liu ,  Kyung S. Lee ,  Jung-Eun Park

发明人： Terrence R. Burke, Jr. ,  Fa Liu ,  Kyung S. Lee ,  Jung-Eun Park

IPC分类号： A61K38/08 ,  A01K61/00 ,  C07K7/06 ,  A61K38/00

CPC分类号： C07K7/06 ,  A61K38/00

摘要： Found in various eukaryotic organisms, polo-like kinases (collectively, Plks) are a conserved subfamily of Ser/Thr protein kinases that play critical roles in cell proliferation. Provided herein are compounds that specifically inhibit the activity of Plks, specifically Plk1. Further provided herein are methods for use of the compounds for the treatment of hyperproliferative disorders, particularly cancer. Also provided are uses of the compounds for the preparation of a medicament.

摘要翻译： 在各种真核生物中发现，polo样激酶（统称为Plks）是Ser / Thr蛋白激酶的保守亚家族，在细胞增殖中起关键作用。 本文提供特异性抑制Plks活性的化合物，特别是Plk1。 本文还提供了用于治疗过度增殖性疾病，特别是癌症的化合物的方法。 还提供了化合物用于制备药物的用途。

公开(公告)号：US10266565B2

公开(公告)日：2019-04-23

申请号：US14111540

申请日：2012-04-12

申请人： Terrence R. Burke, Jr. ,  Fa Liu ,  Kyung S. Lee ,  Jung-Eun Park

发明人： Terrence R. Burke, Jr. ,  Fa Liu ,  Kyung S. Lee ,  Jung-Eun Park

IPC分类号： C07K7/06 ,  C07K1/00 ,  C07K5/08 ,  C12N9/12 ,  A61K47/60 ,  A61K38/00

摘要： Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.

公开(公告)号：US20120065146A1

公开(公告)日：2012-03-15

申请号：US13320726

申请日：2010-05-17

申请人： Terrence R. Burke, JR. ,  Fa Liu ,  Kyung S. Lee ,  Jung-Eun Park

发明人： Terrence R. Burke, JR. ,  Fa Liu ,  Kyung S. Lee ,  Jung-Eun Park

IPC分类号： A61K38/08 ,  C07K7/06 ,  A61P35/00 ,  C40B40/10

CPC分类号： C07K7/06 ,  A61K38/00

摘要： Found in various eukaryotic organisms, polo-like kinases (collectively, Plks) are a conserved subfamily of Ser/Thr protein kinases that play critical roles in cell proliferation. Provided herein are compounds that specifically inhibit the activity of Plks, specifically Plk1. Further provided herein are methods for use of the compounds for the treatment of hyperproliferative disorders, particularly cancer. Also provided are uses of the compounds for the preparation of a medicament.

摘要翻译： 在各种真核生物中发现，polo样激酶（统称为Plks）是Ser / Thr蛋白激酶的保守亚家族，在细胞增殖中起关键作用。 本文提供特异性抑制Plks活性的化合物，特别是Plk1。 本文还提供了用于治疗过度增殖性疾病，特别是癌症的化合物的方法。 还提供了化合物用于制备药物的用途。

公开(公告)号：US20080154297A1

公开(公告)日：2008-06-26

申请号：US12000475

申请日：2007-12-13

申请人： Eun-Kyue Lee ,  Young-Bae Park ,  Chang-Hun Song ,  Jung-Eun Park ,  Hak-Shin Kim ,  Sung-Jin Shin ,  Jeong-Han Kim

发明人： Eun-Kyue Lee ,  Young-Bae Park ,  Chang-Hun Song ,  Jung-Eun Park ,  Hak-Shin Kim ,  Sung-Jin Shin ,  Jeong-Han Kim

IPC分类号： A61B1/32

CPC分类号： A61B17/320016 ,  A61B1/313 ,  A61B17/00008 ,  A61B17/0218 ,  A61B90/37 ,  A61B2017/00796 ,  A61B2017/008 ,  A61B2017/00902 ,  A61B2017/320044

摘要： An endoscopic tissue dissector is disclosed. The endoscopic tissue dissector includes a head for incising and entering tissue, a body including an endoscope passage part coupled to the head and one side coupled to the head, and a handle coupled to the other side of the body. A transfer direction of a load applied to the handle is substantially identical to a transfer direction of a load applied to the body from the handle.

摘要翻译： 公开了一种内窥镜组织剥离器。 内窥镜组织解剖器包括用于切割和进入组织的头部，主体包括联接到头部的内窥镜通道部分和联接到头部的一侧，以及联接到身体的另一侧的手柄。 施加到手柄的负载的传送方向基本上与从手柄施加到身体的负载的传送方向相同。

公开(公告)号：US08044143B2

公开(公告)日：2011-10-25

申请号：US12641752

申请日：2009-12-18

申请人： Jung-Eun Park ,  Bang-Duk Kim ,  In-Sik Shim ,  Doo-Han Ha

发明人： Jung-Eun Park ,  Bang-Duk Kim ,  In-Sik Shim ,  Doo-Han Ha

IPC分类号： C08F8/00

CPC分类号： C08L33/08 ,  C08L51/04 ,  C08L67/02 ,  C08L69/00 ,  C08L2666/18 ,  C08L2666/02

摘要： Disclosed are a polyester/polycarbonate alloy resin composition that includes: (A) a mixed resin including (A-1) a polycarbonate resin having a weight average molecular weight ranging from about 30,000 to about 200,000 g/mol and (A-2) a polyester resin having an intrinsic viscosity of about 0.85 to about 1.52 dl/g; (B) an acryl-based resin; and (C) an impact-reinforcing agent, and a molded product made using the polyester/polycarbonate alloy resin composition.

摘要翻译： 公开了一种聚酯/聚碳酸酯合金树脂组合物，其包含：（A）包含（A-1）重均分子量为约30,000至约200,000g / mol的聚碳酸酯树脂和（A-2）a 特性粘度为约0.85至约1.52dl / g的聚酯树脂; （B）丙烯酸类树脂; 和（C）冲击增强剂，以及使用聚酯/聚碳酸酯合金树脂组合物制成的成型体。

公开(公告)号：US20080284711A1

公开(公告)日：2008-11-20

申请号：US12153264

申请日：2008-05-15

申请人： Ji-Hwan Seol ,  Woo-Jin Kim ,  Jung-Eun Park ,  Moo-Yong Hyun

发明人： Ji-Hwan Seol ,  Woo-Jin Kim ,  Jung-Eun Park ,  Moo-Yong Hyun

IPC分类号： G09G3/36

CPC分类号： G09G3/294 ,  G09G3/2059 ,  G09G3/293 ,  G09G2310/0218 ,  G09G2330/021 ,  G09G2360/16

摘要： A method and apparatus for automatically controlling power of address data in a plasma display panel (PDP), and a PDP device including the apparatus are provided. In this method, first, a difference-sum of pixel value differences between adjacent pixels successively arranged along a column of block is calculated. Then, an address power control level corresponding to the calculated difference-sum for each block is determined. Thereafter, gain information for each block on the basis of the address power control level for each block is determined. Next, a gain for each block corresponding to the gain information for each block is output. Then, the input image signal is multiplied by the gain for each block to correct the input image signal to output the corrected image signal. Accordingly, power consumption, noise, and generation of heat are reduced, and also the brightness is improved.

摘要翻译： 提供一种用于自动控制等离子体显示面板（PDP）中的地址数据的功率的方法和装置，以及包括该装置的PDP装置。 在该方法中，首先，计算沿着一列的连续排列的相邻像素之间的像素值差的差分和。 然后，确定与每个块的计算差分和相对应的地址功率控制电平。 此后，确定基于每个块的地址功率控制电平的每个块的增益信息。 接下来，输出与每个块的增益信息相对应的每个块的增益。 然后，输入图像信号乘以每个块的增益以校正输入图像信号以输出校正的图像信号。 因此，能量消耗，噪声和热量的产生减少，亮度提高。

公开(公告)号：US20110159293A1

公开(公告)日：2011-06-30

申请号：US12980753

申请日：2010-12-29

申请人： Jung-Eun Park ,  Doo-Han Ha

发明人： Jung-Eun Park ,  Doo-Han Ha

IPC分类号： C08L55/02 ,  C08L51/00 ,  B32B27/06

CPC分类号： C08L69/00 ,  C08L51/04 ,  C08L55/02 ,  C08L2205/02 ,  Y10T428/31507

摘要： Disclosed is a polycarbonate resin composition that includes (A) a polycarbonate resin, (B) a rubber modified vinyl-based graft copolymer including a rubbery polymer having an average particle diameter of about 0.05 to about 0.5 μm, and (C) a rubber modified vinyl-based copolymer including a rubber-phase particle having an average particle diameter of about 0.6 to about 10 μm as a dispersion phase. A molded product using the polycarbonate resin composition is also provided.

摘要翻译： 公开了一种聚碳酸酯树脂组合物，其包含（A）聚碳酸酯树脂，（B）包含平均粒径为约0.05〜约0.5μm的橡胶状聚合物的橡胶改性乙烯基类接枝共聚物，（C）橡胶改性 乙烯基类共聚物，其包含平均粒径为约0.6〜约10μm的橡胶相颗粒作为分散相。 还提供了使用聚碳酸酯树脂组合物的成型体。

公开(公告)号：US20110059994A1

公开(公告)日：2011-03-10

申请号：US12865127

申请日：2008-01-31

申请人： Justin Changjoon Lee ,  Eun-Joo Roh ,  Jin-Kyu Choi ,  Kyung-Suk Han ,  Jung-Eun Park ,  Sang-Soo Kang

发明人： Justin Changjoon Lee ,  Eun-Joo Roh ,  Jin-Kyu Choi ,  Kyung-Suk Han ,  Jung-Eun Park ,  Sang-Soo Kang

IPC分类号： A61K31/522 ,  A61P35/00 ,  A61P25/00

CPC分类号： A61K31/522

摘要： A composition for preventing and/or treating brain tumor, containing caffeine and/or its analog, and/or their pharmaceutically acceptable salt, as an active ingredient, is provided. The composition for preventing or treating brain tumor has an activity to inhibit invasion, migration, and proliferation of brain tumor cells, and thereby very effective for the prevention and treatment of brain tumor.

摘要翻译： 提供了用于预防和/或治疗含有咖啡因和/或其类似物的脑肿瘤和/或其药学上可接受的盐作为活性成分的组合物。 用于预防或治疗脑肿瘤的组合物具有抑制脑肿瘤细胞的侵袭，迁移和增殖的活性，因此对预防和治疗脑肿瘤非常有效。