公开(公告)号：EP2872474A2

公开(公告)日：2015-05-20

申请号：EP13747540.6

申请日：2013-07-10

申请人： Georgia State University Research Foundation, Inc. ,  Emory University ,  Children's Healthcare of Atlanta, Inc.

发明人： WANG, Binghe ,  DAI, Chaofeng ,  DRAGANOV, Alexander ,  YANG, Xiaochuan ,  SUN, Guojing ,  YANG, Chunhao ,  CHEN, Weixuan ,  NI, Nanting ,  ZHOU, Muxiang ,  GU, Lubing

IPC分类号： C07C50/34 ,  C07C50/38 ,  C07C69/95 ,  C07C225/24 ,  C07C233/31 ,  C07C233/33 ,  C07C235/84 ,  C07C237/04 ,  C07C247/04 ,  C07C247/10 ,  C07C255/27 ,  C07C311/08 ,  C07C323/22 ,  C07D211/06 ,  C07D213/50

CPC分类号： C07C233/33 ,  C07C66/02 ,  C07C69/95 ,  C07C225/36 ,  C07C233/31 ,  C07C235/16 ,  C07C235/84 ,  C07C237/04 ,  C07C247/04 ,  C07C247/10 ,  C07C247/12 ,  C07C255/19 ,  C07C311/08 ,  C07C323/60 ,  C07C2603/24 ,  C07D213/56 ,  C07D213/61 ,  C07D213/70 ,  C07D261/08 ,  C07D267/12 ,  C07D295/15 ,  C07D307/54 ,  C07D333/24

摘要： Rhein analogues that exhibit anti-proliferative activity, particular against cancer cells, are described herein. In some embodiments, the compounds contain a flat or planar ring system. Such rings system by facilitate non-covalent binding of the compounds to the DNA complex, such as by intercalation. In some embodiment, the compounds contain a flat or planar ring system as described above and one or more substituents which are alkylating moieties, electrophilic groups or Michael acceptors or groups which contain one or more alkylating moieties, electrophilic groups and/or Michael acceptors. The compounds described herein can also contain one more functional groups to improve the solubility of the compounds.

摘要翻译： 本文描述了表现出抗癌增殖活性的特异性抗癌细胞的大黄酸类似物。 在一些实施方案中，化合物包含平面或平面环系统。 通过促进化合物与DNA复合物的非共价结合，例如通过嵌入，这种环系统。 在一些实施方案中，化合物包含如上所述的平面或平面环体系和一个或多个取代基，其是烷基化部分，亲电基团或迈克尔受体或含有一个或多个烷基化部分，亲电子基团和/或迈克尔受体的基团。 本文所述的化合物还可以含有一个以上官能团以改善化合物的溶解度。

公开(公告)号：EP2310054A2

公开(公告)日：2011-04-20

申请号：EP09807338.0

申请日：2009-08-14

申请人： Georgia State University Research Foundation, Inc.

发明人： WANG, Binghe ,  LI, Minyong ,  NI, Nanting ,  LIU, Yidan

IPC分类号： A61K48/00 ,  A61K31/7088 ,  C07H21/00 ,  A61K38/36 ,  A61P7/02

CPC分类号： C12N15/115 ,  A61K31/7088 ,  C12N2310/16

摘要： Boronic acid-modified DNA-based aptamers can be selected to recognize fibrinogen through binding at a glycosylation site and thus are useful for probing the effect of glycosylation pattern changes on the ability for fibrinogen to mediate blood coagulation. In addition, the aptamers of the disclosure also have anticoagulation effects due to their binding to fibrinogen and its cleavage product fibrin. The present disclosure, therefore, encompasses methods for inhibiting fibrin coagulation with an aptamer capable of specifically binding to a glycosylation site of fibrinogen or fibrin. The disclosure further provides oligonucleotide aptamers comprising at least one nucleotide having a boronic acid thereon, where the aptamer is capable of selectively binding to a glycosylation site of fibrinogen, or the derivative thereof.

摘要翻译： 可以选择硼酸修饰的基于DNA的适体通过在糖基化位点结合来识别纤维蛋白原，因此可用于探测糖基化模式改变对纤维蛋白原介导血液凝固的能力的影响。 此外，本公开的适体由于其与纤维蛋白原及其裂解产物纤维蛋白的结合而具有抗凝作用。 因此，本公开内容包括用能够特异性结合纤维蛋白原或纤维蛋白的糖基化位点的适体抑制纤维蛋白凝固的方法。 本公开还提供了包含至少一个在其上具有硼酸的核苷酸的寡核苷酸适体，其中适体能够选择性地结合纤维蛋白原或其衍生物的糖基化位点。

公开(公告)号：EP2155705A2

公开(公告)日：2010-02-24

申请号：EP08828361.9

申请日：2008-06-06

申请人： Georgia State University Research Foundation, Inc.

发明人： WANG, Binghe ,  NI, Nanting ,  WANG, Junfeng ,  LU, Chung-Dar ,  CHOU, Han-Ting ,  LI, Minyong ,  ZHENG, Shilong ,  CHENG, Yunfeng ,  PENG, Hanjing

IPC分类号： C07D291/08 ,  C07D307/91 ,  C07D215/04 ,  C07D333/76 ,  A61P31/04

CPC分类号： C07D333/34 ,  C07F5/025

摘要： The present disclosure encompasses compounds and compositions that are useful as specific AI-2 antagonists for the control of bacterial quorum sensing. Although the AI-2 antagonists according to the present disclosure may not have bactericidal effect, their ability to attenuate virulence, drug resistance, and/or biofilm formation have therapeutic benefits. In addition, the AI-2 antagonists of the present disclosure can also be used as tools to probe bacterial AI-2 functions. The present disclosure also encompasses methods for inhibiting or attenuating microbial virulence, biofilm formation, and drug resistance. The methods are suitable for preventing bacteria from accruing and forming extensive biofilms that may be a health or hygiene hazard or a physical issue, such as in the blockage of water or fuel lines.