公开(公告)号：US09353140B2

公开(公告)日：2016-05-31

申请号：US13512255

申请日：2010-11-24

Applicant: Zeljko M. Prijovic ,  Yu-Lin Leu ,  Steve R. Roffler

Inventor： Zeljko M. Prijovic ,  Yu-Lin Leu ,  Steve R. Roffler

IPC: A61K31/706 ,  C07H15/26 ,  A61P35/00 ,  C07H15/203

CPC classification number: C07H15/203

Abstract: The invention relates to the synthesis of a second-generation camptothecin glucuronide prodrug (BQC-G) of a potent anticancer camptothecin derivative 5,6-dihydro-4H-benzo[de]quinoline-camptothecin (BQC). BQC-G was over 4000 times more water soluble than BQC, displayed good stability in human plasma and was an excellent substrate for enzymatic hydrolysis by bacterial and human β-glucuronidases. BQC-G was about 30 times less toxic than BQC, but was as toxic as BQC after hydrolysis of the glucuronide moiety by β-glucuronidase. In the presence of human serum albumin, BQC-G displayed lower cytotoxicity (IC50=1080 nM) but could be activated by β-glucuronidase to display potent activity (IC50=13.3 nM).

Abstract translation: 本发明涉及有效的抗癌喜树碱衍生物5,6-二氢-4H-苯并[de]喹啉 - 喜树碱（BQC）的第二代喜树碱葡糖苷酸前药（BQC-G）的合成。 BQC-G比BQC水溶液超过4000倍，在人血浆中表现出良好的稳定性，是细菌和人类 - 葡萄糖醛酸酶进行酶水解的优良底物。 BQC-G的毒性比BQC低约30倍，但与葡萄糖醛酸苷酶部分水解后，BQC毒性相当。 在人血清白蛋白存在下，BQC-G显示出更低的细胞毒性（IC50 = 1080nM），但可以被β-葡糖醛酸糖苷酶活化以显示有效活性（IC50 = 13.3nM）。

公开(公告)号：US09324552B2

公开(公告)日：2016-04-26

申请号：US13713792

申请日：2012-12-13

Applicant: Academia Sinica

Inventor： Kent J. Gillig ,  Chung-Hsuan Chen

IPC: H01J49/28 ,  G01N27/62 ,  H01J49/26 ,  H01J49/22 ,  H01J49/00

CPC classification number: H01J49/26 ,  G01N27/624 ,  H01J49/0031 ,  H01J49/22

Abstract: A periodic field differential mobility analyzer apparatus for separating and identifying ionic analytes employs a series of elongated parallel channels, a pump, a first voltage providing an electric field Ex in a direction opposing the gas flow, a second voltage providing an electric field Ey in a direction perpendicular to the gas flow, an ion source, and a detector. The periodic field differential mobility analyzer provides high resolution and sensitivity.

Abstract translation: 用于分离和鉴定离子分析物的周期性场差分迁移率分析仪装置采用一系列细长的平行通道，泵，在与气流相反的方向上提供电场Ex的第一电压，在第一电压中提供电场Ey 垂直于气流的方向，离子源和检测器。 周期场差分迁移率分析仪提供高分辨率和灵敏度。

公开(公告)号：US09321818B2

公开(公告)日：2016-04-26

申请号：US12703102

申请日：2010-02-09

Applicant: Chung-Hsuan Chen ,  Wei-Chao Chang ,  Michael Hsiao ,  Ming-Shyan Huang ,  Chih-Jen Yang

Inventor： Chung-Hsuan Chen ,  Wei-Chao Chang ,  Michael Hsiao ,  Ming-Shyan Huang ,  Chih-Jen Yang

IPC: C12Q1/00 ,  C07K14/47 ,  A61K31/7088 ,  A61K33/24 ,  A61K38/04 ,  A61K45/06 ,  G01N33/574 ,  G01N30/72 ,  G01N33/68

CPC classification number: C07K14/4723 ,  A61K31/7088 ,  A61K33/24 ,  A61K38/04 ,  A61K45/06 ,  G01N30/72 ,  G01N33/57423 ,  G01N33/57488 ,  G01N33/6851 ,  A61K2300/00

Abstract: Methods for diagnosis of non-small cell lung cancers by detection of endogenous peptides in exhaled breath condensate (EBC) are provided. Diagnostic peptides derived from dermcidin (DC) are provided. A specific dermcidin-derived peptide E-R11, having the sequence ENAGEDPGLAR (SEQ ID NO:2), is provided. E-R11 peptide levels in EBC, as measured by mass spectrometry (MS), are highly diagnostic of non-small cell lung cancers. A method for inhibiting growth of lung cancer cells by inhibiting DCD expression by RNA interference also is provided.

Abstract translation: 提供了通过检测呼出气体浓缩物（EBC）中的内源肽来诊断非小细胞肺癌的方法。 提供衍生自皮肤霉素（DC）的诊断肽。 提供具有序列ENAGEDPGLAR（SEQ ID NO：2）的具体的皮肤霉素衍生肽E-R11。 通过质谱（MS）测量，EBC中的E-R11肽水平是非小细胞肺癌的高度诊断。 还提供了通过RNA干扰抑制DCD表达来抑制肺癌细胞生长的方法。

公开(公告)号：US20160083337A1

公开(公告)日：2016-03-24

申请号：US14960025

申请日：2015-12-04

Applicant: Academia Sinica

Inventor： Chi-Huey Wong ,  Che Alex Ma ,  Ting-Jen Rachel Cheng ,  Wei-Chieh Cheng

IPC: C07C235/64 ,  C07C235/84

CPC classification number: C07C235/64 ,  C07C235/84 ,  C07K2299/00 ,  C12Q1/18 ,  C12Q1/48 ,  G01N2333/91102 ,  G01N2500/00

Abstract: The crystal structure at 2.16 Å resolution of the full-length bacterial bifunctional transglycosylase penicillin-binding protein 1b (PBP1b) from Escherichia coli, in complex with its inhibitor moenomycin, is provided. The atomic coordinates of the complex as well as the moenomycin binding site are provided. Three dimensional structures of amino acid residues involved in moenomycin binding and transglycosylation activity are identified. Binding site for peptidoglycan synthesis inhibitors comprising inhibitor-binding site comprises amino acid residues from at least one of transglycosylase (TG), UvrB domain 2 homolog (UB2H) and transmembrane (TM) domains of PBP1b are identified at an atomic level of resolution. Methods for rational drug design based on the atomic coordinates are provided. Methods for screening for antibiotics based on anisotropic binding assay and transglycosylase inhibitor assays are provided. Novel antibiotics based on the screening assays of the invention are disclosed.

Abstract translation: 提供了与其抑制剂新霉素复合的大肠杆菌全长细菌双功能转糖苷酶青霉素结合蛋白1b（PBP1b）的分辨率为2.16的晶体结构。 提供复合物的原子坐标以及霉酚霉素结合位点。 鉴定了涉及霉酚霉素结合和转糖基化活性的氨基酸残基的三维结构。 包含抑制剂结合位点的肽聚糖合成抑制剂的结合位点包含以分辨率的原子级别鉴定的来自转糖苷酶（TG），UvrB结构域2同源物（UB2H）和跨膜（TM）结构域中的至少一种的氨基酸残基。 提供了基于原子坐标的合理药物设计方法。 提供了基于各向异性结合测定法和转糖苷酶抑制剂测定法筛选抗生素的方法。 公开了基于本发明筛选试验的新型抗生素。

公开(公告)号：US09255130B2

公开(公告)日：2016-02-09

申请号：US13056975

申请日：2009-07-29

Applicant: John Yu ,  Alice Yu ,  Ming-Wei Kuo ,  Jui-Chin Chang

Inventor： John Yu ,  Alice Yu ,  Ming-Wei Kuo ,  Jui-Chin Chang

IPC: A61K48/00 ,  C07K14/47 ,  C07K16/18 ,  C12N15/113 ,  C12Q1/68 ,  G01N33/68

CPC classification number: C07K14/4747 ,  A61K48/005 ,  C07K16/18 ,  C12N15/113 ,  C12N2799/025 ,  C12Q1/6876 ,  G01N33/6854

Abstract: Methods and compositions for treating retinal diseases comprising therapeutic amounts of a compound selected from a normal Puf-A gene product, an active polypeptide fragment thereof, an analog thereof or a peptidomimetic thereof. Vectors, including AAV vectors comprising the therapeutic compound are provided. Puf-A compositions suitable for subretinal, intravitreal, topical, subconjunctival, retrobulbar, periocular, suprachoroidal, or intraocular administration are provided. Methods for screening siRNA, RNAi and shRNA, small molecules and monoclonal antibodies that inhibit Puf-A target activity and reduce apoptosis are provided.

Abstract translation: 用于治疗视网膜疾病的方法和组合物包括治疗量的选自正常Puf-A基因产物，其活性多肽片段，其类似物或肽模拟物的化合物。 提供载体，包括包含治疗化合物的AAV载体。 提供适用于视网膜下，玻璃体内，局部，结膜下结膜，球后，眼周，脉络膜或眼内给药的Puf-A组合物。 提供了筛选siRNA，RNAi和shRNA，抑制Puf-A靶活性和减少细胞凋亡的小分子和单克隆抗体的方法。

公开(公告)号：US09240555B2

公开(公告)日：2016-01-19

申请号：US13677317

申请日：2012-11-15

Applicant: Au Optronics Corporation ,  Academia Sinica

Inventor： Chin-Ti Chen ,  Yi-Ting Lee ,  Meng-Ting Lee ,  Po-Hsuan Chiang ,  Chieh-Wei Chen ,  Chung-Chun Lee

IPC: H01L51/54 ,  C09K11/06 ,  H01L51/00 ,  C07D209/86 ,  C09B57/00 ,  C09B57/10 ,  C09B69/00 ,  H01L51/50

CPC classification number: H01L51/0061 ,  C07D209/86 ,  C09B57/00 ,  C09B57/008 ,  C09B57/10 ,  C09B69/008 ,  C09K11/06 ,  C09K2211/1007 ,  C09K2211/1011 ,  C09K2211/1014 ,  C09K2211/1022 ,  C09K2211/1029 ,  C09K2211/185 ,  H01L51/0067 ,  H01L51/0068 ,  H01L51/0072 ,  H01L51/0081 ,  H01L51/0085 ,  H01L51/5016 ,  H01L2251/308

Abstract: An organic luminescent material includes a host luminescent material and a guest luminescent material. The host luminescent material includes a compound represented by formula (1), where n is 0˜8; R2 and R3 respectively represent H, CF3, CN, CH3 or C5H11; R1 is CH3 or one of substituents shown as follows:

Abstract translation: 有机发光材料包括主发光材料和客体发光材料。 主体发光材料包括由式（1）表示的化合物，其中n为0〜8; R2和R3分别表示H，CF3，CN，CH3或C5H11; R1是CH3或如下所示的取代基之一：

公开(公告)号：US09229012B2

公开(公告)日：2016-01-05

申请号：US13942529

申请日：2013-07-15

Applicant: Taipei Medical University ,  Academia Sinica

Inventor： Wei-Chung Yang ,  Hwei-Jiung Wang ,  Shui-Tsung Chen ,  Ken-Fen Lu ,  Ming-Chi Peng

IPC: G01N33/53 ,  G01N33/68 ,  C07K16/18 ,  C07K16/38

CPC classification number: G01N33/6893 ,  C07K16/18 ,  C07K16/38 ,  C07K2317/34 ,  G01N2333/8125 ,  G01N2800/364

Abstract: Provided herein are monoclonal antibodies with a high binding affinity to isoforms of alpha 1-antitrypsin (A1AT), hybridoma cells producing the same, and their uses in diagnosing and/or detecting endometriosis from a serum sample of a subject suspicious of having endometriosis or a subject under health examination.

Abstract translation: 本文提供对α1-抗胰蛋白酶（A1AT）的同种型具有高结合亲和力的单克隆抗体，产生相同的杂交瘤细胞的单克隆抗体及其在诊断和/或检测可疑患有子宫内膜异位症的受试者血清样品中的子宫内膜异位症的用途 受检体检。

公开(公告)号：US20150372247A1

公开(公告)日：2015-12-24

申请号：US14824580

申请日：2015-08-12

Applicant: ACADEMIA SINICA

Inventor： Kuei-Hsien CHEN ,  Hsieh-Cheng HAN ,  Ching-Chun CHANG ,  Li-Chyong CHEN ,  Chan-Yi DU

IPC: H01L51/42 ,  H01L51/44

CPC classification number: H01L51/424 ,  H01L51/0036 ,  H01L51/0043 ,  H01L51/0046 ,  H01L51/0047 ,  H01L51/005 ,  H01L51/0055 ,  H01L51/4246 ,  H01L51/44 ,  Y02E10/549

Abstract: The present invention is related to a process for reducing surface energy of a hole transport layer. The disclosed process comprises providing a hole transport layer; and providing a fluorine-containing layer directly on said hole transport layer. The configuration of said fluorine-containing layer reduces the structural disorder of an active layer and is able to recover a moisture-degraded hole transport layer, and thereby improves the performance of an electric device containing the same.

Abstract translation: 本发明涉及一种降低空穴传输层的表面能的方法。 所公开的方法包括提供空穴传输层; 并在所述空穴传输层上直接提供含氟层。 所述含氟层的结构减少了活性层的结构紊乱，能够回收水分恶化的空穴传输层，从而提高含有该层的电气装置的性能。

公开(公告)号：US20150342973A1

公开(公告)日：2015-12-03

申请号：US14578453

申请日：2014-12-21

Applicant: Chi-Huey WONG ,  Ting-Jen CHENG ,  Che Alex MA ,  Wei-Chieh CHENG

Inventor： Chi-Huey WONG ,  Ting-Jen CHENG ,  Che Alex MA ,  Wei-Chieh CHENG

IPC: A61K31/702

CPC classification number: A61K31/702 ,  A61K31/19 ,  A61K31/365 ,  A61K31/427 ,  A61K31/715 ,  C07K14/195 ,  C07K14/21 ,  C07K14/22 ,  C07K14/235 ,  C07K14/25 ,  C07K14/255 ,  C07K14/26 ,  C07K14/265 ,  C07K14/31 ,  C07K14/315 ,  C07K14/3156 ,  C07K14/32 ,  C07K14/33 ,  G01N33/573 ,  G01N2333/91091 ,  Y02A50/473 ,  Y02A50/475 ,  Y02A50/481

Abstract: Moenomycin inhibits bacterial growth by clocking the transglycosylase activity of class A penicillin-binding proteins (PBPs), which are key enzymes in bacterial cell wall synthesis. The binding affinities of moenomycin A with various truncated PBPs were compared showing that the transmembrane domain is important for moenomycin binding. Full-length class-A PBPs from 16 bacterial species were produced, and their binding activities showed a correlation with the antimicrobial activity of moenomycin against Enterococcus faecalis and Staphylococcus aureus. Moreover, a fluorescence anisotropy-based high-throughput assay was developed and used successfully for identification of transglycosylase inhibitors.

公开(公告)号：US09144591B2

公开(公告)日：2015-09-29

申请号：US14055545

申请日：2013-10-16

Applicant: Academia Sinica

Inventor： Pei-Wen Hsiao

IPC: A61K36/28

CPC classification number: A61K36/28

Abstract: Disclosed herein is a method for treating an androgen-stimulated disease in a subject in need thereof by administering to the subject a composition containing an effective amount of an inhibitor of IκB kinase subunit α activity. The composition can also be administered to a subject at high risk for prostate cancer as a method for reducing the subject's risk thereof. A further method relates to identifying a modulator of transcriptional activity regulated by IκB kinase subunit α. Still another method relates to determining the IκB kinase subunit α-regulated transcriptional activity regulated by in a non-human mammalian test subject.

Abstract translation: 本文公开了通过向受试者施用含有有效量的I＆kgr B激酶亚基α活性抑制剂的组合物来治疗有需要的受试者中的雄激素刺激的疾病的方法。 该组合物也可以作为降低受试者风险的方法施用于患有前列腺癌的高风险的受试者。 另一种方法涉及鉴定由I＆kgr; B激酶亚基α调节的转录活性的调节剂。 另一种方法涉及确定由非人哺乳动物测试受试者调节的I激酶亚基α调节的转录活性。