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1.发明申请ASSAYS USING AMYLOID PRECURSOR PROTEINS WITH MODIFIED BETA-SECRETASE CLEAVAGE SITES TO MONITOR BETA-SECRETASE ACTIVITY 审中-公开使用改性的BETA-SECRETASE CLEAVAGE SITES监测β-分泌酶活性的AMYLOID前驱蛋白的测定
公开(公告)号：WO2004099376A3
公开(公告)日：2005-08-11
申请号：PCT/US2004013451
申请日：2004-04-30
申请人： MERCK & CO INC , HAZUDA DARIA JEAN , DODSON ELIZABETH CHEN , LAI MING-TAIN , XU MIN , SHI XIAO-PING , SIMON ADAM J , WU GUOXIN , LI YUEMING , REGISTER ROBERT BRUCE
发明人： HAZUDA DARIA JEAN , DODSON ELIZABETH CHEN , LAI MING-TAIN , XU MIN , SHI XIAO-PING , SIMON ADAM J , WU GUOXIN , LI YUEMING , REGISTER ROBERT BRUCE
IPC分类号： A61K38/00 , C07K5/107 , C07K5/11 , C07K5/113 , C07K7/06 , C07K14/47 , C07K16/18 , C12P21/06 , C12Q1/37 , G01N33/50 , G01N33/68 , A61K38/07 , A61K38/08
CPC分类号： C07K7/06 , A01K2217/05 , A01K2267/0306 , A61K38/00 , C07K5/1016 , C07K5/1019 , C07K5/1021 , C07K14/4711 , C07K16/18 , C12P21/06 , C12Q1/37 , G01N33/5088 , G01N33/6896 , G01N2500/00 , G01N2800/52
摘要： Provided are methods of identifying inhibitors of beta-secretase that employ modified beta-secretase substrates. The modified beta-secretase substrates have beta-secretase cleavage sites that are altered from wild type. The amino acid sequences of the altered beta-secretase cleavage sites contain different amino acids in at least one of the positions P2-P1-P1'-P2' of the beta-secretase cleavage site. Many of the modified beta-secretase substrates are more efficient substrates for beta-secretase than are corresponding substrates having wild-type sequences, that is, these modified substrates are more susceptible to enzymatic breakdown by beta-secretase. Recombinant polynucleotide molecules encoding the modified beta-secretase substrates are provided. Antibodies that recognize cleavage products of the modified beta-secretase substrates are provided. Stable cell lines expressing the modified beta-secretase substrates are provided. Transgenic animals expressing the modified beta-secretase substrates are provided.
摘要翻译： 提供了鉴定使用修饰的β-分泌酶底物的β-分泌酶抑制剂的方法。 修饰的β-分泌酶底物具有从野生型改变的β-分泌酶切割位点。 改变的β-分泌酶切割位点的氨基酸序列在β-分泌酶切割位点的至少一个位置P2-P1-P1'-P2'中含有不同的氨基酸。 许多修饰的β-分泌酶底物比具有野生型序列的相应底物更有效的β-分泌酶底物，也就是说，这些修饰的底物更易受β-分泌酶的酶分解。 提供了编码经修饰的β-分泌酶底物的重组多核苷酸分子。 提供了识别修饰的β-分泌酶底物的切割产物的抗体。 提供了表达改良的β-分泌酶底物的稳定的细胞系。 提供了表达改良的β-分泌酶底物的转基因动物。
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公开(公告)号：WO2003099202A2
公开(公告)日：2003-12-04
申请号：PCT/US2003/015109
申请日：2003-05-14
IPC分类号： A61K
CPC分类号： C07D317/70 , C07C237/22 , C07C2601/04
摘要： The present invention provides compounds that are inhibitors of the proteolytic activity of the enzyme β-secretase, pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the compounds, processes for making the compounds, and methods of using the compounds to treat Alzheimer s disease.
摘要翻译： 本发明提供了作为β-分泌酶的蛋白水解活性的抑制剂，化合物的药学上可接受的盐，包含该化合物的药物组合物，制备该化合物的方法以及使用该化合物治疗阿尔茨海默病的方法的化合物。
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公开(公告)号：WO2022173840A1
公开(公告)日：2022-08-18
申请号：PCT/US2022/015834
申请日：2022-02-09
申请人： OBI PHARMA, INC. , LAI, Ming-Tain
摘要： The present invention provides antibody or the antigen-binding portion thereof bind to carbohydrate antigen, such as Globo series antigens (e.g. Globo H, SSEA-4 or SSEA-3). Also disclosed herein are pharmaceutical compositions and methods for the inhibition of cancer cells in a subject in need thereof. The pharmaceutical compositions comprise an antibody or an antigen-binding portion thereof and at least one pharmaceutically acceptable carrier.
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公开(公告)号：WO2022173772A1
公开(公告)日：2022-08-18
申请号：PCT/US2022/015720
申请日：2022-02-09
申请人： OBI PHARMA, INC. , LAI, Ming-Tain
IPC分类号： A61K35/17 , C07K16/28 , G01N33/574
摘要： The present disclosure relates to chimeric antigen receptors (CARs), which bind to Globo series antigens (e.g. Globo H, SSEA-3 or SSEA-4), including an antigen-binding fragment (Fab) or a single-chain variable fragment (scFv). Further, the present methods are also provided for administering CARs to a subject in an amount effective to inhibit cancer cells.
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公开(公告)号：WO2020018352A1
公开(公告)日：2020-01-23
申请号：PCT/US2019/041508
申请日：2019-07-12
发明人： HAZUDA, Daria Jean , LAI, Ming-Tain
IPC分类号： A61K31/7076 , A61P31/18
摘要： The instant invention relates to a method for reducing the risk for development of anti-viral treatment resistance due to an HIV mutation in a human subject infected with HIV, comprising administering EFdA in combination with one or more anti-viral agents.
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6.发明申请
公开(公告)号：WO2022231580A1
公开(公告)日：2022-11-03
申请号：PCT/US2021/029552
申请日：2021-04-28
申请人： OBI PHARMA, INC. , LAI, Ming-Tain
发明人： LI, Wan-Fen , WANG, Chun-Chung , CHEN, Lu-Tzu
IPC分类号： A61K31/396 , C07D203/22 , C07F9/02
摘要： A pharmaceutical composition, including a compound l-(3-(3-N,N- dimethylaminocarbonyl)phenoxyl-4-mtrophenyl)-l-ethyl-N,N'- bis(ethylene)phosphoramidate and at least one therapeutic agent including a chemotherapeutic agent or biological agent, and its medical use are provided.
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公开(公告)号：WO2022109601A1
公开(公告)日：2022-05-27
申请号：PCT/US2021/072513
申请日：2021-11-19
申请人： OBI PHARMA, INC. , LAI, Ming-Tain
发明人： YU, Cheng-Der, Tony , CHEN, I-Ju , LEE, Wei-Han , YANG, Chueh-Hao , TSAO, Chun-Yen , HSIEH, Chang-Lin , OU, Chien-Chih , TSAI, Chen-En
摘要： The disclosure provides a method of active immunotherapy for a cancer patient, comprising administering vaccines against Globo series antigens (i.e., Globo H, SSEA-3 and SSEA-4). Specifically, the method comprises administering Globo H-CRM197 (OBI-833/821) in patients with cancer. The disclosure also provides a method of selecting a cancer patient who is suitable as treatment candidate for immunotherapy. Exemplary immune response can be characterized by reduction of the severity of disease, including but not limited to, prevention of disease, delay in onset of disease, decreased severity of symptoms, decreased morbidity and delayed mortality.
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公开(公告)号：WO2020172506A1
公开(公告)日：2020-08-27
申请号：PCT/US2020/019176
申请日：2020-02-21
申请人： OBI PHARMA INC. , LAI, Ming-Tain
发明人： LAI, Ming-Tain , YU, Cheng-Der Tony , HSIEH, Yih-Huang , LIN, Shu-Yi , CHAO, Chin-Sheng , HSIEH, Yin-Cheng
摘要： A new process to synthesis of compound OBI-3424 R-form and S-form products is provided. The "R-form" compound OBI-3423 was first synthesized with 48% overall yield from compound OBI-3424-5 by installation of the labile phosphate motif at later stage. The stereo chemistry is established by 5 steps chemo-enzyme combination synthesis to afford 99% optical purity, After then, the "S-form" compound OBI-3424 is prepared with improving overall yield of 54% from compound OBI-3424-5. The stereo chemistry is established by 4 steps combination of chemo-enzyme synthesis with excellent optical purity of 99%.
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公开(公告)号：WO2023034762A2
公开(公告)日：2023-03-09
申请号：PCT/US2022/075612
申请日：2022-08-30
申请人： OBI PHARMA, INC. , LAI, Ming-Tain
IPC分类号： C07K16/30 , A61K39/395
摘要： The present disclosure relates to treating cancer patients with anti-dendritic cells (anti-DCs)/anti-immunogenic cell death (anti-ICD) bispecific engager combined with tumor ICD inducers to enhance the dendritic cell activity. Exemplary polyvalent proteins include at least one DC binding site and at least one ICD binding site. In certain embodiments, the binding sites may be linked through a constant immunoglobulin region. Anti-DC and anti-ICD monoclonal antibodies are also provided.
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公开(公告)号：WO2020198699A2
公开(公告)日：2020-10-01
申请号：PCT/US2020/025516
申请日：2020-03-27
申请人： OBI PHARMA, INC. , LAI, Ming-Tain
发明人： LAI, Ming-Tain , YU, Cheng-Der Tony , LAI, Ming-Tain , CHEN, I-Ju , CHEN, Yu-Jung , YANG, Ming-Chen
IPC分类号： G01N33/573
摘要： Methods and reagents suitable for in vitro diagnostic assay comprising a qualitative immunohistochemical assay using anti-Globo H antibodies and/or binding fragments thereof are provided. The method comprises the detection of Globo-H expression levels in formalin-fixed, paraffin-embedded (FFPE) cancer tissue using a visualization system. The Globo-H expression can be determined by using tumor scoring showing partial or complete staining at any intensity.
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