专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-2017283878-A1 优先权日:2015-12-11 标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING 权利人:ACADEMIA SINICA 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.
专利号:US-2024173256-A1 优先权日:2022-11-29 标 题:Hdl mimicking targeted drug delivery system for the treatment of solid tumors 发明人:SABNIS NIRUPAMA; LACKO ANDRAS; FUDALA RAFAL 权利人:UNIV OF NORTH TEXAS HEALTH SCIENCE CENTER 摘要:The present disclosure is directed to an SR-B1-targeting nanomicelle and compositions, methods of synthesis and methods of use thereof. The nanomicelle may be an HDL-mimetic drug delivery system and may be cross-linked with DSS. The composition may contain a therapeutic agent with the ability to treat cancers, especially sarcomas.
专利号:US-2016318862-A1 优先权日:2013-09-25 标 题:Synthesis of delta 12-pgj3 and related compounds 发明人:NICOLAOU KYRIACOS C; HERETSCH PHILIPP; HALE CHRISTOPHER R H; EL GHZAOUI ABDELLATIF EL MARROUNI; PULUKURI KIRAN KUMAR; YU RUOCHENG; GROVE CHARLES 权利人:UNIV RICE WILLIAM M 摘要:In one aspect, the present invention provides novel derivatives of Δ 12 -PGJ 3 and modular synthetic pathways to obtaining Δ 12 -PGJ 3 and derivatives thereof. In some aspects, the present derivatives of Δ 12 -PGJ 3 are useful as chemotherapeutic agents. The present disclosure also describes compositions of these derivatives as well as methods of use of the derivatives thereof.
专利号:US-10590158-B2 优先权日:2015-06-29 标题:Total synthesis of shishijimicin A and analogs thereof 发明人:NICOLAOU KYRIACOS C; LI RUOFAN; LU ZHAOYONG; SOHN TE-IK; WOODS JAMES; PITSINOS EMMANOUIL N 权利人:UNIV RICE WILLIAM M 摘要:In one aspect, the present disclosure provides shishijimicin analogs of the formula: wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, antibody drug conjugates of the compounds are also provided.
专利号:US-11465997-B2 优先权日:2017-06-22 标 题 :Synthesis of disorazoles and analogs thereof as potent anticancer agents 发明人:NICOLAOU KYRIACOS C; BELLAVANCE GABRIEL; BUCHMAN MAREK; PULUKURI KIRAN KUMAR; RIGOL STEPHAN 权利人:UNIV RICE WILLIAM M 摘要:In one aspect, the present disclosure provides disorazole analogs of the formula: Formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.
1: Choi YJ, Shin HW, Chun YS, Leutou AS, Son BW, Park JW. Diacetoxyscirpenol as a new anticancer agent to target hypoxia-inducible factor 1. Oncotarget. 2016 Sep 20;7(38):62107-62122. doi: 10.18632/oncotarget.11529. 2: Yang S, De Boevre M, Zhang H, De Ruyck K, Sun F, Wang Z, Cao X, Shen J, De Saeger S, Zhang S. Unraveling the in vitro and in vivo metabolism of diacetoxyscirpenol in various animal species and human using ultrahigh-performance liquid chromatography-quadrupole/time-of-flight hybrid mass spectrometry. Anal Bioanal Chem. 2015 Nov;407(28):8571-83. doi: 10.1007/s00216-015-9016-4. Epub 2015 Sep 11. doi: 10.1021/jf2022176. Epub 2011 Aug 9. 4: Yang L, Zhao Z, Wu A, Deng Y, Zhou Z, Zhang J, Hou J. Determination of trichothecenes A (T-2 toxin, HT-2 toxin, and diacetoxyscirpenol) in the tissues of broilers using liquid chromatography coupled to tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2013 Dec 30;942-943:88-97. doi: 10.1016/j.jchromb.2013.10.034. Epub 2013 Oct 25. Review.
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