专利号:US-2021220331-A1 优先权日:2016-05-03 标题:Inhibitors of ires-mediated protein synthesis 发明人:GERA JOSEPH F; LICHTENSTEIN ALAN; JUNG MICHAEL E; LEE JIHYE; HOLMES BRENT; BENAVIDES-SERRATO ANGELICA 权利人:UNIV CALIFORNIA; THE UNITED STATE GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS 摘要:This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.
专利号:US-2024174698-A1 优先权日:2022-09-23 标题 :Modular synthesis of 1,2-azaborines via ring-opening bn-isostere benzannulation 发明人:DONG GUANGBIN; LYU HAIRONG; CHEN ZHIJIE; WU YIFEI; CHOI SHINYOUNG 权利人:UNIV CHICAGO 摘要:The present disclosure relates generally to 1,2-azaborines and methods of making the same.
专利号:US-12221419-B2 优先权日:2022-03-30 标题:Abietanes and methods of making and using the same 发明人:FREDERICH JAMES H; SOLANS MEGAN M 权利人:FLORIDA STATE UNIV RESEARCH FOUNDATION INCORPORATED; UNIV FLORIDA STATE RES FOUND 摘要:In accordance with the purpose(s) of the present disclosure, as embodied and broadly described herein is versatile polyene cyclization strategy that exploits conjugated β-ionyl derivatives. Photomediated disruption of the extended Ï€-system within these chromophores unveils a contra-thermodynamic polyene that engages in a Heck-type cyclization to afford [4.4.1]-propellanes. The connectivity of overbred polycycles generated from this process is controlled by the position of the requisite C-Halide bond. Thus, compared to conventional biomimetic polyene cyclization, this approach allows for complete control of regiochemistry and facilitates incorporation of both electron-rich and electron-deficient (hetero)aryl groups. This strategy was successfully applied to the total synthesis of abietanes such as, for example, taxodione and salviasperanol, two isomeric abietane-type diterpenes that previously could not be prepared along the same synthetic pathway.
专利号:US-11932558-B1 优先权日:2020-03-02 标 题 :Piezocatalysis using piezoelectric polymers 发明人:EULER WILLIAM B; THACH ANGELA; SUMATHIRATHNE LASANTHI; CROMWELL BENJAMIN B; DUBNICKA MARA 权利人:UNIV OF RHODE ISLAND BOARD OF TRUSTEES 摘要:A piezoelectric polymer used as a piezocatalyst, and methods of manufacture and use therefor. A preferred piezoelectric polymer is poly(vinylidene difluoride) (PVDF) due to its piezoelectric response and good flexibility. The polymer can be doped with a metal, metal salt, metal carbonyl, metal oxide such as ZnO, Co 2 O 3 , or TiO 2 , or ion such as Cr 3+ , Co 2+ , or Zn 2+ . The dopant can be chosen so that when the polymer is PVDF the dopant increases the amount of β-phase PVDF and/or γ-phase PVDF relative to α-phase PVDF, thereby increasing the piezocatalytic response of the polymer. The compound to be decomposed can be adsorbed on the surface of the piezoelectric polymer. Applications include wastewater treatment, CO 2 capture and reduction, hydroformylation, water splitting, and ammonia synthesis.
专利号:US-12312314-B2 优先权日:2018-05-16 标题:Methods and compositions for terpenoid tricycloalkane synthesis 发明人:GRENNING ALEXANDER JAMES; SCOTT SARAH 权利人:UNIV FLORIDA 摘要:In one aspect, the disclosure relates to methods for preparation of intermediates useful for the preparation of terpenoid cores. In a further aspect, the disclosed methods pertain to the preparation of compounds comprising a terpenoid core or scaffold, such as 6/7/5 tricycloalkanes. The disclosed methods utilize abundant starting materials and simple reaction sequences that can be used to tunably and scalably assemble common terpenoid cores. In various aspects, the present disclosure pertains to compounds prepared using the disclosed methods. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
专利号:US-11634452-B2 优先权日:2017-12-11 标 题:Compounds for treating neurodegenerative disorders 发明人:RABHI CHÉRIF; CARIEL LÉON; DA COSTA NOBLE CHRISTIAN; OUAZZANI JAMAL; ARCILE GUILLAUME; LE GOFF GÉRALDINE 权利人:ETHNODYNE; CENTRE NAT RECH SCIENT 摘要:The invention relates to compounds of formula (I), their method of synthesis as well as their use to treat neurodegenerative disorders.
1: Lee EJ, Charles JF, Sinha I, Neppl RL. Loss of HNRNPU in Skeletal Muscle Increases Intramuscular Infiltration of Ly6C Positive Cells, leading to Muscle Atrophy through Activation of NF-κB Signaling. Adv Biol (Weinh). 2024 Jul;8(7):e2400152. doi: 10.1002/adbi.202400152. Epub 2024 May 26. 14(2):163. doi: 10.3390/jpm14020163. 3: Yang H, Cai X, Qiu M, Deng C, Xue H, Zhang J, Yang W, XianZhong W. Heat stress induces ferroptosis of porcine Sertoli cells by enhancing CYP2C9-Ras- JNK axis. Theriogenology. 2024 Feb;215:281-289. doi: 10.1016/j.theriogenology.2023.11.027. Epub 2023 Dec 9. 92:117417. doi: 10.1016/j.bmc.2023.117417. Epub 2023 Jul 17.
合成参考文献
参考文献:10.1016/s0076-6879(05)07046-1 摘要:Berzat AC, Brady DC, Fiordalisi JJ, Cox AD. Using inhibitors of prenylation to block localization and transforming activity. Methods Enzymol. 2006;407():575–97. doi: 10.1016/s0076-6879(05)07046-1. 参考文献:10.1016/j.bcp.2006.05.007 摘要:Erlich S, Tal-Or P, Liebling R, Blum R, Karunagaran D, Kloog Y, Pinkas-Kramarski R. Ras inhibition results in growth arrest and death of androgen-dependent and androgen-independent prostate cancer cells. Biochem Pharmacol. 2006 Aug 14;72(4):427–36. doi: 10.1016/j.bcp.2006.05.007. 参考文献:10.1016/s0076-6879(07)00432-6 摘要:Rotblat B, Ehrlich M, Haklai R, Kloog Y. The Ras inhibitor farnesylthiosalicylic acid (Salirasib) disrupts the spatiotemporal localization of active Ras: a potential treatment for cancer. Methods Enzymol. 2008;439():467–89. doi: 10.1016/s0076-6879(07)00432-6. 参考文献:10.1016/j.ejmech.2014.05.018 摘要:Aguilar BJ, Nkembo AT, Duverna R, Poku RA, Amissah F, Ablordeppey SY, Lamango NS. Polyisoprenylated methylated protein methyl esterase: A putative biomarker and therapeutic target for pancreatic cancer. European Journal of Medicinal Chemistry. 2014 Jun;81():323–33. doi: 10.1016/j.ejmech.2014.05.018. 参考文献:10.1371/journal.pone.0171351 摘要:Schmukler E, Wolfson E, Elazar Z, Kloog Y, Pinkas-Kramarski R. Continuous treatment with FTS confers resistance to apoptosis and affects autophagy. PLoS ONE. 2017 Feb 02;12(2):e0171351. doi: 10.1371/journal.pone.0171351.