(2S)-N-[(1R)-1-(1,3,6,2-Dioxazaborocan-2-yl)-3-Methylbutyl]-3-Phenyl-2-(Pyrazin-2-Ylformamido)Propanamide置于盐酸体系中,用 甲醇,水 用作溶剂,以82.3%的收率获得硼替佐米 参考文献:Proteasome Inhibitor Delanzomib For Use In The Treatment Of Lupus 标题:Proteasome Inhibitor Delanzomib For Use In The Treatment Of Lupus 摘要:本发明提供了一种治疗狼疮的方法,包括向受试者施用化合物a的步骤.
专利号:US-12383499-B2 优先权日:2018-01-01 标题:Scale up synthesis of silicasome nanocarriers 发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG 权利人:UNIV CALIFORNIA 摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).
专利号:US-10973847-B2 优先权日:2017-06-30 标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof 发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.
专利号:US-2014275582-A1 优先权日:2013-03-14 标 题 :Chiral 2-arylpropyl-2-sulfinamide and chiral n-2-arylpropyl-2-sulfinylimines and synthesis thereof 发明人:LI GUIGEN 权利人:LI GUIGEN; UNIV TEXAS TECH; NANJING UNIVERSITY INST OF CHEMISTRY AND BIOMEDICAL SCIENCES 摘要:Provided herein are novel chiral sulfinamide and imine compounds. Also provided herein are methods of synthesizing novel chiral sulfinamide and imine compounds comprising simplified purification methods when compared to prior methods. The novel chiral sulfinamide and imine compounds are useful, for example, in the synthesis of complex natural products and pharmaceutical important compounds.
专利号:US-2024209029-A1 优先权日:2021-04-21 标题:Adiponectin glycopeptides and compositions and methods of use thereof 发明人:WANG YU; LI XUECHEN; XU AIMIN; WU HONGXIANG; ZHANG YIWEI; LI YUANXIN 权利人:UNIV HONG KONG 摘要:An improved method for the chemical synthesis of glycosylated peptides has been developed. The method uses stereoselective glycan synthesis and chemical peptide ligation to produce glycopeptides at lower-cost and with higher efficiency/yield compared to conventional methods. In particular, a method for the large-scale, chemical synthesis of hydroxylated amino acid building blocks and glycosylated amino acids suitable for solid phase peptide synthesis (SPPS) are disclosed. SPPS-based methods using the glycosylated amino acids to chemically synthesize adiponectin-like peptides are also described. In vivo studies show that the adiponectin mimicking glycopeptides exhibit significant anticancer, anti-obesity and insulin sensitizing effects. Pharmaceutical compositions of the synthetic glycopeptides and methods of use thereof in treating diseases associated with deficient adiponectin are also described.
专利号:WO-2017100796-A1 优先权日:2015-12-11 标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI 权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING 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 disgnostic and therapeutic uses.
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.
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合成参考文献
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