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: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-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-2024239805-A1 优先权日:2022-12-16 标 题:Aza-yang cyclization-buchner aromatic ring expansion: collective synthesis of cycloheptatriene-containing azetidine lactones 发明人:SINGH MANVENDRA PAL; BOSKOVIC ZARKO; GASKINS BRYCE 权利人:UNIV KANSAS 摘要:The present disclosure is directed to a compound of Formula I, Formula II, Formula III, Formula IV, or Formula Vor a pharmaceutically acceptable salt and/or solvate thereof.
专利号:US-5171676-A 优先权日:1991-10-31 标 题 :Method of introducing hydroxyl groups into artemisinin and its derivatives 发明人:ZIFFER HERMAN; HU YULIN 权利人:US HEALTH 摘要:The fungus Beauveria sulfurescens has been employed to introduce hydroxyl groups into artemisinin and derivatives of artemisinin, an antimalarial. Hydroxylated derivatives of artemisinin and derivatives of artemisinin produced thereby possess antimalarial activity, and can serve as intermediates in the synthesis of further derivatives useful in treating malaria.
专利号:US-2024287041-A1 优先权日:2021-05-20 标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms 发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.
1: Mbaveng AT, Kuete V, Efferth T. Potential of Central, Eastern and Western Africa Medicinal Plants for Cancer Therapy: Spotlight on Resistant Cells and Molecular Targets. Front Pharmacol. 2017 Jun 2;8:343. doi: 10.3389/fphar.2017.00343. eCollection 2017. Review. 2: Samita F, Ochieng CO, Owuor PO, Manguro LO, Midiwo JO. Isolation of a new β-carboline alkaloid from aerial parts of Triclisia sacleuxii and its antibacterial and cytotoxicity effects. Nat Prod Res. 2017 Mar;31(5):529-536. doi: 10.1080/14786419.2016.1201666. Epub 2016 Jul 3. doi: 10.1177/1535370216647122. Epub 2016 May 2. 4: Kruger M, Boney R, Ordoobadi AJ, Sommers TF, Trapani JG, Coffin AB. Natural Bizbenzoquinoline Derivatives Protect Zebrafish Lateral Line Sensory Hair Cells from Aminoglycoside Toxicity. Front Cell Neurosci. 2016 Mar 30;10:83. doi: 10.3389/fncel.2016.00083. eCollection 2016.
合成参考文献
参考文献:10.1086/322986 摘要:Das A, Asatryan L, Reddy M, Wass C, Stins M, Joshi S, Bonventre J, Kim K. Differential Role of Cytosolic Phospholipase A2in the Invasion of Brain Microvascular Endothelial Cells byEscherichia coliandListeria monocytogenes. J INFECT DIS. 2001 Sep 15;184(6):732–7. doi: 10.1086/322986. 摘要:He L, Liu GQ. Interaction of multidrug resistance reversal agents with P-glycoprotein ATPase activity on blood-brain barrier. Acta Pharmacol Sin. 2002 May;23(5):423–9. 参考文献:10.1211/0022357023330 摘要:Chen WC, Hayakawa S, Yamamoto T, Huang LW, Liu IM, Cheng JT. The plasma glucose lowering action of tetrandrine in streptozotocin-induced diabetic rats. J Pharm Pharmacol. 2004 May;56(5):643–8. doi: 10.1211/0022357023330. 参考文献:10.1016/s0024-3205(01)01230-9 摘要:Zhang YH, Fang LH. Antagonism of morphine-induced antinociception by tetrandrine is dependent on serotonergic mechanisms. Life Sci. 2001 Aug 10;69(12):1429–39. doi: 10.1016/s0024-3205(01)01230-9. 摘要:Chen BA, Zhou Y, Cheng J, Dong Y, Qian XJ, Sheng M, Wang T, Gao F. [Study on the relationship between [Ca2+]i and the MDR formation in K562/A02 cells]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2004 Apr;12(2):159–62.