7-苄氧基-4-氯-6-甲氧基喹唑啉置于盐酸,Sodium Triacetoxyborohydride,Potassium Carbonate,溶剂黄146,三氟乙酸体系中,用 甲醇,二氯甲烷,水,N,N-二甲基甲酰胺,异丙醇 作为反应溶剂,化学反应 7.0H,反应生成 凡德他尼 参考文献:Radiosynthesis Of [11C]Vandetanib And [11C]Chloro-Vandetanib As New Potential Pet Agents For Imaging Of Vegfr In Cancer 标题:Radiosynthesis Of [11C]Vandetanib And [11C]Chloro-Vandetanib As New Potential Pet Agents For Imaging Of Vegfr In Cancer 摘要:Vandetanib (Zd6474) And Its Chlorine Analogue Chloro-Vandetanib Are Potent And Selective Vascular Endothelial Growth Factor Receptor (Vegfr) Tyrosine Kinase Inhibitors With Low Nanomolar Ic50 Values. [c-11]Vandetanib And [c-11]Chloro-Vandetanib,New Potential Pet Agents For Imaging Of Vegfr In Cancer,Were First Designed,Synthesized And Labeled At Nitrogen And Oxygen Positions From Their Corresponding N-And O-Des-Methylated Precursors,In 40-50% Decay Corrected Radiochemical Yield And 370-555 Gbq/mu Mol Specific Activity At End Of Bombardment (Eob). (C) 2011 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Bmcl.2011.04.049
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: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-11155562-B2 优先权日:2014-06-30 标 题 :Synthesis of halichondrin analogs and uses thereof 发明人:KISHI YOSHITO; UEDA ATSUSHI; YAMAMOTO AKIHIKO; KATO DAISUKE 权利人:HARVARD COLLEGE 摘要:The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting microtubule dynamics. Also provided are methods of synthesis, pharmaceutical compositions, kits, methods of treatment, and uses that involve the compounds for treatment of a proliferative disease (e.g., cancer). Compounds of the present invention are particularly useful for the treatment of metastatic breast cancer, non-small cell lung cancer, prostate cancer, and sarcoma. The included methods of synthesis are useful for the preparation of compounds of Formula (I)-(III) along with naturally occurring halicondrins (e.g., halichondrin B & C, norhalichondrin A, B, & C, and homohalichondrin A, B, & C). Also included are methods for interconverting between the halichondrins, norhalichondrins, and homohalichondrins and their unnatural epimers at the C38 ketal stereocenter through the use of an acid-mediated equilibration.
专利号:US-2025206743-A1 优先权日:2022-03-25 标 题:Tyk2 inhibitor synthesis and intermediates thereof 发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG 权利人:TAKEDA PHARMACEUTICALS CO 摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
1: Mormando M, Lauretta R, Puliani G, Bianchini M, Spoltore ME, Appetecchia M. Treatment Outcomes and Toxicities of Multiple Tyrosin Kinase Inhibitors for Metastatic Medullary Thyroid Cancer: A Case Series. Biomedicines. 2024 Dec 23;12(12):2923. doi: 10.3390/biomedicines12122923. 24(1):1569. doi: 10.1186/s12885-024-13345-9. 3: Gulwani D, Upadhyay P, Goel R, Sarangthem V, Singh TD. Nanomedicine mediated thyroid cancer diagnosis and treatment: an approach from generalized to personalized medicine. Discov Oncol. 2024 Dec 18;15(1):789. doi: 10.1007/s12672-024-01677-8. 4: Rouseti GM, Fischer A, Rathfelder N, Grimes K, Waldt A, Cuttat R, Schuierer S, Wild S, Jivkov M, Dubost V, Schadt HS, Odermatt A, Vicart A, Moretti F. Disruption of serotonin homeostasis in intestinal organoids provides insights into drug-induced gastrointestinal toxicity. Toxicology. 2024 Dec 4;511:154028. doi: 10.1016/j.tox.2024.154028. Epub ahead of print. 111(10S1):10S53-10S63. French. doi: 10.1016/S0007-4551(24)00408-9. 22(1):460. doi: 10.1186/s12964-024-01837-x.
合成参考文献
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