合成目标产物 Lenvatinib Mesylate 主要起始原料 Lenvatinib And Methanesulfonic Acid
(文献来源)合成步骤主要原料 Lenvatinib 和 Methanesulfonic Acid
4-((2,2-二甲基-4,6-二氧代-1,3-二噁烷-5-基)甲基氨基)-2-甲氧基苯甲酸甲酯置于吡啶,碳酸氢钠,Formamide,溶剂黄146,Potassium Hydroxide,Sodium T-Butanolate,三氯氧磷体系中,用 丙醇,二苯醚,二氯甲烷,水,二甲基亚砜,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 25.33H,反应生成 乐伐替尼甲磺酸盐 参考文献: Novel Polymorphs Of 4-[3-Chloro-4-(N'-Cyclopropyl Ureido)Phenoxy]-7-Methoxyquinoline-6-Carboxamide,Its Salts And Process For The Preparation Thereof[fr] Nouveaux Polymorphes De 4-[3-Chloro-4-(N'-Cyclopropyl Uréido)Phénoxy]-7-Méthoxyquinoline-6-Carboxamide,Leurs Sels Et Leur Procédé De Préparation 标题: Novel Polymorphs Of 4-[3-Chloro-4-(N'-Cyclopropyl Ureido)Phenoxy]-7-Methoxyquinoline-6-Carboxamide,Its Salts And Process For The Preparation Thereof[fr] Nouveaux Polymorphes De 4-[3-Chloro-4-(N'-Cyclopropyl Uréido)Phénoxy]-7-Méthoxyquinoline-6-Carboxamide,Leurs Sels Et Leur Procédé De Préparation 摘要:本发明涉及由以下结构式-1A所代表的4-[3-氯-4-(N'-环丙基脲基)苯氧基]-7-甲氧基喹啉-6-羧酰胺甲磺酸盐的新型多晶形态及其制备方法.此外,本发明还涉及一种改进的制备4-[3-氯-4-(N'-环丙基脲基)苯氧基]-7-甲氧基喹啉-6-羧酰胺化合物(结构式-1)或其盐及其中间体的方法.
专利号:US-2022118094-A1 优先权日:2019-02-21 标题:Synthesis of biomimetic cell wall structure 发明人:WANG YONG; SHI PENG 权利人:PENN STATE RES FOUND 摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.
专利号:US-2018140724-A1 优先权日:2015-05-27 标 题:Tumor Deliverable Iron and Protein Synthesis Inhibitors as a New Class of Drugs for the Diagnosis and Treatment of Cancer 发明人:DENG CHANGCHUN; LIPSTEIN MARK; O'CONNOR OWEN A 权利人:DENG CHANGCHUN; LIPSTEIN MARK; OCONNOR OWEN A; UNIV COLUMBIA 摘要:Tumor deliverable iron (TDI) drugs and pharmaceutical compositions and kits comprising them are provided and methods for delivering iron to tumors specifically, either intracellularly or extracellularly. As a result, TDI drugs are useful as a sensitizer for radiation therapy, radio-diagnosis, and chemotherapy, and are of interest. In other embodiments, tumor deliverable protein synthesis inhibitors (TDPSI) are provided and can be delivered to tumors, but not normal cells. These TDPSI drugs and pharmaceutical compositions and kits comprising them are useful for their treatment of cancer, either alone or in combination with other active anti-cancer drugs.
专利号:US-2023391824-A1 优先权日:2021-02-08 标题:Rationale, design, synthesis and validation of a small molecule anticancer agent 发明人:JAIN MOHIT; NARENDRAN ARUMUGAVADIVEL 权利人:NARENDRAN ARUMUGAVADIVEL 摘要:LIN28 is an RNA binding protein that binds and inhibits the expression and maturation of Iet7 microRNA that carries key tumor suppressor functions. Thus, LIN28 is a feasible and effective molecular target for directed inhibition with the potential to provide therapeutic benefit to a diverse group of aggressive malignancies. The present disclosure relates generally to the Rationale, Design, Synthesis and Validation of a Novel Small Molecule Inhibitor of LIN28, coined Compound of formula (I), for the Treatment of Adult and Pediatric Malignancies. In addition, indications of this agent to block cancer metastasis, inhibit cancer stem cells to prevent relapse, and to synergize with immunotherapy, chemotherapy and radiotherapy are also been described.
专利号:WO-2025137620-A1 优先权日:2023-12-21 标题:Methods for high quality and high accuracy methylation sequencing 发明人:KENNEDY ANDREW 权利人:GUARDANT HEALTH INC 摘要:Provided herein are methods and compositions for calibrating one or more base calling metrics in a sequencing by synthesis reaction, and for calling at least a portion of nucleobases in a converted region of a DNA molecule using the one or more calibrated base calling metrics. Provided herein are also methods for determining the likelihood that a subject has a disease or condition, such as cancer.
专利号:EP-4288444-A1 优先权日:2021-02-08 标题:Rationale, design, synthesis and validation of a small molecule anticancer agent
专利号:WO-2022165606-A1 优先权日:2021-02-08 标 题:Rationale, design, synthesis and validation of a small molecule anticancer agent
1: Tsukaguchi A, Ihara S, Yasuoka H, Minami S. Lenvatinib-refractory thymic mucinous carcinoma with PIK3CA mutation. Int Cancer Conf J. 2022 Aug 20;12(1):36-40. doi: 10.1007/s13691-022-00573-8. 2: Sano S, Asahi Y, Kamiyama T, Kakisaka T, Orimo T, Nagatsu A, Aiyama T, Kazui K, Shomura H, Ueki S, Sakamoto Y, Shirakawa C, Kamachi H, Sugino H, Mitsuhashi T, Taketomi A. Conversion surgery after lenvatinib treatment for multiple lung metastases from hepatocellular carcinoma. Int Cancer Conf J. 2022 Aug 17;12(1):7-13. doi: 10.1007/s13691-022-00567-6. 3: Furuse J, Izumi N, Motomura K, Inaba Y, Katamura Y, Kondo Y, Yabushita K, Motoyoshi K, Kudo M. Safety and Effectiveness of Lenvatinib in Patients with Unresectable Hepatocellular Carcinoma in Real-World Clinical Practice: An Observational Post-Marketing Study in Japan. Drugs Real World Outcomes. 2023 Jan 5. doi: 10.1007/s40801-022-00348-w. Epub ahead of print.
合成参考文献
参考文献:10.1124/dmd.111.043281 摘要:Inoue K, Asai N, Mizuo H, Fukuda K, Kusano K, Yoshimura T. Unique metabolic pathway of [(14)C]lenvatinib after oral administration to male cynomolgus monkey. Drug Metab Dispos. 2012 Apr;40(4):662–70. doi: 10.1124/dmd.111.043281.