阿法替尼,顺丁烯二酸置于乙醇体系中,用 乙醇 作为反应溶剂,化学反应 5.0H,反应生成 双马来酸盐阿法替尼 参考文献:Process For Preparing Amino Crotonyl Compounds 标题:Process For Preparing Amino Crotonyl Compounds 摘要:一种改进的制备4-[(3-氯-4-氟苯基)氨基]-6-{[4-(N,N-二甲基氨基)-1-氧代-2-丁烯-1-基]氨基}-7-((S)-四氢呋喃-3-氧基)-喹唑啉及相关氨基丙烯酰化合物的方法,以及制备适用于作为药物活性物质的4-[(3-氯-4-氟苯基)氨基]-6-{[4-(N,N-二甲基氨基)-1-氧代-2-丁烯-1-基]氨基}-7-((S)-四氢呋喃-3-氧基)-喹唑啉的适当盐.
专利信息
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-2018371021-A1 优先权日:2017-05-11 标 题 :Peptidomimetic macrocycles and uses thereof 发明人:AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN 权利人:AILERON THERAPEUTICS INC 摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.
专利号:US-12180228-B2 优先权日:2019-06-05 标题:Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof 发明人:MOVASSAGHI MOHAMMAD; OLSSON CHASE ROBERT; SCOTT TONY Z; CHEAH JAIME; PAYETTE JOSHUA NATHANIEL 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.
专利号:US-2024262829-A1 优先权日:2021-04-21 标 题:Peptide nucleic acids, synthesis, and uses thereof 发明人:ROTHMAN JEFFREY 权利人:ONCOGENUITY INC 摘要:The present disclosure provides peptide nucleic acids (PNAs) including cyclic structural moieties such as tetrahydrofuran, pyrrolidinium, pyrrolidine, or N-methyl pyrrolidine, which have surprisingly improved the water solubility and binding affinity of PNA oligomers to ribose-phosphate nucleic acid oligomers. Pharmaceutical compositions including the disclosed PNAs, synthetic methods thereof, and methods of use thereof are also disclosed.
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.
1: Prim N, Fore M, Mennecier B. [Afatinib (BIBW 2992).]. Rev Pneumol Clin. 2014 May 27. pii: S0761-8417(14)00047-9. doi: 10.1016/j.pneumo.2014.03.002. [Epub ahead of print] Review. French. doi: 10.2147/BTT.S40567. eCollection 2014. Review. 3: Bowles DW, Weickhardt A, Jimeno A. Afatinib for the treatment of patients with EGFR-positive non-small cell lung cancer. Drugs Today (Barc). 2013 Sep;49(9):523-35. doi: 10.1358/dot.2013.49.9.2016610. Review. doi: 10.1159/000354627. Epub 2013 Aug 19. Review. doi: 10.1517/17425255.2013.832755. Epub 2013 Aug 28. Review. doi: 10.1007/s40265-013-0111-6. Review. doi: 10.1016/j.lungcan.2013.02.021. Epub 2013 May 10. Review. doi: 10.1586/era.13.31. Epub 2013 Mar 18. Review. doi: 10.1586/era.13.30. Epub 2013 Mar 18. Review. doi: 10.2147/BCTT.S25868. Review.
合成参考文献
参考文献:10.1186/s13045-018-0651-z 摘要:Liu Z, Chen Z, Wang J, Zhang M, Li Z, Wang S, Dong B, Zhang C, Gao J, Shen L. Mouse avatar models of esophageal squamous cell carcinoma proved the potential for EGFR-TKI afatinib and uncovered Src family kinases involved in acquired resistance. Journal of Hematology & Oncology. 2018 Aug 29;11(1):109. doi: 10.1186/s13045-018-0651-z.