amifostine monohydratedibromohydrate du N-(bromoethyl-2)diamino-1,3 propane
合成工艺路线路线简述
氨磷汀置于water Ethanol,乙醇,氮体系中,用 水 用作溶剂,化学反应 5.0H,反应生成氨磷汀三水合物 参考文献:Process For The Preparation Of (Aminoalkylamino)Alkyl Halides And Conversion To Amifostine 标题:Process For The Preparation Of (Aminoalkylamino)Alkyl Halides And Conversion To Amifostine 摘要:本发明涉及制备(ω-氨基烷基氨基)烷基卤化物的过程,将其转化为s-ω-(ω-氨基烷基氨基)烷基磷酰硫酸酯,并纯化反应的结晶产物.制备(ω-氨基烷基氨基)烷基卤化物的过程包括在磺醇溶剂的存在下,在适宜的温度和压力条件下,将适当的醇与溴化剂接触以形成盐,而不会出现过早沉淀.该过程特别适用于将(ω-氨基烷基氨基)乙醇转化为阿米福汀.
专利号:US-2015158809-A9 优先权日:2013-02-26 标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds 发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P 权利人:XENOPORT INC 摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.
专利号:US-2007098676-A1 优先权日:2005-08-10 标 题 :Functionally diverse macromolecules and their synthesis 发明人:SIMANEK ERIC E; HOLLINK EMILY 权利人:SIMANEK ERIC E; HOLLINK EMILY 摘要:Functionally diverse macromolecules and synthetic routes for obtaining the same are disclosed. In certain embodiments, the synthesis proceeds in a divergent manner. In other embodiments, the routes rely on the differential reactivity of monomeric electrophilic triazine building blocks that display protected or unprotected groups. This diversity permits the facile introduction of a variety of diversity groups at multiple positions of these macromolecules, thereby setting the stage for further generational growth of the macromolecule and/or incorporation of other diversity groups such as biocompatible targeting groups.
专利号:US-2007041933-A1 优先权日:2005-08-10 标题:Functionally Diverse Macromolecules and Their Synthesis 发明人:SIMANEK ERIC E; HOLLINK EMILY 权利人:SIMANEK ERIC E; HOLLINK EMILY 摘要:Functionally diverse macromolecules and synthetic routes for obtaining the same are disclosed. In certain embodiments, the synthesis proceeds in a divergent manner. In other embodiments, the routes rely on the differential reactivity of monomeric electrophilic triazine building blocks that display protected or unprotected groups. This diversity permits the facile introduction of a variety of diversity groups at multiple positions of these macromolecules, thereby setting the stage for further generational growth of the macromolecule and/or incorporation of other diversity groups such as biocompatible targeting groups.
专利号:US-2022118123-A1 优先权日:2019-02-22 标 题 :Combination of ar antagonists and targeted thorium conjugates 发明人:HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY 权利人:BAYER AG; BAYER AS 摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.
专利号:US-2024382626-A1 优先权日:2023-05-16 标题 :Irradiation amenable liposomal dye aggregates and methods of synthesis and use thereof 发明人:PORTER TYRONE; STERN NOAH; TUNNELL JAMES; SHRESTHA BINITA 权利人:UNIV TEXAS 摘要:The present invention provides lipid nanoparticles that are amenable to an irradiation at a wavelength at or above 850 nm, have an absorption peak from about 850 to 1100 nm wavelength, and comprise a high transition temperature lipid and a dye (e.g., a J-aggregate of a dye). In some embodiments, the dye (e.g., J-aggregate of the dye) is encapsulated in the lipid nanoparticle. In various embodiments, the present invention also relates to compositions comprising said lipid nanoparticles and methods of generating said lipid nanoparticles and compositions thereof. The present invention further relates to methods relating to the said lipid nanoparticles for imaging, detection, and treatment of diseases or disorders (e.g., phototherapy) in a subject.
专利号:US-2008281105-A1 优先权日:2005-01-18 标题:Novel Quinolinium Salts and Derivatives 发明人:MACDONALD JAMES E; HYSELL MICHELLE K; YU DEHUA; LI HENRY; WONG-STAAL FLOSSIE 权利人:IMMUSOL INC 摘要:The present invention relates generally to the synthesis of novel quinolinium salts and derivative compounds. Such salts and compounds are useful for inhibiting the growth of cancer cells.
1: Rasey JS. Amifostine. Cancer Biother Radiopharm. 1999 Oct;14(5):331-5. doi: 10.1089/cbr.1999.14.331. 98(2):61-80. doi: 10.1159/000502979. Epub 2019 Dec 17. 23(9):3209-3213. doi: 10.31557/APJCP.2022.23.9.3209. 4: Duval M, Daniel SJ. Meta-analysis of the efficacy of amifostine in the prevention of cisplatin ototoxicity. J Otolaryngol Head Neck Surg. 2012 Oct;41(5):309-15. Mucositis Study Group of the Multinational Association of Supportive Care in Cancer/International Society of Oral Oncology (MASCC/ISOO). Systematic review of amifostine for the management of oral mucositis in cancer patients. Support Care Cancer. 2013 Jan;21(1):357-64. doi: 10.1007/s00520-012-1613-6. Epub 2012 Oct 3. 18(11):1077-1090. doi: 10.1080/14740338.2019.1666104. Epub 2019 Sep 17. 30(6 Suppl 18):18-30. doi: 10.1053/j.seminoncol.2003.11.014. 23(4 Suppl 8):18-22. 12(6):738-47. doi: 10.1634/theoncologist.12-6-738. 112:87-100. doi: 10.1016/j.actbio.2020.05.025. Epub 2020 May 23. Erratum in: Acta Biomater. 2022 Nov;153:630-631. 54(7):787-800. doi: 10.1093/ajhp/54.7.787. 2(3):479-89. doi: 10.1517/14656566.2.3.479. 32A Suppl
合成参考文献
参考文献:10.1007/s11010-024-05030-z 摘要:Zhao Z, He D, Wang J, Xiao Y, Gong L, Tang C, Peng H, Qiu X, Liu R, Zhang T, Li J. Swertiamarin relieves radiation-induced intestinal injury by limiting DNA damage. Mol Cell Biochem. 2025 Apr;480(4):2277–90. doi: 10.1007/s11010-024-05030-z.