专利号:US-11434209-B2 优先权日:2018-08-21 标 题 :Method for synthesis of TKX-50 using insensitive intermediate 发明人:KWON KUK TAE; LEE WOONG HEE; SHIM JEONG SUB; LEE SO JUNG 权利人:AGENCY DEFENSE DEV 摘要:The present disclosure relates to a method for synthesis of TKX-50 using an insensitive intermediate, and more specifically, to a method of manufacturing TKX-50 which includes: preparing DCG as a starting material; forming a THP-DAG intermediate from the DCG; and synthesizing TKX-50 through the THP-DAG intermediate.
专利号:US-8921585-B2 优先权日:2010-08-18 标题 :Method of synthesis of substituted hexitols such as dianhydrogalactitol 发明人:BROWN DENNIS M 权利人:DEL MAR PHARMACEUTICALS 摘要:The present invention provides an efficient method of synthesizing and purifying dianhydrohexitols such as dianhydrogalactitol. In general, as applied to dianhydrogalactitol, the method comprises: (1) reacting dulcitol with a concentrated solution of hydrobromic acid at a temperature of about 80° C. to produce dibromogalactitol; (2) reacting the dibromogalactitol with potassium carbonate in t-butanol to produce dianhydrogalactitol; and (3) purifying the dianhydrogalactitol using a slurry of ethyl ether to produce purified dianhydrogalactitol. Another method produces dianhydrogalactitol from dulcitol; this method comprises: (1) reacting dulcitol with a reactant to convert the 1,6-hydroxy groups of dulcitol to an effective leaving group to generate an intermediate; and (2) reacting the intermediate with an inorganic weak base to produce dianhydrogalactitol through an intramolecular S N 2 reaction. Other methods for the synthesis of dianhydrogalactitol from dulcitol are described.
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:CA-2808629-A1 优先权日:2010-08-18 标题 :Method of synthesis of substituted hexitols such as dianhydrogalactitol
专利号:WO-2012024368-A2 优先权日:2010-08-18 标题 :Method of synthesis of substituted hexitols such as dianhydrogalactitol
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合成参考文献
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