3β-Acetoxy-17-Hexanoyloxy-Pregn-5-En-20-One置于盐酸,环己酮,Aluminum Isopropoxide体系中,化学反应生成 己酸孕酮 参考文献:Esters Of 17Alpha-Hydroxyprogesterone 标题:Esters Of 17Alpha-Hydroxyprogesterone
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-8461298-B2 优先权日:2004-11-01 标 题:Compositions and methods for modification of biomolecules 发明人:BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL 权利人:BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL; UNIV CALIFORNIA 摘要:The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
专利号:US-8569265-B2 优先权日:2011-05-06 标题:Deuterated analogs of (4S)-4-ethyl-4-hydroxy-11-[2- (trimethylsilyl)ethyl]-1H-pyrano[3′, 4′:6,7] indolizino [1,2-b]quinoline-3,14(4H, 12H)-dione and methods of use thereof 发明人:CHEN XINGHAI; HUANG QIULI; KOCHAT HARRY; MALAKHOV ANDREY; HAUSHEER FREDERICK H 权利人:CHEN XINGHAI; HUANG QIULI; KOCHAT HARRY; MALAKHOV ANDREY; HAUSHEER FREDERICK H; BIONUMERIK PHARMACEUTICALS INC 摘要:The present invention discloses: (i) two novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (ii) methods of synthesis of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (iii) pharmaceutically-acceptable formulations comprising said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents; and (iv) methods of administration of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof.
专利号:WO-9318775-A1 优先权日:1992-03-19 标 题:Method and composition for suppression of side effects of anti-inflammatory drugs 发明人:BURTON ALBERT F; FREEMAN HUGH J; MCGEER PATRICK L 权利人:UNIV BRITISH COLUMBIA 摘要:This invention pertains to the novel use of N-acetyl glucosamine to overcome or minimize the side-effects of anti-inflammatory agents by providing for the synthesis of essential human tissue components whose formation is inhibited by the action of these drugs. A method of minimizing adverse side effects in a human being who is being treated with anti-inflammatory agents comprising feeding the human being a therapeutic amount of N-acetyl glucosamine, and pharmaceutically acceptable carriers, on a periodic basis.
专利号:US-2025289827-A1 优先权日:2022-12-02 标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof 发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN 权利人:C4 THERAPEUTICS INC 摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.
专利号:US-2023382819-A1 优先权日:2020-10-14 标 题:Processes for synthesis of alpha-emitting radiopharmaceuticals 发明人:MORSE DAVID L; WADAS THADDEUS J; PANDYA DARPAN; TAFRESHI NARGES; BUDZEVICH MIKALAI 权利人:H LEE MOFFITT CANCER CT & RES; UNIV IOWA RES FOUND 摘要:The present disclosure provides processes for the preparation of alpha emitting radiopharmaceutical compositions, in particular DOTATATE complexes of alpha emitting radionuclides, as well as use of such prepared compositions in the treatment of cancers.
1: Mainiero AD, Rouse DJ, Lopes V, Hughes BL. Association of 17α-Hydroxyprogesterone Caproate and Risk of Infection. Obstet Gynecol. 2015 Jul;126(1):103-8. doi: 10.1097/AOG.0000000000000881. doi: 10.2146/ajhp130466. Relationship between 17-alpha hydroxyprogesterone caproate concentration and spontaneous preterm birth. Am J Obstet Gynecol. 2014 Feb;210(2):128.e1-6. doi: 10.1016/j.ajog.2013.10.008. Epub 2013 Oct 7. 4: Manuck TA, Esplin MS, Biggio J, Bukowski R, Parry S, Zhang H, Huang H, Varner MW, Andrews W, Saade G, Sadovsky Y, Reddy UM, Ilekis J; Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) Genomics and Proteomics Network for Preterm Birth Research (GPN-PBR). Predictors of response to 17-alpha hydroxyprogesterone caproate for prevention of recurrent spontaneous preterm birth. Am J Obstet Gynecol. 2016 Mar;214(3):376.e1-8. doi: 10.1016/j.ajog.2015.12.010. Epub 2015 Dec 12. 5: Stringer EM, Vladutiu CJ, Batra P, Stringer JS, Menard MK. Operationalizing 17α-Hydroxyprogesterone Caproate to Prevent Recurrent Preterm Birth: Definitions, Barriers, and Next Steps. Obstet Gynecol. 2016 Dec;128(6):1397-1402. doi: 10.1016/j.ajog.2015.10.934. Epub 2015 Nov 10. Review. e1-105.e12. doi: 10.1016/j.ajog.2016.01.180. Epub 2016 Jan 29. e1-622.e8. doi: 10.1016/j.ajog.2016.07.013. Epub 2016 Jul 11.
合成参考文献
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