📜醋酸氟氢可的松置于potassium Carbonate体系中,化学反应生成氟氢可的松 参考文献:Halogenated Corticoids. I. 9α-Halogen Derivatives Of Cortisone And Hydrocortisone* 标题:Halogenated Corticoids. I. 9α-Halogen Derivatives Of Cortisone And Hydrocortisone* 摘要: Doi:10.1021/ja01562A030
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-2021220331-A1 优先权日:2016-05-03 标题:Inhibitors of ires-mediated protein synthesis 发明人:GERA JOSEPH F; LICHTENSTEIN ALAN; JUNG MICHAEL E; LEE JIHYE; HOLMES BRENT; BENAVIDES-SERRATO ANGELICA 权利人:UNIV CALIFORNIA; THE UNITED STATE GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS 摘要:This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.
专利号:US-10975069-B2 优先权日:2014-04-01 标 题 :Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof 发明人:HAWKINS WILLIAM; MACH ROBERT; SPITZER DIRK; VANGVERAVONG SUWANNA; VAN TINE BRIAN 权利人:UNIV WASHINGTON 摘要:Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described, such as the methanesulfonate salt of a compound of structural Formula IV, n n, wherein n is an integer chosen from 1, 2, 3, 4, and 5, and R 2 is H or methyl. At least one described molecular species exhibits an IC 50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo. It led to a 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.
专利号:US-2024067621-A1 优先权日:2021-02-23 标 题:Polyfluorinated cannabinoid and cannabinoid-like compounds and methods of synthesis and use thereof 发明人:WEAVER JIMMIE D; DAY JON; GROTJAHN SASCHA; SENAWEERA SAMEERA; KOENIG BURKHARD 权利人:WEAVER JIMMIE D; DAY JON; GROTJAHN SASCHA; SENAWEERA SAMEERA; KOENIG BURKHARD; THE BOARD OF REGENTS FOR THE OKLAHOMA AGRICULTURAL AND MECH COLLEGES 摘要:Polyfluorinated compounds are disclosed, including polyfluorinated cannabinoid and cannabinoid-like compounds. Also disclosed are methods of producing the polyfluorinated compounds.
专利号:US-8017776-B2 优先权日:2003-07-15 标题 :Methods for synthesis of acyloxyalkyl compounds 发明人:BHAT LAXMINARAYAN; GALLOP MARK A 权利人:XENOPORT INC 摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
专利号:US-2024287041-A1 优先权日:2021-05-20 标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms 发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.
1: Fleischer J, Wingenfeld K, Kuehl LK, Hinkelmann K, Roepke S, Otte C. Does fludrocortisone influence autobiographical memory retrieval? A study in patients with major depression, patients with borderline personality disorder and healthy controls. Stress. 2015 Nov;18(6):718-22. doi: 10.3109/10253890.2015.1087504. Epub 2015 Oct 12. doi: 10.5326/JAAHA-MS-6201. doi: 10.1152/ajpregu.00033.2015. Epub 2015 May 27. 4: Schultebraucks K, Wingenfeld K, Otte C, Quinkler M. The Role of Fludrocortisone in Cognition and Mood in Patients with Primary Adrenal Insufficiency (Addison's Disease). Neuroendocrinology. 2015 Jul 24. [Epub ahead of print] doi: 10.1002/bmc.3410. Epub 2015 Jan 22. doi: 10.1177/1040638715583530. Epub 2015 Apr 21. doi: 10.1016/j.nlm.2015.02.013. Epub 2015 Feb 28. doi: 10.1155/2015/286029. Epub 2015 Jul 9. 9: Bonfig W, Schwarz HP. Blood pressure, fludrocortisone dose and plasma renin activity in children with classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency followed from birth to 4 years of age. Clin Endocrinol (Oxf). 2014 Dec;81(6):871-5. doi: 10.1111/cen.12498. Epub 2014 Jun 17. doi: 10.1213/XAA.0000000000000105. doi: 10.1111/ceo.12326. Epub 2014 May 5. doi: 10.1007/s00467-014-2842-3. Epub 2014 Jun 9. Hydrocortisone and fludrocortisone for prevention of hospital-acquired pneumonia in patients with severe traumatic brain injury (Corti-TC): a double-blind, multicentre phase 3, randomised placebo-controlled trial. Lancet Respir Med. 2014 Sep;2(9):706-16. doi: 10.1016/S2213-2600(14)70144-4. Epub 2014 Jul 24. Erratum in: Lancet Respir Med. 2014 Sep;2(9):e15. doi: 10.1111/jvim.12426. doi: 10.1097/MPG.0000000000000305. doi: 10.1097/FJC.0000000000000072. doi: 10.4088/PCC.14l01676. eCollection 2014.
合成参考文献
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