泼尼松杂质5置于高氯酸,Chromium(Iii) Chloride Hexahydrate,巯基乙酸,Sodium Hydroxide,锌体系中,用 甲醇,二氯甲烷,二甲基亚砜,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 4.5H,反应生成 地索奈德 参考文献: Novel Process For Preparation Of Glucocorticoid Steroids[fr] Nouveau Procédé De Préparation De Stéroïdes De Type Glucocorticoïde 标题: Novel Process For Preparation Of Glucocorticoid Steroids[fr] Nouveau Procédé De Préparation De Stéroïdes De Type Glucocorticoïde 摘要:本发明揭示了一种制备16,17-孕烷衍生物的16,17-缩醛的方法,其具有式(I)的结构,其中每个取代基独立地选择自; R1为h或ch3; R2为c1-C6直链或支链烷基,炔基或环烷基; 芳基或杂环芳基; 或r1和r2结合形成饱和的,不饱和的c3-C6环或杂环环; R3和r4相同或不同,每个独立地表示h或卤素; R5为-Oh或-ocor,其中r表示h或c1-C6直链,支链或环烷基,可能被取代.
专利号:US-12221452-B2 优先权日:2017-10-04 标题:Synthesis of cantharidin 发明人:DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R 权利人:VERRICA PHARMACEUTICALS INC 摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).
专利号:US-12391691-B2 优先权日:2018-11-16 标题:Synthesis of key intermediate of KRAS G12C inhibitor compound 发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY 权利人:AMGEN INC 摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as
专利号:US-2025206736-A1 优先权日:2019-11-14 标题 :Synthesis of kras g12c inhibitor compound 发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN 权利人:AMGEN INC 摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.
专利号:US-2024082118-A1 优先权日:2021-05-19 标 题:Topical compositions and methods of preparing the same 发明人:ABRAMOVICH SAGI; AVIDOR GAL; LANDA BENZION 权利人:LANDA LABS 2012 LTD 摘要:There is disclosed a composition comprising a water-insoluble thermoplastic compound capable of stimulating collagen synthesis (CSSC), the CSSC having a molecular weight of more than 0.6 kDa and being dispersed in a polar carrier as nano-elements having an average diameter of 200 nm or less and a viscosity of 107 mPa·s or less. The nano-elements of CSSC can be capable of stimulating the synthesis of skin proteins and/or enabling the delivery of active agents upon their application to a surface to be treated therewith. Methods for preparing the compositions and uses thereof are also provided.
专利号:WO-2022226312-A1 优先权日:2021-04-22 标 题:Combination nucleotide pool depletion for treatment of viral infections and cancers 发明人:KUMAR VIKRAM; HESSON DAVID; DEMAREST JAMES 权利人:CLEAR CREEK BIO INC 摘要:The invention provides methods of treating cancers and viral infections by providing a combination of agents that inhibit both nucleotide synthesis and nucleotide salvage in the cells of a subject to prevent cancer proliferation and viral replication. The invention provides methods of depleting nucleotide pools by using both inhibitors of dihydroorotate dehydrogenase (DHODH), such as brequinar, which block synthesis of pyrimidine-based nucleotides, in combination of one or more nucleotide salvage inhibitors, for example deoxycytidine kinase (dCK) inhibitors, Equilibrative nucleoside transporter (ENT) inhibitors, and Uridine-cytidine kinase (UCK) inhibitors, which inhibit salvage of purine and/or pyrimidine-based nucleotides or nucleosides
专利号:US-9051302-B2 优先权日:2008-01-15 标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents 发明人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN 权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG 摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.
1: Yentzer BA, Camacho FT, Young T, Fountain JM, Clark AR, Feldman SR. Good adherence and early efficacy using desonide hydrogel for atopic dermatitis: results from a program addressing patient compliance. J Drugs Dermatol. 2010 Apr;9(4):324-9. 4: Hebert AA; Desonide Foam Phase III Clinical Study Group. Desonide foam 0.05%: safety in children as young as 3 months. J Am Acad Dermatol. 2008 Aug;59(2):334-40. Review. Review. Safety and efficacy of desonide hydrogel 0.05% in pediatric subjects with atopic dermatitis. J Drugs Dermatol. 2007 Feb;6(2):175-81.
合成参考文献
参考文献:10.1007/s00216-010-3484-3 摘要:Peters RJB, Oosterink JE, Stolker AAM, Georgakopoulos C, Nielen MWF. Generic sample preparation combined with high-resolution liquid chromatography–time-of-flight mass spectrometry for unification of urine screening in doping-control laboratories. Analytical and Bioanalytical Chemistry. 2010 Feb 16;396(7):2583–98. doi: 10.1007/s00216-010-3484-3. 参考文献:10.1016/j.jpag.2011.03.005 摘要:Shackelton J, English JC. Fox-Fordyce Disease (Apocrine Miliaria). Journal of Pediatric and Adolescent Gynecology. 2011 Jun;24(3):108–9. doi: 10.1016/j.jpag.2011.03.005.