专利号:US-2009131660-A1 优先权日:2006-04-03 标 题 :SYNTHESIS OF 3-[4-(1,1-DIMETHYL-PROPYL)-PHENYL]-2-METHYL-PROPIONALDEHYDE AND cis-4--2,6-DIMETHYL-MORPHOLINE (AMOROLFINE) 发明人:BOITEAU JEAN-GUY; MUSICKI BRANISLAV 权利人:GALDERMA SA 摘要:3-[4-(1,1-Dimethyl-propyl)-phenyl]-2-methyl-propionaldehyde and cis-4-{3-[4-(1,1-dimethyl-propyl)-phenyl]-2-methyl-propyl}-2,6-dimethyl-morpholine (Amorolfine) are synthesized, first by Heck reacting a compound of general formula (VI): n n n n n n n n n n with 2-methyl-prop-2-en-1-ol of formula (VII): n n n n n n n n n n in the presence of a palladium catalyst and a base, in a solvent selected from among N,N-dimethylformamide, polar protic and non-polar organic solvents, and at a temperature ranging from 60° C. to 150° C., and then conducting an amino reduction by reacting the 3-[4-(1,1-dimethyl-propyl)-phenyl]-2-methyl-propionaldehyde of formula (II) with cis-2,6-dimethyl morpholine of formula (IV): n n n n n n n n n n in the presence of a reducing agent and in a solvent.
专利号:US-10443047-B2 优先权日:2014-05-01 标题 :Increasing cellular lipid production by increasing the activity of diacylglycerol acyltransferase and decreasing the activity of triacylglycerol lipase 发明人:TSAKRAKLIDES VASILIKI; BREVNOVA ELENA E 权利人:NOVOGY INC 摘要:Disclosed are methods and compositions for increasing the triacylglycerol content of a cell by up-regulating diacylglycerol acyltransferase and down-regulating triacylglycerol lipase. In some embodiments, a DGA1 protein is expressed and a native TGL3 gene is knocked out, thereby increasing the synthesis of triacylglycerol and decreasing its consumption, respectively.
专利号:US-2023364251-A1 优先权日:2020-08-06 标 题:Methods for the synthesis of protein-drug conjugates 发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL 权利人:CIDARA THERAPEUTICS INC 摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.
专利号:US-11858880-B2 优先权日:2017-06-16 标题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids
专利号:US-2022298103-A1 优先权日:2014-12-08 标 题 :Anti-fungals targeting the synthesis of fungal shingolipids
专利号:TW-202220698-A 优先权日:2020-08-06 标题:Methods for the synthesis of protein-drug conjugates
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合成参考文献
参考文献:10.1007/s13555-016-0093-x 摘要:Ghannoum M, Sevin K, Sarkany M. Amorolfine 5% Nail Lacquer Exhibits Potent Antifungal Activity Compared to Three Acid-Based Devices Indicated for the Treatment of Onychomycosis: An In Vitro Nail Penetration Assay. Dermatol Ther (Heidelb). 2016 Feb 01;6(1):69–75. doi: 10.1007/s13555-016-0093-x. 参考文献:10.1007/s13555-018-0254-1 摘要:Eertmans F, Doss N, Rossel B, Adriaens E. Daily Application of an Aqueous, Acidifying, Peelable Nail Polish versus Weekly Amorolfine for Topical Onychomycosis Treatment: A Prospective, Randomized, Blinded Trial. Dermatol Ther (Heidelb). 2018 Jul 26;8(3):463–73. doi: 10.1007/s13555-018-0254-1.