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.
专利号:US-2003199558-A1 优先权日:2001-12-28 标 题:Hydroxamic acid and its derivatives as inhibitors of melanocyte tyrosinase for topical skin lighteners 发明人:DOOLEY THOMAS P; CHENG LIN 权利人:INTEGRIDERM INC 摘要:Methods, compounds, and formulations are provided to reduce pigmentation in mammalian skin, comprising hydroxamic acid and its derivatives, and especially benzohydroxamic acid and its derivatives. The compounds preferably inhibit pigment synthesis in melanocytes through inhibition of melanocyte tyrosinase. The methods can be used for lightening skin, and for treating uneven skin complexions, which result from hyperpigmentation-related medical conditions such as melasma, age spots, freckles, ochronosis, and lentigo. The compounds can be used medically or cosmetically, and preferably as topical formulations.
专利号:US-10239856-B2 优先权日:2008-01-15 标题:Synthesis of resorcylic acid lactones useful as therapeutic agents
专利号:US-2004220409-A1 优先权日:2001-02-20 标题 :Flecainide synthesis 发明人:MCDANIEL WILLIAM C; RADHAKRISHNAN JAYARAMAIYER; JANICKI SLAWOMIR J 权利人:MCDANIEL WILLIAM C; RADHAKRISHNAN JAYARAMAIYER; JANICKI SLAWOMIR J 摘要:An improved, highly efficient method for the preparation of flecainide acetate (I) or other pharmaceutically acceptable salts of flecainide. The method involves a technique for preparing the staring material 1,4-bis (2,2,2-trifuoroethoxy) benzene (III) in high yields by reacting 4-fluoro-1-bromobenzene (VI) with TFE in the presence of a base and a copper-containing catalyst.
专利号:US-12036300-B2 优先权日:2021-03-31 标题:Methods and compositions for improving skin 发明人:LIAO I-CHIEN; BRIEVA PATRICIA; JUCHAUX FRANCK; BOUEZ CHARBEL; ZHENG QIAN; QIAN KUN 权利人:OREAL 摘要:A method for managing skin tone comprising reducing the synthesis of melanin by applying a skin treatment composition to skin. The skin treatment composition may include about 0.1 to about 25 wt. % of acetyl trifluoromethylphenyl valylglycine; about 0.5 to about 30 wt. % of a polyol; about 0.1 to about 30 wt. % of a silicone, fatty compound, or a mixtures thereof, wherein the skin treatment composition is an emulsion, and all weight percentages are based on the total weight of the skin treatment composition.
专利号:US-2011217335-A1 优先权日:2008-01-15 标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents
[参考文献]: E V Curto, Et Al. Inhibitors Of Mammalian Melanocyte Tyrosinase: In Vitro Comparisons Of Alkyl Esters Of Gentisic Acid With Other Putative Inhibitors. Biochem Pharmacol. 1999 Mar 15;57(6):663-72.
合成参考文献
摘要:J. Sunkel and H. Staude, Ber. Bunsenges. Physik. Chem. 72, 567 (1968). 参考文献:10.1007/s00726-010-0488-4 摘要:Mikolasch A, Hahn V, Manda K, Pump J, Illas N, Gördes D, Lalk M, Gesell Salazar M, Hammer E, Jülich WD, Rawer S, Thurow K, Lindequist U, Schauer F. Laccase-catalyzed cross-linking of amino acids and peptides with dihydroxylated aromatic compounds. Amino Acids. 2010 Aug;39(3):671–83. doi: 10.1007/s00726-010-0488-4.