专利号:US-7241900-B2 优先权日:2002-02-12 标题 :Synthesis of indole thiazole compounds as ligands for the Ah receptor 发明人:DELUCA HECTOR F; GRZYWACZ PAWEL K; SICINSKI RAFAL R 权利人:WISCONSIN ALUMNI RES FOUND 摘要:A method of synthesizing aromatic ketone compositions of formula I comprising the step of introducing a double bond into the 5 membered ring of the 4,5-dihydro-1,3-azoles moiety of formula II is disclosed. A method of synthesizing aromatic ketone compositions of formula I comprising the step of ring synthesis of the tetrahydro-1,3-azoles of formula XI is also disclosed.
专利号:US-7645788-B2 优先权日:2001-06-06 标题 :Tetramerous derivative of indole-3-carbinol with anti-carcinogenic activity and method of synthesis of said derivative 发明人:MAGNANI MAURO; FIORUCCI CHIARA; FILIPPONE PAOLINO; BRANDI GIORGIO; PAIARDINI MIRKO 权利人:UNIV DEGLI STUDI URBINO 摘要:Use of the tetramerous derivative of indole-3-carbinol having formula I n nfor preparing a medicinal having anti-carcinogenic activity, and method of synthesis of the tetramerous derivative having formula I, in which indole-3-carbinol is reacted with an oxidizing agent so as to cause a polymeric oxidation of indole-3-carbinol.
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-7056348-B2 优先权日:2001-04-19 标题:5-aryl-1,3,3-trimethyl-2-methylene-indoline derivatives and salts thereof, methods for the production and use of said compounds for the temporary coloration of fibers 发明人:SAUTER GUIDO; BRAUN HANS-JUERGEN; REICHLIN NADIA 权利人:WELLA AG 摘要:A method for the synthesis of 5-aryl-1,3,3,-trimethyl-2-methylene-indoline derivatives of Formula (I) or its salts of Formula (Ia) wherein 1 mole of a 5-aryl-2,3,3-trimethyl-3H-indole derivative of Formula (VII) is reacted for 1 to 44 hours at a temperature of 20° to 180° C. in an apolar, aprotic or polar, protic or polar aprotic solvent with 1 to 50 moles of a compound of Formula R1-A; new compounds of Formulas (I)/(Ia) and (V), obtainable by this method as well as an agent containing at least one compound of Formula (I)/(Ia) and a carbonyl/imine compound for dyeing keratinic fibers and a method for temporarily dyeing keratin fibers, for which the keratin fiber is dyed with the aforementioned agent and the dyeing, so obtained, is removed again at any later time by a sulfite preparation.
专利号:US-8399502-B2 优先权日:2008-09-17 标 题 :Analogs of indole-3-carbinol and their use as agents against infection 发明人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN 权利人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN; STANFORD RES INST INT 摘要:Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.
1: Li B, Cong M, Zhu Y, Xiong Y, Jin W, Wan Y, Zhou Y, Ao Y, Wang H. Indole-3-Carbinol Induces Apoptosis of Hepatic Stellate Cells through K63 De-Ubiquitination of RIP1 in Rats. Cell Physiol Biochem. 2017;41(4):1481-1490. doi: 10.1159/000470650. Epub 2017 Mar 24. doi: 10.1002/prp2.299. eCollection 2017 Apr. 3: Zamaratskaia G, Thøgersen R, Čandek-Potokar M, Rasmussen MK. Co-treatment with indole-3-carbinol and resveratrol modify porcine CYP1A and CYP3A activities and expression. Xenobiotica. 2017 Mar 19:1-9. doi: 10.1080/00498254.2017.1300708. [Epub ahead of print] doi: 10.1017/S0954422417000026. Epub 2017 Mar 15. doi: 10.1016/j.msec.2016.12.006. Epub 2016 Dec 14. doi: 10.1016/j.bcp.2016.12.007. Epub 2016 Dec 12. doi: 10.15252/msb.20167311.
合成参考文献
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