专利号:WO-2013138200-A1 优先权日:2012-03-13 标 题 :Green chemistry synthesis of the malaria drug amodiaquine and analogs thereof 发明人:FORTUNAK JOSEPH MARIAN; KULKARNI AMOL ANANT; KING CHRISTOPHER 权利人:UNIV HOWARD 摘要:Methods are provided for a green chemistry one-pot synthesis of amodiaquine and amodiaquine analogs. The methods have a lower environmental impact, lower investment cost, reduced amounts of byproducts and impurities, and a shorter synthesis time, compared to current conventional synthesis methods. The methods reduce the total number of steps in the synthesis from four to five down to two, thereby simplifying production; and allow a reduced number of solvents and reagents to be used in production, thereby reducing the waste generated in the synthesis. The methods can reduce the waste to about 3-5 kilograms of waste generated per kilogram of product produced; and surprisingly improve the overall yield from 60-65% to greater than 90% as compared to the current conventional synthesis methods for amodiaquine and its analogs.
专利号:US-2009298868-A1 优先权日:2007-11-14 标 题:Quinoline compounds as melanogenesis modifiers and uses thereof 发明人:ORLOW SETH J; KOMATSU LI NI 权利人:ORLOW SETH J; KOMATSU LI NI 摘要:A method of identification of quinoline compounds (formula I) that modify melanin synthesis (melanogenesis), and the use of such compounds and compositions thereof to control (e.g., inhibit) melanin production are disclosed. n n n n n n n n n n The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of conditions that are causally related to aberrant melanogenesis activity including by way of non-limiting example, pigmentation deficiencies (albinism) and hyperpigmentation and others.
1: Raobela O, Andriantsoanirina V, Rajaonera DG, Rakotomanga TA, Rabearimanana S, Ralinoro F, Ménard D, Ratsimbasoa A. Efficacy of artesunate-amodiaquine in the treatment of falciparum uncomplicated malaria in Madagascar. Malar J. 2018 Aug 6;17(1):284. doi: 10.1186/s12936-018-2440-0. French. doi: 10.1371/journal.pone.0201556. eCollection 2018. Population Pharmacokinetics of the Antimalarial Amodiaquine: A Pooled Analysis to Optimize Dosing. Antimicrob Agents Chemother. 2018 Jul 23. pii: AAC.02193-17. doi: 10.1128/AAC.02193-17. [Epub ahead of print] doi: 10.1016/j.parepi.2018.02.001. eCollection 2018 May. 7: Ndiaye JA, Diallo I, NDiaye Y, Kouevidjin E, Aw I, Tairou F, Ndoye T, Halleux CM, Manga I, Dieme MN, Ndiop M, Faye B, Olliaro P, Merle CS, Gaye O, Milligan P. Evaluation of Two Strategies for Community-Based Safety Monitoring during Seasonal Malaria Chemoprevention Campaigns in Senegal, Compared with the National Spontaneous Reporting System. Pharmaceut Med. 2018;32(3):189-200. doi: 10.1007/s40290-018-0232-z. Epub 2018 Jun 1. 8: Okoth WA, Dukes E, Sullivan DJ Jr. Superior Pyronaridine Single Dose Pharmacodynamics Compared to Artesunate, Chloroquine and Amodiaquine In A Murine Malaria-Luciferase Model. Antimicrob Agents Chemother. 2018 Jul 2. pii: AAC.00394-18. doi: 10.1128/AAC.00394-18. [Epub ahead of print] doi: 10.12688/wellcomeopenres.11768.2. eCollection 2017.
合成参考文献
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