专利号:US-9295731-B2 优先权日:2013-04-01 标题 :Cleavable drug conjugates, compositions thereof and methods of use 发明人:NGUYEN MARK QUANG 权利人:NGUYEN MARK QUANG 摘要:Base-labile crosslinkers, base-labile conjugates comprising such crosslinkers, methods of their synthesis and use are disclosed.
专利号:WO-2013078523-A1 优先权日:2011-11-29 标题:Heterocyclic n-glycinyl-n-acyl hydrazone compounds, synthesis method, pharmaceutical compositions and treatment method 发明人:MANSSOUR FRAGA CARLOS ALBERTO; DE LACERDA BARREIRO ELIEZER DE JESUS; BARBOSA LACERDA RENATA; PALHARES DE MIRANDA ANA LUISA; LOUBACK DA SILVA LEANDRO; FREITAS DE LIMA CLEVERTON KLEITON 权利人:UNIV RIO DE JANEIRO 摘要:New heterocyclic derivatives are described, having the N-glycinyl-N-acyl hydrazone subunit and acting as analgesic and anti-inflammatory agents with in vitro e in vivo inhibiting activity on pro-inflammatory TNF-α cytokine, and useful therefore for the treatment of pain and acute and chronic inflammation, including: relieving hyperalgesia associated with acute and chronic inflammation in mammals, preferably humans. Also described are pharmaceutical compositions containing these compounds and methods for preparing the same.
专利号:CN-110950848-B 优先权日:2018-09-27 标题 :Synthesis and Application of New Aminopyrazole Derivatives
1: Yang S, Beerahee M. Losmapimod concentration-QT relationship in healthy volunteers: meta-analysis of data from six clinical trials. Eur J Clin Pharmacol. 2013 Jun;69(6):1261-7. doi: 10.1007/s00228-012-1469-1. Epub 2013 Jan 17. doi: 10.1007/s40262-012-0025-6. doi: 10.1055/s-0032-1327368. Epub 2012 Dec 18. Review. German. doi: 10.1002/j.1532-2149.2012.00256.x. Epub 2012 Dec 14. doi: 10.1111/bcp.12063. 6: Melloni C, Sprecher DL, Sarov-Blat L, Patel MR, Heitner JF, Hamm CW, Aylward P, Tanguay JF, DeWinter RJ, Marber MS, Lerman A, Hasselblad V, Granger CB, Newby LK. The study of LoSmapimod treatment on inflammation and InfarCtSizE (SOLSTICE): design and rationale. Am Heart J. 2012 Nov;164(5):646-653.e3. doi: 10.1016/j.ahj.2012.07.030. Epub 2012 Oct 16. doi: 10.1016/j.jcmg.2012.02.016. An oral inhibitor of p38 MAP kinase reduces plasma fibrinogen in patients with chronic obstructive pulmonary disease. J Clin Pharmacol. 2012 Mar;52(3):416-24. doi: 10.1177/0091270010397050. Epub 2011 Nov 16. doi: 10.1161/CIRCULATIONAHA.110.971986. Epub 2011 Jan 24. doi: 10.1124/jpet.109.154443. Epub 2009 Jun 25.
合成参考文献
参考文献:10.1007/s40262-012-0025-6 摘要:Yang S, Lukey P, Beerahee M, Hoke F. Population pharmacokinetics of losmapimod in healthy subjects and patients with rheumatoid arthritis and chronic obstructive pulmonary diseases. Clin Pharmacokinet. 2013 Mar;52(3):187–98. doi: 10.1007/s40262-012-0025-6.