CAS: 585543-15-3; 6-(5-(Cyclopropylcarbamoyl)-3-Fluoro-2-Methylphenyl)-N-Neopentylnicotinamide

该化合物是选择性的p38 分子活性蛋白质动脉抑制器,主要调查其在炎症和变性疾病中的潜在治疗用途,其行动机制包括调节p38α和p38β等异形,在细胞皮质生产和细胞应激反应方面起着关键作用.临床和临床研究表明,Losmapimod在选择与慢性炎相关的路径方面可能具有优势,如...

结构式图片

欧盟法规

ECHA物质C&L通报

合成工艺路线路线简述

    📜3-氟-4-甲基-5-碘苯甲酸置于(1,1'-Bis(Diphenylphosphino)Ferrocene)Palladium(II) Dichloride,四(三苯基膦)钯,氯化亚砜,Potassium Acetate,碳酸氢钠,Sodium Carbonate体系中,用 二氯甲烷,N,N-二甲基甲酰胺,异丙醇 作为反应溶剂,化学反应 29.0H,反应生成 罗斯匹莫
    参考文献:Ep3357916
    标题:Ep3357916

    海关参考信息

    专利信息


    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

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    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.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知