CAS: 356057-34-6; N-(2-(Diethylamino)Ethyl)-2-(2-((4-Fluorobenzyl)Thio)-4-Oxo-4,5,6,7-Tetrahydro-1H-Cyclopenta[d]Pyrimidin-1-yl)-N-((4'-(Trifluoromethyl)-[1,1'-Biphenyl]-4-yl)Methyl)Acetamide

该化合物是一种小分子抑制剂,主要设计针对与脂质蛋白有关的磷脂A2(Lp-PLA2),一种与麻风病和心血管疾病有关的酶,其化学结构具有独特的功能组合,有助于其生物活动.Darapaldib的特点是能够减少动脉壁中的炎症和成块,使它成为心血管病条件下治疗干预的候选体.该物质一般是口服的,并经过各种临床试验,以评估其功效和安全特征.其药用动力学显示中度半衰期,允许在某些研究中每天一次使用.临床结果虽然很有希望,但已经显示出混合的结果,有助于更好地了解其在心血管治疗中的作用.与许多药物一样,其使用的潜在副作用和与其他药物的相互作用是重要的考虑因素.

结构式图片

欧盟法规

C&L通报

上下游产品

N,N-diethyl-N'-(4'-trifluoromethylbiphenyl-4-ylmethyl)ethane-1,2-diamine {2-[(4-fluorobenzyl)sulfanyl]-4-oxo-4,5,6,7-tetrahydro-1H-cyclopenta[d]pyrimidin-1-yl}acetic acid 2-ethoxycarbonyl-1-cyclopentanone 2-mercapto-1,5,6,7-tetrahydro-cyclopentapyrimidin-4-one

合成工艺路线路线简述

    📜2-(2-((4-氟苄基)硫基)-4-氧代-4,5,6,7-四氢-1H-环戊二烯并[d]嘧啶-1置于n,N'-羰基二咪唑体系中,用 异丁基甲基醚 作为反应溶剂,化学反应生成 达普拉缔
    参考文献: Novel Processes[fr] Nouveaux Procédés
    标题: Novel Processes[fr] Nouveaux Procédés
    摘要:本发明涉及制备化合物(i)的方法以及用于制备该化合物的中间体.化合物(i)对治疗心血管和炎症性疾病如动脉粥样硬化具有益处.

    海关参考信息

    专利信息


    专利号:US-10005720-B2
    优先权日:2013-04-05
    标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
    发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
    权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
    摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

    专利号:US-11485721-B2
    优先权日:2017-11-21
    标 题:Method for the metal-free preparation of a biaryl by a photosplicing reaction and their uses
    发明人:KLOSS FLORIAN; NEUWIRTH TONI; HAENSCH VEIT; HERTWECK CHRISTIAN
    权利人:LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST HKI; LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST
    摘要:The present invention relates to a method for the metal-free preparation of a biaryl compound by a photosplicing reaction and its use in the preparation of chemical compounds, preferably of active ingredients e.g. in the fields of pharmaceuticals and agrochemicals. In particular, it refers to a method for the regiocontrolled preparation of a biaryl compound of formula (I): Ar—Ar′ by photochemically reacting a precursor compound of formula (II): Ar—L—Ar′ to form a biaryl compound of general formula: Ar—L—Ar′(II)→Ar—Ar′ (I) wherein Ar and Ar′, independently of each other, represent an unsubstituted or substituted C6-C20 aryl group or a heteroaryl group with 5-20 ring atoms selected from carbon, nitrogen, oxygen and sulfur, and L represents a group —X—Y—Z— as defined herein. The biaryl compounds are generally suitable as intermediates or key building blocks in a very broad spectrum of organic chemical syntheses and their respective utilities. Their use within the field of synthesis of active ingredients is an aspect of the invention, and their use in the preparation of pharmaceutically active ingredients is particularly preferred.

    专利号:US-2018370905-A1
    优先权日:2013-04-05
    标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same

    专利号:US-10906888-B2
    优先权日:2016-07-14
    标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
    发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE
    权利人:PFIZER
    摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:US-10308615-B2
    优先权日:2015-05-29
    标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme
    发明人:CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN
    权利人:PFIZER
    摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:US-2016046560-A1
    优先权日:2013-04-05
    标题 :Compounds useful for the treatment of metabolic disorders and synthesis of the same

    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: Hu C, Tompson D, Magee M, Chen Q, Liu YM, Zhu W, Zhao H, Gross AS, Liu Y. Single and Multiple Dose Pharmacokinetics, Pharmacodynamics and Safety of the Novel Lipoprotein-Associated Phospholipase A2 Enzyme Inhibitor Darapladib in Healthy Chinese Subjects: An Open Label Phase-1 Clinical Trial. PLoS One. 2015 Oct 14;10(10):e0139862. doi: 10.1371/journal.pone.0139862. eCollection 2015.
    2: He Magee M, Shaddinger B, Collins D, Siddiqi S, Soffer J. The pharmacokinetics and safety of darapladib in subjects with severe renal impairment. Br J Clin Pharmacol. 2015 Oct;80(4):654-61. doi: 10.1111/bcp.12661. Epub 2015 Jul 6.
    3: Staurenghi G, Ye L, Magee MH, Danis RP, Wurzelmann J, Adamson P, McLaughlin MM; Darapladib DME Study Group. Darapladib, a lipoprotein-associated phospholipase A2 inhibitor, in diabetic macular edema: a 3-month placebo-controlled study. Ophthalmology. 2015 May;122(5):990-6. doi: 10.1016/j.ophtha.2014.12.014. Epub 2015 Mar 5. doi: 10.1586/14779072.2015.986466. Review. doi: 10.1038/nrcardio.2014.148. Epub 2014 Sep 16. Effect of darapladib on major coronary events after an acute coronary syndrome: the SOLID-TIMI 52 randomized clinical trial. JAMA. 2014 Sep 10;312(10):1006-15. doi: 10.1001/jama.2014.11061. Erratum in: JAMA. 2014 Oct 8;312(14):1473. Dylan P. Steen[corrected to Dylan L. Steen]. doi: 10.1038/nrd4381. doi: 10.1111/bcp.12436.

    合成参考文献


    参考文献:10.1007/s11883-011-0190-3
    摘要:Mangalmurti SS, Davidson MH. The incremental value of lipids and inflammatory biomarkers in determining residual cardiovascular risk. Curr Atheroscler Rep. 2011 Oct;13(5):373–80. doi: 10.1007/s11883-011-0190-3.
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