CAS: 960539-70-2; Daprodustat

该化合物是一种小分子药物,主要用于治疗与慢性肾病有关的贫血症(CKD),它作为一种低缺氧,低能导出因素,通过模仿生理反应对低氧水平的模拟,增强红血杆菌.这个机制刺激了红血球的产物,一种激素,一种激素,一种促进红细胞形成激素的激素.Daprodustat的特点是它能够增加血红球素水平,而不需要传统的红血球素刺激剂,有可能提供一种更安全的替代品,降低高血压和心血管事件的风险.该化合物通过口服管理,并在临床试验中评估其功效和安全性.它的药理学学涉及吸收,代谢和排泄,这些受包括肾功能在内的各种因素的影响.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

1,3-二环己基巴比妥酸 1,3-Dicyclohexyl Barbituric Acid 35824-91-0

合成工艺路线路线简述

  • 960540-96-9 = 960539-70-2
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Ethanol,Water; Rt; 3 H,Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified,Rt
    标题:Preparation Of N-Substituted Pyrimidine-Trione Amino Acid Derivatives As Prolyl Hydroxylase Inhibitors
    参考文献:World Intellectual Property Organization]

    35824-91-0 + 2949-22-6 = 960539-70-2
    反应条件:1.1 Reagents: Triethylamine Solvents: Anisole; 90 Min,70 °C
    标题:Method For Preparing And Purifying An Agent Suitable For Treating Anemia
    参考文献:World Intellectual Property Organization]

    35824-91-0 + 2949-22-6 = 960539-70-2
    反应条件:1.1 Reagents: Diisopropylethylamine Solvents: Dichloromethane; Overnight,Rt1.2 Reagents: Hydrochloric Acid Solvents: Water1.3 Reagents: Sodium Hydroxide Solvents: Ethanol,Water; 3 H,Rt
    标题:Preparation Of Substituted Pyrimidinetrione Compounds Useful For The Treatment Of Human Anemia
    参考文献:China]

    = 960539-70-2 [标题:Reaction Conditions
    标题:Novel Manufacturing Method Of Daprodustat And Precursors Thereof
    参考文献:World Intellectual Property Organization
N,N-二环己脲置于乙醇,N,N-二异丙基乙胺,Sodium Hydroxide体系中,用 二氯甲烷,氯仿 作为反应溶剂,化学反应 7.5H,反应生成 N-[(1,3-二环己基六氢-2,4,6-三氧代-5-嘧啶基)羰基]甘氨酸
参考文献:一种取代的嘧啶三酮化合物及包含该化合物 的组合物及其用途
标题:一种取代的嘧啶三酮化合物及包含该化合物 的组合物及其用途
摘要:本发明提供了一种取代的嘧啶三酮化合物及包含该化合物的组合物及其用途,本发明公开了如式(I)所示的嘧啶三酮化合物,或其晶型,药学上可接受的盐,前药,立体异构体,水合物或溶剂化合物.本发明所述的嘧啶三酮化合物及包含该化合物的组合物可用于调节缺氧诱导因子(Hif)和/或内源性促红细胞反应生成素(Epo),可用于制备调控人体贫血的药物.

海关参考信息

专利信息


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-2024208898-A1
优先权日:2021-03-25
标 题 :Enamine n-oxides: synthesis and application to hypoxia-responsive prodrugs and imaging agents
发明人:KIM JUSTIN; KANG DAHYE; CHEUNG SHELDON T
权利人:DANA FARBER CANCER INST INC
摘要:Disclosed are compounds and pharmaceutically acceptable salts and stereoisomers thereof that are suitable for diagnosis and the treatment of diseases and disorders characterized by, associate with or which exhibit tissue hypoxia, such as, for example, solid tumors. Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds.

专利号:US-2018230127-A1
优先权日:2015-08-13
标题 :Bicyclic-Fused Heteroaryl Or Aryl Compounds
发明人:ANDERSON DAVID RANDOLPH; CURRAN KEVIN JOSEPH; GAVRIN LORI KRIM; GOLDBERG JOEL ADAM; LEE ARTHUR; LOWE MICHAEL DENNIS; PATNY AKSHAY; PIERCE BETSY SUSAN; SAIAH EDDINE; TRZUPEK JOHN DAVID
权利人:PFIZER
摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds of Formula (Ia) are disclosed which are inhibitors of Interleukin-1 receptor associated kinase (IRAK4). Methods of treatment, methods of synthesis, and intermediates are also disclosed as defined in the specification.

专利号:US-10316018-B2
优先权日:2015-08-27
标题 :Bicyclic-fused heteroaryl or aryl compounds as IRAK4 modulators
发明人:LEE KATHERINE LIN; ALLAIS CHRISTOPHE PHILIPPE; DEHNHARDT CHRISTOPH MARTIN; GAVRIN LORI KRIM; HAN SEUNGIL; HEPWORTH DAVID; LEE ARTHUR; LOVERING FRANK ELDRIDGE; MATHIAS JOHN PAUL; OWEN DAFYDD RHYS; PAPAIOANNOU NIKOLAOS; SAIAH EDDINE; STROHBACH JOSEPH WALTER; TRZUPEK JOHN DAVID; WRIGHT STEPHEN WAYNE; ZAPF CHRISTOPH WOLFGANG
权利人:PFIZER
摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:JP-2024512568-A
优先权日:2021-03-25
标 题:Enamine N-oxide: synthesis and application of hypoxia-responsive prodrugs and contrast agents
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主要参考文献


1: Mishra HP, Gupta R, Grover S, Gupta LK. Daprodustat vs Recombinant Human Erythropoietin for Anemia and Cardiovascular Safety in Dialysis-Dependent and Non-Dialysis-Dependent CKD Patients - A Systematic Review and Meta-analysis. Curr Rev Clin Exp Pharmacol. 2026 Jan 7. doi: 10.2174/0127724328377421251117050736. Epub ahead of print. 119(2):322-335. doi: 10.1002/cpt.70094. Epub 2025 Oct 31.
3: Pang S, Wang Z, Fu Y, Huang X. Efficacy and safety of daprodustat versus darbepoetin alfa in the treatment of anemia in chronic renal failure: Systematic review and meta-analysis of randomized controlled trials. J Pharmacol Sci. 2025 May;158(1):68-75. doi: 10.1016/j.jphs.2025.03.006. Epub 2025 Mar 15. 73(2):110-112. English. doi: 10.36290/csf.2024.013.
4:1511596. doi: 10.3389/fneph.2024.1511596.
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