CAS: 56-47-3; 21-(Acetyloxy)-Pregn-4-Ene-3,20-Dione

该化合物是一种合成类固醇激素,主要作为矿质类动物,主要用于肾上腺皮激素,其特点是调节体内电解和水平衡的作用,影响钠的留存量和钾的排泄量;DOCA通常以乙酸形式施用,这增加了其溶解性和生物利用率;化合物的分子配方反映其类固醇结构,由多种环和功能组组成,有助于其生物活动;在研究和临床环境中,它经常用于研究肾上腺功能和高血压;在物理特性方面,DOCA是一种白对白对非白的晶状粉,在标准条件下相对稳定,在有机溶剂中溶解,但在水中较少,其药理效应可包括增加血压和液体的留存量,从而在与心血管健康和内分泌紊乱有关的研究中具有重大意义;但是,与其他类固醇一样,它可能具有副作用,需要谨慎的剂量管理.

结构式图片

欧盟法规

ECHA物质ECHA物质C&L通报REACH预注册

上下游产品

CAS号64-85-7 去氧皮质酮 | CAS号108-24-7 乙酸酐 | CAS号566-78-9 21-乙酰氧基孕烯醇酮 | CAS号62490-13-5 3β-formyloxy-21... | CAS号1171-90-0 Pregna-1,4-dien... | CAS号567-02-2 3alpha,21-二羟基-5... | CAS号298-36-2 21-羟基-5Alpha-孕甾... | CAS号303-01-5 Pregnane-3,20-d... | CAS号111464-71-2 4,5-epoxy-21-hy... | CAS号302-97-6 3-氧代-雄甾-4-烯-17β-羧酸 | CAS号80-92-2 5β-孕烷-3α,20α-二醇 | CAS号64-85-7 去氧皮质酮

合成工艺路线路线简述

    乙烯酮置于丙酮体系中,化学反应生成 醋酸去氧皮质酮
    参考文献:Ch204234
    标题:Ch204234

    海关参考信息

    专利信息


    专利号:US-8546532-B2
    优先权日:2008-04-17
    标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders
    发明人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS
    权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC
    摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.

    专利号:US-2004101523-A1
    优先权日:1989-07-27
    标题:Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension
    发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
    权利人:SEARLE & CO
    摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.

    专利号:WO-9201667-A1
    优先权日:1990-07-25
    标题 :Renal-selective prodrugs for control of renal sympathetic nerve activity in the treatment of hypertension
    发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
    权利人:SEARLE & CO
    摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kydney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase-inhibitors, of which N-acetyl-η-glutamyl fusaric acid hydrazide [represented in formula (a)] is preferred.

    专利号:WO-2022226312-A1
    优先权日:2021-04-22
    标 题:Combination nucleotide pool depletion for treatment of viral infections and cancers
    发明人:KUMAR VIKRAM; HESSON DAVID; DEMAREST JAMES
    权利人:CLEAR CREEK BIO INC
    摘要:The invention provides methods of treating cancers and viral infections by providing a combination of agents that inhibit both nucleotide synthesis and nucleotide salvage in the cells of a subject to prevent cancer proliferation and viral replication. The invention provides methods of depleting nucleotide pools by using both inhibitors of dihydroorotate dehydrogenase (DHODH), such as brequinar, which block synthesis of pyrimidine-based nucleotides, in combination of one or more nucleotide salvage inhibitors, for example deoxycytidine kinase (dCK) inhibitors, Equilibrative nucleoside transporter (ENT) inhibitors, and Uridine-cytidine kinase (UCK) inhibitors, which inhibit salvage of purine and/or pyrimidine-based nucleotides or nucleosides

    专利号:US-9051302-B2
    优先权日:2008-01-15
    标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents
    发明人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN
    权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG
    摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

    专利号:US-2024287041-A1
    优先权日:2021-05-20
    标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
    发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN
    权利人:KARYOPHARM THERAPEUTICS INC
    摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.
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    主要参考文献


    1: Sapouckey SA, Deng G, Sigmund CD, Grobe JL. Potential mechanisms of hypothalamic renin-angiotensin system activation by leptin and DOCA-salt for the control of resting metabolism. Physiol Genomics. 2017 Dec 1;49(12):722-732. doi: 10.1152/physiolgenomics.00087.2017. Epub 2017 Oct 6. Review. doi: 10.1007/s11906-017-0731-4. Review. doi: 10.1016/j.jsbmb.2016.02.002. Epub 2016 Feb 6. Review.
    4: Maayah ZH, El-Kadi AO. The role of mid-chain hydroxyeicosatetraenoic acids in the pathogenesis of hypertension and cardiac hypertrophy. Arch Toxicol. 2016 Jan;90(1):119-36. doi: 10.1007/s00204-015-1620-8. Epub 2015 Nov 2. Review. Review. doi: 10.1161/CIRCRESAHA.116.303697. Review.
    7: Franco M, Bautista-Pérez R, Pérez-Méndez O. Purinergic receptors in tubulointerstitial inflammatory cells: a pathophysiological mechanism of salt-sensitive hypertension. Acta Physiol (Oxf). 2015 May;214(1):75-87. doi: 10.1111/apha.12471. Epub 2015 Feb 28. Review. doi: 10.1589/jpts.27.303. Epub 2015 Jan 9. Review.

    合成参考文献


    参考文献:10.1177/1087057116635503
    摘要:Voter AF, Manthei KA, Keck JL. A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. J Biomol Screen. 2016 Jul;21(6):626–33.
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