CAS: 71002-09-0; Pirazolac

该化合物是属于治疗性衍生物类别的化学化合物,主要被承认用于制药领域,特别是作为抗炎剂.Pirazolac的结构具有一种有助于其生物活动的线粒子环.该复合物的特征典型为:醇衍生物,包括可能影响其药理特性的各种替代物.Pirazolac已知与特定生物目标相互作用,这可能导致其治疗性效果.此外,重要的是考虑其溶性,稳定性和再活性,这可以因具体的配方和条件而不同.许多化学物质,安全数据和处理预防措施对于其在研究和临床环境中的使用至关重要.

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    专利信息


    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.

    专利号:AU-2022276509-A1
    优先权日:2021-05-20
    标题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms

    专利号:US-9994558-B2
    优先权日:2013-09-20
    标题 :Multicyclic compounds and methods of using same
    发明人:BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM; MCCAULEY DILARA; LANDESMAN YOSEF; GOLAN GALI; KALID ORI; SHECHTER SHARON
    权利人:KARYOPHARM THERAPEUTICS INC
    摘要:The invention generally relates to compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders (e.g., PAK-mediated, for example, PAK4-mediated, diseases and disorders).

    专利号:US-4778805-A
    优先权日:1987-06-18
    标题:4,7-benzofurandione derivatives useful as inhibitors of leukotriene synthesis
    发明人:ADAMS JULIAN; GUINDON YVAN; BELANGER PATRICE C; BELLEY MICHEL L; ROKACH JOSHUA
    权利人:MERCK FROSST CANADA
    摘要:4,7-Benzofurandione derivatives of Formula I, pharmaceutical compositions, and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation, psoriasis and allergic conjunctivitis. The compounds are also useful as analgesics and as cytoprotective agents. Also disclosed are novel intermediates useful for the preparation of the 4,7-benzofurandiones of this invention. ##STR1##

    专利号:WO-2022246227-A1
    优先权日:2021-05-20
    标 题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms

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    主要参考文献


    1: Kurowski M, Dunky A, Geddawi M. Transsynovial distribution and protein binding of pirazolac in patients with rheumatoid arthritis. Eur J Clin Pharmacol. 1986;31(3):307-11. doi: 10.1007/BF00981129. 16(1):17-27. 9(8):548-51. doi: 10.1185/03007998509109633. 16(1):39-48. 10(1):41-53. doi: 10.1007/BF03189696. 9(8):542-7. doi: 10.1185/03007998509109632. 16(1):29-37. 16(1):1-6. 2(4):188-91. doi: 10.1023/A:1016396224046. 10(7):494-501. doi: 10.1185/03007998709112409.

    合成参考文献


    参考文献:10.1055/s-0034-1378674
    摘要:Rossi R, Bellina F, Lessi M, Manzini C, Perego L. Synthesis of Multiply Arylated Heteroarenes, Including Bioactive Derivatives, via Palladium-Catalyzed Direct C–H Arylation of Heteroarenes with (Pseudo)Aryl Halides or Aryliodonium Salts. Synthesis. 2014 Oct 15;46(21):2833–83. doi: 10.1055/s-0034-1378674.
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