CAS: 819812-04-9; 2-(2-Ethyl-3,5-Dihydroxy-6-(3-Methoxy-4-(2-Morpholinoethoxy)Benzoyl)Phenyl)-N,N-Bis(2-Methoxyethyl)Acetamide

该化合物是其潜在的治疗用途方面引起了注意,被归类为小分子,并被称为某些蛋白质流动酶的选择性抑制剂,这些蛋白质流动酶在包括细胞生长和分裂在内的各种细胞过程中发挥着关键作用.该化合物的结构通常具有有助于其生物活动和选择性的特定功能群体.KW-2478已经研究其针对癌症等疾病的效果,癌症经常涉及异常的动脉活性活动.其药用动力特性,包括吸收,分布,新陈代谢和排泄物(ADME),对于确定其临床使用是否合适至关重要.此外,持续开展研究的目的是阐明其行动机制和潜在副作用,这对于评估其安全状况至关重要.

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    专利信息


    专利号:WO-2014018862-A1
    优先权日:2012-07-27
    标 题 :Pharmaceutical compositions comprising a heat shock protein inhibitor and a; purine de novo synthesis inhibitor for treating rheumatoid arthritis or cancer
    发明人:FANG YE
    权利人:CORNING INC; FANG YE
    摘要:A pharmaceutical composition including an effective amount of the combination of: an heat shock protein (HSP) inhibitor, and a purine de novo biosynthesis inhibitor, or a pharmaceutically acceptable salt thereof. Also disclosed is a method of treating rheumatoid arthritis or cancer including administering an effective amount of the above mentioned pharmaceutical composition to a patient in need of such treatment, as defined herein.

    专利号:WO-2013002253-A1
    优先权日:2011-06-27
    标 题 :Method for producing benzophenone derivative
    发明人:MATSUMURA TSUTOMU; SAITOH TOSHIKAZU; TAKEMURA KAZUNOBU; KOBAYASHI KENTARO; NITTA MARIKO; HAGIHARA KOJI
    权利人:KYOWA HAKKO KIRIN CO LTD; MATSUMURA TSUTOMU; SAITOH TOSHIKAZU; TAKEMURA KAZUNOBU; KOBAYASHI KENTARO; NITTA MARIKO; HAGIHARA KOJI
    摘要:Provided are: a compound represented by general formula (I) (wherein R 1a and R 1b may be the same as or different from each other and independently represent a benzyl group substituted by one to three halogen atoms, wherein, when the number of the halogen atoms is two or three, the halogen atoms may be the same as or different from each other; R 2 represents a lower alkyl group which may have a substituent; and R 3 represents a lower alkoxycarbonyl group which may have a substituent) or a salt thereof, which is useful in, for example, a method for producing an intermediate for the synthesis of a benzophenone derivative having an anti-tumor activity and the like; a method for producing a benzophenone derivative represented by general formula (III) (wherein R 1a , R 1b , R 2 and R 3 are as defined above; R 4 represents a lower alkyl group which may have a substituent; and R 5 represents an aliphatic heterocyclic alkyl group which may have a substituent) or a salt thereof, the method being characterized by comprising reacting a compound represented by general formula (II) (wherein R 4 and R 5 are as defined above) or a salt thereof in the presence of an acid; and others.

    专利号:US-11312722-B2
    优先权日:2019-05-08
    标 题:Hsp90 inhibitors and uses thereof
    发明人:BROWN LAUREN ELAINE; HUANG DAVID S; COWEN LEAH E; WHITESELL LUKE; MARCYK PAUL
    权利人:UNIV BOSTON; GOVERNING COUNCIL UNIV TORONTO
    摘要:Herein is described the design and synthesis of resorcylate aminopyrazole compounds. These compounds show broad, potent and fungal-selective Hsp90 inhibitory activity. These compounds also find use in treating Hsp90 related diseases.

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    主要参考文献


    1: Soga S. [Drug discovery and research of heat shock protein 90 (Hsp90) inhibitor]. Nihon Yakurigaku Zasshi. 2013 Jan;141(1):9-14. Review. Japanese. Review. doi: 10.1038/bcj.2012.13. Epub 2012 Apr 27.
    4: Nakashima T, Ishii T, Tagaya H, Seike T, Nakagawa H, Kanda Y, Akinaga S, Soga S, Shiotsu Y. New molecular and biological mechanism of antitumor activities of KW-2478, a novel nonansamycin heat shock protein 90 inhibitor, in multiple myeloma cells. Clin Cancer Res. 2010 May 15;16(10):2792-802. doi: 10.1158/1078-0432.CCR-09-3112. Epub 2010 Apr 20.

    合成参考文献


    参考文献:10.1124/mol.119.115964
    摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
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