CAS: 1392136-43-4; (Z)-3-(3-(3,5-Bis(Trifluoromethyl)Phenyl)-1H-1,2,4-Triazol-1-yl)-N'-(Pyridin-2-yl)Acrylohydrazide

结构式图片

上下游产品

3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazole (Z)-isopropyl 3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylate pyrid-2-ylhydrazine (Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylic acid

合成工艺路线路线简述

  • 合成目标产物 Verdinexor (Kpt-335) 主要起始原料 2-Hydrazinopyridine And (Z)-3-(3-(3,5-Bis(Trifluoromethyl)Phenyl)-1H-1,2,4-Triazol-1-yl)Acrylic Acid
  • (文献来源)合成步骤主要原料 2-Hydrazinopyridine 和 (Z)-3-(3-(3,5-Bis(Trifluoromethyl)Phenyl)-1H-1,2,4-Triazol-1-yl)Acrylic Acid
📜3,5-二(三氟甲基)硫代苯甲酰胺置于三乙烯二胺,水,一水合肼,1-丙基磷酸酐,N,N-二异丙基乙胺,Lithium Hydroxide体系中,用 四氢呋喃,二氯甲烷,乙酸乙酯,N,N-二甲基甲酰胺 用作溶剂,化学反应 21.0H,反应生成Verdinexor(kpt-335)抑制剂
参考文献: Hydrazide Containing Nuclear Transport Modulators And Uses Thereof[fr] Modulateurs De Transport Nucléaire Contenant De L'Hydrazide Et Leurs Utilisations
标题: Hydrazide Containing Nuclear Transport Modulators And Uses Thereof[fr] Modulateurs De Transport Nucléaire Contenant De L'Hydrazide Et Leurs Utilisations
摘要:这项发明通常与核运输调节剂有关,例如crm1抑制剂,更具体地涉及一种由结构式(I)表示的化合物,或其药学上可接受的盐,其中变量的值和备选值如本文所定义和描述.该发明还包括合成和使用结构式i的化合物,或其药学上可接受的盐或组合物,例如在与crm1活性相关的生理状况的治疗,调节和/或预防中的应用.

海关参考信息

专利信息


专利号:US-9714226-B2
优先权日:2011-07-29
标题:Hydrazide containing nuclear transport modulators and uses thereof
发明人:SANDANAYAKA VINCENT P; SHACHAM SHARON; MCCAULEY DILARA; SHECHTER SHARON
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: n nor a pharmaceutically acceptable salt thereof, wherein the values and alternative values for 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 the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.

专利号:US-9428490-B2
优先权日:2011-07-29
标 题 :Nuclear transport modulators and uses thereof
发明人:SANDANAYAKA VINCENT P; SHACHAM SHARON; KAUFFMAN MICHAEL; SHECHTER SHARON; MCCAULEY DILARA; LANDESMAN YOSEF; SENAPEDIS WILLIAM; SAINT-MARTIN JEAN-RICHARD
权利人:SANDANAYAKA VINCENT P; SHACHAM SHARON; KAUFFMAN MICHAEL; SHECHTER SHARON; MCCAULEY DILARA; LANDESMAN YOSEF; SENAPEDIS WILLIAM; SAINT-MARTIN JEAN-RICHARD; KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to nuclear transport modulators, e.g CRM1 inhibitors, and more particularly to a compound represented by 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 the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.

专利号:CN-116514773-A
优先权日:2023-04-24
标题 :Verdinexor (KPT-335) and synthesis method of hydrochloride thereof

专利号:CN-116514773-B
优先权日:2023-04-24
标题 :Verdinexor (KPT-335) and synthesis method of hydrochloride thereof

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: Gravina GL, Senapedis W, McCauley D, Baloglu E, Shacham S, Festuccia C. Nucleo-cytoplasmic transport as a therapeutic target of cancer. J Hematol Oncol. 2014 Dec 5;7:85. doi: 10.1186/s13045-014-0085-1. Review.
2: Tan M, Wettersten HI, Chu K, Huso DL, Watnick T, Friedlander S, Landesman Y, Weiss RH. Novel inhibitors of nuclear transport cause cell cycle arrest and decrease cyst growth in ADPKD associated with decreased CDK4 levels. Am J Physiol Renal Physiol. 2014 Dec 1;307(11):F1179-86. doi: 10.1152/ajprenal.00406.2014. Epub 2014 Sep 18.
3: Breit MN, Kisseberth WC, Bear MD, Landesman Y, Kashyap T, McCauley D, Kauffman MG, Shacham S, London CA. Biologic activity of the novel orally bioavailable selective inhibitor of nuclear export (SINE) KPT-335 against canine melanoma cell lines. BMC Vet Res. 2014 Jul 15;10:160. doi: 10.1186/1746-6148-10-160.

合成参考文献


参考文献:10.1186/s12929-021-00753-3
摘要:Lang Y, Jou Y. PSPC1 is a new contextual determinant of aberrant subcellular translocation of oncogenes in tumor progression. Journal of Biomedical Science. 2021 Aug 02;28(1):57. doi: 10.1186/s12929-021-00753-3.
摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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