CAS: 1374639-75-4; 7-Cyclopentyl-N,N-Dimethyl-2-((5-(Piperazin-1-yl)Pyridin-2-yl)Amino)-7H-Pyrrolo[2,3-D]Pyrimidine-6-Carboxamide Succinate

该化合物是环状直系性血管(CDKs)的选择性抑制剂, 特别是CDK4和CDK6, 是癌症研究中引起注意的一种化合物, 主要是研究其在治疗各种恶性肿瘤(包括乳腺癌和其他细胞调节循环衰竭的肿瘤)方面的潜在治疗效应. 杂相形式表明,它是来自氨基酸的盐或酯, 它可以提高其溶解性和生物利用率. LEE011 功能, 干扰视像瘤蛋白的磷酸化, 从而阻止细胞循环从G1到S阶段, 从而减少癌症细胞的扩散. 其致癌特性, 包括吸收,分布,新陈代谢和排泄,对于确定其临床环境中的功效和安全特征至关重要. 与许多调查药物一样, 持续进行的研究对于充分阐明其行动机制, 最佳疗程和病人的潜在副作用至关重要.

结构式图片

欧盟法规

C&L通报

合成工艺路线路线简述

    5-甲酰基尿嘧啶置于盐酸,水,Palladium Diacetate,Potassium Carbonate,R-(+)-1,1'-联萘-2,2'-双二苯膦,N,N-二异丙基乙胺,N-[(Dimethylamino)-3-Oxo-1H-1,2,3-Triazolo[4,5-B]Pyridin-1-Yl-Methylene]-N-Methylmethanaminium Hexafluorophosphate,Sodium Hydroxide,三氯氧磷体系中,用 四氢呋喃,甲醇,水,N,N-二甲基甲酰胺,异丙醇,甲苯 用作溶剂,化学反应 45.34H,反应生成Lee011琥珀酸盐
    参考文献: Ribociclib Intermediate And Process For Preparation Thereof[fr] Intermédiaire De Ribociclib Et Son Procédé De Préparation
    标题: Ribociclib Intermediate And Process For Preparation Thereof[fr] Intermédiaire De Ribociclib Et Son Procédé De Préparation
    摘要:本发明涉及利用新型中间体制备利博西利琼琼酸盐的方法.该发明还涉及制备新型中间体的方法.

    海关参考信息

    专利信息


    专利号:US-2022118094-A1
    优先权日:2019-02-21
    标题:Synthesis of biomimetic cell wall structure
    发明人:WANG YONG; SHI PENG
    权利人:PENN STATE RES FOUND
    摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.

    专利号:US-10336763-B1
    优先权日:2018-05-17
    标题:Crystal form B of ribociclib succinate
    发明人:KAMANI SATYANARAYANA; LU TZU-CHIANG; CHANG HSIN-YUN; MAI CHIN-CHENG
    权利人:CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO LTD
    摘要:The present invention relates to crystal forms B, C and D of Ribociclib succinate salt and derivatives thereof, and their preparation method and composition. The crystal forms B, C and D of Ribociclib succinate salts are obtained by adding 7-cyclopentyl-N,N-dimethyl-2-(5-(piperain-1-yl)pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide solution into succinic acid solution for reaction, stirring the solution under high temperature, filtering the solution after cooling off.

    专利号:US-2023391824-A1
    优先权日:2021-02-08
    标题:Rationale, design, synthesis and validation of a small molecule anticancer agent
    发明人:JAIN MOHIT; NARENDRAN ARUMUGAVADIVEL
    权利人:NARENDRAN ARUMUGAVADIVEL
    摘要:LIN28 is an RNA binding protein that binds and inhibits the expression and maturation of Iet7 microRNA that carries key tumor suppressor functions. Thus, LIN28 is a feasible and effective molecular target for directed inhibition with the potential to provide therapeutic benefit to a diverse group of aggressive malignancies. The present disclosure relates generally to the Rationale, Design, Synthesis and Validation of a Novel Small Molecule Inhibitor of LIN28, coined Compound of formula (I), for the Treatment of Adult and Pediatric Malignancies. In addition, indications of this agent to block cancer metastasis, inhibit cancer stem cells to prevent relapse, and to synergize with immunotherapy, chemotherapy and radiotherapy are also been described.

    专利号:US-2023160018-A1
    优先权日:2020-04-16
    标 题 :Crybetab2 predicts poor breast cancer outcome and sensitizes tumors to nucleolin and cdk inhibition
    发明人:MERINO VANESSA FERREIRA; POMPER MARTIN; SUKUMAR SARASWATI
    权利人:UNIV JOHNS HOPKINS
    摘要:CKYPB2 induces EMT, sternness, protein synthesis and cell cycle progression through regulation of nucleolin, con-tributing to an increase in tumor growth and metastasis. CKYPB2 can be used as a prognostic marker in African American women with TNBC. CKYPB2 can further select patients with TNBC and ER positive tumors that will likely benefit from inhibitors of ribosomal RNA synthesis, CDK4 and nucleolin.

    专利号:WO-2025137620-A1
    优先权日:2023-12-21
    标题:Methods for high quality and high accuracy methylation sequencing
    发明人:KENNEDY ANDREW
    权利人:GUARDANT HEALTH INC
    摘要:Provided herein are methods and compositions for calibrating one or more base calling metrics in a sequencing by synthesis reaction, and for calling at least a portion of nucleobases in a converted region of a DNA molecule using the one or more calibrated base calling metrics. Provided herein are also methods for determining the likelihood that a subject has a disease or condition, such as cancer.

    专利号:EP-4288444-A1
    优先权日:2021-02-08
    标题:Rationale, design, synthesis and validation of a small molecule anticancer agent
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    主要参考文献


    1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548818/ doi: 10.1177/1758835919833867. eCollection 2019. Review.
    3: Poratti M, Marzaro G. Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. Eur J Med Chem. 2019 Jun 15;172:143-153. doi: 10.1016/j.ejmech.2019.03.064. Epub 2019 Apr 4. Review. doi: 10.1007/s40259-019-00337-6. Review. doi: 10.1007/s10549-019-05133-y. Epub 2019 Jan 18. Review. doi: 10.18773/austprescr.2018.058. Epub 2018 Oct 2. Review.
    7: Büyükkaramikli NC, de Groot S, Riemsma R, Fayter D, Armstrong N, Portegijs P, Duffy S, Kleijnen J, Al MJ. Ribociclib with an Aromatase Inhibitor for Previously Untreated, HR-Positive, HER2-Negative, Locally Advanced or Metastatic Breast Cancer: An Evidence Review Group Perspective of a NICE Single Technology Appraisal. Pharmacoeconomics. 2019 Feb;37(2):141-153. doi: 10.1007/s40273-018-0708-4. Review.

    合成参考文献


    参考文献:10.1007/s40262-020-00930-x
    摘要:Groenland SL, Martínez-Chávez A, van Dongen MGJ, Beijnen JH, Schinkel AH, Huitema ADR, Steeghs N. Clinical Pharmacokinetics and Pharmacodynamics of the Cyclin-Dependent Kinase 4 and 6 Inhibitors Palbociclib, Ribociclib, and Abemaciclib. Clin Pharmacokinet. 2020 Dec;59(12):1501–20. doi: 10.1007/s40262-020-00930-x.
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