CAS: 1202402-40-1; (S)-7-(5-Methylfuran-2-yl)-3-((6-(((Tetrahydrofuran-3-yl)Oxy)Methyl)Pyridin-2-yl)Methyl)-3H-[1,2,3]Triazolo[4,5-D]Pyrimidin-5-Amine

该化合物是一个复杂的有机化合物,其特点是其多环结构和各种功能组.该化合物具有三氮-丙胺核心,以其潜在的生物活动为名,特别是在药用化学领域.一个呋喃环和四氢呋喃的出现表明,它可能与生物目标产生有趣的互动,有可能影响其药理特性.(S)配置所显示的立体化学学学可能在其生物活动中也发挥关键作用,因为其气质能对生物系统中的分子行为产生重大影响.

结构式图片

上下游产品

(S)-(6-(((tetrahyd rofuran-3-yl)oxy)methyl)pyridin-2-yl)methanamine 4-(6-[(S)-(tetrahydrofuran-3-yl)oxymethyl]pyridin-2-ylmethyl)pyrimidine-2,4,5-triamine6-chloro-N4-(6-[(S)-(tetrahydrofuran-3-yl)oxymethyl]pyridin-2-ylmethyl)pyrimidine-2,4,5-triamine 7-chloro-3-{6-[(S)-(tetrahydrofuran-3-yl)oxymethyl]pyridin-2-ylmethyl}-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-ylamine 4,4,5,5-tetramethyl-2-(5-methylfuran-2-yl)-1,3,2-dioxaborolane

合成工艺路线路线简述

  • 合成目标产物 Cpi-444 主要起始原料 (S)-7-Chloro-3-((6-(((Tetrahydrofuran-3-yl)Oxy)Methyl)Pyridin-2-yl)Methyl)-3H-[1,2,3]Triazolo[4,5-D]Pyrimidin-5-Amine And 2-Methylfurane-5-Boronic Acid Pinacol Ester
  • (文献来源)合成步骤主要原料 (S)-7-Chloro-3-((6-(((Tetrahydrofuran-3-yl)Oxy)Methyl)Pyridin-2-yl)Methyl)-3H-[1,2,3]Triazolo[4,5-D]Pyrimidin-5-Amine 和 2-Methylfurane-5-Boronic Acid Pinacol Ester
📜2-甲基呋喃-5-硼酸频哪醇酯置于盐酸,四(三苯基膦)钯,草酰氯,三乙醇胺,Sodium Hydride,Sodium Carbonate,N,N-二甲基甲酰胺,Sodium Nitrite体系中,用 四氢呋喃,1,4-二氧六环,水,异丙醇,乙腈 用作溶剂,化学反应 11.33H,反应生成7-(5-甲基-2-呋喃基)-3-[[6-[[[(3S)-四氢-3-呋喃基]氧基]甲基]-2-吡啶基]甲基]-3H-1,2,3-三唑并[4,5-D]嘧啶-5-胺
参考文献: Processes For Making Triazolo [4,5D] Pyramidine Derivatives And Intermediates Thereof[fr] Procédés De Fabrication De Dérivés De Triazolo[4,5D]Pyrimidine Et D'Intermédiaires De Ceux-Ci
标题: Processes For Making Triazolo [4,5D] Pyramidine Derivatives And Intermediates Thereof[fr] Procédés De Fabrication De Dérivés De Triazolo[4,5D]Pyrimidine Et D'Intermédiaires De Ceux-Ci
摘要:本文提供了制备三唑[4,5]嘧啶衍生物和中间体的方法,所述化合物可用于制备包括式(I),(II),(III)或(Iv)化合物在内的药物组合物,用于治疗包括癌症在内的疾病.所提供的组合物适用于体外或体内的配制和给药.

海关参考信息

专利信息


专利号:US-2022259212-A1
优先权日:2019-07-11
标题:Inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan 2,3-dioxygenase
发明人:BOSS CHRISTOPH; CREN SYLVAINE; KIMMERLIN THIERRY; LOTZ-JENNE CARINA; POTHIER JULIEN; TIDTEN-LUKSCH NAOMI
权利人:IDORSIA PHARMACEUTICALS LTD
摘要:The present invention relates to compounds of Formula (I) inhibiting indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) enzymes. Further, their synthesis and their use as medicaments in the treatment of inter alia cancer is disclosed.

专利号:US-11267824-B2
优先权日:2017-08-17
标 题:Inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan 2,3-dioxygenase
发明人:BOSS CHRISTOPH; BUR DANIEL; CREN SYLVAINE; KIMMERLIN THIERRY; LOTZ-JENNE CARINA; POTHIER JULIEN; TIDTEN-LUKSCH NAOMI
权利人:IDORSIA PHARMACEUTICALS LTD
摘要:The present invention relates to compounds of Formula (I) inhibiting indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) enzymes. Further, their synthesis and their use as medicaments in inter alia cancer is disclosed.

专利号:US-2025011313-A1
优先权日:2021-10-28
标 题:Ccr6 receptor modulators
发明人:ALLEMANN OLIVER; HUBLER FRANCIS; MEYER EMMANUEL
权利人:IDORSIA PHARMACEUTICALS LTD
摘要:The present invention relates to compounds of Formula (I), their synthesis and use as CCR6 receptor modulators for the prevention or treatment of e.g. inflammatory/autoimmune diseases/disorders and cancer.

专利号:US-2025042881-A1
优先权日:2021-10-26
标 题 :Ccr6 receptor modulators
发明人:ALLEMANN OLIVER; CAROFF EVA; HUBLER FRANCIS; MEYER EMMANUEL
权利人:IDORSIA PHARMACEUTICALS LTD
摘要:The present invention relates to compounds of Formula (I), their synthesis and use as CCR6 receptor modulators for the prevention or treatment of e.g. inflammatory/autoimmune diseases/disorders and cancer.

专利号:WO-2023057548-A1
优先权日:2021-10-07
标题:Ccr6 receptor modulators
发明人:AISSAOUI HAMED; ALLEMANN OLIVER; CAROFF EVA; MEYER EMMANUEL; RICHARD-BILDSTEIN SYLVIA
权利人:IDORSIA PHARMACEUTICALS LTD
摘要:The present invention relates to compounds of Formula (I), their synthesis and use as CCR6 receptor modulators for the prevention or treatment of e.g. inflammatory/autoimmune diseases/disorders and cancer.

专利号:US-2022259202-A1
优先权日:2019-06-17
标题:1-(4-(aminomethyl)benzyl)-2-butyl-2h-pyrazolo[3,4-c]quinolin-4-amine derivatives and related compounds as toll-like receptor (tlr) 7/8 agonists, as well as antibody drug conjugates thereof for use in cancer therapy and diagnosis
发明人:MEIMETIS LABROS
权利人:SUTRO BIOPHARMA INC
摘要:1-(4-(aminomethyl)benzyl)-2-butyl-2H-pyrazolo[3,4-c]quinolin-4-amine derivatives thereof and related compounds of formula (I) as toll-like receptor (TLR) 7/8 agonists for cancer therapy. Linker payload compounds thereof, and antibody conjugates thereof for cancer diagnosis. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 145 to 156; examples 1 to 3; biological examples 1 to 6; tables 1 and 2).

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: Fong L, Hotson A, Powderly JD, Sznol M, Heist RS, Choueiri TK, George S, Hughes BGM, Hellmann MD, Shepard DR, Rini BI, Kummar S, Weise AM, Riese MJ, Markman B, Emens LA, Mahadevan D, Luke JJ, Laport G, Brody JD, Hernandez-Aya L, Bonomi P, Goldman JW, Berim L, Renouf DJ, Goodwin RA, Munneke B, Ho PY, Hsieh J, McCaffery I, Kwei L, Willingham SB, Miller RA. Adenosine 2A Receptor Blockade as an Immunotherapy for Treatment-Refractory Renal Cell Cancer. Cancer Discov. 2020 Jan;10(1):40-53. doi: 10.1158/2159-8290.CD-19-0980. Epub 2019 Nov 15.
2: Iacovelli R, Ciccarese C, Procopio G, Astore S, Cannella MA, Maratta MG, Rizzo M, Verzoni E, Porta C, Tortora G. Current evidence for second-line treatment in metastatic renal cell carcinoma after progression to immune-based combinations. Cancer Treat Rev. 2022 Apr;105:102379. doi: 10.1016/j.ctrv.2022.102379. Epub 2022 Mar 12. 10(1):16-19. doi: 10.1158/2159-8290.CD-19-1280. 6(10):1136-1149. doi: 10.1158/2326-6066.CIR-18-0056. Epub 2018 Aug 21.

合成参考文献


参考文献:10.1007/978-3-030-98950-7_10
摘要:Kushekhar K, Chellappa S, Aandahl EM, Taskén K. Role of Lymphocytes in Cancer Immunity and Immune Evasion Mechanisms. 2022. In: Biomarkers of the Tumor Microenvironment.
参考文献:10.1007/978-981-16-8845-4_19
摘要:Dey S, Mavuduru RS. Adenosine Pathway in Genitourinary Malignancies: A Promising Immunotherapeutic Target. 2022. In: Biomedical Translational Research.
参考文献:10.1007/7355_2023_158
摘要:Catarzi D, Varano F, Calenda S, Vigiani E, Colotta V. Once Upon a Time Adenosine and Its Receptors: Historical Survey and Perspectives as Potential Targets for Therapy in Human Diseases. 2023. In: Topics in Medicinal Chemistry.
参考文献:10.1007/978-3-031-40901-1_14
摘要:Thapa B, Nelson A, Kilari D. Novel Targets in Development for Advanced Renal Cell Carcinoma. 2023. In: Integrating Multidisciplinary Treatment for Advanced Renal Cell Carcinoma.
参考文献:10.1186/s12943-021-01489-2
摘要:Yi M, Zheng X, Niu M, Zhu S, Ge H, Wu K. Combination strategies with PD-1/PD-L1 blockade: current advances and future directions. Molecular Cancer. 2022 Jan 21;21(1):28. doi: 10.1186/s12943-021-01489-2.
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