📜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.
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).
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.