CAS: 1425381-60-7; 2-(1-(4-((4-(4-Hydroxypiperidin-1-yl)Phenyl)Amino)-5-Oxo-5,6-Dihydropyrimido[4,5-D]Pyridazin-2-yl)Piperidin-4-yl)Acetonitrile

该化合物是一种小分子抑制剂,主要针对Janus kinase(JAK)酶,特别是JAK1和JAK2,它们对于各种细胞细胞和生长因素的信号路径具有关键作用;该化合物在自发性疾病和某些发炎条件下的潜在治疗应用正在受到调查;其行动机制涉及通过抑制JAK-STAT信号路径来调节免疫反应,从而减少炎情并改变免疫细胞功能;Guscitinib的特点是有选择地抑制,目的是尽量减少与更广泛的免疫抑制疗法相关的副作用;该物质通常通过口服方式进行,并经过不同阶段的临床试验,以评估其功效和安全性;与许多调查药物一样,药类,药性,代谢和潜在的药物相互作用是确保最佳治疗结果的关键研究领域;

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C&L通报

合成工艺路线路线简述

    📜1-(4-氨基苯基)-4-羟基哌啶,置于1-(4-氨基苯基)-4-羟基哌啶体系中,化学反应生成化合物gusacitinib
    参考文献:Pyrimido-Pyridazinone Compounds And Methods Of Use Thereof
    标题:Pyrimido-Pyridazinone Compounds And Methods Of Use Thereof
    摘要:本申请提供了新型嘧啶并吡啶嗪酮化合物以及制备和使用这些化合物的方法.通过向患者投药一种或多种化合物,这些化合物可用于治疗患者的炎症.在一种实施方式中,新型嘧啶并吡啶嗪酮化合物为公式(i)中的化合物,其中r1和r2在此定义.

    海关参考信息

    专利信息


    专利号:US-2022170057-A1
    优先权日:2019-04-11
    标题:Microorganisms and methods for the fermentation of cannabinoids
    发明人:SZAMECZ BELA KRISZTIAN; VARSZEGI SZILVIA; NEMETH ATTILA; SZABO LORAND
    权利人:ELESZTO GENETIKA INC
    摘要:Disclosed herein are microorganism and methods that can be used for the synthesis of cannabigerolic acid (CBGA) and cannabinoids. The methods disclosed can be used to produce CBGA, Δ 9 -tetrahydrocannabinolic acid (THCA), cannabidiolic acid (CBDA), cannabichromenic acid (CBGA), Δ 9 -tetrahydrocannabivarinic acid (THCVA), cannabidivarinic acid (CBDVA), cannabichromevarinic acid (CBCVA), Δ 9 -tetrahydrocannabinol (THC), cannabidiol (CBD), cannabichromene (CBC). Enzymes useful for the synthesis of CBGA and cannabinoids, include but are not limited to acyl activating enzyme (AAE1), polyketide synthase (PKS), olivetolic acid cyclase (OAC), prenyltransferase (PT), THCA synthase (THCAS), CBDA synthase (CBDAS), CBC A synthase (CBCAS), HMG-Co reductase (HMG1), and/or famesyl pyrophosphate synthetase (ERG20). The microorganisms can also have one or more genes disrupted, such as gene that that controls beta oxidation of long chain fatty acids.

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    ✅ COA系统入驻 | 共享模式

    主要参考文献

    1. http://cancerres.aacrjournals.org/content/77/13_Supplement/4204 2. Kinase Inhibitors for the Treatment of Immunological Disorders: Marian C. Bryan, and Naomi S. Rajapaksa; Publication Date (Web): June 5, 2018 (Perspective); DOI: 10.1021/acs.jmedchem.8b00667

    合成参考文献


    参考文献:10.1684/ejd.2023.4541
    摘要:Byrne N, Diaz AR, Dege T, Chircop I, Reynaud V, Lé A, Garcia-Piqueras P. Journal Club. 2023 Aug;33(4):451–4. doi: 10.1684/ejd.2023.4541.
    参考文献:10.1007/978-3-031-52147-8_15
    摘要:Jin JQ, Spencer RK, Elhage KG, Davis MS, Hakimi M, Liao W, Bhutani T. Treatment of AD with Abrocitinib. 2024. In: Clinical Cases in Dermatology.
    参考文献:10.1007/s40521-024-00374-9
    摘要:Grafanaki K, Maniatis A, Antonatos C, Vryzaki E, Vasilopoulos Y, Georgiou S, Stratigos AJ, Gregoriou S. Immunological Advancements In Hand Eczema Treatment: Progress With Small Molecules and Biologics. Curr Treat Options Allergy. 2024 Sep 19;11(4):211–27. doi: 10.1007/s40521-024-00374-9.
    参考文献:10.1007/s15012-024-8593-3
    参考文献:10.1007/s12326-024-00691-5
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