CAS: 1354690-24-6; (S)-1-(3-((6-(6-Methoxy-5-(Trifluoromethyl)Pyridin-3-yl)-5,6,7,8-Tetrahydropyrido[4,3-D]Pyrimidin-4-yl)Amino)Pyrrolidin-1-yl)Propan-1-One

该化合物是一种该化合物是一种罕见的PI3K(APDS),它以PI3K路径为目标,调节了过度活性免疫反应,减少淋巴细胞过度扩散,恢复了免疫全息状态,它的高度选择性最大限度地减少了目标外效应,加强了安全性,与更广泛的光谱PI3K抑制剂相比. 临床研究表明它在减少淋巴病扩散和改善APDS病人免疫性功能调节方面的效力. Leniolisib是口头管理的,提供了方便的剂量疗法. 它的行动机制和有利的药用基因特征使它成为解决APDS基本病理的有希望的治疗选择.

结构式图片

上下游产品

[6-(6-Methoxy-5-Trifluoromethyl-Pyridin-3-yl)-5,6,7,8-Tetrahydro-Pyrido[4,3-D]Pyrimidin-4-Yl]-(S)-Pyrrolidin-3-Yl-Amine 1354692-00-4
(S)-3-[6-(6-Methoxy-5-Trifluoromethyl-Pyridin-3-yl)-5,6,7,8-Tetrahydro-Pyrido[4,3-D]Pyrimidin-4-Ylamino]-Pyrrolidine-1-Carboxylic Acid Tert-Butyl Ester 1354691-73-8
(S)-3-(6-Benzyl-5,6,7,8-Tetrahydro-Pyrido[4,3-D]Pyrimidin-4-Ylamino)-Pyrrolidine-1-Carboxylic Acid Tert-Butyl Ester 1354691-71-6
(S)-3-(5,6,7,8-Tetrahydro-Pyrido[4,3-D]Pyrimidin-4-Ylamino)-Pyrrolidine-1-Carboxylic Acid Tert-Butyl Ester 1354691-72-7

合成工艺路线路线简述

  • 合成目标产物 Leniolisib 主要起始原料 1-Pyrrolidinecarboxylic Acid, 3-[[5,6,7,8-Tetrahydro-6-[6-Methoxy-5-(Trifluoromethyl)-3-Pyridinyl]Pyrido[4,3-D]Pyrimidin-4-Yl]Amino]-, 1,1-Dimethylethyl Ester, (3S)- And Propionyl Chloride
  • (文献来源)合成步骤主要原料 1-Pyrrolidinecarboxylic Acid, 3-[[5,6,7,8-Tetrahydro-6-[6-Methoxy-5-(Trifluoromethyl)-3-Pyridinyl]Pyrido[4,3-D]Pyrimidin-4-Yl]Amino]-, 1,1-Dimethylethyl Ester, (3S)- 和 Propionyl Chloride
📜(S)-(-)-N-叔丁氧羰基-3-氨基吡咯烷置于tris-(Dibenzylideneacetone)Dipalladium(0),10 Wt% Pd(Oh)2 On Carbon,甲酸:三乙胺 1:1,Potassium Carbonate,三氟乙酸,2-二-叔丁基磷-2'-甲基联苯体系中,用 N-甲基吡咯烷酮,甲醇,二氯甲烷,叔丁醇 用作溶剂,化学反应 27.33H,反应生成(S)-1-(3-((6-(6-甲氧基-5-(三氟甲基)吡啶-3-基)-5,6,7,8-四氢吡啶并[4,3-D]嘧啶-4-基)氨基)吡咯烷-1-基)丙-1-酮
参考文献:Use Of Inhibitors Of The Activity Or Function Of Pi3K
标题:Use Of Inhibitors Of The Activity Or Function Of Pi3K
摘要:该发明涉及pi3K抑制剂的新用途,其中所述抑制剂对pi3K同工酶δ具有抑制作用,用于治疗患有疟疾,利什曼病,锥虫病,弓形虫病和/或神经囊虫病等疾病或紊乱的受试者的免疫病理学,通过对感染受试者的tlr9的功能抑制.

海关参考信息

专利信息


专利号:US-12441733-B2
优先权日:2018-03-26
标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
发明人:ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
权利人:NOVARTIS AG
摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

专利号:US-12390420-B1
优先权日:2024-10-22
标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof
发明人:EGUCHI MASAKATSU
权利人:BRYET US INC
摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.

专利号:US-2011124634-A1
优先权日:2008-05-13
标 题:Bioactive compounds for treatment of cancer and neurodegenerative diseases
发明人:SUN CONNIE L; LI XIAOYUAN
权利人:PONIARD PHARMACEUTICALS INC
摘要:The invention provides bioactive compounds for the treatment of various malconditions such as cancer and neurodegenerative diseases including Alzheimer's disease. The chemical compounds as disclosed herein are found to show bioactivity in bioassays related to these conditions. Pharmaceutical compositions, combinations and methods of synthesis are provided, as are methods of using the compound, compositions and combinations in the treatment of the diseases.

专利号:CN-116103257-A
优先权日:2023-03-11
标 题 :Reductive amination enzyme mutant and application thereof in synthesis of alkylated pyrrolidine chiral amine

专利号:CN-116103257-B
优先权日:2023-03-11
标题 :Reductive amination enzyme mutants and their application in the synthesis of alkylated pyrrolidine chiral amines

专利号:WO-2024115549-A1
优先权日:2022-11-30
标题:Aryl- and heteroaryl-sulfonamide derivatives as ccr8 modulators
发明人:AISSAOUI HAMED; CORMINBOEUF OLIVIER; DIETHELM STEFAN; REMEN LUBOS; 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 CCR8 receptor modulators in medicine.

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: Pearson D, Garnier M, Luneau A, James AD, Walles M. (19)F-NMR-based determination of the absorption, metabolism and excretion of the oral phosphatidylinositol-3-kinase (PI3K) delta inhibitor leniolisib (CDZ173) in healthy volunteers. Xenobiotica. 2018 Nov
29:1-8. doi: 10.1080/00498254.2018.1523488. [Epub ahead of print] doi: 10.1002/bdd.2157. doi: 10.1016/j.jaci.2018.08.016. Epub 2018 Aug 29.
4: Avery DT, Kane A, Nguyen T, Lau A, Nguyen A, Lenthall H, Payne K, Shi W, Brigden H, French E, Bier J, Hermes JR, Zahra D, Sewell WA, Butt D, Elliott M, Boztug K, Meyts I, Choo S, Hsu P, Wong M, Berglund LJ, Gray P, O'Sullivan M, Cole T, Holland SM, Ma CS, Burkhart C, Corcoran LM, Phan TG, Brink R, Uzel G, Deenick EK, Tangye SG. Germline-activating mutations in PIK3CD compromise B cell development and function. J Exp Med. 2018 Aug 6;215(8):2073-2095. doi: 10.1084/jem.20180010. Epub 2018 Jul 17.

合成参考文献


摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).
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