CAS: 1263774-59-9; 3-((3S,4R)-3-Methyl-6-(7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)-1,6-Diazaspiro[3.4]Octan-1-yl)-3-Oxopropanenitrile

该化合物是一个小分子,主要作为Sphingosine-1-磷(S1P)受体的选择性调节器,该化合物具有潜在的治疗用途,特别是在治疗自动免疫疾病和炎症方面,值得注意;Etrasimod argin 展示了一种有利的药用植物基因特征,包括口服生物利用率高和可控半衰期,便于施药疗程;该化合物的行动机制包括调控淋巴细胞贩运,导致免疫细胞向炎点迁移减少;这一特征使它成为针对诸如肺炎和多发性硬化症等情况的治疗的候选.此外,在临床试验中对其安全特征进行了评估,显示了一种普遍的可耐性副作用.

结构式图片

欧盟法规

C&L通报

上下游产品

3-(3-Methyl-6-(7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)-1,6-Diazaspiro[3.4]Octan-1-yl)-3-Oxopropanenitrile 1263772-79-7

合成工艺路线路线简述

    4-氨基-7H-吡咯[2,3-D]嘧啶置于potassium Carbonate,Caesium Carbonate,三乙胺,三苯基膦,Lithium Hexamethyldisilazane,偶氮二甲酸二乙酯体系中,用 四氢呋喃,1,4-二氧六环,氘代二甲亚砜,二氯甲烷 用作溶剂,化学反应 56.0H,反应生成迪高替尼
    参考文献:一种德高替尼的制备方法
    标题:一种德高替尼的制备方法
    摘要:本发明揭示了一种德高替尼(Delgocitinib)中间体的制备方法,以常见化合物为起始原料,依次进行溴代,酰化,环合,取代以及缩合还原等反应,使其制备过程原料易得,经济环保,为该原料药提供了一条新的制备途径,适于规模化工业生产.

    海关参考信息

    专利信息


    专利号:US-10906888-B2
    优先权日:2016-07-14
    标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
    发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE
    权利人:PFIZER
    摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    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-2025250277-A1
    优先权日:2015-10-16
    标 题 :PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF
    发明人:ALLIAN AYMAN; JAYANTH JAYANTHY; MOHAMED MOHAMED-ESLAM F; MULHERN MATHEW M; NORDSTROM FREDRIK LARS; OTHMAN AHMED A; ROZEMA MICHAEL J; BHAGAVATULA LAKSHMI; MARROUM PATRICK J; MAYER PETER T; SHEIKH AHMAD Y; BORCHARDT THOMAS B; KLÜNDER BEN; CAMP HEIDI S; PADLEY ROBERT J; VOSS JEFFREY W; PANGAN AILEEN L
    权利人:ABBVIE INC
    摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl) pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and vasculitis), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating giant cell arteritis (GCA).

    专利号:US-10308615-B2
    优先权日:2015-05-29
    标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme
    发明人:CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN
    权利人:PFIZER
    摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:US-2018230127-A1
    优先权日:2015-08-13
    标题 :Bicyclic-Fused Heteroaryl Or Aryl Compounds
    发明人:ANDERSON DAVID RANDOLPH; CURRAN KEVIN JOSEPH; GAVRIN LORI KRIM; GOLDBERG JOEL ADAM; LEE ARTHUR; LOWE MICHAEL DENNIS; PATNY AKSHAY; PIERCE BETSY SUSAN; SAIAH EDDINE; TRZUPEK JOHN DAVID
    权利人:PFIZER
    摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds of Formula (Ia) are disclosed which are inhibitors of Interleukin-1 receptor associated kinase (IRAK4). Methods of treatment, methods of synthesis, and intermediates are also disclosed as defined in the specification.

    专利号:US-10316018-B2
    优先权日:2015-08-27
    标题 :Bicyclic-fused heteroaryl or aryl compounds as IRAK4 modulators
    发明人:LEE KATHERINE LIN; ALLAIS CHRISTOPHE PHILIPPE; DEHNHARDT CHRISTOPH MARTIN; GAVRIN LORI KRIM; HAN SEUNGIL; HEPWORTH DAVID; LEE ARTHUR; LOVERING FRANK ELDRIDGE; MATHIAS JOHN PAUL; OWEN DAFYDD RHYS; PAPAIOANNOU NIKOLAOS; SAIAH EDDINE; STROHBACH JOSEPH WALTER; TRZUPEK JOHN DAVID; WRIGHT STEPHEN WAYNE; ZAPF CHRISTOPH WOLFGANG
    权利人:PFIZER
    摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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    主要参考文献


    1: Ho J, Molin S. Delgocitinib in atopic dermatitis. Drugs Today (Barc). 2021 Dec;57(12):719-731. doi: 10.1358/dot.2021.57.12.3352760. 80(6):609-615. doi: 10.1007/s40265-020-01291-2. 187(1):42-51. doi: 10.1111/bjd.21037. Epub 2022 Apr 19.
    4: Nakagawa H, Nemoto O, Igarashi A, Saeki H, Kabashima K, Oda M, Nagata T. Delgocitinib ointment in pediatric patients with atopic dermatitis: A phase 3, randomized, double-blind, vehicle-controlled study and a subsequent open-label, long-term study. J Am Acad Dermatol. 2021 Oct;85(4):854-862. doi: 10.1016/j.jaad.2021.06.014. Epub 2021 Jun 10. 82(4):823-831. doi: 10.1016/j.jaad.2019.12.015. Epub 2020 Feb 3. Erratum in: J Am Acad Dermatol. 2021 Oct;85(4):1069. 148(4):927-940. doi: 10.1016/j.jaci.2021.08.009. Epub 2021 Aug 24.
    7: Kleinman E, Laborada J, Metterle L, Eichenfield LF. What's New in Topicals for Atopic Dermatitis? Am J Clin Dermatol. 2022 Sep;23(5):595-603. doi: 10.1007/s40257-022-00712-0. Epub 2022 Sep 1.

    合成参考文献


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