CAS: 1306760-87-1; (S)-5-(3-(1-((2-Hydroxyethyl)Amino)-2,3-Dihydro-1H-Inden-4-yl)-1,2,4-Oxadiazol-5-yl)-2-Isopropoxybenzonitrile

该化合物是一种选择性的硫化物1-磷受体受体调节器,主要针对S1P受体1和5.该物质用于治疗某些自体免疫性疾病,特别是多发性硬化症和溃化性结膜炎.该化合物展示了一种独特的行动机制,通过调制淋巴细胞贩运来调节淋巴细胞,有效减少循环性淋巴细胞的数量,从而减轻炎症反应.奥萨尼摩德的特征是口服生物利用率和相对较长的半衰期,允许每天一次使用.其化学结构包括双环核心,有助于其特性和能性.该物质经历了广泛的临床试验,在减少疾病活动和改善患者结果方面表现出了功效.与许多药剂一样,潜在的副作用可能包括感染,肝酶升高和心血管影响,需要在治疗期间进行仔细监测.

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(S)-5-(3-(1-Amino-2,3-Dihydro-1H-Inden-4-yl)-1,2,4-Oxadiazol-5-yl)-2-Isopropoxybenzonitrile 1306760-73-5

合成工艺路线路线简述

    📜3-氰基-4-异丙氧基苯甲酸置于三甲基硅醇,Potassium Trimethylsilonate,N,N'-羰基二咪唑体系中,用 四氢呋喃,N-甲基吡咯烷酮 用作溶剂,化学反应 21.5H,反应生成奥扎莫德
    参考文献: Improved Process For Preparing Ozanimod[fr] Procédé Amélioré Pour La Préparation D'Ozanimod
    标题: Improved Process For Preparing Ozanimod[fr] Procédé Amélioré Pour La Préparation D'Ozanimod
    摘要:所提出的发明涉及制备公式(1)的化合物或其盐的过程(即ozanimod):(1).该发明还涉及用于该过程的中间体.

    海关参考信息

    专利信息


    专利号:US-9388147-B2
    优先权日:2009-11-13
    标题 :Selective sphingosine 1 phosphate receptor modulators and methods of chiral synthesis
    发明人:MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TIMONY GREGG ALAN; BROOKS JENNIFER L; PEACH ROBERT; SCOTT FIONA LORRAINE; HANSON MICHAEL ALLEN
    权利人:RECEPTOS INC; CELGENE INTERNAT II SÃ?RL
    摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.

    专利号:WO-2019058290-A1
    优先权日:2017-09-20
    标 题 :IMPROVED PROCESS FOR THE PREPARATION OF AZANIMOD A-AMINO COMPOUND
    发明人:CHINNAPILLAI RAJENDIRAN; PERIYANDI NAGARAJAN; JASTI VENKATESWARALU
    权利人:SUVEN LIFE SCIENCES LTD; CHINNAPILLAI RAJENDIRAN; PERIYANDI NAGARAJAN; JASTI VENKATESWARALU
    摘要:The present invention relates to an improved process for the preparation of an optically active chiral amino compound. The present invention relates in particular to an improved process for the preparation of (S) -1-amino-2,3-dihydro-1H-indene-4-carbonitrile, an important intermediate for the synthesis of ozanimod. The present invention relates more particularly to the preparation of (S) -1-amino-2,3-dihydro-1H-indene-4-carbonitrile using 4-cyano-1-indanone and alpha-methylbenzylamine derivatives. as raw materials. The present invention particularly relates to the preparation of (S) -1-amino-2,3-dihydro-1H-indene-4-carbonitrile comprising a synthesis of diastereoselective chiral amine by protection with chiral auxiliary ï?¡-methyl benzylamine derivatives followed reduction and debenzylation.

    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:AR-116479-A1
    优先权日:2018-09-25
    标题:INTERMEDIARIES FOR THE SYNTHESIS OF OZANIMOD AND PROCEDURE FOR THE PREPARATION OF THE MENTIONED SPHINGOSINE-1-PHOSPHATE RECEPTOR AGONIST AND SUCH INTERMEDIARIES

    专利号:BR-122018077504-B1
    优先权日:2009-11-13
    标题 :METHODS FOR SYNTHESIS OF SELECTIVE SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS

    专利号:US-2023119606-A1
    优先权日:2020-02-18
    标 题:Immune cell modulators
    发明人:SHERDEN NATHANIEL; YU SHEN; STONER ISAAC
    权利人:OCTAGON THERAPEUTICS INC
    摘要:Disclosed are immune cell-selective small molecule compounds that modulate certain immune cell-specific receptors and enzymes, and methods of their synthesis and use to treat proliferative disorders.

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    📌 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: Regueiro M, Siegmund B, Horst S, Moslin R, Charles L, Petersen A, Tatosian D, Wu H, Lawlor G, Fischer M, D'Haens G, Colombel JF. Concomitant Administration of Ozanimod and Serotonergic Antidepressants in Patients With Ulcerative Colitis or Relapsing Multiple Sclerosis. Inflamm Bowel Dis. 2024 Jul
    17:izae136. doi: 10.1093/ibd/izae136. Epub ahead of print.
    200:106845. doi: 10.1016/j.ejps.2024.106845. Epub 2024 Jul 5.
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