CAS: 104206-65-7; 2-(2-Nitro-4-(Trifluoromethyl)Benzoyl)Cyclohexane-1,3-Dione

该化合物是一种合成有机化合物,主要用于治疗遗传性强血糖1型,一种影响氨基酸乙酰胺新陈代谢的稀有遗传障碍;它作为酶4-氢氧苯基苯丙酯二氧基genase的强大抑制剂,对乙基苯丙酮的代谢酶在乙型苯丙胺的代谢途径中至关重要;抑制这种酶,硝基辛酮有效减少与该病有关的有毒代谢物的累积;该化合物一般是口服的,其特点是水溶性较低,影响其配制和投送;硝基辛酮一般具有良好的缓解作用,尽管它可能具有副作用,包括潜在的肝毒性和某些代谢物水平的变化;其发展大大改进了对乙基苯基胺的管理,使病人能够保持更好的生活质量;与任何药物,监测和剂量调整对于优化治疗结果,同时尽量减少不利影响至关重要.

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上下游产品

2-硝基-4-三氟甲基苯甲酸 2-Nitro-4-Trifluoromethylbenzoic Acid 320-94-5
2-硝基-4-(三氟甲基)苯甲酰氯 2-Nitro-4-Trifluoromethyl-Benzoyl Chloride 81108-81-8

合成工艺路线路线简述

    2-硝基-4-三氟甲基苯甲酸置于草酰氯,三甲基氰硅烷,三乙胺,N,N-二甲基甲酰胺体系中,用 二氯甲烷 用作溶剂,化学反应 2.33H,反应生成尼替西农
    参考文献: Pharmaceutical Composition[fr] Composition Pharmaceutique
    标题: Pharmaceutical Composition[fr] Composition Pharmaceutique
    摘要:本发明涉及口服药物组成物,包括尼替酮或其药学上可接受的盐,它们在酪氨酸血症的治疗中的使用,例如遗传性酪氨酸血症1型(ht-1)或黑酸尿症.该组成物具有改善的稳定性特征.本发明还涉及生产尼替酮的过程.

    专利信息


    专利号:US-12234495-B2
    优先权日:2021-04-06
    标 题:Synthesis of beta-hydroxyisovalerate and methods of use
    发明人:VEMURI GOUTHAM; LINDSAY CHRISTOPHER; ROBERG-PEREZ KEVIN; SNOW CHRISTOPHER D; CAMERON ELIZABETH A
    权利人:SASYA INC
    摘要:The biological production of beta-hydroxyisovalerate (βHIV) using at least one non-natural enzyme. The non-natural enzyme for the biologically-derived βHIV provides more beta-hydroxyisovalerate synthase activity than the wild-type parent. The non-natural enzyme having one or more modifications of substrate-specificity positions. The non-natural enzyme can be expressed in a microorganism, such as a yeast or bacteria, wherein the microorganism comprises an active βHIV metabolic pathway for the production of βHIV. Alternatively, the non-natural enzyme can be a βHIV synthase used to produce βHIV in a cell-free environment. The biological derivation of βHIV eliminates toxic by-products and impurities that result from the chemical production of βHIV, such that βHIV produced by a non-natural enzyme prior to any isolation or purification process has not been in substantial contact with any halogen-containing component.

    专利号:US-9783485-B1
    优先权日:2016-11-30
    标题:Crystalline inhibitor of 4-hydroxyphenylpyruvate dioxygenase, and a process of synthesis and crystallization thereof
    发明人:ATTOLINO EMANUELE
    权利人:DIPHARMA S A
    摘要:The present invention relates to an improved synthesis and crystallization process of the 4-hydroxyphenylpyruvate dioxygenase (HPPD) inhibitor 2-(2-nitro-4-trifluoromethylbenzoyl)-1,3-cyclohexanedione, also known as nitisinone or NTBC.

    专利号:US-2025002949-A1
    优先权日:2021-04-06
    标题:Synthesis of beta-hydroxyisovalerate and methods of use

    专利号:US-11920177-B2
    优先权日:2021-04-06
    标题 :Synthesis of beta-hydroxyisovalerate and methods of use

    专利号:US-2022315954-A1
    优先权日:2021-04-06
    标 题 :Synthesis of beta-hydroxyisovalerate and methods of use

    专利号:US-2022325304-A1
    优先权日:2021-04-06
    标 题:Synthesis of beta-hydroxyisovalerate and methods of use
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    主要参考文献


    1: Souri E, Lahiji FR, Nourhashemi T, Jalalizadeh H. A Stability Indicating HPLC Method for the Determination of Nitisinone in Capsules. Indian J Pharm Sci. 2015 May-Jun;77(3):348-51.
    2: Simoncelli M, Samson J, Bussières JF, Lacroix J, Dorais M, Battista R, Perreault S. Cost-Consequence Analysis of Nitisinone for Treatment of Tyrosinemia Type I. Can J Hosp Pharm. 2015 May-Jun;68(3):210-7.
    3: Mistry JB, Jackson DJ, Bukhari M, Taylor AM. Osteoarticular cells tolerate short-term exposure to nitisinone-implications in alkaptonuria. Clin Rheumatol. 2015 May 31. [Epub ahead of print] doi: 10.1007/8904_2015_437. Epub 2015 May 5.

    合成参考文献


    参考文献:10.1111/j.1469-8749.2011.04048.x
    摘要:De Laet C, Munoz VT, Jaeken J, François B, Carton D, Sokal EM, Dan B, Goyens PJ. Neuropsychological outcome of NTBC-treated patients with tyrosinaemia type 1. Dev Med Child Neurol. 2011 Oct;53(10):962–4. doi: 10.1111/j.1469-8749.2011.04048.x.
    参考文献:10.1007/s10545-011-9374-9
    摘要:Ranganath LR, Cox TF. Natural history of alkaptonuria revisited: analyses based on scoring systems. J Inherit Metab Dis. 2011 Dec;34(6):1141–51. doi: 10.1007/s10545-011-9374-9.
    参考文献:10.1111/j.1442-200x.2011.03427.x
    摘要:Couce ML, Dalmau J, del Toro M, Pintos-Morell G, Aldámiz-Echevarría L; Spanish Working Group on Tyrosinemia type 1. Tyrosinemia type 1 in Spain: mutational analysis, treatment and long-term outcome. Pediatr Int. 2011 Dec;53(6):985–9. doi: 10.1111/j.1442-200x.2011.03427.x.
    参考文献:10.1371/journal.pbio.1001099
    摘要:Wu G, Liu N, Rittelmeyer I, Sharma AD, Sgodda M, Zaehres H, Bleidißel M, Greber B, Gentile L, Han DW, Rudolph C, Steinemann D, Schambach A, Ott M, Schöler HR, Cantz T. Generation of Healthy Mice from Gene-Corrected Disease-Specific Induced Pluripotent Stem Cells. PLoS Biol. 2011 Jul 12;9(7):e1001099. doi: 10.1371/journal.pbio.1001099.
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