CAS: 96020-91-6; 2,5-Diamino-2-(Difluoromethyl)Pentanoic Acid Hydrochloride Hydrate

该化合物是可应用于皮肤学的奥尼特脱碳箱酶的强效抑制剂. 它提供高纯度和稳定性,适合药物配方. 它在抑制发型增长方面的效力及其将副作用降到最低的能力有助于其临床用途.

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欧盟法规

C&L通报REACH预注册

合成工艺路线路线简述

  • 875924-42-8 = 96020-91-6
    反应条件:1.1 Reagents: Lithium Bis(Trimethylsilyl)Amide Solvents: 2-Methyltetrahydrofuran,Tetrahydrofuran; -30 °C; 4 H,12 - 15 Bar,160 °C; 3.5 H,160 °C1.2 Reagents: Triethylamine Solvents: Water; Ph 4
    标题:Method For Preparation Of Difluoromethylornithine
    参考文献:World Intellectual Property Organization]

    = 96020-91-6
    反应条件:1.1 Reagents: Sodium Nitrite,Hydrochloric Acid
    标题:Preparation Of Dialkyl 2-Difluoromethyl-2-(2-Cyanoethyl)Malonates And Their Use In Synthesis Of D,L-α-(Difluoromethyl)Ornithine
    参考文献:Switzerland
3-(Difluoromethyl)-2-Oxopiperidine-3-Carbohydrazide,Sodium Nitrite,盐酸 以49%的收率获得产物
参考文献:Mettler,Hanspeter;Greth,Erich
标题:Mettler,Hanspeter;Greth,Erich

海关参考信息

专利信息


专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:US-2008214827-A1
优先权日:2004-02-03
标 题:Synthesis of Cyanoimino-Benzoimidazoles
发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
权利人:EURO CELTIQUE SA
摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

专利号:US-7273888-B2
优先权日:2001-11-16
标题 :Use of difluoromethylornithine (DFMO) for the treatment of amyotrophic lateral sclerosis
发明人:RAMESH TENNORE; SCOTT SEAN
权利人:ALS THERAPY DEV FOUNDATION INC
摘要:The present invention provides methods and compositions for modulating polyamine pathway activity as a means for ameliorating neurodegenarative disorders. In particular, for ameliorating the symptoms or onset of amyotrophic lateral sclerosis (ALS) by modulating the gene and protein products involved the polyamine pathway, such as by inhibiting the enzyme, ornithine decarboxylase (ODC), involved in the synthesis of the polyamine, putrescine. Compositions and methods are disclosed for inhibiting the polyamine pathway producing lower polyamine levels resulting in a beneficial effect on ALS. This can be accomplished by using modulating agents such as analogs, or polyamine analogs, and antiproliferative drugs. In particular, the ODC inhibitor difuoromethylornithine (DFMO) is disclosed as a useful pharmacological agent in the modulation and treatment of ALS. Screening assays for pharmacological agents that are capable of decreasing polyamine levels and/or reducing cell proliferation are also disclosed.

专利号:US-9220714-B2
优先权日:2006-03-16
标 题 :Nitrofuran compounds for the treatment of cancer and angiogenesis
发明人:SAULNIER SHOLLER GISELLE L; SWAMY NARASIMHA; KALKUNTE STAYAN; SINGH RAKESH K; BRARD LAURENT; KIM KYU KWANG
权利人:WOMEN AND INFANTS HOSPITAL OF RHODE ISLAND; UNIV BROWN; WOMEN AND INFANTS HOSPITAL RHODE ISLAND
摘要:The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.

专利号:US-2020150125-A1
优先权日:2017-03-12
标 题:Methods of diagnosing and prognosing cancer
发明人:EREZ AYELET
权利人:YEDA RES & DEV
摘要:Methods of diagnosing cancer are provided. Accordingly there is provided a method of diagnosing cancer in a subject, the method comprising determining a level of urea and/or a pyrimidine synthesis metabolite in a biological sample of the subject, wherein a level of urea below a predetermined threshold; and/or a said level of pyrimidine synthesis metabolite above a predetermined threshold; is indicative of cancer. Also provided are methods of prognosing and treating cancer.

专利号:US-2015352230-A1
优先权日:2013-01-11
标 题:Synthesis and isolation of dendrimer based imaging systems
发明人:MULLEN DOUGLAS GURNETT; BAKER JR JAMES R; BANASZAK HOLL MARK M; HUANG BAOHUA; DOUGHERTY CASEY; BALL JACK
权利人:UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis and isolation of antibodies conjugated with modular dendrimer nanoparticles. In particular, the present invention is directed to antibodies conjugated with novel modular dendrimer nanoparticles having precise numbers of imaging agents, methods of synthesizing the same, compositions comprising such antibodies conjugated with such modular dendrimer nanoparticles, as well as systems and methods utilizing the conjugates (e.g., in imaging settings) (e.g., in diagnostic and/or therapeutic settings) (e.g., for the delivery of therapeutics, imaging, and/or targeting agents).
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主要参考文献


1: Cloete TT, Johansson CC, N'Da DD, Vodnala SK, Rottenberg ME, Breytenbach JC, Ashton M. Mono-, di- and trisubstituted derivatives of eflornithine: synthesis for in vivo delivery of DL-alpha-difluoromethylornithine in plasma. Arzneimittelforschung. 2011;61(5):317-25.
4: Baker N, Alsford S, Horn D. Genome-wide RNAi screens in African trypanosomes identify the nifurtimox activator NTR and the eflornithine transporter AAT6. Mol Biochem Parasitol. 2011 Mar;176(1):55-7. Epub 2010 Nov 18.
5: Zell JA, McLaren CE, Chen WP, Thompson PA, Gerner EW, Meyskens FL. Ornithine decarboxylase-1 polymorphism, chemoprevention with eflornithine and sulindac, and outcomes among colorectal adenoma patients. J Natl Cancer Inst. 2010 Oct 6;102(19):1513-6. Epub 2010 Aug 26.

合成参考文献


参考文献:10.1007/978-3-030-14358-9_5
摘要:Paschou SA, Goulis DG, Tarlatzis BC. Polycystic Ovary Syndrome. 2019. In: ISGE Series.
参考文献:10.1007/bf00203544
摘要:Griffin CA, Slavik M, Chien SC, Hermann J, Thompson G, Blanc O, Luk GD, Baylin SB, Abeloff MD. Phase I trial and pharmacokinetic study of intravenous and oral alpha-difluoromethylornithine. Invest New Drugs. 1987;5(2):177–86. doi: 10.1007/bf00203544.
参考文献:10.1007/978-3-662-58897-0_21
参考文献:10.1007/978-3-030-46391-5_14
摘要:Shoupe D. Choosing the Right Contraceptive. 2020. In: The Handbook of Contraception.
参考文献:10.1007/978-3-030-16115-6_4
摘要:Williams L. Adolescent Gynaecology. 2019. In: Nursing Management of Women’s Health.
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