CAS: 82964-04-3; N-(6-Methoxy-5-(Trifluoromethyl)Naphthalene-1-Carbonothioyl)-N-Methylglycine

该化合物是一个化学化合物,主要因其作为抗艾剂还原酶抑制剂的作用而得到承认,在糖尿病并发症的管理中具有重要作用,其特点是它能够抑制酶(艾氏剂再生酶),从而减少将甘蔗糖转化成沙洛醇,这是一个涉及糖尿病...

结构式图片

上下游产品

tolrestat methyl ester 6-methoxy-1-naphthalenecarboxylic acid methyl ester 5-Methyl-2-methoxy-1-(trifluoromethyl)naphthalene 6-methoxy-5-(trifluoromethyl)-1-naphthalenecarboxylic acid6-methoxy-5-(trifluoromethyl)-1-naphthalenecarboxylic acid 5-(Carboxymethyl-methyl-carbamoyl)-2-methoxy-naphthalene-1-carboxylic acid -thiomethyl-N-methylglycineN-(5-carboxyl)-6-methoxy-1-naphtalenyl-thiomethyl-N-methylglycine oxomethyl>-N-methylglycineN-6-methoxy-5-(trifluoromethyl)-1-naphthalenyloxomethyl-N-methylglycine

合成工艺路线路线简述

    6-Methoxy-5-(Trifluoromethyl)-1-Naphthalenecarboxylic Acid Chloride置于氢氧化钾,Tetraphosphorus Decasulfide体系中,化学反应生成 托瑞司他
    参考文献:N-[5-(三氟甲基)-6-甲氧基-1-萘基]硫代甲基]-N-甲基甘氨酸(tolrestat),一种有效的口服醛糖还原酶抑制剂.
    标题:N-[5-(三氟甲基)-6-甲氧基-1-萘基]硫代甲基]-N-甲基甘氨酸(tolrestat),一种有效的口服醛糖还原酶抑制剂.
    摘要:
    DOI:10.1021/jm00369A003

    海关参考信息

    专利信息


    专利号:US-10005720-B2
    优先权日:2013-04-05
    标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
    发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
    权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
    摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

    专利号:US-6495710-B2
    优先权日:2000-01-14
    标题:Synthesis and use of dimethyl 1,5-naphthalenedicarboxlyates and intermediates therefrom
    发明人:MACEK JOHN A; ROSEN BRUCE I; HOLZHAUER JUERGEN K; BRAMLET JOHN S; LILLWITZ LARRY D; SCHNEIDER DAVID J; LANG LAWRENCE L; PASCHKE EDWARD E; WEIS JOHN M; VISWANATH YENAMANDRA; SAKELLARIDES STEFANOS L
    权利人:BP CORP NORTH AMERICA INC
    摘要:The synthesis of dimethyl-1,5-naphthalenedicarboxylate and polymers and articles formed therefrom is disclosed, as well as applications for dimethyl-1,5-naphthalenedicarboxylate, its corresponding acid 1,5-NDA, and various synthesis intermediates.

    专利号:US-2005004225-A1
    优先权日:2003-04-16
    标题:Oxidoreductase inhibitors and methods of screening and using thereof
    发明人:BALENDIRAN GANESARATNAM K
    摘要:The present invention relates to 1) the design and synthesis of analogs to glutathione conjugates which bind to or interact with aldose reductase (AR) through unique conformations that are distinctly different from the substrates and inhibitors of AR which are members of sugar metabolism; 2) the screening of the analogs to identify those that interact with or inhibit or enhance the activity of AR; and 3) the use of AR ligands, AR inhibitors (AR antagonsits) or AR enhancer (AR agonists) in the detection of AR activity, the modulation of AR activity, and the treatment of conditions in a subject in need of modulating AR activity. Such conditions include but not limited to cardiovascular disease, diabetes, artheriosclerosis, cancer, neoplasm, obesity, cataract, retinopathy, keratopathy, nephropathy, neurosis, thrombosis, faulty union of corneal injury and neuropathy. Examples of the treatment include the use of fibrates as AR inhibitors to treat these conditions.

    专利号:US-2025223262-A1
    优先权日:2022-03-31
    标 题 :Synthesis of morphinans with reduced herg activity and mop binding
    发明人:LAMMERT ECKHARD; SCHOLZ OKKA; OTTER SILKE; HEREBIAN DIRAN; HOFFMANN TORSTEN; SANZ MIGUEL ANGEL; KRAMP LAURENZ; LEVY LAURA MARIANA; HRISTEVA STANIMIRA
    权利人:HEINRICH HEINE UNIV DUESSELDORF; DEUTSCHE DIABETES FORSCHUNGSGESELLSCHAFT E V; TAROS CHEMICALS GMBH & CO KG
    摘要:The invention relates to morphinan-derivatives, processes for their preparation, medicaments containing them and the use of these morphinan-derivatives for the preparation of medicaments.

    专利号:US-2018370905-A1
    优先权日:2013-04-05
    标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same

    专利号:US-9018249-B2
    优先权日:2011-09-13
    标题 :SGLT inhibitors
    发明人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR
    权利人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR; PANACEA BIOTEC LTD
    摘要:The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of Formula I and methods of treating or preventing one or more conditions or diseases that may be regulated or normalized via inhibition of Sodium Glucose Cotransporter-2 (SGLT-2).
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    主要参考文献


    1: Santiago JV, Snksen PH, Boulton AJ, Macleod A, Beg M, Bochenek W, Graepel GJ, Gonen B. Withdrawal of the aldose reductase inhibitor tolrestat in patients with diabetic neuropathy: effect on nerve function. The Tolrestat Study Group. J Diabetes Complications. 1993 Jul-Sep;7(3):170-8. Review. Italian.

    合成参考文献


    参考文献:10.1007/bf00403909|10.1007/s001250050531
    摘要:Forster HG, ter Wee PM, Hohman TC, Epstein M. Impairment of afferent arteriolar myogenic responsiveness in the galactose-fed rat is prevented by tolrestat. Diabetologia. 1996 Aug;39(8):907–14. doi: 10.1007/bf00403909.
    参考文献:10.1016/0022-510x(96)00136-0
    摘要:Brett FM, Kalichman MW, Calcutt NA, Mizisin AP. Effects of seven days of galactose feeding and aldose reductase inhibition on mast cells and vessel morphometry in rat sciatic nerve. Journal of the Neurological Sciences. 1996 Sep;141(1-2):6–12. doi: 10.1016/0022-510x(96)00136-0.
    参考文献:10.1139/o96-038
    摘要:Donnelly SM, Zhou XP, Huang JT, Whiteside CI. Prevention of early glomerulopathy with tolrestat in the streptozotocin-induced diabetic rat. Biochem Cell Biol. 1996;74(3):355–62. doi: 10.1139/o96-038.
    参考文献:10.2337/diacare.19.10.1091
    摘要:Nicolucci A, Carinci F, Graepel JG, Hohman TC, Ferris F, Lachin JM. The efficacy of tolrestat in the treatment of diabetic peripheral neuropathy. A meta-analysis of individual patient data. Diabetes Care. 1996 Oct;19(10):1091–6. doi: 10.2337/diacare.19.10.1091.
    参考文献:10.3317/jraas.2000.021
    摘要:Wu XH, Chen X, Zhang SL, Pang L, To C, Wang TT, Hohman TC, Filep JG, Chan JS. Molecular mechanism(s) of insulin action on the expression of the angiotensinogen gene in kidney proximal tubular cells. J Renin Angiotensin Aldosterone Syst. 2000 Jun;1(2):166–74. doi: 10.3317/jraas.2000.021.
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