📜2,3-Dichlor-4-(2-Methylenbutyryl)Phenol 反应生成 利尿酸 参考文献:Process For Preparation Of Alpha-Aryloxy Acetic Acids And Their Salts 标题:Process For Preparation Of Alpha-Aryloxy Acetic Acids And Their Salts 摘要:一种生产芳氧基乙酸及其盐的方法,包括在无水有机溶剂中将具有r-Oh分子式的醇(其中r为芳基或取代芳基)与碱发生反应,形成芳氧基,然后去除有机溶剂,将芳氧基与一种偏极性无水溶剂(如dmso)中的一种单卤乙酸盐发生反应,形成相应的芳氧基乙酸盐,然后可以回收或可选择性地将芳氧基乙酸盐与酸接触转化为相应的酸.
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-10973847-B2 优先权日:2017-06-30 标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof 发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.
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-2008287407-A1 优先权日:2003-12-10 标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use 发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
专利号:US-7708989-B2 优先权日:1999-10-29 标题 :Methods of treating vascular diseases characterized by nitric oxide insufficiency 发明人:LOSCALZO JOSEPH; VITA JOSEPH A; LOBERG MICHAEL D; WORCEL MANUEL 权利人:NITROMED INC 摘要:The invention provides methods of treating and/or preventing vascular diseases characterized by nitric oxide insufficiency by administering a therapeutically effective amount of at least one nitrosated angiotensin-converting enzyme inhibitor, nitrosated beta-adrenergic blocker, nitrosated cholesterol reducer, nitrosated calcium channel blocker, nitrosated endothelin antagonist, nitrosated angiotensin II receptor antagonist, nitrosated renin inhibitor, and optionally at least one compound used to treat cardiovascular diseases and/or at least one antioxidant, or a pharmaceutically acceptable salt thereof, and/or at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The vascular diseases characterized by nitric oxide insufficiency include a cardiovascular disease and a disease resulting from oxidative stress.
专利号:WO-2017046598-A1 优先权日:2015-09-16 标题:Treatment of acute inflammatory disorders 发明人:CRISANTI ANDREA; CANAVESE MIRIAM 权利人:CRISANTI ANDREA; IMP INNOVATIONS LTD 摘要:The present invention relates to a VEGF receptor agonist for use in the treatment of an acute inflammatory disorder associated with the overproduction of pro-inflammatory cytokine, administered with an agent that induces the synthesis of Nrf2. The invention also relates to pharmaceutical combinations comprising a VEGF receptor agonist and an agent that induces the synthesis of Nrf2, and kits comprising these agents. The described uses, combinations and methods may prevent or reduce the dis-regulated activation of an inflammatory response and reduce endothelial damage.
1: Nguyen BD, Roarke MC, Young JR, Yang M, Osborn HH. Diuretic Renal Scintigraphy in Patients with Sulfonamide Allergies: Possible Alternative Use of Ethacrynic Acid. J Nucl Med Technol. 2015 Dec;43(4):239-41. doi: 10.2967/jnmt.115.161331. Epub 2015 Oct 15. doi: 10.1016/j.taap.2015.03.016. Epub 2015 Mar 25. doi: 10.1021/acs.inorgchem.5b00802. Epub 2015 Jun 15. doi: 10.1039/c4nr05983b. doi: 10.1186/s13054-014-0724-5. 8: Wang M, Gorasiya S, Antoine DJ, Sitapara RA, Wu W, Sharma L, Yang H, Ashby CR Jr, Vasudevan D, Zur M, Thomas DD, Mantell LL. The compromise of macrophage functions by hyperoxia is attenuated by ethacrynic acid via inhibition of NF-κB-mediated release of high-mobility group box-1. Am J Respir Cell Mol Biol. 2015 Feb;52(2):171-82. doi: 10.1165/rcmb.2013-0544OC. 9: Nagy T, Kovács V, Hardi P, Veres TG, Takács I, Jancsó G, Sinay L, Fazekas G, Pintér Ö, Arató E. Inhibition of Glutathione S-Transferase by Ethacrynic Acid Augments Ischemia-Reperfusion Damage and Apoptosis and Attenuates the Positive Effect of Ischemic Postconditioning in a Bilateral Acute Hindlimb Ischemia Rat Model. J Vasc Res. 2015;52(1):53-61. doi: 10.1159/000381984. Epub 2015 May 29. doi: 10.5863/1551-6776-19.1.49.
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