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-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-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-2008227851-A1 优先权日:2007-03-12 标题 :Laulimalide and laulimalide analogs 发明人:WENDER PAUL A 权利人:WENDER PAUL A 摘要:Novel laulimalide analogs, methods for the treatment of proliferative disease and processes for the synthesis of laulimalide and novel laulimalide analogs are described.
专利号:US-10814013-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
1: el Walily AF. Simultaneous determination of the binary mixture of nifedipine and mefruside using derivate spectroscopy, capillary gas-liquid chromatography and high performance liquid chromatography. Acta Pharm Hung. 1997 Mar-May;67(2-3):89-97. German. 6: Schulte KL, Meyer-Sabellek W, Röcker L, Gotzen R, Distler A. Effects of diltiazem alone and combined with mefruside on cardiovascular response at rest and during exercise, carbohydrate metabolism and serum lipoproteins in patients with systemic hypertension. Am J Cardiol. 1987 Oct 1;60(10):826-31. Japanese. doi: 10.1023/A:1016320831469. Italian. 14: Tomasi AM, Pirani R, Masoni C. [Treatment of idiopathic hypertension with guanabenz-mefruside]. Minerva Cardioangiol. 1984 May;32(5):339-44. Italian. Italian.
合成参考文献
摘要:Iyakuhin Kenkyu. Study of Medical Supplies., 6(386), 1975 摘要:Kiso to Rinsho. Clinical Report., 7(1003), 1973 摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664 参考文献:10.1007/bf00561678 摘要:Fleuren HLJ, Verwey-van Wissen CPW, van Rossum JM. Pharmacokinetics of mefruside and two active metabolites in man. European Journal of Clinical Pharmacology. 1980 Jan;17(1):59–69. doi: 10.1007/bf00561678. 参考文献:10.1002/dta.1867 摘要:Cawley AT, Smart C, Greer C, Liu Lau M, Keledjian J. Detection of the selective androgen receptor modulator andarine (S-4) in a routine equine blood doping control sample. Drug Test Anal. 2016 Feb;8(2):257–61. doi: 10.1002/dta.1867.