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-2024368164-A1 优先权日:2021-04-28 标 题 :Purine nucleosides, their intermediates, and methods of preparation thereof 发明人:RAVI RAMA SURESH; JACOBSON KENNETH A; POE RUSSELL BIRCH 权利人:ASTROCYLE PHARMACEUTICALS INC; US HEALTH 摘要:The present invention provides purine nucleoside analog compounds and methods of use thereof for treatment of certain injuries, disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries. The present invention further provides methods of synthesizing such compounds, and intermediates useful in the synthesis of such compounds.
专利号:US-12295961-B2 优先权日:2009-12-31 标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols 发明人:DHINGRA OM 权利人:MARIUS PHARMACEUTICALS INC 摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
1: Agatonovic-Kustrin S, Zivanovic LJ. Spectrophotometric study of polythiazide-palladium (II) complex. J Pharm Biomed Anal. 1989;7(12):1559-64. doi: 10.1208/s12248-012-9449-z. Epub 2013 Jan 5. 6: Gordon AJ, Woeltjen AE. Treatment of Essential hypertension with single daily doses of a prazosin-polythiazide combination: a multicentre study with Minizide. J Int Med Res. 1981;9(5):303-8. Polish.
合成参考文献
参考文献:10.1007/s00216-010-3484-3 摘要:Peters RJB, Oosterink JE, Stolker AAM, Georgakopoulos C, Nielen MWF. Generic sample preparation combined with high-resolution liquid chromatography–time-of-flight mass spectrometry for unification of urine screening in doping-control laboratories. Analytical and Bioanalytical Chemistry. 2010 Feb 16;396(7):2583–98. doi: 10.1007/s00216-010-3484-3. 参考文献:10.3275/7862 摘要:Pedrazzoni M, Girasole G, Giusti A, Barone A, Pioli G, Passeri G, Palummeri E, Bianchi G. Assessment of the 10-year risk of fracture in Italian postmenopausal women using FRAX®: A north Italian multicenter study. Journal of Endocrinological Investigation. 2011 Jul 12;34(11):e386–91. doi: 10.3275/7862. 参考文献:10.1186/1475-2840-10-63 摘要:Biteker M, Dayan A, Can MM, İlhan E, Biteker FS, Tekkeşin A, Duman D. Impaired fasting glucose is associated with increased perioperative cardiovascular event rates in patients undergoing major non-cardiothoracic surgery. Cardiovascular Diabetology. 2011 Jul 14;10(1):63. doi: 10.1186/1475-2840-10-63. 参考文献:10.1007/s10552-011-9819-3 摘要:Kemppainen KJ, Tammela TL, Auvinen A, Murtola TJ. The association between antihypertensive drug use and incidence of prostate cancer in Finland: a population-based case-control study. Cancer Causes Control. 2011 Oct;22(10):1445–52. doi: 10.1007/s10552-011-9819-3. 参考文献:10.1186/1471-2407-11-304 摘要:Sadanandam A, Futakuchi M, Lyssiotis CA, Gibb WJ, Singh RK. A cross-species analysis of a mouse model of breast cancer-specific osteolysis and human bone metastases using gene expression profiling. BMC Cancer. 2011 Jul 20;11():304.