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:EP-1532112-B1 优先权日:2002-07-19 标 题 :Process for the preparation of modification i of n-(1-methylethylaminocarbonyl)-4-(3-methylphenylamino)-3-pyridinesulfonamide 发明人:FILIC DARKO; DUMIC MILJENKO; DANILOVSKI ALEKSANDAR; KLEPIC BOZENA; FISTRIC INES; MARINKOVIC MARINA; HORVAT-MIKULCIC JASNA 权利人:PLIVA HRVATSKA D O O 摘要:The invention relates to a new process for the preparation of modification I of torasemide by precipitation with acids from an alkaline extract of the original reaction mixture of the last phase in the synthesis of torasemide.
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: Geng H, Li B, Song X, Xia Y, Zhou X, Gao J, Chen L. 抑制NKCC1/AQP4通路对改善高原脑水肿大鼠神经损伤的作用 [Effects of Inhibiting the NKCC1/AQP4 Pathway on Neurological Injury Improvement in a Rat Model of High-Altitude Cerebral Edema]. Sichuan Da Xue Xue Bao Yi Xue Ban. 2025 Jan 20;56(1):156-165. Chinese. doi: 10.12182/20250160204. 2: Parkhill M, Salmaso N, D'Angiulli A, Lee V, Aguilar-Valles A. Emerging autism and Fragile X syndrome treatments. Trends Pharmacol Sci. 2025 Mar 17:S0165-6147(25)00024-0. doi: 10.1016/j.tips.2025.02.004. Epub ahead of print. 26(1):63. doi: 10.1186/s40360-025-00890-7. 22(1):80. doi: 10.1186/s12974-025-03407-5.
合成参考文献
参考文献:10.1113/expphysiol.2009.051102 摘要:Flores CA, Cid LP, Sepúlveda FV. Strain-dependent differences in electrogenic secretion of electrolytes across mouse colon epithelium. Exp Physiol. 2010 Jun;95(6):686–98. doi: 10.1113/expphysiol.2009.051102. 参考文献:10.1523/jneurosci.0068-11.2011 摘要:Bos R, Brocard F, Vinay L. Primary Afferent Terminals Acting as Excitatory Interneurons Contribute to Spontaneous Motor Activities in the Immature Spinal Cord. Journal of Neuroscience. 2011 Jul 13;31(28):10184–8. doi: 10.1523/jneurosci.0068-11.2011. 参考文献:10.1371/journal.pone.0021901 摘要:Bergeron MJ, Boggavarapu R, Meury M, Ucurum Z, Caron L, Isenring P, Hediger MA, Fotiadis D. Frog Oocytes to Unveil the Structure and Supramolecular Organization of Human Transport Proteins. PLoS ONE. 2011 Jul 07;6(7):e21901. doi: 10.1371/journal.pone.0021901. 参考文献:10.1007/s11606-011-1785-7 摘要:Erickson B, Dhaliwal G, Henderson MC, Amsterdam E, Rencic J. Effusive Reasoning. Journal of General Internal Medicine. 2011 Jul 15;26(10):1204. doi: 10.1007/s11606-011-1785-7. 参考文献:10.1016/j.ejphar.2011.06.052 摘要:Collins D, Kopic S, Geibel JP, Hogan AM, Medani M, Baird AW, Winter DC. The flavonone naringenin inhibits chloride secretion in isolated colonic epithelia. Eur J Pharmacol. 2011 Oct 01;668(1-2):271–7. doi: 10.1016/j.ejphar.2011.06.052.