📜邻羟基苯甲腈置于哌啶,Sodium Hydroxide体系中,用 四氢呋喃 作为反应溶剂,化学反应 1.17H,反应生成 布新洛尔 参考文献:Antihypertensive Indole Derivatives Of Phenoxypropanolamines With .Beta.-Adrenergic Receptor Antagonist And Vasodilating Activity 标题:Antihypertensive Indole Derivatives Of Phenoxypropanolamines With .Beta.-Adrenergic Receptor Antagonist And Vasodilating Activity 摘要:A Series Of 25 Aryloxypropanolamines Containing The 3-Indolyl-Tert-Butyl [i.E.,1,1-Dimethyl-2-(1H-Indol-3-yl)Ethyl] Or Substituted 3-Indolyl-Tert-Butyl Moiety As The N Substituent Is Reported. These Compounds Have Been Tested For Antihypertensive Activity In Spontaneously Hypertensive Rats (Shr),Beta-Adrenergic Receptor Antagonist Action In Conscious Normotensive Rats,Vasodilating Activity In Ganglion-Blocked Rats With Blood Pressure Maintained By Angiotensin Ii Infusion,And For Intrinsic Sympathomimetic Action (Isa) In Reserpinized Rats. Some Of The Compounds Exhibit Antihypertensive Activity In Combination With Beta Adrenergic Receptor Antagonist And Vasodilating Action. The Structure--Activity Relationships In These Tests Are Discussed. DOI:10.1021/jm00177A015
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-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-11434195-B2 优先权日:2017-07-20 标题:Compositions and methods for treatment of central nervous system tumors 发明人:SVETLOV STANISLAV IGOREVICH 权利人:UNIV FLORIDA 摘要:Compounds, pharmaceutical compositions, and methods for treating cancer, in particular brain cancer, are provided, including amphiphilic fatty acid/alcohol ethers (AIPs) comprising endocannabinoid and FABP motifs covalently linked to a beta-adrenoreceptor antagonist motif in one molecule. The invention includes methods for inhibiting growth of brain cancer cells by contacting the compound(s) with brain cancer cells. The invention provides a method for treating both brain cancer and brain cancer metastases, and for suppression of regrowth of brain cancer cells after radiation, surgical treatment, or chemotherapy of brain cancer. The invention also comprises an optimized chemical synthesis of the AIP compounds and methods of using the compounds, alone or in combination with another agent, for suppressing the growth of brain cancer cells, and enhancing survival of normal CNS cells, or improving recuperation from radiation, surgical or chemotherapy.
专利号:US-8017776-B2 优先权日:2003-07-15 标题 :Methods for synthesis of acyloxyalkyl compounds 发明人:BHAT LAXMINARAYAN; GALLOP MARK A 权利人:XENOPORT INC 摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
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.
专利号:US-9556123-B2 优先权日:2004-07-19 标题:Synthesis of triethylenetetramines 发明人:JONAS MARCO; VAULONT IRENE; SOI ANTONIO; SCHMIDT GUNTHER 权利人:PHILERA NEW ZEALAND LTD 摘要:Methods and intermediates for synthesizing triethylenetetramine and salts thereof, as well as novel triethylenetetramine salts and their crystal structure, and triethylenetetramine salts of high purity.
1: Black-Maier E, Steinberg BA, Piccini JP. Bucindolol hydrochloride in atrial fibrillation and concomitant heart failure. Expert Rev Cardiovasc Ther. 2015 Jun;13(6):627-36. doi: 10.1586/14779072.2015.1031111. Epub 2015 May 11. 14(6):529-535. doi: 10.1007/s11897-017-0364-6. 47(5):347-51. doi: 10.1358/dot.2011.47.5.1579112. 13(4):473-481. doi: 10.1080/17425255.2017.1291631. Epub 2017 Feb 15. GENETIC-AF Trial Investigators. Bucindolol for the Maintenance of Sinus Rhythm in a Genotype-Defined HF Population: The GENETIC-AF Trial. JACC Heart Fail. 2019 Jul;7(7):586-598. doi: 10.1016/j.jchf.2019.04.004. Epub 2019 Apr 29. 6: Gill JS, Beevers DG. Bucindolol. Am J Cardiol. 1985 Oct 1;56(10):704. doi: 10.1016/0002-9149(85)91045-8. 798:57-65. doi: 10.1016/j.ejphar.2016.12.028. Epub 2016 Dec 21. Genotype-Directed Comparative Effectiveness Trial of Bucindolol and Toprol-XL for Prevention of Atrial Fibrillation/Atrial Flutter in Patients with Heart Failure Trial Investigators*. Bucindolol Decreases Atrial Fibrillation Burden in Patients With Heart Failure and the ADRB1 Arg389Arg Genotype. Circ Arrhythm Electrophysiol. 2021 Aug;14(8):e009591. doi: 10.1161/CIRCEP.120.009591. Epub 2021 Jul 16.
合成参考文献
摘要:European Patent Application., #0065295 参考文献:10.1016/s0146-2806(99)90007-5 摘要:Carson PE. Beta-blocker therapy in heart failure: pathophysiology and clinical results. Curr Probl Cardiol. 1999 Jul;24(7):421–60. doi: 10.1016/s0146-2806(99)90007-5. 参考文献:10.1007/s11886-002-0054-0 摘要:Yancy CW. The role of race in heart failure therapy. Curr Cardiol Rep. 2002 May;4(3):218–25. doi: 10.1007/s11886-002-0054-0. 参考文献:10.1080/17425255.2017.1291631 摘要:Rosa GM, Meliota G, Brunelli C, Ferrero S. Pharmacokinetic drug evaluation of bucindolol for the treatment of atrial fibrillation in heart failure patients. Expert Opinion on Drug Metabolism & Toxicology. 2017 Feb 15;13(4):473–81. doi: 10.1080/17425255.2017.1291631.