专利号:US-12208146-B2 优先权日:2018-11-19 标 题 :Reconstituted HDL nanoparticles for delivery of radioactive agents and uses thereof 发明人:LACKO ANDRAS G; PROKAI LASZLO; ISAAC-OLIVÉ KEILA 权利人:UNIV OF NORTH TEXAS HEALTH SCIENCE CENTER; THE AUTONOMOUS UNIV OF THE STATE OF MEXICO 摘要:Despite the widespread use of nanotechnology in radio-imaging applications, lipoprotein based delivery systems received only limited attention so far. The subject application provides for the synthesis of a novel hydrophobic radio-imaging tracer. This tracer, comprising a hydrazinonicotinic acid (HYNIC)-N-dodecylamide and 99mTc conjugate can be encapsulated into rHDL nanoparticles (NPs). These rHDL NPs can selectively target the Scavenger Receptor type B1 (SR-B1) that is overexpressed on most cancer cells due to excess demand for cholesterol for membrane biogenesis and thus can target tumors in-vivo. Details of the tracer synthesis, characterization of rHDL/tracer complex, in-vitro uptake, stability studies and in-vivo application of this new radio-imaging approach are provided.
专利号:US-8686157-B2 优先权日:2003-02-10 标题:Processes for the facile synthesis of diaryl amines and analogues thereof 发明人:SNOONIAN JOHN R; OLIVER-SHAFFER PATRICIA ANN 权利人:SNOONIAN JOHN R; OLIVER-SHAFFER PATRICIA ANN; VERTEX PHARMA 摘要:The present invention relates to processes for the facile synthesis of diaryl amines and analogues thereof. The processes of the present invention produce diaryl amines in high yield and purity. The present invention also relates to intermediates useful in the process of the present invention.
专利号:US-8742118-B2 优先权日:2011-10-27 标题 :Methods for preparing intermediates of perampanel 发明人:FONTANA FRANCESCO; STABILE PAOLO 权利人:F I S —FABBRICA ITALIANA SINT S P A 摘要:Methods for the synthesis of 2-alkoxy-5-(pyridin-2-yl)pyridine of formula I n nor salts thereof are provided.
专利号:US-7151112-B1 优先权日:2001-09-04 标题:Pharmaceutical uses and synthesis of nicotinamides 发明人:CUTSHALL NEIL S; JEFFREY SCOTT C 权利人:UCB SA 摘要:This invention is directed to methods of using a compound of the formula n nand pharmaceutically acceptable salts thereof, wherein n, X, R 1 and R 2 are disclosed herein, for treating inflammatory events in an animal subject.
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-6090810-A 优先权日:1995-09-01 标题:Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities 发明人:KLEIN ELLIOTT S; JOHNSON ALAN T; STANDEVEN ANDREW M; BEARD RICHARD L; GILLETT SAMUEL J; DUONG TIEN T; NAGPAL SUNIL; VULIGONDA VIDYASAGAR; TENG MIN; CHANDRARATNA ROSHANTHA A 权利人:ALLERGAN SALES INC 摘要:Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.
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合成参考文献
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