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-8884051-B2 优先权日:2010-10-20 标题:Synthesis of methylene malonates using rapid recovery in the presence of a heat transfer agent 发明人:MALOFSKY BERNARD M; MALOFSKY ADAM G; DEY TANMOY; SULLIVAN JEFFREY M; CHEN YANGBIN; WOJCIAK STANLEY C; COCKREM MICHAEL C 权利人:MALOFSKY BERNARD M; MALOFSKY ADAM G; DEY TANMOY; SULLIVAN JEFFREY M; CHEN YANGBIN; WOJCIAK STANLEY C; COCKREM MICHAEL C; BIOFORMIX INC 摘要:The present invention provides a method of making a methylene malonate monomer that includes the steps of reacting a malonic acid ester with a source of formaldehyde optionally in the presence of an acidic or basic catalyst and optionally in the presence of an acidic or non-acidic solvent to form reaction complex. The reaction is optionally performed in the presence of or contacted with an energy transfer means such as a heat transfer agent, a heat transfer surface, a source of radiation or a laser such that reaction complex is substantially vaporized to produce a vapor phase comprising methylene malonate monomer which may be isolated. The present invention further provides methylene malonate monomers prepared by the method of the invention, as well as compositions and products formed from the methylene malonate monomers, including monomer-based products (e.g., inks, adhesives, coatings, sealants or reactive molding) and polymer-based products (e.g., fibers, films, sheets, medical polymers, composite polymers and surfactants).
专利号:US-5449822-A 优先权日:1991-12-12 标题:Preparation of ethylenediaminetriacetic acid 发明人:PARKER BRIAN A; CULLEN BARRY A; GAUDETTE ROGER R 权利人:HAMPSHIRE CHEMICAL CORP 摘要:Synthesis of ethylenediaminetriacetic acid (ED3A) or its salts is disclosed. A salt of N,N'-ethylenediaminediacetic acid (ED2AH2) is condensed with formaldehyde to form a stable 5-membered ring intermediate. The addition of cyanide across this cyclic material forms ethylenediamine N,N'-diacetic acid-N'-cyanomethyl or salts thereof (mononitrile-diacid). The nitrile in aqueous solutions may be spontaneously cyclized to form 2-oxo-1,4-piperazinediacetic acid (3KP) or salts thereof, which is the desired cyclic intermediate. In the presence of excess base, salts of ED3A are formed in excellent yield and purity. Alternatively, the starting material is ED2AHaXb, where x is a base cation, e.g., an alkali or alkaline earth metal, a is 1 to 2, and b is 0 to 1 in aqueous solutions. The reaction mixture also can be acidified to ensure complete formation of carboxymethyl-2-oxopiperazine (the lactam) prior to the reaction. Formaldehyde is added, essentially resulting in the hydroxymethyl derivative. On the addition of a cyanide source, 1-cyanomethyl-4-carboxymethyl-2-ketopiperazine (mononitrile diacid) or a salt thereof is formed. Upon the addition of any suitable base or acid, this material may be hydrolyzed to 3KP. The addition of a base will open this ring structure to form the salt of ED3A.
专利号:US-9603928-B2 优先权日:2013-06-19 标题:Medicinal composition for promoting synthesis of protoporphyrin IX 发明人:ISHIZUKA MASAHIRO; OTO URARA; KAMIYA ATSUKO; TAKAHASHI KIWAMU; TANAKA TOHRU; OZAWA TOSHIYUKI; MORIMOTO KUNIYUKI; WATANABE KEITARO 权利人:SBI PHARMACEUTICALS CO LTD; UNIV OSAKA CITY 摘要:The object of the present invention is to elucidate the resistance mechanism in infections that show resistance to ALA-PDT that uses a single ALA, and to provide a novel treatment method against these infections. The present invention provides a pharmaceutical composition for promoting protoporphyrin IX production in ALA-PDT for treating infection, characterized in that it comprises a substance that promotes the conversion from coproporphyrinogen III to protoporphyrin IX.
专利号:US-11161823-B2 优先权日:2019-03-11 标 题 :Anticancer 1,3-dioxane-4,6-dione derivatives and method of combinatorial synthesis thereof 发明人:ISLAM IMADUL; AL-KAYSI RABIH O; BOUDJELAL MOHAMED; ALI RIZWAN; NEHDI ATEF; ALGHANEM BANDAR 权利人:NAT GUARD HEALTH AFFAIRS; KING SAUD BIN ABDULAZIZ UNIV FOR HEALTH SCIENCES; KING ABDULLAH INTERNATIONAL MEDICAL RES CENTER; KING ABDULLAH INETRNATIONAL MEDICAL RES CENTER 摘要:Compounds, methods of synthesis, and methods of cancer treatment by arylidene-1,3-dioxane-4,6-diones. A Meldrum's acid-based chemistry and hybrid solid-liquid method. The method includes protection of ketone and aldehyde components and simultaneous immobilization on the solid phase, introduction of substituents, grafts and derivatives compatible with the protection, detachment and restoration of active carbonyl reactivity, reaction of ketone library with malonate, reacting of the products with the aldehyde library in liquid phase and separation of the products by preparative HPLC.
专利号:US-9125942-B2 优先权日:2010-01-19 标题 :Paramagnetic metal-nanodiamond conjugates 发明人:MANUS LISA M; MASTARONE DANIEL J; HO DEAN; MEADE THOMAS J 权利人:MANUS LISA M; MASTARONE DANIEL J; HO DEAN; MEADE THOMAS J; UNIV NORTHWESTERN 摘要:The present invention provides compositions and methods for the synthesis of conjugates of paramagnetic metal ions and nanodiamonds, and uses thereof. In particular, the present invention provides synthesis of paramagnetic metal-nanodiamond conjugates and methods using such compositions as molecular imaging probes.
1: Ahmadpour S, Noaparast Z, Abedi SM, Hosseinimehr SJ. (99m)Tc-HYNIC-(tricine/EDDA)-FROP peptide for MCF-7 breast tumor targeting and imaging. J Biomed Sci. 2018 Feb 19;25(1):17. doi: 10.1186/s12929-018-0420-x. 2: Kazemi Z, Zahmatkesh MH, Abedi SM, Hosseinimehr SJ. Biological Evaluation of 99mTc-HYNIC-EDDA/tricine-(Ser)-D4 Peptide for Tumor Targeting. Curr Radiopharm. 2017 Aug 24;10(2):123-130. doi: 10.2174/1874471010666170519165430. doi: 10.5603/NMR.2016.0019. Review. doi: 10.5603/NMR.2016.0016. doi: 10.4274/Mirt.68552. Epub 2013 Dec 10.
合成参考文献
摘要:L. C. Thompson, J. Inorg. Nucl. Chem. 24, 1083 (1962). 摘要:G. Degischer and G. H. Nancollas, Inorg. Chem. 9, 1259 (1970). 摘要:N. M. Dyatlova, M. I. Kabachnik, T. Y. Medved, M. V. Rudomino and Y. F. Belugin, Dokl. Chem. (Engl. Transl.) 161, 307 (1965). 参考文献:10.1128/jb.186.2.374-382.2004 摘要:LaMarca BBD, Zhu W, Arceneaux JEL, Byers BR, Lundrigan MD. Participation of fad and mbt Genes in Synthesis of Mycobactin in Mycobacterium smegmatis. J Bacteriol. 2004 Jan 15;186(2):374–82. doi: 10.1128/jb.186.2.374-382.2004. 参考文献:10.1080/07391102.1994.10508040 摘要:Zhong M, Kallenbach NR. Mapping tRNA and 5S RNA Tertiary Structures by Charge Dependent Fe(II)-Catalyzed Cleavage. Journal of Biomolecular Structure and Dynamics. 1994 Feb;11(4):901–11. doi: 10.1080/07391102.1994.10508040.