其它别名(3E)-3-[[(1S,4As,8As)-Decahydro-5,5,8A-Trimethyl-2-Methylene-1-Naphthalenyl]Methylene]Dihydro-5-Methoxy-2(3H)3-[(1E)-2-[(1S,4As,8As)-Decahydro-5,5,8A-Trimethyl-2-Methylene-1-Naphthalenyl]Ethenyl]Furan; (+)-Coronarin E-Furanone; Coronarin D Methyl Ethe ; D
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-7122693-B2 优先权日:1988-04-11 标题 :Acetaldehyde acetal compounds, their synthesis, and uses thereof 发明人:BELLEAU EXECUTRIX OF ESTATE PI; DIXIT DILIP M; NGUYEN-BA NGHE 权利人:SHIRE BIOCHEM INC 摘要:The acetaldehyde compounds, 2-thiobenzoylacetaldehyde diethylacetal, 2-benzoyloxyacetaldehyde bis(2-methoxyethyl)acetal, 2-hydroxyacetaldehyde bis( 2-methoxyethyl)acetal, 2-thiobenzoylacetaldehyde bis(2-methoxy-ethyl)acetal, and 2-thioacetaldehyde bis(2-methoxyethyl)acetal, are useful as intermediates in the synthesis of substituted 1,3-oxathiolanes and substituted 1,3-dioxolanes.
专利号:US-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:US-6730790-B2 优先权日:2002-03-01 标 题:Chlorinated heterocyclic compounds and methods of synthesis 发明人:KWIATKOWSKI STEFAN; GOLINSKI MIROSLAW 权利人:R T ALAMO VENTURES I LLC 摘要:Compositions of the present invention comprise chlorinated heterocyclic compounds, including racemic monochloroflosequinan, purified enantiomers of monochloroflosequinan and the sulfone derivative of monochloroflosequinan. The methods of the present invention comprise the synthesis of racemic monochloroflosequinan and derivatives thereof, including the sulfone derivative. Intermediates in the synthesis are also provided. The methods further comprise the synthesis of enantiomers of monochloroflosequinan.
专利号:WO-9925699-A1 优先权日:1997-11-19 标 题:Salts of 5,5'-arylidenebisbarbituric and 5,5'-arylidenebis(2-thiobarbituric) acids and 5,5'-arylidenebis(2-thiobarbituric) acids having an antibacterial, anti-chlamydial, antiviral and immuno-modulating activity 发明人:ASHKINAZI RIMMA ILIINICHNA 权利人:TETS VIKTOR VENIAMINOICH; ASHKINAZI RIMMA ILIINICHNA 摘要:The present invention relates to the production of new chemical substances having an anti-microbial, antiviral, immuno-modulating and anti-tumoral activity. This invention more precisely relates to the synthesis of new substances consisting of 5,5'-arylidenebis(2-thiobarbituric) acids and in salts of 5,5'-arylidenebisbarbituric and 5,5'-arylidenebis(2-thiobarbituric) acids of general formula (I) where X is oxygen or sulphur. R1 is hydrogen, a nitro group or an alkoxy group, R2 is hydrogen, a nitro group, an alkoxy group or halogen and Cat+ is a proton or a pyridin- or 2-hydroxyethylammonium-cation. In the preferred embodiments of these substances, the following conditions are observed: X=O, Cat+ is pyridine, R1=H and R2=Cl (I); X=O, Cat+ is pyridine, R1=H and R2=NO2 (II); X=O, Cat+ is H3N+CH2CH2OH, R1=H and R2=NO2 (III); X=S, Cat+ is pyridine, R1=H and R2=Cl (IV); X=S, Cat+ is pyridine, R1=H and R2=OH (V); X=S, Cat+ is pyridine, R1=NO2 and R2=H (VI); X=S, Cat+ is pyridine and R1=R2=MeO (VII); X=O, Cat+ is pyridine, R1=H and R2=Br (VIII); X=O, Cat?+ is H+, R1¿=H and R2=Cl (IX); X=O, Cat?+ is H+, R1¿=H and R2=NO2 (X). This invention also relates to eight synthesis instances of these substances, to three tables representing the chemical and physical characteristics of the substances thus obtained and to the results of five series of experiments. These synthesis instances, tables and results demonstrate the biological properties of these substances on myco-bacteria, on herpes viruses and on Chlamydia trachomatis as well as their interferon-inducing activity and the absence of acute toxicity.
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.
1: Ciacciarelli M, Zerbinati C, Violi F, Iuliano L. Dipyridamole: a drug with unrecognized antioxidant activity. Curr Top Med Chem. 2015;15(9):822-9. Review. doi: 10.1016/j.phrs.2014.05.008. Epub 2014 May 24. Review. doi: 10.1177/0036933013496926. Review. doi: 10.1016/j.jclinepi.2012.01.019. Review. doi: 10.1159/000338053. Epub 2012 Aug 9. Review. doi: 10.3310/hta15310. Review. doi: 10.1111/j.1749-6632.2010.05732.x. Review. doi: 10.1111/j.1749-6632.2010.05737.x. Review. 9: d'Esterre CD, Lee TY. Effect of dipyridamole during acute stroke: exploring antithrombosis and neuroprotective benefits. Ann N Y Acad Sci. 2010 Oct;1207:71-5. doi: 10.1111/j.1749-6632.2010.05801.x. Review. doi: 10.2146/ajhp080645. Review. doi: 10.3233/CH-2010-1274. Review. doi: 10.1002/ccd.22030. Review. doi: 10.1586/14737175.8.11.1661. Review. Review. doi: 10.1161/ATVBAHA.107.160226. Epub 2008 Jan 3. Review. 16: Halkes PH, Algra A. Anticoagulants, aspirin and dipyridamole in the secondary prevention of cerebral ischaemia: which is the best for which patient? Cerebrovasc Dis. 2007;24 Suppl
合成参考文献
参考文献:10.1007/s00259-005-1965-y 摘要:Schuijf JD, Poldermans D, Shaw LJ, Jukema JW, Lamb HJ, de Roos A, Wijns W, van der Wall EE, Bax JJ. Diagnostic and prognostic value of non-invasive imaging in known or suspected coronary artery disease. European Journal of Nuclear Medicine and Molecular Imaging. 2005 Nov 30;33(1):93–104. doi: 10.1007/s00259-005-1965-y. 参考文献:10.1161/01.res.26.6.743 摘要:Afonso S. Inhibition of coronary vasodilating action of dipyridamole and adenosine by aminophylline in the dog. Circ Res. 1970 Jun;26(6):743–52. doi: 10.1161/01.res.26.6.743. 参考文献:10.1155/2011/687624 摘要:Voulgari C, Tentolouris N, Stefanadis C. The ECG Vertigo in Diabetes and Cardiac Autonomic Neuropathy. Experimental Diabetes Research. 2011;2011():1–17. doi: 10.1155/2011/687624. 参考文献:10.1007/bf00586582 摘要:Raff WK, Drechsel U, Scholtholt J, Lochner W. [Effect of nitroglycerin on the heart]. Pflugers Arch. 1970;317(4):336–43. doi: 10.1007/bf00586582. 参考文献:10.1007/s12265-011-9306-y 摘要:Prichard HL, Manson RJ, DiBernardo L, Niklason LE, Lawson JH, Dahl SLM. An Early Study on the Mechanisms that Allow Tissue-Engineered Vascular Grafts to Resist Intimal Hyperplasia. Journal of Cardiovascular Translational Research. 2011 Jul 12;4(5):674. doi: 10.1007/s12265-011-9306-y.