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-9562068-B2 优先权日:2014-10-17 标 题 :Process for the preparation of 7 α-(methoxycarbonyl)-3-OXO-17alpha-pregn-4,9(11)-dien-21,17-carbolactone, a useful intermediate for the synthesis of molecules with pharmacological activity 发明人:LENNA ROBERTO; DI BRISCO RICCARDO; BARBIERI FRANCESCO 权利人:IND CHIMICA SRL; IND CHIMICA SRL 摘要:An improved process for the preparation of intermediate (V) through the elimination of a molecule of water from intermediate (IV) is described. n nIntermediate (V) is a key molecule for the synthesis of eplerenone, a synthetic steroid with pharmacological activity used in the treatment of chronic pathological conditions, including hypertension.
专利号:US-8367394-B2 优先权日:2007-07-04 标题:Process for the synthesis of 9α-hydroxy-steroids 发明人:OLASZ KATALIN; TEGDES ANIKO; GANCSOS VALERIA; HANTOS GABOR; KOENCZOEL KALMAN; BALOGH GABOR; ERDELYI SANDOR 权利人:RICHTER GEDEON NYRT; OLASZ KATALIN; TEGDES ANIKO; GANCSOS VALERIA; HANTOS GABOR; KOENCZOEL KALMAN; BALOGH GABOR; ERDELYI SANDOR 摘要:The present invention relates to a novel selective synthesis of 9α-hydroxy-steroid derivatives of the general formula (I) (I)—wherein the meaning of -A-A′- is —CH 2 —CH 2 — or —CHâ•?CH— group—by the bioconversion of compounds of the general formula (II) (II) wherein the meaning of -A-A′- is —CH 2 —CH 2 — or —CHâ•?CH— group—by using Nocardia farcinica bacterium strain, deposition number of which is NCAIM (P)—B 001342, as hydroxylating microorganism in the bioconversion.
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:US-6610844-B2 优先权日:1996-12-11 标题:Processes for preparation of 9,11-epoxy steroids and intermediates useful therein 发明人:NG JOHN S; LIU CHIN; ANDERSON DENNIS K; LAWSON JON P; WIECZOREK JOSEPH; KUNDA SASTRY A; LETENDRE LEO J; POZZO MARK J; SING YUEN-LUNG L; WANG PING T; YONAN EDWARD E; WEIER RICHARD M; KOWAR THOMAS R; BAEZ JULIO A; ERB BERNHARD 权利人:SEARLE & CO 摘要:Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula Iwherein-A-A- represents the group -CHR4-CHR5- or -CR4=CR5-;R3, R4 and R5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano and aryloxy;R1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical;-B-B- represents the group -CHR6-CHR7- or an alpha- or beta-oriented group:where R6 and R7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy; andR8 and R9 are independently selected from the group consisting of hydrogen, hydroxy, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy, or R8 and R9 together comprise a carbocyclic or heterocyclic ring structure, or R8 or R9 together with R6 or comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring.
1: Struthers A, Krum H, Williams GH. A comparison of the aldosterone-blocking agents eplerenone and spironolactone. Clin Cardiol. 2008 Apr;31(4):153-8. doi: 10.1002/clc.20324. 2: Provenzano M, Puchades MJ, Garofalo C, Jongs N, D'Marco L, Andreucci M, De Nicola L, Gorriz JL, Heerspink HJL; ROTATE-3 study group; ROTATE-3 study group members. Albuminuria-Lowering Effect of Dapagliflozin, Eplerenone, and Their Combination in Patients with Chronic Kidney Disease: A Randomized Crossover Clinical Trial. J Am Soc Nephrol. 2022 Aug;33(8):1569-1580. doi: 10.1681/ASN.2022020207. Epub 2022 Apr 19. 3: Filippatos G, Anker SD, Böhm M, Gheorghiade M, Køber L, Krum H, Maggioni AP, Ponikowski P, Voors AA, Zannad F, Kim SY, Nowack C, Palombo G, Kolkhof P, Kimmeskamp-Kirschbaum N, Pieper A, Pitt B. A randomized controlled study of finerenone vs. eplerenone in patients with worsening chronic heart failure and diabetes mellitus and/or chronic kidney disease. Eur Heart J. 2016 Jul 14;37(27):2105-14. doi: 10.1093/eurheartj/ehw132. Epub 2016 Apr 29.
合成参考文献
参考文献:10.1161/hypertensionaha.111.171280 摘要:Lindschau C, Kirsch T, Klinge U, Kolkhof P, Peters I, Fiebeler A. Dehydroepiandrosterone-induced phosphorylation and translocation of FoxO1 depend on the mineralocorticoid receptor. Hypertension. 2011 Sep;58(3):471–8. doi: 10.1161/hypertensionaha.111.171280. 参考文献:10.4061/2011/346985 摘要:Essick EE, Sam F. Cardiac Hypertrophy and Fibrosis in the Metabolic Syndrome: A Role for Aldosterone and the Mineralocorticoid Receptor. International Journal of Hypertension. 2011;2011():1–12. doi: 10.4061/2011/346985. 参考文献:10.4061/2011/417594 摘要:Demede M, Pandey A, Innasimuthu L, Jean-Louis G, McFarlane SI, Ogedegbe G. Management of Hypertension in High-Risk Ethnic Minority with Heart Failure. International Journal of Hypertension. 2011;2011():1–8. doi: 10.4061/2011/417594. 参考文献:10.1007/s10741-011-9265-z 摘要:Carubelli V, Metra M, Lombardi C, Bettari L, Bugatti S, Lazzarini V, Dei Cas L. Renal dysfunction in acute heart failure: epidemiology, mechanisms and assessment. Heart Fail Rev. 2012 Mar;17(2):271–82. doi: 10.1007/s10741-011-9265-z. 参考文献:10.1038/hr.2011.89 摘要:Lee WY, Kwon CH, Rhee EJ, Park JB, Kim YK, Woo SY, Kim S, Sung KC. The effect of body mass index and fasting glucose on the relationship between blood pressure and incident diabetes mellitus: a 5-year follow-up study. Hypertension Research. 2011 Jul 14;34(10):1093–7. doi: 10.1038/hr.2011.89.