专利号:US-2023286918-A1 优先权日:2020-07-02 标 题:Manufacturing process for 3,5-dichloropicolinonitrile for synthesis of vadadustat 发明人:JURKAUSKAS VALDAS; JUNG YOUNG CHUN; KWON TAESOO; KANNAN ARUNACHALAM; GONDI VIJAYA BHASKER 权利人:AKEBIA THERAPEUTICS INC 摘要:Disclosed herein are methods and processes of preparing vadadustat or a pharmaceutically acceptable salts thereof, and intermediates (e.g., a compound of Formula (I), (I-F), (II), or (IV), or a pharmaceutically acceptable salts thereof) useful for the synthesis of vadadustat.
专利号:US-7279572-B2 优先权日:2003-05-22 标题:Process for the 2-stage synthesis of hexanitrohexaazaisowurtzitane starting from a primary amine 发明人:CAGNON GUY; ECK GENEVIEVE; HERVE GREGOIRE; JACOB GUY 权利人:SNPE MATERIAUX ENERGETIQUES 摘要:A subject-matter of the present invention is a novel process for the synthesis of hexanitrohexaazaisowurtzitane (HNIW), a compound of use as energetic filler in powders, propellants and explosives. n This process comprises a first stage of reaction of an α,β-dicarbonyl derivative with a primary amine which makes it possible to form a hexasubstituted hexaazaisowurtzitane derivative. n The HNIW is subsequently obtained directly, in a single reaction stage, by nitration of the hexasubstituted hexaazaisowurtzitane derivative. n This process, in only 2 stages starting from a primary amine, is particularly simple and inexpensive.
专利号:WO-9429243-A1 优先权日:1993-06-11 标 题 :Synthesis of substituted triphenylenes, useful as discotic liquid crystals 发明人:BUSHBY RICHARD JAMES; CAMMINDGE ANDREW NEIL; HEADDOCK GARETH; BORNER RUTH CAROL; BODEN NEVILLE 权利人:BRITISH TECH GROUP; BUSHBY RICHARD JAMES; CAMMINDGE ANDREW NEIL; HEADDOCK GARETH; BORNER RUTH CAROL; BODEN NEVILLE 摘要:Unsymmetrically substituted triphenylenes required in the synthesis of polymeric discotic liquid crystals are made using iron (III) chloride in organic solvent at room temperature to effect the oxidative coupling of 1,2-dialkoxybenzenes to 3,3',4,4'-tetraalkoxybiphenyls. This is followed by a reductive workup. The same oxidation-reduction protocol also proves effective in the trimerisation of 1,2-dialkoxybenzenes.
专利号:US-7211590-B2 优先权日:2002-08-01 标 题:Nitrosated proton pump inhibitors, compositions and methods of use 发明人:FANG XINQIN; GARVEY DAVID S; LETTS L GORDON 权利人:NITROMED INC 摘要:The invention describes novel nitrosated proton pump inhibitor compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated proton pump inhibitor 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 nitrosated proton pump inhibitor 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 nitrosated proton pump inhibitor compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating gastrointestinal disorders; facilitating ulcer healing; decreasing the recurrence of ulcers; improving gastroprotective properties, anti-Helicobacter pylori properties or antacid properties of proton pump inhibitors; decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds; treating bacterial infections and/or viral infections.
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-7708989-B2 优先权日:1999-10-29 标题 :Methods of treating vascular diseases characterized by nitric oxide insufficiency 发明人:LOSCALZO JOSEPH; VITA JOSEPH A; LOBERG MICHAEL D; WORCEL MANUEL 权利人:NITROMED INC 摘要:The invention provides methods of treating and/or preventing vascular diseases characterized by nitric oxide insufficiency by administering a therapeutically effective amount of at least one nitrosated angiotensin-converting enzyme inhibitor, nitrosated beta-adrenergic blocker, nitrosated cholesterol reducer, nitrosated calcium channel blocker, nitrosated endothelin antagonist, nitrosated angiotensin II receptor antagonist, nitrosated renin inhibitor, and optionally at least one compound used to treat cardiovascular diseases and/or at least one antioxidant, or a pharmaceutically acceptable salt thereof, and/or 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. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The 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 may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The vascular diseases characterized by nitric oxide insufficiency include a cardiovascular disease and a disease resulting from oxidative stress.