叔丁基过氧化氢置于titanium(Iv) Isopropylate,水,(R)-1,1'-Bi-2-Naphthol体系中,用 氯仿,水 用作溶剂,化学反应 73.5H,以77%的收率获得泰妥拉唑 参考文献: The Enantiomer Of Tenatoprazole And The Use Thereof In Therapy[fr] Enantiomere De Tenatoprazole Et Son Utilisation Dans Une Therapie 标题: The Enantiomer Of Tenatoprazole And The Use Thereof In Therapy[fr] Enantiomere De Tenatoprazole Et Son Utilisation Dans Une Therapie 摘要:本发明涉及到替纳托普拉唑的光学活性物质,即(+)-和(-)-5-甲氧基-2-{[(4-甲氧基-3,5-二甲基-2-吡啶基)甲基]亚砜基}-1H-咪唑[4,5-B]吡啶.该化合物及其制药组合物可用作抗溃疡药物.
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-2008280855-A1 优先权日:2005-06-22 标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles 发明人:CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO 权利人:NYCOMED GMBH 摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.
专利号:US-7332505-B2 优先权日:1999-02-26 标 题 :Nitrosated and nitrosylated proton pump inhibitors, compositions and methods of use 发明人:GARVEY DAVID S; LETTS L GORDON; RICHARDSON STEWART K; TAM SANG WILLIAM; WANG TIANSHENG 权利人:NITROMED INC 摘要:The present invention describes novel nitrosated and/or nitrosylated proton pump inhibitor compounds, and novel compositions comprising at least one proton pump inhibitor compound that is optionally substituted with at least one NO and/or NO 2 group, and, optionally, at least one compound that donates, transfers, or releases nitric oxide, induces the production of endogenous nitric oxide or endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase, and/or at least one nonsteroidal antiinflammatory drug, selective COX-2 inhibitor, antacid, bismuth-containing reagent, acid-degradable antibacterial compound, and mixtures thereof. The present invention also provides methods for treating and/or preventing gastrointestinal disorders; facilitating ulcer healing; decreasing the recurrence of ulcers; improving gastroprotective properties, anti- Helicobacter pylon properties or antacid properties of proton pump inhibitors; decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds; treating Helicobacter pylori and viral infections. The compounds and/or compositions of the present invention can also be provided in the form of a pharmaceutical kit.
专利号:EP-2451810-B1 优先权日:2009-07-07 标 题 :Continuous flow process for the preparation of sulphoxide compounds 发明人:KULKARNI AMOL ARVIND; JOSHI RAMESH ANNA; NIVANGUNE NAYANA TUSHAR; JAGTAP MANISHA ABDHIMAN 权利人:COUNCIL SCIENT IND RES 摘要:A continuous micromixer based process for the synthesis of sulphoxide compounds with a reaction time of less than or equal one minute is disclosed. The process shows selectivity of >95% towards the sulphoxide compounds.
专利号:US-9631181-B2 优先权日:2009-12-08 标 题 :Synthesis of prazole compounds 发明人:BONG YONG KOY; CLAY MICHAEL D; COLLIER STEVEN J; MIJTS BENJAMIN; VOGEL MICHAEL; ZHANG XIYUN; ZHU JUN; NAZOR JOVANA; SMITH DEREK J; SONG SHIWEI 权利人:CODEXIS INC 摘要:The present disclosure relates to non-naturally occurring monooxygenase polypeptides useful for preparing prazole compounds, polynucleotides encoding the polypeptides, and methods of using the polypeptides.
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