(2S)-2-(4,6-Dimethoxypyrimidin-2-Yloxy)-3-Methoxy-3,3-Diphenyl Ethyl Propionate置于水,Sodium Hydroxide体系中,用 1,4-二氧六环 用作溶剂,化学反应 8.0H,以1.32 G的收率获得达卢生坦 参考文献:Method For Preparing Optically Pure (+)-Ambrisentan And (+)-Darusentan 标题:Method For Preparing Optically Pure (+)-Ambrisentan And (+)-Darusentan 摘要:公开了一种制备光学纯的(+)-安立生坦和(+)-达鲁生坦的方法,包括:首先催化β-不饱和烯烃的不对称环氧化,使用从果糖或其水合物衍生的手性酮作为催化剂,然后将产物依次进行环氧化合物的开环反应和取代反应,以获得光学纯的(+)-安立生坦和(+)-达鲁生坦.
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-2010160351-A1 优先权日:2008-12-19 标题:Pharmaceutical compositions and methods for treating hyperuricemia and related disorders 发明人:JENKINS HELEN; KITT MICHAEL; PEARLMAN RODNEY; SERAFINI TITO; THORSETT EUGENE 权利人:NUON THERAPEUTICS INC 摘要:Disclosed is a pharmaceutical composition comprising (a) a first therapeutic agent, wherein the first therapeutic agent is a compound of formula II: n n n n n n n n n n n n or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , X and n are as defined herein; (b) a second therapeutic agent, wherein the second therapeutic agent is a uric acid synthesis inhibitor or a uricosuric agent; and (c) a pharmaceutically acceptable diluent or carrier.
专利号:US-2014315720-A1 优先权日:2012-10-24 标 题 :Polysaccharide ester microspheres and methods and articles relating thereto 发明人:FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY 权利人:CELANESE ACETATE LLC 摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.
专利号:WO-2010071865-A1 优先权日:2008-12-19 标 题:Pharmaceutical compositions and methods for treating hyperuricemia and related disorders 发明人:JENKINS HELEN; KITT MICHAEL; PEARLMAN RODNEY; SERAFINI TITO; THORSETT EUGENE 权利人:NUON THERAPEUTICS INC; JENKINS HELEN; KITT MICHAEL; PEARLMAN RODNEY; SERAFINI TITO; THORSETT EUGENE 摘要:Disclosed is a pharmaceutical composition comprising (a) a first therapeutic agent, wherein the first therapeutic agent is a compound of formula II or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , X and n are as defined herein; (b) a second therapeutic agent, wherein the second therapeutic agent is a uric acid synthesis inhibitor or a uricosuric agent; and (c) a pharmaceutically acceptable diluent or carrier.
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合成参考文献
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