📜Pyridin-2-Yl-Carbamic Acid 2-[6-(5-Isopropyl-Pyridine-2-Sulfonylamino)-5-(2-Methoxy-Phenoxy)-2-Morpholin-4-Yl-Pyrimidin-4-Yloxy]-Ethyl Ester,氯化铵,叠氮化钠 以to Form 5-Isopropyl-Pyridine-2-Sulfonic Acid {6-(2-Hydroxy-Ethoxy)-5-(2-Methoxy-Phenoxy)-2-[2-(1H-Tetrazol-5-yl)-Pyridin-4-Yl]-Pyrimidin-4-Yl}-Amide的收率获得替唑生坦 参考文献:Process For The Manufacture Of 2,5-Disubstituted Pyridines 标题:Process For The Manufacture Of 2,5-Disubstituted Pyridines 摘要:本发明涉及一种制备式(I)的2,5-二取代吡啶的方法,其中包括以下步骤:A)将式(II)的化合物r.Sup.1-Ch.Dbd.Ch-R.Sup.2(II)与式(III)的丙烯酸化合物反应,以形成式(Iv)的化合物;B)在无水条件下将式(Iv)的化合物与氢卤酸反应.其中,R.Sup.1表示低碳基,R.Sup.2表示二(低碳基)氨基或具有氮原子上的游离价键的5-或6-成员的-N-杂环基团,X表示卤素.
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-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
专利号:US-6004965-A 优先权日:1994-12-20 标题 :Sulfonamides 发明人:BREU VOLKER; BURRI KASPAR; CASSAL JEAN-MARIE; CLOZEL MARTINE; HIRTH GEORGES; LOEFFLER BERND-MICHAEL; MUELLER MARCEL; NEIDHART WERNER; RAMUZ HENRI 权利人:HOFFMANN LA ROCHE 摘要:Compounds of the formula: ##STR1## where A, B, R 1 -R 8 are as described herein are endothelin inhibitors that can be used in treating diseases associated with endothelin, such as high blood pressure. Chemical synthesis of these compounds and pharmaceutical compositions containing these compounds are also useful.
专利号:TW-201518323-A 优先权日:2013-07-25 标题 :Synthesis of biological conjugates of APELIN polypeptides
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: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.