📜(3,4-亚甲基二氧基)-6-甲基苄氯 以71%的收率获得n-(4-氯-3-甲基-5-异恶唑基)-2-[(2-甲基-4,5-亚甲二氧基苯基)乙酰]噻吩-3-磺酰胺 参考文献:Formulation Of Sulfonamides For Treatment Of Endothelin-Mediated Disorders 标题:Formulation Of Sulfonamides For Treatment Of Endothelin-Mediated Disorders 摘要:提供了药物可接受的噻吩基,呋喃基和吡咯基磺酰胺的制剂以及使用这些制剂调节或改变内皮素肽家族活性的方法.特别是,提供了n-(异恶唑基)噻吩磺酰胺,N-(异恶唑基)呋喃磺酰胺和n-(异恶唑基)吡咯磺酰胺的钠盐的制剂以及使用这些磺酰胺盐通过将受体与磺酰胺盐接触来抑制内皮素肽与内皮素受体结合的方法.还提供了通过施用有效量的一个或多个这些磺酰胺盐或抑制或增加内皮素活性的前药来治疗内皮素介导的疾病的方法.
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-5705629-A 优先权日:1995-10-20 标 题:Methods for H-phosphonate synthesis of mono- and oligonucleotides 发明人:BHONGLE NANDKUMAR 权利人:HYBRIDON INC 摘要:New methods of synthesizing mono- and oligo- nucleotide H-phosphonates are disclosed. The methods comprise contacting a mononucleoside with phosphonic acid and benzoyl anyhydride to yield the corresponding mononucleoside H-phosphonate. Preferrably a catalytic amount of triphosgene is also used. A similar procedure can be used to couple a first mononucleoside to a second mononucleoside or to an oligonucleotide, the method comprising contacting, in the presence of benzoic anhydride and, preferrably, a catalytic amount of triphosgene, a mononucleotide or oligonucleotide having a free 5' hydroxyl with a mononucleoside having a 3' hydroxyl-bearing phosphorous moiety (preferably H-phosphonate).
专利号:WO-9817675-A1 优先权日:1996-10-18 标 题:Improved methods for h-phosphonate synthesis of mono- and oligonucleotides 发明人:BHONGLE NANDKUMAR 权利人:HYBRIDON INC 摘要:New methods of synthesizing mono- and oligo- nucleotide H-phosphonates are disclosed. The methods comprise contacting a mononucleoside with phosphonic acid and benzoyl anhydride to yield the corresponding mononucleoside H-phosphonate. Preferably, a catalytic amount of triphosgene is also used. A similar procedure can be used to couple a first mononucleoside to a second mononucleoside or to an oligonucleotide, the method comprising contacting, in the presence of benzoic anhydride and, preferably, a catalytic amount of triphosgene, a mononucleotide or oligonucleotide having a free 5'hydroxyl with a mononucleoside having a 3'hydroxyl-bearing phosphorous moiety (preferably H-phosphonate).
专利号:US-10906888-B2 优先权日:2016-07-14 标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-10308615-B2 优先权日:2015-05-29 标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-2013345311-A1 优先权日:2004-07-19 标 题 :Synthesis Of Triethylenetetramines
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