CAS: 60940-34-3; 2-Phenylbenzo[d][1,2]Selenazol-3(2H)-One

2-氯-N-苯基苯甲酰胺置于copper(L) Iodide,1,10-菲罗啉,Potassium Selenocyanate,Caesium Carbonate体系中,用 乙腈 作为反应溶剂,化学反应 16.0H,以5%的收率获得产物依布硒
参考文献:热和光诱导的铜促进的c-Se键形成:2-烷基-1,2-苯并亚硒唑-3(2 H)-One的合成及对结核分枝杆菌的评价
标题:热和光诱导的铜促进的c-Se键形成:2-烷基-1,2-苯并亚硒唑-3(2 H)-One的合成及对结核分枝杆菌的评价
摘要:以ebselen(1A)为代表的2-烷基-1,2-苯并硒代咪唑-3(2 H)-酮正在广泛地用于一系列医学应用中.我们都描述了一种新的热和光致铜介导的硒氰酸钾(ksecn)和之间的交叉耦合ñ取代邻-Halobenzamides以形成2-烷基-1,2-苯并异硒唑-3(2 ħ)-酮含有c-硒键.铜配体(1,10-菲咯啉)通过可能涉及原子转移(at)的机制促进加热过程中c-Se键的形成,而在没有配体的情况下,光诱导的活化可能通过单电子转移(set)进行机制.一个15 2-烷基-1,2-苯并亚硒唑-3(2 H)-准备好了.文库的一个成员是含叠氮化物的衍生物1J,它能够经受应变促进的叠氮化物-炔烃环加成反应.评价该文库对结核分枝杆菌(mtb)生长和mtb抗原85C(mtb Ag85C)活性的抑制作用.化合物1F最有效,最小抑制浓度(mic)为12.5μg/ Ml,Mtb Ag85C表观ic 50为8
DOI:10.1021/acs.Joc.7B00440

专利信息

专利号:WO-2023169082-A1
优先权日:2022-10-24
标 题:Synthesis method and application of benzothiadiazole-1-ketone compound and derivative thereof
发明人：YI WEI; ZHOU ZHI; WU LIEXIN
权利人:UNIV GUANGZHOU MEDICAL
摘要:Disclosed in the present invention are a synthesis method and application of a benzoselenazole-1-ketone compound and a derivative thereof. Sulfoximine and the element selenium are used as raw materials, and by means of a rhodium catalysis direct C-H functionalization reaction, synthesis of a series of benzoselenazole-1-ketone compounds is achieved. The solution has the advantages of strong functional group compatibility, wide substrate universality, mild conditions, simple operations, and high efficiency and universality. Meanwhile, sulfoximine and the element selenium are used as initial raw materials, a direct C-H functionalization reaction is carried out, and by means of chiral phosphoric acid, synthesis of the chiral benzoselenazole-1-ketone compound is achieved. The application prospect is good, and a sulfydryl structure in biomacromolecules such as polypeptides, saccharides, drug molecules and proteins can be specifically marked. Good anti-SARS-CoV-2 virus activity is exhibited, a trastuzumab biological conjugate can effectively image HER 2 receptors on the cell surface, displays strong fluorescence, and can be applied to the preparation of an imaging reagent for the HER 2 receptor on the cell surface.

专利号:US-7141238-B2
优先权日:1998-04-02
标题:Compositions for reducing UV-induced inhibition of collagen biosynthesis in human skin
发明人：FISHER GARY J; VOORHEES JOHN J
权利人:UNIV MICHIGAN
摘要:Exposure of human skin to ultraviolet (UV) radiation from the sun not only induces the production of enzymes (matrix metalloproteinases) that degrade collagen, but also inhibits the synthesis of new collagen by inhibiting the synthesis of procollagen. This UV-induced inhibition of the synthesis of collagen can be prevented by the topical application of a retinoid or c-JUN inhibitor to the skin prior to exposure to UV radiation.

专利号:US-8304409-B2
优先权日:2002-07-03
标 题:Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use
发明人：EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI
权利人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI; NICOX SA
摘要:The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, 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 NSAID, 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 NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.

专利号:US-2002183366-A1
优先权日:2001-03-23
标题:Cyclooxygenase-2 inhibitors, compositions and methods of use
发明人：GARVEY DAVID S; SCHROEDER JOSEPH D
摘要:This invention describes novel compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, 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, optionally, at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal toxicity or other toxicities; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.

专利号:US-7211598-B2
优先权日:2002-06-28
标 题:Oxime and/or hydrozone containing nitrosated and/or nitrosylated cyclooxygenase-2 selective inhibitors, compositions and methods of use
发明人：GARVEY DAVID S; RANATUNGE RAMANI R; RICHARDSON STEWART K
权利人:NITROMED INC
摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors having at least one oxime group or hydrazone group and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor having at least one oxime group or hydrazone group, 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 kits comprising at least one COX-2 selective inhibitor having at least one oxime group or hydrazone group, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention having at least one oxime group or hydrazone group can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.

专利号:US-7244753-B2
优先权日:2002-07-29
标 题:Cyclooxygenase-2 selective inhibitors, compositions and methods of use
发明人：GARVEY DAVID S; KHANAPURE SUBHASH P; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D
权利人:NITROMED INC
摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, 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 kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.