CAS: 51803-78-2; N-(4-Nitro-2-Phenoxyphenyl)Methanesulfonamide

上下游产品

CAS号51765-51-6 2-苯氧基甲烷磺酰苯胺 | CAS号94-13-3 对羟基苯甲酸丙酯 | CAS号62-44-2 非那西丁 | CAS号5422-92-4 4-硝基-2-苯氧基苯胺 | CAS号99-76-3 尼泊金甲酯 | CAS号99-96-7 4-羟基苯甲酸 | CAS号51765-60-7 N-(4-Amino-2-ph... | CAS号109032-22-6 4-HYDROXY NIMESULIDE

2-(4-Nitro-2-Phenoxyphenyl)Isoindoline-1,3-Dione置于一水合肼,三乙胺体系中,用 甲醇,二氯甲烷 作为反应溶剂,化学反应 45.0H,反应生成 尼美舒利
参考文献:Isomeric Methoxy Analogs Of Nimesulide For Development Of Brain Cyclooxygense-2 (Cox-2)-Targeted Imaging Agents: Synthesis,In Vitro Cox-2-Inhibitory Potency,And Cellular Transport Properties
标题:Isomeric Methoxy Analogs Of Nimesulide For Development Of Brain Cyclooxygense-2 (Cox-2)-Targeted Imaging Agents: Synthesis,In Vitro Cox-2-Inhibitory Potency,And Cellular Transport Properties
摘要:Nimesulide Analogs Bearing A Methoxy Substituent Either At The Ortho-,Meta-Or Para-Position On The Phenyl Ring,Were Designed,Synthesized,And Evaluated For Potential As Radioligands For Brain Cyclooxygenase-2 (Cox-2) Imaging. The Synthesis Of Nimesulide And Regioisomeric Methoxy Analogs Was Based On The Copper-Mediated Arylation Of Phenolic Derivatives For The Construction Of Diaryl Ethers. These Isomeric Methoxy Analogs Displayed Lipophilicity Similar To That Of Nimesulide Itself,As Evidenced By Their HPLC Logp(7.4) Values. In Vitro Inhibition Studies Using A Colorimetric Cox (Ovine) Inhibitor-Screening Assay Demonstrated That The Para-Methoxy Substituted Analog Retains The Inhibition Ability And Selectivity Observed For Parent Nimesulide Toward Cox-2 Enzyme,Whereas The Meta-And Ortho-Methoxy Substituents Detrimentally Affected Cox-2-Inhibition Activity,Which Was Further Supported By Molecular Docking Studies. Bidirectional Transport Cellular Studies Using Caco-2 Cell Culture Model In The Presence Of The P-Glycoprotein (P-Gp) Inhibitor,Verapamil,Showed That P-Gp Did Not Have A Significant Effect On The Efflux Of The Para-Methoxy Substituted Analog. Further Investigations Using The Radiolabeled Form Of The Para-Methoxy Substituted Analog Is Warranted For In Vivo Characterization. (C) 2015 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmc.2015.10.007

专利信息

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:US-8546532-B2
优先权日:2008-04-17
标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders
发明人：BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS
权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC
摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.

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-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-2003157061-A1
优先权日:2001-12-05
标 题 :Combinations of a cyclooxygenase-2 selective inhibitor and a TNFalpha antagonist and therapeutic uses therefor
发明人：BENNETT DENNIS A
权利人:PHARMACIA CORP
摘要:A method for the prevention, treatment, or inhibition of pain, inflammation, or inflammation-related disorder and for the prevention, treatment, or inhibition of a cardiovascular disease or disorder in a subject that is in need of such prevention, treatment or inhibition, involves the administration to the subject of a cyclooxygenase-2 selective inhibitor or prodrug thereof and a TNFα antagonist. A method can also involve the treatment, prevention, or inhibition of cancer in a subject in need of such treatment, prevention, or inhibition, by administering to the subject a cyclooxygenase-2 selective inhibitor or prodrug thereof and a TNFα antagonist which is selected from the group consisting of a compound that affects the synthesis of TNFα, a compound that inhibits the binding of TNFα with a receptor specific for TNFα, and a compound that interferes with intracellular signaling triggered by TNFα binding with a receptor. Compositions, pharmaceutical compositions and kits that can be used with the methods are also described.