CAS: 78967-07-4; 2-(3,4-Bis(4-Methoxyphenyl)Isoxazol-5-yl)Acetic Acid

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CAS号131454-49-4 methyl 2-[3,4-b... | CAS号112453-43-7 2-[4-(4-methoxy...

📜[(4-甲氧苯基)次甲基]氮烷氧化置于正丁基锂,Sodium Hydride体系中,用 四氢呋喃 作为反应溶剂,化学反应 2.0H,反应生成 莫非佐酸
参考文献:Translational Impact Of Novel Widely Pharmacological Characterized Mofezolac-Derived Cox-1 Inhibitors Combined With Bortezomib On Human Multiple Myeloma Cell Lines Viability
标题:Translational Impact Of Novel Widely Pharmacological Characterized Mofezolac-Derived Cox-1 Inhibitors Combined With Bortezomib On Human Multiple Myeloma Cell Lines Viability
摘要:A Set Of Novel Diarylisoxazoles Has Been Projected Using Mofezolac (1) As A Lead Compound To Investigate Structure-Inhibitory Activity Relationships Of New Compounds And The Cyclooxygenases (Coxs) Catalytic Activity. Mofezolac Was Chosen Because Is The Most Potent And Selective Reversible Cox-1 Inhibitor [cox-1 Ic50 = 0.0079 Mu M And Cox-2 Ic50 > 50 Mu M,With A Selectivity Index (Si) In Favor Of Cox-1 Higher Than 6300]. Seventeen New Compounds Were Synthesized In Fair To Good Yields And Evaluated For Their Coxs Inhibitory Activity And Selectivity. Sls Ranged Between 1 And Higher Than 11903,4-Bis(4-Methoxyphenyl)-5-Vinylisoxazole (22) Has The Highest Si With Cox-1 Ic50 = 0.042 Mu M And Cox-2 Ic50 > 50 Mu M. 1 And 22 Were Superior To Aspirin In Inhibiting Platelet Aggregation (Ic50 = 0.45,0.63 And 1.11 Mu M,Respectively) In Human Platelet Rich Plasma (Hprp) Assay. They Did Not Induce Blood Coagulation And Hemolysis,And Are Neither Genotoxic Nor Mutagen. 1 And 22 Slightly Increase Bortezomib Cytotoxic Effect On Multiple Myeloma (Mm) Cell Lines (Nci-H929 And Rpmi-8226) And Affects Mm Cell Cycle And Apoptosis When Co-Administered With The Proteasome Inhibitor Bortezomib,A Drug Clinically Used To Treat Plasma Cell Neoplasms Including Mm. In Addition,Structure-Based Binding Mode Of 1 And 22,Through Fingerprints For Ligands And Proteins (Flag) Calculation,Allowed To Explain The One Order Of Magnitude Difference Between Cox-1 Ic50 Values Of The Two Compounds. Specifically,The Higher Inhibitory Potency Seems Due To The Formation Of A H-Bond Between Cox-1 S530 And The Carboxyl,Present In 1 And Absent In 22. (C) 2018 Elsevier Masson Sas. All Rights Reserved.
DOI:10.1016/j.Ejmech.2018.12.029

专利信息

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-9051302-B2
优先权日:2008-01-15
标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents
发明人：WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN
权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG
摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

专利号:US-2024287041-A1
优先权日:2021-05-20
标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
发明人：BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.

专利号:US-6593347-B2
优先权日:1998-10-30
标题 :Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use
发明人：BANDARAGE UPUL K; DONG QING; FANG XINQIN; GARVEY DAVID S; MERCER GREGORY J; RICHARDSON STEWART K; SCHROEDER JOSEPH D; WANG TIANSHENG
权利人:NITROMED INC
摘要:The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, 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. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.

专利号:AU-2022276509-A1
优先权日:2021-05-20
标题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms