氟尼辛杂质d(Ep)置于氢氧化钾体系中,用 甲醇 用作溶剂,化学反应 3.0H,以90%的收率获得氟尼克辛 参考文献:Improved Process For The Preparation Of 2-Methyl-3-Trifluoromethylaniline: A Versatile Intermediate For Flunixin Synthesis 标题:Improved Process For The Preparation Of 2-Methyl-3-Trifluoromethylaniline: A Versatile Intermediate For Flunixin Synthesis 摘要:A Detailed New Experimental Investigation Into The Synthesis Of Flunixin Via 2-Methyl-3-Trifluoromethylaniline Is Described. The Coupling Process Between 2-Methyl-3-Trifluoromethylaniline And 2-Chloronicotinate Was Achieved Stoichiometrically And In High Yield,When Ethylene Glycol Was Used As Reaction Solvent At 160-Degrees-C. Doi:10.3987/com-94-6822
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-2013035307-A1 优先权日:2010-01-26 标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers 发明人:PRESTWICH GLENN D; KENNEDY THOMAS P 权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P 摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.
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-5914322-A 优先权日:1992-02-20 标 题:Treatment of disease and conditions 发明人:FALK RUDOLF EDGAR; ASCULAI SAMUEL SIMON 权利人:HYAL PHARMA CORP 摘要:A topically applied transdermally penetrating systemic independent acting pharmaceutical combination and formulation for the treatment of a disease or condition of the skin and exposed tissue for example, basal cell carcinoma, the precancerous, often recurrent, actinic keratoses lesions, fungal lesions, 'liver' spots and like lesions (found for the most part in the epidermis), squamous cell tumours, metastatic cancer of the breast to the skin, primary and metastatic melanoma in the skin, genital warts (condyloma acuminata) cervical cancer, and HPV (Human Papilloma Virus) including HPV of the cervix, psoriasis (both plaque-type psoriasis and nail bed psoriasis), corns on the feet and hair loss on the head of pregnant women, comprising, together with pharmaceutical excipients suitable for topical application, a therapeutically effective non-toxic amount of a drug which inhibits prostaglandin synthesis administered with, or carried in, an amount of hyaluronic acid and/or salts thereof and/or homologues, analogues, derivatives, complexes, esters, fragments, and/or sub-units of hyaluronic acid (preferably hyaluronic acid and salts thereof) sufficient to facilitate the drug's penetration through the skin and tissue (including any scar tissue) at the site requiring treatment, to block prostaglandin synthesis.
专利号:US-5792753-A 优先权日:1991-07-03 标 题:Compositions comprising hyaluronic acid and prostaglandin-synthesis-inhibiting drugs 发明人:FALK RUDOLF EDGAR; ASCULAI SAMUEL SIMON 权利人:HYAL PHARMA CORP 摘要:A topically administrable pharmaceutical composition is disclosed which comprises a therapeutically effective amount of a drug which inhibits prostaglandin synthesis, and an amount of a form of hyaluronic acid sufficient to transport the composition through the skin into the epidermis or dermis where the composition remains until discharged via the lymphatic system, wherein n (a) the drug is 1-5% by weight of the composition, and n (b) the form of hyaluronic acid is 1-3% by weight of the composition, has a molecular weight greater than about 150,000 daltons and less than 750,000 daltons, and is selected from the group consisting of hyaluronic acid and salts thereof.
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合成参考文献
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