专利号:US-2006069260-A1 优先权日:2004-09-28 标 题:Preparation of N-aryl pyridones 发明人:ZHANG HUIPING; CHEN BANG-CHI; ZHAO RULIN 权利人:ZHANG HUIPING; CHEN BANG-CHI; ZHAO RULIN 摘要:A novel process and intermediates thereof for making N-aryl pyridones of the type shown below from appropriate pyridinolates is described. n nThese compounds are useful as intermediates for the synthesis of clinical candidates.
专利号:US-2008025986-A1 优先权日:2003-06-06 标 题 :Methods of Treating Tnf-Mediated Disorders 发明人:OZES OSMAN N; BLATT LAWRENCE M 权利人:OZES OSMAN N; BLATT LAWRENCE M 摘要:The present invention provides methods of treating TNF-α-mediated disorders, the methods generally involving administering to an individual in need thereof effective amounts of pirfenidone or a pirfenidone analog and a second therapeutic agent that reduces TNF-α synthesis or that reduces TNF-α binding to a TNF receptor. The present invention further provides methods for treating non-alcoholic steatohepatitis, the method generally involving administering to an individual in need thereof an effective amount of pirfenidone. The present invention further provides methods of treating end-stage or advanced Type II diabetes, the methods generally involving administering to an individual in need thereof effective amounts of pirfenidone and insulin.
专利号:US-3839346-A 优先权日:1972-12-18 标 题:N-substituted pyridone and general method for preparing pyridones 发明人:GADEKAR S 权利人:AFFILIATED MED RES 摘要:1. A PROCESS FOR THE SYNTHESIS OF PYRIDONES OF THE FORMULA 1-A,2-(O=),3-R3,4-R4,5-R5,6-R6-1,2-DIHYDROPYRIDINE WHEREIN A IS AN AROMATIC RADICAL SELECTED FROM THE GROUP CONSISTING OF PHENYL, TOLYL, CHLOROPHENYL, TRIFLUOROMETHYLPHENYL, NAPHTHYL, PYRIDYL, FURYL, THIENYL, THIAZOLYL, PYRIMIDYL, QUINOLYL, IMIDAZOLYL; UP TO TWO OF THE TERMS R3, R4, R5 AND R6 ARE INDIVIDUALLY EACH HYDROGEN OR ALKYL UP TO 6 CARBON ATOMS, ARYL OR SUBSTITUTED ARYL RADICALS WHICH CONSISTS ESSENTIALLY OF THE STEPS OF REACTING A PYRIDONE OF THE FORMULA 2-(O=),3-R3,4-R4,5-R5,6-R6-1,2-DIHYDROPYRIDINE, OR ITS TAUTOMER, 2-(HO-),3-R3,4-R4,5-R5,6-R6-PYRIDINE IN WHICH R3, R4, R5 AND R6 ARE SET FORTH ABOVE, WITH A HALOGENATED COMPOUND OF THE FORMULA AX, WHEREIN X IS EITHER CHLORINE, BROMINE OR IODINE, AT TEMPERATURES RANGING BETWEEN THE MELTING POINT AND BOILING POINT OF SAID HALOGENATED COMPOUND, IN THE PRESENCE OF AN ALKALI METAL CARBONATE AND FINELY DIVIDED METALLIC COPPER.
专利号:US-6300349-B1 优先权日:1995-09-19 标题:Inhibition of tumor necrosis factor alpha 发明人:MARGOLIN SOLOMON B 摘要:In a preferred embodiment, a method for the inhibition of the synthesis and release of tumor necrosis factor from various cells, comprising: administering to a human or other mammal an effective dose of one or more pharmaceutical substances selected from the group consisting of N-substituted 2(1H) pyridones, N-substituted 3(1H) pyridones, and pharmaceutically acceptable salts thereof.
专利号:EP-0866656-B1 优先权日:1995-09-19 标题:Use of n-substituted pyridones as tumor necrosis factor alpha inhibitors 发明人:MARGOLIN SOLOMON B 权利人:MARGOLIN SOLOMON B 摘要:In a preferred embodiment, a method for the inhibition of the synthesis and release of tumor necrosis factor from various cells, comprising: administering to a human or other mammal an effective dose of one or more pharmaceutical substances selected from the group consisting of N-substituted 2(1H) pyridones, N-substituted 3(1H) pyridones, and pharmaceutically acceptable salts thereof.
参考文献:10.1055/s-2008-1072569 摘要:Zhang H, Chen B, Wang B, Chao S, Zhao R, Lim N, Balasubramanian B. Tetrabutylammonium Pyridin-2-olate: A New Reagent for the Efficient Synthesis of N-Aryl Pyridin-2-ones. Synthesis. 2008 May;2008(10):1523–6. doi: 10.1055/s-2008-1072569.