CAS: 4394-00-7; 2-((3-(Trifluoromethyl)Phenyl)Amino)Nicotinic Acid

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CAS号2942-59-8 2-氯烟酸 | CAS号98-16-8 间三氟甲苯胺 | CAS号137488-50-7 1-(3'-trifluoro... | CAS号137488-49-4 1-(3'-trifluoro... | CAS号137488-48-3 1-(3'-trifluoro... | CAS号735318-84-0 2-(3-trifluorom... | CAS号66898-62-2 他尼氟酯 | CAS号70458-49-0 2-[3-(trifluoro...

1-(3'-Trifluoromethylphenyl)-4H-1,2-Dihydro-Pyrido-<2,3-D>-<1,3>-Oxazin-4-One置于水体系中,用 甲醇 作为反应溶剂,化学反应生成 氟尼酸
参考文献:1,2-Dihydro-3,1-Benzoxazin-4-One 和 4-H-1,2-Dihydro-Pyrido-[2,3-D]-[1,3]-Oxazin-4-One 衍生物有潜力前药:第二部分:水解
标题:1,2-Dihydro-3,1-Benzoxazin-4-One 和 4-H-1,2-Dihydro-Pyrido-[2,3-D]-[1,3]-Oxazin-4-One 衍生物有潜力前药:第二部分:水解
摘要:研究了潜在前药 1A-1F,2A-2G 和 3A-3E 在不同 Ph 值的甲醇-缓冲混合物 (3:7) 中自发水解的动力学,并开发了一种简单的分析紫外光谱方法.结果表明,在这些条件下,大多数新的潜在前药非常迅速地重新转化为其母体药物.所有潜在的前药在 Ph 4.0 和 8.0 之间都非常敏感,在 20oc 下的半衰期 < 50 分钟,除了化合物 1F,2F 和 3D.化合物 1B 和 1C 非常敏感,以至于在混合储备溶液和缓冲液-甲醇-混合物的过程中,它们会重新转化为其母体药物.
DOI:10.1002/ardp.2503241112

专利信息

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-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-4782173-A
优先权日:1983-08-03
标题 :Synthesis of methionine hydroxy analog or derivative, and esters thereof; synthesis of 1-acyloxy-4-hydrocarbylthiopropene, and products
发明人：BURRINGTON JAMES D; CESA MARK C
权利人:STANDARD OIL CO OHIO
摘要:Discloses (1) reacting a 3-(hydrocarbylthio) propionaldehyde with a compound (2) reacting latter compound with CO and R''YH where y is O or S to make (3) hydrolyzing this compound; (4) certain new 1-acyloxy-3-methylthiopropenes and (5) the methyl ester of 2-acetoxy-4-(methylthio)thiobutanoic acid.

专利号:US-6362009-B1
优先权日:1997-11-21
标 题 :Solid phase synthesis of heterocycles
发明人：MUNOZ BENITO; CHEN CHIXU
权利人:MERCK & CO INC
摘要:Methods for solid phase and combinatorial synthesis using a resin activation/capture approach are provided. In particular, methods for the production of dihydropyridones, N-acyidihydropyridones, tetrahydropyridones, pyridines, aminopyridines, N-acyltetrahydropyridines and tetrahydropyridines compounds and libraries containing such compounds are provided. Methods for screening the libraries and compounds and pharmaceutical compositions containing compounds prepared by the methods are provided.

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-8017776-B2
优先权日:2003-07-15
标题 :Methods for synthesis of acyloxyalkyl compounds
发明人：BHAT LAXMINARAYAN; GALLOP MARK A
权利人:XENOPORT INC
摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.