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(4-amino-2-(methylthio)pyrimidin-5-yl)methanol acetic acid 4-chloro-2-methanesulfanylpyrimidine-5-carboxylic acid ethyl ester ethyl 4-amino-2-methylmercaptopyrimidine-5-carboxylate 6-(3,5-dimethoxyphenyl)-2-(methylsulfanyl)pyrido[2,3-d]pyrimidin-7-amine 6-(2-bromo-phenyl)-2-methylsulfanyl-pyrido[2,3-d]pyrimidine-7-carboxylic acid 6-(2,6-dichlorophenyl)-2-methylsulfanyl-8H-pyrido[2,3-d]pyrimidin-7-one 4-氨基-2-(甲基硫代)嘧啶-5-腈置于二异丁基氢化铝,盐酸体系中,用 四氢呋喃,二氯甲烷,水 作为反应溶剂,化学反应 2.5H,以53.1%的收率获得产物4-氨基-2-甲巯基嘧啶-5-甲醛
参考文献: Compounds And Compositions As Protein Kinase Inhibitors[fr] Composes Et Compositions Convenant Comme Inhibiteurs De Proteine-Kinases
标题: Compounds And Compositions As Protein Kinase Inhibitors[fr] Composes Et Compositions Convenant Comme Inhibiteurs De Proteine-Kinases
专利信息
专利号:US-8188113-B2
优先权日:2006-09-14
标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C
权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC
摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
专利号:US-7196090-B2
优先权日:2002-07-25
标题 :Kinase inhibitors
发明人:CONNOLLY CLEO J CHIVIKAS; DEUR CHRISTOPHER JAMES; HAMBY JAMES MARINO; HOYER DENTON WADE; LIMBERAKIS CHRIS; REED JESSICA ELIZABETH; SCHROEDER MEL CONRAD; TAYLOR CLARKE
权利人:WARNER LAMBERT CO
摘要:This invention provides phenyl-substituted pyrimidopyrimidines, dihydropyrimido-pyrimidines, pyridopyrimidines, naphthyridines, and pyridopyrazines of the general formula: n nthat inhibit cyclin-dependent kinase and tyrosine kinase enzymes, methods and intermediate compounds for their synthesis, as well as pharmaceutical compositions and methods for their use in treating, inhibiting or preventing maladies associated with cell proliferative disorders, including angiogenesis, atherosclerosis, restenosis, and cancer.
专利号:IL-180256-A
优先权日:2004-07-15
标题 :Pyrido [d – 2,3] pyrimidinyl-amine history, intermediates for synthesis, process for preparation of compounds, drug, pharmaceutical preparation, and use of history for drug preparation