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-7034154-B2 优先权日:1999-08-10 标 题:Synthesis of substituted pyrazolopyrimidines 发明人:GROSS RAYMOND S; WILCOXEN KEITH M; OGLESBY RICHARD CHRISTOPHER 权利人:NEUROCRINE BIOSCIENCES INC 摘要:Methods of making substituted pyrazolopyrimidines generally and, more particularly, N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide. Such compounds have utility over a wide range of indications, including treatment of insomnia. In the practice of the present invention, improved techniques which do not require use and/or isolation of the pyrazole intermediate are disclosed, as well as improved techniques for making the reaction intermediates themselves. Such techniques offer significant advantages, including enhanced efficiency, particularly in the context of large scale manufacture.
专利号:US-6472528-B1 优先权日:1999-08-10 标题 :Synthesis of substituted pyrazolopyrimidines
专利号:US-2003004346-A1 优先权日:1999-08-10 标题:Synthesis of substituted pyrazolopyrimidines
参考标题:Efficient Approach To Amide Bond Formation With Nitriles And Peroxides: One-Pot Access To Boronated β-Ketoamides 作者:Babasaheb Sopan Gore,Gopal Chandru Senadi,Amol Milind Garkhedkar,Jeh-Jeng Wang |发布日期:2017.9.4 摘要:An Efficient, Mild And Practical Approach For The Synthesis Of Amides From Nitriles And Peroxides Is Reported In The Presence Of Boron Trifluoride Ethereate. In This Protocol, We Utilized Peroxides As C1 Synthons For The Amidation Reaction. Also, We Successfully Prepared Boron‐containing β‐ketoamides In A One‐pot Assembly From β‐ketonitriles. A Variety Of Functional Groups Were Tolerated In Moderate
合成参考文献
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