3-硝基苯硼酸置于barium Dihydroxide,Iron Hydroxide,水体系中,化学反应生成 3-乙酰胺基苯硼酸 参考文献:Seaman; Johnson,Journal Of The American Chemical Society,1931,Vol. 53,P. 713 标题:Seaman; Johnson,Journal Of The American Chemical Society,1931,Vol. 53,P. 713
专利号:US-2009196912-A1 优先权日:2004-07-30 标 题:Pyridinylamines 发明人:EICKHOFF JAN ELKE; HAFENBRADL DORIS; SCHWAB WILFRIED; COTTON MATTHEW; KIEBL BERT MATTHIAS; ZECH BIRGIT; MULLER STEFAN; HARRIS JOHN; SAVIC VLADIMIR; MACRITCHIE JACKIE 权利人:GPC BOTECH AG 摘要:Described are pyridinylamines and pharmaceutically acceptable salts thereof, the use of these pyridinylamines for the prophylaxis and/or treatment of various diseases such as infectious diseases, including opportunistic infections, prion diseases immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as pharmaceutical compositions containing at least one pyridinylamine and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the pyridinylamines are disclosed.
专利号:US-6531477-B1 优先权日:1998-10-13 标 题:6-substituted pyrazolo [3,4-d] pyrimidin-4-ones useful as cyclin dependent kinase inhibitors 发明人:MARKWALDER JAY A; SEITZ STEVEN P; SHERK SUSAN R 权利人:DU PONT PHARM CO 摘要:The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II):that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T.This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:US-6559152-B2 优先权日:1998-10-13 标 题 :6-substituted pyrazolo[3,4-d]pyrimidin-4-ones useful as cyclin dependent kinase inhibitors 发明人:MARKWALDER JAY A; SEITZ STEVEN P; SHERK SUSAN R 权利人:DU PONT PHARM CO 摘要:The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II):that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T.This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:US-7781470-B2 优先权日:1999-09-13 标题:Aminodicarboxylic acid derivatives having pharmaceutical properties 发明人:ALONSO-ALIJA CRISTINA; HEIL MARKUS; FLUBACHER DIETMAR; NAAB PAUL; PERNERSTORFER JOSEF; STASCH JOHANNES-PETER; WUNDER FRANK; DEMBOWSKY KLAUS; PERZBORN ELIZABETH; STAHL ELKE 权利人:BAYER SCHERING PHARMA AG 摘要:The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, n nwherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.
专利号:US-8178559-B2 优先权日:2004-12-30 标 题:Organic compounds 发明人:BREITENSTEIN WERNER; EHARA TAKERU; EHRHARDT CLAUS; GROSCHE PHILIPP; HITOMI YUKO; IWAKI YUKI; KANAZAWA TAKANORI; KONISHI KAZUHIDE; MAIBAUM JUERGEN KLAUS; MASUYA KEIICHI; IWASAKI ATSUKO; OSTERMANN NILS; SUZUKI MASAKI; TOYAO ATSUSHI; YOKOKAWA FUMIAKI 权利人:BREITENSTEIN WERNER; EHARA TAKERU; EHRHARDT CLAUS; GROSCHE PHILIPP; HITOMI YUKO; IWAKI YUKI; KANAZAWA TAKANORI; KONISHI KAZUHIDE; MAIBAUM JUERGEN KLAUS; MASUYA KEIICHI; IWASAKI ATSUKO; OSTERMANN NILS; SUZUKI MASAKI; TOYAO ATSUSHI; YOKOKAWA FUMIAKI; NOVARTIS AG 摘要:3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.
专利号:US-10202374-B2 优先权日:2014-02-27 标题 :6-aryl-4-phenylamino-quinazoline analogs as phosphoinositide-3-kinase inhibitors 发明人:VISHWAKARMA RAM ASREY; BHARATE SANDIP BIBISHAN; BHUSHAN SHASHI; YADAV RAMMOHAN RAO; GURU SANTOSH KUMAR; JOSHI PRASHANT 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to 6-aryl-4-phenylamino quinazolines of formula I wherein, R and R′ are as herein described. The present invention particularly relates to synthesis and anticancer and phoshpoinositide-3-kinase-α (PI3K-α) inhibitory activity. In addition, the invention relates to methods of using compounds for treating or preventing various cancers such as pancreatic, prostate, breast and melanoma.