2-氯-4-[3-碘-1-(异丙基)-1H-吡唑-4-基]嘧啶置于四(三苯基膦)钯 吡啶,Sodium Carbonate,三乙胺体系中,用 1,4-二氧六环,乙醇,二氯甲烷,水,异丙醇,甲苯 用作溶剂,化学反应 80.0H,反应生成康奈非尼 参考文献: Compounds And Compositions As Protein Kinase Inhibitors[fr] Composés Et Compositions En Tant Qu'Inhibiteurs De Protéine Kinase 标题: Compounds And Compositions As Protein Kinase Inhibitors[fr] Composés Et Compositions En Tant Qu'Inhibiteurs De Protéine Kinase 摘要:这项发明提供了一类新型的化合物,其化学式为1,包括这些化合物的药物组合物以及使用这些化合物来治疗或预防与异常或失调的激酶活性相关的疾病或障碍的方法,特别是涉及b-Raf异常激活的疾病或障碍.
专利号:US-11612610-B2 优先权日:2018-12-14 标题:Mito-magnolol compounds and methods of synthesis and use thereof 发明人:KALYANARAMAN BALARAMAN; ZIELONKA JACEK MICHAL; CHENG GANG; HARDY MICAEL JOËL; OUARI OLIVIER 权利人:MEDICAL COLLEGE WISCONSIN INC; AIX MARSEILLE UNIV; MEDICAL COLLEGE OF WISCONSIN INC 摘要:The present invention provides mito-magnolol compounds, pharmaceutical compositions thereof, and methods of using the mito-magnolol compounds in the treatment of cancer, especially anti-cancer therapy or kinase resistant cancers.
专利号:US-2025289827-A1 优先权日:2022-12-02 标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof 发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN 权利人:C4 THERAPEUTICS INC 摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.
专利号:US-2025313551-A1 优先权日:2022-12-15 标题 :Process for the preparation of a quinazolinone derivative 发明人:DOTT PASCAL JEAN CLAUDE; FANTASIA SERENA MARIA; GUILLEMOT-PLASS MAUD; KALDRE DAINIS; LARI GIACOMO MARCO; MODOLO-CHELLAT ISABELLE GEORGETTE HUGUETTE; SEDELMEIER JOERG MATHIAS; TROKOWSKI SEBASTIAN 权利人:HOFFMANN LA ROCHE 摘要:The present invention relates to a new process for the preparation of (3R)—N-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide, as well as to a novel intermediate useful for the synthesis of said compound at large scale.
专利号:US-2018371021-A1 优先权日:2017-05-11 标 题 :Peptidomimetic macrocycles and uses thereof 发明人:AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN 权利人:AILERON THERAPEUTICS INC 摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.
专利号:US-2022259212-A1 优先权日:2019-07-11 标题:Inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan 2,3-dioxygenase 发明人:BOSS CHRISTOPH; CREN SYLVAINE; KIMMERLIN THIERRY; LOTZ-JENNE CARINA; POTHIER JULIEN; TIDTEN-LUKSCH NAOMI 权利人:IDORSIA PHARMACEUTICALS LTD 摘要:The present invention relates to compounds of Formula (I) inhibiting indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) enzymes. Further, their synthesis and their use as medicaments in the treatment of inter alia cancer is disclosed.
专利号:US-12390420-B1 优先权日:2024-10-22 标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof 发明人:EGUCHI MASAKATSU 权利人:BRYET US INC 摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.
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